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1. 发明授权

US5134147A 1,2-benzisoxazole compounds 失效
标题翻译： 1,2-苯并异恶唑化合物
公开(公告)号：US5134147A
公开(公告)日：1992-07-28
申请号：US779828
申请日：1991-10-21
申请人： Jean L. Peglion , Francis Colpaert
发明人： Jean L. Peglion , Francis Colpaert
IPC分类号： A61K31/44 , A61K31/445 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D413/04 , C07D413/06 , C07D413/14 , C07D471/04 , C07D493/04
CPC分类号： C07D413/04 , C07D413/14 , C07D471/04 , C07D493/04
摘要： Compounds of formula I ##STR1## in which m represents an integer from 0 to 5, n represents an integer from 1 to 2, p is equal to 0, 1 or 2,X, Y and Z, which may be identical or different, each represent a hydrogen atom, a halogen atom, a linear or branched alkyl radical, a trifluoromethyl radical, an alkoxy radical, an alkylthio radical or a hydroxyl radical, andR represents a 2-benzofuranyl or 2,3-dihydro-2-benzofuranyl radical (it being possible for each to be substituted on the benzene ring), a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran-2-yl radical, a 4-oxo-4H-chromen-2-yl radical (optionally substituted on the benzene ring), a benzocyclobutenyl radical of formula A or an indanyl radical of formula B: ##STR2## (in which: R.sub.1 and R.sub.2, which may be identical or different, each represent a hydrogen atom, a halogen atom, a trifluoromethyl radical, an alkyl radical, an alkoxy radical, a hydroxyl radical, a hydroxyalkyl radical or an alkylthio radical, or together form a methylenedioxy radical or an ethylenedioxy radical, and R.sub.3 represents a hydrogen atom or a linear or branched alkyl radical having 1 to 6 carbon atoms),or a radical of formula C: ##STR3## (in which R.sub.4, R.sub.5 and R.sub.6, which may be identical or different, each represent a hydrogen atom, a halogen atom, a trifluoromethyl radical, a hydroxyl radical, an alkyl radical, an alkoxy radical or an alkylthio radical,their optical isomers and their addition salts with a pharmaceutically acceptable organic or inorganic acid.
摘要翻译：式I的化合物（I）其中m表示0至5的整数，n表示1至2的整数，p等于0,1或2，X，Y和Z可以相同或不同的，各自表示氢原子，卤素原子，直链或支链烷基，三氟甲基，烷氧基，烷硫基或羟基，R表示2-苯并呋喃基或2,3-二氢 - 2-苯并呋喃基（每个可以在苯环上取代），2,3,6,7-四氢苯并[1,2-b：4,5-b']二呋喃-2-基， 4-氧代-4H-色烯-2-基（在苯环上任选取代），式A的苯并环丁烯基或式B的茚满基基团：（A）（B）（B）其中R 1和R 2可以相同或不同，各自表示氢原子，卤素原子，三氟甲基，烷基，烷氧基，羟基，羟基烷基或烷硫基，或一起用于（C）（其中R 4，R 5和R 6）的基团，其中R 1，R 2，R 3，R 4，R 5，R 6和R 6独立地选自氢原子或具有1至6个碳原子的直链或支链烷基）其可以相同或不同，各自表示氢原子，卤素原子，三氟甲基，羟基，烷基，烷氧基或烷硫基，它们的光学异构体及其与药学上可接受的有机物的加成盐或无机酸。

