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    • 15. 发明申请
    • TABLET WITH CONTROLLED RELEASE OF ALFUZOSINE CHLORYDRATE
    • 控制释放ALFUZOSINE CHLORYDRATE的药片
    • WO1998008515A1
    • 1998-03-05
    • PCT/FR1997001515
    • 1997-08-22
    • SYNTHELABOJAGOTEC AGMAGGI, LaurettaCONTE, UbaldoGRENIER, PascalVERGNAULT, GuyDUFOUR, AlainJARREAU, François, XavierRAUCH-DESANTI, Clémence
    • SYNTHELABOJAGOTEC AG
    • A61K31/505
    • A61K9/2086A61K31/517
    • The invention concerns a pharmaceutical tablet for oral administration, for the controlled release of alfuzosine chlorhydrate at the proximal segments of the gastrointestinal tract, characterised in that it consists of: a) a first layer (1) capable of swelling noticeably and rapidly in contact with aqueous biological liquids, said layer being produced by a mixture or a granule containing hydrophilic polymers constituting 5.0 to 90 % and preferably 10 to 85 % of the layer weight; b) a second layer (2) adjacent to or superposed on the first layer, in which is carried the alfuzosine chlorhydrate, this layer being formed with hydrophilic polymers and other auxiliary substances, so as to give to the preparation suitable compressibility properties and to enable the release of the alfuzosine chlorhydrate in a predetermined lapse of time; c) and optionally a third layer (3) obtained by compression and applied on layer (2), generally consisting in particular of hydrophilic polymers which gel and/or swell and then can be optionally eroded and acting as a barrier modulating the release of the alfuzosine of layer (2), layer (3) being almost impermeable to the passage of the active substance. The invention is applicable to a pharmaceutical composition.
    • 本发明涉及一种用于口服给药的药物片剂,用于在胃肠道的近端节段控制释放盐酸阿夫福兹,其特征在于,其包括:a)能够明显和快速地溶胀的第一层(1),其与 水性生物液体,所述层由含有构成层重量的5.0〜90%,优选为10〜85%的亲水性聚合物的混合物或颗粒制成; b)邻近或重叠在第一层上的第二层(2),其中载有氢氟酸低聚水合物,该层由亲水性聚合物和其它辅助物质形成,以便制备合适的可压缩性,并使得 在预定的时间内释放氢氟酸阿福佐星; c)和任选的通过压缩获得并施加在层(2)上的第三层(3),其通常特别地由亲水性聚合物组成,所述亲水性聚合物凝胶化和/或膨胀,然后可以任选地被侵蚀并且用作调节释放 层(2)的阿夫福星,层(3)对于活性物质的通过几乎是不可渗透的。 本发明可应用于药物组合物。
    • 20. 发明申请
    • 1H-PYRIDO[3,4-b]INDOLE-4-CARBOXAMIDE DERIVATIVES, PREPARATION AND APPLICATION THEREOF IN THERAPEUTICS
    • 1H-吡啶并[3,4-b]吲哚-4-羧酰胺衍生物,其在治疗中的制备和应用
    • WO1998015552A1
    • 1998-04-16
    • PCT/FR1997001750
    • 1997-10-03
    • SYNTHELABOEVANNO, YannickSEVRIN, MireilleMALOIZEL, ChristianLEGALLOUDEC, OdetteGEORGE, Pascal
    • SYNTHELABO
    • C07D471/04
    • C07D471/04
    • The invention concerns compounds of general formula (I) in which X represents hydrogen or an halogen or an alkyl, alkoxy, trifluoromethyl or phenylmethoxy group, R1 represents hydrogen or an alkyl, cyclopropyl or phenylmethyl group, R2 represents either an alkyl group optionally substituted, or a phenylalkyl group optionally substituted, or a cyclohexylmethyl group, or a thienylmethyl group, or a pyridinylmethyl group, or a phenyl group optionally substituted, or a pyridinyl group, or a 5-methyl-1,2-oxazolyl group, or a 5-methyl-1,3,4-thiadiazolylgroup, or a naphtalenyl group, R3 and R4 each represent hydrogen or an alkyl, 2-methoxyethyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonylalkyl or phenylalkyl group, or form together, with the nitrogen atom which carries them, either a pyrrolidinyl group optionally substituted or a piperidinyl group, or a morpholinyl group, or a 4-methylpiperazinyl group, or an azetidinyl group, or a thiazolidinyl group, and the bond between the carbon atoms in positions 3 and 4 is simple or double. The invention is applicable in therapeutics.
    • 本发明涉及通式(I)的化合物,其中X表示氢或卤素或烷基,烷氧基,三氟甲基或苯基甲氧基,R 1表示氢或烷基,环丙基或苯基甲基,R 2表示任选取代的烷基, 或任选取代的苯基烷基,或环己基甲基,或噻吩基甲基或吡啶基甲基,或任选取代的苯基,或吡啶基或​​5-甲基-1,2-恶唑基或5 - 甲基-1,3,4-噻二唑基或萘基,R3和R4各自表示氢或烷基,2-甲氧基乙基,羟基烷基,羧基烷基,烷氧基羰基烷基或苯基烷基,或与携带它们的氮原子一起形成 ,任选取代的吡咯烷基或哌啶基,或吗啉基或4-甲基哌嗪基,或氮杂环丁烷基或噻唑烷基,以及碳原子之间的键 位置3和4是简单或双重。 本发明适用于治疗。