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1. 发明授权

US6096771A Isoxazole derivatives 失效
标题翻译：异恶唑衍生物
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。

2. 发明授权

US5965591A Isoxazole derivatives 失效
标题翻译：异恶唑衍生物
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。

3. 发明授权

US6005116A Isoxazole compounds useful for the prophylaxis or treatment of nervous diseases 失效
标题翻译：用于预防或治疗神经疾病的异恶唑化合物
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。

4. 发明授权

US5321037A Isoxazole derivatives for use as cerebro-active drugs and central muscle relaxants 失效
标题翻译：异恶唑衍生物用作脑脊液药物和中枢肌肉松弛剂
公开(公告)号：US5321037A
公开(公告)日：1994-06-14
申请号：US26271
申请日：1993-03-04
申请人： Mitsuo Nagano , Junichi Sakai , Nobuyoshi Iwata , Kazuo Kobayashi , Masao Kozuka , Kenji Yoshimi , Katsunori Kato , Yoshiko Kubo , Toshiyuki Tonohiro , Takao Hara
发明人： Mitsuo Nagano , Junichi Sakai , Nobuyoshi Iwata , Kazuo Kobayashi , Masao Kozuka , Kenji Yoshimi , Katsunori Kato , Yoshiko Kubo , Toshiyuki Tonohiro , Takao Hara
IPC分类号： A61K31/42 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , C07D261/12 , C07D261/20
CPC分类号： A61K31/445 , A61K31/42 , A61K31/495 , A61K31/535 , A61K31/55 , C07D261/12 , C07D261/20
摘要： Compounds of formula (I): ##STR1## [in which: either (a) the dotted line ( ) is a single bond; A=is oxygen; and B is a group of formula (II): ##STR2## (in which m is 0 and n is 0 or 1) or (b) the dotted line ( ) is a double bond; A=is said group of formula (II) in which m is 1 and n is 0 or 1; and B is absent; and R.sup.1 is hydrogen, halogen, alkyl, alkenyl, alkynyl, optionally substituted benzyl or optionally substituted phenyl; R.sup.2 is hydrogen, halogen, alkyl, optionally substituted phenyl or heterocyclic; or R.sup.1 and R.sup.2, together with the carbon atoms to which they are attached, are a hydrocarbon ring fused to the isoxazole ring; R.sup.3 and R.sup.4 are each hydrogen, alkyl, optionally substituted benzyl or optionally substituted phenyl; or R.sup.3, R.sup.4 and the nitrogen atom to which they are attached together represent an alicyclic amino group]; and salts thereof may be used for the treatment of cerebral circulatory problems and for use as centrally acting muscle relaxants.
摘要翻译：（I）化合物：其中：（a）虚线（）是单键; A =是氧; （II）（其中m为0且n为0或1）或（b）虚线（）为双键的式（II）的基团： A =是式（II）的基团，其中m是1，n是0或1; B不存在 R 1为氢，卤素，烷基，烯基，炔基，任选取代的苄基或任选取代的苯基; R2是氢，卤素，烷基，任选取代的苯基或杂环; 或R 1和R 2与它们所连接的碳原子一起是与异恶唑环稠合的烃环; R 3和R 4各自为氢，烷基，任选取代的苄基或任选取代的苯基; 或R 3，R 4和它们所连接的氮原子一起表示脂环族氨基]。其盐可用于治疗脑循环问题并用作中枢肌肉松弛剂。

