1. A method of pacing a vehicle in an amusement park ride, comprising:
at a first location in the ride, releasing or launching the vehicle with energy to travel an entire length of a section of the ride;
providing a controller with memory storing speed settings for the vehicle in a portion of the ride;
positioning a plurality of magnetic thrusters proximate to the portion of the ride at a second location spaced apart from the first location within the section of the ride, the magnetic thrusters including at least one position sensor communicatively linked to the controller;
in response to a signal from the at least one position sensor after the releasing or launching, operating the controller to determine a velocity of the vehicle in the portion of the ride at more than one location along the portion of the ride;
with the controller, comparing the determined velocity with the stored speed settings;
determining a magnetic force to apply to the vehicle based on the comparing; and
operating the magnetic thrusters to generate the magnetic force that acts upon the vehicle to pace the vehicle by selectively operating individual ones of the plurality of magnetic thrusters over the portion of the ride,
wherein after operating the magnetic thruster to generate the magnetic force the vehicle continues to coast in a direction of travel at a velocity greater than zero and within a velocity range defined by the stored speed settings,
wherein the vehicle is coasting at an initial velocity upon entering the portion of the track in the direction of travel that is within the velocity range, and
wherein the magnetic force is selected in the determining to retain the vehicle at a velocity within the velocity range along the portion of the ride.
2. The method of claim 1, wherein the determining of the magnetic force comprises determining a direction of the magnetic force relative to a direction of travel of the vehicle, whereby the magnetic force is selected to be a decelerating force or an accelerating force.
3. The method of claim 2, wherein speed settings comprise an upper speed trigger and a lower speed trigger and wherein the determining of the magnetic force comprises applying the magnetic force as a decelerating force when the determined velocity is greater than about the upper speed trigger and as an accelerating force when the determined velocity is less than about the lower speed trigger.
4. The method of claim 1, wherein the vehicle comprises a magnetic array and wherein the magnetic thruster comprises at least one linear synchronous motor (LSM) and the operating comprises powering and controlling the at least one LSM to apply the magnetic force to the magnetic array to accelerate or to decelerate the vehicle along a present direction of travel for the vehicle in the portion of the ride.
5. The method of claim 1, further comprising in response to a second signal from the at least one position sensor, operating of the controller to determine a second velocity of the vehicle in the portion of the ride, comparing the second determined velocity with the stored speed settings, determining a second magnetic force to apply to the vehicle based on the comparing of the second determined velocity, and operating of the magnetic thruster to generate a second magnetic force to act on the magnet array of the vehicle, wherein the second magnetic force differs in at least direction from the magnetic force.
6. The method of claim 1, wherein the amusement park ride comprises a track upon which the vehicle travels and wherein the controlled portion of the ride comprises a curved or inclined section of the track.
7. A magnetic pacer assembly for pacing a vehicle that has an affixed magnet array and is traveling along a track or guideway, comprising:
a magnetic propulsion device positioned proximate to the track selectively operable to generate a magnetic field that applies a decelerating force upon the magnet array of the vehicle and to generate a magnetic field that applies an accelerating force upon the magnet array of the vehicle; wherein the magnetic propulsion device is provided at a first location in the track for applying a launching force with energy to travel an entire length of a section of the track, and further includes a plurality of magnetic thrusters proximate to the track at a second location spaced apart from the first location within the section of the track; and wherein individual ones of the plurality of magnetic thrusters are operated over the portion of the track;
a position sensor assembly; and
a controller receiving position signals for the vehicle from the position sensor assembly, determining a velocity of the vehicle based on the position signals, and based on the determined velocity operating the magnetic propulsion device to generate the magnetic field corresponding to the decelerating force or to the accelerating force,
wherein the position sensor assembly comprises a plurality of sensors positioned in a spaced apart manner along the length of the magnetic propulsion device and wherein the controller operates to receive the position signals as the vehicle travels along the length, to determine a velocity at more than one point along the length, and to operate the magnetic propulsion device more than once as the vehicle travels on the track proximate to the magnetic propulsion device to retain the vehicle at a velocity within the velocity range defined by the speed setting stored in a memory in the controller.
8. The assembly of claim 7, further comprising memory accessible by the controller that stores first and second velocity bounds defining a velocity range, wherein the controller operates the magnetic propulsion device to generate the magnetic field corresponding to the decelerating force when the determined velocity exceeds about the first velocity bound and operates the magnetic propulsion device to generate the magnetic field corresponding to the accelerating force when the determined velocity is less than about the second velocity bound.
9. The assembly of claim 7, wherein the operating of the magnetic propulsion device more than once comprises alternatively generating the magnetic fields associated with the decelerating and accelerating forces.
10. The assembly of claim 9, wherein the magnetic propulsion device comprises a plurality of linear synchronous motors (LSMs) arranged end-to-end along the track and wherein each of the LSMs is independently and concurrently operable to generate one of the magnetic fields.
11. The assembly of claim 7, wherein the controller selects magnitudes for the magnetic fields and the operating of the magnetic propulsion device comprises generating the magnetic fields with the selected magnitudes.
12. The assembly of claim 7, wherein the controller selects durations for the magnetic fields and the operating of the magnetic propulsion device comprises generating the magnetic fields with the selected durations.
13. An amusement park ride with enhanced pacing, comprising:
a plurality of vehicles for carrying passengers;
a track defining a path for the ride and supporting the vehicles, wherein the track includes a show portion;
a show system generating a show display when the vehicles are positioned in the show portion of the track, wherein the show display is adapted for the vehicles to travel through the show portion within a velocity range; and
a magnetic pacer assembly comprising a magnetic thruster positioned adjacent the show portion of the track and a controller operating to determine a velocity of at least one of the vehicles in the show portion of the track and, based on the determined velocity, to operate the magnetic thruster to generate a magnetic field that applies a force upon at least one of the vehicles,
wherein the force is a decelerating force when the determined velocity is greater than an upper limit of the velocity range and is an accelerating force when the determined velocity is less than a lower limit of the velocity range and
wherein the controller operates a least a second time to determine a second velocity of at least one of the vehicles and, based on the determined second velocity, to second operate the magnetic thruster to generate a magnetic field that applies a second force upon the at least one of the vehicles that differs from the first applied force in at least one of direction and magnitude and p1 wherein the magnetic pacer assembly is provided at a first location in the track for applying a lunching force with energy to travel an entire length of a section of the track, and further includes a plurality of magnetic thrusters proximate to the track at a second location spaced apart from the first location within the section of the track; and wherein individual ones of the plurality of magnetic thrusters are operated over the portion of the track.
