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9 条记录 (耗时 0.017 秒)

    ESTROGEN RECEPTOR MODULATORS
    1.
    发明公开
    ESTROGEN RECEPTOR MODULATORS 有权
    雌激素受体调节剂

    公开(公告)号：EP1827421A2

    公开(公告)日：2007-09-05

    申请号：EP05852923.1

    申请日：2005-12-05

    申请人： Merck & Co., Inc.

    发明人： GREENLEE, Mark, L. ,  MENG, Dongfang ,  SPERBECK, Donald, M. ,  WILDONGER, Kenneth, J.

    IPC分类号： A61K31/41 ,  C07D403/12

    CPC分类号： C07D249/16

    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： 本发明涉及化合物及其衍生物，它们的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有关的多种病症，包括：骨损失，骨折，骨质疏松症，转移性骨疾病，佩吉特氏病，牙周病， 软骨退化，子宫内膜异位，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，年龄相关的轻度认知障碍，脑退行性疾病，再狭窄，男子女性型乳房，血管平滑肌细胞增殖，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，特别是乳房，子宫和前列腺。

    ESTROGEN RECEPTOR MODULATORS
    3.
    发明公开
    ESTROGEN RECEPTOR MODULATORS 有权
    雌激素受体调节剂

    公开(公告)号：EP1943224A2

    公开(公告)日：2008-07-16

    申请号：EP06849833.6

    申请日：2006-09-29

    申请人： Merck & Co., Inc.

    发明人： GREENLEE, Mark, L. ,  MENG, Dongfang ,  PARKER, Dann, L., Jr. ,  SUN, Wanying ,  WILDONGER, Kenneth, J. ,  WILKENING, Robert, R.

    IPC分类号： C07D231/00 ,  A61K31/416 ,  A61K31/4192

    CPC分类号： C07D249/16 ,  C07D231/54 ,  C07D235/02 ,  C07D405/04 ,  C07D413/04

    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, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

    THIOL DERIVATIVE, METALLO-BETA-LACTAMASE INHIBITORS
    9.
    发明公开
    THIOL DERIVATIVE, METALLO-BETA-LACTAMASE INHIBITORS 审中-公开
    巯基衍生物的金属-β-内酰胺酶抑制剂

    公开(公告)号：EP1192128A1

    公开(公告)日：2002-04-03

    申请号：EP00941349.3

    申请日：2000-06-12

    申请人： Merck & Co., Inc.

    发明人： BALKOVEC, James, M. ,  GREENLEE, Mark, L. ,  HAMMOND, Milton, L. ,  HECK, James, V.

    IPC分类号： C07C315/00 ,  C07C53/00 ,  C07C59/147

    CPC分类号： C07D307/91 ,  C07C323/56 ,  C07C327/32 ,  C07D213/56 ,  C07D333/38

    摘要： Thiol derivative compounds, pharmaceutically acceptable salts, and biolabile esters thereof, useful for inhibiting metallo-β-lactamases, bacterial enzymes which confer resistance to clinically relevant ß-lactam antibiotics, characterized by general formula (I): wherein: R1 is selected from straight, branched, unsaturated or alicyclic alkyl, optionally substituted with from 1 to 3 R¿x? groups; and (CH2)nAr, where Ar is an aryl selected from the group consisting of phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl, dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where n is 0, 1, 2 or 3, and where Ar is optionally substituted with 1 to 3 Rx groups; R?2¿ is selected from hydrogen; and a group of formula (II): wherein: R3 is selected from hydrogen; straight, branched, unsaturated or alicyclic alkyl, optionally substituted with from 1 to 3 R¿x? groups; (CH2)nAr, where Ar is an aryl selected from phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where Ar is optionally substituted with 1 to 3 Rx groups, and where n is 0, 1, 2 or 3; and a group of formula (III): wherein: R?4¿ is selected from hydrogen; and straight or branched alkyl; R5 is selected from hydrogen; straight, branched, unsaturated or alicyclic alkyl, optionally substituted with 1 to 3 R¿x? groups, where the alkyl group is optionally interrupted by X, where X is selected from O, S, NH and N(COCH3); allyloxy and 9-fluorenylmethyloxy; and (CH2)nAr, where Ar is selected from phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl, dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where n is 0, 1, 2 or 3, and where Ar is optionally substituted with 1 to 3 Rx groups; and Rx is selected from OR, CN, C(O)NH2, C(O)NHR, C(O)N(R)2, OC(O)NH2, OC(O)R, CHO, SO2NH2, SOR, CF3, C(O)R, COOR, F, Cl, Br, I, OCH2Ph, NHR, N(R)2, NHCOR, NHCO2t-Bu, NHCO2allyl, NH2, and R, where R is hydrogen, C1 to C15 alkyl, or aryl. The invention is further directed to a pharmaceutical composition containing the compound, as well as a method for treating bacterial infections in animals or humans, wherein the composition can be administered in combination with a β-lactam antibiotic.