公开(公告)号：EP0966282A1

公开(公告)日：1999-12-29

申请号：EP98903447.0

申请日：1998-01-07

申请人： MERCK & CO., INC.

发明人： BEERE, Polly, A. ,  CHANG, Paul, I. ,  PITT, Bertram ,  RUCINSKA, Ewa, J. ,  SEGAL, Robert ,  SHARMA, Divakar ,  SNAVELY, Duane, B.

IPC分类号： C07D401 ,  A61K31 ,  A61K38 ,  A61K45 ,  A61P9 ,  C07D207 ,  C07D403 ,  C07D405 ,  C07D409

CPC分类号： A61K38/04 ,  A61K31/41 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/519

摘要： Angiotensin II receptor antagonists are useful in reducing and preventing mortality and sudden cardiac death in symptomatic heart failure patients. Losartan potassium has been shown to reduce mortality and sudden cardiac death in this patient population. Additionally, losartan potassium has been shown to reduce the need for hospitalization of symptomatic heart failure patients.

公开(公告)号：EP0948327A1

公开(公告)日：1999-10-13

申请号：EP97952573.0

申请日：1997-12-19

申请人： MERCK & CO., INC.

发明人： ADAMS, Alan, D. ,  VON LANGEN, Derek ,  TOLMAN, Richard, L. ,  KOYAMA, Hiroo

IPC分类号： C07D307 ,  A61K31 ,  A61P3 ,  A61P9 ,  A61P13 ,  A61P27 ,  C07D209 ,  C07D213 ,  C07D403 ,  C07D405 ,  C07D407 ,  C07D409 ,  C07D411 ,  C07D413

CPC分类号： A61K31/135 ,  A61K31/343 ,  A61K31/395 ,  A61K31/40 ,  A61K31/404 ,  A61K31/41 ,  A61K31/415 ,  A61K31/423 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/517 ,  C07D209/12 ,  C07D209/18 ,  C07D213/56 ,  C07D307/80 ,  C07D307/83 ,  C07D307/92 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D411/02 ,  C07D413/04 ,  C07D413/12

摘要： The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compound which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.

摘要翻译： 本发明涉及作为有用的抗糖尿病化合物的芳基和杂芳基氧乙酸型化合物。 还公开了使用这些化合物治疗糖尿病和相关疾病以及降低甘油三酯水平的组合物和方法。

公开(公告)号：EP0946178A1

公开(公告)日：1999-10-06

申请号：EP97941644.0

申请日：1997-09-15

申请人： MERCK & CO., INC.

发明人： GOULD, Robert, J. ,  NICHTBERGER, Steven, A. ,  RHYMER, Patricia, A. ,  OLOFSSON, Lars

IPC分类号： A61K31 ,  A61K38 ,  A61K45 ,  A61P7 ,  A61P9

CPC分类号： A61K45/06

摘要： The instant invention involves a combination therapy and pharmaceutical compositions comprised of a therapeutically effective amount of a cholesterol reducing agent such as an HMG-CoA reductase inhibitor in combination with a platelet aggregation inhibitor which is useful for inhibiting platelet aggregation, for inhibiting the formation of thrombotic occlusions, and for treating, preventing and reducing the risk of occurrence of cardiovascular and cerebrovascular events and related vaso-occlusive disorders.

公开(公告)号：EP0937068A1

公开(公告)日：1999-08-25

申请号：EP97913800.0

申请日：1997-10-24

申请人： MERCK & CO., INC.

发明人： BREEN, Patrick ,  DIENEMANN, Erik, A. ,  EPSTEIN, Albert, D. ,  LARSON, Karen, A. ,  KENNEDY, Michael, T. ,  MAHADEVAN, Hari

IPC分类号： C07D403

CPC分类号： C07D403/10

摘要： Losartan potassium is an angiotensin II antagonist useful in the treatment of hypertension and congestive heart failure (I). This invention relates to the process for the controlled crystallization of losartan potassium utilizing anti-solvent addition combined with massive seeding in order to obtain the desired crystal morphology and bulk physical properties necessary for successful formulation.

公开(公告)号：EP0931141A2

公开(公告)日：1999-07-28

申请号：EP97944395.0

申请日：1997-09-23

申请人： MERCK & CO., INC.

发明人： SARDANA, Vinod, V. ,  BLUE, Jeffrey, T.

IPC分类号： G01N33 ,  C12N9 ,  C12Q1

CPC分类号： C12N9/503

摘要： The protease of Hepatitis C virus (HCV) is purified without detergent, and is useful as a screening tool for HCV antivirals as well as a diagnostic tool for diseases resulting from HCV infection.

公开(公告)号：EP0923556A1

公开(公告)日：1999-06-23

申请号：EP97936396.0

申请日：1997-08-05

申请人： MERCK & CO., INC.

