US 2015/0031685 A1Published application

Substituted heterocyclic acetamides as kappa opioid receptor (kor) agonists

AssigneeDr. Reeddy's Laboratories Ltd.

InventorsPradip Kumar Sasmal, Chintakunta Vamseekrishna, Vijay Potluri, Ashok Tehim, Yonghua Gai, Hang Zhang

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Abstract

The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.

Claims32

Dependent claims

A compound of formula (I),

stereoisomers thereof or pharmaceutically acceptable salts thereof;
wherein,
R1 represents hydrogen, alkyl, haloalkyl or —(CH2)m-cycloalkyl;
R2 represents (1) cycloalkyl (2) an group selected from heterocyclyl, heteroaryl, or aryl, wherein such group is optionally substituted with 1 to 3 substituents selected independently from cyano, hydroxyl, alkyl, alkynyl, alkoxy, halogen, haloalkyl, haloalkoxy, —COORa, —CONRaRf, —O—(CH2)n—R7 or R11;
R3 is an optionally substituted group selected from
Optional substituent on R3, in each occurrence, independently selected from halogen, alkyl or haloalkyl;
R4 is selected from hydrogen, hydroxyl, halogen, alkyl, alkoxy, or haloalkyl;
R5 and R6, each are independently selected from hydrogen or alkyl;
R7 is selected from cyano, tetrazolyl, —COORa, —CONRaRf or
R8, in each occurrence, is independently selected from hydrogen, halogen, alkyl or —(CH2)q—R9;
R9is —COORa or
R10 is selected from hydrogen, cyano, —COORa, —CONRaRf or tetrazolyl;
R11 is selected from (1) (C3-C6)cycloalkyl, benzyl,
or (2) 5-6 membered heteroaryl optionally substituted with 1 to 2 substituents selected independently from alkyl, haloalkyl, haloalkoxy or —(CH2)m—(C3-C6)cycloalkyl;
Ra and Rb, in each occurrence, independently selected from hydrogen, alkyl, heterocyclyl or heteroaryl;
Rb, in each occurrence, independently selected from hydrogen, alkyl or alkoxy,
Ra, in each occurrence, independently selected from hydrogen, alkyl, haloalkyl or —S(O)2-alkyl;
Rf in each occurrence, independently selected from hydrogen or alkyl;
m is selected from 0, 1, 2, 3 or 4;
n and q, each independently selected from 1 or 2;
provided that when R2 is phenyl optionally substituted with alkyl, alkoxy or halogen, R1 is alkyl and one of R5 and R6 represents hydrogen, then R3 does not represent the following rings
wherein Ri, in each occurrence, represents hydrogen or alkyl.

