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1. 发明申请

WO2004000858A2 NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE 审中-公开
标题翻译：作为RNA依赖性RNA病毒聚合酶抑制剂的核苷衍生物
公开(公告)号：WO2004000858A2
公开(公告)日：2003-12-31
申请号：PCT/US2003/019172
申请日：2003-06-17
申请人： MERCK & CO., INC. , ISIS PHARMACEUTICALS, INC. , CARROLL, Steven, S. , OLSEN, David, B. , DURETTE, Philippe, L. , BHAT, Balkrishen , DANDE, Prasad , ELDRUP, Anne, B.
发明人： CARROLL, Steven, S. , OLSEN, David, B. , DURETTE, Philippe, L. , BHAT, Balkrishen , DANDE, Prasad , ELDRUP, Anne, B.
IPC分类号： C07H
CPC分类号： C07H19/04 , C07H19/06 , C07H19/10 , C07H19/12 , C07H19/16 , C07H19/167 , C07H19/20
摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
摘要翻译：本发明提供作为RNA依赖性RNA病毒聚合酶抑制剂的核苷化合物及其某些衍生物。这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和/或用于治疗丙型肝炎感染。本发明还描述了单独或与其它对RNA依赖性RNA病毒感染（特别是HCV感染）有活性的试剂组合的药物组合物。还公开了本发明的核苷化合物抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

2. 发明公开

EP1551421A2 NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE 审中-公开
标题翻译： NUCLEUSIDDERIVATE作为病毒抑制剂; RNA依赖性RNA聚合酶
公开(公告)号：EP1551421A2
公开(公告)日：2005-07-13
申请号：EP03751777.8
申请日：2003-06-17
申请人： Merck & Co., Inc. , Isis Pharmaceuticals, Inc.
发明人： CARROLL, Steven, S. , OLSEN, David, B. , DURETTE, Philippe, L. , BHAT, Balkrishen , DANDE, Prasad , ELDRUP, Anne, B.
IPC分类号： A61K31/70 , C07H19/06 , C07H19/10 , C07H19/167 , C07H19/20
CPC分类号： C07H19/04 , C07H19/06 , C07H19/10 , C07H19/12 , C07H19/16 , C07H19/167 , C07H19/20
摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

3. 发明申请

WO2008079206A1 NUCLEOSIDE CYCLIC PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 审中-公开
标题翻译：用于治疗RNA依赖性RNA病毒感染的核苷酸环磷酰胺
公开(公告)号：WO2008079206A1
公开(公告)日：2008-07-03
申请号：PCT/US2007/025637
申请日：2007-12-14
申请人： MERCK & CO., INC. , ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A. , MEPPEN, Malte , NARJES, Frank , PACINI, Barbara , GARDELLI, Cristina , DURETTE, Philippe, L.
发明人： MEPPEN, Malte , NARJES, Frank , PACINI, Barbara , GARDELLI, Cristina , DURETTE, Philippe, L.
IPC分类号： A01N43/04 , C07H19/06
CPC分类号： C07H19/06
摘要： The present invention provides nucleoside cyclic phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside cyclic phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside cyclic phosphoramidates of the present invention. (I),
摘要翻译：本发明提供了作为RNA依赖性RNA病毒聚合酶抑制剂前体的结构式（I）核苷环状氨基磷酸酯。这些化合物是RNA依赖性RNA病毒复制抑制剂的前体，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体，作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。本发明还描述了含有这种核苷环状氨基磷酸酯的药物组合物，或者与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合。还公开了本发明的核苷环状氨基磷酸酯抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。（一世），

4. 发明申请

WO2006065335A2 FLUORINATED PYRROLO[2,3-D]PYRIMIDINE NUCLEOSIDES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 审中-公开
标题翻译：氟化吡咯并[2,3-D]嘧啶核苷用于治疗RNA依赖性RNA病毒感染
公开(公告)号：WO2006065335A2
公开(公告)日：2006-06-22
申请号：PCT/US2005/037224
申请日：2005-10-17
申请人： MERCK & CO., INC. , MACCOSS, Malcolm , OLSEN, David, B. , LEONE, Joseph , DURETTE, Philippe, L.
发明人： MACCOSS, Malcolm , OLSEN, David, B. , LEONE, Joseph , DURETTE, Philippe, L.
IPC分类号： A61K31/7072 , A61K31/519
CPC分类号： C07H19/14
摘要： The present invention provides fluorinated pyrrolo[2,3, d ]pyrimidine nucleoside compounds which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaeutical compositions containing such fluorinated pyrrolo[2,3- d ]pyrimidine nucleoside alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the fluorinated pyrrolo[2,3- d ]pyrimidine nucleoside of the present invention.
摘要翻译：本发明提供氟化吡咯并[2,3，d]嘧啶核苷化合物，其是RNA依赖性RNA病毒聚合酶的抑制剂。这些化合物是RNA依赖性RNA病毒复制的抑制剂，并且可用于治疗RNA依赖性RNA病毒感染。它们作为丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体特别有用，作为HCV复制抑制剂的前体和/或用于治疗丙型肝炎感染。本发明还描述了含有这种氟化吡咯并[2,3-d]嘧啶核苷的药物组合物，所述组合物单独或与其他活性物质联合用于抗RNA依赖性RNA病毒感染，特别是HCV感染。还公开了用氟化吡咯并[2,3-d]嘧啶核苷抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。本发明。

