公开(公告)号：US5527811A

公开(公告)日：1996-06-18

申请号：US274263

申请日：1994-07-13

申请人： Hideaki Natsugari ,  Tetsuji Imamoto ,  Yuzo Ichimori

发明人： Hideaki Natsugari ,  Tetsuji Imamoto ,  Yuzo Ichimori

IPC分类号： C07D217/24 ,  C07D401/12 ,  C07D521/00 ,  A61K31/47 ,  C07D405/06

CPC分类号： C07D231/12 ,  C07D217/24 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12

摘要： Compounds represented by the formula: ##STR1## wherein the ring A and the ring B each stand for an optionally substituted benzene ring; Ar stands for an optionally substituted aryl group or an optionally substituted heterocyclic group; Q stands for an oxygen atom or a sulfur atom; R stands for a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted hydroxyl group or an optionally substituted amino group; X stands for --O-- or --NR.sup.1 -- wherein R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon group; Y stands for --O--, --NR.sup.2 -- wherein R.sup.2 stands for a hydrogen atom or an optionally substituted hydrocarbon group, or a bond; m denotes 1, 2 or 3, and n denotes 0, 1 or 2, and salts thereof which have excellent calcium- or substance P receptor-antagonistic activity, being useful for treating a cerebralvascular disorder in mammals such as cerebralischemia, cerebral edema and neuronal damage, their production and use.

摘要翻译： 由下式表示的化合物：其中环A和环B各自代表任选取代的苯环; Ar表示任选取代的芳基或任选取代的杂环基; Q代表氧原子或硫原子; R代表氢原子，任选取代的烃基，任选取代的羟基或任选取代的氨基; X代表-O-或-NR1-，其中R1代表氢原子或任选取代的烃基; Y代表-O-，-NR2-，其中R2代表氢原子或任选取代的烃基，或键; m表示1,2或3，n表示0,1或2，其具有优异的钙或物质P受体拮抗活性的盐可用于治疗哺乳动物如脑缺血，脑水肿和神经元的脑血管障碍 损坏，生产和使用。

公开(公告)号：US5294625A

公开(公告)日：1994-03-15

申请号：US964851

申请日：1992-12-18

申请人： Giichi Goto ,  Hidefumi Yukimasa ,  Tetsuji Imamoto

发明人： Giichi Goto ,  Hidefumi Yukimasa ,  Tetsuji Imamoto

IPC分类号： C12N9/99 ,  A61K31/00 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/451 ,  A61P9/00 ,  A61P25/28 ,  C07D211/26 ,  C07D211/32 ,  C07D211/70 ,  C07D213/36 ,  C07D213/38 ,  C07D213/50 ,  C07D521/00 ,  A61K31/443

CPC分类号： C07D231/12 ,  C07D211/26 ,  C07D211/32 ,  C07D211/70 ,  C07D213/38 ,  C07D213/50 ,  C07D233/56 ,  C07D249/08

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。

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。

公开(公告)号：US06251861B1

公开(公告)日：2001-06-26

申请号：US08881878

申请日：1997-06-24

申请人： Tetsuji Imamoto ,  Yasutaka Nagisa

发明人： Tetsuji Imamoto ,  Yasutaka Nagisa

IPC分类号： A61K3812

CPC分类号： A61K38/12 ,  A61K38/08

摘要： A pharmaceutical composition comprising a compound having anti-endothelin activity is useful for the prophylaxis or treatment of cerebral infarction.

摘要翻译： 包含具有抗内皮素活性的化合物的药物组合物可用于预防或治疗脑梗死。

公开(公告)号：US5441967A

公开(公告)日：1995-08-15

申请号：US171163

申请日：1993-12-22

申请人： Giichi Goto ,  Hidefumi Yukimasa ,  Tetsuji Imamoto

发明人： Giichi Goto ,  Hidefumi Yukimasa ,  Tetsuji Imamoto

IPC分类号： C12N9/99 ,  A61K31/00 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/451 ,  A61P9/00 ,  A61P25/28 ,  C07D211/26 ,  C07D211/32 ,  C07D211/70 ,  C07D213/36 ,  C07D213/38 ,  C07D213/50 ,  C07D521/00 ,  C07D401/04

CPC分类号： C07D231/12 ,  C07D211/26 ,  C07D211/32 ,  C07D211/70 ,  C07D213/38 ,  C07D213/50 ,  C07D233/56 ,  C07D249/08

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, .sub.-- means either a single bond or a double bond (provided that when A means a bond, .sub.-- 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， - 表示单键或双键（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。

公开(公告)号：US5177087A

公开(公告)日：1993-01-05

申请号：US461114

申请日：1990-01-04

申请人： Giichi Goto ,  Hidefumi Yukimasa ,  Tetsuji Imamoto

发明人： Giichi Goto ,  Hidefumi Yukimasa ,  Tetsuji Imamoto

IPC分类号： C12N9/99 ,  A61K31/00 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/451 ,  A61P9/00 ,  A61P25/28 ,  C07D211/26 ,  C07D211/32 ,  C07D211/70 ,  C07D213/36 ,  C07D213/38 ,  C07D213/50 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D211/26 ,  C07D211/32 ,  C07D211/70 ,  C07D213/38 ,  C07D213/50 ,  C07D233/56 ,  C07D249/08

摘要： There is provided 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.