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    Vitamin D compounds and method of preparing these compounds
    2.
    发明授权
    Vitamin D compounds and method of preparing these compounds 失效
    维生素D化合物及其制备方法

    公开(公告)号：US6075015A

    公开(公告)日：2000-06-13

    申请号：US863947

    申请日：1997-05-27

    申请人： Jose P. Sestelo ,  Antonio Mourino ,  Jose L. Mascarenas ,  Sebastianus J. Halkes ,  Jan Zorgdrager ,  Gerhardus D. H. Dijkstra ,  Jan-Paul van de Velde

    发明人： Jose P. Sestelo ,  Antonio Mourino ,  Jose L. Mascarenas ,  Sebastianus J. Halkes ,  Jan Zorgdrager ,  Gerhardus D. H. Dijkstra ,  Jan-Paul van de Velde

    IPC分类号： C07C35/32 ,  C07C45/29 ,  C07C49/477 ,  C07C49/513 ,  C07C401/00 ,  A61K31/59

    CPC分类号： C07C401/00 ,  C07C35/32 ,  C07C45/292 ,  C07C49/477 ,  C07C49/513 ,  Y10S514/861 ,  Y10S514/863

    摘要： Vitamin D.sub.3 analogues of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or hydroxy, R.sub.2 is (C.sub.1 -C.sub.3)alkyl, hydroxy(C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.2)alkoxymethyl, (C.sub.2 -C.sub.3)alkenyl, or (C.sub.2 -C.sub.3)alkynyl, R.sub.3 is a branched or unbranched, saturated or unsaturated aliphatic 3- to 5- membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy, R.sub.4 is sec. or tert. (C.sub.3 -C.sub.6)alkyl or (C.sub.3 -C.sub.6)cycloalkyl, A and B are each individually hydrogen or methyl, or A and B together from methylene. The compounds of the present invention exhibit pharmacotherapeutic activities, including in particular, the treatment of osteoporosis, renal osteodystrophy, osteomalacia, skin disorders such as psoriasis and other hyperproliferative skin diseases, eczema and dermatitis, nmyopathy, leukemia, breast and colon cancer, osteosarcomas, squamous cell carcinomas, melanoma, certain immunological disorders, and transplant rejections. Several methods of synthesis, including reaction of an ester compound of general formula (IX) with an inorganometallic compound of formula (III) followed by deprotection or, alternatively, first finalization of the C.sub.17 -side chain are also disclosed.

    摘要翻译： 式（I）的维生素D3类似物：其中R1是氢或羟基，R2是（C1-C3）烷基，羟基（C1-C3）烷基，（C1-C2）烷氧基甲基，（C2-C3）烯基或（ C 2 -C 3）炔基，R 3是支链或非支链的饱和或不饱和的脂族3-至5-元烃基或氧杂烃双基，在主链中具有至少3个原子，并且任选地被一个或多个选自环氧基， 氟和羟基，R4是秒。 或叔。 （C 3 -C 6）烷基或（C 3 -C 6）环烷基，A和B各自独立地为氢或甲基，或A和B一起为亚甲基。 本发明的化合物具有药物治疗活性，特别包括治疗骨质疏松症，肾性骨营养不良，骨软化症，皮肤疾病如牛皮癣和其它过度增生性皮肤病，湿疹和皮炎，纳米病，白血病，乳腺和结肠癌，骨肉瘤， 鳞状细胞癌，黑素瘤，某些免疫性疾病和移植排斥。 还公开了几种合成方法，包括通式（IX）的酯化合物与式（III）的无机金属化合物反应，然后进行脱保护，或者也可以首先终止C17-侧链。

    Mesylates of piperazine derivatives and process for their preparation
    10.
    发明授权
    Mesylates of piperazine derivatives and process for their preparation 失效
    哌嗪衍生物的甲磺酸酯及其制备方法

    公开(公告)号：US07030241B2

    公开(公告)日：2006-04-18

    申请号：US10468098

    申请日：2002-02-14

    申请人： Marcel P. M. van Aar ,  Stefanus J. Schouten ,  Jan Zorgdrager ,  Michiel C. Heslinga

    发明人： Marcel P. M. van Aar ,  Stefanus J. Schouten ,  Jan Zorgdrager ,  Michiel C. Heslinga

    IPC分类号： C07D403/00 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00

    CPC分类号： C07D263/58

    摘要： The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step. The invention relates to the mesylate of compounds of the formula (I) wherein X is a bicyclic heterocyclic phenyl group and Y is methyl, ethyl (optionally substituted with fluorine), cycloalkyl (3–7C) methyl, benzyl or m-phenyl benzyl

    摘要翻译： 本发明涉及一组哌嗪衍生物的甲磺酸盐，以及以高产率和高纯度经济地制备这些甲磺酸盐的方法。 根据本发明的方法，在单个反应步骤中合并哌嗪环和甲磺酸酯形成。 本发明涉及式（I）化合物的甲磺酸酯，其中X为双环杂环苯基，Y为甲基，乙基（任选被氟取代），环烷基（3-7C）甲基，苄基或间苯基苄基