公开(公告)号：EP1144435A2

公开(公告)日：2001-10-17

申请号：EP00904486.8

申请日：2000-01-21

申请人： Elan Pharmaceuticals, Inc. ,  AMERICAN HOME PRODUCTS CORPORATION

发明人： DRESSEN, Darren, B. ,  KREFT, Anthony ,  KUBRAK, Dennis ,  MANN, Charles, William ,  PLEISS, Michael, A. ,  STACK, Gary, Paul ,  THORSETT, Eugene, D.

IPC分类号： C07K5/00

CPC分类号： C07K5/06173 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191

摘要： Disclosed are pyroglutamic acid derivatives and related 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.

公开(公告)号：EP0861248A1

公开(公告)日：1998-09-02

申请号：EP96937782.0

申请日：1996-10-29

申请人： AMERICAN HOME PRODUCTS CORPORATION

发明人： KANG, Young, Hee ,  STACK, Gary, Paul

IPC分类号： A61K ,  C07D ,  A61K31 ,  A61P25 ,  C07D405 ,  C07D493

CPC分类号： C07D493/04 ,  C07D405/12

摘要： The compounds of formula (I), wherein R?1, R4 and R5¿ are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido; or, R1 is defined as above and R?4 and R5¿, taken together, are ortho substituted methylenedioxy, ethylenedioxy, or propylenedioxy; R?2 and R3¿ are, independently, hydrogen or alkyl; n is 3 or 4; or pharmaceutically acceptable salts thereof, are useful in the treatment of depression and related disorders.

摘要翻译： 其中R 1，R 4和R 5'独立地为氢，烷基，烷氧基，芳烷氧基，烷酰氧基，羟基，卤素，三氟甲基，氨基，单烷基氨基或二烷基氨基，烷酰氨基或烷基磺酰氨基 ; 或者R1如上所定义，并且R4和R5一起为邻位取代的亚甲二氧基，亚乙二氧基或亚丙基二氧基; R 2和R 3独立地是氢或烷基; n是3或4; 或其药学上可接受的盐可用于治疗抑郁症和相关病症。

公开(公告)号：EP0861248B1

公开(公告)日：2001-12-12

申请号：EP96937782.9

申请日：1996-10-29

申请人： AMERICAN HOME PRODUCTS CORPORATION

发明人： KANG, Young, Hee ,  STACK, Gary, Paul

IPC分类号： C07D405/12 ,  A61K31/40 ,  C07D493/04

CPC分类号： C07D493/04 ,  C07D405/12

摘要： The compounds of formula (I), wherein R?1, R4 and R5¿ are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido; or, R1 is defined as above and R?4 and R5¿, taken together, are ortho substituted methylenedioxy, ethylenedioxy, or propylenedioxy; R?2 and R3¿ are, independently, hydrogen or alkyl; n is 3 or 4; or pharmaceutically acceptable salts thereof, are useful in the treatment of depression and related disorders.

公开(公告)号：EP0932609A1

公开(公告)日：1999-08-04

申请号：EP97910866.0

申请日：1997-10-10

申请人： AMERICAN HOME PRODUCTS CORPORATION

发明人： STACK, Gary, Paul

IPC分类号： A61K31 ,  A61P25 ,  A61P43 ,  C07D491 ,  C07D519

CPC分类号： C07D491/04

摘要： The compounds of formula (I) wherein X is H2 or O; R1 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; Z is defined by formula (II), (III) or (IV) wherein R2 is hydrogen, alkyl, cycloalkyl, phenyl optionally substituted with R1 as defined above, φ-phenylalkyl or φ-diphenylalkyl, in which the phenyl ring is optionally substituted with R1 as defined above, or R2 is naphthyl, indolyl, indazolyl, thienyl, pyridinyl, pyrimidinyl, quinolinyl, benzoisothiazolyl or benzisoxazolyl, each optionally substituted with R1 as defined above; R3 is hydrogen and R4 is hydrogen, 1-benzimidazolyl-2-one, indolyl, benzoisothiazolyl or benzisoxazolyl, each optionally substituted with R1 as defined above, or R4 is -Y-Ar, in which Y is C=O, CHOH, or (CH¿2?)m, wherein m is 0 to 4, and Ar is phenyl, optionally substituted with R?1¿ as defined above; or R?3 and R4¿, taken together with the carbon atom to which they are attached form (V) or (VI) in which R5 is hydrogen and R6 is phenyl, naphthyl, thienyl, indolyl, benzoisothiazolyl or benzisoxazolyl, each optionally substituted with R1 as defined above; or R?5 and R6¿, taken together with the carbon atoms to which they are attached complete a benzene ring optionally substituted with R1; or a pharmaceutically acceptable salt thereof; are useful for the treatment of brain dopamine dysregulation.

公开(公告)号：EP0658160A1

公开(公告)日：1995-06-21

申请号：EP93920245.0

申请日：1993-08-20

申请人： AMERICAN HOME PRODUCTS CORPORATION

发明人： STACK, Gary, Paul ,  ABOU-GHARBIA, Magid, Abdel-Megid

IPC分类号： A61K31 ,  A61P25 ,  A61P39 ,  C07D405 ,  C07D493

CPC分类号： C07D405/12 ,  C07D493/04

摘要： A compound of formula (1), wherein R?1 and R2¿ are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido or sulfonamido, or R?1 and R2¿ together are methylenedioxy, ethylenedioxy or propylenedioxy; R3 is hydrogen or alkyl; n is one of the integers 2, 3 or 4; or a pharmaceutically acceptable salt thereof, are antipsychotic agents.

公开(公告)号：EP1144435B1

公开(公告)日：2006-04-12

申请号：EP00904486.8

申请日：2000-01-21

申请人： ELAN PHARMACEUTICALS, INC. ,  Wyeth

发明人： DRESSEN, Darren, B. ,  KREFT, Anthony ,  KUBRAK, Dennis ,  MANN, Charles, William ,  PLEISS, Michael, A. ,  STACK, Gary, Paul ,  THORSETT, Eugene, D.

IPC分类号： C07K5/00

CPC分类号： C07K5/06173 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191

摘要： Disclosed are pyroglutamic acid derivatives and related 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.