公开(公告)号：EP1331937A2

公开(公告)日：2003-08-06

申请号：EP01987196.1

申请日：2001-10-19

申请人： Merck & Co., Inc.

发明人： PATANE, Michael, A.

IPC分类号： A61K31/553 ,  A61P19/10 ,  C07D267/16

CPC分类号： C07D471/04 ,  A61K31/00 ,  A61K31/553 ,  A61K31/66 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to a novel dibenzoxazepine derivative, its synthesis, and its use as an αξ integrin receptor antagonist. More particularly, the compound of the present invention is an antagonist of the integrin receptors αξβ3 and αξβ5 and therefor useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, artherosclerosis, inflammatory arthritis, cancer and metastatic tumor growth.

公开(公告)号：EP1322596A1

公开(公告)日：2003-07-02

申请号：EP01973294.0

申请日：2001-09-21

申请人： Merck & Co., Inc.

发明人： FINKE, Paul, E. ,  MEURER, Laura, C. ,  MILLS, Sander, G. ,  MACCOSS, Malcolm ,  QI, Hongbo

IPC分类号： C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07D207/16 ,  C07D211/34 ,  C07D241/04 ,  A61K31/397 ,  A61K31/40 ,  A61K31/41 ,  A61K31/445 ,  A61K31/495 ,  A61K31/195 ,  A61P25/26 ,  C07D205/04 ,  C07D401/04 ,  C07C217/52 ,  C07C62/34 ,  C07C43/196

CPC分类号： C07D257/04 ,  C07C43/196 ,  C07C51/09 ,  C07C62/34 ,  C07C217/52 ,  C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07C2601/08 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/16 ,  C07D211/60 ,  C07D211/62 ,  C07D265/30 ,  C07D401/04

摘要： The present invention is directed to certain novel compounds represented by structural formula (I), or a pharmaceutically acceptable salt thereof, wherein R?3, R5, R6, R7, R8, R11, R12, R13¿, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.

公开(公告)号：EP1280821A1

公开(公告)日：2003-02-05

申请号：EP01924404.5

申请日：2001-03-28

申请人： Merck & Co., Inc.

发明人： CULLY, Doris, F. ,  ZHENG, Yingcong

IPC分类号： C07K14/47 ,  C07K14/705 ,  C12N5/10 ,  C12N15/12 ,  C12N15/63 ,  C12N15/64 ,  G01N33/53 ,  G01N33/567

CPC分类号： C07K14/705

摘要： The present invention relates in part to isolated nucleic acid molecules (polynucleotides) which encode Dermacentor variabilis ligand gated ion channel proteins. The present invention also relates to recombinant vectors and recombinant hosts which contain a DNA fragment encoding D. variabilis LGIC/GluCl channels, substantially purified forms of associated D. variabilis channel proteins and recombinant membrane fractions comprising these proteins, associated mutant proteins, and methods associated with identifying compounds which modulate associated Dermacentor variabilis LGIC/GluCl, which will be useful as insecticides and acaracides.

公开(公告)号：EP1268495A1

公开(公告)日：2003-01-02

申请号：EP01916792.3

申请日：2001-03-21

申请人： MERCK FROSST CANADA INC. ,  BANYU PHARMACEUTICAL CO., LTD.

发明人： BAYLY, Christopher ,  OHKUBO, Mitsuru

IPC分类号： C07F9/38 ,  A61K31/66 ,  A61P3/04 ,  A61P3/10 ,  C07F9/40 ,  C07F9/60 ,  C07F9/58 ,  C07F9/6524 ,  C07F9/653 ,  C07F9/553 ,  C07F9/655 ,  C07F9/59 ,  C07F9/6539 ,  C07F9/6512 ,  C07F9/6558 ,  C07F9/6518 ,  C07F9/6506

CPC分类号： C07F9/65583 ,  A61K31/66 ,  A61K45/06 ,  C07F9/3882 ,  C07F9/4056 ,  C07F9/5537 ,  C07F9/582 ,  C07F9/591 ,  C07F9/60 ,  C07F9/6506 ,  C07F9/65068 ,  C07F9/65122 ,  C07F9/65128 ,  C07F9/65182 ,  C07F9/6524 ,  C07F9/65312 ,  C07F9/65318 ,  C07F9/6539 ,  C07F9/65395 ,  C07F9/6552 ,  C07F9/65522 ,  A61K2300/00

摘要： The invention encompasses the novel class of compounds represented by the formula (I), which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.

