公开(公告)号：EP1667978A2

公开(公告)日：2006-06-14

申请号：EP04816878.5

申请日：2004-09-17

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

发明人： DINSMORE, Christopher, J. ,  BERGMAN, Jeffrey, M. ,  MCINTYRE, Charles, J. ,  CLAREMON, David, A.

IPC分类号： C07D217/16 ,  A61K31/47

CPC分类号： C07D217/24 ,  A61K31/4725 ,  A61K31/5377 ,  A61K45/06 ,  C04B35/632 ,  C07D401/12 ,  C07D405/12

摘要： The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

公开(公告)号：EP1651628A2

公开(公告)日：2006-05-03

申请号：EP04757246.6

申请日：2004-07-20

申请人： Merck & Co., Inc. (a New Jersey corp.) ,  Merck Sharp & Dohme de Espana S.A.E.

发明人： SINGH, Sheo Bux ,  WANG, Jun ,  BASILIO, Angela ,  GENILLOUD, Olga ,  HERNANDEZ, Pilar ,  TORMO, Jose Ruben

IPC分类号： C07D311/94 ,  C07D311/96 ,  A61K31/352

CPC分类号： C12R1/465 ,  C07D493/08 ,  C12P17/06

摘要： Fermentation of a nutrient medium with a eubacterium Streptomyces sp. yields a novel antibacterial compound of structure (I).

公开(公告)号：EP1635773A2

公开(公告)日：2006-03-22

申请号：EP04753832.7

申请日：2004-06-02

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

发明人： FONG, Tung, M. ,  ERONDU, Ngozi, E ,  MACNEIL, Douglas, J. ,  MCINTYRE, James, H. ,  VAN DER PLOEG, Leonardus, H. T.

IPC分类号： A61K8/18

CPC分类号： A61K31/4747 ,  A61K31/155 ,  A61K31/352 ,  A61K31/353 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to compositions comprising an anti-obesity agent and an anti-hypertensive agent useful for the treatment of hypertension, hypertension associated with obesity, and hypertension-related disorders. The present invention further relates to methods of treating or preventing obesity, and obesity-related disorders, in a subject in need thereof by administering a composition of the present invention. The present invention further provides for pharmaceutical compositions, medicaments, and kits useful in carrying out these methods.

公开(公告)号：EP0771209B1

公开(公告)日：2002-09-04

申请号：EP95926602.4

申请日：1995-06-07

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

发明人： DeFEO-JONES, Deborah ,  FENG, Dong-Mei ,  GARSKY, Victor M. ,  JONES, Raymond E. ,  OLIFF, Allen I.

IPC分类号： A61K38/00 ,  A61K38/08 ,  A61K38/10 ,  A61K38/16 ,  A61P13/08 ,  A61P35/00

CPC分类号： C07K14/47 ,  A61K38/00 ,  A61K47/62 ,  A61K47/65

摘要： Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.

公开(公告)号：EP0873336B1

公开(公告)日：2002-03-27

申请号：EP96944249.0

申请日：1996-12-10

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

发明人： GOULET, Mark ,  ASHTON, Wallace, T. ,  CHU, Lin ,  FISHER, Michael, H. ,  GIROTRA, Narindar, N. ,  LIN, Peter ,  WYVRATT, Matthew, J.

IPC分类号： C07D401/12 ,  A61K31/40 ,  C07D401/14 ,  C07D487/08 ,  C07D413/14

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D487/08

摘要： There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

公开(公告)号：EP1112259A1

公开(公告)日：2001-07-04

申请号：EP99948170.8

申请日：1999-09-09

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

发明人： NELSON, Todd, D. ,  BHUPATHY, Mahadevan

IPC分类号： C07D265/32

CPC分类号： C07D265/32

摘要： The present invention is concerned with a novel process for the preparation of N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one of formula (5). This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.

公开(公告)号：EP0755374B1

公开(公告)日：2000-08-16

申请号：EP95915464.2

申请日：1995-03-31

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

发明人： HO, Guo-Jie ,  MATHRE, David A. ,  SONG, Zhiguo ,  EMERSON, Khateeta

IPC分类号： C07C231/02 ,  C07K1/02 ,  C07K1/06 ,  C07K1/08

CPC分类号： C07D295/26 ,  C07C2602/42 ,  C07D211/76 ,  C07D401/06 ,  C07D401/14 ,  C07D453/04 ,  C07K1/023 ,  C07K1/026

公开(公告)号：EP1011667A1

公开(公告)日：2000-06-28

申请号：EP98926171.4

申请日：1998-06-01

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

发明人： GOULET, Mark ,  UJJAINWALLA, Feroze ,  WALSH, Thomas, F. ,  WYVRATT, Matthew, J., Jr. ,  YOUNG, Jonathan, R. ,  CHU, Lin

IPC分类号： A61K31/41 ,  A61K31/44 ,  C07D249/08 ,  C07D257/04 ,  C07D271/06 ,  C07D401/14

CPC分类号： C07D231/12 ,  A61K38/09 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D471/08 ,  C07D487/08 ,  A61K31/00 ,  A61K2300/00

摘要： There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

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：EP0956352A1

公开(公告)日：1999-11-17

申请号：EP97944467.0

申请日：1997-09-26

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

发明人： ARMSTRONG, Marcy, E. ,  KEYS, Robert, D. ,  LEWIS, John, A. ,  LIU, Margaret, A. ,  McCLEMENTS, William, L.

IPC分类号： C12N15 ,  A61K31 ,  A61K39 ,  A61K48 ,  A61P31 ,  C07K14

CPC分类号： C07K14/005 ,  A61K2039/51 ,  C12N2710/16622

摘要： Genes encoding herpes simplex virus type 2 (HSV-2) proteins were cloned into eukaryotic expression vectors to express the encoded proteins in mammalian muscle cells in vivo. Animals were immunized by injection of these DNA constructs, termed polynucleotide vaccines or PNV, into their muscles. In a DNA titration, it was found that a single immunization of 0.5 νg of (one) PNV, gave ⊃90 % seroconversion by ten weeks post immunization. Immune antisera neutralized both HSV-2 and HSV-1 in cell culture. When animals were challenged with HSV-2, significant (p∫.001) protection from lethal infection was achieved following PNV vaccination. DNA constructs may be full-length, truncated and/or mutated forms and may be delivered along or in combination in order to optimize immunization and protection from HSV infection.