1. A shopping cart for interaction with inventory, comprising:
a holder for receiving at least one acquired item from a plurality of inventory items having inventory RFID tags, the at least one acquired item having been read by an RFID reader; and
a list-making component for creating and maintaining an interim list of the at least one acquired item and for providing a final list for reconciliation, the interim list associating the at least one acquired item with a personal item having a personal RFID tag, the personal RFID tag being read by the RFID reader.
2. The shopping cart of claim 1, wherein the RFID reader is coupled to the holder.
3. The shopping cart of claim 1, wherein the RFID reader is coupled to the list-making component.
4. The shopping cart of claim 1, wherein the RFID reader is coupled to a cell phone.
5. The shopping cart of claim 1, further comprising:
an exit for receiving the final list and receiving an indication of agreement.
6. The shopping cart of claim 1, wherein the holder is virtual and represented on a web page and the list-making component is associated with the web page.
7. The shopping cart of claim 1, wherein the holder is physical and coupled to the list-making component.
8. The shopping cart of claim 1, further comprising a plurality of exits in communication with the list-making component that allow passage upon a valid sale.
9. The shopping cart of claim 8, wherein the exits do not allow passage upon an invalid sale.
10. The shopping cart of claim 8, wherein the exits set an alarm upon an invalid sale.
11. The shopping cart of claim 1, wherein the at least one acquired item is read by the RFID reader when the at least one acquired item is placed in the holder.
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):
wherein,
R1 and R2 are independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C3-7 cycloalkyl and benzyl, or alternatively R1 and R2 taken together with the nitrogen atom to which they are attached form a saturated or partially unsaturated 4- to 7-membered heterocyclyl optionally having one carbon replaced with >O, >S, \u2550N\u2014, >NH or >N(C1-4 alkyl), wherein the heterocyclyl is optionally substituted with 1-3 independently selected C1-6 alkyl substituents;
R3 is H or C1-6 alkyl, optionally substituted with NH2;
n is 2, 3, 4 or 5;
m is 0 or 1;
Y1 is a covalent bond, C1-4 alkane-diyl, or cis or trans C2-4 alkene-diyl, optionally substituted with 1 or 2 independently selected C1-4 alkyl substituents;
R4 is H, C1-4 alkyl or phenyl;
R5 is selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C3-7 cycloalkyl, phenyl, thienyl, benzhydryl and \u2014Y3-Ra, where Y3 is C1-3 alkane-diyl or C2-3 alkene-diyl, and Ra is selected from the group consisting of C3-7 cycloalkyl, phenyl, naphthyl, biphenyl, benzylsulfanyl, benzyloxy, thienyl, furyl, thiazolyl, oxazolyl, imidazolyl, 1H-indol-2-yl, 1H-indol-3-yl and pyridyl;
or alternatively R4 and R5 taken together with the carbon atom to which they are attached form a saturated or partially unsaturated 3- to 7-membered monocyclic carbocyclyl, optionally benzofused;
where R5 is substituted at any stable position except Y3 with 0, 1 or 2 substituents independently selected from the group consisting of hydroxy, sulfanyl, halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 alkylsulfanyl, carboxy, amino and carbamoyl, and Y3 is substituted with 0, 1 or 2 substituents independently selected from the group consisting of fluoro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy and amino; or alternatively R4 and R5 taken together is substituted with 0, 1 or 2 substituents independently selected from the group consisting of hydroxy, halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy and amino;
R6 is H or C1-4 alkyl;
X is selected from the group consisting of >C\u2550O, >C\u2550S, >C\u2550N\u2014CN and >C\u2550CHNO2;
Y2 is a covalent bond or methylene;
R7 is H, halo or C1-4 alkyl;
R8 is selected from the group consisting of H, phenyl, \u2014O-phenyl, \u2014O-tetrahydronaphthyl, \u2014SO0-2-phenyl, thienyl and pyridyl;
or alternatively R7 and R8 taken together with the phenyl to which they are attached form fluorenyl or tetrahydronaphthyl;
where R8, or R7 and R8 taken together, is substituted with 0, 1 or 2 substituents independently selected from the group consisting of hydroxy, cyano, nitro, amino, dimethylamino, halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, \u2014(CO)\u2014C1-4 alkyl and \u2014(SO2)\u2014C1-4 alkyl;
and stereoisomers, solvates, pharmaceutically acceptable salts and polymorphs, thereof.
