Author: claimsbot

1. A vehicle transmission comprising:
a main transmission configured to output the number of revolutions per unit time of a power source at a predetermined gear ratio by performing switching between a plurality of speed-changing gear pairs;
a sub-transmission disposed downstream of the main transmission and configured to convert an output of the main transmission selectively at one of two different gear ratios, the sub-transmission being configured to be switched by a manual operation;
main transmission shift position sensing means for sensing a gear position of the main transmission; and
sub-transmission shift position sensing means for sensing a gear position of the sub-transmission,
wherein the main transmission is an automatic transmission which performs gear shifting with gear shift timing according to one of gear shift maps, the one gear shift map being selected in accordance with a throttle opening degree of a vehicle and a vehicle speed,
the sub-transmission is configured to be switched between a drive position and a low position having a larger reduction ratio than the drive position,
the gear shift maps comprise a first gear shift map corresponding to the drive position of the sub-transmission and a second gear shift map corresponding to the low position thereof, and
the vehicle transmission further comprises map switching means for performing switching between the first gear shift map and the second gear shift map in accordance with sensing signals from the sub-transmission shift position sensing means.
2. The vehicle transmission according to claim 1,
wherein each of the first gear shift map and the second gear shift map comprises a shift-up boundary line specifying gear shift timing for upshifting and a shift-down boundary line specifying gear shift timing for downshifting, and
the shift-up boundary line and the shift-down boundary line of the second gear shift maps are set at lower speed positions than those of the first gear shift map.
3. The vehicle transmission according to claim 1, wherein switching between the first map and the second map is carried out after a predetermined time elapses from completion of switching of the sub-transmission.
4. The vehicle transmission according to claim 1, wherein the main transmission comprises a twin clutch for performing switching between adjacent speed-changing gears by alternately engaging and disengaging a first clutch and a second clutch.
5. A vehicle transmission comprising:
a main transmission configured to output rotational drive force generated by a power source at a predetermined gear ratio by selecting a main transmission gear position among a plurality of speed-changing gear pairs, the main transmission being an automatic transmission configured to perform gear shifting according to a gear shift map selected between a first gear shift map and a second gear shift map in accordance with a throttle opening degree and a vehicle speed;
a sub-transmission configured to change rotational speed of the rotational drive force output from the main transmission by manually selecting a sub-transmission gear position between a drive position and a low position having a reduction ratio larger than a reduction ratio of the drive position, the first gear shift map corresponding to the drive position, the second gear shift map corresponding to the low position;
a sub-transmission shift position sensor configured to sense the sub-transmission gear position of the sub-transmission; and
a map switching device configured to perform switching between the first gear shift map and the second gear shift map in accordance with sensing signals from the sub-transmission shift position sensor.
6. The vehicle transmission according to claim 5, further comprising:
a main transmission shift position sensor configured to sense the gear position of the main transmission.
7. The vehicle transmission according to claim 5,
wherein each of the first gear shift map and the second gear shift map comprises a shift-up boundary line specifying gear shift timing for upshifting and a shift-down boundary line specifying gear shift timing for downshifting,
the shift-up boundary line of the second gear shift map is set at lower speed position than the shift-up boundary line of the first gear shift map, and
the shift-down boundary line of the second gear shift map is set at lower speed position than the shift-down boundary line of the first gear shift map.
8. The vehicle transmission according to claim 5, wherein switching between the first gear shift map and the second gear shift map is carried out after a predetermined time elapses from completion of switching of the sub-transmission.
9. The vehicle transmission according to claim 5, wherein the main transmission comprises a twin clutch for performing switching between adjacent speed-changing gears among the plurality of speed-changing gear pairs by alternately engaging and disengaging a first clutch and a second clutch.
10. The vehicle transmission according to claim 7,
wherein each of the first gear shift map and the second gear shift map comprises an additional shift-down boundary line specifying gear shift timing for downshifting involving braking, and
the additional shift-down boundary line of the first gear shift map is set at higher speed position than the shift-down boundary line of the first gear shift map when the throttle opening degree is lower than a predetermined value and the braking is performed,
the additional shift-down boundary line of the second gear shift map is set at higher speed position than the shift-down boundary line of the second gear shift map when the throttle opening degree is lower than a predetermined value and the braking is performed.
11. A vehicle transmission comprising:
a main transmission configured to output rotational drive force generated by a power source at a predetermined gear ratio by selecting a main transmission gear position among a plurality of speed-changing gear pairs, the main transmission being an automatic transmission configured to perform gear shifting according to a gear shift map selected between a first gear shift map and a second gear shift map, the gear shift map being selected in accordance with throttle opening degree and a vehicle speed;
a sub-transmission configured to change rotational speed of the rotational drive force output from the main transmission by manually selecting a sub-transmission gear position between a drive position and a low position having a reduction ratio larger than a reduction ratio of the drive position, the first gear shift map corresponding to the drive position, the second gear shift map corresponding to the low position;
sub-transmission shift position sensing means for sensing the sub-transmission gear position of the sub-transmission; and
map switching means for performing switching between the first gear shift map and the second gear shift map in accordance with sensing signals from the sub-transmission shift position sensing means.

