ESTRATRIENE DERIVATIVES COMPRISING HETEROCYCLIC BIOISOSTERES FOR THE PHENOLIC A-RING
    1.
    发明申请
    ESTRATRIENE DERIVATIVES COMPRISING HETEROCYCLIC BIOISOSTERES FOR THE PHENOLIC A-RING 审中-公开
    包含苯酚环的杂环生物活性成分的雌激素衍生物

    公开(公告)号:US20110190246A1

    公开(公告)日:2011-08-04

    申请号:US13055388

    申请日:2009-07-14

    CPC分类号: C07J71/0047

    摘要: The present invention is directed to novel pyrazolo-estrien and triazolo-estrien-derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by an estrogen receptor such as hot flashes, vaginal dryness, osteopenia, osteoporosis, hyperlipidemia, loss of cognitive function, degenerative brain diseases, cardiovascular diseases, cerebrovascular diseases, hormone sensitive cancers and hyperplasia (in tissues including breast, endometrium, and cervix in women and prostate in men), endometriosis, uterine fibroids, osteoarthritis; and as contraceptive agents either alone or in combination with a progestogen or progestogen antagonist. The compounds of the invention are selective estrogen receptor modulators.

    摘要翻译: 本发明涉及新颖的吡唑并雌三烯衍生物,含有它们的药物组合物及其用于治疗或预防由雌激素受体介导的疾病和疾病,例如潮热,阴道干燥,骨质减少,骨质疏松症, 高脂血症,认知功能丧失,退行性脑疾病,心血管疾病,脑血管疾病,激素敏感性癌症和增生(包括男性和女性前列腺中的乳腺,子宫内膜和子宫颈组织),子宫内膜异位症,子宫肌瘤,骨关节炎; 并且作为避孕药单独使用或与孕激素或孕激素拮抗剂组合。 本发明的化合物是选择性雌激素受体调节剂。

    Process for the preparation of &agr;-haloketones
    3.
    发明授权
    Process for the preparation of &agr;-haloketones 失效
    α-卤代酮的制备方法

    公开(公告)号:US06667422B2

    公开(公告)日:2003-12-23

    申请号:US10233925

    申请日:2002-09-03

    IPC分类号: C07C4563

    摘要: A process for preparing an &agr;-haloketone of the formula (1) where R1 is an optionally heteroatom-containing and optionally substituted hydrocarbon radical, R2 is a hydrogen, alkyl, aralkyl or aryl radical, and X is a halogen radical, by reacting a carboxylic acid derivative of the general formula (2) where L is a leaving group, with a mono- or dienolate of a silyl ester of the formula (3) where R3 and R4 are identical or different alkyl, aryl, alkenyl or aralkyl radicals; and hydrolyzing the reaction product immediately afterwards by adding acid and decarboxylating to (1). The product &agr;-haloketone may be reduced to the corresponding &agr;-haloalcohol.

    摘要翻译: 制备式(1)的α-卤代酮的方法,其中R 1是任选含杂原子的和任选取代的烃基,R 2是氢,烷基,芳烷基或芳基,X是卤素 自由基,其中L是离去基团的通式(2)的羧酸衍生物与式(3)的甲硅烷基酯的单或二烯醇酯反应,其中R 3和R 4相同 或不同的烷基,芳基,烯基或芳烷基;然后通过加入酸和脱羧至(1),立即水解反应产物。 产物α-卤代酮可以还原成相应的α-卤代醇。