发明人： DOLLING, Ulf, H. ,  FREY, Lisa, F. ,  TILLYER, Richard, D. ,  TSCHAEN, David, M.

IPC分类号： C07D213 ,  C07D263 ,  C07D401 ,  C07D405 ,  C07D413 ,  C07D498 ,  C07F7

CPC分类号： C07D401/04 ,  C07D263/06 ,  C07D405/06 ,  C07D413/04 ,  C07F7/1892

摘要： This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.

摘要翻译： 本发明涉及合成内皮素拮抗剂的关键中间体和使用不对称共轭加成反应合成该关键中间体。

公开(公告)号：EP0922052A1

公开(公告)日：1999-06-16

申请号：EP97905980.0

申请日：1997-02-18

申请人： MERCK & CO., INC.

发明人： HESS, John, W. ,  CASKEY, C., Thomas ,  LIU, Qingyun ,  PHILLIPS, Michael, S.

IPC分类号： G01N33 ,  C07K14 ,  C12N1 ,  C12N5 ,  C12N15 ,  C12Q1 ,  C12R1

CPC分类号： C07K14/72

摘要： The rat ob receptor gene has been isolated and cloned. Two different alleles have been identified: the wild-type, and the fa-allele which differs from the wild-type by only one base pair. The base pair change, however, introduces an MspI restriction site into the DNA sequence, and also results in an amino acid change. Also part of the invention are the novel receptors, vectors containing the nucleic acid encoding the receptors, host cells transformed with this gene, and assays which use the gene or protein and identify new ligands.

公开(公告)号：EP0921820A1

公开(公告)日：1999-06-16

申请号：EP97932580.0

申请日：1997-06-20

申请人： MERCK & CO., INC.

发明人： MORSY, Manal, A. ,  GU, Ming, Cheng ,  ZHAO, Jing ,  CASKEY, C., Thomas

IPC分类号： A61K48 ,  A61K38 ,  A61P3 ,  C07K14 ,  C12N15

CPC分类号： C12N15/86 ,  A61K38/2264 ,  A61K48/00 ,  C07K14/5759 ,  C07K14/715 ,  C12N2710/10343

摘要： Gene therapy can treat obesity in mammals. An obesity regulating gene is delivered to a mammal. Preferably, the gene encodes leptin or a leptin receptor. The protein which is delivered and expressed in vivo is more effective than protein which is injected into the animal.

摘要翻译： 基因疗法可以治疗哺乳动物的肥胖症。 肥胖调节基因被递送给哺乳动物。 优选地，该基因编码瘦蛋白或瘦蛋白受体。 在体内递送并表达的蛋白质比注射到动物体内的蛋白质更有效。

公开(公告)号：EP0915847A1

公开(公告)日：1999-05-19

申请号：EP97934091.0

申请日：1997-07-21

申请人： MERCK & CO., INC.

发明人： FISHER, Michael, H. ,  NAYLOR, Elizabeth, M. ,  OK, Hyun ,  PARMEE, Emma, R. ,  SHIH, Thomas ,  WEBER, Ann, E.

IPC分类号： C07D277 ,  A61K31 ,  A61P1 ,  A61P3 ,  A61P25 ,  A61P43 ,  C07C311 ,  C07D209 ,  C07D213 ,  C07D215 ,  C07D233 ,  C07D261 ,  C07D271 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D413 ,  C07D417 ,  C07D471 ,  C07D491 ,  C07D495 ,  C07D519

CPC分类号： C07C311/21 ,  C07C311/47 ,  C07D209/08 ,  C07D213/38 ,  C07D213/73 ,  C07D215/36 ,  C07D233/32 ,  C07D271/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Substituted sulfonamides are selective β3 adrenergic receptor agonists with very little β1 and β2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used as reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

公开(公告)号：EP0914611A1

公开(公告)日：1999-05-12

申请号：EP97924507.0

申请日：1997-04-18

申请人： MERCK & CO., INC.

发明人： ROSENBLUM, Charles, I. ,  VAN DER PLOEG, Leonardus ,  QURESHI, Sajjad, A. ,  CULLY, Doris, F. ,  HESS, John, W. ,  TOTA, Michael, R. ,  CHEN, Fang

IPC分类号： C12N15 ,  C07K14 ,  C12N1 ,  C12N5 ,  C12Q1 ,  G01N33

CPC分类号： C07K14/715 ,  C07K14/4705 ,  C12Q1/6897

摘要： A trans-activation assay for leptin is described. Leptin response elements are located proximal to a promoter, and the promoter region is operatively linked to a reporter gene. When leptin binds with the receptor, the reporter gene is transcribed.