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 pulsed eddy current sensor probe comprising: a sensor array board;
a plurality of sensors arranged on said sensor array board and operable to sense and generate output signals from the transient electromagnetic flux in a part being inspected, each of said sensors having a differential output comprising a positive and a negative output, wherein said sensors are positioned at an edge of said sensor array board, and each of said sensors has an axis of sensitivity that is oriented substantially normal to said edge;
at least one drive coil disposed adjacent to said sensors and operable to transmit transient electromagnetic flux into the part being inspected;
a first multiplexer arranged on said sensor array board and operable to switch between said sensors; and
a second multiplexer arranged on said sensor array board and operable to switch between said sensors,

wherein said first multiplexer is connected to the positive outputs of said sensors, and
wherein said second multiplexer is connected to the negative outputs of said sensors.
2. The pulsed eddy current sensor probe of claim 1, further comprising a connector operable to connect said multiplexers to an external device.
3. The pulsed eddy current sensor probe of claim 2, wherein said connector is disposed on said sensor array board.
4. The pulsed eddy current sensor probe of claim 1, wherein said sensors form a linear array on said sensor array board.
5. The pulsed eddy current sensor probe of claim 4, further comprising a magnetic shielding disposed between said sensors and said drive coil.
6. The pulsed eddy current sensor probe of claim 1, wherein said sensors form a linear array on said sensor array board.
7. The pulsed eddy current sensor probe of claim 6, wherein said sensors comprise giant magnetoresistance (GMR) sensors.
8. The pulsed eddy current sensor probe of claim 7, wherein said drive coil extends around said linear array of GMR sensors and is operable to generate a magnetic flux that is oriented in a direction substantially along the axis of sensitivity of the GMR sensors.
9. The pulsed eddy current sensor probe of claim 8, further comprising a magnetic shielding disposed between said sensors and said drive coil.
10. The pulsed eddy current sensor probe of claim 1, wherein said sensor array board comprises a printed circuit board.
11. A pulsed eddy current sensor probe comprising:
a plurality of sensor array boards;
a plurality of sensors arranged in a linear array on each of said sensor array boards and operable to sense and generate output signals from the transient electromagnetic flux in a part being inspected, each of said sensors having a differential output comprising a positive and a negative output, wherein said sensors are positioned at an edge of each of said sensor array boards to form the respective linear arrays, wherein each of said sensors has an axis of sensitivity that is oriented substantially normal to said edge of the respective sensor array board;
a plurality of drive coils disposed adjacent to said sensors and operable to transmit transient electromagnetic flux into the part being inspected;
a plurality of first multiplexers; and
a plurality of second multiplexers, each of said first and second multiplexers being arranged on a respective one of said sensor array boards and operable to switch between said sensors on the respective sensor array board, wherein each of said first multiplexers is connected to the positive outputs of said sensors on the respective sensor array board,

wherein each of said second multiplexers is connected to the negative outputs of said sensors on the respective sensor array board, and
wherein said sensor array boards are arranged to form a two-dimensional sensor array.
12. The pulsed eddy current sensor probe of claim 11, wherein at least one drive coil is connected to a respective one of each of said sensor array boards.
13. The pulsed eddy current sensor probe of claim 11, further comprising a plurality of connectors, wherein at least one of said connectors is disposed on each of said sensor array boards, and wherein each of said connectors is operable to connect to said first and second multiplexers on the respective one of said sensor array boards.
14. The pulsed eddy current sensor probe of claim 11, wherein each of said drive coils extends around the respective linear array of sensors and is operable to generate a magnetic field that is oriented in a direction substantially along the axis of sensitivity of the sensors.
15. The pulsed eddy current sensor probe of claim 14, wherein said sensors comprise giant magnetoresistance (GMR) sensors.
16. The pulsed eddy current sensor probe of claim 14, further comprising a plurality of magnetic shieldings, each of said magnetic shieldings being disposed between said sensors and the respective one of said drive coils.
17. A pulsed eddy current sensor probe comprising:
a plurality of sensor array boards;
a plurality of sensors arranged in a linear array on each of said sensor array boards and operable to sense and generate output signals from the transient electromagnetic flux in a part being inspected, each of said sensors having a differential output comprising a positive and a negative output;
a plurality of drive coils disposed adjacent to said sensors and operable to transmit transient electromagnetic flux into the part being inspected;
a plurality of first muitiplexers;and
a plurality of second multiplexers, each of said first and second multiplexers being arranged on a respective one of said sensor array boards and operable to switch between said sensors on the respective sensor array board, wherein each of said first multiplexers is connected to the positive outputs of said sensors on the respective sensor array board, wherein each of said second multiplexers is connected to the negative outputs of said sensors on the respective sensor array board,
a motherboard connected to each of said connectors,

wherein said sensor array boards are arranged to form a two-dimensional sensor array.
18. The pulsed eddy current sensor probe of claim 17, further comprising a demultiplexer disposed on said motherboard,
wherein at least one drive coil is connected to a respective one of each of said sensor array boards, and
wherein said demultiplexer is operable to receive a plurality of control signals and a plurality of drive pulses and to selectively drive each of said drive coils in response to the control signals.
19. The pulsed eddy current sensor probe of claim 17, wherein at least one drive coil is connected to a respective one of each of said sensor array boards, said pulsed eddy current sensor probe further comprising an enabling circuit adapted to selectively enable a respective one of said sensor array boards via the respective one of said connectors for driving the respective one of said drive coils and for collecting a plurality of output signals using the sensors arranged in said linear array on the respective sensor array board.
