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    Derivatives of glycinamide, their preparation and their use
    1.
    发明授权
    Derivatives of glycinamide, their preparation and their use 失效
    甘氨酰胺的衍生物，其制备及其用途

    公开(公告)号：US4639468A

    公开(公告)日：1987-01-27

    申请号：US768185

    申请日：1985-08-23

    申请人： Romeo Roncucci ,  Claude L. Gillet ,  Alexis H. Cordi ,  Mark A. Martens ,  Joseph L. Roba ,  Paul J. Niebes ,  Georges E. Lambelin ,  William R. Van Dorsser

    发明人： Romeo Roncucci ,  Claude L. Gillet ,  Alexis H. Cordi ,  Mark A. Martens ,  Joseph L. Roba ,  Paul J. Niebes ,  Georges E. Lambelin ,  William R. Van Dorsser

    IPC分类号： A61K31/16 ,  A61K31/165 ,  A61K31/195 ,  A61K31/205 ,  C07C233/00 ,  C07C233/12 ,  C07C233/30 ,  C07C237/00 ,  C07C271/06 ,  C07C271/22

    CPC分类号： C07C255/00 ,  C07C271/22

    摘要： A glycinamide derivative of the general formula I: ##STR1## wherein: R is a linear or ramified alkyl group C.sub.5 -C.sub.18, a linear or ramified alkenyl group C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9, C.sub.10, C.sub.11, C.sub.12, C.sub.13, C.sub.14, C.sub.15, C.sub.16, C.sub.17 or C.sub.18, a linear or ramified alkynyl group C.sub.4 -C.sub.10, a linear or ramified acyl group C.sub.4 -C.sub.18, a linear or ramified alkyl group C.sub.1 -C.sub.10, substituted by a phenoxy group, by a hydroxy radical, by an acetoxy radical, by a carboxy radical, by a linear or ramified alkoxycarbonyl group C.sub.1 -C.sub.4, by a carbonyl radical, by a carboxaldehyde group, by an acetal or cetal group, by one or more phenyl groups, by one or more phenyl groups substituted by a halogen atom such as fluorine, chlorine or bromine,R.sub.1 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9 or C.sub.10, a linear or ramified acyl group C.sub.1 -C.sub.6, a benzoyl group, a linear or ramified alkoxycarbonyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7 or C.sub.8, a carboxamidomethyl group,R.sub.2 represents hydrogen, a linear or ramified alkyl C.sub.1, C.sub.2, C.sub.3, a phenyl group,R.sub.3 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7 or C.sub.8, a phenyl group, optionally substituted by a halogen atom, such as fluorine, chlorine or bromine,R.sub.4 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7 or C.sub.8 as well as salts of these derivatives with non toxic and pharmaceutically usable acids.

    摘要翻译： 通式I的甘氨酰胺衍生物：其中：R是直链或支链烷基C5-C18，直链或支链烯基C5，C6，C7，C8，C9，C10，C11，C12 C13，C14，C15，C16，C17或C18，直链或支链炔基C4-C10，线性或分枝酰基C4-C18，被苯氧基取代的直链或支链烷基C1-C10，由 羟基自由基，乙酰氧基，羧基，直链或分支的烷氧羰基C1-C4，羰基，羧醛基，缩醛或鲸蜡基，一个或多个苯基，被 一个或多个被卤素原子如氟，氯或溴取代的苯基，R 1表示氢，直链或支链烷基C1，C2，C3，C4，C5，C6，C7，C8，C9或C10，线性 或分支酰基C 1 -C 6，苯甲酰基，直链或支链烷氧基羰基C1，C2，C3，C4，C5，C6，C7或C8，羧酰胺基甲基，R2表示氢，线性或柱塞 烷基C1，C2，C3，苯基，R3表示氢，直链或支链烷基C1，C2，C3，C4，C5，C6，C7或C8，任选被卤素原子取代的苯基， 作为氟，氯或溴，R 4表示氢，直链或支链烷基C1，C2，C3，C4，C5，C6，C7或C8，以及这些衍生物与无毒和可药用酸的盐。

    Benzimidazole derivatives, their use, and compositions containing these derivatives
    4.
    发明授权
    Benzimidazole derivatives, their use, and compositions containing these derivatives 失效
    苯并咪唑衍生物，它们的用途和含有这些衍生物的组合物

    公开(公告)号：US4338330A

    公开(公告)日：1982-07-06

    申请号：US145144

    申请日：1980-04-30

    申请人： Claude L. Gillet ,  Joseph L. Roba ,  Michel Snyers ,  William R. Van Dorsser ,  Georges E. Lambelin

    发明人： Claude L. Gillet ,  Joseph L. Roba ,  Michel Snyers ,  William R. Van Dorsser ,  Georges E. Lambelin

    IPC分类号： A61K31/135 ,  A61K31/16 ,  A61K31/165 ,  A61K31/415 ,  A61K31/4184 ,  A61P3/06 ,  A61P7/02 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/12 ,  A61P21/02 ,  A61P23/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/20 ,  C07C67/00 ,  C07C213/00 ,  C07C217/60 ,  C07C231/00 ,  C07C231/12 ,  C07C233/18 ,  C07C233/22 ,  C07C233/36 ,  C07C233/60 ,  C07C233/73 ,  C07C235/20 ,  C07C237/30 ,  C07D235/18 ,  C07D303/22 ,  C07D317/58 ,  C07D405/12

    CPC分类号： C07D317/58 ,  C07D235/18 ,  C07D303/22

    摘要： A derivative of benzimidazole of the general formula I: ##STR1## wherein: R.sub.1 represents a linear or ramified alkyl radical C.sub.1,C.sub.2,C.sub.3,C.sub.4,C.sub.5,C.sub.6,C.sub.7,C.sub.8,C.sub.9,C.sub.10,C.sub.11,C.sub.12,C.sub.13,C.sub.14,C.sub.15, C.sub.16,C.sub.17 or C.sub.18, a cycloalkyl radical C.sub.3,C.sub.4,C.sub.5,C.sub.6,C.sub.7 or C.sub.8, a linear or ramified alkyl radical C.sub.1,C.sub.2,C.sub.3,C.sub.4 or C.sub.5 substituted by one or more radicals selected from the group comprising:phenyl, phenoxy, phenylthio, phenylsufinyl radicals;phenyl, phenoxy, phenylthio, phenylsulfinyl radicals substituted by one or more linear or ramified alkyl radicals C.sub.1,C.sub.2, C.sub.3 or C.sub.4, by one or more linear or ramified alkoxy radicals C.sub.1,C.sub.2, C.sub.3 or C.sub.4, by a methylenedioxy radical, for one or more halogen atoms, such as fluorine, chlorine or bromine;linear or ramified alkylcarboxamido groups C.sub.1,C.sub.2,C.sub.3,C.sub.4,C.sub.5 or C.sub.6 optionally substituted by a phenyl or phenoxy radical;cycloalkylcarboxamido groups C.sub.1,C.sub.4,C.sub.5,C.sub.6,C.sub.7 or C.sub.8, R.sub.2 represents hydrogen, one or more linear or ramified alkyl radicals C.sub.1,C.sub.2,C.sub.3 or C.sub.4, one or more linear or ramified alkoxy radicals C.sub.1,C.sub.2,C.sub.3 or C.sub.4, one or more halogen atoms, such as fluorine, chlorine and bromine, R.sub.3 represents hydrogen, one or more linear or ramified alkyl radicals C.sub.1,C.sub.2,C.sub.3 or C.sub.4, one or more linear or ramified alkoxy radicals C.sub.1,C.sub.2,C.sub.3 or C.sub.4, one or more halogen atoms such as fluorine, chlorine and bromine, one or more nitro groups, as well as esters and salts of such derivatives with non toxical and pharmaceutically acceptable acids.

    摘要翻译： 通式I的苯并咪唑衍生物：其中：R1表示直链或支链烷基C1，C2，C3，C4，C5，C6，C7，C8，C9，C10，C11，C12，C13， C14，C15，C16，C17或C18，环烷基C3，C4，C5，C6，C7或C8，被一个或多个选自以下基团的基团取代的直链或支链烷基C1，C2，C3，C4或C5 包括：苯基，苯氧基，苯硫基，苯基亚乙基基; 苯基，苯氧基，苯硫基，被一个或多个直链或支链烷基C1，C2，C3或C4取代的苯基亚磺酰基，被一个或多个线性或分枝的烷氧基C1，C2，C3或C4被亚甲二氧基取代，一个 或更多个卤素原子，如氟，氯或溴; 线性或分支的烷基羧酰胺基C1，C2，C3，C4，C5或C6，任选被苯基或苯氧基取代; 环烷基羧酰胺基C1，C4，C5，C6，C7或C8，R2代表氢，一个或多个直链或支链烷基C1，C2，C3或C4，一个或多个线性或分枝的烷氧基C1，C2，C3或C4， 一个或多个卤素原子，例如氟，氯和溴，R 3表示氢，一个或多个直链或支链烷基C1，C2，C3或C4，一个或多个线性或分枝的烷氧基C1，C2，C3或C4， 一个或多个卤素原子如氟，氯和溴，一个或多个硝基，以及这些衍生物的酯和盐与非毒性和药学上可接受的酸。

    Alkyl and cycloalkylthiophenylalkylaminoalkanols, their salts and the preparation thereof
    5.
    发明授权
    Alkyl and cycloalkylthiophenylalkylaminoalkanols, their salts and the preparation thereof 失效
    烷基和环烷硫基苯基烷基氨基链烷醇，其盐及其制备

    公开(公告)号：US4228187A

    公开(公告)日：1980-10-14

    申请号：US718534

    申请日：1976-08-30

    申请人： Georges E. Lambelin ,  Claude L. Gillet ,  Joseph L. Roba

    发明人： Georges E. Lambelin ,  Claude L. Gillet ,  Joseph L. Roba

    IPC分类号： A61K31/135 ,  A61K31/445 ,  A61P9/00 ,  A61P9/08 ,  A61P9/12 ,  C07C67/00 ,  C07C313/00 ,  C07C319/20 ,  C07C323/32 ,  C07D295/084 ,  C07C91/06

    CPC分类号： C07D295/092

    摘要： Amino-alcohols of the formula ##STR1## wherein R.sub.1 represents either a linear or branched chain alkyl radical having 1 to 4 carbon atoms, or a cycloalkyl radical having 5 or 6 carbon atoms; R.sub.2 represents a lower alkyl radical having 1 or 2 carbon atoms; R.sub.3 represents a linear or branched chain alkyl radical having 3 to 10 carbon atoms which radical is optionally substituted by phenyl; R.sub.4 represents hydrogen, or, together with R.sub.3 and the adjacent nitrogen atom, a heterocyclic nucleus of the piperidine type and the corresponding non-toxic salts of said amino-alcohols; preparation of the above and their use as antispasmodic, peripheral vasodilatory and anti-hypertensive agents and as an agent having a protective activity against anoxia of the myocardium.

    摘要翻译： 式（I）的氨基醇，其中R 1表示具有1至4个碳原子的直链或支链烷基或具有5或6个碳原子的环烷基; R2表示具有1或2个碳原子的低级烷基; R3表示具有3至10个碳原子的直链或支链烷基，该基团任选被苯基取代; R4表示氢，或者与R3和相邻氮原子一起是哌啶类型的杂环核和所述氨基醇的相应无毒盐; 上述的制备及其用作解痉药，外周血管扩张剂和抗高血压剂以及作为对心肌缺氧的保护作用的药剂。

    Tricyclic glycinamide derivatives as anti-convulsants
    8.
    发明授权
    Tricyclic glycinamide derivatives as anti-convulsants 失效
    三环甘氨酰胺衍生物作为抗惊厥药

    公开(公告)号：US5141960A

    公开(公告)日：1992-08-25

    申请号：US720337

    申请日：1991-06-25

    申请人： Alexis A. Cordi ,  Claude L. Gillet

    发明人： Alexis A. Cordi ,  Claude L. Gillet

    IPC分类号： C07C237/06 ,  C07D337/12

    CPC分类号： C07C237/06 ,  C07D337/12 ,  C07C2103/32

    摘要： A class of tricyclic glycinamide derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of most interest are those of the formula ##STR1## wherein each of X and Y is hydrido; wherein Z is selected from methylene, ethylene, ethenylene, thiomethylene and thioethylene; and wherein each of R.sup.1, R.sup.2 and R.sup.3 is hydrido; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类用于治疗CNS功能障碍如癫痫和惊厥性疾病的三环甘氨酰胺衍生物。 最令人感兴趣的化合物是下式的化合物：其中X和Y各自是氢的; 其中Z选自亚甲基，亚乙基，亚乙烯基，亚甲基和硫代亚乙基; 并且其中R1，R2和R3各自是氢的; 或其药学上可接受的盐。

    Glycyl urea derivatives as anti-convulsants
    10.
    发明授权
    Glycyl urea derivatives as anti-convulsants 失效
    甘氨酰脲衍生物作为抗惊厥药

    公开(公告)号：US5288905A

    公开(公告)日：1994-02-22

    申请号：US761111

    申请日：1991-09-17

    申请人： Alex A. Cordi ,  Claude L. Gillet

    发明人： Alex A. Cordi ,  Claude L. Gillet

    IPC分类号： C07C275/50 ,  C07C275/48

    CPC分类号： C07C275/50

    摘要： A class of glycyl urea derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of interest are those of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is a group independently selected from hydrido, alkyl, aralkyl, aryloxyalkyl and arylthioalkyl, any one of which groups having a substitutable position may be substituted with one or more radicals selected from halo, alkyl of one to about ten carbon atoms, alkenyl of two to about ten carbon atoms, alkynyl of two to about ten carbon atoms, haloalkyl, alkoxy, alkylthio, alkylsulfinyl and alkylsulfonyl; or a pharmaceutically-acceptable salt thereof; with the proviso that when each of R.sup.1 and R.sup.2 is ethyl, then R.sup.3 and R.sup.4 cannot be hydrido simultaneously.

    摘要翻译： 描述了一类甘氨酰脲衍生物用于治疗CNS功能障碍如癫痫和惊厥性疾病。 感兴趣的化合物是式（*化学结构*）的化合物，其中R 1，R 2，R 3和R 4各自独立地选自氢，烷基，芳烷基，芳氧基烷基和芳硫基烷基，其中任何一个具有可取代位置的基团 被一个或多个选自卤素，1至约10个碳原子的烷基，2至约10个碳原子的烯基，2至约10个碳原子的炔基，卤代烷基，烷氧基，烷硫基，烷基亚磺酰基和烷基磺酰基取代; 或其药学上可接受的盐; 条件是当R 1和R 2各自为乙基时，则R 3和R 4不能同时氢化。