14. The amusement park ride of claim 13, wherein the magnetic thruster comprises a plurality of linear synchronous motors (LSMs) arranged in series along the track and wherein each of the LSMs are independently operable to generate a magnetic field that accelerates or decelerates the vehicles by applying the magnetic field to a magnetic array provided on the vehicles.
15. The amusement park ride of claim 13, wherein the show portion of the track comprises at least one curved or inclined portion.
16. The amusement park ride of claim 13, wherein the magnetic pacer assembly further comprises a plurality of position sensors positioned along the magnetic thruster and wherein the controller determines two or more velocities for at least one of the vehicles along the magnetic thruster and operates the magnetic thruster to generate magnetic fields based on the two or more velocities.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
1. A compound of the formula:
or a pharmaceutically acceptable salt thereof,
where R, is:
(I) C1-C6 alkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, C1-C7 alkyl (optionally substituted with C1-C3 alkyl and C1-C3 alkoxy), \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl, \u2014OC\u2550O NR1-aR1-b where R1-a and R1-b are as defined above,
(II) \u2014CH2\u2014S(O)0-2\u2014(C1-C6 alkyl),
(III) \u2014CH2\u2014CH2\u2014S(O)0-2\u2014(C1-C6 alkyl),
(IV) C2-C6 alkenyl with one or two double bonds, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(V) C2-C6 alkynyl with one or two triple bonds, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(VI) \u2014(CH2)n1\u2014(R1-aryl) where n1 is zero or one and where R1-aryl is phenyl, 1-naphthyl, 2-naphthyl and indanyl, indenyl, dihydronaphthayl, tetralinyl optionally substituted with one, two, three or four of the following substituents on the aryl ring:
(A) C1-C6 alkyl optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014NR1-aR1-b where R1-a and R1-b are as defined above, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy,
(B) C2-C6 alkenyl with one or two double bonds, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(C) C2-C6 alkynyl with one or two triple bonds, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(D) \u2014F, Cl, \u2014Br and \u2014I,
(F) \u2014C1-C6 alkoxy optionally substituted with one, two or three \u2014F,
(G) \u2014NRN-2RN-3 where RN-2 and RN-3 are as defined below,
(H) \u2014OH,
(I) \u2014C\u2261N,
(J) C3-C7 cycloalkyl, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(K) \u2014CO\u2014(C1-C4 alkyl),
(L) \u2014SO2\u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(M) \u2014CO\u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(N) \u2014SO2\u2014(C1-C4 alkyl),
(VII) \u2014(CH2)n1\u2014(R1-heteroaryl) where n1 is as defined above and where R1-heteroaryl is selected from the group consisting of pyridinyl, pyrimidinyl, quinolinyl, benzothienyl, indolyl, indolinyl, pryidazinyl, pyrazinyl, isoindolyl, isoquinolyl, quinazolinyl, quinoxalinyl, phthalazinyl, imidazolyl, isoxazolyl, pyrazolyl, oxazolyl, thiazolyl, indolizinyl, indazolyl, benzothiazolyl, benzimidazolyl, benzofuranyl, furanyl, thienyl, pyrrolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, oxazolopyridinyl, imidazopyridinyl, isothiazolyl, naphthyridinyl, cinnolinyl, carbazolyl, beta-carbolinyl, isochromanyl, chromanyl, tetrahydroisoquinolinyl, isoindolinyl, isobenzotetrahydrofuranyl, isobenzotetrahydrothienyl, isobenzothienyl, benzoxazolyl, pyridopyridinyl, benzotetrahydrofuranyl, benzotetrahydrothienyl, purinyl, benzodioxolyl, triazinyl, phenoxazinyl, phenothiazinyl, pteridinyl, benzothiazolyl, imidazopyridinyl, imidazothiazolyl, dihydrobenzisoxazinyl, benzisoxazinyl, benzoxazinyl, dihydrobenzisothiazinyl, benzopyranyl, benzothiopyranyl, coumarinyl, isocoumarinyl, chromonyl, chromanonyl, pyridinyl-N-oxide tetrahydroquinolinyl dihydroquinolinyl dihydroquinolinonyl dihydroisoquinolinonyl dihydrocoumarinyl dihydroisocoumarinyl isoindolinonyl benzodioxanyl benzoxazolinonyl pyrrolyl N-oxide, pyrimidinyl N-oxide, pyridazinyl N-oxide, pyrazinyl N-oxide, quinolinyl N-oxide, indolyl N-oxide, indolinyl N-oxide, isoquinolyl N-oxide, quinazolinyl N-oxide, quinoxalinyl N-oxide, phthalazinyl N-oxide, imidazolyl N-oxide, isoxazolyl N-oxide, oxazolyl N-oxide, thiazolyl N-oxide, indolizinyl N-oxide, indazolyl N-oxide, benzothiazolyl N-oxide, benzimidazolyl N-oxide, pyrrolyl N-oxide, oxadiazolyl N-oxide, thiadiazolyl N-oxide, triazolyl N-oxide, tetrazolyl N-oxide, benzothiopyranyl S-oxide, and benzothiopyranyl S,S-dioxide, where the R1-heteroaryl group is bonded to \u2014(CH2)n1\u2014 by any ring atom of the parent RN-heteroaryl group substituted by hydrogen such that the new bond to the R1-heteroaryl group replaces the hydrogen atom and its bond, where heteroaryl is optionally substituted with one, two, three or four of:
(1) C1-C6 alkyl optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014NR1-aR1-b where R1-a and R1-b are as defined above, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy,
(2) C2-C6 alkenyl with one or two double bonds, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(3) C2-C6 alkynyl with one or two triple bonds, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(4) \u2014F, \u2014Cl, \u2014Br and \u2014I,
(6) -C1-C6 alkoxy optionally substituted with one, two, or three \u2014F,
(7) \u2014NRN-2RN-3 where RN-2 and RN-3 are as defined below,
(8) \u2014OH,
(9) \u2014C\u2261N,
(10) C3-C7 cycloalkyl, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(11) \u2014CO\u2014(C1-C4 alkyl),
(12) \u2014SO2\u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(13) \u2014CO\u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(14) \u2014SO2\u2014(C1-C4 alkyl), with the proviso that when n1 is zero R1-heteroaryl is not bonded to the carbon chain by nitrogen,
(VIII) \u2014(CH2)n1\u2014(R1-heterocycle) where n1 is as defined above and R1-heterocycle is selected from the group consisting of morpholinyl, thiomorpholinyl, thiomorpholinyl S-oxide, thiomorpholinyl S,S-dioxide, piperazinyl, homopiperazinyl, pyrrolidinyl, pyrrolinyl, tetrahydropyranyl, piperidinyl, tetrahydrofuranyl, tetrahydrothienyl, homopiperidinyl, homomorpholinyl, homothiomorpholinyl, homothiomorpholinyl S,S-dioxide, oxazolidinonyl, dihydropyrazolyl, dihydropyrrolyl dihydropyrazinyl, dihydropyridinyl, dihydropyrimidinyl, dihydrofuryl, dihydropyranyl, tetrahydrothienyl S-oxide, tetrahydrothienyl S,S-dioxide, and homothiomorpholinyl S-oxide where the R1-heterocycle group is bonded by any atom of the parent R1-heterocycle group substituted by hydrogen such that the new bond to the R1-heterocycle group replaces the hydrogen atom and its bond, where heterocycle is optionally substituted with one, two, three or four:
(1) C1-C6 alkyl optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014NR1-aR1-b where R1-a and R1-b are as defined above, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy,
(2) C2-C6 alkenyl with one or two double bonds, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(3) C2-C6 alkynyl with one or two triple bonds, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(4) \u2014F, \u2014Cl, \u2014Br and \u2014I,
(5) C1-C6 alkoxy,
(6) -C1-C6 alkoxy optionally substituted with one, two, or three \u2014F,
(7) \u2014NRN-2RN-3 where RN-2 and RN-3 are as defined below,
(8) \u2014OH,
(9) \u2014C\u2261N,
(10) C3-C7 cycloalkyl, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(11) \u2014CO\u2014(C1-C4 alkyl),
(12) \u2014SO2\u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(13) \u2014CO\u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(14) \u2014SO2\u2014(C1-C4 alkyl),
(15) \u2550O, with the proviso that when n1 is zero R1-heterocycle is not bonded to the carbon chain by nitrogen; where R2 is selected from the group consisting of:
(I) \u2014H,
(II) C1-C6 alkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(III) \u2014(CH2)0-4-R2-1 where R2-1 is R1-aryl or R1-heteroaryl where R1-aryl and R1-heteroaryl are as defined above;
(IV) C2-C6 alkenyl with one or two double bonds, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(V) C2-C6 alkynyl with one or two triple bonds, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(VI) \u2014(CH2)0-4\u2014C3-C7 cycloalkyl, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl, where R3 is selected from the group consisting of:
(I) \u2014H,
(II) C1-C6 alkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(III) \u2014(CH2)0-4\u2014R2-1 where R2-1 is R1-aryl or R1-heteroaryl where R1-aryl and R1-heteroaryl are as defined above;
(IV) C2-C6 alkenyl with one or two double bonds,
(V) C2-C6 alkynyl with one or two triple bonds,
(VI) \u2014(CH2)0-4\u2014C3-C7 cycloalkyl, optionally substituted with one, two or three substituents selected from the group consisting of \u2014F, \u2014Cl, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl, and where R2 and R3 are taken together with the carbon to which they are attached to form a carbocycle of three, four, five, six, and seven carbon atoms, optionally where one carbon atom is replaced by a heteroatom selected from the group consisting of \u2014O\u2014, \u2014S\u2014, \u2014SO2\u2014, \u2014NRN-2\u2014, where RN-2 is as defined below;
