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公开(公告)号:US5434165A
公开(公告)日:1995-07-18
申请号:US976499
申请日:1992-11-13
申请人: Masayasu Kurono , Yutaka Baba , Tomoo Suzuki , Tsunemasa Suzuki , Kiyotaka Hirooka , Kiichi Sawai
发明人: Masayasu Kurono , Yutaka Baba , Tomoo Suzuki , Tsunemasa Suzuki , Kiyotaka Hirooka , Kiichi Sawai
IPC分类号: C07C211/59 , C07D213/72 , C07D215/38 , C07D219/08 , C07D487/04 , C07D471/04 , A61K31/41 , A61K31/47 , C07D403/14
CPC分类号: C07D487/04 , C07C211/59 , C07D213/72 , C07D215/38 , C07D219/08
摘要: An aromatic amino-substituted compound represented by formula: ##STR1## wherein A represents CH, N, or N.fwdarw.O; R.sub.1 represents a nitro group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, or an acyl group; and R.sub.3 represents a group: ##STR2## wherein m represents 0 or 1; n represents an integer of from 0 to 3; R.sub.4 and R.sub.5 each represents a hydrogen atom or a lower alkyl group; R.sub.6 and R.sub.7 each represents a hydrogen atom or a straight chain or branched lower alkyl group; R.sub.4 and R.sub.6 may be joined together to form an alkylene chain forming a heterocyclic ring; R.sub.5 and R.sub.7 may be joined together to form an alkylene chain forming a heterocyclic ring and R.sub.6 and R.sub.7 may be joined together to form an alkylene chain forming a heterocyclic ring,or a pharmaceutically acceptable salt thereof, a process for producing the same, and a method for preventing or treating brain disfunction such as senile dementia or Alzheimer's disease by administering a nootropic agent containing the same as an active ingredient are disclosed.
摘要翻译: 由下式表示的芳族氨基取代的化合物:其中A表示CH,N或N-> O; R1表示硝基或氨基; R2表示氢原子,低级烷基或酰基; 并且R 3表示基团:其中m表示0或1; n表示0〜3的整数, R4和R5各自表示氢原子或低级烷基; R6和R7各自表示氢原子或直链或支链的低级烷基; R4和R6可以连接在一起形成形成杂环的亚烷基链; R5和R7可以连接在一起以形成形成杂环的亚烷基链,并且R 6和R 7可以连接在一起形成形成杂环的亚烷基链,或其药学上可接受的盐,其制备方法和 公开了通过施用含有其作为活性成分的诱导剂来预防或治疗脑功能障碍的方法,例如老年性痴呆或阿尔茨海默氏病。
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公开(公告)号:US5530138A
公开(公告)日:1996-06-25
申请号:US312638
申请日:1994-09-27
申请人: Yutaka Baba , Tomoo Suzuki , Tsunemasa Suzuki , Kiyotaka Hirooka , Masayasu Kurono , Kiichi Sawai
发明人: Yutaka Baba , Tomoo Suzuki , Tsunemasa Suzuki , Kiyotaka Hirooka , Masayasu Kurono , Kiichi Sawai
IPC分类号: A61K31/00 , A61K31/40 , A61K31/407 , A61P25/00 , A61P25/02 , A61P25/18 , A61P25/28 , C07D487/04 , C07D451/02
CPC分类号: C07D487/04
摘要: There is disclosed a compound shown by a formula of ##STR1## wherein R.sub.1 is a hydrogen atom alkyl group having 1-4 carbon atoms or acyl group having 1-4 carbon atoms: R.sub.2 and R.sub.3 are a hydrogen atom, alkyl group having 1-4 carbon atoms, phenyl radical, halogen atom, cyano radical, acyl group having 1-4 carbon atoms, nitro radical, alkoxy group having 1 or 2 carbon atoms, or substituted or non-substituted amino group, respectively; n is an integer of 1-3; and dotted line means a possible ring, and a salt thereof. The compound and salt bind with muscarinic receptor in brain to develop a powerful actuation thereof and thus those can be used as an effective ingredient for preventing and curing senile dementias, and more particularly Alzheimer's disease.
摘要翻译: 公开了由下式表示的化合物,其中R1是具有1-4个碳原子的氢原子烷基或具有1-4个碳原子的酰基:R2和R3是氢原子,具有1- 4个碳原子,苯基,卤素原子,氰基,具有1-4个碳原子的酰基,硝基,具有1或2个碳原子的烷氧基,或取代或未取代的氨基; n为1-3的整数; 虚线表示可能的环及其盐。 化合物和盐与脑中的毒蕈碱受体结合以发挥其强力的作用,因此可以将其用作预防和治愈老年性痴呆,特别是阿尔茨海默氏病的有效成分。
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公开(公告)号:US4939126A
公开(公告)日:1990-07-03
申请号:US217523
申请日:1988-07-11
申请人: Masayasu Kurono , Tsunemasa Suzuki , Tomoo Suzuki , Kiyotaka Hirooka , Yukiharu Matsumoto , Hiroshi Ozawa , Kiichi Sawai
发明人: Masayasu Kurono , Tsunemasa Suzuki , Tomoo Suzuki , Kiyotaka Hirooka , Yukiharu Matsumoto , Hiroshi Ozawa , Kiichi Sawai
IPC分类号: C07F7/10 , A61K31/695 , A61P25/28 , C07F7/08
CPC分类号: C07F7/0812
摘要: 1-Pyrrolidineacetamide derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen atom or a trialkylsilyl group, R.sub.2 and R.sub.3 are hydrogen atom, respectively, when R.sub.1 is hydrogen atom, R.sub.4 is an alkyl group, R.sub.5 is a radical of ##STR2## in which R.sub.6 and R.sub.7 are an alkyl group, respectively, m and n are an integer of 1 to 3, respectively,or R.sub.4 represents together with R.sub.5 a hetero cyclic ring having nitrogen and silicon atoms or piperazine ring having a substituent of ##STR3## in which R.sub.6 and n have the meanings as referred to, and R.sub.2 and R.sub.4 as well as R.sub.3 and R.sub.5 form a hetero cyclic ring, respectively, connected with an alkylene chain, where R.sub.1 is the trialkylsilyl group, salts thereof, a process for the preparation thereof, as well as use thereof as for a medicine.
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