5. 发明授权

US5116839A Use of isoxazolin-3-one derivatives as antidepressants 失效
标题翻译：使用ISOXAZOLIN-3-ONE衍生物作为抗病毒剂
公开(公告)号：US5116839A
公开(公告)日：1992-05-26
申请号：US537517
申请日：1990-06-13
申请人： Nobuyoshi Iwata , Kenji Yoshimi , Mitsuo Nagano
发明人： Nobuyoshi Iwata , Kenji Yoshimi , Mitsuo Nagano
IPC分类号： A61K9/48 , A61K31/41 , A61K31/42 , A61K31/535 , A61K38/01
CPC分类号： A61K31/535 , A61K31/42
摘要： A method of treating depression comprising administering to a patient an effective antidepressive amount of a compound of the formula (I) ##STR1## wherein the endocyclic dotted line ##STR2## is a single bond; the exocyclic dotted line ##STR3## is a double bond; A is oxygen; B is a group of the formula (II) ##STR4## wherein m is 0 and n is 0 or 1; R.sup.3, R.sup.4 and the nitrogen to which they are attached together represent an alicyclic amino having a total of 5 or 6 ring atoms, of which one ring atom is the nitrogen and one ring atom is optionally an additional heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, the alicyclic amino being unsubstituted or, where there is an additional nitrogen heteroatom, the alicyclic amino having as a substituent a C.sub.1 -C.sub.3 alkyl on the additional nitrogen heteroatom; R.sup.1 is hydrogen or halogen; and R.sup.2 is an unsubstituted phenyl, a substituted phenyl having a substituent selected from the group consisting of C.sub.1-3 alkyl, C.sub.1-3 alkoxy, halogen and nitro, an unsubstituted 5- or 6-membered heterocyclic group having one or more of oxygen, sulfur or a nitrogen as heteroatoms, or a substituted 5- or 6-membered heterocyclic group having one or more of oxygen, sulfur or a nitrogen as heteroatoms and having at least one substituent selected from the group consisting of C.sub.1 -C.sub.3 alkyl, C.sub.1-3 alkoxy, halogen and nitro; or a pharmaceutically acceptable acid addition salt thereof.

6. 发明授权

US5262413A Use of isoxazolin-3-one derivatives as antidepressants 失效
标题翻译：异恶唑啉-3-酮衍生物作为抗抑郁药的使用
公开(公告)号：US5262413A
公开(公告)日：1993-11-16
申请号：US11208
申请日：1993-01-29
申请人： Nobuyoshi Iwata , Kenji Yoshimi , Mitsuo Nagano
发明人： Nobuyoshi Iwata , Kenji Yoshimi , Mitsuo Nagano
IPC分类号： A61K31/42 , A61K31/535 , A61K31/41 , A61K31/54
CPC分类号： A61K31/535 , A61K31/42
摘要： A method of treating depression comprising administering to a patient an effective amount of a compound of the formula (Ib): ##STR1## wherein R.sup.1b is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, an unsubstituted benzyl group, a substituted benzyl having at least one substitutent (b) selected from the group consisting of C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, hydroxy, halogen, nitro, amino and C.sub.2 -C.sub.4 aliphatic carboxylic acylamino; unsubstituted phenyl or a substituted phenyl having at least one substitutent (b); R.sup.2b is hydrogen, C.sub.1 -C.sub.4 alkyl, unsubstituted phenyl, substituted phenyl having at least one substitutent (b), unsubstituted 5- or 6- membered heterocyclic having an oxygen, sulfur or nitrogen as a heteroatom, or substituted 5- or 6- membered heterocyclic having an oxygen, sulfur or nitrogen as a heteroatom and having at least one substitutent (b); and R.sup.3b and R.sup.4b are the same or different and each is hydrogen, C.sub.1 -C.sub.4 alkyl, unsubstituted benzyl, substituted benzyl having at least one substituent (b), unsubstituted phenyl, or substituted phenyl having at least one substitutent (b); or R.sup.3b, R.sup.4b and the nitrogen atom to which they are attached together represent an alicyclic amino group having a total of 5 or 6 ring atoms, or which one ring atom is the nitrogen atom and one ring atom is optionally an additional heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, the alicyclic amino group being unsubstituted or, where there is an additional nitrogen heteroatom, the alicyclic amino group having a C.sub.1 -C.sub.3 alkyl substitutent on the additional nitrogen heteroatom; or a pharmacologically acceptable acid addition salt thereof.
摘要翻译：治疗抑郁症的方法包括向患者施用有效量的式（Ib）化合物：其中R 1b是氢，卤素，C 1 -C 4烷基，C 2 -C 4烯基，C 2 -C 4炔基，未取代的苄基，具有至少一个选自C 1 -C 3烷基，C 1 -C 3烷氧基，羟基，卤素，硝基，氨基和C 2 -C 4脂族羧酸酰基氨基的取代基（b）的取代苄基; 未取代的苯基或具有至少一个取代基（b）的取代苯基; R2b是氢，C1-C4烷基，未取代的苯基，具有至少一个取代基（b）的取代苯基，具有氧，硫或氮作为杂原子的未取代的5-或6-元杂环，或取代的5-或6-元具有氧，硫或氮作为杂原子且具有至少一个取代基（b）的杂环基; 并且R 3b和R 4b相同或不同，各自为氢，C 1 -C 4烷基，未取代的苄基，具有至少一个取代基的取代苄基（b），未取代的苯基或具有至少一个取代基（b）的取代的苯基。或R 3b，R 4b和它们所连接的氮原子一起表示具有总共5或6个环原子的脂环族氨基，或者一个环原子是氮原子，一个环原子任选地是选自以下的杂原子：由氮，氧和硫组成的组，脂环族氨基是未取代的，或者在另外的氮杂原子上，在另外的氮杂原子上具有C1-C3烷基取代基的脂环族氨基; 或其药理学上可接受的酸加成盐。

