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1. 发明申请

WO2003099211A3 MITOTIC KINESIN INHIBITORS 审中-公开
公开(公告)号：WO2003099211A3
公开(公告)日：2003-12-04
申请号：PCT/US2003/015861
申请日：2003-05-19
申请人： MERCK & CO., INC. , COLEMAN, Paul, J. , HARTMAN, George, D. , NEILSON, Lou Anne
发明人： COLEMAN, Paul, J. , HARTMAN, George, D. , NEILSON, Lou Anne
IPC分类号： C07D239/36
摘要： The present invention relates to dihydropyrimidone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

2. 发明申请

WO2006007491A1 MITOTIC KINESIN INHIBITORS 审中-公开
公开(公告)号：WO2006007491A1
公开(公告)日：2006-01-19
申请号：PCT/US2005/022730
申请日：2005-06-27
申请人： MERCK & CO., INC. , BERGMAN, Jeffrey, M. , COLEMAN, Paul, J. , FRALEY, Mark, E. , GARBACCIO, Robert, M. , HARTMAN, George, D. , LI, Chunze , NEILSON, Lou Anne , OLSON, Christy, M. , TASBER, Edward, S.
发明人： BERGMAN, Jeffrey, M. , COLEMAN, Paul, J. , FRALEY, Mark, E. , GARBACCIO, Robert, M. , HARTMAN, George, D. , LI, Chunze , NEILSON, Lou Anne , OLSON, Christy, M. , TASBER, Edward, S.
IPC分类号： C07D498/04 , C07D519/00 , A61K31/5383 , A61P35/00
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention relates to tricyclic pyrazoles according to Formula (I) 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驱动蛋白的根据式（I）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。

3. 发明申请

WO2003099211A2 MITOTIC KINESIN INHIBITORS 审中-公开
公开(公告)号：WO2003099211A2
公开(公告)日：2003-12-04
申请号：PCT/US2003/015861
申请日：2003-05-19
申请人： MERCK & CO., INC. , COLEMAN, Paul, J. , HARTMAN, George, D. , NEILSON, Lou Anne
发明人： COLEMAN, Paul, J. , HARTMAN, George, D. , NEILSON, Lou Anne
IPC分类号： A61K
CPC分类号： C07D239/36 , C07D239/52 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to dihydropyrimidone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related 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驱动蛋白的二氢嘧啶酮化合物。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。

4. 发明申请

WO2003034987A2 ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：雄激素受体调节剂及其使用方法
公开(公告)号：WO2003034987A2
公开(公告)日：2003-05-01
申请号：PCT/US2002/033252
申请日：2002-10-15
申请人： MERCK & CO., INC. , COLEMAN, Paul, J. , NEILSON, Lou Anne
发明人： COLEMAN, Paul, J. , NEILSON, Lou Anne
IPC分类号： A61K
CPC分类号： C07D491/04 , C07D471/04 , C07D491/10
摘要： Compounds of structural formula (I) are disclosed as useful for modulating the androgen receptor (AR) in a tissue selective manner in a patient in need of such modulation, and in particular for antagonizing AR in the prostate of a male patient or in the uterus of a female patient and agonizing AR in bone and/or muscle tissue. These compounds are useful in the treating 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. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.
摘要翻译：结构式（I）的化合物被公开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（AR），并且特别用于拮抗前列腺中的AR 的男性患者或女性患者的子宫中，并且在骨骼和/或肌肉组织中激动性AR。这些化合物可用于治疗由雄激素缺乏引起的或可通过雄激素给药而改善的疾病，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，老化皮肤，男性性腺机能减退，女性性行为女性绝经后症状，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。此外，这些化合物可单独用作药物组合物成分，并与其它活性剂组合使用。

5. 发明申请

WO2004112699A2 MITOTIC KINESIN INHIBITORS 审中-公开
公开(公告)号：WO2004112699A2
公开(公告)日：2004-12-29
申请号：PCT/US2004/018137
申请日：2004-06-08
申请人： MERCK & CO., INC. , COLEMAN, Paul, J. , NEILSON, Lou Anne
发明人： COLEMAN, Paul, J. , NEILSON, Lou Anne
IPC分类号： A61K
CPC分类号： C07D487/04 , C07D491/048
摘要： The present invention relates to bicyclic dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related 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驱动蛋白的双环二氢吡咯化合物。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。