19 more elements

A compound selected from

N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
N-[(1S)-2-[(3S)-3-hydroxypyrrolidin-1-yl]-1-phenylethyl]-2-(3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)acetamide,
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamide;
(S)-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)-N-methylacetamide;
N-((S)-1-(3-cyanophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-methylacetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)acetamide;
2-(1,1-dioxido-3-oxo-2,3-dihydrobenzo[d]isothiazol-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methylacetamide;
2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethyl)phenyl)ethyl)-N-methylacetamide;
5-(2-(((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)(methyl)amino)-2-oxoethyl)-1,3-dihydrobenzo[c]isothiazol-1-ium 2,2-dioxide 2,2,2-trifiuoroacetate;
N-((S)-1-(3-(difluoromethoxy)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-methylacetamide;
2-(3,3-difluoro-2-oxoindolin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methylacetamide;
2-(3,3-difluoro-2-oxoindolin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)acetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-ethyl-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)acetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-methoxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)-N-methylacetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)-N-(2,2,2-trifluoroethyl)acetamide 2,2,2-trifluoroacetate,
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-(2-((S)-3-hydroxypyrrolidin-1-yl)-1-(tetrahydro-2H-pyran-4-yl)ethyl)-N-methylacetamide-2,2,2-trifluoroacetate;
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamido)ethyl)benzoic acid;
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamdo)ethyl)benzamide;
(S)-2-(3-benzyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-(1-(3-hydroxyphenyl)-2-(pyrrolidin-1-yl)ethyl)acetamide;
N-((S)-1-(3-(1H-tetrazol-5-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(1-methyl-2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)acetamide;
2-(3-((S)-1-(2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-methylacetamido)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)phenoxy)acetic acid;
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl)benzoic acid;
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl)benzamide;
N-((S)-1-(3-cyanophenyl)-2-((S)-3-fluoropyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
N-((S)-1-(3-(2-amino-2-oxoethoxy)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(2-(methylsulfonamido)-2-oxoethoxy)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
3-((S)-2-((S)-3-fluoropyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl)benzoic acid;
2-(3-((S)-2-((S)-3-fluoropyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl)phenoxy)acetic acid;
N-((S)-1-(3-(2-amino-2-oxoethoxy)phenyl)-2-((S)-3-fluoropyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamido)ethyl)benzoic acid,
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)acetamido)ethyl)benzamide;
N-((S)-1-(3-ethynylphenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(thiazol-2-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
N-((S)-1-(3-(but-1-yn-1-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-methylacetamide;
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl)-N-(2,2,2-trifluoroethyl)benazmide;
N,N-diethyl-3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl)benzamide;
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamido)ethyl)-N,N-dimethylbenzamide 2,2,2-trifluoroacetate;
N-((S)-1-(3-(2-(diethylamino)-2-oxoethoxy)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
N-((S)-1-(3-(2-(diethylamino)-2-oxoethoxy)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide;
N-((S)-1-(3-fluoro-5-(thiazol-2-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(2-methyl-2H-tetrazol-5-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-2-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
(S)-2-(3-(3-cyanobenzyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
(S)-N-methyl-2-(2-oxo-1,2-dihydroquinolin-6-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2-(2-oxo-1,2-dihydroquinolin-6-yl)acetamide;
(S)-N-methyl-2-(2-oxo-1,2-dihydroquinolin-7-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
(S)-N-methyl-2-(3-methyl-2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-5-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
N-((S)-2-((R)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-2-(2-oxo-1,2-dihydroquinolin-6-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2-(2-oxo-1,2-dihydroquinolin-7-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-2-dimethyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)propanamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-2-(2-oxo-1,2-dihydroquinolin-7-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-2-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)propanamide;
(S)-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
(S)-2-(3-benzyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-(1-(3-(4-methoxybenzyloxy)phenyl)-2-(pyrrolidin-1-yl)ethyl)acetamide;
2-(3-(4-cyanobenzyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-2-(2-oxoindolin-6-yl)acetamide;
(S)-2-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
N-(1-(1-benzyl-1H-pyrazol-4 yl)-2-(pyrrolidin-1-yl)ethyl)-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
