Estrogen receptor modulators
    26.
    发明授权
    Estrogen receptor modulators 有权
    雌激素受体调节剂

    公开(公告)号:US07709508B2

    公开(公告)日:2010-05-04

    申请号:US12378198

    申请日:2009-02-12

    IPC分类号: A61K31/4192

    CPC分类号: A61K31/4192

    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.

    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,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,炎症性肠病,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。

    Spirocyclic 6-amido-carbapenems and azetidinones
    30.
    发明授权
    Spirocyclic 6-amido-carbapenems and azetidinones 失效
    螺环6-氨基 - 碳青霉烯类和氮杂环丁酮

    公开(公告)号:US5183887A

    公开(公告)日:1993-02-02

    申请号:US727192

    申请日:1991-07-09

    摘要: New antibacterial spirocyclic 6-amido carbapenems of the structural formulas: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-8 substituted or unsubstituted alkyl, or C.sub.6-10 substituted or unsubstituted aryl; R.sup.5 is hydrogen or a protecting group for alcohol; R.sup.6 is hydrogen or a protecting group for amido nitrogen; R.sup.7 is hydrogen or a protecting group for amido nitrogen; and R.sup.8 is hydroxy, hydrogen, C.sub.1-8 substituted or unsubstituted thioalkyl, C.sub.6-10 substituted or unsubstituted thioaryl, 5 or 6 membered, substituted or unsubstituted thioheteroaryl; and a process for their synthesis through novel spirocyclic 4-amido azetidinones are disclosed.

    摘要翻译: 其中R1是氢,C1-8取代或未取代的烷基或C6-10取代或未取代的芳基;新的抗菌螺环6-酰氨基碳青霉烯结构式: R5是氢或醇的保护基; R6是氢或氨基氮的保护基; R7是氢或酰氨基的保护基; R8为羟基,氢,C1-8取代或未取代的硫代烷基,C6-10取代或未取代的硫代芳基,5或6元取代或未取代的硫代杂芳基; 并且公开了通过新的螺环4-酰氨基氮杂环丁酮合成的方法。