发明名称 Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
摘要 The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.;
申请公布号 US9493412(B2) 申请公布日期 2016.11.15
申请号 US201214346751 申请日期 2012.09.24
申请人 Bristol-Myers Squibb Company 发明人 Qiao Jennifer X.;Finlay Heather;Jiang Ji;Lloyd John;Hu Carol Hui;Pi Zulan;Tora George O.;Neels James;Hangeland Jon J.;Friends Todd J.
分类号 C07D207/38;C07D409/12;C07D471/04;C07D401/12;C07D413/12;C07D417/12;C07D403/12;C07D401/04;C07D405/12;C07F7/08 主分类号 C07D207/38
代理机构 代理人 Sun Jing G.;Jacobsen Barry H.;Lu Yong
主权项 1. A compound of Formula (II):or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein: R1 is independently selected from the group consisting of: C1-6 alkyl substituted with 0-2 Ra, —(CH2)2N(C1-4 alkyl)(—CH═CHCF3), and —(CH2)n—W—R1a; W is independently selected from the group consisting of: a bond, NH, N(C1-4 alkyl), CO, CONH, CON(C1-4 alkyl), SO2, NHCO2, and CHRf; R1a is independently selected from the group consisting of: C3-6 cycloalkyl substituted with 0-2 Rc, phenyl substituted with 0-2 Rb, naphthyl substituted with 0-2 Rb, dihydroindenyl substituted with 0-2 Rc, and a 5- to 6-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NRe, O, and S(O)p; and wherein said heterocycle is substituted with 0-2 Rc; R5 is independently selected from the group consisting of: C5-6 cycloalkyl, phenyl, thienyl, pyrazolyl, imidazolyl, thiazolyl, tetrahydropyranyl, piperidinyl, pyridyl, and benzothiazolyl; and wherein each moiety is substituted with 0-2 Rd; L is X1—Y—X2; X1 is independently selected from the group consisting of: a bond, —CH═CH—, O, NH, —CH2O—, —CO—, —SO2—; X2 is independently selected from the group consisting of: —CH2—, —(CH2)2—, —(CH2)3—, —(CH2)4—, —CH(C1-4 alkyl)-, —O(CH2)2—, and —O(CH2)3—; Y is independently selected from the group consisting of: C3-6 cycloalkylene, C4-6 cycloalkenylene, phenylene, pyridylene, piperidinylene, oxadiazolylene, alternatively, R5-L- is Ra is, independently at each occurrence, selected from the group consisting of: halogen, CF3, CF2CF3, OCH2CF3, NH(C1-4 alkyl), CONH2, CONH(C1-4 alkyl), NHSO2(C1-4 alkyl), and N(C1-4 alkyl)SO2(C1-4 alkyl); Rb is, independently at each occurrence, selected from the group consisting of: halogen, C1-4 alkyl, CF3, OCF3, CONH2, and CONH(C1-4 alkyl); Rc is, independently at each occurrence, selected from the group consisting of: ═O and Rb; Rd is, independently at each occurrence, selected from the group consisting of: halogen, OH, C1-4 alkyl, C1-4 alkoxy, CF3, OCF3, CN, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2, CO(C1-4 alkyl), CO2(C1-4 alkyl), NHCO(C1-4 alkyl), —CH2NHCO(C1-4 alkyl), CONH2, CONH(C1-4 alkyl), CON(C1-4 alkyl)2, SO2(C1-4 alkyl), SO2NH2, —SO2NH(C1-4 alkyl), —SO2NH(C3-6 cycloalkyl), —NHSO2(C1-4 alkyl), —CH2NHSO2(C1-4 alkyl), and Si(C1-4 alkyl)3; Re is, independently at each occurrence, selected from the group consisting of: H, C1-4 alkyl, CO2(C1-4 alkyl), CO2(benzyl), phenyl, and benzyl; Rf is, independently at each occurrence, selected from the group consisting of: C1-4 alkyl, CO2(C1-4 alkyl), and CONH2; n is, independently at each occurrence, selected from 0, 1, 2, and 3; and p is, independently at each occurrence, selected from 0, 1, and 2; wherein said 5- to 10-membered heterocycle is each independently selected from the group consisting of pyridinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, pyrazinyl, piperazinyl, piperidinyl, imidazolyl, imidazolidinyl, indolyl, tetrazolyl, isoxazolyl, morpholinyl, oxazolyl, oxadiazolyl, oxazolidinyl, tetrahydrofuranyl, thiadiazinyl, thiadiazolyl, thiazolyl, triazinyl, triazolyl, benzimidazolyl, 1H-indazolyl, benzofuranyl, benzothiofuranyl, benztetrazolyl, benzotriazolyl, benzisoxazolyl, benzoxazolyl, oxindolyl, benzoxazolinyl, benzthiazolyl, benzisothiazolyl, isatinoyl, isoquinolinyl, octahydroisoquinolinyl, tetrahydroisoquinolinyl, tetrahydroquinolinyl, isoxazolopyridinyl, quinazolinyl, quinolinyl, isothiazolopyridinyl, thiazolopyridinyl, oxazolopyridinyl, imidazolopyridinyl, and pyrazolopyridinyl.
地址 Princeton NJ US