5. 发明申请

WO2008085508A3 NUCLEOSIDE ARYL PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 审中-公开
公开(公告)号：WO2008085508A3
公开(公告)日：2008-07-17
申请号：PCT/US2007/026468
申请日：2007-12-28
申请人： MERCK & CO., INC. , ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A. , NARJES, Frank , GARDELLI, Cristina , DONGHI, Monica , ATTENNI, Barbara , DURETTE, Philippe, L.
发明人： NARJES, Frank , GARDELLI, Cristina , DONGHI, Monica , ATTENNI, Barbara , DURETTE, Philippe, L.
IPC分类号： A01N43/04 , A61K31/70 , C07H19/04 , C07H19/10 , C07H19/20 , C07H19/048
摘要： The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention. (I)

6. 发明申请

WO1992021360A1 SUBSTITUTED N-CARBOXYALKYLPEPTIDYL DERIVATIVES AS ANTIDEGENERATIVE ACTIVE AGENTS 审中-公开
标题翻译：取代的N-羧基甲基衍生物作为抗真菌剂
公开(公告)号：WO1992021360A1
公开(公告)日：1992-12-10
申请号：PCT/US1992003809
申请日：1992-05-01
申请人： MERCK & CO., INC.
发明人： MERCK & CO., INC. , SAHOO, Soumya, P. , POLO, Scott, A. , DURETTE, Philippe, L. , ESSER, Craig, K. , HAGMANN, William, K. , KOPKA, Ihor, E. , CHAPMAN, Kevin, T. , CALDWELL, Charles, G.
IPC分类号： A61K37/00
CPC分类号： C07K5/022 , A61K38/00
摘要： Novel N-carboxyalkylpeptidyl compounds of formula (I) are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.
摘要翻译：发现式（I）的新型N-羧基烷基肽基化合物是基质金属蛋白酶介导的疾病的有用的抑制剂，包括骨关节炎，类风湿性关节炎，脓毒性关节炎，某些癌症中的肿瘤侵袭，牙周病，角膜溃疡，蛋白尿，疏水性表皮松解性大疱性炎症和与动脉粥样硬化斑块破裂相关的冠状动脉血栓形成。基质金属蛋白酶是含有蛋白酶的家族，包括但不限于基质溶素，胶原酶和明胶酶，其能够降解关节软骨和基底膜的主要成分。本文所要求的抑制剂也可用于预防可能导致永久性残疾的外伤性损伤后的病理后遗症。这些化合物也可以通过预防排卵或植入作为避孕的手段。

7. 发明公开

EP0586537A1 SUBSTITUTED N-CARBOXYALKYLPEPTIDYL DERIVATIVES AS ANTIDEGENERATIVE ACTIVE AGENTS 失效
标题翻译：作为抗衰老活性剂的取代的N-羧基烷基哌啶基衍生物
公开(公告)号：EP0586537A1
公开(公告)日：1994-03-16
申请号：EP92912475.0
申请日：1992-05-01
申请人： MERCK & CO. INC.
发明人： SAHOO, Soumya, P. , POLO, Scott, A. , DURETTE, Philippe, L. , ESSER, Craig, K. , HAGMANN, William, K. , KOPKA, Ihor, E. , CHAPMAN, Kevin, T. , CALDWELL, Charles, G.
IPC分类号： A61K38 , A61P1 , A61P3 , A61P7 , A61P9 , A61P13 , A61P15 , A61P27 , A61P29 , A61P35 , A61P43 , C07K5 , C07K14
CPC分类号： C07K5/022 , A61K38/00
摘要： On constate que les nouveaux composés N-carboxyalkylpeptidyle de la formule (I) présentent une utilité en tant qu'inhibiteurs des maladies à médiation par métalloendoprotéinase, telles que l'arthrose, la polyarthrite rheumatoïde, l'arthrite septique, l'invasion tumorale dans certains cancers, la paradontolyse, l'ulcération de la cornée, la protéineurie, l'épidermolyse bulleuse dystrophique, la thrombose coronaire associée à la rupture de plaques athéromatoses. Les métalloendoprotéinases fondamentales sont une famille de protéinases contenant du zinc renfermant de manière non exclusive de la stromélysine, de la collagénase et de la gélatinase, et qui sont capables de dégrader les principaux composants du cartilage articulaire et des membranes basales. Les inhibiteurs considérés dans la présente invention peuvent également servir à prévenir les sequelles pathologiques consécutives à des traumatismes pouvant entraîner une capacité permanente. Ces composés peuvent également servir de moyen de régulation des naissances par prévention de l'ovulation ou de l'implantation.
摘要翻译：据发现，该新型化合物式的N- carboxyalkylpeptidyle（I）可用作métalloendoprotéinase介导的疾病，例如骨关节炎，类风湿关节炎，脓毒性关节炎，肿瘤侵袭的抑制剂某些癌症，牙周疾病，角膜溃疡，中protéineurie，营养不良性表皮松解症，与破athéromatoses板相关联的冠状动脉血栓形成。基本métalloendoprotéinases是包含含有不限于基质溶素，胶原酶和明胶酶锌蛋白酶的家族，并且其能够降解关节软骨和基底膜的主要成分的。本发明中考虑的抑制剂也可以用于预防可能导致永久能力的创伤引起的病理性后遗症。这些化合物还可以通过防止排卵或植入作为控制生育的手段。

