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1. 发明申请

WO2003029268A1 ANDROSTANE 17-BETA-CARBOXAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：安哥拉17-β-羧酰胺作为雄激素受体调节剂
公开(公告)号：WO2003029268A1
公开(公告)日：2003-04-10
申请号：PCT/US2002/030864
申请日：2002-09-27
申请人： MERCK & CO., INC. , WANG, Jiabing , DUGGAN, Mark, E. , WHITMAN, David, B.
发明人： WANG, Jiabing , DUGGAN, Mark, E. , WHITMAN, David, B.
IPC分类号： C07J3/00
CPC分类号： A61K31/568 , A61K31/56 , A61K31/663 , C07J3/00 , A61K2300/00
摘要： Compounds of structural formula as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.
摘要翻译：公开了本文定义的结构式的化合物可用于在需要这种调节的患者中以组织选择性方式调节雄激素受体的方法，以及在患者中激活雄激素受体的功能的方法特别是其中雄性患者的前列腺或女性患者的子宫中的雄激素受体的功能被阻断并在骨和/或肌肉组织中活化的方法。这些化合物可用于治疗由雄激素缺乏引起的疾病或可通过雄激素给药改善的疾病，包括骨质疏松症，牙周病，骨折，骨重建手术后的骨损伤，肌肉减少症，虚弱，衰老皮肤，男性性腺机能减退，女性性功能障碍，妇女绝经后症状，动脉粥样硬化，高胆固醇血症，高脂血症，再生障碍性贫血和其他造血障碍，胰腺癌，肾癌，前列腺癌，关节炎和关节修复，单独或与其他活性剂组合。

2. 发明申请

WO2008143856A1 OXO BRIDGED DIAZEPAN OREXIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2008143856A1
公开(公告)日：2008-11-27
申请号：PCT/US2008/006128
申请日：2008-05-14
申请人： MERCK & CO., INC. , COX, Christopher, D. , WHITMAN, David, B.
发明人： COX, Christopher, D. , WHITMAN, David, B.
IPC分类号： A01N43/62 , A61K31/55
CPC分类号： C07D498/08
摘要： The present invention is directed to oxo bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲素受体的拮抗剂的氧代桥连的二氮杂环庚烷化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲素受体的疾病中的用途。

3. 发明申请

WO2008008551A2 2-SUBSTITUTED PROLINE BIS-AMIDE OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2-取代的脯氨酸双 - 酰胺类黄素受体拮抗剂
公开(公告)号：WO2008008551A2
公开(公告)日：2008-01-17
申请号：PCT/US2007/016125
申请日：2007-07-13
申请人： MERCK & CO., INC. , COX, Christopher, D. , WHITMAN, David, B. , BRESLIN, Michael, J.
发明人： COX, Christopher, D. , WHITMAN, David, B. , BRESLIN, Michael, J.
IPC分类号： A61K31/401
CPC分类号： C07D403/06 , C07D403/12 , C07D403/14
摘要： The present invention is directed to 2-substituted proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲素受体拮抗剂的2-取代的脯氨酸双酰胺化合物，其可用于治疗或预防神经病学和精神病学障碍以及食欲素受体为参与其中。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗其中涉及食欲肽受体的这些疾病中的用途。

4. 发明申请

WO2007126935A3 DIAZEPAN OREXIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2007126935A3
公开(公告)日：2007-11-08
申请号：PCT/US2007/007738
申请日：2007-03-27
申请人： MERCK & CO., INC. , BRASHEAR, Karen, M. , COLEMAN, Paul, J. , COX, Christopher, D. , SMITH, Anthony, M. , WHITMAN, David, B.
发明人： BRASHEAR, Karen, M. , COLEMAN, Paul, J. , COX, Christopher, D. , SMITH, Anthony, M. , WHITMAN, David, B.
IPC分类号： A61P3/04 , A61K31/55 , C07D243/08
摘要： The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

