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    • 9. 发明授权
      US5663352A 4-phenyl-4-phenylpropyl(enyl)-piperidines as tachykinin antagonists 失效
    • 4-phenyl-4-phenylpropyl(enyl)-piperidines as tachykinin antagonists
    • US5663352A
    • 1997-09-02
    • US583014
    • 1996-01-19
    • Angus Murray MacLeod , Kevin John Merchant , Graeme Irvine Stevenson
    • Angus Murray MacLeod , Kevin John Merchant , Graeme Irvine Stevenson
    • A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/53 , A61P1/08 , A61P25/04 , A61P25/06 , A61P29/00 , A61P43/00 , C07D211/18 , C07D211/22 , C07D211/32 , C07D401/06 , C07D211/14 , C07D211/12
    • C07D401/06 , C07D211/18 , C07D211/22 , C07D211/32
    • The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein X represents a propylene or propenylene chain optionally substituted by one or more of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 ; m is 2, 3 or 4; n is 0, 1 or 2 when m is 2 or 3, and n is 0 or 1 when m is 4; R.sup.1 represents optionally substituted phenyl; R.sup.2 represents optionally substituted phenyl, heteroaryl, benzhydryl or benzyl; R.sup.3 represents H, COR.sup.9, CO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, COCO.sub.2 R.sup.10, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, hydroxy, cyano, COR.sup.9, NR.sup.10 R.sup.11, C(NOH)NR.sup.10 R.sup.11, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15 and optionally substituted phenyl), Y--R.sup.8 or CO--Z--(CH.sub.2).sub.q --R.sup.12 ; R.sup.4 and R.sup.5 each independently represent H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, hydroxy or C.sub.1-6 alkoxy, or R.sup.4 and R.sup.5 together form a group .dbd.O; R.sup.6 and R.sup.7 each independent represents H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, hydroxy or C.sub.1-6 alkoxy or R.sup.6 and R.sup.7 together form a group .dbd.O; R.sup.8 represents an optionally substituted aromatic heterocycle; R.sup.9 represents H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, or phenyl; R.sup.10 and R.sup.11 each independently represent H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or C.sub.3-5 cycloalkylmethyl; R.sup.12 represents NR.sup.13 R.sup.14 or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; R.sup.13 and R.sup.14 each independently represent H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, optionally substituted phenyl or phenylC.sub.1-4 alkyl; R.sup.15 represents C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, trifluoromethyl or optionally substituted phenyl; Y represents a hydrocarbon chain of 1, 2, 3 or 4 carbon atoms which may optionally be substituted by oxo; Z represents CH.sub.2, O, S or NR.sup.10 ; and q represents 0, 1, 2, 3, 4, 5 or 6. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.
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