(S)-t-butyl-2-(3-(1-(2-(3-benzyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamido)-2-(pyrrolidin-1-yl)ethyl)phenoxy)acetate;
(S)-2-(3-benzyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-(1-(3-(benzyloxy)phenyl)-2-(pyrrolidin-1-yl) ethyl)-N-methylacetamide;
N-((S)-1-cyclohexyl-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
2-(3-(3-cyanobenzyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methylacetamide;
N-((S)-1-cyclohexyl-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
(S)-tert-butyl-2-(3-(1-(2-(3-benzyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-methyl acetamido)-2-(pyrrolidin-1-yl)ethyl)phenoxy)acetate;
N-((S)-1-cyclohexyl-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(2-oxoindolin-6-yl)acetamide;
N-((S)-1-cyclohexyl-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
(S)-N-(1-(3-cyanophenyl)-2-(pyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
2-(3-(3-cyanobenzyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)acetamide;
N-((S)-1-(3-cyanophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
(S)-tert-butyl 2-(3-(2-(3-hydroxypyrrolidin-1-yl)-1-(2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamido)ethyl)phenoxy)acetate;
2-(3-(4-cyanobenzyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methylacetamide;
N-(1-(3-(cyanomethoxy)phenyl)-2-(3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
tert-butyl 2-(3-((S)-2-((R)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamido)ethyl)phenoxy)acetate;
N-((S)-1-(3-cyanophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
N-((S)-1-(3-(1H-tetrazol-5-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-methylacetamide;
2-(3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(1-methyl-2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)acetamido)ethyl)phenoxy)acetic acid;
(S)-methyl 3-((2-oxo-5-(2-oxo-2-(1-phenyl-2-(pyrrolidin-1-yl)ethylamino)ethyl)benzo[d]oxazol-3 (2H)-yl)methyl)benzoate;
(S)-tert-butyl 2-(2-oxo-5-(2-oxo-2-(1-phenyl-2-(pyrrolidin-1-yl)ethylamino)ethyl)benzo[d]oxazol-3(2H)-yl)acetate;
(S)-2-(2-oxo-5-(2-oxo-2-(1-phenyl-2-(pyrrolidin-1-yl)ethylamino)ethyl)benzo[d]oxazol-3(2H)-yl)acetic acid hydrochloride;
(S)-N-(1-(3-hydroxyphenyl)-2-(pyrrolidin-1-yl)ethyl)-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
(S)-2-(3-(1-(2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamido)-2-(pyrrolidin-1-yl)ethyl)phenoxy)acetic acid hydrochloride;
2-(5-(2-(((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)(methyl)amino)-2-oxoethyl)-2-oxobenzo[d]oxazol-3(2H)-yl)acetic acid;
2-(3-(1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)-2-(pyrrolidin-1-yl)ethyl)phenoxy)acetic acid hydrochloride;
3-((5-(2-(((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)(methyl)amino)-2-oxoethyl)-2-oxobenzo[d]oxazol-3(2H)-yl)methyl)benzamide;
(S)-2-(3-benzyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-(1-(3-hydroxyphenyl)-2-(pyrrolidin-1-yl)ethyl)-N-methylacetamide;
(R)-2-(3-(1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamido)-2-(pyrrolidin-1-yl)ethyl)phenoxy)acetic acid;
(S)-3-((2-oxo-5-(2-oxo-2-(1-phenyl-2-(pyrrolidin-1-yl)ethylamino)ethyl)benzo[d]oxazol-3(2H)-yl)methyl)benzamide;
2-(3-(1-(2-(2-oxoindolin-6-yl)acetamido)-2-(pyrrolidin-1-yl)ethyl)phenoxy)acetic acid;
(S)-N-(1-(3-(2H-tetrazol-5-yl)phenyl)-2-(pyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
(S)-2-(3-(2-(3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamido)ethyl)phenoxy)acetic acid triflouroacetate;
(S)-2-(3-(2-(3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl) phenoxy)acetic acid hydrochloride;
2-(3-((S)-2-((R)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamido)ethyl)phenoxy)acetic acid;
2-(5-(2-(((S)-1-cyclohexyl-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)(methyl)amino)-2-oxoethyl)-2-oxobenzo[d]oxazol-3(2H)-yl)acetic acid;
Methyl 4((5-(2-(((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenyethyl)(methyl)amino)-2-oxoethyl)-2-oxobenzo[d]oxazol-3(2H)-yl)methyl)benzoate;
N-((S)-1-(3-(2H-tetrazol-5-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
(S)-2-(3-(2-(3-hydroxypyrrolidin-1-yl)-1-(2-(2-oxoindolin-6-yl)acetamido) ethyl)phenoxy)acetic acid hydrochloride;
(S)-2-(3-(2-(3-hydroxypyrrolidin-1-yl)-1-(2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamido)ethyl)phenoxy)acetic acid;
2-(3-(3-(2H-tetrazol-5-yl)benzyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)acetamide;
2-(3-(3-(2H-tetrazol-5-yl)benzyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methylacetamide;
2-(3-(4-(1H-tetrazol-5-yl)benzyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methylacetamide;
(R)-N-(1-(3-((2H-tetrazol-5-yl)methoxy)phenyl)-2-(3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
2-(3-(4 (1H-tetrazol-5-yl)benzyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)acetamide;
N-((S)-1-(3-(2H-tetrazol-5-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
N-((S)-1-(3-cyanophenyl)-2-((S)-3-fluoropyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
N-((S)-1-(3-(2H-tetrazol-5-yl)phenyl)-2-((S)-3-fluoropyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
N-((S)-1-(3-(2H-tetrazol-5-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
N-((S)-1-(3-(2H-tetrazol-5-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(1-methyl-2-oxoindolin-6-yl)acetamide;
(R)-N-(1-(3-((2H-tetrazol-5-yl)methoxy)phenyl)-2-(3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide;
N-((S)-1-(3-(2H-tetrazol-5-yl)phenyl)-2-((S)-3-fluoropyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide;
