发明授权
US5185369A Synthetic heteroaryl polyamines as excitatory amino acid
neurotransmitter antagonists
失效
合成异星形聚氨酯作为激素氨基酸神经递质拮抗剂
- 专利标题: Synthetic heteroaryl polyamines as excitatory amino acid neurotransmitter antagonists
- 专利标题(中): 合成异星形聚氨酯作为激素氨基酸神经递质拮抗剂
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申请号: US749038申请日: 1991-08-23
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公开(公告)号: US5185369A公开(公告)日: 1993-02-09
- 发明人: Nicholas A. Saccomano , Robert A. Volkmann
- 申请人: Nicholas A. Saccomano , Robert A. Volkmann
- 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
- 主分类号: A61K31/295
- IPC分类号: A61K31/295 ; A61K31/40 ; A61K31/403 ; A61K31/404 ; A61K31/44 ; A61K31/4402 ; A61K31/4406 ; A61K31/4409 ; A61K31/4418 ; A61K31/47 ; A61P25/00 ; C07D209/18 ; C07D209/20 ; C07D209/42 ; C07D213/56 ; C07D213/81 ; C07D213/82 ; C07D215/12 ; C07D215/14 ; C07D215/48 ; C07D215/50 ; C07D215/54 ; C07D241/42 ; C07D241/44 ; C07D403/12 ; C07F17/02
摘要:
Compounds having the formula R-(CH.sub.2).sub.m -CO-R' wherein R is ferrocene, a 5 to 7 member azacyclic system or an 8 to 11 member azabicyclic system, having 1 or 2 nitrogen atoms, or any such system substituted with one or more of F, Cl, Br, OH, C1 to C4 alkyl, C1 to C4 alkoxy, CF.sub.3, phenyl, amino, C1 to C4 alkylamino and di(C1 to C4 alkyl)amino; m is 0 or 1; and R' is--[NH(CH.sub.2).sub.n ].sub.x NH.sub.2, with each n being independently 2 to 5 and x being 1 to 6; ##STR1## with each n being independently 2 to 5, x being 0 to 4, y and z being independently 1 to 5 and the sum of x and the greater of y and z being 1 to 5; or ##STR2## with each a being 2 to 5, each b being 2 to 5, each n being independently 2 to 5, x being 0 to 3, each y being 0 or 1, z being 0 to 3 and x+y+z being 0 to 4, and their pharmaceutically acceptable acid addition salts are potent excitatory amino acid neurotransmitter antagonists. These compounds are useful as mammalian psychotherapeutants, as the active ingredient in pharmaceutical compositions for treating conditions in mammals which are mediated by excitatory amino acid neurotransmitters and in the control of invertebrate pests.
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