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1. 发明申请

WO2005115147A3 HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译： HIV逆转录酶抑制剂
公开(公告)号：WO2005115147A3
公开(公告)日：2007-04-19
申请号：PCT/US2005016671
申请日：2005-05-12
申请人： MERCK & CO INC , ANGELETTI P IST RICHERCHE BIO , SHAW-REID CATHRYN A , MILLER MICHAEL D , HAZUDA DARIA J , FERRER MARC , SUR SYLVIE M , SUMMA VINCENZO , LYLE TERRY A , KINZEL OLAF , PESCATORE GIOVANNA , MURAGLIA ESTER , ORVIETO FEDERICA , WILLIAMS PETER D
发明人： SHAW-REID CATHRYN A , MILLER MICHAEL D , HAZUDA DARIA J , FERRER MARC , SUR SYLVIE M , SUMMA VINCENZO , LYLE TERRY A , KINZEL OLAF , PESCATORE GIOVANNA , MURAGLIA ESTER , ORVIETO FEDERICA , WILLIAMS PETER D
IPC分类号： A61K31/41 , A01N43/64
CPC分类号： C07D257/04 , A61K31/41
摘要： Tetrazolyl derivatives of Formula (I): are HIV reverse transcriptase inhibitors, wherein U is O, S(O) n where n is an integer equal to zero, 1 or 2, or N(R 4 ); V is optionally substituted C 1-8 alkylene; W is C(O)N(R 2 ) or a direct bond linking V to R 3 ; and R 1 , R 2 , R 3 and R 4 are defined herein. The derivatives of Formula I are useful in the inhibition of HIV reverse transcriptase, the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The derivatives are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The derivatives 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：式（I）的四唑基衍生物：HIV逆转录酶抑制剂，其中U是O，S（O）n N，其中n是等于零，1或2的整数，或N（R 0 > 4 ）; V是任选取代的C 1-8烷基亚烷基; W是C（O）N（R 2）或连接V至R 3的直接键; 和R 1，R 2，R 3和R 4在本文中定义。式I的衍生物可用于抑制HIV逆转录酶，预防和治疗艾滋病毒感染以及预防，延迟发病和治疗艾滋病。这些衍生物用于抗艾滋病毒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。衍生物及其盐可以用作药物组合物中的成分，任选地与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

2. 发明申请

WO2007050510A2 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译： HIV整合酶抑制剂
公开(公告)号：WO2007050510A2
公开(公告)日：2007-05-03
申请号：PCT/US2006041280
申请日：2006-10-23
申请人： MERCK & CO INC , WAI JOHN S , WILLIAMS PETER D , LYLE TERRY A
发明人： WAI JOHN S , WILLIAMS PETER D , LYLE TERRY A
IPC分类号： A61K31/498 , C07D487/04
CPC分类号： C07D487/04
摘要： Substituted hydroxytetrahydropyrrolopyrazinone and substituted hydroxytetrahydro-pyrazolopyrazinone compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein R 1 , R 2 , R 3 , R 4 ; R 5 , X, ring A, and Q are as 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：式（I）的取代的羟基四氢吡咯并吡嗪酮和取代的羟基四氢吡唑并吡嗪酮化合物是HIV整合酶的抑制剂和HIV复制的抑制剂：（I）其中R 1，R 2，R 1， SUP> 3 ，R ^{4 ; R 5，X，环A和Q如本文所定义。这些化合物可用于预防和治疗HIV感染以及预防，延缓艾滋病的发作和治疗。这些化合物本身作为化合物或以药学上可接受的盐的形式用于抗HIV感染和AIDS。化合物及其盐可以用作药物组合物中的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。}

3. 发明申请

WO2005086700A3 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：WO2005086700A3
公开(公告)日：2006-09-08
申请号：PCT/US2005007106
申请日：2005-03-04
申请人： MERCK & CO INC , MORRISSETTE MATTHEW M , WILLIAMS PETER D , WAI JOHN S , FISHER THORSTEN E , LYLE TERRY A
发明人： MORRISSETTE MATTHEW M , WILLIAMS PETER D , WAI JOHN S , FISHER THORSTEN E , LYLE TERRY A
IPC分类号： C07D221/18 , C07D211/08 , C07D211/68 , C07D211/80 , C07D213/02 , C07D401/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00 , C07D471/04 , C07D471/10
CPC分类号： C07D471/04 , C07D471/10
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein Z, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 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：式I化合物是HIV整合酶和HIV复制抑制剂的抑制剂：（I）其中Z，R 1，R 2，R 3， R 4，R 5，R 6，R 7，R 8，和R 9在本文中定义。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。