(S)-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
(S)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methylacetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-2-(2-thioxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2-(2-thioxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methylacetamide;
(S)-2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)acetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethyl)phenyl)ethyl)-N-methylacetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-1-(3-fluorophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methylacetamide;
N-((S)-1-cyclohexyl-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-methylacetamide
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-methoxyphenyl)ethyl)-N-methylacetamide;
(S)-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)acetamide;
(S)-N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-(1-phenyl-2-(pyrrolidin-1-yl)ethyl)acetamide;
N-(2-((S)-3-hydroxypyrrolidin-1-yl)-1-(tetrahydro-2H-pyran4-yl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-methoxyphenyl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethyl)phenyl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)acetamide;
N-((S)-1-(3-fluorophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)acetamide;
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)acetamide;
2-(1-benzyl-2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methylacetamide;
2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methylacetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)-N-propylacetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)-N-isopropylacetamide;
N-cyclopropyl-2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)acetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)-N-isobutylacetamide;
N-(cyclopropylmethyl)-2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)acetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(4-(trifluoromethoxy)phenyl)ethyl)-N-methylacetamide;
2-(2,2-dimethyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)-N-methylacetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(2,2,2-trifluoroethoxy)phenyl)ethyl)-N-methylacetamide;
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(m-tolyl)ethyl)-N-methylacetamide
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-1-(4-fluoro-3-(trifluoromethoxy)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methylacetamide
N-((S)-1-(3,5-dimethylphenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-methylacetamide
2-(2,2-dimethyl-1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(trifluoromethoxy)phenyl)ethyl)-N-methylacetamide
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-1-(3-fluoro-5-(2,2,2-trifluoroethoxy)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methylacetamide
N-((S)-1-(3-cyclopropylphenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-methylacetamide
N-((S)-1-(3-cyanophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide
N-((S)-1-(3-cyanophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-oxo-3,4- dihydro-2 H-benzo[b][1,4]thiazin-6-yl)acetamide
N-((S)-1-(3-cyanophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydro-2 H-benzo[b][1,4]oxazin-6-yl)acetamide
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)acetamido)ethyl)benzoic acid
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)acetamido)ethyl)benzoic acid
N-((S)-1-(3-cyanophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-2-(2-oxoindolin-5-yl)acetamide
N-((S)-1-(3-cyanophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamide
2-(3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl)phenoxy)acetic acid
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamido)ethyl)benzamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2-(2-oxoindolin-5-yl)acetamide
N-((S)-2-((S)-3-fluoropyrrolidin-1-yl)-1-(3-(2-(methylsulfonamido)-2-oxoethoxy)phenyl) ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-1-(3-cyanophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamide
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamido)ethyl)benzamide
3-((S)-2-((S)-3-fluoropyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl)benzamide
2-(3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamido)ethyl)phenoxy)acetic acid
2-(3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)acetamido)ethyl)phenoxy)acetic acid
N-((S)-1-(3-(2-amino-2-oxoethoxy)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(1,1-dioxido-3-oxo-3,4 dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-methylacetamide
2-(3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-5-yl)acetamido)ethyl)phenoxy)acetic acid
N-((S)-1-(3-(2-amino-2-oxoethoxy)phenyl)-2-((S)-3-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide
2-(3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4 dihydroquinoxalin-6-yl)acetamido)ethyl)phenoxy)acetic acid
2-(3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4-dihydro2H-benzo[b][1,4]thiazin-6-yl)acetamido)ethyl)phenoxy)acetic acid
N-((S)-1-(3-(2-amino-2-oxoethoxy)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)acetamide
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(2-(methylsulfonamido)-2-oxoethoxy)phenyl)ethyl)-N-methylacetamide
N-((S)-1-(3-(2-amino-2-oxoethoxy)phenyl)-2-((S)-3-hydroxypyrrolidin)ethyl)-N-methyl-2-(3-oxo-3,4 dihydro-2H-benzo[b][1,4]thiazin-6-yl)acetamide
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)acetamido)ethyl)benzoic acid
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl)-N-(methylsulfonyl)benzamide
