发明名称 Cyclopentylpyrazoles 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 US8853418(B2) 申请公布日期 2014.10.07
申请号 US201313968470 申请日期 2013.08.16
申请人 Janssen Pharmaceutica NV 发明人 Winters Michael;Sui Zhihua;Flores Christopher
分类号 A61K31/695;C07D231/56;C07D401/12;C07D231/54;C07D405/12;C07F7/18;C07D405/04;C07D401/04;C07D403/04;C07D491/113;A61K31/416 主分类号 A61K31/695
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, trifluoromethoxy, 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; R3 is hydrogen, chloro, or fluoro; Q is selected from the group consisting of Q1, Q2, and Q3; whereinR4 is selected from the group consisting of hydrogen, C1-4alkyl, C1-4alkoxy, cyano, fluoro, chloro, hydroxy, di(C1-4alkyl)amino, (C1-4alkyl)amino, amino, C1-4alkylcarbonyl, and C1-4alkylsulfonyl;R5 and R6 are each 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 C1-6alkyl, hydroxy(C1-4)alkyl, C1-6alkoxy, hydroxy, allyl, 2-methylprop-1-enyl, cyano, oxime, phenoxy, C1-4alkoxycarbonyl, C3-6cycloalkyl, 4,4-dimethyl-cyclohexyl, C3-6cycloalkyl(C1-4)alkyl, C3-6cycloalkyloxy, C1-6alkylcarbonyloxy, di(C1-4alkyl)aminocarbonyloxy, di(C1-4alkyl)aminocarbonyloxy-C1-4alkyl, C1-4alkoxycarbonylamino-C1-4alkyl, C3-6cycloalkyl(C1-4alkoxy, C3-6cycloalkylcarbonyloxy, di(C1-4alkyl)aminosulfonyl-amino, di(C1-4alkyl)aminosulfonyl-(N-methyl)amino, C1-4alkylsulfonyl-(N-methyl)amino, C1-4alkylsulfonylamino, C1-4alkylsulfonylamino-C1-4alkyl, C1-4alkylcarbonylamino-C1-4alkyl, di(C1-4alkyl)aminocarbonylamino-C1-4alkyl, trifluoromethylcarbonylamino, trifluoromethylcarbonylamino-C1-4alkyl, 2,5-dioxo-pyrrolidin-1-yl, 2-oxo-pyrrolidin-1-yl, 3,3-difluoro-pyrrolidin-1-yl, 3,3-diethyl-pyrrolidin-1-yl, 3,3-dimethyl-pyrrolidin-1-yl, pyrrolidin-1-yl, pyridinyloxy, trimethylsilyloxy, oxo, (tetrahydro-2H-pyran-2-yl)oxy, morpholin-4-yl, 2,6-dimethyl-morpholin-4-yl, morpholin-4-ylcarbonyloxy, morpholin-4-ylcarbonyloxy-C1-4alkyl, 6-(morpholin-4-yl)-pyrimidin-3-yl, 4-methyl-piperidin-1-yl, (1,2,4)-bicyclo[2.2.1]heptan-2-yloxy, tetrahydro-2H-pyran-4-ylcarbonyloxy, tetrahydro-2H-pyran-4-yl(C1-4alkoxy, 1,2,3,4-tetrahydroquinolin-3-yl, aminocarbonyl, pyridin-3-yl optionally substituted with one to two substituents each independently selected from the group consisting of C1-4alkyl, C1-4alkoxy, chloro, cyclopropyl, morpholin-4-yl, and C1-4alkoxycarbonyl; 1H-1,2,3-triazol-1-yl optionally substituted with one to two substituents each independently selected from the group consisting of C1-4alkyl, 2-hydroxypropan-2-yl, methoxymethyl, C3-6cycloalkyl, C1-4alkoxycarbonyl, C1-4alkylcarbonyloxy-C1-4alkyl, and trimethylsilyl; 1H-imidazol-1-yl optionally independently substituted with one to three C1-3alkyl substituents; and a spirofused heterocyclyl independently selected from the group consisting of 4,4,5,5-tetramethyl-1,3-dioxolan-2-yl, 4,5-dimethyl-1,3-dioxolan-2-yl, 1,3-dioxan-2-yl, 4,6-dimethyl-1,3-dioxan-2-yl, (3a,6a)-tetrahydro-3aH-cyclopenta[d][1,3]dioxol-2-yl, 5,5-dimethyl-1,3-dioxan-2-yl, and (3a,7a)-hexahydrobenzo[d][1,3]dioxol-2-yl; provided that a compound of Formula (I) is other than N-[3-(4-chlorophenyl)-2-(2-methoxyphenyl)-2,4,5,6-tetrahydrocyclopenta[c]pyrazol-5-yl]-N,N′,N′-trimethylsulfamide; or 3-(4-chlorophenyl)-2-(2-methoxyphenyl)-4′,4′,5′,5′-tetramethyl-2,6-dihydro-4H-spiro[cyclopenta[c]pyrazole-5,2′-[1,3]dioxolane];or an enantiomer, diastereomer, or pharmaceutically acceptable salt thereof.
地址 Beerse BE
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