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    Vitamin D compounds and method of preparing these compounds
    3.
    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。

    Bicyclo[10.2.0]tetradecan-13-one, fragrance use thereof, process for preparing same and dichlorinated intermediate used in said process
    6.
    发明授权
    Bicyclo[10.2.0]tetradecan-13-one, fragrance use thereof, process for preparing same and dichlorinated intermediate used in said process 失效
    双环[10.2.0]十四烷-13-酮，其香料用途，其制备方法和用于所述方法的二氯化中间体

    公开(公告)号：US5077274A

    公开(公告)日：1991-12-31

    申请号：US596506

    申请日：1990-10-12

    申请人： William J. Evers ,  Howard H. Heinsohn, Jr.

    发明人： William J. Evers ,  Howard H. Heinsohn, Jr.

    IPC分类号： C07C45/45 ,  C07C45/65 ,  C07C49/385 ,  C07C49/477 ,  C11B9/00

    CPC分类号： C11B9/0049 ,  C07C45/455 ,  C07C45/65 ,  C07C49/385 ,  C07C49/477

    摘要： Described is the novel compound, bicyclo[10.2.0]tetradecan-13-one having the structure: ##STR1## as well as the use thereof in augmenting or enhancing the aroma of consumable materials including perfume compositions, colognes and perfumed articles (including solid or liquid anionic, cationic, nonionic or zwitterionic detergents, fabric softeners, cosmetic powders and hair preparations). Also described is a process for preparing said bicyclo[10.2.0]tetradecan-13-one using as a reaction intermediate the compound having the structure: ##STR2##

    摘要翻译： 描述了具有以下结构的新型化合物双环[10.2.0]十四烷-13-酮，以及其在增加或增强消耗材料的香气中的用途，包括香料组合物，古龙水和香料制品（包括固体 或液体阴离子，阳离子，非离子或两性离子洗涤剂，织物柔软剂，化妆粉和头发制剂）。 还描述了制备所述双环[10.2.0]十四烷-13-酮的方法，该方法使用具有以下结构的化合物进行反应：

    Bicyclic ketones
    7.
    发明授权
    Bicyclic ketones 失效
    双环酮

    公开(公告)号：US4304944A

    公开(公告)日：1981-12-08

    申请号：US124526

    申请日：1980-02-25

    申请人： Brian J. Willis ,  Robert G. Eilerman

    发明人： Brian J. Willis ,  Robert G. Eilerman

    IPC分类号： C07C45/62 ,  C07C45/67 ,  C07C49/443 ,  C07C49/633 ,  C11B9/00 ,  C07C49/477 ,  C07C49/623

    CPC分类号： C11B9/0049 ,  C07C45/62 ,  C07C45/67 ,  C07C49/443 ,  C07C49/633

    摘要： Novel bicyclic ketones having the structure: ##STR1## wherein R is a C.sub.1 -C.sub.5 alkyl group, either straight-chain or branched, and saturated analogs have been prepared. These compounds exhibit floral and woody odors and/or desirable flavor properties, and are useful as fragrance and/or flavor materials. The compounds are conveniently prepared from alkylidene cyclopentanones by Michael addition with alkyl metalloacetoacetates and subsequent decarboxylative cyclization of the adducts. The saturated analogs may then be prepared by hydrogenation.

    摘要翻译： 具有以下结构的新型双环酮：其中R是直链或支链的C 1 -C 5烷基和饱和类似物。 这些化合物表现出花香和木质气味和/或期望的风味特性，并且可用作香料和/或香料材料。 通过与烷基金属乙酰乙酸酯进行迈克尔加成，随后加成的脱羧环化，方便地由亚烷基环戊酮制备化合物。 然后可以通过氢化制备饱和类似物。