where RN is:
(I) RN-1\u2014XN\u2014 where XN is selected from the group consisting of:
(A) \u2014CO\u2014,
(B) \u2014SO2\u2014,
(C) \u2014(CR\u2032R\u2033)1-6 where R\u2032 and R\u2033 are the same or different and are \u2014H and C1-C4 alkyl,
(D) \u2014CO\u2014(CR\u2032R\u2033)1-6\u2014XN-1 where XN-1 is selected from the group consisting of \u2014O\u2014, \u2014S\u2014 and \u2014NR\u2032\u2014 and where R\u2032 and R\u2033 are as defined above,
(E) a single bond;
where RN-1 is selected from the group consisting of:
(A) RN-aryl where RN-aryl is phenyl, 1-naphthyl, 2-naphthyl, tetralinyl, indanyl, dihydronaphthyl or 6,7,8,9-tetrahydro-5H-benzoacycloheptenyl, optionally substituted with one, two or three of the following substituents which can be the same or different and are:
(1) C1-C6 alkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(2) \u2014OH,
(3) \u2014NO2,
(4) \u2014F, \u2014Cl, \u2014Br, \u2014I,
(5) \u2014CO\u2014OH,
(6) \u2014C\u2261N,
(7) \u2014(CH2)0-4\u2014CO\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are selected from the group consisting of:
(a) \u2014H,
(b) \u2014C1-C6 alkyl optionally substituted with one substitutent selected from the group consisting of:
\u2003(i) \u2014OH,
\u2003(ii) \u2014NH2,
(c) \u2014C1-C6 alkyl optionally substituted with one to three \u2014F, \u2014Cl, \u2014Br, \u2014I,
(d) \u2014C3-C7 cycloalkyl,
(e) \u2014(C1-C2 alkyl)-(C3-C7 cycloalkyl),
(f) \u2014(C1-C6 alkyl)-O\u2014(C1-C3 alkyl),
(g) \u2014C2-C6 alkenyl with one or two double bonds,
(h) \u2014C2-C6 alkynyl with one or two triple bonds,
(i) \u2014C1-C6 alkyl chain with one double bond and one triple bond,
(j) \u2014R1-aryl where R1-aryl is as defined above,
(k) \u2014R1-heteroaryl where R1-heteroaryl is as defined above,
(8) \u2014(CH2)0-4\u2014CO\u2014(C1-C12 alkyl),
(9) \u2014(CH2)0-4\u2014CO\u2014(C2-C12 alkenyl with one, two or three double bonds),
(10) \u2014(CH2)0-4\u2014CO\u2014(C2-C12 alkynyl with one, two or three triple bonds),
(11) \u2014(CH2)0-4\u2014CO\u2014(C3-C7 cycloalkyl),
(12) \u2014(CH2)0-4\u2014CO\u2014R1-aryl where R1-aryl is as defined above,
(13) \u2014(CH2)0-4\u2014CO\u2014R1-heteroaryl where R1-heteroaryl is as defined above,
(14) \u2014(CH2)0-4\u2014CO\u2014R1-heterocycle where R1-heterocycle is as defined above,
(15) \u2014(CH2)0-4\u2014CO\u2014RN-4 where RN-4 is selected from the group consisting of morpholinyl, thiomorpholinyl, piperazinyl, piperidinyl, homomorpholinyl, homothiomorpholinyl, homothiomorpholinyl S-oxide, homothiomorpholinyl S,S-dioxide, pyrrolinyl and pyrrolidinyl where each group is optionally substituted with one, two, three, or four of C1-C6 alkyl,
(16) \u2014(CH2)0-4\u2014CO\u2014O\u2014RN-5 where RN-5 is selected from the group consisting of:
(a) C1-C6 alkyl,
(b) \u2014(CH2)0-2\u2014(R1-aryl) where R1-aryl is as defined above,
(c) C2-C6 alkenyl containing one or two double bonds,
(d) C2-C6 alkynyl containing one or two triple bonds,
(e) C3-C7 cycloalkyl,
(f) \u2014(CH2)0-2\u2014(R1-heteroaryl) where R1-heteroaryl is as defined above,
(17) \u2014(CH2)0-4\u2014SO2\u2014NRN-2RN-3 where RN-2 and RN-3 are as defined above,
(18) \u2014(CH2)0-4\u2014SO\u2014(C1-C8 alkyl),
(19) \u2014(CH2)0-4\u2014SO2\u2014(C1-C12 alkyl),
(20) \u2014(CH2)0-4\u2014SO2\u2014(C3-C7 cycloalkyl),
(21) \u2014(CH2)0-4\u2014N(H or RN-5)\u2014CO\u2014O\u2014RN-5 where RN-5 can be the same or different and is as defined above,
(22) \u2014(CH2)0-4\u2014N(H or RN-5)\u2014CO\u2014N(RN-5)2, where RN-5 can be the same or different and is as defined above,
(23) \u2014(CH2)0-4\u2014N\u2014CS\u2014N (RN-5)2, where RN-5 can be the same or different and is as defined above,
(24) \u2014(CH2)0-4\u2014N(\u2014H or RN-5)\u2014CO\u2014RN-2 where RN-5 and RN-2 can be the same or different and are as defined above,
(25) \u2014(CH2)0-4\u2014NRN-2RN-3 where RN-2 and RN-3 can be the same or different and are as defined above,
(26) \u2014(CH2)0-4\u2014RN-4 where RN-4 is as defined above,
(27) \u2014(CH2)0-4\u2014O\u2014CO\u2014(C1-C6 alkyl),
(28) \u2014(CH2)0-4\u2014O\u2014P (O)\u2014(ORN-aryl-1)2 where RN-aryl-1 is \u2014H or C1-C4 alkyl,
(29) \u2014(CH2)0-4\u2014O\u2014CO\u2014N(RN-5)2 where RN-5 is as defined above,
(30) \u2014(CH2)0-4\u2014O\u2014CS\u2014N(RN-5)2 where RN-5 is as defined above,
(31) \u2014(CH2)0-4\u2014O\u2014(RN-5)2 where RN-5 is as defined above,
(32) \u2014(CH2)0-4\u2014O\u2014(RN-5)2\u2014COOH where RN-5 is as defined above,
(33) \u2014(CH2)0-4\u2014S\u2014( RN-5)2 where RN-5 is as defined above,
(34) \u2014(CH2)04\u2014O\u2014(C1-C6 alkyl optionally substituted with one, two, three, four, or five of \u2014F),
(35) C3-C7 cycloalkyl,
(36) C2-C6 alkenyl with one or two double bonds optionally substituted with C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(37) C2-C6 alkynyl with one or two triple bonds optionally substituted with C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(38) \u2014(CH2)0-4\u2014N(\u2014H or RN-5)\u2014SO\u2014RN-2 where RN-5 and RN-2 can be the same or different and are as described above,
(39) \u2014(CH2)0-4\u2014C3-C7 cycloalkyl,
(B) \u2014RN-heteroaryl where RN-heteroaryl is selected from the group consisting of pyridinyl, pyrimidinyl, quinolinyl, benzothienyl, indolyl, indolinyl, pryidazinyl, pyrazinyl, isoindolyl, isoquinolyl, quinazolinyl, quinoxalinyl, phthalazinyl, imidazolyl, isoxazolyl, pyrazolyl, oxazolyl, thiazolyl, indolizinyl, indazolyl, benzothiazolyl, benzimidazolyl, benzofuranyl, furanyl, thienyl, pyrrolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, oxazolopyridinyl, imidazopyridinyl, isothiazolyl, naphthyridinyl, cinnolinyl, carbazolyl, beta-carbolinyl, isochromanyl, chromanyl, tetrahydroisoquinolinyl, isoindolinyl, isobenzotetrahydrofuranyl, isobenzotetrahydrothienyl, isobenzothienyl, benzoxazolyl, pyridopyridinyl, benzotetrahydrofuranyl, benzotetrahydrothienyl, purinyl, benzodioxolyl, triazinyl, henoxazinyl, phenothiazinyl, pteridinyl, benzothiazolyl, imidazopyridinyl, imidazothiazolyl, dihydrobenzisoxazinyl, benzisoxazinyl, benzoxazinyl, dihydrobenzisothiazinyl, benzopyranyl, benzothiopyranyl, coumarinyl, isocoumarinyl, chromonyl, chromanonyl, pyridinyl-N-oxide, tetrahydroquinolinyl dihydroquinolinyl dihydroquinolinonyl dihydroisoquinolinonyl dihydrocoumarinyl dihydroisocoumarinyl isoindolinonyl benzodioxanyl benzoxazolinonyl pyrrolyl N-oxide, pyrimidinyl N-oxide, pyridazinyl N-oxide, pyrazinyl N-oxide, quinolinyl N-oxide, indolyl N-oxide, indolinyl N-oxide, isoquinolyl N-oxide, quinazolinyl N-oxide, quinoxalinyl N-oxide, phthalazinyl N-oxide, imidazolyl N-oxide, isoxazolyl N-oxide, oxazolyl N-oxide, thiazolyl N-oxide, indolizinyl N-oxide, indazolyl N-oxide, benzothiazolyl N-oxide, benzimidazolyl N-oxide, pyrrolyl N-oxide, oxadiazolyl N-oxide, thiadiazolyl N-oxide, triazolyl N-oxide, tetrazolyl N-oxide, benzothiopyranyl S-oxide, and benzothiopyranyl S,S-dioxide, where the RN-heteroaryl group is bonded by any atom of the parent RN-heteroaryl group substituted by hydrogen such that the new bond to the RN-heteroaryl group replaces the hydrogen atom and its bond, where heteroaryl is optionally substituted with one, two, three, or four of:
(1) C1-C6 alkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(2) \u2014OH,
(3) \u2014NO2,
(4) \u2014F, \u2014Cl, \u2014Br, \u2014I,
(5) \u2014CO\u2014OH,
(6) \u2014C\u2261N,
(7) \u2014(CH2)0-4\u2014CO\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are selected from the group consisting of:
(a) \u2014H,
(b) \u2014C1-C6 alkyl optionally substituted with one substitutent selected from the group consisting of:
\u2003(i) \u2014OH,
\u2003(ii) \u2014NH2,
(c) \u2014C1-C6 alkyl optionally substituted with one to three \u2014F, \u2014Cl, \u2014Br, \u2014I,
(d) \u2014C3-C7 cycloalkyl,
(e) \u2014(C1-C2 alkyl)-(C3-C7 cycloalkyl),
(f) \u2014(C1-C6 alkyl)-O\u2014(C1-C3 alkyl),
(g) \u2014C2-C6 alkenyl with one or two double bonds,
(h) \u2014C2-C6 alkynyl with one or two triple bonds,
(i) \u2014C1-C6 alkyl chain with one double bond and one triple bond,
(j) \u2014R1-aryl where R1-aryl is as defined above,
(k) -R1-heteroaryl where R1-heteroaryl is as defined above,
(8) \u2014(CH2)0-4\u2014CO\u2014(C1-C12 alkyl),
(9) \u2014(CH2)0-4\u2014CO\u2014(C2-C12 alkenyl with one, two or three double bonds),
(10) \u2014(CH2)0-4\u2014CO\u2014(C2-C12 alkynyl with one, two or three triple bonds),
(11) \u2014(CH2)0-4\u2014CO\u2014(C3-C7 cycloalkyl),
(12) \u2014(CH2)0-4\u2014CO\u2014R1-aryl where R1-aryl is as defined above,
(13) \u2014(CH2)0-4\u2014CO\u2014R1-heteroaryl where R1-heteroaryl is as defined above,
(14) \u2014(CH2)0-4\u2014CO\u2014R1-heterocycle where R1-heterocycle is as defined above,