20. The pulsed eddy current sensor probe of claim 19, wherein said enabling circuit comprises a demultiplexer disposed on said motherboard, wherein said demultiplexer is operable to receive a plurality of control signals and a plurality of drive pulses and to selectively drive each of said drive coils in response to the control signals via the respective connector.
21. The pulsed eddy current sensor probe of claim 20, wherein said enabling circuit further comprises a plurality of switches.
22. A method of inspecting a part comprising:
positioning a linear array of sensors adjacent to a surface of the part, wherein each of the sensors has an axis of sensitivity aligned substantially normal to the surface of the part;
generating a magnetic flux that is oriented in a direction substantially along the axis of sensitivity of the sensors to transmit transient electromagnetic flux into the part;
sensing the transient electromagnetic flux in the part being inspected;
generating a differential output signal using one of the sensors, wherein said generation of the magnetic field and said sensing and generating the differential output signal using one of the sensors are repeated for at least a subset of the sensors in the linear array to acquire a plurality of the differential output signals, each of the differential output signals comprising a positive and a negative output;
indexing and storing the differential output signals to indicate the respective sensors used to generate the differential output signals;
generating a calibration curve for each of the sensors;
calculating a plurality of informative parameter values for the differential output signals, each of the informative parameter values being associated with a respective one of the sensors; and
comparing the informative parameter values with the respective calibration curves.
23. The inspection method of claim 22, wherein the linear array of sensors is disposed on a sensor array board, said inspection method further comprising performing on-board multiplexing to switch between the sensors.
24. A method of inspecting a part comprising:
positioning a two dimensional sensor array adjacent to a surface of the part, wherein the two dimensional sensor array comprises a plurality of linear arrays of sensors, wherein each of the linear arrays is disposed on a respective one of a plurality of sensor array boards, and wherein each of the sensors has an axis of sensitivity aligned substantially normal to the surface of the part;
generating a magnetic flux that is oriented in a direction substantially along the axis of sensitivity of the sensors to transmit transient electromagnetic flux into the part;
sensing the transient electromagnetic flux in the part being inspected and generating a differential output signal using one of the sensors, wherein said generation of the magnetic field and said sensing and generating the differential output signal using one of the sensors are repeated for at least a subset of the sensors in respective ones of at least a subset of the linear arrays to acquire a plurality of the differential output signals, each of the differential output signals comprising a positive and a negative output; and
performing on-board multiplexing to switch between the sensors within a respective one of the linear arrays.
25. The inspection method of claim 24, further comprising indexing and storing the differential output signals to indicate the respective sensors used to generate the differential output signals.
26. The inspection method of claim 25, further comprising:
generating a calibration curve for each of the sensors;
calculating a plurality of informative parameter values for the differential output signals, each of the informative parameter values being associated with a respective one of the sensors in the two dimensional sensor array; and
comparing the informative parameter values with the respective calibration curves.
27. The inspection method of claim 24, wherein a drive coil is disposed on each of the sensor array boards, the inspection method further comprising:
enabling a respective one of the sensor array boards;
selectively driving the drive coil on the respective sensor array board to generate the magnetic field for transmitting transient electromagnetic flux into the part; and
collecting the differential output signals using the sensors in the linear array on the respective sensor array board,
wherein the steps of enabling, selectively driving and collecting are repeated for each of the sensor array boards for collecting the differential output signals from the sensors within each of the linear arrays forming the two dimensional sensor array.

1. A method of establishing a first password, consisting of a first character string, for an electronic device having a reduced keyboard for ambiguous or unambiguous entry of characters and a second corresponding password when the first character string is entered ambiguously, the method comprising:
entering said first password into said electronic device using a first key depression sequence wherein said first key depression sequence specifies the first character string unambiguously;
storing the first character string as the first password;
converting the first key depression sequence into a second character string wherein the second character string would result from entry of the first character string on the reduced keyboard ambiguously; and
storing said second character string as the second corresponding password.
2. The method according to claim 1, wherein a multi-tap system is used for the unambiguous entry of characters.
3. The method according to claim 1, wherein said reduced keyboard is a reduced QWERTY keyboard.
4. The method according to claim 1, wherein said handheld electronic device is adapted to selectively employ a software-based text disambiguation function when characters are entered ambiguously.
5. A method of controlling access to a handheld electronic device, said handheld electronic device having a reduced keyboard for ambiguous or unambiguous entry of characters, comprising:
permitting access to said handheld electronic device when a first password, consisting of a first character string, is received by said handheld electronic device; and
permitting access to said handheld electronic device when a second password is received by said handheld electronic device, said second password being received when the first character string is entered into said handheld electronic device ambiguously, wherein said second password is established by entering said first password into said handheld electronic device using a first key depression sequence wherein said a first key depression sequence specifies the first character string unambiguously, converting the first key depression sequence into a second character string wherein the second character string would result from entry of the first character string on the reduced keyboard ambiguously, and storing said second character string as said second password.
6. The method according to claim 5, wherein a multi-tap system is used for the unambiguous entry of characters.
7. The method according to claim 5, wherein said reduced keyboard is a reduced QWERTY keyboard.
8. The method according to claim 5, wherein said handheld electronic device is adapted to selectively employ a software-based text disambiguation function when characters are entered ambiguously.
