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US 11,447,475 B2Granted
Isoxazole N-linked carbamoyl cyclohexyl acids as LPA antagonists
AssigneeBristol-Myers Squibb Company
InventorsPeter Tai Wah Cheng, Yan Shi, Robert F. Kaltenbach, III, Ying Wang, Hao Zhang
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Abstract
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.
Claims18
A compound according to Formula (Ia):
- or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein
- X1, X2 and X3 are each independently CR6;
- Y1 is NR3;
- Y2 is
- Y3 is O;
- L is a covalent bond or CH2;
- R1 is —C(O)OR10;
- R3 and R4a are independently hydrogen, C1-6 alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy;
- R4 is C1-10 alkyl, C1-10 deuterated alkyl, C1-10 haloalkyl, C1-10 alkenyl, C3-8 cycloalkyl, 6 to 10-membered aryl, —(C1-6 alkylene)-(C3-8 cycloalkyl), or —(C1-6 alkylene)-(6 to 10-membered aryl);
- wherein each of the alkyl, alkylene, alkenyl, cycloalkyl, and aryl, by itself or as part of other moiety, is independently substituted with 0 to 3 R8;
- R5 and R6 are each independently hydrogen, halo, cyano, hydroxyl, amino, C1-6 alkyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy;
- R8 are each independently deuterium, halo, hydroxyl, amino, cyano, C1-6 alkyl, C1-6 deuterated alkyl, C2-6 alkenyl, C2-6 alkynyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, haloalkoxy, phenyl, or 5 to 6 membered heteroaryl;
- or alternatively, two R8, taken together with the atom(s) to which they are attached, form a 3 to 6-membered carbocyclic ring each of which is independently substituted with 0 to 3 R12;
- R10 is hydrogen or C1-10 alkyl;
- and
- R12 is halo, cyano, hydroxyl, amino, C1-6 alkyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, haloalkoxy, phenyl, or 5 to 6 membered heteroaryl.
13 more elements
Dependencies are inferred from the claim text.