(15) \u2014(CH2)0-4\u2014CO\u2014RN-4 where RN-4 is selected from the group consisting of morpholinyl, thiomorpholinyl, piperazinyl, piperidinyl, homomorpholinyl, homothiomorpholinyl, homothiomorpholinyl S-oxide, homothiomorpholinyl S,S-dioxide, pyrrolinyl and pyrrolidinyl where each group is optionally substituted with one, two, three, or four of C1-C6 alkyl,
(16) \u2014(CH2)0-4\u2014CO\u2014O\u2014RN-5 where RN-5 is selected from the group consisting of:
(a) C1-C6 alkyl,
(b) \u2014(CH2)0-2-(R1-aryl) where R1-aryl is as defined above,
(c) C2-C6 alkenyl containing one or two double bonds,
(d) C2-C6 alkynyl containing one or two triple bonds,
(e) C3-C7 cycloalkyl,
(f) \u2014(CH2)0-2-(R1-heteroaryl) where R1-heteroaryl is as defined above,
(17) \u2014(CH2)0-4\u2014SO2\u2014NRN-2RN-3 where RN-2 and RN-3 are as defined above,
(18) \u2014(CH2)0-4\u2014SO\u2014(C1-C8 alkyl),
(19) \u2014(CH2)0-4\u2014SO2\u2014(C1-C12 alkyl),
(20) \u2014(CH2)0-4\u2014SO2\u2014(C3-C7 cycloalkyl),
(21) \u2014(CH2)0-4\u2014N(H or RN-5)\u2014CO\u2014O\u2014RN-5 where RN-5 can be the same or different and is as defined above,
(22) \u2014(CH2)0-4\u2014N(H or RN-5)\u2014CO\u2014N(RN-5)2, where RN-5 can be the same or different and is as defined above,
(23) \u2014(CH2)0-4\u2014N\u2014CS\u2014N(RN-5)2, where RN-5 can be the same or different and is as defined above,
(24) \u2014(CH2)0-4\u2014N(\u2014H or RN-5)\u2014CO\u2014RN-2 where RN-5 and RN-2 can be the same or different and are as defined above,
(25) \u2014(CH2)0-4\u2014NRN-2RN-3 where RN-2 and RN-3 can be the same or different and are as defined above,
(26) \u2014(CH2)0-4\u2014RN-4 where RN-4 is as defined above,
(27) \u2014(CH2)0-4\u2014O\u2014CO\u2014(C1-C6 alkyl),
(28) \u2014(CH2)0-4\u2014O\u2014P(O)\u2014(ORN-aryl-1)2 where RN-aryl-1 is \u2014H or C1-C4 alkyl,
(29) \u2014(CH2)0-4\u2014O\u2014CO\u2014N(RN-5)2 where RN-5 is as defined above,
(30) \u2014(CH2)0-4\u2014O\u2014CS\u2014N(RN-5)2 where RN-5 is as defined above,
(31) \u2014(CH2)0-4\u2014O\u2014(RN-5)2 where RN-5 is as defined above,
(32) \u2014(CH2)0-4\u2014O\u2014(RN-5)2\u2014COOH where RN-5 is as defined above,
(33) \u2014(CH2)0-4\u2014S\u2014( RN-5)2 where RN-5 is as defined above,
(34) \u2014(CH2)0-4\u2014O\u2014(C1-C6 alkyl optionally substituted with one, two, three, four, or five of \u2014F),
(35) C3-C7 cycloalkyl,
(36) C2-C6 alkenyl with one or two double bonds optionally substituted with C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(37) C2-C6 alkynyl with one or two triple bonds optionally substituted with C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C=-N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(38) \u2014(CH2)0-4\u2014N(\u2014H or RN-5) \u2014SO2\u2014RN-2 where RN-5 and RN-2 can be the same or different and are as described above,
(39) \u2014(CH2)0-4\u2014C3-C7 cycloalkyl,
(C) RN-aryl\u2014W\u2014RN-aryl,
(D) RN-aryl\u2014W\u2014RN-heteroaryl,
(E) RN-aryl\u2014W\u2014RN-1-heterocycle, where RN-heterocycle is defined as R1-heterocycle is defined above,
(F) RN-heteroaryl\u2014W\u2014RN-aryl,
(G) RN-heteroaryl\u2014W\u2014RN-heteroaryl,
(H) RN-heteroaryl\u2014W\u2014RN-1-heterocycle, where RN-1-heterocycle is defined as R1-heterocycle is defined above,
(I) RN-heterocycle\u2014W\u2014RN-aryl,
(J) RN-heterocycle\u2014W\u2014RN-heteroaryl,
(K) RN-heterocycle\u2014W\u2014RN-1-heterocycle,
where W is
(1) \u2014(CH2)0-4\u2014,
(2) \u2014O\u2014,
(3) \u2014S(O)0-2\u2014,
(4) \u2014N(RN-5)\u2014 where RN-5 is as defined above, or
(5) \u2014CO\u2014;
(II) \u2014CO\u2014(C1-C10 alkyl) where alkyl is optionally substituted with one two or three substitutents selected from the group consisting of:
(A) \u2014OH,
(B) \u2014C1-C6 alkoxy,
(C) \u2014C1-C6 thioalkoxy,
(D) \u2014CO\u2014O\u2014RN-8 where RN-8 is \u2014H, C1-C6 alkyl or -phenyl,
(E) \u2014CO\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(F) \u2014CO\u2014RN-4 where RN-4 is as defined above,
(G) \u2014SO2\u2014(C1-C8 alkyl),
(H) \u2014SO2\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(I) \u2014NH\u2014CO\u2014(C1-C6 alkyl),
(J) \u2014NH\u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(K) \u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(L) \u2014RN-4 where RN-4 is as defined above,
(M) \u2014O\u2014CO\u2014(C1-C6 alkyl),
(N) \u2014O\u2014CO\u2014NRN-8RN-8 where RN-8 are the same or different and are as defined above,
(O) \u2014O\u2014(C1-C5 alkyl)-COOH,
(P) \u2014O\u2014(C1-C6 alkyl optionally substitued with one, two, or three of \u2014F, \u2014CI, \u2014Br, \u2014I),
(Q) \u2014NH\u2014SO2\u2014(C1-C6 alkyl),
(R) \u2014F, \u2014Cl,
(III) \u2014CO\u2014(C1-C6 alkyl)-O\u2014(C1-C6 alkyl) where alkyl is optionally substituted with one, two, or three substitutents selected from the group consisting of
(A) \u2014OH,
(B) \u2014C1-C6 alkoxy,
(C) \u2014C1-C6 thioalkoxy,
(D) \u2014CO\u2014O\u2014RN-8 where RN-8 is \u2014H, C1-C6 alkyl or -phenyl,
(E) \u2014CO\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(F) \u2014CO\u2014RN-4 where RN-4 is as defined above,
(G) \u2014SO2\u2014(C1-C8 alkyl),
(H) \u2014SO2\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(I) \u2014NH\u2014CO\u2014(C1-C6 alkyl),
(J) \u2014NH\u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(K) \u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(L) \u2014RN-4 where RN-4 is as defined above,
(M) \u2014O\u2014CO\u2014(C1-C6 alkyl),
(N) \u2014O\u2014CO\u2014NRN-8RN-8 where RN-8 are the same or different and are as defined above,
(O) \u2014O\u2014(C1-C5 alkyl)-COOH,
(P) \u2014O\u2014(C1-C6 alkyl optionally substitued with one, two, or three of \u2014F, \u2014CI, \u2014Br, \u2014I),
(Q) \u2014NH\u2014SO2-(C1-C6 alkyl),
(R) \u2014F, \u2014Cl,
(IV) \u2014CO\u2014(C1-C6 alkyl)-S\u2014(C1-C6 alkyl) where alkyl is optionally substituted with one, two, or three of substitutents selected from the group consisting of
(A) \u2014OH,
(B) \u2014C1-C6 alkoxy,
(C) \u2014C1-C6 thioalkoxy,
(D) \u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(E) \u2014CO\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(F) \u2014CO\u2014RN-4 where RN-4 is as defined above,
(G) \u2014SO2\u2014(C1-C8 alkyl),
(H) \u2014SO2\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(I) \u2014NH\u2014CO\u2014(C1-C6 alkyl)
(J) \u2014NH\u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(K) \u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(L) \u2014RN-4 where RN-4 is as defined above,
(M) \u2014O\u2014CO\u2014(C1-C6 alkyl),
(N) \u2014O\u2014CO\u2014NRN-8RN-8 where the RN-8s are the same or different and are as defined above,
(O) \u2014O\u2014(C1-C5 alkyl)-COOH,
(P) \u2014O\u2014(C1-C6 alkyl optionally substitued with one, two, or three of \u2014F, \u2014Cl, \u2014Br, \u2014I),
(Q) \u2014NH\u2014SO2\u2014(C1-C6 alkyl),
(R) \u2014F, \u2014Cl,
(V) \u2014CO\u2014CH(\u2014(CH2)0-2\u2014O\u2014RN-10)\u2014(CH2)0-2-RN-arylRN-heteroaryl) where RN-aryl and RN-heteroaryl are as defined above, where RN-10 is selected from the group consisting of:
(A) \u2014H,
(B) C1-C6 alkyl,
(C) C3-C7 cycloalkyl,
(D) C2-C6 alkenyl with one double bond,
(E) C2-C6 alkynyl with one triple bond,
(F) R1-aryl where R1-aryl is as defined above,
(G) RN-heteroaryl where RN-heteroaryl is as defined above,
(VI) \u2014CO\u2014(C3-C8 cycloalkyl) where cycloalkyl is optionally substituted with one or two substitutents selected from the group consisting of:
(A) \u2014(CH2)0-4\u2014OH,
(B) \u2014(CH2)0-4-C1-C6 alkoxy,
(C) \u2014(CH2)0-4-C1-C6 thioalkoxy,
(D) \u2014(CH2)0-4\u2014CO\u2014O\u2014RN-8 where RN-8 is \u2014H, C1-C6 alkyl or -phenyl,
(E) \u2014(CH2)0-4\u2014CO\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(F) \u2014(CH2)0-4\u2014CO\u2014RN-4 where RN-4 is as defined above,
(G) \u2014(CH2)0-4\u2014SO2\u2014(C1-C8 alkyl),
(H) \u2014(CH2)0-4\u2014SO2\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(I) \u2014(CH2)0-4\u2014NH\u2014CO\u2014(C1-C6 alkyl),
(J) \u2014NH\u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(K) \u2014(CH2)0-4\u2014NRN-2RN-3 where RN-2 and RN-3 are the same or different and are as defined above,
(L) \u2014(CH2)0-4-RN-4 where RN-4 is as defined above,
(M) \u2014O\u2014CO\u2014(C1-C6 alkyl),
(N) \u2014O\u2014CO\u2014NRN-8RN-8 where the RN-8s are the same or different and are as defined above,
(O) \u2014O\u2014(C1-C5 alkyl)-COOH,
(P) \u2014O\u2014(C1-C6 alkyl optionally substitued with one, two, or three of \u2014F, \u2014Cl, \u2014Br, \u2014I),
(Q) \u2014NH\u2014SO2\u2014(C1-C6 alkyl),
(R) \u2014F, \u2014Cl,
where RC is:
(I) \u2014C1-C10 alkyl optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above, \u2014OC\u2550O NR1-aR1-b where R1-a and R1-b are as defined above, \u2014S(\u2550O)0-2 R1-a where R1-a is as defined above, \u2014NR1-aC\u2550O NR1-aR1-b where R1-a and R1-b are as defined above, \u2014C\u2550O NR1-aR1-b where R1-a and R1-b are as defined above, and \u2014S(\u2550O)2 NR1-aR1-b where R1-a and R1-b are as defined above,
(II) \u2014(CH2)0-3\u2014(C3-C8) cycloalkyl where cycloalkyl can be optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014CO\u2014OH, \u2014CO\u2014O\u2014(C1-C4 alkyl), \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(III) \u2014(CRC-xRC-y)0-4\u2014RC-aryl where RC-x and RC-y are \u2014H,