2. 发明授权

US5026863A 1,4-dihydropyridine compounds 失效
标题翻译： 1,4-二氢吡啶化合物
公开(公告)号：US5026863A
公开(公告)日：1991-06-25
申请号：US518019
申请日：1990-05-02
申请人： Jean L. Peglion , Yves M. Gargouil , Jean P. Vilaine
发明人： Jean L. Peglion , Yves M. Gargouil , Jean P. Vilaine
IPC分类号： C07D211/90 , C07D401/12 , C07D405/04
CPC分类号： C07D401/12 , C07D211/90 , C07D405/04
摘要： The invention relates to new compounds of formula I: ##STR1## in which Ar represents a phenyl radical having one to five identical or different substituents selected from chloro or fluoro,Y, Z, Y.sub.1 and Z.sub.1, which may be identical or different, each represents a hydrogen atom, a straight-chain or branched lower alkyl radical containing 1 to 4 carbon atoms, a cyclopropyl radical, a dicyclopropylmethyl radical, a 2,2-dicyclopropylethyl radical, a 2,2-dicyclopropylethenyl radical, a 3,3-dicyclopropylpropyl radical, a 3,3-dicyclopropyl-1-propenyl radical, a straight-chain or branched alkenyl radical containing 2 to 5 carbon atoms or a phenyl radical substituted with a nitro radical,W represents a straight-chain or branched lower alkyl radical containing 1 to 4 carbon atoms,V represents an oxygen atom,U represents a methyleneoxy radical or an ethyleneoxy radical,m and n, which may be identical or different, each represents an integer which may take a value from 2 to 4, inclusive, R.sub.1 and R.sub.2, which may be identical or different, each represents a hydrogen atom, a straight-chain or branched lower alkyl radical containing 1 to 4 carbon atoms, or a straight-chain or branched lower alkenyl radical containing 2 to 4 carbon atoms,in the racemic form or in the form of an optical isomer, or an the addition salts thereof with a pharmaceutically acceptable inorganic or organic acid.Medicinal products.
摘要翻译：本发明涉及新的式I化合物：其中Ar表示具有1-5个相同或不同的选自氯或氟，Y，Z，Y 1和Z 1的取代基的苯基，其可以相同或相同，各自表示氢原子，含有1至4个碳原子的直链或支链低级烷基，环丙基，二环丙基甲基，2,2-二环丙基乙基，2,2-二环戊基苯基，3 3-二环丙基丙基，3,3-二环丙基-1-丙烯基，含2至5个碳原子的直链或支链烯基或被硝基取代的苯基，W代表直链或支链含有1〜4个碳原子的低级烷基，V表示氧原子，U表示亚甲基氧基或亚乙基氧基，m和n可以相同或不同，表示可以取2〜4的整数，包括，R1 an d R2可以相同或不同，各自表示氢原子，含有1至4个碳原子的直链或支链低级烷基，或含有2至4个碳原子的直链或支链低级烯基，其中外消旋形式或旋光异构体的形式，或其与药学上可接受的无机或有机酸的加成盐。药用产品。

3. 发明授权

US5100902A 1,2-benzisoxazole compounds 失效
标题翻译： 1,2-苯并噻唑化合物
公开(公告)号：US5100902A
公开(公告)日：1992-03-31
申请号：US604789
申请日：1990-10-26
申请人： Jean L. Peglion , Francis Colpaert
发明人： Jean L. Peglion , Francis Colpaert
IPC分类号： A61K31/44 , A61K31/445 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D413/04 , C07D413/06 , C07D413/14 , C07D471/04 , C07D493/04
CPC分类号： C07D413/04 , C07D413/14 , C07D471/04 , C07D493/04
摘要： Compounds of formula I ##STR1## in which m represents an integer from 0 to 5, n represents an integer from 1 to 2, p is equal to 0, 1 or 2,X, Y and Z, which may be identical or different, each represent a hydrogen atom, a halogen atom, a linear or branched alkyl radical, a trifluoromethyl radical, an alkoxy radical, an alkylthio radical or a hydroxyl radical, andR represents a 2-benzofuranyl or 2,3-dihydro-2-benzofuranyl radical (it being possible for each to be substituted on the benzene ring), a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran-2-yl radical, a 4-oxo-4H-chromen-2-yl radical (optionally substituted on the benzene ring), a benzocyclobutenyl radical of formula A or an indanyl radical of formula B: ##STR2## (in which: R.sub.1 and R.sub.2, which may be identical or different, each represent a hydrogen atom, a halogen atom, a trifluoromethyl radical, an alkyl radical, an alkoxy radical, a hydroxyl radical, a hydroxyalkyl radical or an alkylthio radical, or together form a methylenedioxy radical or an ethylenedioxy radical, and R.sub.3 represents a hydrogen atom or a linear or branched alkyl radical having 1 to 6 carbon atoms),or a radical of formula C: ##STR3## (in which R.sub.4, R.sub.5 and R.sub.6, which may be identical or different, each represent a hydrogen atom, a halogen atom, a trifluoromethyl radical, a hydroxyl radical, an alkyl radical, an alkoxy radical or an alkylthio radical,their optical isomers and their addition salts with a pharmaceutically acceptable organic or inorganic acid.
摘要翻译：式I的化合物（I）其中m表示0至5的整数，n表示1至2的整数，p等于0,1或2，X，Y和Z可以相同或不同的，各自表示氢原子，卤素原子，直链或支链烷基，三氟甲基，烷氧基，烷硫基或羟基，R表示2-苯并呋喃基或2,3-二氢 - 2-苯并呋喃基（每个可以在苯环上取代），2,3,6,7-四氢苯并[1,2-b：4,5-b']二呋喃-2-基， 4-氧代-4H-色烯-2-基（在苯环上任选取代），式A的苯并环丁烯基或式B的茚满基基团：（A）（B）（B）其中R 1和R 2可以相同或不同，各自表示氢原子，卤素原子，三氟甲基，烷基，烷氧基，羟基，羟基烷基或烷硫基，或一起用于（C）（其中R 4，R 5和R 6）的基团，其中R 1，R 2，R 3，R 4，R 5，R 6和R 6独立地选自氢原子或具有1至6个碳原子的直链或支链烷基）其可以相同或不同，各自表示氢原子，卤素原子，三氟甲基，羟基，烷基，烷氧基或烷硫基，它们的光学异构体及其与药学上可接受的有机物的加成盐或无机酸。

