Aminobenzene compounds to prevent nerve cell degradation
    11.
    发明授权
    Aminobenzene compounds to prevent nerve cell degradation 失效
    氨基苯化合物防止神经细胞降解

    公开(公告)号:US5580883A

    公开(公告)日:1996-12-03

    申请号:US266614

    申请日:1994-06-28

    摘要: A compound useful for central antioxidant having inhibitory activity of degeneration and necrocytosis of cerebral cells of the formula (I): ##STR1## wherein A and B are independently (1) a group of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are independently hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted heterocyclic group, or R.sub.1 together with R.sub.2 and the nitrogen atom to which they are bound may form a cyclic amino group, provided that both R.sub.1 and R.sub.2 are not hydrogen atom at the same time, or (2) a group of the formula: ##STR3## wherein D is O or S, R.sub.3 is hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group, m is 1, 2, or 3 and n is 0, 1, 2, 3 or 4;p is 1 or 2, provided that both A may be the same or different when p is 2; andR.sub.4, R.sub.5 and R.sub.6 are independently hydrogen atom, a lower alkyl or a lower alkoxy, or R.sub.5 and R.sub.6 may bond together to form --CH.dbd.CH--CH.dbd.CH--, or a salt thereof.

    摘要翻译: 可用于具有式(I)的脑细胞的变性和坏死细胞增多抑制活性的中枢抗氧化剂的化合物:其中R 1和R 2独立地为氢原子,任选取代的烃残基或 任选取代的杂环基,或R 1与R 2一起并且与它们结合的氮原子可以形成环状氨基,条件是R 1和R 2不得同时为氢原子,或(2)式 :其中D是O或S,R 3是氢原子,任选取代的烃残基或任选取代的酰基,m是1,2或3,n是0,1,2,3或4; p为1或2,条件是当p为2时,A可以相同或不同; 并且R 4,R 5和R 6独立地为氢原子,低级烷基或低级烷氧基,或者R 5和R 6可以键合在一起形成-CH = CH-CH = CH-或其盐。

    Tetracyclic condensed heterocyclic compounds and their use
    15.
    发明授权
    Tetracyclic condensed heterocyclic compounds and their use 失效
    四环稠合杂环化合物及其用途

    公开(公告)号:US5620973A

    公开(公告)日:1997-04-15

    申请号:US330133

    申请日:1994-10-25

    CPC分类号: C07D471/06 C07D487/04

    摘要: A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R.sup.1 represents H or a hydrocarbon group which may be substituted; Y represents an amino or nitrogen-containing saturated heterocyclic group which may be substituted, its salt, inhibiting excellent cholinesterase inhibitory activity and monoamine uptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.

    摘要翻译: 式(Ⅰ)的新化合物,其中Ar表示可被取代的四环稠合杂环基; R1表示H或可被取代的烃基; Y表示可被取代的氨基或含氮饱和杂环基,其盐,抑制优异的胆碱酯酶抑制活性和单胺摄取抑制活性,因此可用作老年痴呆症的治疗和/或预防药物。

    Method for improving brain function using cholinesterase-inhibiting
aminoketone compounds
    16.
    发明授权
    Method for improving brain function using cholinesterase-inhibiting aminoketone compounds 失效
    使用胆碱酯酶抑制性氨基酮化合物改善脑功能的方法

    公开(公告)号:US5434179A

    公开(公告)日:1995-07-18

    申请号:US215619

    申请日:1994-03-22

    摘要: An aminoketone compound of the formula ##STR1## wherein ring A' means a five through eight-membered cyclic group which may be substituted and may contain one or two hetero atom(s) of O, S, N, as the ring-constituents; R.sup.1' means a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.2' means a hydrogen atom or a lower alkyl group; R.sup.3' means an aromatic group which may be substituted; R.sup.4' means a hydrogen atom, a lower alkyl group or aromatic group which may be substituted; n' means an integer of 2 to 7, or a salt thereof, is useful as an cholinesterase inhibitors and a cerebral function ameliorating agent.