2. The compound of claim 1 wherein R1 and R2 are independently selected from the group consisting of H, methyl, ethyl, propyl, i-propyl, ethenyl, allyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and benzyl.
3. The compound of claim 1 wherein, optionally substituted, R1 and R2 taken together with the nitrogen atom to which they are attached is selected from the group consisting of 2-pyrrolin-1-yl, 3-pyrrolin-1-yl, pyrrolidin-1-yl, 2-imidazolin-1-yl, imidazolidin-1-yl, 2-pyrazolin-1-yl, pyrazolidin-1-yl, piperidin-1-yl, morpholin-4-yl, thiomorpholin-4-yl and piperazin-1-yl.
4. The compound of claim 1 wherein, optionally substituted, R3 is independently selected from the group consisting of H, methyl, ethyl and propyl.
5. The compound of claim 1 wherein n is 2 or 3.
6. The compound of claim 1 wherein m is 1.
7. The compound of claim 1 wherein, optionally substituted, Y1 is independently selected from the group consisting of a covalent bond, methdiyl, eth-1,2-diyl, prop-1,3-diyl, but-1,4-diyl, cis-ethen-1,2-diyl and trans-ethen-1,2-diyl.
8. The compound of claim 1 wherein R4 is independently selected from the group consisting of H, methyl, ethyl, propyl and phenyl.
9. The compound of claim 1 wherein, optionally substituted, R5 is independently selected from the group consisting of methyl, ethyl, propyl, i-propyl, butyl, t-butyl, i-butyl, ethenyl, allyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, thienyl, benzhydryl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl, naphthylmethyl, biphenylmethyl, benzylsulfanylmethyl, benzyloxymethyl, thienylmethyl, furylmethyl, thiazolylmethyl, oxazolylmethyl, imidazolylmethyl, 1H-indol-2-ylmethyl, 1H-indol-3-ylmethyl, pyridylmethyl and phenylethyl.
10. The compound of claim 1 wherein R4 and R5 taken together with the carbon atom to which they are attached is selected from the group consisting of cyclobutan-1,1-diyl, cyclopentan-1,1-diyl, cyclohexan-1,1-diyl and indan-2,2-diyl.
11. The compound of claim 1 wherein R6 is selected from the group consisting of H, methyl, ethyl and propyl.
12. The compound of claim 1 wherein Y2 is a covalent bond.
13. The compound of claim 1 wherein X is >C\u2550O.
14. The compound of claim 1 wherein X is >C\u2550S.
15. The compound of claim 1 wherein X is >C\u2550N\u2014CN.
16. The compound of claim 1 wherein X is >C\u2550CHNO2.
17. The compound of claim 1 wherein R7 is selected from the group consisting of H, bromo, chloro, fluoro, iodo, methyl, ethyl, propyl, and t-butyl.
18. The compound of claim 1 wherein, optionally substituted, R is selected from the group consisting of phenyl and \u2014O-phenyl.
19. The compound of claim 1 wherein, optionally substituted, R7 and R8 taken together with the phenyl to which they are attached is fluorenyl.