9. A handheld electronic device, comprising:
a reduced keyboard for ambiguous or unambiguous entry of characters;
a processor; and
a memory storing a plurality of routines executable by said processor, wherein one or more of said routines include instructions for implementing a method of establishing a first password, consisting of a first character string, for said handheld electronic device and a second corresponding password when the first character string is entered ambiguously, the method comprising:
receiving said first password in said handheld electronic device when said first password is entered using a first key depression sequence wherein said first key depression sequence specifies the first character string unambiguously;
storing the first character string as the first password;
converting the first key depression sequence into a second character string wherein the second character string would result from entry of the first character string on the reduced keyboard ambiguously; and
storing said second character string as the second corresponding password.
10. The handheld electronic device according to claim 9, wherein a second one or more of said routines implements a multi-tap system for the unambiguous entry of characters.
11. The handheld electronic device according to claim 9, wherein said reduced keyboard is a reduced QWERTY keyboard.
12. The handheld electronic device according to claim 9, wherein a second one or more of said routines implements a software-based text disambiguation function that may be selectively employed when characters are entered ambiguously.
13. A handheld electronic device, comprising:
a reduced keyboard for ambiguous or unambiguous entry of characters;
a processor; and
a memory storing a plurality of routines executable by said processor, wherein one or more of said routines include instructions for:
permitting access to said handheld electronic device when a first password, consisting of a first character string, is received by said handheld electronic device; and
permitting access to said handheld electronic device when a second password is received by said handheld electronic device, said second password being received when the first character string is entered into said handheld electronic device ambiguously, wherein said second password is established by entering said first password into said handheld electronic device using a first key depression sequence wherein said first key depression sequence specifies the first character string unambiguously, converting the first key depression sequence into a second character string wherein the second character string would result from entry of the first character string on the reduced keyboard ambiguously, and storing said second character string as said second password.
14. The handheld electronic device according to claim 13, wherein a second one or more of said routines implements a multi-tap system for the unambiguous entry of characters.
15. The handheld electronic device according to claim 13, wherein said reduced keyboard is a reduced QWERTY keyboard.
16. The handheld electronic device according to claim 13, wherein a second one or more of said routines implements a software-based text disambiguation function that may be selectively employed when characters are entered ambiguously.

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 formula (I),
or pharmaceutically acceptable salt or prodrug thereof, wherein
X is a member selected from the group consisting of CH2, CHF and CF2;
R is selected from the group consisting of alkylcarbonyl, arylcarbonyl, cyano, heterocyclecarbonyl, R4R5NC(O)\u2014, B(OR6)2, (1,2,3)-dioxoborolane and 4,4,5,5-tetramethyl-(1,2,3)-dioxoborolane;
R1 is selected from the group consisting of alkoxyalkyl, alkyl, alkylcarbonyl, alkenyl, alkynyl, allenyl, arylalkyl, cycloalkyl, cycloalkylalkyl, cyano, haloalkyl, haloalkenyl, heterocyclealkyl, and hydroxyalkyl;
R2 and R3 are independently selected from the group consisting of hydrogen, alkoxyalkyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocycle, heterocyclealkyl, hydroxyalkyl; or
R2 and R3 taken together with the atoms to which they are attached form a mono or bicyclic heterocycle selected from the group consisting of 2-indolinyl, 2-indolyl, 3-isoquinoline, 2-piperazine, 2-piperidine, 2-pyrrolidine, 2-pyrrole, 2-pyridine, 2-quinolinyl, 2-tetrahydroquinolinyl, and 3-tetrahydroisoquinolinyl, wherein said heterocycle may be substituted with 0, 1, 2 or 3 substituents independently selected from alkenyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkyl, alkylcarbonyl, alkylcarbonylalkyl, alkylcarbonyloxy, alkylsulfonyl, alkylthio, alkynyl, aryl, arylalkoxy, arylalkyl, arylcarbonyl, aryloxy, carboxy, carboxyalkyl, cyano, cyanoalkyl, formyl, halogen, haloalkyl, hydroxy, hydroxyalkyl, mercapto, nitro, phenyl, RARBN\u2014, RCRDNC(O)\u2014, and RCRDNS(O)2\u2014;
R4, R5 and R6 are each independently selected from the group consisting of hydrogen, alkyl, and arylalkyl;
RA and RB are each independently selected from the group consisting of alkyl, alkylcarbonyl, alkoxycarbonyl, alkylsulfonyl; or RA and RB taken together with the nitrogen to which they are attached form a ring selected from the group consisting of piperidine, piperazine and morpholine; and
RC and RD are each independently selected from the group consisting of hydrogen and alkyl.
2. The compound according to claim 1, wherein
R is cyano.
3. The compound according to claim 1, wherein
R is cyano; and
R1 is a member selected from the group consisting of alkyl, alkenyl, and alkynyl.
4. The compound according to claim 1, wherein
R is cyano;
R1 is a member selected from the group consisting of alkyl, alkenyl, and alkynyl; and
R2 is a member selected from the group consisting of alkoxyalkyl, alkyl, cycloalkyl, cycloalkylalkyl, arylalkyl, and heterocyclealkyl.