5. 发明申请

WO2006127550A1 PROLINE BIS-AMIDE OREXIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2006127550A1
公开(公告)日：2006-11-30
申请号：PCT/US2006/019649
申请日：2006-05-22
申请人： MERCK & CO., INC. , BERGMAN, Jeffrey, M. , COLEMAN, Paul, J. , COX, Christopher , HARTMAN, George, D. , LINDSLEY, Craig , MERCER, Swati Pal , ROECKER, Anthony, J. , WHITMAN, David, B.
发明人： BERGMAN, Jeffrey, M. , COLEMAN, Paul, J. , COX, Christopher , HARTMAN, George, D. , LINDSLEY, Craig , MERCER, Swati Pal , ROECKER, Anthony, J. , WHITMAN, David, B.
IPC分类号： C07D403/12
CPC分类号： C07D403/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is directed to proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲素受体的拮抗剂的脯氨酸双酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲素受体的疾病中的用途。

6. 发明申请

WO2006086358A2 MITOTIC KINESIN INHIBITORS 审中-公开
公开(公告)号：WO2006086358A2
公开(公告)日：2006-08-17
申请号：PCT/US2006/004214
申请日：2006-02-06
申请人： MERCK & CO., INC. , BRESLIN, Michael, J. , COLEMAN, Paul, J. , COX, Christopher, D. , NEILSON, Lou Anne , WHITMAN, David, B.
发明人： BRESLIN, Michael, J. , COLEMAN, Paul, J. , COX, Christopher, D. , NEILSON, Lou Anne , WHITMAN, David, B.
IPC分类号： A61K31/416
CPC分类号： C07D491/052
摘要： The present invention relates to tricyclic pyrazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译：本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的三环吡唑。本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

7. 发明申请

WO2007025069A2 DIAZASPIRODECANE OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译： DIAZASPIRODECANE OREXIN受体拮抗剂
公开(公告)号：WO2007025069A2
公开(公告)日：2007-03-01
申请号：PCT/US2006/033124
申请日：2006-08-24
申请人： MERCK & CO., INC. , BRESLIN, Michael, J. , COX, Christopher, D. , WHITMAN, David, B.
发明人： BRESLIN, Michael, J. , COX, Christopher, D. , WHITMAN, David, B.
IPC分类号： A61K31/4747 , C07D471/10
CPC分类号： C07D471/10
摘要： The present invention is directed to diazaspirodecane compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲素受体的拮抗剂的二氮杂螺十一烷化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲素受体的疾病中的用途。

8. 发明申请

WO2007019234A3 AMINOETHANE SULFONAMIDE OREXIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2007019234A3
公开(公告)日：2007-02-15
申请号：PCT/US2006/030301
申请日：2006-07-31
申请人： MERCK & CO., INC. , COX, Christopher, D. , COLEMAN, Paul, J. , WHITMAN, David, B.
发明人： COX, Christopher, D. , COLEMAN, Paul, J. , WHITMAN, David, B.
IPC分类号： A61K31/66 , A01N57/00
摘要： The present invention is directed to aminoethane sulfonamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

9. 发明申请

WO2010048010A1 2,5-DISUBSTITUTED PIPERIDINE OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2,5-取代的哌啶氧黄嘌呤受体拮抗剂
公开(公告)号：WO2010048010A1
公开(公告)日：2010-04-29
申请号：PCT/US2009/060736
申请日：2009-10-15
申请人： MERCK SHARP & DOHME CORP. , BRESLIN, Michael, J. , COLEMAN, Paul, J. , COX, Christopher, D. , SCHREIER, John, D. , WHITMAN, David, B.
发明人： BRESLIN, Michael, J. , COLEMAN, Paul, J. , COX, Christopher, D. , SCHREIER, John, D. , WHITMAN, David, B.
IPC分类号： C07D413/00 , C07D413/02
CPC分类号： C07D413/14 , C07D401/10 , C07D401/14 , C07D417/14
摘要： The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲素受体拮抗剂的2,5-二取代的哌啶酰胺化合物，其可用于治疗或预防神经病学和精神病学障碍以及食欲素受体为参与其中。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗其中涉及食欲肽受体的这些疾病中的用途。

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