Bristol-Myers Squibb Compnay

Other

Syngene International Limited

Peter Tai Wah Cheng

Yan Shi

Hao Zhang

Jun Li

Robert F Kaltenbach, Iii

Jun Shi

Shiwei Tao

Ying Wang

James R Corte

Lawrence J Kennedy

Tianan Fang

Steven J Walker

Sutjano Jusuf

Kumaravel Selvakumar

Suresh Dhanusu

Wei Meng

Rulin Zhao

David J Donnelly

Ramesh Babu Reddigunta

Bei Wang

Tritin Tran

Joonyoung Kim

Robert F Kaltenbach Iii

Ramesh Badu Reddigunta

Mark Liu

Iii Robert F Kaltenbach

Robert F Iii Kaltenbach

The present invention provides compounds of Formula (I): (I), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Cyclobutyl carboxylic acids as LPA antagonists

The present invention provides compounds of Formula (I), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Triazole carboxylic acids as LPA antagonists

The present invention provides compounds of Formula (Ia) or (Ib) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Oxabicyclo acids as LPA antagonists

The present invention provides compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Isoxazole carboxylic acids as LPA antagonists

Cyclopentyl acids as LPA antagonists

The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Triazole n-linked carbamoyl cyclohexyl acids as LPA antagonists

Triazole N-linked carbamoyl cyclohexyl acids as LPA antagonists

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Carbamoyloxymethyl triazole cyclohexyl acids as LPA antagonists

The present invention provides compounds of Formula (Ia) and (Ib): (Ia) or (Ib), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors. 

Isoxazole N-linked carbamoyl cyclohexyl acids as LPA antagonists

The present invention provides compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein X, X, X, and Xare each independently CRor N; provided that no more than two of X, X, X, or Xare N; Qis N or NR; one of Qand Qis CR, and the other is N or NR; and the dashed circle denotes optional bonds forming an aromatic ring; Yis O or NR; Yis &#x2014;CO&#x2014;, &#x2014;SO&#x2014;, or &#x2014;S(O(NH)&#x2014;; Yis O or NR; provided that (1) Yand Yare not both O, and (2) when Yis C(O), Yis not O; L is a covalent bond or Calkylene substituted with 0 to 4 R; Ris (&#x2014;CH)R; a is an integer of 0 or 1; Ris each independently halo, cyano, hydroxyl, amino, Calkyl, Ccycloalkyl, Cheterocyclyl, alkylamino, haloalkyi, hydroxyalkyi, aminoalkyi, alkoxy, alkoxyalkyl, haloalkoxyalkyl, or haloalkoxy; n is an integer of 0, 1, or 2; Rand Rare independently hydrogen, Calkyl, haloalkyi, hydroxyalkyi, aminoalkyi, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; Ris Calkyl, Chaloalkyi, Cdeuterated alkyl, Calkenyl, Ccycloalkyl, 6 to 10-membered aryl, 3 to 8-membered heterocyclyl, &#x2014;(Calkylene)&#x2014;(Ccycloalkyl), &#x2014;(Calkylene)&#x2014;(6 to 10-membered aryl), &#x2014;(Calkylene)&#x2014;(3 to 8-membered heterocyclyl), or &#x2014;(Calkylene)&#x2014;(5 to 6-membered heteroaryl); wherein each of the alkyl, alkylene, alkenyl, cycloalkyl, aryl, heterocyclyl, and heteroaryl, by itself or as part of other moiety, is independently substituted with 0 to 3 R; or alternatively, Rand R, taken together with the N and 0 atoms which they are attached, form a 4 to 9-membered heterocyclic ring moiety which is substituted with 0 to 3 R; or alternatively, (Rand R) or (Rand R), taken together with the atoms to which they are attached to, form a 5 to 8-membered heterocyclic ring moiety which is substituted with 0 to 3 R; Ris hydrogen, Calkyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; Rand Rare each independently hydrogen, halo, cyano, hydroxyl, amino, alkyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; Ris halo, oxo, cyano, hydroxyl, amino, Calkyl, Ccycloalkyl, Cheterocyclyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; Rare each independently deuterium, halo, hydroxyl, amino, cyano, Calkyl, Cdeuterated alkyl, Calkenyl, Calkynyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, haloalkoxy, phenyl, or 5 to 6-membered heteroaryl; or alternatively, two R, taken together with the atom(s) to which they are attached, form a 3 to 6-membered carbocyclic ring or a 3 to 6-membered heterocyclic ring each of which is independently substituted with 0 to 3 R; Ris selected from &#x2014;CN, &#x2014;C(O)OR, &#x2014;C(O)NRR&#x2014;, &#x2014;CO&#x2014;NH&#x2014;CO&#x2014;R, &#x2014;CO&#x2014;NH&#x2014;SO&#x2014;R, &#x2014;CO&#x2014;NH&#x2014;SO&#x2014;R, &#x2014;SO&#x2014;OH, &#x2014;SO&#x2014;NH&#x2014;CO&#x2014;R, &#x2014;P(O)(OH), tetrazol-5-yl, &#x2014;CH&#x2014;CO&#x2014;NH&#x2014;CO&#x2014;R, &#x2014;CH&#x2014;CO&#x2014;NH&#x2014;SO&#x2014;R, &#x2014;CH&#x2014;CO&#x2014;NH&#x2014;SO&#x2014;R, &#x2014;CH&#x2014;SO&#x2014;OH, &#x2014;CH&#x2014;SO&#x2014;NH&#x2014;CO&#x2014;R, &#x2014;CH&#x2014;P(O)(OH), tetrazol-5-ylmethylene; Ris Calkyl, Ccycloalkyl, haloalkyl, hydroxyalkyi, aminoalkyi, alkoxyalkyi, or haloalkoxyalkyi; Ris hydrogen or Calkyl; and Rand Rare each independently hydrogen, Calkyl, Ccycloalkyl, Cheterocyclyl, alkylamino, haloalkyi, hydroxyalkyi, aminoalkyi, alkoxyalkyi, haloalkoxyalkyi, alkoxy, or haloalkoxy; and Ris halo, cyano, hydroxyl, amino, Calkyl, alkylamino, haloalkyi, hydroxyalkyi, aminoalkyi, alkoxyalkyi, haloalkoxyalkyi, alkoxy, haloalkoxy, phenyl, or 5 to 6-membered heteroaryl. These compounds are selective LPA receptor inhibitors. 

Pyrazole n-linked carbamoyl cyclohexyl acids as LPA antagonists

The present invention provides compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors. 

Cyclohexyl acid pyrazole azoles as LPA antagonists

The present invention provides compounds of Formula (Ia) or (Ib): (Ia) or (Ib), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors. 

Cyclohexyl acid isoxazole azines as LPA antagonists

The present invention provides compounds of Formula (I): Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors. 

Cyclohexyl acid triazole azoles as LPA antagonists

The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors. 

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Princeton, NJ, United States of America

Peter Tai Wah Cheng