4. 发明授权

US4874878A Certain dihydrobenzofuran butanoic and pentanoic acid derivatives 失效
标题翻译：某些二氢苯并呋喃丁酸和戊酸衍生物
公开(公告)号：US4874878A
公开(公告)日：1989-10-17
申请号：US301160
申请日：1989-01-24
申请人： Jean L. Peglion , Jean C. Poignant , Joel Vian
发明人： Jean L. Peglion , Jean C. Poignant , Joel Vian
IPC分类号： A61K31/34 , A61K31/343 , A61P25/20 , A61P25/24 , A61P25/26 , C07D307/77 , C07D307/79 , C07D307/91 , C07D307/92 , C07D307/93 , C07D409/12
CPC分类号： C07D307/79 , C07D307/92 , C07D307/93 , C07D409/12
摘要： Compounds of the general formula I ##STR1## in which R.sub.1 and R.sub.2, which may be identical or different, each denote a hydrogen atom, a benzyl radical, a cyclohexylmethyl radical or a linear or branched alkyl radical containing from 1 to 10 carbon atoms, optionally substituted with a hydroxy radical, with a carboxy radical or with an alkoxy radical having 1 to 5 carbon atoms, with an alkoxycarbonyl radical having 2 to 6 carbon atoms, with an alkylphenyl radical having 7 to 16 carbon atoms or with a 2-alkylthienyl radical having 5 to 14 carbon atoms,R.sub.3 denotes a hydrogen atom or a linear or branched alkyl radical containing from 1 to 4 carbon atoms,A denotes a single bond or a methylene radical, or a radical of formula ##STR2## in which R.sub.4 is a linear or branched alkyl radical containing from 1 to 4 carbon atoms. These products are useful in anti-depressant, anti-aggressive, or dopaminergic modulation therapy and the corresponding bicyclic compounds are useful as intermediates for ring closure and production of the tricyclic compounds having the foregoing formula.
摘要翻译：通式I的化合物其中R 1和R 2可以相同或不同，分别表示氢原子，苄基，环己基甲基或含有1-10个碳原子的直链或支链烷基，任选被羟基取代，具有羧基或具有1至5个碳原子的烷氧基，具有2至6个碳原子的烷氧基羰基，具有7至16个碳原子的烷基苯基或具有2-烷基噻吩基具有5至14个碳原子的基团，R 3表示氢原子或含有1至4个碳原子的直链或支链烷基，A表示单键或亚甲基，或者式为“IMAGE”的基团，其中R4为含有1至4个碳原子的直链或支链烷基。这些产品可用于抗抑郁剂，抗侵袭性或多巴胺能调节疗法，并且相应的双环化合物可用作闭环和制备具有上述配方的三环化合物的中间体。

