发明授权
US6034082A 5-azabicyclo(3.1.0)hexylalkyl-2-piperiodones and --glutarimides as
neurokinin receptor antagonists
失效
5-氮杂二环(3.1.0)己基烷基-2-哌啶酮和γ-谷氨酰胺作为神经激肽受体拮抗剂
- 专利标题: 5-azabicyclo(3.1.0)hexylalkyl-2-piperiodones and --glutarimides as neurokinin receptor antagonists
- 专利标题(中): 5-氮杂二环(3.1.0)己基烷基-2-哌啶酮和γ-谷氨酰胺作为神经激肽受体拮抗剂
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申请号: US74931申请日: 1998-05-13
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公开(公告)号: US6034082A公开(公告)日: 2000-03-07
- 发明人: Alexander Roderick MacKenzie , Allan Patrick Marchington , Donald Stuart Middleton , Sandra Dora Meadows
- 申请人: Alexander Roderick MacKenzie , Allan Patrick Marchington , Donald Stuart Middleton , Sandra Dora Meadows
- 申请人地址: NY New York
- 专利权人: Pfizer Inc.
- 当前专利权人: Pfizer Inc.
- 当前专利权人地址: NY New York
- 优先权: GBX9524157 19951125
- 主分类号: A61K31/00
- IPC分类号: A61K31/00 ; A61K31/4427 ; A61K31/445 ; A61K31/4465 ; A61K31/4523 ; A61K31/454 ; A61K31/535 ; A61K31/5375 ; A61K31/5377 ; A61P1/00 ; A61P11/00 ; A61P13/00 ; A61P13/02 ; A61P15/00 ; A61P17/00 ; A61P25/00 ; A61P25/04 ; A61P27/16 ; A61P29/00 ; A61P37/08 ; A61P43/00 ; C07D401/06 ; C07D243/08 ; C07D401/02 ; C07D413/14
摘要:
Compounds of formula (I) ##STR1## and salts thereof, wherein: R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4)alky aryl or aryl(C.sub.1 -C.sub.4)alkyl; wherein the C.sub.1 -C.sub.6 alkyl group is optionally substituted by fluorine and the C.sub.3 -C.sub.7 cycloalkyl or C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4)alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C.sub.1 -C.sub.4 alkoxy or halo(C.sub.1 -C.sub.4)alkoxy; R.sup.2 is phenyl optionally substituted with one or two halo substituents or is indolyl, thienyl, benzothienyl or naphthyl; R.sup.3 is NH.sub.2,--NR.sup.4 SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --NR.sup.4 SO.sub.2 aryl, --NR.sup.4 SO.sub.2 N(R.sup.4).sub.2, NR.sup.4 CO(C.sub.1 -C.sub.6 alkyl), --NR.sup.4 CO aryl or a group or formula (a) ##STR2## wherein W is O, NR.sup.5, CH(OH), CHCO.sub.2 H, CHN(R.sup.4).sub.2, CHF, CF.sub.2, C.dbd.O or CH.sub.2 ; R.sup.4 is H or C.sub.1 -C.sub.6 alkyl; R.sup.5 is H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl, C.sub.2 -C.sub.6 alkanoyl, C.sub.4 -C.sub.8 cycloalkanoly, C.sub.3 -C.sub.7 cycloalkyl(C.sub.2 -C.sub.6)alkanoyl, aryl CO--, C.sub.1 -C.sub.6 alkylSO.sub.2 --, (R.sup.4).sub.2 NSO.sub.2 --, C.sub.3 -C.sub.7 cycloalkylSO.sub.2 --, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl-SO.sub.2 --, or arylSO.sub.2 --; X is CH.sub.2 or C.dbd.O; m is 0, 1 or 2 with the proviso that m is not O when W is NR.sup.5, C.dbd.O, or O; and n is an integer of from 1 to 4. These compounds are neurokinin receptor antagonists of utility in the treatment of a variety of medical conditions including urinary incontinence, asthma and related conditions.
公开/授权文献
- USD399498S Removable hard disk drive holder and cassette 公开/授权日:1998-10-13