COMPOSITIONS AND METHODS FOR THE TREATMENT OF MULTIPLE SCLEROSIS
    6.
    发明公开
    COMPOSITIONS AND METHODS FOR THE TREATMENT OF MULTIPLE SCLEROSIS 审中-公开
    用于治疗多发性硬化症的组合物和方法

    公开(公告)号:EP2852569A2

    公开(公告)日:2015-04-01

    申请号:EP13794171.2

    申请日:2013-05-16

    发明人: KANDULA, Mahesh

    摘要: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing multiple sclerosis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of neurodegenerative diseases and other neuro-inflammatory diseases.

    摘要翻译: 本发明涉及式I和式II的化合物或其可药用盐,以及其多晶型物,溶剂化物,对映异构体,立体异构体和水合物。 该药物组合物包含有效量的式I或式II的化合物; 并且可以配制用于治疗或预防多发性硬化症的方法用于口服,口腔,直肠,局部,透皮,透粘膜,静脉内,肠胃外施用,糖浆或注射。 这样的组合物可以用于治疗神经退行性疾病和其他神经炎症疾病。

    COMPOUNDS FOR AND METHOD OF INHIBITING PHOSPHODIESTERASE IV
    9.
    发明公开
    COMPOUNDS FOR AND METHOD OF INHIBITING PHOSPHODIESTERASE IV 失效
    VERBINDUNGEN UND VERFAHREN ZUR HEMMUNG VON PHOSPHODIESTERASE IV

    公开(公告)号:EP0796093A1

    公开(公告)日:1997-09-24

    申请号:EP96903491.0

    申请日:1996-01-11

    申请人: Euroceltique S.A.

    摘要: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram as well as with improved selectivity with regard to PDE III inhibition. In certain aspects of the invention, the compounds also demonstrate PDE V inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.

    摘要翻译: 含有巯基的PDE IV抑制剂,其含有下式的苯基或苄基取代的部分:不同且各自为O或S; R1选自氢,饱和或不饱和的直链或支链C 2--12烷基,在环烷基部分含有3至10个碳原子的环烷基和环烷基 - 烷基; R2 = R1或-CH3; R3是氢,卤素或饱和或不饱和的直链或支链C 1-12烷基,在环烷基部分含有3-7个碳原子的环烷基或环烷基 - 烷基; Z是选自-CH 2 CONH-或-CH 2 NHCO-的键,并且R 4是苯基或苄基,其可以是未取代的或被一个或多个卤素原子,烷基,羟基,氰基,羧基,烷氧基,烷氧基羰基 酰胺基,甲酰胺基,取代或未取代的氨基,在环烷基部分含有3至10个碳原子的环烷基和环烷基 - 烷基,优选含约6至约10个碳原子的芳基或芳烷基,或含有氮的杂环基, 环中的氧或硫; 烷基,烷氧基,环烷基,环烷基烷基,芳基和芳基 - 烷基是饱和或不饱和的,未被取代或被卤素原子,羟基,氰基,羧基,烷氧基,烷氧基羰基,甲酰胺基或取代或未取代的氨基取代, 或一个或多个具有1至3个碳原子的低级烷基; 条件是R4不能被多于一个甲氧基取代。 与茶碱或咯利普兰相比,以及与PDE III抑制有关的改善的选择性。 还公开了含有其的药物组合物和治疗方法。