20. The compound of claim 1 selected from the group consisting of:
(S)-2-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(S)-2-{N\u2032-4-(4-Fluoro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(R)-3-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
3-{N\u2032-4-(3,4-Dichloro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
3-{N\u2032-4-(4-Chloro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
3-N\u2032-Methyl-N\u2033-(4-p-tolyloxy-phenyl)-guanidino-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(S)-2-{N\u2032-4-(4-Chloro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
3-{N\u2032-4-(4-Fluoro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(S)-2-{N\u2032-4-(4-Chloro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-N-(2-diisopropylamino-ethyl)-3-phenyl-propionamide;
(R)-2-{N\u2032-4-(4-Chloro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(R)-4-{N\u2032-4-(4-Chloro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-5-phenyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(R)-4-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-5-phenyl-pentanoic acid (2-isopropylamino-ethyl)-amide;
3-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-N-(2-diisopropylamino-ethyl)-3-phenyl-propionamide;
3-N\u2032-(9H-Fluoren-2-yl)-N\u2033-cyano-guanidino-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(R)-4-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-5-phenyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-{N\u2032-4-(4-Chloro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(R)-4-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-5-phenyl-pentanoic acid (2-diethylamino-ethyl)-amide;
(R)-4-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-5-phenyl-pentanoic acid (2-dimethylamino-ethyl)-amide;
(R)-4-{N\u2032-4-(4-Fluoro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-5-phenyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(R)-4-{N\u2032-4-(3,4-Dichloro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-5-phenyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(R)-4-N\u2032-Cyano-N\u2033-(4-p-tolyloxy-phenyl)-guanidino-5-phenyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
3-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(S)-3-{N\u2032-4-(4-Chloro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-4-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-butyramide;
(S)-2-{N\u2032-4-(4-Chloro-phenoxy)-phenyl-N\u2033-cyano-guanidino}-N-(2-dimethylamino-ethyl)-3-phenyl-propionamide;
(S)-3-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-5-methyl-hexanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-3-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-4-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-butyramide;
(S)-4-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-5-phenyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
3-N\u2032-Cyano-N\u2033-(4-phenoxy-phenyl)-guanidino-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(R)-4-N\u2032-Cyano-N\u2033-(4-phenoxy-phenyl)-guanidino-5-phenyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide; and
(R)-2-(N\u2032-Biphenyl-4-yl-N\u2033-cyano-guanidino)-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
and stereoisomers, solvates, pharmaceutically acceptable salts and polymorphs, thereof.
21. The compound of claim 1 selected from the group consisting of:
1-(R)-1-Benzyl-4-(2-pyrrolidin-1-yl-ethylamino)-butyl-3-biphenyl-4-yl-urea;
(S)-2-{3-4-(4-Chloro-phenoxy)-phenyl-ureido}-N-(2-diisopropylamino-ethyl)-3-phenyl-propionamide;
(S)-2-{3-4-(4-Chloro-phenoxy)-phenyl-ureido}-N-(2-dimethylamino-ethyl)-3-phenyl-propionamide;
(R)-3-(3-Biphenyl-4-yl-ureido)-N-(2-pyrrolidin-1-yl-ethyl)-3-p-tolyl-propionamide;
(S)-N-(2-Diisopropylamino-ethyl)-2-3-(4-phenoxy-phenyl)-ureido-3-phenyl-propionamide;
(E)-(S)-4-{3-4-(4-Fluoro-phenoxy)-phenyl-ureido}-5-phenyl-pent-2-enoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-(3-Biphenyl-4-yl-ureido)-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(S)-2-(3-Biphenyl-4-yl-ureido)-N-(3-diethylamino-propyl)-3-phenyl-propionamide;
(S)-2-(3-Biphenyl-4-yl-ureido)-N-(2-isopropylamino-ethyl)-3-phenyl-propionamide;
