公开(公告)号：US6005116A

公开(公告)日：1999-12-21

申请号：US148905

申请日：1998-08-26

申请人： Koichi Kojima ,  Junichi Sakai ,  Naozumi Samata ,  Masao Kozuka ,  Kenji Yoshimi ,  Tsugio Kaneko

发明人： Koichi Kojima ,  Junichi Sakai ,  Naozumi Samata ,  Masao Kozuka ,  Kenji Yoshimi ,  Tsugio Kaneko

IPC分类号： A61K31/42 ,  A61K31/422 ,  A61P25/16 ,  A61P25/28 ,  C07D261/10 ,  C07D261/12 ,  C07D413/04 ,  C07D417/04 ,  A61K31/425

CPC分类号： C07D413/04 ,  C07D261/12

摘要： Isoxazole compounds having the following general formula: ##STR1## wherein R.sup.1 represents an optionally substituted aryl group or aromatic heterocyclic group; R.sup.2 represents a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, an alkoxy group, a cyano group, a carboxyl group, an alkanoyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group; R.sup.3 represents an optionally substituted amino group or a saturated heterocyclic group; X represents an oxygen atom or a sulfur atom; and n is an integer of from 2 to 6. These compounds have excellent monoamine oxidase inhibitory activity and are useful as a therapeutic agent or a preventive agent against nervous diseases such as depression.

摘要翻译： 异恶唑化合物，其具有以下通式：其中R 1表示任选取代的芳基或芳族杂环基; R2表示氢原子，卤素原子，任选取代的烷基，烯基，炔基，环烷基，环烯基，烷氧基，氰基，羧基，烷酰基，烷氧基羰基 基团或任选取代的氨基甲酰基; R3表示任选取代的氨基或饱和杂环基; X表示氧原子或硫原子; n为2〜6的整数。这些化合物具有优异的单胺氧化酶抑制活性，可用作抑制诸如抑郁症等神经疾病的治疗剂或预防剂。

公开(公告)号：US5965591A

公开(公告)日：1999-10-12

申请号：US806854

申请日：1997-02-26

申请人： Koichi Kojima ,  Junichi Sakai ,  Yuichi Aizawa ,  Naozumi Samata ,  Masao Kozuka ,  Kenji Yoshimi ,  Isao Kaneko ,  Kazuo Koyama

发明人： Koichi Kojima ,  Junichi Sakai ,  Yuichi Aizawa ,  Naozumi Samata ,  Masao Kozuka ,  Kenji Yoshimi ,  Isao Kaneko ,  Kazuo Koyama

IPC分类号： A61K31/42 ,  A61K31/423 ,  A61K31/424 ,  A61K31/44 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  C07D261/20 ,  C07D498/02 ,  C07D498/04

CPC分类号： C07D261/20

摘要： An isoxazole compound having the following formula: wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 1; n is 1 to 6; ring A represents a phenyl ring or a naphthyl ring; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.

摘要翻译： 具有下式的异恶唑化合物：其中R 1表示氢，卤素，烷基，烷氧基，羟基，烷硫基，氨基，烷酰基，烷酰基氨基，烷酰氧基，烷氧基羰基，羧基，（烷硫基）硫代羰基，氨基甲酰基，硝基或氰基; R2代表氨基; m为1; n为1至6; 环A表示苯环或萘环; X表示氧或硫。 异恶唑化合物具有优异的单胺氧化酶抑制活性，可用于治疗帕金森病，抑郁症和阿尔茨海默氏病。

公开(公告)号：US6096771A

公开(公告)日：2000-08-01

申请号：US243885

申请日：1999-02-03

申请人： Koichi Kojima ,  Junichi Sakai ,  Yuichi Aizawa ,  Naozumi Samata ,  Masao Kozuka ,  Kenji Yoshimi ,  Isao Kaneko ,  Kazuo Koyama

发明人： Koichi Kojima ,  Junichi Sakai ,  Yuichi Aizawa ,  Naozumi Samata ,  Masao Kozuka ,  Kenji Yoshimi ,  Isao Kaneko ,  Kazuo Koyama

IPC分类号： A61K31/42 ,  A61K31/423 ,  A61K31/424 ,  A61K31/44 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  C07D261/20 ,  C07D498/02 ,  C07D498/04

CPC分类号： C07D261/20

摘要： An isoxazole compound having the following formula: ##STR1## wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 2 or 3; n is 1 to 6; ring A represents a phenyl ring, a naphthyl ring or an aromatic heterocycle; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.

摘要翻译： 具有下式的异恶唑化合物：其中R 1表示氢，卤素，烷基，烷氧基，羟基，烷硫基，氨基，烷酰基，烷酰基氨基，烷酰氧基，烷氧基羰基，羧基，（烷硫基）硫代羰基，氨基甲酰基，硝基或氰基; R2代表氨基; m为2或3; n为1至6; 环A表示苯环，萘环或芳香杂环; X表示氧或硫。 异恶唑化合物具有优异的单胺氧化酶抑制活性，可用于治疗帕金森病，抑郁症和阿尔茨海默氏病。