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US 2017/0247311 A1Published application
Cyclobutane containing carboxylic acid gpr120 modulators
AssigneeBristol-Myers Squibb Company
InventorsYan Shi, Ying Wang, Peter T.W. Cheng, Shung C. Wu
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Abstract
The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
Claims10
A compound of formula (I)
- or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate or a hydrate thereof, wherein:
- designates a single or double bond;
- x and y can be both a single bond;
- when x is a double bond, then y is a single bond and R3 is absent;
- when y is a double bond, then x is a single bond and R4 is absent;
- X is independently selected from:
- a bond, O, CH2, —CH2CH2—, —OCH2—, and —CH2O—;
- Y is independently a bond, a hydrocarbon linker substituted with 0-2Ra, a hydrocarbon-heteroatom linker substituted with 0-2Ra, or —(CH2)1-3—(O)0-1—(CH2)1-3—(C3-4 cycloalkyl substituted with 0-2Ra)—(CH 2)0-2;
- wherein said hydrocarbon linker has one to six carbon atoms and may be straight or branched, saturated or unsaturated;
- and said hydrocarbon-heteroatom linker has one to four carbon atoms and one group selected from O, CO, S, NH, CONH, and NHCO;
- W is independently selected from:
- a bond and O;
- R1 is —W—R5;
- R2, at each occurrence, is independently selected from:
- halogen, C1-6 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 haloalkyl, C1-6 haloalkoxy, and C1-4 haloalkylthio;
- R3 and R4, at each occurrence, are independently selected from:
- H, C1-4 alkyl, and C1-4 alkoxy;
- R3 may combine with X to form a 3- to 4 carbocycle;
- R4 may combine with Y to form a 3- to 4 carbocycle;
- R5 is independently selected from:
- C3-10 carbocycle, pyridyl, thiazolyl and dihydrobenzofuranyl;
- wherein each moiety is substituted with 0-1R6 and 0-3R7;
- R6 is independently selected from:
- C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio and —(X1)0-1—(CH2)0-2—R8;
- X1 is independently selected from:
- O, S, NH and CO;
- R7, at each occurrence, is independently selected from:
- halogen, C1-4 alkyl and C1-4 alkoxy;
- R8 is independently selected from:
- C3-6 carbocycle and a 5- to 6-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NRb, O, and S;
- wherein said carbocycle and heterocycle are substituted with 0-3Rc;
- Ra, at each occurrence, is independently selected from:
- halogen, OH, C1-4 alkyl, C1-4 haloalkyl, and C1-4 alkoxy;
- Rb, at each occurrence, is independently selected from:
- H, C1-4 alkyl, and —(CH2)0-2-phenyl;
- Rc, at each occurrence, is independently selected from:
- halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 haloalkyl, C1-4 haloalkoxy, and COPh;
- and
- n is independently 0, 1, or 2.
36 more elements
Dependencies are inferred from the claim text.