7. 发明授权

US5217970A Use of isoxazolin-3-one derivatives as antidepressants 失效
标题翻译：异恶唑啉-3-酮衍生物作为抗抑郁药的使用
公开(公告)号：US5217970A
公开(公告)日：1993-06-08
申请号：US856494
申请日：1992-03-24
申请人： Nobuyoshi Iwata , Kenji Yoshimi , Mitsuo Nagano
发明人： Nobuyoshi Iwata , Kenji Yoshimi , Mitsuo Nagano
IPC分类号： A61K31/42 , A61K31/535
CPC分类号： A61K31/535 , A61K31/42
摘要： A method of treating depression comprising administering to a patient an effective antidepressive amount of a compound of the formula ##STR1## wherein either (i) the endocyclic dotted line ( ) is a double bond; the exoxyclic dotted line ( ) is a single bond;A is ##STR2## m is 1; n is 0; R.sup.3 and R.sup.4 are hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl or phenyl or R.sup.3, R.sup.4 and the nitrogen to which they are attached represent an alicyclic amino having 5 or 6 ring atoms, of which one ring atom is nitrogen and one ring atom is optionally an additional nitrogen, oxygen or sulfur heteroatom; R.sup.1 is hydrogen, halogen C.sub.1 -C.sub.4 alkyl C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, benzyl or phenyl; and R.sup.2 is hydrogen, C.sub.1 -C.sub.4 alkyl phenyl or a 5- or 6- membered heterocyclic; or(ii) the endocyclic dotted line ( ) is a single bond; the exocyclic dotted line ( ) is a double bond;A is oxygen;B is ##STR3## m is 0; n is 1; R.sup.3, R.sup.4 and the nitrogen to which they are attached together represent an alicyclic amino group having 5 or 6 ring atoms, of which one ring atom is nitrogen and one ring atom is optionally an additional nitrogen, oxygen or sulfur heteroatom; and R.sup.1 and R.sup.2, together with the carbon to which they are attached, represent phenyl fused to the isoxazole ring.
摘要翻译：一种治疗抑郁症的方法，包括向患者施用有效的抗抑郁量的下式化合物，其中（i）内环虚线（）是双键; 外消旋虚线（）是单键; A是 m是1; n为0; R3和R4是氢，C1-C4烷基，苄基或苯基或R3，R4，它们所连接的氮代表具有5或6个环原子的脂环族氨基，其中一个环原子是氮，一个环原子是任选的另外的氮，氧或硫杂原子; R1是氢，卤素C1-C4烷基C2-C4烯基，C2-C4炔基，苄基或苯基; 和R 2是氢，C 1 -C 4烷基苯基或5-或6-元杂环; 或（ii）内环虚线（）是单键; 环外虚线（）是双键; A是氧气; B是 m是0; n为1; R3，R4和它们所连接的氮一起表示具有5或6个环原子的脂环族氨基，其中一个环原子是氮，一个环原子任选地是另外的氮，氧或硫杂原子; 并且R 1和R 2与它们所连接的碳一起表示与异恶唑环稠合的苯基。

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