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    • 1. 发明授权
    • Certain dihydrobenzofuran butanoic and pentanoic acid derivatives
    • 某些二氢苯并呋喃丁酸和戊酸衍生物
    • US4874878A
    • 1989-10-17
    • US301160
    • 1989-01-24
    • Jean L. PeglionJean C. PoignantJoel Vian
    • Jean L. PeglionJean C. PoignantJoel Vian
    • A61K31/34A61K31/343A61P25/20A61P25/24A61P25/26C07D307/77C07D307/79C07D307/91C07D307/92C07D307/93C07D409/12
    • C07D307/79C07D307/92C07D307/93C07D409/12
    • 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.
    • 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。
    • 3. 发明授权
    • 2,4,5,6,7,8-Hexahydronaphtho[2,3-b]furan useful as an intermediate
    • 2,4,5,6,7,8-六氢萘并[2,3-b]呋喃,可用作中间体
    • US4885373A
    • 1989-12-05
    • US303545
    • 1989-01-27
    • Jean L. PeglionJean C. PoignantJoel Vian
    • Jean L. PeglionJean C. PoignantJoel Vian
    • C07D307/91A61K31/34A61K31/343A61K31/38A61K31/40A61K31/4025A61P25/20A61P25/24A61P25/26C07D307/92C07D405/04C07D405/12C07D409/12
    • C07D307/92C07D405/12C07D409/12
    • 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.
    • 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。
    • 4. 发明授权
    • Pharmacologically active amino-5,6,7,8-tetrahydronaphtho [2,3-B] furan
compounds
    • 药理活性氨基-5,6,7,8-四氢萘并[2,3-B]呋喃化合物
    • US4863951A
    • 1989-09-05
    • US173285
    • 1988-03-25
    • Jean L. PeglionJean C. PoignantJoel Vian
    • Jean L. PeglionJean C. PoignantJoel Vian
    • C07D307/91A61K31/34A61K31/343A61K31/38A61K31/40A61K31/4025A61P25/20A61P25/24A61P25/26C07D307/92C07D405/04C07D405/12C07D409/12
    • C07D307/92C07D405/12C07D409/12
    • 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.
    • 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。
    • 7. 发明授权
    • 2,6-piperazinedione compounds
    • 2,6-哌嗪二酮化合物
    • US4820707A
    • 1989-04-11
    • US70967
    • 1987-07-08
    • Gilbert LavielleJean C. Poignant
    • Gilbert LavielleJean C. Poignant
    • A61K31/495A61P25/18A61P25/20C07D241/08C07D401/06C07D401/14C07D403/12C07D403/08
    • C07D401/06C07D241/08C07D403/12
    • The invention relates to 2,6-piperazinedione derivatives of general formula I ##STR1## in which: A and B each denote a methylene radical or a carbonyl radical with the proviso, however, that A and B never simultaneously denote the same radical,R.sub.1 denotes a diphenylmethyl radical optionally substituted on the benzene rings with a halogen atom, a cyclohexyl radical, a pyridylmethyl group, or a benzyl radical optionally substituted with a halogen atom or with an alkoxy radical containing from 1 to 4 carbon atoms,R.sub.2 denotes a pyrimidinyl radical or a phenyl radical optionally substituted with a halogen atom, with an alkyl radical having from 1 to 4 carbon atoms, with a trifluoromethyl radical or with an alkoxy radical containing from 1 to 4 carbon atoms,n is an integer from 2 to 4,and their addition salts with a pharmaceutically acceptable inorganic or organic acid.
    • 本发明涉及通式I(I)的2,6-哌嗪二酮衍生物,其中:A和B各自表示亚甲基或羰基,但条件是A和B从不同时表示相同 自由基,R1表示在苯环上任选被卤素原子取代的二苯基甲基,环己基,吡啶基甲基或任选被卤素原子或含有1至4个碳原子的烷氧基取代的苄基,R 2 表示嘧啶基或任选被卤素原子取代的苯基,具有1至4个碳原子的烷基,具有三氟甲基或含有1至4个碳原子的烷氧基,n是2的整数 至4,以及它们与药学上可接受的无机酸或有机酸的加成盐。