C1-C4 alkyl optionally substituted with one or two \u2014OH,
C1-C4 alkoxy optionally substituted with one, two, or three of \u2014F,
\u2014(CH2)0-4-C3-C7 cycloalkyl,
C2-C6 alkenyl containing one or two double bonds,
C2-C6 alkynyl containing one or two triple bonds, phenyl,
and where RC-x and RC-y are taken together with the carbon to which they are attached to form a carbocycle of three, four, five, six and seven carbon atoms, optionally where one carbon atom is replaced by a heteroatom selected from the group consisting of \u2014O\u2014, \u2014S\u2014, \u2014SO2\u2014, \u2014NRN-2\u2014 and RC-aryl is defined as RN-aryl is defined above;
(IV) \u2014(CRC-xRC-y)0-4\u2014RC-heteroaryl where RC-heteroaryl is defined as RN-heteroaryl is defined above and RC-x and RC-y are as defined above,
(V) \u2014(CRC-xRC-y)0-4\u2014RC-aryl\u2014RC-aryl where RC-aryl, RC-x and RC-y are as defined above,
(VI) \u2014(CRC-xRC-y)0-4\u2014RC-aryl\u2014RC-heteroaryl where RC-aryl, RC-heteroaryl, RC-x and RC-y are as defined above,
(VII) \u2014(CRC-xRC-y)0-4\u2014RC-heteroaryl\u2014RC-aryl where RC-heteroaryl, RC-aryl, RC-x and RC-y are as defined above,
(VIII) \u2014(CRC-xRC-y)0-4\u2014RC-heteroaryl\u2014RC-heteroaryl where RC-heteroaryl, RC-x and RC-y are as defined above,
(IX) \u2014(CRC-xRC-y)0-4\u2014RC-aryl\u2014RC-heterocycle where RC-aryl, RC-x and RC-y are as defined above, and RC-heterocycle is defined as RN-heterocycle is defined above,
(X) \u2014(CRC-xRC-y)0-4\u2014RC-heteroaryl\u2014RC-heterocycle where RC-heteroaryl, RC-heterocycle, RC-x and RC-y are as defined above,
(XI) \u2014(CRC-xRC-y)0-4\u2014RC-heterocycle\u2014RC-aryl where RC-heterocycle, RC-aryl, RC-x and RC-y are as defined above,
(XII) \u2014(CRC-xRC-y)0-4\u2014RC-heterocycle\u2014RC-heteroaryl where RC-heterocycle, RC-heteroaryl, RC-x and RC-y are as defined above,
(XIII) \u2014(CRC-xRC-y)0-4\u2014RC-heterocycle\u2014RC-heterocycle where RC-heterocycle, RC-x and RC-y are as defined above,
(XIV) \u2014(CRC-xRC-y)0-4\u2014RC-heterocycle where RC-heterocycle, RC-x and RC-y are as defined above,
(XV) \u2014C(RC-1)(RC-2)1-3\u2014CO\u2014N\u2014(RC-3)2 where RC-1, and RC-2 are the same or different and are selected from the group consisting of:
(A) \u2014H,
(B) \u2014C1-C6 alkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(C) C2-C6 alkenyl with one or two double bonds, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(D) C2-C6 alkynyl with one or two triple bonds, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(E) \u2014(CH2)1-2\u2014S(O)0-2\u2014(C1-C6 alkyl),
(F) \u2014(CH2)0-4\u2014C3-C7 cycloalkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(G) \u2014(C1-C4 alkyl)-RC\u2032-aryl where RC\u2032-aryl is as defined for R1-aryl,
(H) \u2014(C1-C4 alkyl)-RC-heteroaryl where RC-heteroaryl is as defined above,
(I) \u2014(C1-C4 alkyl)-RC-heterocycle where RC-heterocycle is as defined above,
(J) \u2014RC-heteroaryl where RC-heteroaryl is as defined above,
(K) \u2014RC-heterocycle where RC-heterocycle is as defined above,
(M) \u2014(CH2)1-4\u2014RC-4\u2014(CH2)0-4\u2014RC\u2032-aryl where RC-4 is \u2014O\u2014, \u2014S\u2014 or \u2014NRC-5\u2014 where RC-5 is C1-C6 alkyl, and where RC\u2032-aryl is defined above,
(N) \u2014(CH2)1-4\u2014RC-4\u2014(CH2)0-4\u2014RC-heteroaryl where RC-4 and RC-heteroaryl are as defined above,
(O) \u2014RC\u2032-aryl where RC\u2032-aryl is as defined above, and where RC-3 is the same or different and is:
(A) \u2014H,
(B) \u2014C1-C6 alkyl optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(C) C2-C6 alkenyl with one or two double bonds, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(D) C2-C6 alkynyl with one or two triple bonds, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(E) \u2014(CH2)0-4\u2014C3-C7 cycloalkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(F) \u2014RC\u2032-aryl where RC\u2032-aryl is as defined above,
(G) \u2014RC-heteroaryl where RC-heteroaryl is as defined above,
(H) \u2014RC-heterocycle where RC-heterocycle is as defined above,
(I) \u2014(C1-C4 alkyl)-RC\u2032-aryl where RC\u2032-aryl is as defined above,
(J) \u2014(C1-C4 alkyl)-RC-heteroaryl where RC-heteroaryl is as defined above,
(K) \u2014(C1-C4 alkyl)-RC-heterocycle where RC-heterocycle is as defined above,
(XVI) \u2014CH(RC-aryl)2 where RC-aryl are the same or different and are as defined above,
(XVII) \u2014CH(RC-heteroaryl)2 where RC-heteroaryl are the same or different and are as defined above,
(XVIII) \u2014CH(RC-aryl)(RC-heteroaryl) where RC-aryl and RC-heteroaryl are as defined above,
(XIX) -cyclopentyl, -cyclohexyl, or -cycloheptyl ring fused to RC-aryl or RC-heteroaryl or RC-heterocycle where RC-aryl or RC-heteroaryl or RC-heterocycle are as defined above where one carbon of cyclopentyl, cyclohexyl, or -cycloheptyl is optionally replaced with NH, NRN-5, O, S(\u2550O)0-2 , and where cyclopentyl, cyclohexyl, or -cycloheptyl can be optionally substituted with one or two \u2014C1-C3 alkyl, \u2014F, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2550O, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(XX) C2-C10 alkenyl containing one or two double bonds optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(XXI) C2-C10 alkynyl containing one or two triple bonds optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(XXI) \u2014(CH2)0-1\u2014CHRC-6\u2014(CH2)0-1\u2014RC-aryl where RC-aryl is as defined above and RC-6 is \u2014(CH2)0-6\u2014OH,
(XXII) \u2014(CH2)0-1\u2014CHRC-6\u2014(CH2)0-1\u2014RC-heteroaryl where RC-heteroaryl and RC-6 is as defined above,
(XXIII) \u2014CH(\u2014RC-aryl or RC-heteroaryl)\u2014CO\u2014O(C1-C4 alkyl) where RC-aryl and RC-heteroaryl are as defined above,
(XXIV) \u2014CH (\u2014CH2\u2014OH)\u2014CH(\u2014OH)-micro-NO2,
(XXV) (C1-C6 alkyl)-O\u2014(C1-C6 alkyl)-OH,
(XXVII) \u2014CH2\u2014NH\u2014CH2\u2014CH(\u2014O\u2014CH2\u2014CH3)2,
(XXVIII) \u2014H,
(XXIX) \u2014(CH2)0-6\u2014C(\u2550NR1-a)(NR1-aR1-b) where R1-a and R1-b are as defined above; and
where R4 is:
where x is 0 or 1 and R5 is H or is:
(I) RP-1 wherein RP-1 is selected from the group consisting of:
(A) \u2014Y\u2014RP-aryl where Y is absent or is oxygen, and RP-aryl is phenyl, 1-naphthyl, 2-naphthyl, tetralinyl, indanyl, or 6,7,8,9-tetrahydro-5H-benzoacycloheptenyl, optionally substituted with one, two or three of the following substituents which can be the same or different and are:
(1) C1-C6 alkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are independently \u2014H or C1-C6 alkyl,
(2) \u2014OH,
(3) \u2014NO2,
(4) \u2014F, \u2014Cl, \u2014Br, \u2014I,
(5) \u2014CO\u2014OH,
(6) \u2014C\u2261N,
(7) \u2014(CH2)0-4\u2014CO\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are selected from the group consisting of:
(a) \u2014H,
(b) \u2014C1-C6 alkyl optionally substituted with one substituent selected from the group consisting of:
\u2003(i) \u2014OH,
\u2003(ii) \u2014NH2,
(c) \u2014C1-C6 alkyl optionally substituted with one to three \u2014F, \u2014Cl, \u2014Br, \u2014I,
(d) \u2014C3-C7 cycloalkyl,
(e) \u2014(C1-C2 alkyl)-(C3-C7 cycloalkyl),
(f) \u2014(C1-C6 alkyl)-O\u2014(C1-C3 alkyl),
(g) \u2014(C2-C6 alkenyl with one or two double bonds,
(h) \u2014C2-C6 alkynyl with one or two triple bonds,
(i) \u2014C1-C6 alkyl chain with one double bond and one triple bond,
(j) \u2014RP-aryl where \u2014RP-aryl is defined above,
(k) \u2014RP-heteroaryl where RP-heteroaryl is defined below,
(l) \u2014C(O)C1-C6 alkyl,
(8) \u2014(CH2)0-4\u2014CO\u2014(C1-C12 alkyl),
(9) \u2014(CH2)0-4\u2014CO\u2014(C2-C12) alkenyl with one, two or three double bonds,
(10) \u2014(CH2)0-4\u2014CO\u2014(C2-C12) alkynyl with one, two or three triple bonds,
(11) \u2014(CH2)0-4\u2014CO\u2014(C3-C7 cycloalkyl),
(12) \u2014(CH2)0-4\u2014CO\u2014RP-aryl where RP-aryl is as defined above,
(13) \u2014(CH2)0-4\u2014CO\u2014RP-heteroaryl where RP-heteroaryl is as defined below,
(14) \u2014(CH2)0-4\u2014CO\u2014RP-heterocycle where RP-heterocycle is selected from the group consisting of:
(A) morpholinyl,
(B) thiomorpholinyl,
(C) thiomorpholinyl S-oxide,
(D) thiomorpholinyl S,S-dioxide,
(E) piperazinyl,
(F) homopiperazinyl,
(G) pyrrolidinyl,
(H) pyrrolinyl,
(I) tetrahydropyranyl,
(J) piperidinyl,
(K) tetrahydrofuranyl,
(L) tetrahythiophenyl,
(M) homopiperidinyl,
(N) imidazolidine,
(O) imidazolidine dione, and
(P) dithiane,
where the RP-heterocycle group is bonded by any atom of the parent RP-heterocycle group substituted by hydrogen such that the new bond to the RP-heterocycle group replaces the hydrogen atom and its bond, where heterocycle is optionally substituted with one thru four:
(1) C1-C6 alkyl optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014O\u2014CO\u2014(C1-C6 alkyl), and \u2014NR1-aR1-b where R1-a and R1-b are as defined above, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy,
(2) C2-C6 alkenyl with one or two double bonds,
