发明名称 Substituted piperazinylcamphor derivatives as oxytocin antagonists
摘要 PCT No. PCT/US94/07769 Sec. 371 Date Jan. 16, 1996 Sec. 102(e) Date Jan. 16, 1996 PCT Filed Jul. 11, 1994 PCT Pub. No. WO95/02587 PCT Pub. Date Jan. 26, 1995The invention is directed to a series of novel compounds of the formula <IMAGE> where Y is carbonyl or sulfonyl; R7 and R8 are alkyl, or R7 and R8, together with the carbon to which they are attached, form a C3-6 carbocyclic ring; R9 and R10 are each independently selected from hydrogen, hydroxyl, oximido, methyl, carboxyl, carboxyalkyl, unsubstituted or substituted alkoxycarbonyl, alkylcarbonyloxyalkyl, cyanoalkyl, hydroxyalkyl or unsubstituted amino; R11 is hydrogen, oxo, -N(R12)-CO-R13 or -CO-N(R14)-R15; R12 is hydrogen or unsubstituted or substituted alkyl; R13 is alkoxyl, unsubstituted or substituted heterocyclic rings selected from <IMAGE> <IMAGE> <IMAGE> <IMAGE> or unsubstituted or substituted alkyl; and R14 and R15 are each independently selected from hydrogen or unsubstituted or substituted alkyl. The Y moiety cannot be bonded to the camphor ring at the 3 or 6 positions. Such compounds are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery.
申请公布号 AU7329294(A) 申请公布日期 1995.02.13
申请号 AU19940073292 申请日期 1994.07.11
申请人 MERCK & CO., INC. 发明人 MARK G. BOCK;DOUG W. HOBBS
分类号 C07D295/18;A61K31/38;A61K31/382;A61K31/445;A61K31/4465;A61K31/4468;A61K31/495;A61P7/02;A61P7/10;A61P9/12;A61P13/02;A61P15/00;A61P43/00;C07B59/00;C07D207/16;C07D207/26;C07D207/277;C07D211/22;C07D211/58;C07D211/60;C07D211/62;C07D213/30;C07D213/38;C07D233/54;C07D233/64;C07D295/185;C07D295/26;C07D303/34;C07D309/14;C07D309/28;C07D335/02;C07D453/02 主分类号 C07D295/18
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