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1.发明公开SUBSTITUTED PHENYLALANINE TYPE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 失效取代的苯丙氨酸衍生物，血液白细胞抑制其VLA-4介导的粘附
公开(公告)号：EP1001972A1
公开(公告)日：2000-05-24
申请号：EP98937990.4
申请日：1998-07-30
发明人： THORSETT, Eugene, D. , SEMKO, Christopher, M. , SARANTAKIS, Dimitrios , PLEISS, Michael, A. , LOMBARDO, Louis, John , KREFT, Anthony , KONRADI, Andrei, W. , GRANT, Francine, S. , DRESSEN, Darren, B. , DAPPEN, Michael, S. , BAUDY, Reinhardt, Bernhard , ASHWELL, Susan
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06165
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 are also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
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2.发明公开
公开(公告)号：EP0994895A1
公开(公告)日：2000-04-26
申请号：EP98937991.2
申请日：1998-07-30
发明人： THORSETT, Eugene, D. , SEMKO, Christopher, M. , PLEISS, Michael, A. , KONRADI, Andrei, W. , GRANT, Francine, S. , DRESSEN, Darren, B. , BAUDY, Reinhardt, Bernhard
CPC分类号： C07K5/06026 , A61K38/00 , C07K5/06078 , C07K5/06165
摘要： Diclosed 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 arthristis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
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3.发明公开4-AMINO-PHENYLALANINE TYPE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 失效WITH A 4-氨基苯丙氨酸LINKS，血液白细胞抑制其VLA-4介导的粘附
公开(公告)号：EP1001974A1
公开(公告)日：2000-05-24
申请号：EP98937049.9
申请日：1998-07-30
发明人： ASHWELL, Susan , GRANT, Francine, S. , KONRADI, Andrei, W. , KREFT, Anthony , LOMBARDO, Louis, John , PLEISS, Michael, A. , SARANTAKIS, Dimitrios , SEMKO, Christopher, M. , THORSETT, Eugene, D.
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06165
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.
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4.发明公开CARBAMYLOXY COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 失效氨基甲酰氧基化合物，用来抑制VLA-4介导的白细胞
公开(公告)号：EP1000051A1
公开(公告)日：2000-05-17
申请号：EP98937052.3
申请日：1998-07-31
发明人： THORSETT, Eugene, D. , SEMKO, Christopher, M. , SARANTAKIS, Dimitrios , PLEISS, Michael, A. , KREFT, Anthony , KONRADI, Andrei, W. , GRANT, Francine, S. , DRESSEN, Darren, B. , ASHWELL, Susan , BAUDY, Reinhardt, Bernhard , LOMBARDO, Louis, John
IPC分类号： C07D311/18 , C07D207/48 , C07D277/56 , C07D279/12 , C07D277/06 , C07D403/12 , A61K31/18 , A61K31/415 , A61K31/425 , A61K31/54 , A61K31/495
CPC分类号： C07K5/06026 , A61K38/00 , C07K5/0215 , C07K5/06139 , C07K5/06165
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.
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5.发明公开BENZYL COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 失效苄THAT INHIBIT血液白细胞的VLA-4-介导的粘附
公开(公告)号：EP1001975A1
公开(公告)日：2000-05-24
申请号：EP98937054.9
申请日：1998-07-31
发明人： THORSETT, Eugene, D. , SEMKO, Christopher, M. , PLEISS, Michael, A. , LOMBARDO, Louis, John , KONRADI, Andrei, W. , GRANT, Francine, S. , DRESSEN, Darren, B. , DAPPEN, Michael, S.
IPC分类号： C07K5/078 , C07D207/16 , A61K38/05 , A61K31/40
CPC分类号： C07K5/06165 , C07K5/06139
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, wherein the disease may be, for example, asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The coumpounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
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6.发明公开DIPEPTIDE AND RELATED COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 失效二肽和相关化合物，血液白细胞抑制其VLA-4介导的粘附
公开(公告)号：EP1001971A1
公开(公告)日：2000-05-24
申请号：EP98937053.1
申请日：1998-07-31
发明人： THORSETT, Eugene, D. , SEMKO, Christopher, M. , PLEISS, Michael, A. , LOMBARDO, Louis, John , GRANT, Francine, S. , DRESSEN, Darren, B. , DAPPEN, Michael, S.
CPC分类号： C07K5/06026 , A61K38/00 , C07K5/06104 , C07K5/06139 , C07K5/06165
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 brains diseases such as multiple sclerosis.
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7.发明公开SULFONYLATED DIPEPTIDE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 失效磺酰化的二肽血液白细胞抑制其VLA-4介导的粘附
公开(公告)号：EP0994896A1
公开(公告)日：2000-04-26
申请号：EP98939871.4
申请日：1998-07-31
发明人： THORSETT, Eugene, D. , SEMKO, Christopher, M. , PLEISS, Michael, A. , KREFT, Anthony , KONRADI, Andrei, W. , GRANT, Francine, S. , BAUDY, Reinhardt, Bernhard , SARANTAKIS, Dimitrios
CPC分类号： C07K5/06165 , A61K38/00 , C07K5/06139 , C07K5/06191
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.
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8.发明公开MULTIVALENT VLA-4 ANTAGONISTS COMPRISING POLYETHYLENE GLYCOL MOIETIES 审中-公开用聚乙二醇 - 共享的多方VALENTE VLA-4拮抗剂
公开(公告)号：EP1765412A2
公开(公告)日：2007-03-28
申请号：EP05770402.5
申请日：2005-07-08
发明人： KONRADI, Andrei, W. , PLEISS, Michael, A. , SEMKO, Christopher, M. , YEDNOCK, Theodore , SMITH, Jenifer, L.
IPC分类号： A61K47/48
CPC分类号： A61K45/06 , A61K31/785 , A61K47/60 , A61Q5/00
摘要： Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates 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 conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
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9.发明公开
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
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).
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10.发明授权CARBAMYLOXY COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 失效氨基甲酰氧基化合物，用来抑制VLA-4介导的白细胞
公开(公告)号：EP1000051B1
公开(公告)日：2004-05-19
申请号：EP98937052.3
申请日：1998-07-31
申请人： Elan Pharmaceuticals, Inc. , Wyeth
发明人： THORSETT, Eugene, D. , SEMKO, Christopher, M. , SARANTAKIS, Dimitrios , PLEISS, Michael, A. , KREFT, Anthony , KONRADI, Andrei, W. , GRANT, Francine, S. , DRESSEN, Darren, B. , ASHWELL, Susan , BAUDY, Reinhardt, Bernhard , LOMBARDO, Louis, John
IPC分类号： C07D311/18 , C07D207/48 , C07D277/56 , C07D279/12 , C07D277/06 , C07D403/12 , A61K31/18 , A61K31/415 , A61K31/425 , A61K31/54 , A61K31/495
CPC分类号： C07K5/06026 , A61K38/00 , C07K5/0215 , C07K5/06139 , C07K5/06165
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.
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