(3) C2-C6alkynyl with one or two triple bonds,
(4) \u2014F, Cl, \u2014Br and \u2014I,
(5) C1-C6 alkoxy,
(6) \u2014O\u2014C1-C6 alkyl optionally substituted with one thru three \u2014F,
(7) \u2014NRP-2RP-3 where RP-2 and RP-3 are as defined above,
(8) \u2014OH,
(9) \u2014C\u2261N,
(10) C3-C7 cycloalkyl,
(11) \u2014CO\u2014(C1-C4 alkyl),
(12) \u2014SO2\u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(13) \u2014CO\u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(14) \u2014SO2\u2014(C1-C4 alkyl);
(15) \u2550O; or
(16) \u2014O\u2014CO\u2014(C1-C6 alkyl);
(15) \u2014(CH2)0-4\u2014CO\u2014RN-4 where RN-4 is selected from the group consisting of morpholinyl, thiomorpholinyl, piperazinyl, piperidinyl, homomorpholinyl, homothiomorpholinyl, homomorpholinyl S-oxide, homothiomorpholinyl S,S-dioxide, pyrrolinyl and pyrrolidinyl where each group is optionally substituted with one, two, three, or four of: C1-C6 alkyl,
(16) \u2014(CH2)0-4\u2014CO\u2014O\u2014RN-5 where RN-5 is selected from the group consisting of:
(a) C1-C6 alkyl,
(b) \u2014(CH2)0-2 (RP-aryl) where RP-aryl is as defined above,
(c) C2-C6 alkenyl containing one or two double bonds,
(d) C2-C6 alkynyl containing one or two triple bonds,
(e) C3-C7 cycloalkyl,
(f) \u2014(CH2)0-2\u2014(RP-heteroaryl) where RP-heteroaryl is as defined below,
(17) \u2014(CH2)0-4\u2014SO2\u2014NRP-2RP-3 where RP-2 and RP-3 are as defined above,
(18) \u2014(CH2)0-4\u2014SO\u2014(C1-C8 alkyl)
(19) \u2014(CH2)0-4\u2014SO2\u2014(C1\u2014C12 alkyl)
(20) \u2014(CH2)0-4\u2014SO2\u2014(C3-C7 cycloalkyl),
(21) \u2014(CH2)0-4\u2014N(H or RN-5)\u2014CO\u2014O\u2014RN-5 where RN-5 can be the same or different and is as defined above,
(22) \u2014(CH2)0-4\u2014N(H or RN-5) \u2014CO\u2014N (RN-5) 2, where RN-5 can be the same or different and is as defined above,
(23) \u2014(CH2)0-4\u2014N\u2014CS\u2014N (RN-5)2, where RN-5 can be the same or different and is as defined above,
(24) \u2014(CH2)0-4\u2014N(\u2014H or RN-5)\u2014CO\u2014RP-2 where RN-5 and RP-2 can be the same or different and are as defined above,
(25) \u2014(CH2)0-4\u2014NRP-2RP-3 where RP-2 and RP-3 can be the same or different and are as defined above,
(26) \u2014(CH2)0-4-RN-4 where RN-4 is as defined above,
(27) \u2014(CH2)0-4\u2014O\u2014CO\u2014(C1-C6 alkyl)
(28) \u2014(CH2)0-4\u2014O\u2014P(O)\u2014(ORN-aryl-1)2 where RN-aryl-1 is \u2014H or C1-C4 alkyl,
(29) \u2014(CH2)0-4\u2014O\u2014CO\u2014N(RN-5)2 where RN-5 is as defined above,
(30) \u2014(CH2)0-4\u2014O\u2014CS\u2014N (RN-5)2 where RN-5 is as defined above,
(31) \u2014(CH2)0-4\u2014O\u2014(RN-5)2 where RN-5 is as defined above,
(32) \u2014(CH2)0-4\u2014O\u2014( RN-5)2\u2014COOH where RN-5 is as defined above,
(33) \u2014(CH2)0-4\u2014S\u2014( RN-5)2 where RN-5 is as defined above,
(34) \u2014(CH2)0-4\u2014O\u2014(C1-C6 alkyl optionally substituted with one, two, three, four, or five of: \u2014F),
(35) C3-C7 cycloalkyl,
(36) C2-C6 alkenyl with one or two double bonds optionally substituted with C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(37) C2-C6 alkynyl with one or two triple bonds optionally substituted with C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(38) \u2014(CH2)0-4\u2014N(\u2014H or RN-5)\u2014SO2-RP-2 where RN-5 and RP-2 can be the same of different and are as described above,
(39) \u2014(CH2)0-4\u2014C3-C7 cycloalkyl,
(B) \u2014Y\u2014RP-heteroaryl where Y is absent or is oxygen, and RP-heteroaryl is selected from the group consisting of:
(A) pyridinyl,
(B) pyrimidinyl,
(C) quinolinyl,
(F) benzothienyl,
(G) indolyl,
(H) indolinyl,
(I) pryidazinyl,
(J) pyrazinyl,
(K) isoindolyl,
(L) isoquinolyl,
(M) quinazolinyl,
(N) quinoxalinyl,
(O) phthalazinyl,
(P) imidazolyl,
(Q) isoxazolyl,
(R) pyrazolyl,
(S) oxazolyl,
(T) thiazolyl,
(U) indolizinyl,
(V) indazolyl,
(W) benzothiazolyl,
(X) benzimidazolyl,
(Y) benzofuranyl,
(Z) furanyl,
(AA) thienyl,
(BB) pyrrolyl,
(CC) oxadiazolyl,
(DD) thiadiazolyl,
(EE) triazolyl,
(FF) tetrazolyl,
(II) oxazolopyridinyl,
(JJ) imidazopyridinyl,
(KK) isothiazolyl,
(LL) naphthyridinyl,
(MM) cinnolinyl,
(NN) carbazolyl,
(OO) beta-carbolinyl,
(PP) isochromanyl,
(QQ) chromanyl,
(SS) tetrahydroisoquinolinyl,
(TT) isoindolinyl,
(UU) isobenzotetrahydrofuranyl,
(VV) isobenzotetrahydrothienyl,
(WW) isobenzothienyl,
(XX) benzoxazolyl,
(YY) pyridopyridinyl,
(ZZ) benzotetrahydrofuranyl,
(AAA) benzotetrahydrothienyl,
(BBB) purinyl,
(CCC) benzodioxolyl,
(DDD) triazinyl,
(EEE) phenoxazinyl,
(FFF) phenothiazinyl,
(GGG) pteridinyl,
(HHH) benzothiazolyl,
(III) imidazopyridinyl,
(JJJ) imidazothiazolyl,
(KKK) dihydrobenzisoxazinyl,
(LLL) benzisoxazinyl,
(MMM) benzoxazinyl,
(NNN) dihydrobenzisothiazinyl,
(OOO) benzopyranyl,
(PPP) benzothiopyranyl,
(QQQ) coumarinyl,
(RRR) isocoumarinyl,
(SSS) chromonyl,
(TTT) chromanonyl,
(UUU) pyridinyl-N-oxide,
where the RP-heteroaryl group is bonded by any atom of the parent RP-heteroaryl group substituted by hydrogen such that the new bond to the RP-heteroaryl group replaces the hydrogen atom and its bond, where heteroaryl is optionally substituted with one, two, three, or four of:
(1) C1-C6 alkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(2) \u2014OH,
(3) \u2014NO2,
(4) \u2014F, \u2014Cl, \u2014Br, \u2014I,
(5) \u2014CO\u2014OH,
(6) \u2014C\u2261N,
(7) \u2014(CH2)0-4\u2014CO\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are selected from the group consisting of:
(a) \u2014H,
(b) \u2014C1-C6 alkyl optionally substituted with one substitutent selected from the group consisting of:
\u2003(i) \u2014OH,
\u2003(ii) \u2014NH2,
(c) \u2014C1-C6 alkyl optionally substituted with one to three \u2014F, \u2014Cl, \u2014Br, \u2014I,
(d) \u2014C3-C7 cycloalkyl,
(e) \u2014(C1-C2 alkyl)-(C3-C7 cycloalkyl),
(f) \u2014(C1-C6 alkyl)-O\u2014(C1-C3 alkyl),
(g) \u2014C2-C6 alkenyl with one or two double bonds,
(h) \u2014C2-C6 alkynyl with one or two triple bonds,
(i) \u2014C1-C6 alkyl chain with one double bond and one triple bond,
(j) \u2014RP-aryl where RP-aryl is as defined above,
(k) \u2014RP-heteroaryl where RP-heteroaryl is as defined above,
(8) \u2014(CH2)0-4\u2014CO\u2014(C1-C12 alkyl),
(9) \u2014(CH2)0-4\u2014CO\u2014(C2-C12 alkenyl with one, two or three double bonds),
(10) \u2014(CH2)0-4\u2014CO\u2014(C2-C12 alkynyl with one, two or three triple bonds),
(11) \u2014(CH2)0-4\u2014CO\u2014(C3-C7 cycloalkyl),
(12) \u2014(CH2)0-4\u2014CO\u2014RP-aryl where RP-aryl is as defined above,
(13) \u2014(CH2)0-4\u2014CO\u2014RP-heteroaryl where RP-heteroaryl is as defined above,
(14) \u2014(CH2)0-4\u2014CO\u2014RP-heterocycle where RP-heterocycle is as defined above,
(15) \u2014(CH2)0-4\u2014CO\u2014RN-4 where RN-4 is selected from the group consisting of morpholinyl, thiomorpholinyl, piperazinyl, piperidinyl, homomorpholinyl, homothiomorpholinyl, homomorpholinyl S-oxide, homothiomorpholinyl S,S-dioxide, pyrrolinyl and pyrrolidinyl where each group is optionally substituted with one, two, three, or four of: C1-C6 alkyl,
(16) \u2014(CH2)0-4\u2014CO\u2014O\u2014RN-5 where RN-5 is selected from the group consisting of:
(a) C1-C6 alkyl,
(b) \u2014(CH2)0-2\u2014(RP-aryl) where RP-aryl is as defined above,
(c) C2-C6 alkenyl containing one or two double bonds,
(d) C2-C6 alkynyl containing one or two triple bonds,
(e) C3-C7 cycloalkyl,
(f) \u2014(CH2)0-2\u2014(RP-heteroaryl) where RP-heteroaryl is as defined above,
(17) \u2014(CH2)0-4\u2014SO2\u2014NRP-2RP-3 where RP-2 and RP-3 are as defined above,
(18) \u2014(CH2)0-4\u2014SO\u2014(C1-C8 alkyl),
(19) \u2014(CH2)0-4\u2014SO2\u2014(C1-C12 alkyl),
(20) \u2014(CH2)0-4\u2014SO2\u2014(C3-C7 cycloalkyl),
(21) \u2014(CH2)0-4\u2014N(H or RN-5)\u2014CO\u2014O\u2014RN-5 where RN-5 can be the same or different and is as defined above,
(22) \u2014(CH2)0-4\u2014N(H or RN-5)\u2014CO\u2014N(RN-5)2, where RN-5 can be the same or different and is as defined above,
(23) \u2014(CH2)0-4\u2014N\u2014CS\u2014N(RN-5)2, where RN-5 can be the same or different and is as defined above,
(24) \u2014(CH2)0-4\u2014N(\u2014H or RN-5)\u2014CO\u2014RP-2 where RN-5 and RP-2 can be the same or different and are as defined above,
(25) \u2014(CH2)0-4\u2014NRP-2RP-3 where RP-2 and RP-3 can be the same or different and are as defined above,
(26) \u2014(CH2)0-4\u2014RN-4 where RN-4 is as defined above,
(27) \u2014(CH2)0-4\u2014O\u2014CO\u2014(C1-C6 alkyl),
(28) \u2014(CH2)0-4\u2014O\u2014P(O)\u2014(ORN-aryl-1)2 where RN-aryl-1 is \u2014H or C1-C4 alkyl,
(29) \u2014(CH2)0-4\u2014O\u2014CO\u2014N(RN-5)2 where RN-5 is as defined above,
(30) \u2014(CH2)0-4\u2014O\u2014CS\u2014N(RN-5)2 where RN-5 is as defined above,
(31) \u2014(CH2)0-4\u2014O\u2014(RN-5)2 where RN-5 is as defined above,
(32) \u2014(CH2)0-4\u2014O\u2014( RN-5)2\u2014COOH where RN-5 is as defined above,
(33) \u2014(CH2)0-4\u2014S\u2014( RN-5)2 where RN-5 is as defined above,
(34) \u2014(CH2)0-4\u2014O\u2014(C1-C6 alkyl optionally substituted with one, two, three, four, or five of: \u2014F),
(35) C3-C7 cycloalkyl,