    摘要翻译: 式IMAMA的氨基酮化合物,其中环A'表示可以被取代的五至八元环基,并且可以含有一个或两个作为环组成的O,S,N的杂原子; R1'表示氢原子或可被取代的烃残基; R2'表示氢原子或低级烷基; R3'表示可被取代的芳基; R4'表示氢原子,可以被取代的低级烷基或芳基; n'表示2〜7的整数或其盐可用作胆碱酯酶抑制剂和脑功能改善剂。

    Benzylpiperidine compounds and their use
    17.
    发明授权
    Benzylpiperidine compounds and their use 失效
    苄基哌啶化合物及其用途

    公开(公告)号:US5294625A

    公开(公告)日:1994-03-15

    申请号:US964851

    申请日:1992-12-18

    摘要: 1. A cyclic amine compound of the formula ##STR1## wherein B means a saturated or unsaturated 5- to 7-membered aza-heterocyclic group which may be substituted; A means a bond or an alkylene or alkenylene group which may be substituted by hydrocarbon residues, oxo, hydroxyimino, and/or hydroxy, --means either a single bond or a double bond (provided that when A means a bond, --means a single bond); R.sub.2 and R.sub.3 independently mean a hydrogen atom or a hydrocarbon residue which may be substituted (provided that both of R.sub.2 and R.sub.3 are not hydrogen atoms) or jointly form a cyclic amino group together with the adjacent nitrogen atom, n is 0, 1 or 2 and p is 1 or 2 or a physiologically acceptable salt thereof.The compounds are useful for therapy of cerebral edema, acute symptoms in cerebral apoplexy and protection of brain and nerve cell, or useful as anticholinesterase or as brain function-improving agent.

    摘要翻译: 1.下式的环胺化合物其中B表示可被取代的饱和或不饱和的5-至7-元氮杂杂环基; A表示可以被烃残基,氧代,羟基亚氨基和/或羟基取代的键或亚烷基或亚烯基, - 单键或双键(条件是当A表示键时, - 表示单键 键); R2和R3独立地表示氢原子或可被取代的烃残基(条件是R2和R3都不是氢原子)或与相邻的氮原子一起形成环氨基,n是0,1或2 和p为1或2或其生理上可接受的盐。 该化合物可用于治疗脑水肿,脑中风的急性症状和保护脑和神经细胞,或用作抗胆碱酯酶或脑功能改善剂。

    Azaspiro compounds and their use
    18.
    发明授权
    Azaspiro compounds and their use 失效
    阿扎西罗化合物及其用途

    公开(公告)号:US4804665A

    公开(公告)日:1989-02-14

    申请号:US137713

    申请日:1987-12-24

    IPC分类号: C07D471/10 A61K31/395

    CPC分类号: C07D471/10

    摘要: Azaspiro compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, a hydrocarbon residue which may have a substituent, or an acyl group which may have a substituent; R.sub.3 represents hydrogen or a hydrocarbon residue which may have a substituent; each of X.sub.1 and X.sub.2 is oxygen or sulfur; Y represents oxygen, sulfur or a group of the formula: --N(R.sub.4)--, wherein R.sub.4 represents hydrogen or a lower alkyl group; m represents 0 or 1; n represents 0 or 1, and its salt are novel compounds, possess excellent brain function-improving action, and are of use as drugs for the prevention and therapy of senile dementia of Alzheimer type, vascular-type dementia and dementia derived from Alzheimer's disease, Pick's disease, Huntington's disease, Creutzfeldt-Jakob's disease, Parkinson's disease and spinocerebellar degeneration.

    Heterocyclic compounds, their production and use
    20.
    发明授权
    Heterocyclic compounds, their production and use 失效
    杂环化合物,其生产和使用

    公开(公告)号:US06319916B1

    公开(公告)日:2001-11-20

    申请号:US08051831

    申请日:1993-04-23

    IPC分类号: C07D26702

    摘要: A compound of the formula: wherein ring A is an optionally substituted benzene ring; ring B′ is an optionally substituted non-aromatic heterocyclic ring having, the same or different, two or more hetero atoms; R1 is a hydrogen atom or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; Y is an optionally substituted amino group or an optionally substituted N-containing saturated heterocyclic group; n denotes an integer of 1 to 10, provided that when the ring B′ is a 5- to 7-membered ring, the ring B′ contains at least one nitrogen atom as hetero atom and n denotes an integer of 2 to 10, or a salt thereof. The compounds and salts thereof have an excellent cholinesterase inhibitory activity and antidepressant activity, and are useful as therapeutic and/or prophylactic medicaments of senile dementia.

    摘要翻译: 下式的化合物:其中环A是任选取代的苯环; 环B'是具有相同或不同的两个或更多个杂原子的任选取代的非芳族杂环; R1是氢原子或任选取代的烃基,其可以在重复n时彼此不同; Y是任选取代的氨基或任选取代的含N的饱和杂环基; n表示1〜10的整数,条件是当环B'为5-至7-元环时,环B'含有至少一个氮原子作为杂原子,n表示2至10的整数,或 其盐。 其化合物及其盐具有优异的胆碱酯酶抑制活性和抗抑郁活性,可用作老年性痴呆的治疗和/或预防药物。