(R)-3-(3-Biphenyl-4-yl-ureido)-4-methyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-{3-4-(4-Chloro-phenoxy)-phenyl-ureido}-N-(2-methylamino-ethyl)-3-phenyl-propionamide;
(S)-2-(3-Biphenyl-4-yl-ureido)-N-(3-pyrrolidin-1-yl-propyl)-3-thiophen-2-yl-propionamide;
(E)-(S)-4-3-(4-Phenoxy-phenyl)-ureido-5-phenyl-pent-2-enoic acid (2-methylamino-ethyl)-amide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (2-diethylamino-ethyl)-amide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (2-isopropylamino-ethyl)-amide;
(E)-(S)-4-3-(4-Phenoxy-phenyl)-ureido-5-phenyl-pent-2-enoic acid (2-ethylamino-ethyl)-amide;
3-(3-Biphenyl-4-yl-ureido)-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
3-(3-Biphenyl-4-yl-ureido)-3-(4-methoxy-phenyl)-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-(3-chloro-phenyl)-pent-2-enoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pentanoic acid (2-isopropylamino-ethyl)-amide;
(S)-2-{2-4-(4-Chloro-phenoxy)-phenylamino-acetylamino}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(S)-3-{2-4-(4-Chloro-phenoxy)-phenylamino-acetylamino}-4-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-butyramide;
3-(3-Biphenyl-4-yl-ureido)-N-(2-isopropylamino-ethyl)-3-phenyl-propionamide;
(S)-2-(3-Biphenyl-4-yl-ureido)-N-(2-diisopropylamino-ethyl)-3-phenyl-propionamide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (2-propylamino-ethyl)-amide;
(S)-2-{3-4-(4-Fluoro-phenoxy)-phenyl-ureido}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(S)-2-{3-4-(4-Methoxy-phenoxy)-phenyl-ureido}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
2-(3-Biphenyl-4-yl-ureido)-N-(2-dimethylamino-ethyl)-N-methyl-3-phenyl-propionamide;
(R)-2-(3-Biphenyl-4-yl-1-methyl-ureido)-N-(2-dimethylamino-ethyl)-3-phenyl-propionamide;
(S)-2-(3-Biphenyl-4-yl-1-methyl-ureido)-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(S)-3-Phenyl-N-(2-pyrrolidin-1-yl-ethyl)-2-{3-4-(5,6,7,8-tetrahydro-naphthalen-2-yloxy)-phenyl-ureido}-propionamide;
(S)-N-(2-Diisopropylamino-ethyl)-3-phenyl-2-3-(4-thiophen-2-yl-phenyl)-ureido-propionamide;
(S)-2-3-(4-Iodo-phenyl)-ureido-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(S)-3-Biphenyl-4-yl-2-(3-biphenyl-4-yl-ureido)-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
2-3-(4-Phenoxy-phenyl)-ureido-2-propyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-N-(2-Amino-ethyl)-2-(3-biphenyl-4-yl-ureido)-3-cyclohexyl-propionamide;
(S)-2-(3-Biphenyl-4-yl-ureido)-3-phenyl-N-(2-piperazin-1-yl-ethyl)-propionamide;
(S)-N,N-Bis-(3-amino-propyl)-2-(3-biphenyl-4-yl-ureido)-3-phenyl-propionamide;
1-3-(4-Phenoxy-phenyl)-ureido-cyclopentanecarboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-3-(9H-Fluoren-2-yl)-ureido-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(S)-2-3-(4-Phenoxy-phenyl)-ureido-N-(2-pyrrolidin-1-yl-ethyl)-3-thiazol-4-yl-propionamide;
(S)-3,3-Dimethyl-2-3-(4-phenoxy-phenyl)-ureido-N-(3-pyrrolidin-1-yl-propyl)-butyramide;
(S)-2-3-(4-Phenoxy-phenyl)-ureido-3,3-diphenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(R)-3-Benzylsulfanyl-2-3-(4-phenoxy-phenyl)-ureido-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(S)-2-(3-Biphenyl-4-yl-ureido)-3-pyridin-4-yl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(S)-3-Methyl-2-3-(4-phenoxy-phenyl)-ureido-N-(2-pyrrolidin-1-yl-ethyl)-butyramide;
(S)-2-(3-Biphenyl-4-yl-ureido)-2-phenyl-N-(3-pyrrolidin-1-yl-propyl)-acetamide;
(S)-2-(3-Biphenyl-4-yl-ureido)-4-phenyl-N-(3-pyrrolidin-1-yl-propyl)-butyramide;
(S)-3-Naphthalen-2-yl-2-3-(4-phenoxy-phenyl)-ureido-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
2-3-(4-Phenoxy-phenyl)-ureido-2,2-diphenyl-N-(2-pyrrolidin-1-yl-ethyl)-acetamide;
2-(3-Biphenyl-4-yl-ureido)-indan-2-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-{3-4-(4-Chloro-benzenesulfonyl)-phenyl-ureido}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (3-diethylamino-propyl)-amide;
(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pentanoic acid (2-propylamino-ethyl)-amide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-(4-methoxy-phenyl)-pent-2-enoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
