发明名称 PHTHALIMIDE-PIPERIDINE, -PYRROLIDINE AND -AZEPINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MUSCARINIC RECEPTOR (ANT-)AGONISTS
摘要 The compounds of the present invention have formula (I) wherein m and n are independently 0 or 1; o and p are independently 1 or 2; X is C(R)2, O, S(O)q, NR, C(=O), CHOR, C=NOR, NC(=O)OR, NC(=O)N(R)2, NC(=O)R, CHC(=O)OR, CHC(=O)N(R)2, CHC(=O)R, NS(O)2R, (1) or (2), wherein q is 0, 1 or 2; R is H, lower alkyl, alkoxyl, arylalkyl, alkynyl, alkenyl or cycloalkyl; D is CH or N; E is C=O, S(=O), S(=O)2 C=S or C=NR; and J is O, CR, C(R)2, NR or NRC(=O); R<1>, R<2>, and R<3> are independently H, lower alkyl, halogen, lower alkoxyl, OH, HOCH2, aryl, arylalkyl, SR or N(R)2; and A is (3) wherein a, b, c and d are independently CH or N, with the proviso that no more than two of a, b, c, d are N; and R<4> is H, lower alkyl, halogen, lower alkoxyl, OH, HOCH2, aryl, arylalkyl, SR or N(R)2. The use of the compounds and pharmaceutically acceptable salts thereof to treat glaucoma, myopia, psychosis and various other conditions involving muscarinic receptors is also disclosed.
申请公布号 WO9932479(A1) 申请公布日期 1999.07.01
申请号 WO1998US27585 申请日期 1998.12.22
申请人 ALCON LABORATORIES, INC.;DANTANARAYANA, ANURA 发明人 DANTANARAYANA, ANURA
分类号 C07D401/04;C07D405/04;(IPC1-7):C07D401/04;A61K31/445;C07D401/14 主分类号 C07D401/04
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