发明名称 Substituted N-phenyl-1-(4-Pyridinyl)-1H-pyrazol-3-amines
摘要 The present invention relates to N-phenyl-1-(4-pyridinyl)-1H-pyrazol-3-amine derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to formula (I); Wherein R1, R2, R3, R4, R5, R6 have the meaning defined in the claims. ;The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.
申请公布号 US8791144(B2) 申请公布日期 2014.07.29
申请号 US201013496120 申请日期 2010.09.16
申请人 Janssen Pharmaceutica NV 发明人 Macdonald Gregor James;Thuring Johannes Wilhelmus John F.;Van den Keybus Frans Alfons Maria;Van Roosbroeck Yves Emiel Maria
分类号 A61K31/4439;C07D401/04 主分类号 A61K31/4439
代理机构 代理人 Herridge Peter L.
主权项 1. A compound according to formula (I)or a stereochemically isomeric form thereof, wherein R1 and R2 each independently represent hydrogen or C1-4alkyl; R3 is C1-6alkyl optionally substituted with one or more substituents independently selected from the group consisting of hydroxyl, cyano, C1-6alkyloxy, benzyloxy, RxRyN—C(═O)—, and RzO—C(═O)—; Rx and Ry each independently represent hydrogen, C1-4alkyl, cycloC3-6alkyl or (cycloC3-6alkyl)C1-4alkyl; Rz represents hydrogen or C1-3alkyl; R4, R5 and R6 each independently represent hydrogen, halo, C1-6alkyl, cyano, trifluoromethyl, trifluoromethoxy, or methoxy; or R4 and R5 when attached to 2 vicinal carbon atoms together form a bivalent radical of formula —O—CF2—O—; or a pharmaceutically acceptable addition salt thereof.
地址 Beerse BE