5. 发明授权

US4851429A Pharmaceutically useful tricyclic amines derived from 2,3,5,6,7,8-hexahydronaphtho(2,3-B)furan and from 2,3,6,7,8,9-hexahydro-5H-benzocyclohepta(2,3-B)furan 失效
标题翻译：衍生自2,3,5,6,7,8-六氢萘并（2,3-B）呋喃的化学有用的三环胺和2,3,6,7,8,9-六氢-5H-苯并环庚三烯（2,3 -B）呋喃
公开(公告)号：US4851429A
公开(公告)日：1989-07-25
申请号：US173286
申请日：1988-03-25
申请人： Jean L. Peglion , Jean C. Poignant , Joel Vian
发明人： Jean L. Peglion , Jean C. Poignant , Joel Vian
IPC分类号： A61K31/34 , A61K31/343 , A61P25/20 , A61P25/24 , A61P25/26 , C07D307/77 , C07D307/79 , C07D307/91 , C07D307/92 , C07D307/93 , C07D409/12
CPC分类号： C07D307/79 , C07D307/92 , C07D307/93 , C07D409/12
摘要： Compound of general formula I ##STR1## in which R.sub.1 and R.sub.2, which may be identical or different, each denote a hydrogen atom, a benzyl radical, a cyclohexylmethyl radical or a linear or branched alkyl radical containing from 1 to 10 carbon atoms, optionally substituted with a hydroxy radical, with a carboxy radical or with an alkoxy radical having 1 to 5 carbon atoms, with an alkoxycarbonyl radical having 2 to 6 carbon atoms, with an alkylphenyl radical having 7 to 16 carbon atoms or with a 2-alkylthienyl radical having 5 to 14 carbon atoms,R.sub.3 denotes a hydrogen atom or a linear or branched alkyl radical containing from 1 to 4 carbon atoms,A denotes a single bond or a methylene radical, or a radical of formula ##STR2## in which R.sub.4 is a linear or branched alkyl radical containing from 1 to 4 carbon atoms.These products are useful in anti-depressant, anti-aggressive, or dopaminergic modulation therapy and the corresponding bicyclic compounds are useful as intermediates for ring closure and production of the tricyclic compounds having the foregoing formula.
摘要翻译：通式I的化合物其中R 1和R 2可以相同或不同，分别表示氢原子，苄基，环己基甲基或含有1-10个碳原子的直链或支链烷基，任选地被羟基取代，具有羧基或具有1至5个碳原子的烷氧基，具有2至6个碳原子的烷氧基羰基，具有7至16个碳原子的烷基苯基或2-烷基噻吩基具有5至14个碳原子，R 3表示氢原子或含有1至4个碳原子的直链或支链烷基，A表示单键或亚甲基，或下式的基团：其中R 4为含有1至4个碳原子的直链或支链烷基。这些产品可用于抗抑郁剂，抗侵袭性或多巴胺能调节疗法，并且相应的双环化合物可用作闭环和制备具有上述配方的三环化合物的中间体。

6. 发明授权

US4983740A Process for 1,4-dihydropyridine compounds 失效
标题翻译： 1,4-二氢吡啶化合物的方法
公开(公告)号：US4983740A
公开(公告)日：1991-01-08
申请号：US386430
申请日：1989-07-27
申请人： Jean L. Peglion , Yves M. Gargouil , Jean P. Vilaine
发明人： Jean L. Peglion , Yves M. Gargouil , Jean P. Vilaine
IPC分类号： C07D211/90 , C07D401/12 , C07D405/04
CPC分类号： C07D401/12 , C07D211/90 , C07D405/04
摘要： The invention relates to a process for producing new compounds of formula I: ##STR1## and isomers thereof, as well as acid addition salts thereof, in which the symbols have the meanings set forth in the specification.
摘要翻译：本发明涉及一种制备新的式I化合物的方法：其中符号具有本说明书中阐述的含义的式I（I）及其异构体及其酸加成盐。

7. 发明授权

US4885373A 2,4,5,6,7,8-Hexahydronaphtho[2,3-b]furan useful as an intermediate 失效
标题翻译： 2,4,5,6,7,8-六氢萘并[2,3-b]呋喃，可用作中间体
公开(公告)号：US4885373A
公开(公告)日：1989-12-05
申请号：US303545
申请日：1989-01-27
申请人： Jean L. Peglion , Jean C. Poignant , Joel Vian
发明人： Jean L. Peglion , Jean C. Poignant , Joel Vian
IPC分类号： C07D307/91 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/40 , A61K31/4025 , A61P25/20 , A61P25/24 , A61P25/26 , C07D307/92 , C07D405/04 , C07D405/12 , C07D409/12
CPC分类号： C07D307/92 , C07D405/12 , C07D409/12
摘要： Compounds of general formula I, ##STR1## in which: R.sub.1 denotes a hydrogen atom or, with the proviso, however, that the amino radical is at the 7-position, a linear or branched alkyl radical containing 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen atom or, with the proviso, however, that the amino radical is at the 6-position, a linear or branched alkyl radical containing 1 to 4 carbon atoms,R.sub.3 and R.sub.4, which may be identical or different, each denote a hydrogen atom, a benzyl radical, a cyclohexylmethyl radical, a linear or branched alkylene radical containing from 1 to 5 carbon atoms, a linear or branched alkyl radical containing from 1 to 10 carbon atoms (optionally substituted with a hydroxy radical, with a carboxy radical or with an alkoxy radical having 1 to 5 carbon atoms, with an alkoxycarbonyl radical having 2 to 6 carbon atoms, with an alkylphenyl radical or with an alkyl-2-thienyl radical), a halogenated alkyl radical containing from 1 to 5 carbon atoms, or form, together with the nitrogen to which they are attached, a 2-oxo-1-pyrrolidinyl radical,A-B denotes, with the oxygen to which it is attached, an ethyleneoxy radical, an ethynyleneoxy, a 2-oxo-1-oxyethylene radical or a 2-hydroxy-1-oxyethylene radical.The compounds of Formula I possess antidepressant, antiggressive, and dopaminergic properties.
摘要翻译：通式I的化合物，其中：R1表示氢原子，或者条件是氨基位于7-位，含有1至4个碳原子的直链或支链烷基，R2 表示氢原子，或者条件是，氨基位于6位，含有1至4个碳原子的直链或支链烷基，R3和R4可以相同或不同，分别表示氢原子，苄基，环己基甲基，含有1至5个碳原子的直链或支链亚烷基，含有1至10个碳原子的直链或支链烷基（任选被羟基取代，具有羧基）或具有1至5个碳原子的烷氧基，具有2至6个碳原子的烷氧羰基，与烷基苯基或与烷基-2-噻吩基反应），含有1至5个碳原子的卤代烷基，或形式，连同与它们连接的氮，2-氧代-1-吡咯烷基，AB表示与其连接的氧，乙烯氧基，乙炔氧基，2-氧代-1-氧乙烯基或2-羟基 -1-氧乙烯基。式I的化合物具有抗抑郁药，抗过敏药和多巴胺能药物。