3-(3-Biphenyl-4-yl-ureido)-N-(2-diethylamino-ethyl)-3-phenyl-propionamide;
(S)-3-3-(9H-Fluoren-2-yl)-ureido-5-methyl-hexanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
N-(2-Amino-ethyl)-2-(3-biphenyl-4-yl-ureido)-3-phenyl-propionamide;
(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pentanoic acid (2-amino-ethyl)-amide;
(E)-(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (2-amino-ethyl)-amide;
2-(3-Biphenyl-4-yl-ureido)-N-(2-morpholin-4-yl-ethyl)-3-phenyl-propionamide;
(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pentanoic acid (2-amino-ethyl)-amide;
(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pentanoic acid (3-amino-propyl)-amide;
(S)-N-(2-Amino-ethyl)-3-phenyl-2-(3-phenyl-ureido)-propionamide;
(S)-N-(2-Amino-ethyl)-2-3-(4-phenoxy-phenyl)-ureido-3-phenyl-propionamide;
2-(3-Biphenyl-4-yl-ureido)-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
2-(3-Biphenyl-4-yl-ureido)-3-phenyl-N-(2-piperidin-1-yl-ethyl)-propionamide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-{3-4-(4-Chloro-phenoxy)-phenyl-ureido}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(E)-(S)-4-3-(4-Phenoxy-phenyl)-ureido-5-phenyl-pent-2-enoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-3-(4-tert-Butyl-phenyl)-ureido-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
2-(3-Biphenyl-4-yl-ureido)-N-(2-dimethylamino-ethyl)-3-phenyl-propionamide;
1-(3-Biphenyl-4-yl-ureido)-cyclopentanecarboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(R)-4-3-(4-Phenoxy-phenyl)-ureido-5-phenyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-{3-4-(3,4-Dichloro-phenoxy)-phenyl-ureido}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(E)-(S)-4-3-(4-Phenoxy-phenyl)-ureido-5-phenyl-pent-2-enoic acid (2-amino-ethyl)-amide;
(R)-4-3-(4-Phenoxy-phenyl)-ureido-5-phenyl-pentanoic acid (2-amino-ethyl)-amide;
(E)-(S)-4-3-(4-Phenoxy-phenyl)-ureido-5-phenyl-pent-2-enoic acid (3-pyrrolidin-1-yl-propyl)-amide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (3-pyrrolidin-1-yl-propyl)-amide;
(S)-2-3-(4-Phenoxy-phenyl)-ureido-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (2-methylamino-ethyl)-amide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (2-dimethylamino-ethyl)-amide;
(E)-(S)-4-3-(4-Phenoxy-phenyl)-ureido-5-phenyl-pent-2-enoic acid (2-dimethylamino-ethyl)-amide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (3-methylamino-propyl)-amide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (3-dimethylamino-propyl)-amide;
(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pentanoic acid (3-dimethylamino-propyl)-amide;
(Z)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-3-(3-Phenoxy-phenyl)-ureido-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(S)-2-(3-Biphenyl-4-yl-ureido)-N-(2-diethylamino-ethyl)-3-phenyl-propionamide;
2-(3-Biphenyl-4-yl-ureido)-2-propyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pentanoic acid (2-methylamino-ethyl)-amide;
(S)-3-(3-Biphenyl-4-yl-ureido)-4-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-butyramide;
(S)-3-3-(4-Phenoxy-phenyl)-ureido-4-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-butyramide;
(S)-3-(3-Biphenyl-4-yl-ureido)-5-methyl-hexanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-5-Methyl-3-3-(4-phenoxy-phenyl)-ureido-hexanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-3-(2-Phenoxy-phenyl)-ureido-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(S)-3-(3-Biphenyl-4-yl-ureido)-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(R)-3-(3-Biphenyl-4-yl-ureido)-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
N-(2-Amino-ethyl)-3-(3-biphenyl-4-yl-ureido)-3-phenyl-propionamide;
(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pentanoic acid (2-diethylamino-ethyl)-amide;
3-(3-Biphenyl-4-yl-ureido)-N-(2-dimethylamino-ethyl)-3-phenyl-propionamide;
(E)-(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (3-pyrrolidin-1-yl-propyl)-amide;
(S)-N-(2-Dimethylamino-ethyl)-2-3-(4-phenoxy-phenyl)-ureido-3-phenyl-propionamide;
3-(3-Biphenyl-4-yl-ureido)-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(S)-3-(3-Biphenyl-4-yl-ureido)-N-(2-dimethylamino-ethyl)-4-phenyl-butyramide;
