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35 条记录 (耗时 0.02 秒)

    Peptide derivatives, their production and use
    1.
    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

    申请人： Giichi Goto ,  Akinobu Nagaoka ,  Mitsuhiro Wakimasu

    发明人： Giichi Goto ,  Akinobu Nagaoka ,  Mitsuhiro Wakimasu

    IPC分类号： C07K14/575 ,  A61K38/00 ,  A61K38/11 ,  A61P25/00 ,  C07K1/02 ,  C07K1/113 ,  C07K7/06 ,  C07K7/16 ,  A61K37/02

    CPC分类号： C07K7/16 ,  A61K38/00 ,  Y02P20/55 ,  Y10S930/26

    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。

    Method for improving brain function using cholinesterase-inhibiting aminoketone compounds
    3.
    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

    申请人： Giichi Goto ,  Akinobu Nagaoka ,  Yuji Ishihara

    发明人： Giichi Goto ,  Akinobu Nagaoka ,  Yuji Ishihara

    IPC分类号： A61K31/135 ,  A61K31/40 ,  C07C225/16 ,  C07D295/108

    CPC分类号： C07D295/108 ,  A61K31/135 ,  A61K31/40 ,  C07C225/16

    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。

    Azaspiro compounds and their use
    4.
    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

    申请人： Giichi Goto ,  Akinobu Nagaoka

    发明人： Giichi Goto ,  Akinobu Nagaoka

    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.

    Composition for inhibiting production or secretion of amyloid .beta. protein to treat Down's syndrome
    7.
    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

    申请人： Mitsuru Kakihana ,  Takuo Kosaka ,  Akinobu Nagaoka ,  Giichi Goto

    发明人： Mitsuru Kakihana ,  Takuo Kosaka ,  Akinobu Nagaoka ,  Giichi Goto

    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。

    Inhibitor of vascular permeability enhancer
    9.
    发明授权
    Inhibitor of vascular permeability enhancer 失效
    血管通透性增强剂的抑制剂

    公开(公告)号：US5604210A

    公开(公告)日：1997-02-18

    申请号：US456723

    申请日：1995-06-01

    申请人： Akinobu Nagaoka ,  Tetsuji Imamoto ,  Tsuneo Asano ,  Yoshihiro Sugiura ,  Giichi Goto

    发明人： Akinobu Nagaoka ,  Tetsuji Imamoto ,  Tsuneo Asano ,  Yoshihiro Sugiura ,  Giichi Goto

    IPC分类号： A61K31/52 ,  A61K31/70

    CPC分类号： A61K31/7076

    摘要： The present invention relates to prevention or treatment a brain edema, an intracranial hemorrhage and a cerebral infarction by administering a pharmaceutically effective amount of a compound or a pharmaceutically acceptable salt thereof, for inhibiting a vascular permeability enhancer, which the compound is of the formula: ##STR1## wherein A is halogen, --X--R.sup.3 in which X is O, S, NH or NHNH, and R.sup.3 is H, acyl, a hydrocarbon group or an aromatic heterocyclic group, or --Y.dbd.R.sup.4 in which Y is N or NHN, and R.sup.4 is a divalent hydrocarbon group, and R.sup.1 is H, halogen, a hydrocarbon group, a heterocyclic group or --Z--R.sup.5 in which Z is O, S or NH, and R.sup.5 is H, a hydrocarbon group or an aromatic heterocyclic group;R.sup.2 is H, halogen, a hydrocarbon group or a heterocyclic group;B is --W--R.sup.6 in which W is CH.sub.2, CO or CS, and R.sup.6 is OH, alkoxy, acyloxy, alkylsulfinyl, alkylsulfonyl, phosphoric acid or amino, or B together with E form a cyclic phosphoric ester; andD and E are H, amino, azido, halogen or OH.

    摘要翻译： 本发明涉及通过施用药学有效量的化合物或其药学上可接受的盐来抑制血管通透性增强剂来预防或治疗脑水肿，颅内出血和脑梗死，该化合物具有下式： （I）其中A是卤素，X-R 3，其中X是O，S，NH或NHNH，R 3是H，酰基，烃基或芳族杂环基，或-Y = R 4，其中 Y是N或NHN，R4是二价烃基，R1是H，卤素，烃基，杂环基或-Z-R5，其中Z是O，S或NH，R5是H，烃 基团或芳族杂环基团; R2是H，卤素，烃基或杂环基; B为-W-R 6，其中W为CH 2，CO或CS，R 6为OH，烷氧基，酰氧基，烷基亚磺酰基，烷基磺酰基，磷酸或氨基，或B与E一起形成环状磷酸酯; 并且D和E是H，氨基，叠氮基，卤素或OH。