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    ESTROGEN RECEPTOR MODULATORS
    2.
    发明申请
    ESTROGEN RECEPTOR MODULATORS 审中-公开
    雌激素受体调节剂

    公开(公告)号：WO2008057309A3

    公开(公告)日：2008-08-07

    申请号：PCT/US2007022798

    申请日：2007-10-29

    Applicant: MERCK & CO INC ,  ZHANG ZHOUPENG ,  WILKENING ROBERT R ,  GREENLEE MARK L ,  FRIED AMY KATHLEEN

    Inventor： ZHANG ZHOUPENG ,  WILKENING ROBERT R ,  GREENLEE MARK L ,  FRIED AMY KATHLEEN

    IPC: C07C49/00

    CPC classification number: C07C62/38 ,  C07C45/63 ,  C07C45/65 ,  C07C45/66 ,  C07C45/673 ,  C07C45/676 ,  C07C45/78 ,  C07C49/747 ,  C07C49/755 ,  C07C305/22 ,  C07C2603/16 ,  C07C2603/86

    Abstract: 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.

    Abstract translation: 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各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特病，牙周炎 疾病，软骨变性，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。

    ANTIFUNGAL AGENTS
    5.
    发明申请
    ANTIFUNGAL AGENTS 审中-公开
    反真菌药

    公开(公告)号：WO2010019203A8

    公开(公告)日：2011-03-17

    申请号：PCT/US2009004557

    申请日：2009-08-07

    Applicant: MERCK SHARP & DOHME ,  GREENLEE MARK L ,  WILKENING ROBERT ,  APGAR JAMES ,  WILDONGER KENNETH JAMES ,  MENG DONGFANG ,  PARKER DANN L JR

    Inventor： GREENLEE MARK L ,  WILKENING ROBERT ,  APGAR JAMES ,  WILDONGER KENNETH JAMES ,  MENG DONGFANG ,  PARKER DANN L JR

    IPC: A01N37/18

    CPC classification number: A01N43/653 ,  A61K31/4196 ,  C07J71/0005

    Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (l,3)-ß-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating, and/or preventing fungal infections and associated diseases and conditions.

    Abstract translation: 本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。 还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这种化合物作为抗真菌剂和/或（1,3）-β-D-葡聚糖合酶抑制剂的方法。 所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。

    2-(FLUORENONYL)-CARBAPENEMS, COMPOSITIONS AND METHODS OF USE
    8.
    发明申请
    2-(FLUORENONYL)-CARBAPENEMS, COMPOSITIONS AND METHODS OF USE 审中-公开
    2-（氟甲基） - 氨基甲酸酯，组合物和使用方法

    公开(公告)号：WO1997004770A1

    公开(公告)日：1997-02-13

    申请号：PCT/US1996012392

    申请日：1996-07-26

    Applicant: MERCK & CO., INC. ,  GREENLEE, Mark, L. ,  LAUB, Joanne, B. ,  ROUEN, Gregory, P.

    Inventor： MERCK & CO., INC.

    IPC: A61K31/40

    CPC classification number: C07D477/14

    Abstract: Carbapenems are disclosed in which the 2-position sidechain contains a fluorenone moiety that is substituted by a bis cationic group. The compounds are of general formula (I). The compounds are effective for treating methicillin resistant staphylococcus aureus (MRSA) and methicillin resistant coagulase negative staphylococcus (MRCNS). Pharmaceutical compositions and methods of treatment are also included.

    Abstract translation: 公开了其中2位侧链含有被双​​阳离子基团取代的芴酮部分的碳青霉烯。 该化合物具有通式（I）。 该化合物可有效治疗耐甲氧西林金黄色葡萄球菌（MRSA）和耐甲氧西林凝固酶阴性葡萄球菌（MRCNS）。 还包括药物组合物和治疗方法。

    ANTIFUNGAL AGENTS
    10.
    发明申请
    ANTIFUNGAL AGENTS 审中-公开
    反真菌药

    公开(公告)号：WO2010019203A1

    公开(公告)日：2010-02-18

    申请号：PCT/US2009/004557

    申请日：2009-08-07

    Applicant: MERCK SHARP & DOHME CORP. ,  GREENLEE, Mark, L. ,  WILKENING, Robert ,  APGAR, James ,  WILDONGER, Kenneth, James ,  MENG, Dongfang ,  PARKER, Dann, L.

    Inventor： GREENLEE, Mark, L. ,  WILKENING, Robert ,  APGAR, James ,  WILDONGER, Kenneth, James ,  MENG, Dongfang ,  PARKER, Dann, L.

    IPC: A01N37/18

    CPC classification number: A01N43/653 ,  A61K31/4196 ,  C07J71/0005

    Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (l,3)- β -D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating, and/or preventing fungal infections and associated diseases and conditions.

    Abstract translation: 本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。 还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这些化合物作为（1,3）-β-D-葡聚糖合酶的抗真菌剂和/或抑制剂的方法。 所公开的化合物，其药学上可接受的盐，水合物和前药以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。

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