(36) C2-C6 alkenyl with one or two double bonds optionally substituted with C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(37) C2-C6 alkynyl with one or two triple bonds optionally substituted with C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014NR1-aR1-b where R1-a and R1-b are as defined above,
(38) \u2014(CH2)0-4\u2014N(\u2014H or RN-5)\u2014SO2\u2014RP-2 where RN-5 and RP-2 can be the same of different and are as described above,
(39) \u2014(CH2)0-4\u2014C3-C7 cycloalkyl,
(C) RP-aryl\u2014W\u2014RP-aryl,
(D) RP-aryl\u2014W\u2014RP-heteroaryl,
(E) RP-aryl\u2014W\u2014RP-heterocycle,
(F) RP-heteroaryl\u2014W\u2014RP-aryl,
(G) RP-heteroaryl\u2014W\u2014RP-heteroaryl,
(H) RP-heteroaryl\u2014W\u2014RP-heterocycle,
(I) RP-heterocycle\u2014W\u2014RP-aryl,
(J) RP-heterocycle\u2014W\u2014RP-heteroaryl,
(K) RP-heterocycle\u2014W\u2014RP-heterocycle, where W is
(1) \u2014(CH2)0-4\u2014,
(2) \u2014O\u2014,
(3) \u2014S(O)0-2\u2014,
(4) \u2014N(RN-5)\u2014 where RN-5 is as defined above;
(5) \u2014CO\u2014; or
(6) \u2014O\u2014(CH2)1-4\u2014,
(L) \u2014Y\u2014RP-heterocycle where Y is absent or is oxygen, and RP-heterocycle is defined above;
(II) \u2014(C1-C10 alkyl) where alkyl is optionally substituted with one, two, or three substituents selected from the group consisting of:
(A) \u2014OH,
(B) \u2014C1-C6 alkoxy,
(C) \u2014C1-C6 thioalkoxy,
(D) \u2014CO\u2014O\u2014RN-8 where RN-8 is \u2014H, C1-C6 alkyl, phenyl or benzyl,
(E) \u2014CO\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(F) \u2014CO\u2014RN-4 where RN-4 is as defined above,
(G) \u2014SO2\u2014(C1-C8 alkyl),
(H) \u2014SO2\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(I) \u2014NH\u2014CO\u2014(C1-C6 alkyl),
(J) \u2014NH\u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(K) \u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(L) \u2014RN-4 where RN-4 is as defined above,
(M) \u2014O\u2014CO\u2014(C1-C6 alkyl),
(N) \u2014O\u2014CO\u2014NRN-8RN-8 where the RN-8s are the same or different and are as defined above,
(O) \u2014O\u2014(C1-C5 alkyl)-COOH,
(P) \u2014O\u2014(C1-C6 alkyl) optionally substituted with one, two, or three of \u2014F, \u2014Cl, \u2014Br, \u2014I,
(Q) \u2014NH\u2014SO2\u2014(C1-C6 alkyl),
(R) \u2014F, \u2014Cl,
(III) \u2014X-T-(C1-C6 alkyl) where X is absent or is C1-C6 alkyl, T is oxygen or is NRP-2, and where alkyl is optionally substituted with one, two, or three substituents selected from the group consisting of:
(A) \u2014OH,
(B) \u2014C1-C6 alkoxy,
(C) \u2014C1-C6 thioalkoxy,
(D) \u2014CO\u2014O\u2014RN-8 where RN-8 is \u2014H, C1-C6 alkyl, phenyl, or benzyl,
(E) \u2014CO\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(F) \u2014CO\u2014RN-4 where RN-4 is as defined above,
(G) \u2014SO2\u2014(C1-C8 alkyl),
(H) \u2014SO2\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(I) \u2014NH\u2014CO\u2014(C1-C6 alkyl)
(J) \u2014NH\u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(K) \u2014NRP- 2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(L) \u2014RN-4 where RN-4 is as defined above,
(M) \u2014O\u2014CO\u2014(C1-C6 alkyl),
(N) \u2014O\u2014CO\u2014NRN-8RN-8 where the RN-8s are the same or different and are as defined above,
(O) \u2014O\u2014(C1-C5 alkyl)-COOH,
(P) \u2014O\u2014(C1-C6) alkyl optionally substituted with one, two, or three of \u2014F, \u2014Cl, \u2014Br, \u2014I,
(Q) \u2014NH\u2014SO2\u2014(C1-C6 alkyl),
(R) \u2014F, \u2014Cl,
(S) \u2014O\u2014RP-aryl,
(T) \u2014O\u2014RP-heteroaryl, or
(U) \u2014O\u2014RP-hetrocycle,
(IV) \u2014(C1-C6 alkyl)-Z-(C1-C6 alkyl) where Z is S or O, and alkyl is optionally substituted with one, two, or three substituents selected from the group consisting of:
(A) \u2014OH,
(B) \u2014C1-C6 alkoxy,
(C) \u2014C1-C6 thioalkoxy,
(D) \u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(E) \u2014CO\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(F) \u2014CO\u2014RN-4 where RN-4 is as defined above,
(G) \u2014SO2\u2014(C1-C8 alkyl),
(H) \u2014SO2\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(I) \u2014NH\u2014CO\u2014(C1-C6 alkyl),
(J) \u2014NH\u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(K) \u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(L) \u2014RN-4 where RN-4 is as defined above,
(M) \u2014O\u2014CO\u2014(C1-C6 alkyl),
(N) \u2014O\u2014CO\u2014NRN-8RN-8 where the RN-8S are the same or different and are as defined above,
(O) \u2014O\u2014(C1-C5 alkyl)-COOH,
(P) \u2014O\u2014(C1-C6)alkyl optionally substituted with one, two, or three of \u2014F, \u2014Cl, \u2014Br, \u2014I,
(Q) \u2014NH\u2014SO2\u2014(C1-C6 alkyl),
(R) \u2014F, \u2014Cl,
(V) \u2014CH (\u2014(CH2)0-2\u2014O\u2014RN-10)\u2014(CH2)0-2\u2014RP-arylRP-heteroaryl) where RP-aryl and RP-heteroaryl are as defined above, where RN-10 is selected from the group consisting of:
(A) \u2014H,
(B) C1-C6 alkyl,
(C) C3-C7 cycloalkyl,
(D) C2-C6 alkenyl with one double bond,
(E) C2-C6 alkynyl with one triple bond,
(F) RP-aryl where RP-aryl is as defined above,
(G) RP-heteroaryl where RP-heteroaryl is as defined above,
(VI) \u2014(C3-C8 cycloalkyl) where cycloalkyl is optionally substituted with one or two substituents selected from the group consisting of:
(A) \u2014(CH2)0-4\u2014OH,
(B) \u2014(CH2)0-4-C1-C6 alkoxy,
(C) \u2014(CH2)0-4-C1-C6 thioalkoxy,
(D) \u2014(CH2)0-4\u2014CO\u2014O\u2014RN-8 where RN-8 is \u2014H, C1-C6 alkyl, phenyl or benzyl,
(E) \u2014(CH2)0-4\u2014CO\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(F) \u2014(CH2)0-4\u2014CO\u2014RN-4 where RN-4 is as defined above,
(G) \u2014(CH2)0-4\u2014SO2\u2014(C1-C8 alkyl),
(H) \u2014(CH2)0-4\u2014SO2\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(I) \u2014(CH2)0-4\u2014NH\u2014CO\u2014(C1-C6 alkyl),
(J) \u2014NH\u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(K) \u2014(CH2)0-4\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(L) \u2014(CH2)0-4\u2014RN-4 where RN-4 is as defined above,
(M) \u2014O\u2014CO\u2014(C1-C6 alkyl),
(N) \u2014O\u2014CO\u2014NRN-8RN-8 where the RN-8s are the same or different and are as defined above,
(O) \u2014O\u2014(C1-C5 alkyl)-COOH,
(P) \u2014O\u2014C1-C6 alkyl optionally substituted with one, two, or three of: \u2014F, \u2014Cl, \u2014Br, \u2014I,
(Q) \u2014NH\u2014SO2\u2014(C1-C6 alkyl),
(R) \u2014F, \u2014Cl;
(VII) \u2014(CRP-xRP-y)0-4\u2014RP-1 where RP-1 is as defined above and each of RP-x and RP-y are independently any combination of:
(A) \u2014H,
(B) C1-C6 alkyl, optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C3 alkoxy, \u2014COOH, \u2014COO(C1-C6 alkyl), \u2014CONR1aR1b and \u2014NR1-aR1-b where R1-a and R1-b are \u2014H or C1-C6 alkyl,
(C) \u2014CH2\u2014S\u2014(C1-C6 alkyl),
(D) \u2014CH2\u2014CH2\u2014S\u2014(C1-C6 alkyl),
(E) C2-C6 alkenyl with one or two double bonds,
(F) C2-C6 alkynyl with one or two triple bonds,
(G) \u2014(CH2)n1\u2014(RP-aryl) where n1 is zero or one, where RP-aryl is as defined above,
(H) \u2014(CH2)n1\u2014(RP-heteroaryl) where n1 and RP-heteroaryl are as defined above, or
(I) \u2014(CH2)n1\u2014(RP-heterocycle) where n1 and RP-heterocycle are as defined above,
(J) \u2014(CH2)0-3\u2014(C3-C7) cycloalkyl where cycloalkyl can be optionally substituted with one, two or three substituents selected from the group consisting of C1-C3 alkyl, \u2014F, \u2014Cl, \u2014Br, \u2014I, \u2014OH, \u2014SH, \u2014C\u2261N, \u2014CF3, C1-C6 alkoxy, \u2014O-phenyl, \u2014CO\u2014OH, \u2014CO\u2014O\u2014(C1-C4 alkyl), and \u2014NR1-aR1-b where R1-a and R1-b are as defined above, or
(K) F, Cl, Br or I,
(L) \u2014NRP-2;
or RP-x and RP-y are taken together with the carbon to which they are attached to form a carbocycle of three thru seven carbon atoms, optionally where one carbon atom is replaced by a heteroatom selected from the group consisting of \u2014O\u2014, \u2014S\u2014, \u2014SO2\u2014, and \u2014NRP-2\u2014;
(VIII) \u2014(C1-C6 alkyl)-Z-(C1-C6 alkyl)-T-(C1-C6 alkyl)- wherein Z is S or O, T is O or NRP-2, and alkyl is optionally substituted with one, two, or three substituents selected from the group consisting of:
(A) \u2014OH,
(B) \u2014C1-C6 alkoxy,
(C) \u2014C1-C6 thioalkoxy,
(D) \u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(E) \u2014CO\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(F) \u2014CO\u2014RN-4 where RN-4 is as defined above,
(G) \u2014SO2\u2014(C1-C8 alkyl),
(H) \u2014SO2\u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(I) \u2014NH\u2014CO\u2014(C1-C6 alkyl),
(J) \u2014NH\u2014CO\u2014O\u2014RN-8 where RN-8 is as defined above,
(K) \u2014NRP-2RP-3 where RP-2 and RP-3 are the same or different and are as defined above,
(L) \u2014RN-4 where RN-4 is as defined above,
(M) \u2014O\u2014CO\u2014(C1-C6 alkyl),
(N) \u2014O\u2014CO\u2014NRN-8RN-8 where the RN-8s are the same or different and are as defined above,
(O) \u2014O\u2014(C1-C5 alkyl)-COOH,
(P) \u2014O\u2014(C1-C6 alkyl) optionally substituted with one, two, or three of \u2014F, \u2014Cl, \u2014Br, \u2014I,
(Q) \u2014NH\u2014SO2\u2014(C1-C6 alkyl),
(R) \u2014F, \u2014Cl.
