公开(公告)号：EP0789571A1

公开(公告)日：1997-08-20

申请号：EP95943332.0

申请日：1995-11-13

申请人： MERCK & CO., INC.

发明人： GUTHIKONDA, Ravindra N. ,  GRANT, Stephan K. ,  MACCOSS, Malcolm ,  SHAH, Shrenik K. ,  SHANKARAN, Kothandaraman ,  CALDWELL, Charles G. ,  DURETTE, Philippe L.

IPC分类号： C07D215 ,  A61K31 ,  A61P1 ,  A61P11 ,  A61P25 ,  A61P29 ,  A61P37 ,  A61P43 ,  C07D207 ,  C07D209 ,  C07D211 ,  C07D219 ,  C07D221 ,  C07D223 ,  C07D225 ,  C07D241 ,  C07D243 ,  C07D265 ,  C07D267 ,  C07D279 ,  C07D281 ,  C07D471 ,  C07D487 ,  C07D491

CPC分类号： C07D215/38 ,  C07D207/22 ,  C07D211/72 ,  C07D211/74 ,  C07D211/78 ,  C07D221/04 ,  C07D223/12 ,  C07D225/02 ,  C07D241/06 ,  C07D241/44 ,  C07D243/08 ,  C07D243/14 ,  C07D265/36 ,  C07D267/10 ,  C07D279/12 ,  C07D279/16 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

摘要： Disclosed herein are the heterocyclic compounds and pharmaceutically acceptable salts thereof which have been found to be useful in the treatment of nitric oxide synthase mediated diseases and disorders.

公开(公告)号：EP1558243A2

公开(公告)日：2005-08-03

申请号：EP03777911.3

申请日：2003-10-24

申请人： Merck & Co., Inc.

发明人： BUTORA, Gabor ,  MILLS, Sander, G. ,  PASTERNAK, Alexander ,  SHANKARAN, Kothandaraman ,  YANG, Lihu ,  ZHOU, Changyou ,  GOBLE, Stephen, D.

IPC分类号： A61K31/351 ,  C07D257/04 ,  C07D263/48 ,  C07D309/14 ,  C07D491/02

CPC分类号： C07D311/00 ,  C07C237/24 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/08 ,  C07C2602/10 ,  C07D211/58 ,  C07D211/96 ,  C07D305/08 ,  C07D307/22 ,  C07D309/14 ,  C07D311/02 ,  C07D311/68 ,  C07D311/74 ,  C07D313/04 ,  C07D319/06 ,  C07D333/36 ,  C07D335/02 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D491/04 ,  C07D491/107 ,  C07D493/08

摘要： The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

公开(公告)号：EP1171122A1

公开(公告)日：2002-01-16

申请号：EP00921700.1

申请日：2000-04-05

申请人： Merck & Co., Inc.

发明人： CHAPMAN, Kevin ,  HALE, Jeffrey ,  KIM, Dooseop ,  LYNCH, Christopher ,  SHAH, Shrenik ,  SHANKARAN, Kothandaraman ,  SHEN, Dong-Ming ,  WILLOUGHBY, Christopher ,  MACCOSS, Malcolm ,  MILLS, Sander, G. ,  LOEBACH, Jennifer, L. ,  GUTHIKONDA, Ravindra, N.

IPC分类号： A61K31/40 ,  A61K31/4025 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61P9/10 ,  A61P31/18

CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is directed to pyrrolidine compounds of formula (I) (wherein R?1, R2, R3, R4, R5, R6, R14¿ and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.

公开(公告)号：EP1755603A2

公开(公告)日：2007-02-28

申请号：EP05741852.7

申请日：2005-04-22

申请人： Merck & Co., Inc.

发明人： YANG, Lihu ,  MILLS, Sander, G. ,  SHANKARAN, Kothandaraman

IPC分类号： A61K31/4745

CPC分类号： C07D471/04

摘要： Compounds of Formula I (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.

公开(公告)号：EP1742919A2

公开(公告)日：2007-01-17

申请号：EP05779916.5

申请日：2005-04-22

申请人： Merck & Co., Inc.

发明人： YANG, Lihu ,  MILLS, Sander, G. ,  MORRIELLO, Gregori, J. ,  GUIADEEN, Deodialsingh ,  SHANKARAN, Kothandaraman

IPC分类号： C07D217/00 ,  A61K31/47

CPC分类号： C07D471/04 ,  C07D405/12

摘要： Compounds of Formula I: I (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.

公开(公告)号：EP0861238A1

公开(公告)日：1998-09-02

申请号：EP96937836.0

申请日：1996-10-28

申请人： MERCK & CO., INC.

发明人： CALDWELL, Charles, G. ,  HAGMANN, William, K. ,  MacCOSS, Malcolm ,  SHAH, Shrenik, K. ,  SHANKARAN, Kothandaraman ,  FURMAN, Karla, L.

IPC分类号： A61K31 ,  A61P1 ,  A61P3 ,  A61P9 ,  A61P11 ,  A61P13 ,  A61P15 ,  A61P17 ,  A61P25 ,  A61P27 ,  A61P29 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07D243 ,  C07D267 ,  C07D281 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D413 ,  C07D417 ,  C07D487 ,  C07D495 ,  C07D498 ,  C07D513

CPC分类号： C07D243/08 ,  C07D267/16 ,  C07D281/06

摘要： Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These diseases and disorders include hypotension, septic shock, toxic shock syndrome, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn, eczema or psoriasis and respiratory conditions such as bronchitis, asthma, oxidant-induced lung injury and acute respiratory distress (ARDS), glomerulonephritis, restenosis, inflammatory sequelae of viral infections, myocarditis, heart failure, atherosclerosis, osteoarthritis, rheumatoid arthritis, septic arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension, retinitis and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis.