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    • 2. 发明授权
    • Derivatives of glycinamide, their preparation and their use
    • 甘氨酰胺的衍生物,其制备及其用途
    • US4639468A
    • 1987-01-27
    • US768185
    • 1985-08-23
    • Romeo RoncucciClaude L. GilletAlexis H. CordiMark A. MartensJoseph L. RobaPaul J. NiebesGeorges E. LambelinWilliam R. Van Dorsser
    • Romeo RoncucciClaude L. GilletAlexis H. CordiMark A. MartensJoseph L. RobaPaul J. NiebesGeorges E. LambelinWilliam R. Van Dorsser
    • A61K31/16A61K31/165A61K31/195A61K31/205C07C233/00C07C233/12C07C233/30C07C237/00C07C271/06C07C271/22
    • C07C255/00C07C271/22
    • 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.
    • 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。
    • 3. 发明授权
    • Benzimidazole derivatives, their use, and compositions containing these
derivatives
    • 苯并咪唑衍生物,它们的用途和含有这些衍生物的组合物
    • US4338330A
    • 1982-07-06
    • US145144
    • 1980-04-30
    • Claude L. GilletJoseph L. RobaMichel SnyersWilliam R. Van DorsserGeorges E. Lambelin
    • Claude L. GilletJoseph L. RobaMichel SnyersWilliam R. Van DorsserGeorges E. Lambelin
    • A61K31/135A61K31/16A61K31/165A61K31/415A61K31/4184A61P3/06A61P7/02A61P9/00A61P9/06A61P9/08A61P9/12A61P21/02A61P23/02A61P25/00A61P25/02A61P25/20C07C67/00C07C213/00C07C217/60C07C231/00C07C231/12C07C233/18C07C233/22C07C233/36C07C233/60C07C233/73C07C235/20C07C237/30C07D235/18C07D303/22C07D317/58C07D405/12
    • C07D317/58C07D235/18C07D303/22
    • 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.
    • 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。