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    • 10. 发明公开
    • 에스트로겐 수용체 조절제
    • 雌激素受体调节剂
    • KR1020070083896A
    • 2007-08-24
    • KR1020077009961
    • 2005-10-28
    • 머크 샤프 앤드 돔 코포레이션
    • 윌케닝로버트알프라이드아미
    • C07C49/747C07C251/44C07C255/47A61K31/12
    • C07C251/44C07B2200/07C07C45/676C07C45/68C07C45/69C07C49/747C07C49/755C07C255/47C07C2603/86C07C2603/97
    • The present invention relates to gibbane derivatives of formula (I), 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.
    • 本发明涉及式(I)的赤霉素衍生物,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,子宫肌瘤病,热潮红症,低密度脂蛋白胆固醇水平升高,心血管疾病,认知功能障碍,年龄相关性轻度认知障碍,脑退行性疾病,再狭窄,男子乳腺发育不良,血管平滑肌细胞增生,肥胖,失禁 ,炎症,炎性肠病,肠易激综合征,性功能障碍,高血压,视网膜变性和癌症,特别是乳腺,子宫和前列腺。