Benzylpiperidine compounds and their use
    21.
    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
    23.
    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.

    Peptide derivatives, their production and use
    27.
    发明授权
    Peptide derivatives, their production and use 失效
    肽衍生物,其生产和使用

    公开(公告)号:US4748154A

    公开(公告)日:1988-05-31

    申请号:US939103

    申请日:1986-12-08

    摘要: A peptide derivative of the general formula ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1-18 alkyl group or a substituted or unsubstituted phenyl C.sub.1-3 alkyl group;A is an amino or N--C.sub.1-6 alkylamino acid residue;B is a hydroxyl group, a substituted or unsubstituted amino group, or an amino acid or an amide thereof,or a physiologically acceptable salt thereof, can be advantageously used for the treatment and/or prevention of a disease including, among others, senile dementia (Alzheimer's dementia), cerebrovascular dementia, Alzheimer's disease, Pick's disease, Huntington's chorea, Creutzfeldt-Jakob disease, Parkinson's disease, and dementia due to spinocerebellar degeneration.

    摘要翻译: 通式为“IMAGE”的肽衍生物,其中R 1为氢原子,C 1-18烷基或取代或未取代的苯基C 1-3烷基; A是氨基或N-C 1-6烷基氨基酸残基; B是羟基,取代或未取代的氨基或氨基酸或其酰胺或其生理学上可接受的盐可有利地用于治疗和/或预防疾病,包括老年性痴呆 (阿尔茨海默氏痴呆症),脑血管性痴呆,阿尔茨海默病,皮克病,亨廷顿舞蹈病,克雅氏病,帕金森氏病和由脊髓小脑变性引起的痴呆。

    Isoindolinone derivatives, production and use thereof
    28.
    发明授权
    Isoindolinone derivatives, production and use thereof 失效
    异吲哚啉酮衍生物,其生产和使用

    公开(公告)号:US4695572A

    公开(公告)日:1987-09-22

    申请号:US774470

    申请日:1985-09-10

    摘要: A compound of the formula ##STR1## wherein X is hydrogen, halogen or nitro; Ar is phenyl or naphthyridinyl which may optionally be substituted; and either one of Z.sup.1 and Z.sup.2 is hydrogen and the other is lower alkanoyloxy or hydroxy, each of Z.sup.1 and Z.sup.2 is lower alkoxy, or Z.sup.1 and Z.sup.2 combinedly represent hydroxyimino, oxo or a group of the formula: ##STR2## in which Y is oxygen or sulfur and A is a branched or unbranched lower alkylene chain; and a salt thereof, act on the central nervous system but are weak in adverse effects such as hypnotic and muscle relaxant effects.

    摘要翻译: 式(Ⅰ)化合物,其中X是氢,卤素或硝基; Ar是任选被取代的苯基或萘啶基; 并且Z 1和Z 2中的任一个是氢,另一个是低级烷酰氧基或羟基,Z 1和Z 2各自是低级烷氧基,或者Z 1和Z 2组合地表示羟基亚氨基,氧代或下式的基团:其中Y是 氧或硫,A是支链或非支链的低级亚烷基链; 及其盐起作用于中枢神经系统,但是具有不利影响,例如催眠和肌肉松弛作用。

    Composition for inhibiting production or secretion of amyloid .beta.
protein to treat Down's syndrome
    29.
    发明授权
    Composition for inhibiting production or secretion of amyloid .beta. protein to treat Down's syndrome 失效
    用于抑制淀粉样蛋白β蛋白的产生或分泌以治疗唐氏综合征的组合物

    公开(公告)号:US5965568A

    公开(公告)日:1999-10-12

    申请号:US646354

    申请日:1996-05-10

    IPC分类号: A61K31/475 A61K31/44

    CPC分类号: A61K31/475

    摘要: A pharmaceutical composition for inhibiting production or secretion of amyloid .beta. protein, which comprises a compound of the formula (I): ##STR1## wherein ring A is an optionally substituted benzene ring, R represents OR.sup.1, ##STR2## or SR.sup.1, wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is selected from a hydrogen atom, an optionally substituted hydrocarbon group or R.sup.2 and R.sup.3, taken together with the adjacent nitrogen atom, form an optionally substituted nitrogen-containing heterocyclic group, and Y is an optionally substituted alkyl group, or a pharmaceutically acceptable salt thereof, if necessary, with a pharmaceutically acceptable excipient, carrier or diluent.

    摘要翻译: PCT No.PCT / JP96 / 00265 Sec。 371日期:1996年5月10日 102(e)日期1996年5月10日PCT提交1996年2月8日PCT公布。 WO96 / 25161 PCT出版物 日本1996年8月22日用于抑制淀粉样β蛋白的产生或分泌的药物组合物,其包含式(I)的化合物:其中环A是任选取代的苯环,R表示OR 1或SR 1,其中R 1,R 2 和R3相同或不同,各自选自氢原子,任选取代的烃基或与相邻的氮原子一起形成的R 2和R 3,形成任选取代的含氮杂环基,Y是任选取代的 烷基或其药学上可接受的盐,如果需要,与药学上可接受的赋形剂,载体或稀释剂。