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

WO2004112699A3 MITOTIC KINESIN INHIBITORS 审中-公开
公开(公告)号：WO2004112699A3
公开(公告)日：2004-12-29
申请号：PCT/US2004/018137
申请日：2004-06-08
申请人： MERCK & CO., INC. , COLEMAN, Paul, J. , NEILSON, Lou Anne
发明人： COLEMAN, Paul, J. , NEILSON, Lou Anne
IPC分类号： A01N43/58
摘要： The present invention relates to bicyclic dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

8. 发明申请

WO2005110414A2 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：艾滋病毒整合抑制剂
公开(公告)号：WO2005110414A2
公开(公告)日：2005-11-24
申请号：PCT/US2005/015200
申请日：2005-05-03
申请人： MERCK & CO., INC. , WAI, John, S. , VACCA, Joseph, P. , ZHUANG, Linghang , KIM, Boyoung , LYLE, Terry, A. , WISCOUNT, Catherine, M. , EGBERTSON, Melissa, S. , NEILSON, Lou Anne , EMBREY, Mark , FISHER, Thorsten, E. , STAAS, Donnette, D.
发明人： WAI, John, S. , VACCA, Joseph, P. , ZHUANG, Linghang , KIM, Boyoung , LYLE, Terry, A. , WISCOUNT, Catherine, M. , EGBERTSON, Melissa, S. , NEILSON, Lou Anne , EMBREY, Mark , FISHER, Thorsten, E. , STAAS, Donnette, D.
IPC分类号： A61K31/502
CPC分类号： A61K31/5025 , C07D487/14 , Y02A50/414
摘要： Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：羟基取代的吡嗪并吡咯并哒嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。在一个实施方案中，二酮化合物具有式（I），其中R 1，R 2，R 3，R 4，R 5，R 6和R 7定义于此。这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。这些化合物被用作抗HIV感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

9. 发明申请

WO2006014877A2 POTASSIUM CHANNEL INHIBITORS 审中-公开
公开(公告)号：WO2006014877A2
公开(公告)日：2006-02-09
申请号：PCT/US2005/026337
申请日：2005-07-25
申请人： MERCK & CO., INC. , BILODEAU, Mark, T. , DINSMORE, Christopher, J. , BERGMAN, Jeffrey, M. , TROTTER, B. Wesley , NEILSON, Lou Anne , WU, Zhicai , MANLEY, Peter , HARTNETT, John
发明人： BILODEAU, Mark, T. , DINSMORE, Christopher, J. , BERGMAN, Jeffrey, M. , TROTTER, B. Wesley , NEILSON, Lou Anne , WU, Zhicai , MANLEY, Peter , HARTNETT, John
IPC分类号： A61K31/506 , A61K31/444 , C07D401/14 , C07D403/14
CPC分类号： C07D213/75 , C07D213/06 , C07D213/61 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/76 , C07D401/14 , C07D413/14
摘要： The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

10. 发明申请

WO2008030412A2 SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
标题翻译： SPIROPIPERIDINEβ-分泌酶抑制剂治疗ALZEIMER'S DISEASE
公开(公告)号：WO2008030412A2
公开(公告)日：2008-03-13
申请号：PCT/US2007/019259
申请日：2007-09-04
申请人： MERCK & CO., INC. , SUNESIS PHARMACEUTICALS, INC. , EGBERTSON, Melissa, S. , STAUFFER, Shaun, R. , COBURN, Craig, A. , BARROW, James, C. , YANG, Wenjin , LU, Wanli , FAHR, Bruce , NEILSON, Lou Anne , WAI, Jenny M.
发明人： EGBERTSON, Melissa, S. , STAUFFER, Shaun, R. , COBURN, Craig, A. , BARROW, James, C. , YANG, Wenjin , LU, Wanli , FAHR, Bruce , NEILSON, Lou Anne , WAI, Jenny M.
IPC分类号： A61K31/4747
CPC分类号： C07D471/10 , C07D498/10
摘要： The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译：本发明涉及式（I）的螺哌啶化合物及其互变异构体，它们是β-分泌酶的抑制剂并且可用于治疗其中β-分泌酶涉及诸如阿尔茨海默氏病等。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治疗涉及β-分泌酶的疾病中的用途。

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