公开(公告)号：EP1017382B1

公开(公告)日：2006-03-01

申请号：EP98924988.3

申请日：1998-05-29

申请人： Merck & Co., Inc. (a New Jersey corp.)

发明人： DURETTE, Philippe, L. ,  HAGMANN, William, K. ,  MacCOSS, Malcolm ,  MILLS, Sander, G. ,  MUMFORD, Richard, A.

IPC分类号： C07K14/705 ,  A61K31/42 ,  A61K31/415 ,  A61K31/425 ,  A61K31/505 ,  C07C255/03 ,  C07D207/08 ,  C07D217/18 ,  C07D231/04 ,  C07D263/04 ,  C07D277/04 ,  C07K5/06

CPC分类号： C07K5/06165 ,  A61K38/00 ,  C07K5/06139 ,  C07K5/06191

摘要： Compounds of formula (I) are antagonists of VLA-4 and/or alpha 4 beta 7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

公开(公告)号：EP1725542A1

公开(公告)日：2006-11-29

申请号：EP05729422.5

申请日：2005-03-07

申请人： Merck & Co., Inc.

发明人： HAGMANN, William, K. ,  LIN, Linus, S. ,  LIU, Ping ,  MUMFORD, Richard, A. ,  REGER, Thomas, S. ,  SMITH, Nicholas, D. ,  STOCK, Nicholas, S. ,  ZUNIC, Jasmine

IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/44

CPC分类号： C07K5/06026 ,  C07D401/12 ,  C07D401/14

摘要： Compounds of Formula I are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn’s disease, multiple sclerosis, asthma, and rheumatoid arthritis.

公开(公告)号：EP1017382A1

公开(公告)日：2000-07-12

申请号：EP98924988.3

申请日：1998-05-29

申请人： Merck & Co., Inc. (a New Jersey corp.)

发明人： DURETTE, Philippe, L. ,  HAGMANN, William, K. ,  MacCOSS, Malcolm ,  MILLS, Sander, G. ,  MUMFORD, Richard, A.

IPC分类号： A61K31/42 ,  A61K31/415 ,  A61K31/425 ,  A61K31/505 ,  C07C255/03 ,  C07D207/08 ,  C07D217/18 ,  C07D231/04 ,  C07D263/04 ,  C07D277/04 ,  C07D285/12 ,  C07D295/023 ,  C07D413/10 ,  C07D417/10

CPC分类号： C07K5/06165 ,  A61K38/00 ,  C07K5/06139 ,  C07K5/06191

摘要： Compounds of formula (I) are antagonists of VLA-4 and/or α4β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

摘要翻译： 式（I）化合物是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理。 这些化合物可以配制成药物组合物并适用于治疗哮喘，变态反应，炎症，多发性硬化和其他炎症和自身免疫性疾病。

公开(公告)号：EP0831714A1

公开(公告)日：1998-04-01

申请号：EP96917942.0

申请日：1996-06-03

申请人： MERCK & CO., INC.

发明人： CALAYCAY, Jimmy, R. ,  MUMFORD, Richard, A. ,  SCHMIDT, Jack, A. ,  WEIDNER, Jeffrey, R.

IPC分类号： C07K16 ,  C12P21

CPC分类号： C07K16/40

摘要： Monospecific antibodies are produced which are specific for the carboxyl-terminal region of human inducible nitric oxide synthase (hiNOS). These monospecific antibodies are used in an assay systems to detect hiNOS. Elevations of hiNOS occur in hepatitis and inflammatory bowel disease, as well as numerous inflammatory diseases. The monospecific antibodies and the assay systems are used to quantitate hiNOS as a readout of hiNOS activity and to evaluate potential hiNOS modulators.

公开(公告)号：EP1034164B1

公开(公告)日：2004-05-19

申请号：EP98959547.5

申请日：1998-11-24

申请人： MERCK & CO., INC.

发明人： DURETTE, Philippe, L. ,  HAGMANN, William, K. ,  KOPKA, Ihor, E. ,  MACCOSS, Malcolm ,  MILLS, Sander, G. ,  MUMFORD, Richard, A. ,  MAGRIOTIS, Plato, A.

IPC分类号： C07D207/16 ,  C07D207/48 ,  C07D211/34 ,  C07D211/96 ,  C07D217/26 ,  C07D241/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  A61K31/40 ,  A61K31/47 ,  A61K31/495

CPC分类号： C07D401/12 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

摘要： β-Alanine derivatives of formula (I) are antagonists of VLA-4 and/or α4β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

公开(公告)号：EP1001764A1

公开(公告)日：2000-05-24

申请号：EP98926122.7

申请日：1998-05-29

申请人： Merck & Co., Inc. (a New Jersey corp.)

