公开(公告)号：EP1507533B1

公开(公告)日：2010-04-14

申请号：EP03736768.7

申请日：2003-05-27

申请人： ELAN PHARMACEUTICALS, INC.

发明人： KONRADI, Andrei W. ,  SEMKO, Christopher M. ,  XU, Ying-zi ,  STAPPENBECK, Frank ,  STUPI, Brian P. ,  SMITH, Jenifer ,  THORSETT, Eugene, D. ,  PLEISS, Michael, A.

IPC分类号： C07D239/50 ,  A61K31/505

CPC分类号： C07D239/50

摘要： Disclosed are compounds which bind 4 integrins, where the 4integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by 4integrins, where the 4 integrin is preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

公开(公告)号：EP1507533A2

公开(公告)日：2005-02-23

申请号：EP03736768.7

申请日：2003-05-27

申请人： Elan Pharmaceuticals, Inc.

发明人： KONRADI, Andrei W. ,  SEMKO, Christopher M. ,  XU, Ying-zi ,  STAPPENBECK, Frank ,  STUPI, Brian P. ,  SMITH, Jenifer ,  THORSETT, Eugene, D. ,  PLEISS, Michael, A.

IPC分类号： A61K31/505

CPC分类号： C07D239/50

摘要： Disclosed are compounds which bind 4 integrins, where the 4integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by 4integrins, where the 4 integrin is preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

公开(公告)号：EP1940827B1

公开(公告)日：2011-03-16

申请号：EP06804266.2

申请日：2006-09-28

申请人： Elan Pharmaceuticals Inc. ,  Wyeth LLC

发明人： SEMKO, Christopher, Michael ,  XU, Ying-zi ,  STAPPENBECK, Frank ,  SMITH, Jenifer Lea ,  ROSSITER, Kassandra Inez ,  FUKUDA, Juri Y. ,  KONRADI, Andrei W.

IPC分类号： C07D405/12 ,  C07D409/12 ,  C07D401/14 ,  C07D417/12 ,  C07D239/50 ,  C07D401/12 ,  A61K31/506 ,  A61P29/00

CPC分类号： C07D417/12 ,  C07D239/50 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14

摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis (Formula I).

公开(公告)号：EP1507775A1

公开(公告)日：2005-02-23

申请号：EP03731419.2

申请日：2003-05-27

申请人： Elan Pharmaceuticals, Inc.

发明人： KONRADI, Andrei, W. ,  SEMKO, Christopher, M. ,  XU, Ying-zi ,  STAPPENBECK, Frank ,  STUPI, Brian, P. ,  SMITH, Jenifer ,  THORSETT, Eugene, D. ,  PLEISS, Michael, A.

IPC分类号： C07D401/10 ,  A61P19/02 ,  A61P29/00

CPC分类号： C07D401/12 ,  C07D239/50 ,  C07D403/12

摘要： Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

公开(公告)号：EP1940827A1

公开(公告)日：2008-07-09

申请号：EP06804266.2

申请日：2006-09-28

申请人： Elan Pharmaceuticals Inc. ,  Wyeth

发明人： SEMKO, Christopher, Michael ,  XU, Ying-zi ,  STAPPENBECK, Frank ,  SMITH, Jenifer Lea ,  ROSSITER, Kassandra Inez ,  FUKUDA, Juri Y. ,  KONRADI, Andrei W.

IPC分类号： C07D405/12 ,  C07D409/12 ,  C07D401/14 ,  C07D417/12 ,  C07D239/50 ,  C07D401/12 ,  A61K31/506 ,  A61P29/00

CPC分类号： C07D417/12 ,  C07D239/50 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14

摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis (Formula I).

公开(公告)号：EP1916985A2

公开(公告)日：2008-05-07

申请号：EP06813596.1

申请日：2006-08-18

申请人： Elan Pharmaceuticals Inc.