8. 发明公开

EP1804812A2 FLUORINATED PYRROLOÝ2,3-D¨PYRIMIDINE NUCLEOSIDES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 审中-公开
标题翻译：氟化吡咯并[2,3-d]嘧啶核苷FOR RNA依赖性RNA病毒感染的治疗
公开(公告)号：EP1804812A2
公开(公告)日：2007-07-11
申请号：EP05851224.5
申请日：2005-10-17
申请人： Merck & Co., Inc.
发明人： MACCOSS, Malcolm , OLSEN, David, B. , LEONE, Joseph , DURETTE, Philippe, L.
IPC分类号： A61K31/7052 , A61K31/7042 , C07H19/14
CPC分类号： C07H19/14
摘要： The present invention provides fluorinated pyrrolo[2,3,d]pyrimidine nucleoside compounds which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaeutical compositions containing such fluorinated pyrrolo[2,3-d]pyrimidine nucleoside alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the fluorinated pyrrolo[2,3-d]pyrimidine nucleoside of the present invention.

9. 发明公开

EP1034164A1 SUBSTITUTED BETA-ALANINE DERIVATIVES AS CELL ADHESION INHIBITORS 有权
标题翻译： β-丙氨酸衍生物作为细胞粘附抑制剂
公开(公告)号：EP1034164A1
公开(公告)日：2000-09-13
申请号：EP98959547.5
申请日：1998-11-24
申请人： MERCK & CO., INC.
发明人： DURETTE, Philippe, L. , HAGMANN, William, K. , KOPKA, Ihor, E. , MACCOSS, Malcolm , MILLS, Sander, G. , MUMFORD, Richard, A. , MAGRIOTIS, Plato, A.
IPC分类号： C07D207/16 , C07D207/48 , C07D211/34 , C07D211/96 , C07D217/26 , C07D241/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , A61K31/40 , A61K31/42 , A61K31/44 , A61K31/47 , A61K31/445 , A61K31/495
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60 , C07D217/26 , C07D241/04 , C07D403/12 , C07D405/12 , C07D413/12
摘要： β-Alanine derivatives of formula (I) are antagonists of VLA-4 and/or α4β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

10. 发明公开

EP0998282A1 SULFONAMIDES AS CELL ADHESION INHIBITORS 失效
标题翻译：磺酰胺作为细胞粘附抑制剂
公开(公告)号：EP0998282A1
公开(公告)日：2000-05-10
申请号：EP98924989.1
申请日：1998-05-29
申请人： Merck & Co., Inc. (a New Jersey corp.)
发明人： DURETTE, Philippe, L. , HAGMANN, William, K. , MacCOSS, Malcolm , MILLS, Sander, G. , MUMFORD, Richard, A.
IPC分类号： A61K31/42 , A61K31/415 , A61K31/425 , A61K31/505 , C07C255/03 , C07D207/08 , C07D217/18 , C07D231/04 , C07D263/04 , C07D277/04 , C07D285/12 , C07D295/023 , C07D413/10 , C07D417/10
CPC分类号： C07K5/06191 , A61K38/05 , C07K5/06026 , C07K5/06034 , C07K5/06052 , C07K5/06078 , C07K5/06113 , C07K5/06139
摘要： Compounds of formula (I) are antagonists of VLA-4 and/or α4-β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
摘要翻译：式（I）化合物是VLA-4和/或α4-β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理。这些化合物可以配制成药物组合物并适用于治疗哮喘，变态反应，炎症，多发性硬化和其他炎症和自身免疫性疾病。

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