2. A compound or salt according to claim 1 wherein R1 is \u2014(CH2)0-1\u2014(R1-aryl).
3. A compound or salt according to claim 1 wherein R2\u2550R3\u2550H.
4. A compound or salt according to claim 1 wherein Rc is
(a) \u2014(CRC-xRC-y)0-4\u2014RC-aryl,
(b) \u2014(CRC-xRC-y)0-4\u2014RC-heteroaryl or
(c) \u2014(CRC-xRC-y)0-4\u2014RC-heterocycle.
5. A compound or salt according to claim 1 wherein R4 is
6. A compound or salt according to claim 1 wherein RN is RN-1\u2014XN\u2014 where XN is \u2014CO\u2014, where RN-1 is RN-aryl or RN-heteroaryl.
7. A compound or salt according to claim 1 selected from the group consisting of 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)propyl 4-nitrophenyl carbonate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)propyl 4-methylpiperazine-1-carboxylate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-72-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl 2-(dimethylamino)ethyl carbonate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl 2-(acetylamino)ethylcarbamate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl piperazine-1-carboxylate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl 2-aminoethylcarbamate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl 3-aminopropylcarbamate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl (3R)-3-aminopyrrolidine-1-carboxylate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)propyl O-benzyl-L-tyrosinate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl L-tyrosinate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl 3-methoxypropanoate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl (2-hydroxyethoxy)acetate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl D-lysinate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl 2-(2-methoxyethoxy)ethoxyacetate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl {2-2-(dimethylamino)ethyl-(methyl)aminoethoxy}acetate, 1-(benzylamino)methyl-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonylbenzoyl}amino)-propyl (4-methylpiperazin-1-yl)acetate, (1R, 2S)-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonyl-5-methylbenzoyl}-amino)-1-{(3-pent-1-ynylbenzyl)aminomethyl}propyl (4-methylpiperazin-1-yl)acetate, (1R, 2S)-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonyl-5-methylbenzoyl}-amino)-1-{(3-pent-1-ynylbenzyl)aminomethyl}propyl 4-methylpiperazine-1-carboxylate, (1R, 2S)-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonyl-5-methylbenzoyl}-amino)-1-{(3-pent-1-ynylbenzyl)aminomethyl}propyl piperazine-1-carboxylate, (1R, 2S)-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonyl-5-methylbenzoyl}-amino)-1-{(3-pent-1-ynylbenzyl)aminomethyl}propyl {2-2-(dimethylamino)ethyl(methyl)aminoethoxy}acetate, (1R, 2S)-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonyl-5-methylbenzoyl}-amino)-1-{(3-pent-1-ynylbenzyl)aminomethyl}propyl (2-methoxyethoxy)acetate, (1R, 2S)-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonyl-5-methylbenzoyl}-amino)-1-{(3-pent-1-ynylbenzyl)aminomethyl}propyl L-tyrosinate, (1R, 2S)-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonyl-5-methylbenzoyl}-amino)-1-{(3-pent-1-ynylbenzyl)aminomethyl}propyl (3R)-3-aminopyrrolidine-1-carboxylate, (1R,2S)-3-(3,5-difluorophenyl)-2-({3-(dipropylamino)carbonyl-5-methylbenzoyl}-amino)-1-{(3-pent-1-ynylbenzyl)aminomethyl}propyl tetrahydrofuran-3-yl carbonate, N\u2032-(1S,2R)-1-benzyl-3-(cyclohexylamino)-2-hydroxypropyl-N,N-dipropylisophthalamide, (1R,2S)-1-(cyclohexylamino)methyl-2-({3-(dipropylamino)carbonylbenzoyl}-amino)-3-phenylpropyl 4-methylpiperazine-1-carboxylate, (1R,2S)-1-(cyclohexylamino)methyl-2-({3-(dipropylamino)carbonylbenzoyl}-amino)-3-phenylpropyl piperazine-1-carboxylate, (1R,2S)-1-(cyclohexylamino)methyl-2-({3-(dipropylamino)carbonylbenzoyl}-amino)-3-phenylpropyl {2-2-(dimethylamino)ethyl(methyl)aminoethoxy}acetate, (1R,2S)-1-(cyclohexylamino)methyl-2-({3-(dipropylamino)carbonylbenzoyl}-amino)-3-phenylpropyl (2-methoxyethoxy)acetate, (1R,2S)-1-(cyclohexylamino)methyl-2-({3-(dipropylamino)carbonylbenzoyl}-amino)-3-phenylpropyl L-tyrosinate, (1R,2S)-1-(cyclohexylamino)methyl-2-({3-(dipropylamino)carbonylbenzoyl}-amino)-3-phenylpropyl (3R)-3-aminopyrrolidine-1-carboxylate, and (1R,2S)-1-(cyclohexylamino)methyl-2-({3-(dipropylamino)carbonylbenzoyl}-amino)-3-phenylpropyl tetrahydrofuran-3-yl carbonate.
8. A method for the treatment or prevention of Alzheimer’s disease, mild cognitive impairment Down’s syndrome, Hereditary Cerebral Hemorrhage with Amyloidosis of the Dutch-Type, cerebral amyloid angiopathy, other degenerative dementias, dementias of mixed vascular and degenerative origin, dementia associated with Parkinson’s disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, diffuse Lewy body type of Alzheimer’s disease compriseing administration of a therapeutically effective amount of a compound or salt according to claim 1, to a patient in need thereof.
9. A method of treatment as in claim 8, wherein the patient is a human.
10. A method of treatment according to claim 8, wherein the disease is dementia.
11-13. (canceled)
14. A compound according to claim 1, wherein R1 is \u2014CH2-phenyl or \u2014CH2-pyridinyl where the ring portions of each are optionally substituted with 1, 2, 3, or 4 groups independently selected from halogen, C1-C4 alkoxy, hydroxy, \u2014NO2, and C1-C4 alkyl, wherein C1-C4 alkyl is optionally substituted with 1, 2, or 3 substituents independently selected from halogen, OH, SH, NH2, NH(C1-C6 alkyl), N\u2014(C1-C6 alkyl)(C1-C6 alkyl), C\u2261N, CF3.
15. A compound according to claim 1, wherein R1 is \u2014CH2-phenyl or \u2014CH2-pyridinyl where the phenyl or pyridinyl rings are each optionally substituted with 1 or 2 groups independently selected from halogen, C1-C2 alkyl, C1-C2 alkoxy, hydroxy, \u2014CF3, and \u2014NO2.
16. wherein R1 is \u2014CH2-phenyl or \u2014CH2-pyridinyl where the phenyl or pyridinyl rings are each optionally substituted with 2 groups independently selected from halogen, C1-C2 alkyl, C1-C2 alkoxy, hydroxy, and \u2014NO2.
17. A compound according to claim 1, wherein R1 is \u2014CH2-pyridinyl, benzyl, 3,5-difluorobenzyl, or 5-hydroxybenzyl.
18. A compound according to claim 1, wherein RN is \u2014CO\u2014RN-1, wherein RN-1 is as defined above, or RN is \u2014CO\u2014(C1-C10 alkyl), where the C1-C10 alkyl is optionally substituted.
19. A compound according to claim 1, wherein RN is \u2014CO\u2014RN-1, wherein RN-1 is RN-aryl, RN-heteroaryl, or RN-heterocycle, each of which is optionally substituted as indicated above, or RN is \u2014CO\u2014(C1-C10 alkyl), wherein C1-C10 alkyl is optionally substituted as indicated above.
20. A compound according to claim 1, wherein RN is \u2014CO\u2014RN-1, wherein RN-1 is RN-aryl, or RN-heteroaryl, each of which is optionally substituted with 1, 2, or 3 groups independently selected from \u2014OR, \u2014NO2, C1-C6 alkyl, halogen, \u2014C\u2261N, \u2014OCF3, \u2014CF3, \u2014(CH2)0-4\u2014CO\u2014NRN-2RN-3, and \u2014(CH2)0-4\u2014N(RN-2)\u2014SO2-RN-2.