发明名称 TETRAZOLONE-SUBSTITUTED DIHYDROPYRIDINONE MGAT2 INHIBITORS
摘要 The present invention provides compounds of Formula (I): a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyl-transferase type 2 (MGAT2) inhibitors which may be used as medicaments.;
申请公布号 US2017015648(A1) 申请公布日期 2017.01.19
申请号 US201515123773 申请日期 2015.03.05
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 Ahmad Saleem
分类号 C07D401/04;C07D417/14;C07D401/14;C07D409/14;A61K45/06;A61K31/4439 主分类号 C07D401/04
代理机构 代理人
主权项 1. A compound of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate or a hydrate thereof, wherein: ring A is independently phenyl or a 5- to 6-membered heteroaryl comprising carbon atoms and 1-4 heteroatoms selected from N, NRe, O and S; wherein said phenyl and heteroaryl are substituted with 0-1 R6 and 0-2 R7;R1 is independently selected from: —(CH2)m—(C3-6 carbocycle substituted with 0-2 Rb and 0-2 Rg), —(CH2)m-(5- to 6-membered heteroaryl comprising carbon atoms and 1-4 heteroatoms selected from N, NRe, O and S; wherein said heteroaryl is substituted with 0-1 Rb and 0-2 Rg), and (a C1-12 hydrocarbon chain substituted with 0-3 Ra; wherein said hydrocarbon chain may be straight or branched, saturated or unsaturated);R2 is independently selected from: C1-4 alkyl, C3-4 cycloalkyl, and C1-4 haloalkyl;R3 is independently selected from: H, F, C1-4 alkyl and CN;R4 is independently selected from: H, F, and C1-4 alkyl;R3 and R4 may be combined with the carbon atom to which they are attached to form a 3- to 6-membered carbocycle;R6 is independently selected from: halogen, C1-6 alkyl substituted with 0-2 Rh, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, CO(C1-4 alkyl), —(CH2)m—C3-6 carbocycle, —(CH2)m—NRfRi, CN, ORi, SRi, and (a 4- to 6-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NRe, O, and S);R7 is independently selected from: halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, and C1-4 haloalkoxy;alternatively, R6 and R7, together with the carbon atoms to which they are attached, combine to form a 5- to 6-membered carbocyclic ring or a 5- to 6-membered heterocyclic ring comprising carbon atoms and 1-3 heteroatoms selected from N, NRe, O, and S; wherein said heterocycle is substituted with 0-2 Rg;Ra is, at each occurrence, independently selected from: halogen, OH, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, N(C1-4 alkyl)2, COOH, and —(CH2)n—Rc;Rb is, at each occurrence, independently selected from: halogen, OH, C1-10 alkyl, C1-10 alkoxy, C1-10 haloalkyl, C1-10 haloalkoxy, C1-10 alkylthio, C1-10 haloalkylthio, N(C1-4 alkyl)2, —CONH(C4-20 alkyl), —CONH(C4-20 haloalkyl), —O(CH2)sO(C1-6 alkyl), —O(CH2)sO(C1-6 haloalkyl), Rc, and —(CH2)n—(O)t—(CH2)mRc;Rc is, at each occurrence, independently selected from: C3-6 cycloalkyl substituted with 0-2 Rd, C3-6 cycloalkenyl substituted with 0-2 Rd, —(CH2)m-(phenyl substituted with 0-3 Rd), and (a 5- to 6-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NRe, O, and S; wherein said heterocycle is substituted with 0-2 Rd);Rd is, at each occurrence, independently selected from: halogen, OH, CN, NO2, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, tetrazolyl, OBn and phenyl;Re is, at each occurrence, independently selected from: H, C1-8 alkyl, C1-8 haloalkyl, —(CH2)n—C3-6 carbocycle, CO(C1-4 alkyl) and COBn;Rf is, at each occurrence, independently selected from: H and C1-4 alkyl;Rg is, at each occurrence, independently selected from: halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, and C1-4 haloalkoxy;Rh is, at each occurrence, independently selected from: OH, halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, and C1-4 haloalkoxy;Ri is, at each occurrence, independently selected from the group consisting of C1-4 alkyl, C3-4 cycloalkyl and phenyl;n, at each occurrence, is independently 0 or 1;m, at each occurrence, is independently 0, 1, 2, 3, or 4;s, at each occurrence, is independently 1, 2, or 3; andt, at each occurrence, is independently 0 or 1.
地址 Princeton NJ US