5. The compound according to claim 1, wherein
R is cyano;
R1 is a member selected from the group consisting of alkyl, alkenyl, and alkynyl; and
R2 is a member selected from the group consisting of hydrogen, alkyl, cycloalkyl, and heterocycle; and
R3 is hydrogen.
6. The compounds according to claim 5, that is a member selected from the group consisting of
(2S,5R)-5-ethynyl-1-L-leucylpyrrolidine-2-carbonitrile;
(2S,5R)-1-((2S)-2-amino-2-cyclopentylethanoyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-((2S)-2-amino-2-cyclopentylethanoyl)-5-vinylpyrrolidine-2-carbonitrile;
(2S,5R)-1-((2S)-2-amino-2-cyclohexylethanoyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5S)-5-ethyl-1-L-leucylpyrrolidine-2-carbonitrile;
(2S,5S)-1-((2S)-2-amino-2-cyclohexylethanoyl)-5-ethylpyrrolidine-2-carbonitrile;
(2S,5S)-1-L-leucyl-5-methylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-L-leucylpyrrolidine-2-carbonitrile;
(2S,5R)-1-((2S)-2-amino-2-cyclopentylethanoyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-((2R)-2-amino-2-cyclohexylethanoyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5S)-1-((2S)-2-amino-2-cyclopentylethanoyl)-5-methylpyrrolidine-2-carbonitrile;
(2S,5R)-1-((2S)-2-amino-2-cyclopentylethanoyl)-5-prop-1-ynylpyrrolidine-2-carbonitrile;
(2S,5S)-4,4-difluoro-5-methyl-1-L-valylpyrrolidine-2-carbonitrile;
(2S,5S)-4,4-difluoro-1-L-leucyl-5-methylpyrrolidine-2-carbonitrile;
(2S,5R)-1-((2S)-2-amino-2-cyclohexylethanoyl)-5-vinylpyrrolidine-2-carbonitrile;
(2S,5R)-1-((2R)-2-amino-2-cyclopentylethanoyl)-5-vinylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(3-pyridin-4-yl-L-alanyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-L-leucyl-5-prop-1-ynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(3-methyl-L-valyl)-5-prop-1-ynylpyrrolidine-2-carbonitrile;
(2S,5S)-1-L-isoleucyl-5-methylpyrrolidine-2-carbonitrile;
(2S,5S)-1-(3-cyclopropyl-L-alanyl)-5-methylpyrrolidine-2-carbonitrile;
(2S,5S)-5-methyl-1-L-valylpyrrolidine-2-carbonitrile;
(2S,5S)-5-methyl-1-(4-methyl-L-leucyl)pyrrolidine-2-carbonitrile;
(2S,5S)-1-(3-cyclohexyl-L-alanyl)-5-methylpyrrolidine-2-carbonitrile.
7. The compound according to claim 1, wherein
R is cyano;
R1 is a member selected from the group consisting of alkyl, alkenyl, and alkynyl; and
R2 is hydrogen; and
R3 is cycloalkyl, wherein cycloalkyl is a member selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cycloheptyl, and cyclooctyl.
8. The compound according to claim 7, that is a member selected from the group consisting of
(2S,5R)-1-{N-((1R,2R,4S)-bicyclo(2.2.1)hept-2-yl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-((1R,4S)-bicyclo(2.2.1)hept-2-yl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-1-adamantylglycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-cyclohexylglycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(1-(methoxymethyl)cyclopentyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-((2S)-2-hydroxycyclopentyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-cyclopentylglycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(1-(hydroxymethyl)cyclopentyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1-(hydroxymethyl)cyclopentyl)glycyl}-5-prop-1-ynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-cyclopentylglycyl)-5-prop-1-ynylpyrrolidine-2-carbonitrile;
(2S,5S)-1-(N-cyclopentylglycyl)-5-methylpyrrolidine-2-carbonitrile;
(2S,5S)-1-{N-(1-(hydroxymethyl)cyclopentyl)glycyl}-5-methylpyrrolidine-2-carbonitrile;
(2S,5S)-1-{N-((2R,5S)-hexahydro-2,5-methanopentalen-3a(1H)-yl)glycyl}-5-methylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(1-(1-hydroxy-1-methylethyl)cyclopentyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-((2R,5S)-hexahydro-2,5-methanopentalen-3a(1H)-yl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-cyclopentylglycyl-(N-methyl 1-aminocyclopentanecarboxy)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-cyclopropylglycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-((5R,7S)-3-hydroxy-1-adamantyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-cycloheptylglycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-cyclobutylglycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-cyclobutylglycyl)-5-prop-1-ynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-((2S)-2-hydroxycyclopentyl)glycyl}-5-prop-1-ynylpyrrolidine-2-carbonitrile;
(2S,5S)-5-methyl-1-{N-((1S,2S,3S,5R)-2,6,6-trimethylbicyclo(3.1.1)hept-3-yl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5S)-1-{N-((5R,7S)-3-hydroxy-1-adamantyl)glycyl}-5-methylpyrrolidine-2-carbonitrile;
(1S,3R)-3-({2-(2S,5R)-2-cyano-5-ethynylpyrrolidin-1-yl-2-oxoethyl}amino)-N-(pyridin-2-ylmethyl)cyclopentanecarboxamide;
(1S,3R)-3-({2-(2S,5R)-2-cyano-5-ethynylpyrrolidin-1-yl-2-oxoethyl}amino)-N-quinolin-2-ylcyclopentanecarboxamide; and
methyl (1S,3R)-3-({2-(2S,5R)-2-cyano-5-ethynylpyrrolidin-1-yl-2-oxoethyl}amino)cyclopentanecarboxylate.
