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1.发明公开CYCLIC KETAL BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权循环缩酮ALSβ-分泌酶抑制剂用于治疗阿尔茨海默氏病的治疗
公开(公告)号：EP1912963A2
公开(公告)日：2008-04-23
申请号：EP06789003.8
申请日：2006-07-28
申请人： Merck & Co., Inc.
IPC分类号： C07D307/22 , A61K31/443 , A61K31/341
CPC分类号： C07D307/22 , C07D405/12
摘要： The present invention is directed to cyclic ketal compounds of formula (I); 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.
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2.发明公开MACROCYCLIC TERTIARY AMINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权万家乐CYCLICAL叔胺β-分泌酶抑制剂用于治疗阿尔茨海默氏病的治疗
公开(公告)号：EP1814537A2
公开(公告)日：2007-08-08
申请号：EP05825640.5
申请日：2005-11-14
申请人： Merck & Co., Inc.
发明人： NANTERMET, Philippe, G. , RAJAPAKSE, Hemaka, A. , SELNICK, Harold, G. , LINDSLEY, Stacey , MOORE, Keith, P. , STACHEL, Shawn, J.
IPC分类号： A61K31/33
CPC分类号： C07D273/01 , C07D267/00 , C07D313/00 , C07D321/00 , C07D323/00 , C07D413/04 , C07D498/08
摘要： The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I), 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.
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3.发明公开BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权苄基醚和苄氨基β-分泌酶抑制剂用于治疗阿尔茨海默氏病的治疗
公开(公告)号：EP1673078A2
公开(公告)日：2006-06-28
申请号：EP04789263.3
申请日：2004-09-29
申请人： Merck & Co., Inc.
IPC分类号： A61K31/195
CPC分类号： C07D213/81 , C07C255/57 , C07C311/08 , C07C2601/02 , C07D207/06 , C07D207/08 , C07D213/76 , C07D295/192 , C07D333/20 , C07D405/04
摘要： The present invention is directed to compounds 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.
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4.发明公开MACROCYCLIC AMINOPYRIDYL BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权阿尔茨海默氏病的治疗MACRO CYCLICAL AMINIOPYRIDYL-β分泌酶抑制剂
公开(公告)号：EP1817312A1
公开(公告)日：2007-08-15
申请号：EP05849049.1
申请日：2005-11-18
申请人： Merck & Co., Inc.
IPC分类号： C07D471/04 , C07D421/04 , C07D413/04 , C07D401/04 , A61K31/4353
CPC分类号： C07D491/08
摘要： The present invention is directed to macrocyclic aminopyridyl compounds represented by general formula (I), 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.
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5.发明公开2,3,4,6-SUBSTITUTED PYRIDYL DERIVATIVE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权2,3,4,6-取代的吡啶基衍生物化合物AS BETA-SEKTRETASE抑制剂用于治疗阿尔茨海默氏病的治疗
公开(公告)号：EP1817311A2
公开(公告)日：2007-08-15
申请号：EP05851916.6
申请日：2005-11-18
申请人： Merck & Co., Inc.
发明人： NANTERMET, Philippe, G. , STANTON, Matthew, G. , RAJAPAKSE, Hemaka, A. , SELNICK, Harold, G. , BARROW, James, C. , STAUFFER, Shaun, R. , VACCA, Joseph, P. , MOORE, Keith, P. , STACHEL, Shawn, J.
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is directed to 2,3,4,6-substituted pyridyl derivative compounds 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.
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公开(公告)号：EP1359913A1
公开(公告)日：2003-11-12
申请号：EP02723093.7
申请日：2002-02-05
申请人： Merck & Co., Inc.
IPC分类号： A61K31/4439 , A61K31/497 , C07D401/12 , C07D403/12
CPC分类号： C07D241/20 , A61K38/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/14 , C07K5/06078 , C07K5/06191
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein R2 is R3 is selected from the group consisting of 1) hydrogen, 2) halogen, 3) C 1-4 alkyl, 4) C 3-7 cycloalkyl, 5) CF3, 6) OCF3, 7) C 1-4 alkoxy, and 8) cyano; and R12 is a 5-membered heteroaryl ring having 2, 3, or 4 heteroatoms, provided that at least 1 heteroatom is N, and at most 1 of the heteroatoms is S, said ring being unsubstituted or substituted, at any one ring atom, with CH3.
