- 专利标题: Esters of 3-hydroxy-piperidinemethanol derivatives
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申请号: US117980申请日: 1998-08-11
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公开(公告)号: US6096761A公开(公告)日: 2000-08-01
- 发明人: Jean-Paul Rene Marie Bosmans , John Christopher Love , Michel Anna Jozef Decleyn , Henri Elisabeth Frans D'Haen
- 申请人: Jean-Paul Rene Marie Bosmans , John Christopher Love , Michel Anna Jozef Decleyn , Henri Elisabeth Frans D'Haen
- 申请人地址: BEX Beerse
- 专利权人: Janssen Pharmaceutica N.V.
- 当前专利权人: Janssen Pharmaceutica N.V.
- 当前专利权人地址: BEX Beerse
- 优先权: BEX96200379 19960215
- 主分类号: A01N43/40
- IPC分类号: A01N43/40 ; A01N43/58 ; C07D211/68 ; C07D237/30 ; C07D401/00
摘要:
The present invention of compounds of formula (I), ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R.sup.1 is C.sub.1-6 alkyloxy, C.sub.2-6 alkenyloxy or C.sub.2-6 alkynyloxy; R.sup.2 is hydrogen or C.sub.1-6 alkyloxy, or when taken together R.sup.1 and R.sup.2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C.sub.1-6 alkyl; R.sup.3 is hydrogen or halo; R.sup.4 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.2-6 alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R.sup.5 -, Alk-X--R.sup.6, -Alk-Y--C(.dbd.O)--R.sup.8, or -Alk-Y--C(.dbd.O)--NR.sup.10 R.sup.11 wherein each Alk is C.sub.1-12 alkanediyl; and R.sup.5 is hydrogen, cyano, C.sub.1-6 alkylsulfonylamino, C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, aryl, di(aryl)methyl or a heterocyclic ringsystem; R.sup.6 is hydrogen, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, aryl or heterocyclic ringsystem; X is O, S, SO.sub.2 or NR.sup.7 ; said R.sub.7 being hydrogen, C.sub.1-6 alkyl or aryl; R.sup.8 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, aryl, arylC.sub.1-6 alkyl, di(aryl)methyl, C.sub.1-6 alkyloxy or hydroxy; Y is NR.sup.9 or a direct bond; said R.sup.9 being hydrogen, C.sub.1-6 alkyl or aryl R.sup.10 and R.sup.11 each independently are hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, aryl or arylC.sub.1-6 alkyl, or R.sup.10 and R.sup.11 combined with the nitrogen atom bearing R.sup.10 and R.sup.11 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C.sub.1-6 alkyl, amino or mono or di(C.sub.1-6 alkyl)amino, or said R.sup.10 and R.sup.11 combined with the nitrogen bearing R.sup.10 and R.sup.11 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C.sub.1-6 alkyl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
公开/授权文献
- US5345980A Method and apparatus an aerosol container 公开/授权日:1994-09-13
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