公开(公告)号：EP1248618B1

公开(公告)日：2006-03-22

申请号：EP00980817.1

申请日：2000-11-27

申请人： MERCK FROSST CANADA INC. ,  Merck & Co., Inc.

发明人： CLAS, Sophie, Dorothee ,  O'SHEA, Paul ,  DALTON, Chad ,  CROCKER, Louis, S. ,  MCCAULEY, James, A. ,  TILLYER, Richard, D. ,  DAVIES, Ian

IPC分类号： A61K31/44 ,  C07D213/22 ,  A61K31/444

CPC分类号： A61K31/444 ,  C07D213/61

摘要： Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase -2 (COX-2) inhibitor.

公开(公告)号：EP1248618A1

公开(公告)日：2002-10-16

申请号：EP00980817.1

申请日：2000-11-27

申请人： MERCK FROSST CANADA INC. ,  MERCK & CO., INC.

发明人： CLAS, Sophie, Dorothee ,  O'SHEA, Paul ,  DALTON, Chad ,  CROCKER, Louis, S. ,  MCCAULEY, James, A. ,  TILLYER, Richard, D. ,  DAVIES, Ian

IPC分类号： A61K31/44 ,  C07D213/22

CPC分类号： A61K31/444 ,  C07D213/61

摘要： Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase -2 (COX-2) inhibitor.

公开(公告)号：EP1565453A1

公开(公告)日：2005-08-24

申请号：EP03783661.6

申请日：2003-11-18

申请人： Merck & Co., Inc.

发明人： MCCAULEY, James, A. ,  CLAREMON, David, A. ,  LIVERTON, Nigel, J.

IPC分类号： C07D401/06 ,  A61K31/445

CPC分类号： C07D401/06

摘要： 2-[(4-Benzyl)-1-piperidinyl)-methyl]benzimidazole-5-ol derivatives are NMDA NR2B receptor antagonists useful in the treatment of pain and other NMDA mediated diseases.

公开(公告)号：EP1129094A2

公开(公告)日：2001-09-05

申请号：EP99961637.8

申请日：1999-11-10

申请人： Merck & Co., Inc.

发明人： KAUFMAN, Michael, J. ,  MCCAULEY, James, A. ,  RUSH, Daniel, J. ,  TSCHAEN, David, M. ,  VARSOLONA, Richard, J. ,  HO, Guo-Jie

IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61P25/28

CPC分类号： C07D487/04

摘要： There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.

公开(公告)号：EP1019402A1

公开(公告)日：2000-07-19

申请号：EP96936869.5

申请日：1996-10-23

申请人： MERCK & CO., INC.

发明人： DRAPER, Jerome, P. ,  DUBOST, David, C. ,  KAUFMAN, Michael, J. ,  MCCAULEY, James, A. ,  VANDRILLA, Jennifer, L. ,  VARSOLONA, Richard, J.

IPC分类号： C07D471/10 ,  A61K31/445

CPC分类号： C07D471/10 ,  A61K38/00 ,  C07K5/06034

摘要： This invention is concerned with polymorphic forms of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonylspiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyloxy)ethyl]-2-amino-2-methylpropanamide methanesulfonate which is a growth hormone secretagogue that is useful in food animals to promote their growth thereby rendering the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, and to treat medical conditions which are improved by the anabolic effects of growth hormone. The instant polymorphic forms have advantages over the other known forms of N-[1(R)-[(1,2-dihydro-1-methanesulfonylspiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyloxy)-ethyl]-2-amino-2-methylpropanamide methanesulfonate in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations. The present invention is also concerned with processes for preparing these polymorphic forms, pharmaceutical formulations comprising these polymorphic forms as active ingredients and the use of the polymorphic form of the compound and their formulations in the treatment of certain disorders.