N-((S)-1-(3-ethynylphenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-1-(3-ethynylphenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl)ethyl)-N-methylacetamide
2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-((S)-1-(3-ethynylphenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methylacetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide
N-((S)-1-(3-(1,2,4-oxadiazol-3-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide 2,2,2-trifluoroacetate
N-((S)-1-(3-(1,2,4-oxadiazol-3-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-methylacetamide
2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)-N-methylacetamide 2,2,2-trifluoroacetate
N,N-diethyl-3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dhydrobenzo[d]thiazol-5-yl)acetamido)ethyl)benzamide
N-((S)-1-(3-(1,2,4-oxadiazol-3-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide 2,2,2-trifluoroacetate
N-((S)-1-(3-(1,2,4-oxadiazol-3-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamide 2,2,2-trifluoroacetate
N-((S)-1-(3-(1H-imidazol-2-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(thiazol-2-yl)phenyl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide
N-((S)-1-(3-cyano-5-fluorophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide hydrochloride
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamide
3-((S)-1-(2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-methylacetamido)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-(2,2,2-trifluoroethyl)benzamide
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamido)ethyl)-N-(2,2,2-trifluoroethyl)benzamide
N-((S)-1-(3-cyano-5-fluorophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-1-(3-(1H-imidazol-2-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide 2,2,2-trifluoroacetate
N-((S)-1-(3-cyano-5-fluorophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-methylacetamide
N-((S)-1-(3-cyano-5-fluorophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamide
2-(1,1-dioxido-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-((S)-1-(3-ethynylphenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methylacetamide
N-((S)-1-(3-(1H-imidazol-2-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-methylacetamide
N-((S)-1-(3-cyanophenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-methylacetamide
N-((S)-1-(3-(but-1-yn-1-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-1-(3-(but-1-yn-1-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamide
N-((S)-1-(3-(but-1-yn-1-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamide
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxoindolin-6-yl)acetamido)ethyl)-N,N-dimethylbenzamide
3-((S)-1-(2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-methylacetamido)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N,N-diethylbenzamide
N,N-diethyl-3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamido)ethyl)benzamide 2,2,2-trifluoroacetate
3-((S)-1-(2-(2,2-dioxido-1,3-dihydrobenzo[c]isothiazol-6-yl)-N-methylacetamido)-2-((S)-3-hydroxypyrrolidin-1-yl) ethyl)-N,N-dimethylbenzamide
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(3-oxo-3,4-dihydroquinoxalin-6-yl)acetamido)ethyl)-N,N-dimethylbenzamide
N-((S)-1-(3-(1,2,4 oxadiazol-3-yl)phenyl)-2-(S)-3-hydroxypyrrolidin-1-yl)ethyl)-2-(1,1-dioxido-3-oxo-3,4 dihydro-2H-benzo[b][1,4]thiazin-6-yl)-N-methylacetamide2,2,2-trifluoroacetate
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(1-methyl-1H-imidazol-2-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-1-(3-(5-ethyl-1,2,4-oxadiazol-3-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-methylthiazol-2-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(thiazol-5-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(thiazol-4-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(4-methylthiazol-2-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(2-methylthiazol-5-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(2-methylthiazol-4-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(1-methyl-1H-imidazol-5-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-1-(3-(1,3,4-oxadiazol-2-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(1-methyl-1H-imidazol-4-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-1-(3-(1-(cyclopropylmethyl)-1H-imidazol-2-yl)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
N-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(3-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)ethyl)-N-methyl-2-(2-oxoindolin-6-yl)acetamide
3-((S)-2-((S)-3-hydroxypyrrolidin-1-yl)-1-(N-methyl-2-(2-oxo-2,3-dihydrobenzo[d]thiazol-5-yl)acetamido)ethyl)-N-(2,2,2-trifluoroethyl)benzamide
or a stereoisomer thereof or a pharmaceutically acceptable salt thereof.

226 more elements

Dependencies are inferred from the claim text.

Facts

Application: 14/382,645Filed 5 Mar 2013
Priority: 5 Mar 2012
Published: 29 Jan 2015
Term ends: Not estimatedThe source records don’t support an estimate.

Classification32 codes

C07D 417/14
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms,…
A61K 31/404
Condensed with carbocyclic rings, e.g. carbazole: indoles, e.g. pindolol
A61K 31/423
Oxazoles: condensed with carbocyclic rings
A61K 31/428
Thiazoles: condensed with carbocyclic rings

Family

Application61/606,632Us provisional application · filed 5 Mar 2012
US 9,487,510 B2Related patent
US 2015/0031685 A1This patent

From the US filing history. Foreign family members aren’t listed.

Timeline

Citations

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