8. 发明授权

US4863951A Pharmacologically active amino-5,6,7,8-tetrahydronaphtho [2,3-B] furan compounds 失效
标题翻译：药理活性氨基-5,6,7,8-四氢萘并[2,3-B]呋喃化合物
公开(公告)号：US4863951A
公开(公告)日：1989-09-05
申请号：US173285
申请日：1988-03-25
申请人： Jean L. Peglion , Jean C. Poignant , Joel Vian
发明人： Jean L. Peglion , Jean C. Poignant , Joel Vian
IPC分类号： C07D307/91 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/40 , A61K31/4025 , A61P25/20 , A61P25/24 , A61P25/26 , C07D307/92 , C07D405/04 , C07D405/12 , C07D409/12
CPC分类号： C07D307/92 , C07D405/12 , C07D409/12
摘要： Compounds of general formula I, ##STR1## in which: R.sub.1 denotes a hydrogen atom or, with the proviso, however, that the amino radical is at the 7-position, a linear or branched alkyl radical containing 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen atom or, with the proviso, however, that the amino radical is at the 6-position, a linear or branched alkyl radical containing 1 to 4 carbon atoms,R.sub.3 and R.sub.4, which may be identical or different, each denote a hydrogen atom, a benzyl radical, a cyclohexylmethyl radical, a linear or branched alkylene radical containing from 1 to 5 carbon atoms, a linear or branched alkyl radical containing from 1 to 10 carbon atoms (optionally substituted with a hydroxy radical, with a carboxy radical or with an alkoxy radical having 1 to 5 carbon atoms, with an alkoxycarbonyl radical having 2 to 6 carbon atoms, with an anlkyphenyl radical or with an alkyl-2-theinyl radical), a halogenated alkyl radical containing from 1 to 5 carbon atoms, or form, together with the nitrogen to which they are attached, a 2-oxo-1-pyrrolidinyl radical,A-B denotes, with the oxygen to which it is attached, an ethyleneoxy radical, an ethynyleneoxy, a 2-oxo-1-oxyethylene radical or a 2-hydroxy-1-oxyethylene radical.The compounds of the formula I possess antidepressant, antiaggressive, and dopaminergic properties.
摘要翻译：通式I的化合物，其中：R1表示氢原子，或者条件是氨基位于7-位，含有1至4个碳原子的直链或支链烷基，R2 表示氢原子，或者条件是，氨基位于6位，含有1至4个碳原子的直链或支链烷基，R3和R4可以相同或不同，分别表示氢原子，苄基，环己基甲基，含有1至5个碳原子的直链或支链亚烷基，含有1至10个碳原子的直链或支链烷基（任选被羟基取代，具有羧基）或具有1至5个碳原子的烷氧基，具有2至6个碳原子的烷氧基羰基，具有烷基-2-炔基的烷基），含有1至5个碳原子的卤代烷基，或形式，连同与它们连接的氮，2-氧代-1-吡咯烷基，AB表示与其连接的氧，乙烯氧基，乙炔氧基，2-氧代-1-氧乙烯基或2-羟基 -1-氧乙烯基。式I的化合物具有抗抑郁药，抗侵袭性和多巴胺能性质。

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