9. The compound according to claim 1, wherein
R is cyano,
R1 is a member selected from the group consisting of alkyl, alkenyl, and alkynyl; and
R2 is hydrogen; and
R3 is
R7 is a member selected from the group consisting of hydrogen and alkyl; and
R9 is a member selected from the group consisting of hydrogen, aryl, and heterocycle.
10. The compound according to claim 9, that is a member selected from the group consisting of
(2S,5R)-5-ethynyl-1-(N-(4-trans-hydroxycyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-trans-{(4\u2032-fluoro-5-(trifluoromethyl)-1,1\u2032-biphenyl-2-yl)oxy}cyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-trans(4-(trifluoromethoxy)phenoxy)cyclohexyl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-hydroxy-1-methylcyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(1-methyl-4-trans(pyridin-3-yloxy)cyclohexyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{4-trans((5-chloropyridin-3-yl)oxy)cyclohexyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(4-cyanophenoxy)cyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-trans{(5-(trifluoromethyl)pyridin-2-yl)oxy}cyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-trans(3-pyridin-4-yl-4-(trifluoromethyl)phenoxy)cyclohexyl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(4-trans(pyridin-2-yloxy)cyclohexyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(1-methyl-4-trans(5-cyano-pyridin-2-yloxy)cyclohexyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(4-trans(pyrimidin-2-yloxy)cyclohexyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(4-trans(5-cyano-pyridin-2-yloxy)cyclohexyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-trans(4-(trifluoromethyl)phenoxy)cyclohexyl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-((5-fluoropyridin-3-yl)oxy)-1-methylcyclohexyl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-trans(4-carboxy-phenoxy)cyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-trans(2-(2-oxopyrrolidin-1-yl)-4-(trifluoromethyl)phenoxy)cyclohexyl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(4-cyano-2-methoxyphenoxy)cyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{4-trans((5-chloropyridin-2-yl)oxy)cyclohexyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(1-methyl-4-trans(pyridin-2-yloxy)cyclohexyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-trans((5-fluoropyridin-3-yl)oxy)cyclohexyl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{4-trans((5-bromopyridin-2-yl)oxy)cyclohexyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(4-trans(pyridin-3-yloxy)cyclohexyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-prop-1-ynyl-1-(N-{4-(4-(trifluoromethyl)phenoxy)cyclohexyl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(4-cyano-2-fluorophenoxy)cyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(4-trans(3-fluorophenoxy)-1-methylcyclohexyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(3-cyanophenoxy)cyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(1-methyl-4-{(5-(trifluoromethyl)pyridin-2-yl)oxy}cyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{4-trans((5-chloropyridin-2-yl)oxy)cyclohexyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-trans{(4\u2032-fluoro-2-(trifluoromethyl)-1,1\u2032-biphenyl-4-yl)oxy}cyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-trans{(4\u2032-fluoro-6-(trifluoromethyl)-1,1\u2032-biphenyl-3-yl)oxy}cyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{4-(3-cyano-4-trans(trifluoromethyl)phenoxy)cyclohexyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(3-bromophenoxy)cyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(4-cyano-3-fluorophenoxy)cyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{4-(2-cyano-4-trans(trifluoromethyl)phenoxy)cyclohexyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(3-cyanophenoxy)-1-methylcyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(4-chlorophenoxy)cyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-trans{(6-methyl-4-(trifluoromethyl)pyridin-2-yl)oxy}cyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{4-trans(2-cyano-3-(trifluoromethyl)phenoxy)cyclohexyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-trans(4-pyridin-4-yl-3-(trifluoromethyl)phenoxy)cyclohexyl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{4-trans(3-cyano-5-(trifluoromethyl)phenoxy)cyclohexyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(4-(4-fluorophenoxy)-1-methylcyclohexyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(4-(3-fluorophenoxy)-1-methylcyclohexyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(1-methyl-4-{(5-(trifluoromethyl)pyridin-2-yl)oxy}cyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-trans(3-(trifluoromethyl)phenoxy)cyclohexyl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{4-trans((3-bromopyridin-2-yl)oxy)cyclohexyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-trans{(4-(trifluoromethyl)pyridin-2-yl)oxy}cyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{4-trans((5-chloropyridin-2-yl)oxy)-1-methylcyclohexyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(3-cyanophenoxy)-1-methylcyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-trans(2-carboxy-4-(trifluoromethyl)phenoxy)cyclohexyl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(3-chlorophenoxy)cyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(1-methyl-4-trans{(5-(trifluoromethyl)pyridin-2-yl)oxy}cyclohexyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(4-trans(4-bromophenoxy)cyclohexyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-(4-trans hydroxycyclohexyl)glycyl)-5-prop-1-ynylpyrrolidine-2-carbonitrile;
(2S,5S)-1-(N-(4-trans hydroxycyclohexyl)glycyl)-5-methylpyrrolidine-2-carbonitrile; and
6-{4-({2-(2S,5R)-2-cyano-5-ethynylpyrrolidin-1-yl-2-oxoethyl}amino)-4-methylcyclohexyloxy}-N,N-dimethylnicotinamide.