4. 发明申请

WO2004032834A3 THROMBIN INHIBITORS 审中-公开
标题翻译： THROMBIN抑制剂
公开(公告)号：WO2004032834A3
公开(公告)日：2004-06-10
申请号：PCT/US0330867
申请日：2003-09-30
申请人： MERCK & CO INC , STAAS DONNETTE D , LYLE TERRY A , WILLIAMS PETER D , SANDERSON PHILIP E J
发明人： STAAS DONNETTE D , LYLE TERRY A , WILLIAMS PETER D , SANDERSON PHILIP E J
IPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12
CPC分类号： C07D417/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12
摘要： Compounds of the invention (Formula I) are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: I.The compounds are useful for preventing or treating unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels, in a mammal.
摘要翻译：本发明的化合物（式I）可用于抑制具有以下结构的凝血酶和相关的血栓形成闭塞：I，该化合物可用于预防或治疗不稳定心绞痛，难治性心绞痛，心肌梗塞，短暂性脑缺血发作，心房纤颤，血栓形成中风，栓塞性中风，深静脉血栓形成，播散性血管内凝血，纤维蛋白的眼部积聚以及再通血管的再闭塞或再狭窄。

5. 发明申请

WO2004024078A3 DIHYDROXYPYRIDOPYRAZINE-1,6-DIONE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：用作HIV整合酶抑制剂的二羟基吡啶并吡嗪-1,6-二酮化合物
公开(公告)号：WO2004024078A3
公开(公告)日：2004-05-13
申请号：PCT/US0328366
申请日：2003-09-10
申请人： MERCK & CO INC , WAI JOHN S , KIM BOYOUNG , FISHER THORSTEN E , ZHUANG LINGHANG , WILLIAMS PETER D , LYLE TERRY A , LANGFORD H MARIE , ROBINSON KYLE A
发明人： WAI JOHN S , KIM BOYOUNG , FISHER THORSTEN E , ZHUANG LINGHANG , WILLIAMS PETER D , LYLE TERRY A , LANGFORD H MARIE , ROBINSON KYLE A
IPC分类号： A61K20060101 , A61K31/498 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61P31/18 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14
CPC分类号： C07D471/14 , C07D471/04
摘要： 8,9-Dihydroxydihydropyridopyrazine-1,6-diones and 8,9-dihydroxypyridopyrazine-1,6-diones are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the pyridopyrazinediones are of Formula (I): (I),wherein R , R , R , R and R 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.
摘要翻译： 8,9-二羟基二氢吡啶并吡嗪-1,6-二酮和8,9-二羟基吡啶并吡嗪-1,6-二酮是HIV整合酶抑制剂和HIV复制抑制剂。在一个实施方案中，吡啶并吡嗪二酮具有式（I）：（I），其中R 1，R 2，R 3，R 4和R 5如本文所定义。这些化合物可用于预防和治疗HIV感染以及预防，延缓艾滋病的发作和治疗。这些化合物本身作为化合物或以药学上可接受的盐的形式用于抗HIV感染和AIDS。化合物及其盐可以用作药物组合物中的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。描述了预防，治疗或延缓AIDS发作的方法以及预防或治疗HIV感染的方法。

6. 发明申请

WO2005110414A3 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：WO2005110414A3
公开(公告)日：2006-02-16
申请号：PCT/US2005015200
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 , A61K31/5025 , C07D487/12 , C07D487/14 , A61K31/4985
CPC分类号： A61K31/5025 , C07D487/14
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
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，二酮化合物是式（I），其中R

8. 发明公开

EP1549315A4 DIHYDROXYPYRIDOPYRAZINE-1,6-DIONE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS 审中-公开
标题翻译： DIHYDROXYPYRIDOPYRAZIN -1,6- DION化合物作为HIV整合酶抑制剂
公开(公告)号：EP1549315A4
公开(公告)日：2007-05-23
申请号：EP03749574
申请日：2003-09-10
申请人： MERCK & CO INC
发明人： WAI JOHN S , KIM BOYOUNG , FISHER THORSTEN E , ZHUANG LINGHANG , WILLIAMS PETER D , LYLE TERRY A , LANGFORD H MARIE , ROBINSON KYLE A
IPC分类号： C07D471/04 , A61K20060101 , A61K31/498 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61P31/18 , C07D471/14 , C07D487/04 , C07D487/14
CPC分类号： C07D471/14 , C07D471/04

9. 发明公开

EP1017393A4 PYRAZINONE THROMBIN INHIBITORS 审中-公开
标题翻译： -pyrazinone凝血酶抑制剂
公开(公告)号：EP1017393A4
公开(公告)日：2002-01-23
申请号：EP98946835
申请日：1998-09-03
申请人： MERCK & CO INC
发明人： SANDERSON PHILIP E , LYLE TERRY A , DORSEY BRUCE D
IPC分类号： C07D241/20 , A61K31/4965 , A61K31/497 , A61P7/02 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14

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