摘要翻译： 本发明的化合物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物：或其药学上可接受的盐，其中R2是R3选自1）氢，2）卤素，3）C1-4 烷基，4）C 3-7环烷基，5）CF 3，6）OCF 3，7）C 1-4烷氧基和8）氰基; 且R 12为具有2,3或4个杂原子的5元杂芳基环，条件是至少1个杂原子为N且至多1个杂原子为S，所述环在任何一个环原子处未被取代或被取代， 与CH3。
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公开(公告)号：EP1124822A1
公开(公告)日：2001-08-22
申请号：EP99958684.5
申请日：1999-10-28
发明人： SANDERSON, Philip, E. , LYLE, Terry, A. , DORSEY, Bruce, D. , STANTON, Matthew, G. , STAAS, Donnette , COBURN, Craig , NAYLOR-OLSEN, Adel, M. , MORRISSETTE, Matthew, M. , SELNICK, Harold, G. , NANTERMET, Philippe, G. , WILLIAMS, Peter, D. , STAUFFER, Kenneth, J. , BURGEY, Christopher , ISAACS, Richard
IPC分类号： C07D403/12 , C07D401/12 , A61K31/437 , A61K31/4375 , A61K31/4995
CPC分类号： C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D413/14 , C07D471/04
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the structure (I) or a pharmaceutically acceptable salt thereof, wherein b is NY1 or O; c is CY2 or N; d is CY3 or N; e is CY4 or N; f is CY5 or N; g is CY6 or N; Y?4, Y5, and Y6¿ are independently hydrogen, C¿1-4? alkyl, or halogen; Y?1 and Y2¿ are independently hydrogen, C¿1-4? alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy, and Y?3¿ is hydrogen, C¿1-4? alkyl, C3-7 cycloalkyl, halogen, -CN, NH2, OH or C1-4 alkoxy; A is (II), (III), (IV), (V) or (VI); and W, W?1, R1, R3, R4, R5¿, X and Z are defined in the specification.
摘要翻译： 本发明化合物可用于抑制具有结构（I）的凝血酶和相关的血栓形成性闭塞物或其药学上可接受的盐，其中b是NY1或O; c是CY2或N; d是CY3或N; e是CY4或N; f是CY5或N; g是CY6或N; Y 4，Y 5和Y 6独立地是氢，C 1-4 - 烷基或卤素; Y 1和Y 2独立地是氢，C 1-4 - 烷基，C 3-7环烷基，卤素，NH 2，OH或C 1-4烷氧基，Y 3是氢，C 1-4 - 烷基，C 3-7环烷基，卤素，-CN，NH 2，OH或C 1-4烷氧基; A是（II），（III），（IV），（V）或（VI）; W，W 1，R 1，R 3，R 4，R 5'，X和Z在说明书中定义。
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8.发明公开1,3,5-SUBSTITUTED PHENYL DERIVATIVE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权用于治疗阿尔茨海默病SUITABLE 1,3,5-取代PHENYLDERIVATVERBINDUNGEN的治疗ALSβ-分泌酶抑制剂
公开(公告)号：EP1740559A1
公开(公告)日：2007-01-10
申请号：EP05738682.3
申请日：2005-04-15
申请人： Merck & Co., Inc.
发明人： BARROW, James, C. , MCGAUGHEY, Georgia, B. , NANTERMET, Philippe, G. , RAJAPAKSE, Hemaka, A. , SELNICK, Harold, G. , STAUFFER, Shaun, R. , COBURN, Craig, A.
IPC分类号： C07D271/10
CPC分类号： C07D271/10 , C07D249/06 , C07D249/08 , C07D263/32 , C07D263/62 , C07D271/06 , C07D285/12 , C07D307/14 , C07D307/42 , C07D307/44 , C07D307/52 , C07D307/54 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14
摘要： The present invention is directed to 1,3,5-phenyl substituted derivative compounds 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.
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9.发明公开BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER S DISEASE 有权苄基和苄ASβ-分泌阿尔茨海默氏病的治疗抑制剂
公开(公告)号：EP1689713A1
公开(公告)日：2006-08-16
申请号：EP04811618.0
申请日：2004-11-19
申请人： Merck & Co., Inc.
发明人： NANTERMET, Philippe, G. , RAJAPAKSE, Hemaka, A. , SELNICK, Harold, G. , STAUFFER, Shaun, R. , YOUNG, Mary Beth
IPC分类号： C07D213/02 , A61K31/44
CPC分类号： C07C255/46 , C07C311/08 , C07C2601/02 , C07C2601/08 , C07D207/06 , C07D213/76 , C07D295/192 , C07D401/06
摘要： The present invention is directed to benzylether and benzylamino derivative compounds 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.
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10.发明公开SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权SPIROPIPERIDININHIBITORENβ-分泌阿尔茨海默氏病的治疗
公开(公告)号：EP1910364A2
公开(公告)日：2008-04-16
申请号：EP06787495.8
申请日：2006-07-14
发明人： COBURN, Craig, A. , EGBERTSON, Melissa, S. , GRAHAM, Samuel, L. , MCGAUGHEY, Georgia, B. , STAUFFER, Shaun, R. , RAJAPAKSE, Hemaka, A. , NANTERMET, Philippe, G. , STACHEL, Shawn, R. , YANG, Wenjin , LU, Wanli , FAHR, Bruce
IPC分类号： C07D471/10 , A61K31/438 , A61P25/28
CPC分类号： C07D471/10
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.
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