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10 条记录 (耗时 0.031 秒)

    Synthesis Of 1,5-Disubstituted-2-Hydroxy-Gibbatetraen-6-Ones
    2.
    发明申请
    Synthesis Of 1,5-Disubstituted-2-Hydroxy-Gibbatetraen-6-Ones 审中-公开
    1,5-二取代-2-羟基 - 赤霉烯-6-酮的合成

    公开(公告)号：US20070293706A1

    公开(公告)日：2007-12-20

    申请号：US11666318

    申请日：2005-10-28

    申请人： Robert Wilkening ,  Amy Fried ,  Dann Parker

    发明人： Robert Wilkening ,  Amy Fried ,  Dann Parker

    IPC分类号： C07C45/61 ,  C07C49/755

    CPC分类号： C07C49/747 ,  C07C2603/86

    摘要： 1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones are useful as estrogen receptor modulators and as precursors to estrogen receptor modulators. The current invention provides a method for the synthesis of 1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones from simple indanone starting materials via a Robinson-type annulation followed by an internal alkylation reaction. This invention further describes the novel use of a fluoroethyl substituent as a latent alkylating group for an internal cyclization reaction.

    摘要翻译： 1,5-二取代-2-羟基 - 赤霉烯-6-酮可用作雌激素受体调节剂和雌激素受体调节剂的前体。 本发明提供了通过罗宾逊型环状化合物随后进行内部烷基化反应从简单的茚酮原料合成1,5-二取代-2-羟基 - 赤霉烯-6-酮的方法。 本发明进一步描述了氟乙基取代基作为内部环化反应的潜在烷基化基团的新用途。

    Estrogen receptor modulators
    4.
    发明申请
    Estrogen receptor modulators 失效

    公开(公告)号：US20060094779A1

    公开(公告)日：2006-05-04

    申请号：US11261692

    申请日：2005-10-28

    申请人： Robert Wilkening ,  Amy Fried

    发明人： Robert Wilkening ,  Amy Fried

    IPC分类号： A61K31/277 ,  A61K31/15 ,  A61K31/12 ,  C07C255/61

    CPC分类号： C07C251/44 ,  C07B2200/07 ,  C07C45/676 ,  C07C45/68 ,  C07C45/69 ,  C07C49/747 ,  C07C49/755 ,  C07C255/47 ,  C07C2603/86 ,  C07C2603/97

    摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

    Estrogen receptor modulators
    6.
    发明申请
    Estrogen receptor modulators 有权
    雌激素受体调节剂

    公开(公告)号：US20060041003A1

    公开(公告)日：2006-02-23

    申请号：US10528008

    申请日：2003-09-15

    申请人： Dann Parker ,  Robert Wilkening ,  Dongfang Meng ,  Ronald Ratcliffe

    发明人： Dann Parker ,  Robert Wilkening ,  Dongfang Meng ,  Ronald Ratcliffe

    IPC分类号： A61K31/403 ,  A61K31/12

    CPC分类号： C07C255/56 ,  C07C45/28 ,  C07C45/46 ,  C07C45/63 ,  C07C45/676 ,  C07C45/68 ,  C07C45/73 ,  C07C49/747 ,  C07C49/755 ,  C07C255/47 ,  C07C2603/30 ,  C07C47/575

    摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Pagets disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

    摘要翻译： 本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。 本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特氏病，牙周病， 软骨变性，子宫内膜异位症，子宫肌瘤疾病，潮热，LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增殖，肥胖症，失禁和癌症，特别是 乳房，子宫和前列腺。