(S)-N-(2-Dimethylamino-ethyl)-3-3-(4-phenoxy-phenyl)-ureido-4-phenyl-butyramide;
(S)-2-(3-Biphenyl-4-yl-ureido)-N-(2-pyrrolidin-1-yl-ethyl)-3-thiophen-2-yl-propionamide;
(S)-2-(3-Biphenyl-4-yl-ureido)-3-pyridin-3-yl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
2-(3-Biphenyl-4-yl-ureido)-2,2-diphenyl-N-(2-pyrrolidin-1-yl-ethyl)-acetamide;
3-(3-Biphenyl-4-yl-ureido)-3-(4-chloro-phenyl)-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(R)-4-Methyl-3-3-(4-phenoxy-phenyl)-ureido-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(R)-3-(3-Biphenyl-4-yl-ureido)-4-methyl-pentanoic acid (2-diisopropylamino-ethyl)-amide;
(R)-4-Methyl-3-3-(4-phenoxy-phenyl)-ureido-pentanoic acid (2-diisopropylamino-ethyl)-amide;
(E)-(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (2-diisopropylamino-ethyl)-amide;
(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pentanoic acid (2-diisopropylamino-ethyl)-amide;
(S)-2-(3-Biphenyl-3-yl-ureido)-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(S)-3-(3-Biphenyl-4-yl-ureido)-N-(2-pyrrolidin-1-yl-ethyl)-3-p-tolyl-propionamide;
(E)-(S)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (3-amino-propyl)-amide;
(E)-(R)-4-(3-Biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid (3-amino-propyl)-amide;
1-(S)-1-Benzyl-2-(2-pyrrolidin-1-yl-ethylamino)-ethyl-3-(4-phenoxy-phenyl)-urea; and
1-(S)-1-Benzyl-4-(2-pyrrolidin-1-yl-ethylamino)-butyl-3-biphenyl-4-yl-urea;
and stereoisomers, solvates, pharmaceutically acceptable salts and polymorphs, thereof.
22. The compound of claim 1 selected from the group consisting of:
(S)-2-{3-4-(4-Chloro-phenoxy)-phenyl-thioureido}-3-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide;
(S)-N-(2-Diisopropylamino-ethyl)-2-{3-4-(4-fluoro-phenoxy)-phenyl-thioureido}-3-phenyl-propionamide;
(R)-4-(3-Biphenyl-4-yl-thioureido)-5-phenyl-pentanoic acid (2-pyrrolidin-1-yl-ethyl)-amide;
(S)-2-(3-Biphenyl-4-yl-thioureido)-3-phenyl-N-(3-pyrrolidin-1-yl-propyl)-propionamide;
(S)-2-{3-4-(4-Chloro-phenoxy)-phenyl-thioureido}-N-(2-diisopropylamino-ethyl)-3-phenyl-propionamide; and
(S)-N-(2-Diisopropylamino-ethyl)-3-phenyl-2-3-(4-p-tolyloxy-phenyl)-thioureido-propionamide;
and stereoisomers, solvates, pharmaceutically acceptable salts and polymorphs, thereof.
23. A method for the treatment or prevention of a disease state selected from the group consisting of muscle spasticity, tinnitus, epilepsy and neuropathic pain comprising administering to a mammal in need thereof an effective amount of a compound of formula (I):
wherein,
R1 and R2 are independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C3-7 cycloalkyl and benzyl, or alternatively R1 and R2 taken together with the nitrogen atom to which they are attached form a saturated or partially unsaturated 4- to 7-membered heterocyclyl optionally having one carbon replaced with >O, >S, \u2550N\u2014, >NH or >N(C1-4 alkyl), wherein the heterocyclyl is optionally substituted with 1-3 independently selected C1-6 alkyl substituents;
R3 is H or C1-6 alkyl, optionally substituted with NH2;
n is 2, 3, 4 or 5;
m is 0 or 1;
Y1 is a covalent bond, C1-4 alkane-diyl, or cis or trans C2-4 alkene-diyl, optionally substituted with 1 or 2 independently selected C1-4 alkyl substituents;
R4 is H, C1-4 alkyl or phenyl;
R5 is selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C3-7 cycloalkyl, phenyl, thienyl, benzhydryl and \u2014Y3\u2014Ra, where Y3 is C1-3 alkane-diyl or C2-3 alkene-diyl, and Ra is selected from the group consisting of C3-7 cycloalkyl, phenyl, naphthyl, biphenyl, benzylsulfanyl, benzyloxy, thienyl, furyl, thiazolyl, oxazolyl, imidazolyl, 1H-indol-2-yl, 1H-indol-3-yl and pyridyl;
or alternatively R4 and R5 taken together with the carbon atom to which they are attached form a saturated or partially unsaturated 3- to 7-membered monocyclic carbocyclyl, optionally benzofused;
