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    • 3. 发明授权
      US4639468A Derivatives of glycinamide, their preparation and their use 失效
    • 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 Roncucci , Claude L. Gillet , Alexis H. Cordi , Mark A. Martens , Joseph L. Roba , Paul J. Niebes , Georges E. Lambelin , William R. Van Dorsser
    • Romeo Roncucci , Claude L. Gillet , Alexis H. Cordi , Mark A. Martens , Joseph L. Roba , Paul J. Niebes , Georges E. Lambelin , William R. Van Dorsser
    • A61K31/16 , A61K31/165 , A61K31/195 , A61K31/205 , C07C233/00 , C07C233/12 , C07C233/30 , C07C237/00 , C07C271/06 , C07C271/22
    • C07C255/00 , C07C271/22
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 5. 发明授权
      US4338330A Benzimidazole derivatives, their use, and compositions containing these derivatives 失效
    • 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. Gillet , Joseph L. Roba , Michel Snyers , William R. Van Dorsser , Georges E. Lambelin
    • Claude L. Gillet , Joseph L. Roba , Michel Snyers , William R. Van Dorsser , Georges E. Lambelin
    • 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
    • C07D317/58 , C07D235/18 , C07D303/22
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 10. 发明授权
      US3954871A 1-(4-Alkylthiopheny)-2-substituted amino-alcohols and their salts 失效
    • 1-(4-Alkylthiopheny)-2-substituted amino-alcohols and their salts
    • 1-（4-烷基噻吩）-2-取代的氨基醇及其盐
    • US3954871A
    • 1976-05-04
    • US456216
    • 1974-03-29
    • Nguyen Phuc Buu-Hoi , Georges E. Lambelin , Joseph L. Roba , Claude Gillet , Guy D. Jacques
    • Nguyen Phuc Buu-Hoi , Georges E. Lambelin , Joseph L. Roba , Claude Gillet , Guy D. Jacques
    • A61K31/135 , A61K31/33 , C07D217/04 , C07D295/08 , C07D295/084 , C07D295/13 , C07C91/22
    • C07D295/13 , A61K31/135 , A61K31/33 , C07D217/04 , C07D295/08 , C07D295/092 , Y10S514/929
    • The new amino-alcohols according to the invention are represented by the formula ##SPC1##Wherein: R.sub.1 represents a RS, RSO or RSO.sub.2 group in which R is a linear or branched alkyl group (C.sub.1 -C.sub.10), an acetyl radical or hydrogen; R.sub.2 and R.sub.3, which may be identical or different, represent a halogen atom or an alkyl (C.sub.1 -C.sub.3), amino, alkylamino (C.sub.1 -C.sub.4), acylamino, nitro, carboxy, carbalkoxy, trifluoromethyl, alkoxy (C.sub.1 -C.sub.4) or alkylthio (C.sub.1 -C.sub.4) radical; R.sub.4 represents hydrogen or a linear or branched alkyl radical containing 1 - 4 carbon atoms; R.sub.5 and R.sub.6, which may be identical or different, represent hydrogen, a substituted or not, linear or branched alkyl (C.sub.1 -C.sub.16) radical, a cycloalkyl (C.sub.5 -C.sub.6) radical, an alkynyl (C.sub.3 -C.sub.4) radical, an alkenyl (C.sub.3 -C.sub.4) radical or a heterocycle of the kind piperidine, morpholine, pyridine or pyridimine, R.sub.5 and R.sub.6 can also form with adjacent nitrogen atom a heterocyclic radical, substituted or not; one of said R.sub.2 and R.sub.3 can be a hydrogen atom or can be both a hydrogen atom provided that simultaneously R is a lower alkyl (C.sub.1 -C.sub.3) radical in the group RS, R.sub.4 and R.sub.5 are hydrogen atoms and R.sub.6 is an isopropyl or t-butyl radical or if simultaneously R is a methyl radical in the group RSO.sub.2, R.sub.4 and R.sub.5 are hydrogen atoms and R.sub.6 is an isopropyl radical.When R.sub.5 and R.sub.6 represent an alkyl, the latter can be substituted by amino, alkylamino, hydroxy, alkoxy, phenoxy, substituted phenoxy, phenyl, substituted phenyl radical or a heterocycle such as piperidino or morpholino.
    • 根据本发明的新氨基醇由下式表示：R1表示其中R是直链或支链烷基（C1-C10），乙酰基或氢的RS，RSO或RSO2基团; R2和R3可以相同或不同，表示卤素原子或（C1-C3）烷基，氨基，烷基氨基（C1-C4），酰氨基，硝基，羧基，烷氧羰基，三氟甲基，烷氧基（C1-C4）或 烷硫基（C 1 -C 4）基; R4表示氢或含有1-4个碳原子的直链或支链烷基; R 5和R 6可以相同或不同，表示氢，取代或未取代的直链或支链烷基（C1-C16）基，环烷基（C5-C6）基，炔基（C3-C4）基，烯基 （C 3 -C 4）基或类哌啶，吗啉，吡啶或哒嗪的杂环，R 5和R 6也可以与相邻的氮原子一起形成杂环基，被取代或未被取代; 所述R2和R3之一可以是氢原子或既可以是氢原子，条件是同时R是基团RS中的低级烷基（C1-C3）基团，R4和R5是氢原子，R6是异丙基或t 丁基或如果同时R是基团R 2 O 2中的甲基，则R 4和R 5是氢原子，R 6是异丙基。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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