公开(公告)号：EP1874295A1

公开(公告)日：2008-01-09

申请号：EP06750228.6

申请日：2006-04-14

申请人： Merck & Co., Inc. ,  Aton Pharma, Inc.

发明人： HUBBS, Jed, Lee ,  MAMPREIAN, Dawn, M. ,  METHOT, Joey, L. ,  MILLER, Thomas, A. ,  OTTE, Karin, M. ,  SILIPHAIVANH, Phieng ,  SLOMAN, David, L. ,  STANTON, Matthew, G. ,  WILSON, Kevin, J. ,  WITTER, David, J.

IPC分类号： A61K31/38 ,  C07D333/22

CPC分类号： C07D333/70 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14

摘要： The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

公开(公告)号：EP1991226A2

公开(公告)日：2008-11-19

申请号：EP07751483.4

申请日：2007-02-23

申请人： Merck & Co., Inc.

发明人： GRIMM, Jonathan, B. ,  HUBBS, Jed, L. ,  MILLER, Thomas ,  OTTE, Karin, M. ,  SILIPHAIVANH, Phieng ,  STANTON, Matthew, G. ,  WILSON, Kevin ,  WITTER, David ,  ZHOU, Hua

IPC分类号： A61K31/4439

CPC分类号： C07C237/42 ,  C07D333/20

摘要： The present invention relates to a novel class of compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

公开(公告)号：EP1079835A1

公开(公告)日：2001-03-07

申请号：EP99923087.3

申请日：1999-05-14

申请人： MERCK & CO., INC.

发明人： SANDERSON, Philip, E. ,  STANTON, Matthew, G. ,  BALANI, Suresh, K.

IPC分类号： A61K31/535

CPC分类号： C07D401/12 ,  C07D241/20

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having structure (A), wherein (B).

公开(公告)号：EP2320737A1

公开(公告)日：2011-05-18

申请号：EP09805356.4

申请日：2009-07-27

申请人： Merck & Co., Inc.

发明人： KATZ, Jason ,  KNOWLES, Sandra, L. ,  JEWELL, James, P. ,  SLOMAN, David, L. ,  STANTON, Matthew, G. ,  NOUCTI, Njamkou

IPC分类号： A01N43/78 ,  A61K31/425

CPC分类号： A61K31/425 ,  C07D417/04 ,  C07D417/14

摘要： The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.

公开(公告)号：EP1954698B1

公开(公告)日：2009-06-24

申请号：EP06837965.0

申请日：2006-11-17

申请人： Merck & Co., Inc.

发明人： BERK, Scott, C. ,  CLOSE, Joshua ,  HAMBLETT, Christopher ,  HEIDEBRECHT, Richard, W. ,  KATTAR, Solomon, D. ,  KLIMAN, Laura, T. ,  MAMPREIAN, Dawn, M. ,  METHOT, Joey, L. ,  MILLER, Thomas ,  SLOMAN, David, L. ,  STANTON, Matthew, G. ,  TEMPEST, Paul ,  ZABIEREK, Anna, A.

IPC分类号： C07D471/10 ,  C07D487/10 ,  C07D491/10 ,  C07D498/10 ,  A61K31/438 ,  A61K31/407 ,  A61K31/424 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D471/10 ,  C07D487/10 ,  C07D491/10 ,  C07D491/107 ,  C07D498/10

公开(公告)号：EP2063710A2

公开(公告)日：2009-06-03

申请号：EP07837578.9

申请日：2007-08-31

申请人： Merck & Co., Inc.

发明人： STANTON, Matthew, G. ,  MUNOZ, Benito ,  SLOMAN, David, L. ,  HUBBS, Jed ,  HAMBLETT, Christopher

IPC分类号： A01N43/40 ,  A61K31/435 ,  C07D211/34

CPC分类号： C07D211/38

摘要： Compounds of formula (I). Selectively inhibit production of Aβ(1-42) and hence find use in treatment of diseases associated with deposition of β-amyloid in the brain.

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.

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

申请人： Merck & Co., Inc. ,  Barrow, James C.

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。

公开(公告)号：EP1976511A2

公开(公告)日：2008-10-08

申请号：EP07762514.3

申请日：2007-01-09

申请人： Merck & Co., Inc.

发明人： MILLER, Thomas, A. ,  SLOMAN, David, L. ,  STANTON, Matthew, G. ,  WILSON, Kevin, J. ,  WITTER, David, J.

IPC分类号： A61K31/38

CPC分类号： C07D231/40 ,  C07D333/20 ,  C07D333/70 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

摘要： The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

公开(公告)号：EP1697308A2

公开(公告)日：2006-09-06

申请号：EP04814367.1

申请日：2004-12-15

申请人： Merck & Co., Inc.

发明人： BARROW, James, C. ,  COBURN, Craig, A. ,  NANTERMET, Philippe, G. ,  SELNICK, Harold, G. ,  STACHEL, Shawn, J. ,  STANTON, Matthew, G. ,  STAUFFER, Shaun, R. ,  ZHUANG, Linghang ,  DAVIS, Jennifer, R.

IPC分类号： C07C237/00 ,  C07D213/02 ,  A61K31/18 ,  A61K31/44

CPC分类号： C07D213/81 ,  C07D213/75 ,  C07D257/04 ,  C07D401/04 ,  C07D409/12 ,  C07D413/12

摘要： The present invention is directed to phenylamide and pyridylamide 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.