where R5 is substituted at any stable position except Y3 with 0, 1 or 2 substituents independently selected from the group consisting of hydroxy, sulfanyl, halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 alkylsulfanyl, carboxy, amino and carbamoyl, and Y3 is substituted with 0, 1 or 2 substituents independently selected from the group consisting of fluoro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy and amino; or alternatively R4 and R5 taken together is substituted with 0, 1 or 2 substituents independently selected from the group consisting of hydroxy, halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy and amino;
R6 is H or C1-4 alkyl;
X is selected from the group consisting of >C\u2550O, >C\u2550S, >C\u2550N\u2014CN and >C\u2550CHNO2;
Y2 is a covalent bond or methylene;
R7 is H, halo or C1-4 alkyl;
R8 is selected from the group consisting of H, phenyl, \u2014O-phenyl, \u2014O-tetrahydronaphthyl, \u2014SO0-2-phenyl, thienyl and pyridyl;
or alternatively R7 and R8 taken together with the phenyl to which they are attached form fluorenyl or tetrahydronaphthyl;
where R8, or R7 and R8 taken together, is substituted with 0, 1 or 2 substituents independently selected from the group consisting of hydroxy, cyano, nitro, amino, dimethylamino, halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, \u2014(CO)\u2014C1-4 alkyl and \u2014(SO2)\u2014C1-4 alkyl;
and stereoisomers, solvates, pharmaceutically acceptable salts and polymorphs, thereof.
24. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective dose of a compound of formula (I):
wherein,
R1 and R2 are independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C3-7 cycloalkyl and benzyl, or alternatively R1 and R2 taken together with the nitrogen atom to which they are attached form a saturated or partially unsaturated 4- to 7-membered heterocyclyl optionally having one carbon replaced with >O, >S, \u2550N\u2014, >NH or >N(C1-4 alkyl), wherein the heterocyclyl is optionally substituted with 1-3 independently selected C1-6 alkyl substituents;
R3 is H or C1-6 alkyl, optionally substituted with NH2;
n is 2, 3, 4 or 5;
m is 0 or 1;
Y1 is a covalent bond, C1-4 alkane-diyl, or cis or trans C2-4 alkene-diyl, optionally substituted with 1 or 2 independently selected C1-4 alkyl substituents;
R4 is H, C1-4 alkyl or phenyl;
R5 is selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C3-7 cycloalkyl, phenyl, thienyl, benzhydryl and \u2014Y3\u2014Ra, where Y3 is C1-3 alkane-diyl or C2-3 alkene-diyl, and Ra is selected from the group consisting of C3-7 cycloalkyl, phenyl, naphthyl, biphenyl, benzylsulfanyl, benzyloxy, thienyl, furyl, thiazolyl, oxazolyl, imidazolyl, 1H-indol-2-yl, 1H-indol-3-yl and pyridyl;
or alternatively R4 and R5 taken together with the carbon atom to which they are attached form a saturated or partially unsaturated 3- to 7-membered monocyclic carbocyclyl, optionally benzofused;
where R5 is substituted at any stable position except Y3 with 0, 1 or 2 substituents independently selected from the group consisting of hydroxy, sulfanyl, halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 alkylsulfanyl, carboxy, amino and carbamoyl, and Y3 is substituted with 0, 1 or 2 substituents independently selected from the group consisting of fluoro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy and amino; or alternatively R4 and R5 taken together is substituted with 0, 1 or 2 substituents independently selected from the group consisting of hydroxy, halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy and amino;
R6 is H or C1-4alkyl;
X is selected from the group consisting of >C\u2550O, >C\u2550S, >C\u2550N\u2014CN and >C\u2550CHNO2;
Y2 is a covalent bond or methylene;
R7 is H, halo or C1-4 alkyl;
R8 is selected from the group consisting of H, phenyl, \u2014O-phenyl, \u2014O-tetrahydronaphthyl, \u2014SO0-2-phenyl, thienyl and pyridyl;
or alternatively R7 and R8 taken together with the phenyl to which they are attached form fluorenyl or tetrahydronaphthyl;
where R8, or R7 and R8 taken together, is substituted with 0, 1 or 2 substituents independently selected from the group consisting of hydroxy, cyano, nitro, amino, dimethylamino, halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, \u2014(CO)\u2014C1-4 alkyl and \u2014(SO2)\u2014C1-4 alkyl;
and stereoisomers, solvates, pharmaceutically acceptable salts and polymorphs, thereof.