Use of idebenone and analogues against &bgr; amyloid induced cytotoxicity
    1.
    发明授权
    Use of idebenone and analogues against &bgr; amyloid induced cytotoxicity 失效
    使用艾地苯醌和类似物对β淀粉样蛋白诱导的细胞毒性

    公开(公告)号:US06271266B1

    公开(公告)日:2001-08-07

    申请号:US09180463

    申请日:1998-11-09

    IPC分类号: A61K31185

    CPC分类号: A61K31/047 A61K31/122

    摘要: A compound of the formula: wherein R1 represents a lower alkyl; R2 represents H, an optionally substituted alkyl or an optionally substituted alkenyl; R3 and R4 each represents an optionally substituted lower alkyl or a lower alkoxy, or R3 and R4 form, taken together, an optionally substituted butadienylene; and X1 and X2 each represents an optionally esterified or etherified hydroxy, or a salt thereof is useful for protecting cells from the cytotoxicity of &bgr;-amyloid protein.

    摘要翻译: 下式的化合物:其中R 1表示低级烷基; R 2表示H,任选取代的烷基或任选取代的烯基; R 3和R 4各自表示任选取代的低级烷基或低级烷氧基,或者R 3和R 4一起形成任选取代的亚二烯基; 并且X 1和X 2各自表示任选酯化或醚化的羟基,或其盐可用于保护细胞免受β-淀粉样蛋白的细胞毒性。

    Aminobenzene compounds to prevent nerve cell degradation
    2.
    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
    5.
    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。

    Heterocyclic compounds, their production and use
    6.
    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。

    Tetracyclic condensed heterocyclic compounds their production, and use
    7.
    发明授权
    Tetracyclic condensed heterocyclic compounds their production, and use 失效
    四环稠合杂环化合物的生产和使用

    公开(公告)号:US5814642A

    公开(公告)日:1998-09-29

    申请号:US681911

    申请日:1996-07-30

    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 acid 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酸或含氮饱和杂环基,其盐,抑制优异的胆碱酯酶抑制活性和单胺摄取抑制活性,因此可用作老年性痴呆的治疗和/或预防药物。