发明人： DURETTE, Philippe, L. ,  HAGMANN, William, K. ,  MacCOSS, Malcolm ,  MILLS, Sander, G. ,  MUMFORD, Richard, A. ,  VAN RIPER, Gail, M. ,  SCHMIDT, Jack, A. ,  KEVIN, Nancy, J.

IPC分类号： A61K31/395 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61K31/425 ,  A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  C07D205/02 ,  C07D209/04 ,  C07D209/14 ,  C07D209/30 ,  C07D217/12 ,  C07D235/02 ,  C07D233/64 ,  C07D241/02 ,  C07D257/04 ,  C07D265/30 ,  C07D275/02 ,  C07D277/02 ,  C07D277/08 ,  C07D295/08

CPC分类号： A61K31/472 ,  A61K31/401 ,  A61K31/445 ,  A61K31/4725 ,  A61K38/00 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191

摘要： Compounds of formula (I) are antagonists of VLA-4 and/or α4β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

摘要翻译： 式（I）化合物是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理。 这些化合物可以配制成药物组合物并适用于治疗哮喘，变态反应，炎症，多发性硬化和其他炎症和自身免疫性疾病。

公开(公告)号：EP0835448A1

公开(公告)日：1998-04-15

申请号：EP96919038.0

申请日：1996-06-03

申请人： MERCK & CO., INC.

发明人： CALAYCAY, Jimmy, R. ,  HUMES, John, L. ,  MUMFORD, Richard, A. ,  SINGER, Irwin, I. ,  WEIDNER, Jeffrey, R.

IPC分类号： C07K16 ,  C12N9

CPC分类号： C12N9/0075 ,  C07K16/40

摘要： Monospecific antibodies are produced which are specific for the carboxyl-terminal region of human inducible nitric oxide synthase (hiNOS). These monospecific antibodies are used in an assay system to detect hiNOS. Elevations of hiNOS occur in hepatitis and inflammatory bowel disease, as well as numerous inflammatory diseases. The monospecific antibodies and the assay systems are used to quantitate hiNOS as a readout of hiNOS activity and to evaluate potential hiNOS modulators.

公开(公告)号：EP1389200A1

公开(公告)日：2004-02-18

申请号：EP02725194.1

申请日：2002-03-15

申请人： Merck & Co., Inc.

发明人： DOHERTY, George ,  LIN, Linus, S. ,  HAGMANN, William, K. ,  KAMENECKA, Theodore, M. ,  YANG, Ginger Xu-Qiang ,  CHANG, Linda, L. ,  SHAH, Shrenik, K. ,  MUMFORD, Richard, A.

IPC分类号： C07D401/02 ,  A61K31/44

CPC分类号： C07D401/12 ,  C07D401/14

摘要： Compounds of formula (I) are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

公开(公告)号：EP1034164A1

公开(公告)日：2000-09-13

申请号：EP98959547.5

申请日：1998-11-24

申请人： MERCK & CO., INC.

发明人： DURETTE, Philippe, L. ,  HAGMANN, William, K. ,  KOPKA, Ihor, E. ,  MACCOSS, Malcolm ,  MILLS, Sander, G. ,  MUMFORD, Richard, A. ,  MAGRIOTIS, Plato, A.

IPC分类号： C07D207/16 ,  C07D207/48 ,  C07D211/34 ,  C07D211/96 ,  C07D217/26 ,  C07D241/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  A61K31/40 ,  A61K31/42 ,  A61K31/44 ,  A61K31/47 ,  A61K31/445 ,  A61K31/495

CPC分类号： C07D401/12 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

摘要： β-Alanine derivatives of formula (I) are antagonists of VLA-4 and/or α4β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

公开(公告)号：EP0998282A1

公开(公告)日：2000-05-10

申请号：EP98924989.1

申请日：1998-05-29

申请人： Merck & Co., Inc. (a New Jersey corp.)

发明人： DURETTE, Philippe, L. ,  HAGMANN, William, K. ,  MacCOSS, Malcolm ,  MILLS, Sander, G. ,  MUMFORD, Richard, A.

IPC分类号： A61K31/42 ,  A61K31/415 ,  A61K31/425 ,  A61K31/505 ,  C07C255/03 ,  C07D207/08 ,  C07D217/18 ,  C07D231/04 ,  C07D263/04 ,  C07D277/04 ,  C07D285/12 ,  C07D295/023 ,  C07D413/10 ,  C07D417/10

CPC分类号： C07K5/06191 ,  A61K38/05 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/06078 ,  C07K5/06113 ,  C07K5/06139

摘要： Compounds of formula (I) are antagonists of VLA-4 and/or α4-β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

摘要翻译： 式（I）化合物是VLA-4和/或α4-β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理。 这些化合物可以配制成药物组合物并适用于治疗哮喘，变态反应，炎症，多发性硬化和其他炎症和自身免疫性疾病。