公开(公告)号：EP1158984A1

公开(公告)日：2001-12-05

申请号：EP99971320.9

申请日：1999-10-26

申请人： Merck & Co., Inc.

发明人： BERGMAN, Jeffrey, M.

IPC分类号： A61K31/495 ,  C07D267/00 ,  C07D281/00 ,  C07D291/00 ,  C07D245/00 ,  C07D487/22 ,  C07D225/00 ,  C07D513/22

CPC分类号： C07D498/14 ,  C07D498/22

摘要： The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit a prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

公开(公告)号：EP1147107A1

公开(公告)日：2001-10-24

申请号：EP00906932.9

申请日：2000-01-14

申请人： Merck & Co., Inc.

发明人： FRALEY, Mark, E. ,  HUNGATE, Randall, W. ,  TEBBEN, Andrew, J.

IPC分类号： C07D471/04 ,  C07D401/14 ,  A61K31/4439 ,  A61K31/444

CPC分类号： C07D409/14

摘要： The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases and conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy, and the like in mammals.

公开(公告)号：EP0840733B1

公开(公告)日：2001-10-24

申请号：EP96925277.4

申请日：1996-07-08

申请人： MERCK & CO., INC.

发明人： CHENG, Chen, Y. ,  LARSEN, Robert, D. ,  McCAULEY, James, A. ,  VANDRILLA, Jennifer, L. ,  VERHOEVEN, Thomas, R.

IPC分类号： C07D403/06 ,  A61K31/41

CPC分类号： C07D249/08 ,  A61K31/4196 ,  C07D231/12 ,  C07D233/56

摘要： The bisulfate salt of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine is a selective agonist of 5-HT1-like receptors and is useful in the treatment of migraine and associated disorders.

公开(公告)号：EP0830350B1

公开(公告)日：2001-10-04

申请号：EP96920612.7

申请日：1996-06-03

申请人： MERCK & CO., INC.

发明人： CLAREMON, David, A. ,  LIVERTON, Nigel ,  SELNICK, Harold, G. ,  SMITH, Garry, R.

IPC分类号： C07D243/12 ,  A61K31/55

CPC分类号： C07D243/12

摘要： This invention is concerned with novel compounds represented by structural formula (I) which are useful in the treatment of arrhythmia.

公开(公告)号：EP1129105A1

公开(公告)日：2001-09-05

申请号：EP99971813.3

申请日：1999-11-05

申请人： Merck & Co., Inc.

发明人： MACNEIL, Douglas, J. ,  WEINBERG, David, H. ,  VAN DER PLOEG, Leonardus, H., T.

IPC分类号： C07H21/04 ,  C12N1/20 ,  C12N15/00 ,  C12P21/06

CPC分类号： C07K14/723

摘要： The present invention relates to rhesus monkey DNA molecules encoding the melanocortin-4 receptor protein, recombinant vectors comprising DNA molecules encoding rhesus MC-4R, recombinant host cells which contain a recombinant vector encoding rhesus MC-4R, the rhesus MC-4R protein encoded by the DNA molecule, and methods of identifying selective agonists and antagonists of rhesus MC-4R.

公开(公告)号：EP0777659B1

公开(公告)日：2001-06-06

申请号：EP95927862.3

申请日：1995-08-07

申请人： MERCK SHARP & DOHME LTD.

发明人： HARRISON, Timothy ,  OWENS, Andrew, Pate ,  SWAIN, Christopher, John

IPC分类号： C07D265/32 ,  C07D413/06 ,  A61K31/535

CPC分类号： C07D413/06 ,  C07D265/32 ,  C07D487/08 ,  C07F7/1856

公开(公告)号：EP1097147A1

公开(公告)日：2001-05-09

申请号：EP99937204.8

申请日：1999-07-06

申请人： MERCK & CO., INC.

发明人： FRALEY, Mark, E. ,  HUNGATE, Randall, W. ,  HOFFMAN, William, F. ,  HUCKLE, William, R. ,  KENDALL, Richard, L. ,  THOMAS, Kenneth, A., Jr.

IPC分类号： C07D263/48 ,  C07D277/46 ,  A61K31/42 ,  A61K31/425

CPC分类号： A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  C07D263/48 ,  C07D277/20 ,  C07D277/46 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

摘要： The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases and conditions such as angiogenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.

公开(公告)号：EP1089750A1

公开(公告)日：2001-04-11

申请号：EP99930491.8

申请日：1999-06-21

申请人： MERCK & CO., INC.

发明人： RESZKA, Alfred, A.

IPC分类号： A61K38/00 ,  A61K38/07 ,  A61K31/66 ,  C07K5/00

CPC分类号： A61K38/07 ,  A61K38/06 ,  A61K38/55 ,  C07K5/0827 ,  C07K5/1027 ,  A61K2300/00

摘要： The present invention relates to oral compositions and methods for inhibiting bone resorption in a mammal while counteracting the occurrence of potentially adverse gastrointestinal effects. The compositions useful herein comprise the combination of a pharmaceutically effective amount of a nitrogen-containing bisphosphonate or a pharmaceutically-acceptable salt thereof and a pharmaceutically effective amount of a caspase inhibitor.

摘要翻译： 本发明涉及口服组合物和方法，用于抑制哺乳动物中的骨吸收，同时抵消可能不利的胃肠作用的发生。 可用于本文的组合物包含药学有效量的含氮双膦酸盐或其药学上可接受的盐与药学有效量的半胱天冬酶抑制剂的组合。

公开(公告)号：EP1082325A1

公开(公告)日：2001-03-14

申请号：EP99925849.4

申请日：1999-05-26

申请人： MERCK & CO., INC.

发明人： DININNO, Frank, P.

IPC分类号： C07D499/887 ,  A61K31/43

CPC分类号： C07D499/88

摘要： The present invention relates to penem antibacterial agents in which the penem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula (I). Pharmaceutical compositions and methods of use are also included.

摘要翻译： 本发明涉及青霉烯类抗菌剂，其中青霉烯核与6元碳环稠合。 该化合物进一步被各种取代基取代，包括至少一个阳离子基团。 该化合物由式（I）表示。 药物组合物和使用方法也包括在内。

公开(公告)号：EP1071685A1

公开(公告)日：2001-01-31

申请号：EP99916629.1

申请日：1999-04-12

申请人： MERCK & CO., INC.

发明人： PYE, Philip, J. ,  REIDER, Paul, J. ,  ROSSEN, Kai ,  VOLANTE, Ralph, P.

IPC分类号： C07D477/14

CPC分类号： C07D477/04 ,  C07D205/08

摘要： An efficient method for the synthesis of a compound of formula (2) is disclosed which comprises reacting a 4-acyl-2-azetidinone with a titanium, zirconium or hafnium enolate of a 1-hydroxy-2-butanone derivative.