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：EP1033983A1

公开(公告)日：2000-09-13

申请号：EP98961767.5

申请日：1998-11-23

申请人： MERCK & CO., INC.

发明人： CHANG, Linda ,  HAGMANN, William, K. ,  MACCOSS, Malcolm

IPC分类号： A61K31/165 ,  A61K31/40 ,  A61K31/41 ,  A61K31/44 ,  A61K31/425 ,  A61K31/445 ,  A61K47/12

CPC分类号： C07D493/08 ,  C07C311/19 ,  C07C311/20 ,  C07C2601/14 ,  C07D207/16

摘要： Cyclic amino acid 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.

摘要翻译： 式I的环状氨基酸衍生物是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学。 这些化合物可以配制成药物组合物，并且适用于治疗哮喘，过敏，炎症，多发性硬化和其它炎性和自身免疫性疾病。

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。

公开(公告)号：EP0724592B1

公开(公告)日：1999-01-07

申请号：EP94931961.0

申请日：1994-10-21

申请人： Merck & Co., Inc.

发明人： DURETTE, Philippe, L. ,  HAGMANN, William, K. ,  LANZA, Thomas, J., Jr. ,  SAHOO, Soumya, P. ,  RASMUSSON, Gary, H. ,  TOLMAN, Richard, L. ,  VON LANGEN, Derek

IPC分类号： C07J73/00 ,  A61K31/58

CPC分类号： C07J73/005

摘要： Compounds of formula (I) are inhibitors of the 5 alpha -reductase 1 isozyme, and are useful alone, or in combination with a 5 alpha -reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

公开(公告)号：EP0666846A1

公开(公告)日：1995-08-16

申请号：EP94901205.0

申请日：1993-10-26

申请人： MERCK & CO. INC.

发明人： DOHERTY, James, B. ,  DORN, Conrad, P. ,  DURETTE, Philippe, L. ,  FINKE, Paul, E. ,  MacCOSS, Malcolm ,  MILLS, Sander, G. ,  SHAH, Shrenik, K. ,  SAHOO, Soumya, P. ,  POLO, Scott, A. ,  HAGMANN, William, K.

IPC分类号： A61K31 ,  A61P29 ,  C07D205 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D413 ,  C07D417

CPC分类号： C07D401/12 ,  C07D205/08 ,  C07D403/12 ,  C07D405/12

摘要： New substituted azetidinones of general formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.

公开(公告)号：EP1682494A1

公开(公告)日：2006-07-26

申请号：EP04796666.8

申请日：2004-10-27

申请人： Merck & Co., Inc.

发明人： SHAH, Shrenik, K. ,  TRUONG, Quang, T. ,  QI, Hongbo ,  HAGMANN, William, K.

IPC分类号： C07C255/59

CPC分类号： C07D213/74 ,  C07C255/58 ,  C07C317/28 ,  C07C317/48 ,  C07C323/63 ,  C07C2601/04 ,  C07C2601/14 ,  C07D207/32 ,  C07D207/325 ,  C07D213/38 ,  C07D213/57 ,  C07D213/61 ,  C07D213/64 ,  C07D231/12 ,  C07D231/38 ,  C07D239/26 ,  C07D249/06 ,  C07D249/08 ,  C07D249/14

摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson’s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, including alcohol and nicotine addiction, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

摘要翻译： 结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，并且可用于治疗，预防和抑制由CB1受体介导的疾病。 本发明化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化症和格林 - 巴利综合征的神经炎症和病毒性脑炎的炎性后遗症，脑血管障碍 事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。 这些化合物还可用于治疗药物滥用障碍，包括酒精和尼古丁成瘾，治疗肥胖症或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

公开(公告)号：EP1546115A2

公开(公告)日：2005-06-29

申请号：EP03759514.7

申请日：2003-09-23

申请人： Merck & Co., Inc.

发明人： KOPKA, Ihor, E. ,  LI, Bing ,  HAGMANN, William, K.

IPC分类号： C07D239/28 ,  C07D239/34 ,  C07D239/47 ,  C07D239/48 ,  C07D239/52 ,  C07D239/58 ,  A61K31/505 ,  A61K31/506 ,  A61P25/18 ,  A61P25/28

CPC分类号： C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/47 ,  C07D239/52 ,  C07D239/54 ,  C07D239/56 ,  C07D401/12 ,  C07D487/08

摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

公开(公告)号：EP1494997A1

公开(公告)日：2005-01-12

申请号：EP03746565.5

申请日：2003-04-01

申请人： Merck & Co., Inc.

发明人： HAGMANN, William, K. ,  LIN, Linus, S. ,  SHAH, Shrenik, K.

IPC分类号： C07C233/05 ,  C07D311/04 ,  C07D215/02 ,  C07D471/02 ,  C07D277/62 ,  C07D235/02 ,  C07D401/04 ,  C07D495/02 ,  A61K31/165 ,  A61K31/34 ,  A61K31/47 ,  A61K31/44 ,  A61K31/425 ,  A61K31/415 ,  A61K31/38

CPC分类号： C07D249/08 ,  C07C233/66 ,  C07C235/42 ,  C07C235/84 ,  C07C237/20 ,  C07D207/27 ,  C07D207/325 ,  C07D209/88 ,  C07D213/40 ,  C07D213/61 ,  C07D213/81 ,  C07D213/82 ,  C07D215/48 ,  C07D215/50 ,  C07D217/02 ,  C07D231/12 ,  C07D231/14 ,  C07D231/56 ,  C07D233/32 ,  C07D233/56 ,  C07D233/90 ,  C07D235/24 ,  C07D239/28 ,  C07D239/80 ,  C07D241/24 ,  C07D257/04 ,  C07D261/18 ,  C07D263/58 ,  C07D271/08 ,  C07D277/56 ,  C07D277/68 ,  C07D295/155 ,  C07D307/85 ,  C07D401/04 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C40B40/00

摘要： Novel compounds of structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as, the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

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.