发明名称 Pyrrolopyrazoles as N-type calcium channel blockers
摘要 Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows:; wherein R1, R2, R3, Q, and G are defined herein.
申请公布号 US8846949(B2) 申请公布日期 2014.09.30
申请号 US201313968476 申请日期 2013.08.16
申请人 Janssen Pharmaceutica NV 发明人 Winters Michael;Sui Zhihua
分类号 C07D231/56;A61K31/695;C07D487/04 主分类号 C07D231/56
代理机构 代理人 Herridge Peter L.
主权项 1. A compound of Formula (I) wherein R1 is selected from the group consisting of C1-4alkyl, C1-4alkoxy, 2,2-difluoroethoxy, di(C1-4alkyl)amino, trifluoromethoxy, fluoro, and trifluoromethyl;R2 is hydrogen; or, R2 may be taken with R1 and the phenyl ring to which R1 and R2 are both attached to form 2,3-dihydrobenzofuran-7-yl or 1,3-benzodioxol-4-yl;R3 is hydrogen, methyl, methoxy, chloro, or fluoro;Q is selected from the group consisting of Q1, Q2, and Q3; wherein R4 is selected from the group consisting of hydrogen, C1-4alkyl, C1-4alkoxy, cyano, fluoro, and chloro;R5 is independently selected from the group consisting of hydrogen, C1-4alkyl, C1-4alkoxy, cyano, chloro, and di(C1-4alkyl)amino;G is selected from the group consisting of 4-methylphenyl, 3-cyanophenyl, 4-cyanophenyl, 4-methoxycarbonylphenyl, 2-chloro-quinolin-6-yl, morpholin-4-ylsulfonyl, morpholin-4-yl(C1-4alkyl)aminosulfonyl, 2,6-dimethylmorpholin-4-ylsulfonyl, C6-10aryl(C1-4alkylsulfonyl, C6-10aryloxy(C1-4)alkylsulfonyl, 3,5-dimethylisoxazol-4-yl-sulfonyl, C1-4alkoxycarbonyl(C1-4)alkyl-sulfonyl, trifluoromethylsulfonyl, C3-7cycloalkylsulfonyl, 2,2,2-trifluoroethylsulfonyl, di(C1-4alkyl)aminosulfonyl, di(C1-4alkyl)aminosulfonylamino(C1-4alkyl-sulfonyl, C1-4alkylsulfonylamino(C1-4alkyl-sulfonyl, 2,5-dione-pyrrolidin-1-yl-(C1-4alkylsulfonyl, (2H)-1,3-dione-1H-isoindol-1-yl-(C1-4alkyl-sulfonyl, 1,1-dioxidotetrahydrothiophen-3-yl)sulfonyl, C1-6alkylsulfonyl, di(C1-4alkyl)aminosulfonyl, pyrrolidin-1-ylsulfonyl, piperidin-1-ylsulfonyl, 4-(R6)-piperidin-1-ylsulfonyl wherein R6 is C1-4alkoxycarbonyl or C1-4alkyl; azepan-1-ylsulfonyl, methoxymethylcarbonyl, trifluoromethylcarbonyl, C1-4alkoxycarbonylamino(C2-4)alkyl-carbonyl, C1-4alkoxycarbonylaminomethylcarbonyl, trifluoromethylsulfonylaminomethylcarbonyl, trifluoromethoxycarbonyl, C1-4alkylsulfonylaminomethyl-carbonyl, C1-4alkoxycarbonyl, di(C1-4alkyl)aminocarbonyl, C1-4alkoxycarbonyl, pyridinylcarbonyl, furanylcarbonyl, and 5-methylisoxazol-3-ylcarbonyl;or an enantiomer, diastereomer, or pharmaceutically acceptable salt thereof.
地址 Beerse BE