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107 条记录 (耗时 0.064 秒)

    Halogenated antituberculosis agents
    97.
    发明授权
    Halogenated antituberculosis agents 失效
    卤化抗结核药

    公开(公告)号：US06482982B1

    公开(公告)日：2002-11-19

    申请号：US09803006

    申请日：2001-03-08

    申请人： Farzad Kobarfard ,  Joel M. Kauffman

    发明人： Farzad Kobarfard ,  Joel M. Kauffman

    IPC分类号： C07C33706

    CPC分类号： C07C281/14 ,  C07C337/08

    摘要： Halogenated derivatives of two synthetic anti-tuberculosis agents, thioacetazone and p-aminosalicylic acid, have been synthesized. In general, the halogenated compound has the structure of Structure I: wherein X1 is a halogen and X2 is a second halogen or hydrogen, and Y is sulfur or oxygen; or, has the structure of Structure IV: wherein X1 is a halogen and X2 is a second halogen or hydrogen. Alternatively, the halogenated compounds may be pharmaceutically acceptable salts of these compounds. These halogenated derivatives possess anti-mycobacterial activity and are particularly useful for the treatment of Mycobacterium tuberculosis infections. In particular, fluorinated analogs of thioacetazone and p-amino-salicylic acid have been synthesized for use as anti-tuberculosis therapeutic agents either alone or in combination with other conventional anti-tuberculosis therapeutic agents.

    摘要翻译： 已经合成了两种合成抗结核药物硫代乙酮和对氨基水杨酸的卤代衍生物。 通常，卤代化合物具有结构I的结构：其中X1是卤素，X2是第二个卤素或氢，Y是硫或氧; 或具有结构IV的结构：其中X1是卤素，X2是第二个卤素或氢。 或者，卤化化合物可以是这些化合物的药学上可接受的盐。 这些卤代衍生物具有抗分枝杆菌活性，特别可用于治疗结核分枝杆菌感染。 特别地，已经合成硫代乙酮和对氨基水杨酸的氟化类似物单独使用或与其它常规抗结核治疗剂组合用作抗结核治疗剂。

    Elevation of HDL cholesterol by 4-[(aminothioxomethyl)hydrazono]-4-arylbutyl carbamates
    100.
    发明授权
    Elevation of HDL cholesterol by 4-[(aminothioxomethyl)hydrazono]-4-arylbutyl carbamates 失效
    4 - [（氨基硫代甲基）亚肼基] -4-芳基丁基氨基甲酸酯升高HDL胆固醇

    公开(公告)号：US5977170A

    公开(公告)日：1999-11-02

    申请号：US96089

    申请日：1998-06-11

    申请人： Thomas Joseph Commons ,  Susan Christman

    发明人： Thomas Joseph Commons ,  Susan Christman

    IPC分类号： C07C337/08 ,  C07C255/27 ,  A61K31/27 ,  C07C271/10

    CPC分类号： C07C337/08

    摘要： This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sub.4 and R.sub.5 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thenyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH.

    摘要翻译： 本发明涉及通过施用下式化合物来提高HDL胆固醇水平来治疗动脉粥样硬化：其中R 1，R 2和R 3独立地是氢，C 1 -C 6烷基或 - （CH 2）0-6Ph，其中Ph被任选取代 卤素，氰基，硝基，C 1 -C 6烷基，C 1 -C 6烷氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH; R 4和R 5独立地是氢，C 1 -C 6烷基，C 3 -C 8环烷基或 - （CH 2）0-6Ar 1，其中Ar 1是苯基，萘基，呋喃基，吡啶基或者正丁基，Ar 1可以任选地被卤素，氰基，硝基， C 1 -C 6烷基，苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH; 氰基，硝基，C 1 -C 6烷基，苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH中的任意一个被取代的苯基，萘基，呋喃基，吡啶基或噻吩基。