11. The compound according to claim 1, wherein
R is cyano;
R1 is a member selected from the group consisting of alkyl, alkenyl, and alkynyl;
R2 is hydrogen;
R3 is alkyl; wherein the alkyl group of R3 is optionally substituted with a member of the group consisting of alkoxy, alkoxycarbonyl, alkoxycarbonylNRa, alkylNRa, carboxy, and hydroxy; and
Ra is a member selected from the group consisting of hydrogen and alkyl.
12. The compound according to claim 11, that is selected from the group consisting of
(2S,5R)-5-ethynyl-1-(N-(1,1,3,3-tetramethylbutyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-(tert-butyl)glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-(1,1-dimethylpropyl)glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(3-(methylamino)propyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-(4-tert-butoxycarbonylbutyl)glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(3-hydroxy-2,2-dimethylpropyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(3-(N-tert-butoxycarbonyl-N-methylamino)propyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-carboxybutyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(3-isopropoxypropyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5S)-1-(N-isopropylglycyl)-5-methylpyrrolidine-2-carbonitrile;
(2S,5S)-1-(N-(tert-butyl)glycyl)-5-methylpyrrolidine-2-carbonitrile; and
(2R,5S)-1-(tert-butylamino)acetylpyrrolidine-2,5-dicarbonitrile.
13. The compound according to claim 1, wherein
R is cyano;
R1 is a member selected from the group consisting of alkyl, alkenyl, and alkynyl; and
R2 is hydrogen; and
R3 is a member selected from the group consisting of aryl and heterocycle; wherein said heterocycle is a member selected from the group consisting of azetidinyl, azepanyl, aziridinyl, diazepinyl, 1,3-dioxolanyl, dioxanyl, dithianyl, furyl, imidazolyl, imidazolinyl, imidazolidinyl, isothiazolyl, isothiazolinyl, isothiazolidinyl, isoxazolyl, isoxazolinyl, isoxazolidinyl, morpholinyl, oxadiazolyl, oxadiazolinyl, oxadiazolidinyl, oxazolyl, oxazolinyl, oxazolidinyl, piperazinyl, pyranyl, pyrazinyl, pyrazolyl, pyrazolinyl, pyrazolidinyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothienyl, tetrazinyl, tetrazolyl, thiadiazolyl, thiadiazolinyl, thiadiazolidinyl, thiazolyl, thiazolinyl, thiazolidinyl, thienyl, thiomorpholinyl, 1,1-dioxidothiomorpholinyl(thiomorpholine sulfone), thiopyranyl, triazinyl, triazolyl, and trithianyl.
14. The compound according to claim 13, that is a member selected from the group consisting of
(2S,5R)-5-ethynyl-1-(N-tetrahydro-2H-pyran-4-ylglycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-tetrahydrofuran-3-ylglycyl)pyrrolidine-2-carbonitrile; and
(2S,5S)-1-(N-2,3-dihydro-1H-inden-1-ylglycyl)-5-methylpyrrolidine-2-carbonitrile.
15. The compound according to claim 1, wherein
R is cyano;
R1 is a member selected from the group consisting of alkyl, alkenyl, and alkynyl; and
R2 is hydrogen; and
R3 is a member selected from the group consisting of arylalkyl and heterocyclealkyl.
16. The compound according to claim 15, that is a member selected from the group of
(2S,5R)-5-ethynyl-1-{N-(2-(4-fluorophenyl)-1,1-dimethylethyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5S)-1-{N-(2-(3,4-dimethoxyphenyl)ethyl)glycyl}-5-methylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(tetrahydrofuran-2-ylmethyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(pyridin-2-ylmethyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(2-pyridin-4-ylethyl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-((1-tert-butoxycarbonylpiperidin-4-yl)methyl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-iodobenzyl)glycyl)pyrrolidine-2-carbonitrile.
17. The compound according to claim 1, wherein
R is cyano,
R1 is a member selected from the group consisting of alkyl, alkenyl, and alkynyl;
R2 is hydrogen;
R3 is
R7 is a member selected from the group consisting of hydrogen, alkyl and alkoxyalkyl; and
R8 is a member selected from the group consisting of hydrogen, alkylcarbonyl, aryl and heterocycle.
18. The compound according to claim 17, that is a member selected from the group consisting of
(2S,5R)-5-ethynyl-1-(N-(4-methyl-1-pyridin-2-ylpiperidin-4-yl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-methyl-1-(3-cyano-pyridin-2-yl)piperidin-4-yl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(1-(3-cyano-pyridin-3-yl)piperidin-4-yl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-{N-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-methyl-1-(5-(trifluoromethyl)pyridin-2-yl)piperidin-4-yl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1-(5-chloropyridin-2-yl)-4-methylpiperidin-4-yl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(1-pyridin-2-ylpiperidin-4-yl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-methyl-1-(4-(trifluoromethyl)pyrimidin-2-yl)piperidin-4-yl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-methyl-1-(5-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(4-methyl-1-(5-cyano-pyridin-3-yl)piperidin-4-yl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(1-tert-butoxycarbonyl-piperidin-4-yl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(1-5-cyano-pyridin-2-ylpiperidin-4-yl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1-(3-cyanophenyl)-4-methylpiperidin-4-yl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-{4-methyl-1-(4-(trifluoromethyl)pyridin-2-yl)piperidin-4-yl}glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-piperidin-4-ylglycyl)pyrrolidine-2-carbonitrile; and
(2S,5R)-5-ethynyl-1-({4-methyl-1-(5-nitropyridin-2-yl)piperidin-4-ylamino}acetyl)pyrrolidine-2-carbonitrile; and
(2S,5R)-5-ethynyl-1-({4-methyl-1-5-(methylsulfonyl)pyridin-2-ylpiperidin-4-yl}amino)acetylpyrrolidine-2-carbonitrile.