发明人： BOWERS, Simeon ,  GAROFALO, Albert, W. ,  HOM, Roy, K. ,  KONRADI, Andrei, W. ,  MATTSON, Matthew, N. ,  NEITZEL, Martin, L. ,  SEMKO, Christopher, M. ,  TRUONG, Anh, P. ,  WU, Jing ,  XU, Ying-zi

IPC分类号： A61K8/00

CPC分类号： C07D451/14 ,  C07D471/08 ,  C07D471/18 ,  C07D471/22 ,  C07D498/08

摘要： The invention provides N-cyclic sulfonamido compounds and salts of Formula (I): wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula (I) are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula (I).

公开(公告)号：EP1572678A2

公开(公告)日：2005-09-14

申请号：EP03800037.8

申请日：2003-12-18

申请人： ELAN PHARMACEUTICALS, INC.

发明人： GRANT, Francine, S. ,  DAPPEN, Michael, S. ,  XU, Ying-zi ,  BARTULIS, Sarah ,  HOLCOMB, Ryan, C. ,  KASAR, Ramesh, A. ,  PLEISS, Michael, A. ,  THORSETT, Eugene, D. ,  YE, Michael ,  KONRADI, Andrei, W.

IPC分类号： C07D401/06

CPC分类号： C07D213/40 ,  C07C311/21 ,  C07D207/337 ,  C07D211/26 ,  C07D211/34 ,  C07D213/56 ,  C07D213/74 ,  C07D239/26 ,  C07D243/24 ,  C07D295/13 ,  C07D295/185 ,  C07D401/04 ,  C07D471/04

摘要： Disclosed are certain substituted N-phenylsulfonamide derivatives and related compounds. These compounds are useful as bradykinin antagonists to relieve adverse symptoms in mammals mediated, at least in part, by bradykinin including pain, inflammation, bronchoconstriction, cerebral edema, etc.

摘要翻译： 公开了某些取代的N-苯基磺酰胺衍生物和相关化合物。 这些化合物可用作缓激肽拮抗剂以缓解哺乳动物中的至少部分由缓激肽介导的不良症状，包括疼痛，炎症，支气管收缩，脑水肿等。

公开(公告)号：EP1881982B1

公开(公告)日：2013-11-20

申请号：EP06770821.4

申请日：2006-05-22

申请人： Elan Pharmaceuticals Inc.

发明人： STAPPENBECK, Frank ,  KONRADI, Andrei ,  JAGODZINSKI, Jacek ,  SEMKO, Christopher, M. ,  XU, Ying-zi ,  SMITH, Jenifer, L. ,  ROSSITER, Kassandra

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/506 ,  A61P29/00

CPC分类号： C07D471/04

摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein the variables A, n, R5, R21-R24 and Q are defined herein. These compounds bind VLA-4. Certain of these compound also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

公开(公告)号：EP1940826B1

公开(公告)日：2010-12-29

申请号：EP06804253.0

申请日：2006-09-28

申请人： Elan Pharmaceuticals Inc. ,  Wyeth LLC

发明人： SEMKO, Christopher, Michael ,  XU, Ying-zi ,  STAPPENBECK, Frank ,  SMITH, Jenifer, Lea ,  ROSSITER, Kassandra, Inez ,  FUKUDA, Juri, Y. ,  KONRADI, Andrei, W.

IPC分类号： C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D239/50 ,  C07D401/12 ,  A61K31/506 ,  A61P29/00

CPC分类号： C07D403/02 ,  C07D239/50 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis (Formula I).

公开(公告)号：EP1507775B1

公开(公告)日：2008-12-31

申请号：EP03731419.2

申请日：2003-05-27

申请人： ELAN PHARMACEUTICALS, INC.

发明人： KONRADI, Andrei, W. ,  SEMKO, Christopher, M. ,  XU, Ying-zi ,  STAPPENBECK, Frank ,  STUPI, Brian, P. ,  SMITH, Jenifer ,  THORSETT, Eugene, D. ,  PLEISS, Michael, A.

IPC分类号： C07D401/10 ,  A61P19/02 ,  A61P29/00 ,  A61K31/505 ,  C07D239/69

CPC分类号： C07D401/12 ,  C07D239/50 ,  C07D403/12

摘要： Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.