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    • 1. 发明申请
    • ESTROGEN RECEPTOR MODULATORS
    • 雌激素受体调节剂
    • WO2004073610A2
    • 2004-09-02
    • PCT/US2004/003678
    • 2004-02-09
    • MERCK & CO., INC.SUN, WanyingCAMA, Lovji, D.
    • SUN, WanyingCAMA, Lovji, D.
    • A61K
    • C07D491/04
    • 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, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer.
    • 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,男子女性发育不良,血管平滑肌细胞增殖,肥胖症,失禁和癌症。
    • 3. 发明申请
    • CARBAPENEM ANTIBACTERIAL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
    • 卡巴因抗菌化合物,含有这些化合物的组合物和处理方法
    • WO1998011108A1
    • 1998-03-19
    • PCT/US1997015831
    • 1997-09-08
    • MERCK & CO., INC.CAMA, Lovji, D.WILKENING, Robert, R.RATCLIFFE, Ronald, W.BLIZZARD, Timothy, A.
    • MERCK & CO., INC.
    • C07D487/04
    • C07D477/14Y02P20/55
    • The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a sulfonamide containing ring system linked to the carbapenem nucleus through a CH2 group. The compounds are represented by formula (I) including pharmaceutically acceptable salts thereof, wherein: R represents H or methyl; CO2M represents a carboxylic acid, a carboxylate anion, a pharmaceutically acceptable ester group or a carboxylic acid protected by a protecting group; P represents hydrogen, hydroxyl, F or hydroxyl protected by a hydroxyl-protecting group; X and X represent hydrogen or X and X taken together represent a carbonyl group; and one of AB, BC and CD represents a fused aryl, heteroaryl or heteroarylium ring, and the other variables represent R, said fused aryl, heteroaryl or heteroarylium ring being substituted with from 1-4 R groups. Pharmaceutical compositions and methods of use are also included.
    • 本发明涉及碳青霉烯类抗菌剂,其中碳青霉烯细胞核在2-位被具有通过CH2基连接到碳青霉烯核的含磺酰胺的环系统取代。 化合物由式(I)表示,包括其药学上可接受的盐,其中:R 1表示H或甲基; CO 2 M表示羧酸,羧酸根阴离子,药学上可接受的酯基或被保护基保护的羧酸; P表示氢,羟基,F或被羟基保护基保护的羟基; X 1和X 2代表氢或X 1和X 2一起代表羰基; 并且AB,BC和CD之一代表稠合芳基,杂芳基或杂芳基环,其它变量表示R,所述稠合芳基,杂芳基或杂芳基环被1-4个R基团取代。 还包括药物组合物和使用方法。