19. The compound according to claim 1, wherein
R is cyano;
R1 is selected from the group consisting of alkyl, alkenyl, and alkynyl; and
R2 is hydrogen; and
R3 is
R7 is a member selected from the group consisting of hydrogen, alkyl and alkoxyalkyl; and
R8 is a member selected from the group consisting of arylcarbonyl and heterocyclecarbonyl.
20. The compound according to claim 19, that is a member selected from the group consisting of
(2S,5R)-5-ethynyl-1-{N-(4-methyl-1-(4-methoxycarbonylbenzoyl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1-(4-chlorobenzoyl)piperidin-4-yl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-5-ethynyl-1-(N-(1-isonicotinoyl-4-methylpiperidin-4-yl)glycyl)pyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1-(4-chlorobenzoyl)-4-methylpiperidin-4-yl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1-(4-cyanobenzoyl)-4-methylpiperidin-4-yl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1-(4-bromobenzoyl)-4-methylpiperidin-4-yl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile.
21. The compound according to claim 1, wherein
R is cyano;
R1 is a member selected from the group consisting of alkyl, alkenyl, alkynyl, allenyl and cycloalkyl; and
R2 is hydrogen; and
R3 is a member selected from the group consisting of aryl-O-alkyl-, aryl-NH-alkyl-, heterocycle-O-alkyl- and heterocycle-NH-alkyl-.
22. The compound according to claim 21, that is a member selected from the group consisting of
(2S,5R)-1-{N-(1,1-dimethyl-2-(5-cyano-pyridin-2-yloxy)ethyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1,1-dimethyl-2-(quinolin-4-ylamino)ethyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(2-(1,3-benzothiazol-2-ylamino)-1,1-dimethylethyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{1,1-dimethyl-2-((3-cyano-6-methylpyridin-2-yl)amino)ethyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-(1,1-dimethyl-2-{(5-(trifluoromethyl)pyridin-2-yl)oxy}ethyl)glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-{1,1-dimethyl-2-((3-cyano-6-methylpyridin-2-yl)oxy)ethyl}glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1,1-dimethyl-2-(3-cyanopyridin-2-ylamino)ethyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-(1,1-dimethyl-2-{(4-(trifluoromethyl)pyrimidin-2-yl)amino}ethyl)glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1,1-dimethyl-2-(5-methoxycarbonylpyridin-2-ylamino)ethyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(2-(2-cyano-5-fluorophenoxy)-1,1-dimethylethyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-(2-{(3-chloro-5-(trifluoromethyl)pyridin-2-yl)amino}ethyl)glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-{N-(1,1-dimethyl-2-(5-cyano-pyridin-2-ylamino)ethyl)glycyl}-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5R)-1-(N-(2-(4-carboxy-anilino)-1,1-dimethylethyl)glycyl)-5-ethynylpyrrolidine-2-carbonitrile;
(2S,5S)-5-methyl-1-{N-(2-(5-cyano-pyridin-2-ylamino)ethyl)glycyl}pyrrolidine-2-carbonitrile.
23. The compound according to claim 1, wherein
R is cyano;
R1 is selected from the group consisting of alkyl, alkenyl, and alkynyl; and
R2 and R3 taken together with the atoms they are attached form a mono or bicyclic heterocycle selected from the group consisting of 3-isoquinoline, 2-pyrrolidinyl, 2-quinolinyl, 2-tetrahydroquinolinyl, and 3-tetrahydroisoquinolinyl.
24. The compound according to claim 23, that is a member selected from the group consisting of
(2S,5R)-5-ethynyl-1-((3S)-1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl)pyrrolidine-2-carbonitrile;
(2S,5S)-4,4-difluoro-5-methyl-1-((5S)-5-methyl-L-prolyl)pyrrolidine-2-carbonitrile;
(2S,5S)-5-methyl-1-((3S)-1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl)pyrrolidine-2-carbonitrile;
(2S,5S)-5-methyl-1-L-prolylpyrrolidine-2-carbonitrile;
(2S,5S)-5-methyl-1-((5S)-5-methyl-L-prolyl)pyrrolidine-2-carbonitrile.
25. A method of treating diabetes, comprising administration of a therapeutically effective amount of a compound of formula (I).
26. A method of treating type II diabetes, comprising administration of a therapeutically effective amount of a compound of formula (I).
27. A method of treating hyperglycemia, comprising administration of a therapeutically effective amount of a compound of formula (I).
28. A method of treating Syndrome X, comprising administration of a therapeutically effective amount of a compound of formula (I).
29. A method of treating hyperisulinemia, comprising administration of a therapeutically effective amount of a compound of formula (I).
30. A method of treating obesity, comprising administration of a therapeutically effective amount of a compound of formula (I).