摘要翻译： 本发明包括由式（I）表示的新型化合物，它们是PTP-1B酶的抑制剂。 本发明还包括治疗或预防PTP-1B介导的疾病（包括糖尿病）的药物组合物和方法。

公开(公告)号：EP1268494A1

公开(公告)日：2003-01-02

申请号：EP01916791.5

申请日：2001-03-21

申请人： Merck Frosst Canada & Co.

发明人： LI, Chun, Sing ,  LAU, Cheuk, K. ,  THERIEN, Michel ,  GAUTHIER, Jacques, Y. ,  BAYLY, Christopher ,  DUFRESNE, Claude ,  FORTIN, Rejean ,  LEBLANC, Yves ,  ROY, Patrick ,  WANG, Zhaoyin

IPC分类号： C07F9/38 ,  C07F9/40 ,  A61K31/66 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07F9/65583 ,  A61K31/66 ,  A61K45/06 ,  C07F9/3882 ,  C07F9/4056 ,  C07F9/5537 ,  C07F9/582 ,  C07F9/591 ,  C07F9/60 ,  C07F9/6506 ,  C07F9/65068 ,  C07F9/65122 ,  C07F9/65128 ,  C07F9/65182 ,  C07F9/6524 ,  C07F9/65312 ,  C07F9/65318 ,  C07F9/6539 ,  C07F9/65395 ,  C07F9/6552 ,  C07F9/65522 ,  A61K2300/00

摘要： The invention encompasses the novel class of compounds represented by formula (I), which are inhibitors of the PTP-1B enzyme . The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.

摘要翻译： 本发明包括式（I）代表的新型化合物，它们是PTP-1B酶的抑制剂。 本发明还包括治疗或预防PTP-1B介导的疾病（包括糖尿病）的药物组合物和方法。

公开(公告)号：EP1023062B1

公开(公告)日：2002-12-18

申请号：EP98953450.8

申请日：1998-10-13

申请人： MERCK & CO., INC.

发明人： BLIZZARD, Timothy, A. ,  RATCLIFFE, Ronald, W.

IPC分类号： A61K31/40 ,  C07D477/14 ,  C07D519/00

CPC分类号： C07D477/14

公开(公告)号：EP1261584A1

公开(公告)日：2002-12-04

申请号：EP01916290.8

申请日：2001-02-28

申请人： Merck & Co., Inc.

发明人： BRANDS, Karel, J., M. ,  CONRAD, Karen, M. ,  WILLIAMS, John, M.

IPC分类号： C07D207/12 ,  C07D207/16

CPC分类号： C07D207/16

摘要： Crystalline 2S-cis-3-[[(4-mercapto-2-pyrrolidinyl)carbonyl]-amino]benzoic acid and salts and solvates thereof are disclosed. A crystalline type is described.

公开(公告)号：EP1259494A1

公开(公告)日：2002-11-27

申请号：EP01910624.4

申请日：2001-02-14

申请人： Merck & Co., Inc.

发明人： LIU, Kun ,  XU, Libo ,  JONES, A., Brian

IPC分类号： C07D261/20 ,  A61K31/423

CPC分类号： C07D261/20 ,  A61K31/00 ,  A61K45/06

摘要： A class of aryloxyacetic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

公开(公告)号：EP1257559A1

公开(公告)日：2002-11-20

申请号：EP01910442.1

申请日：2001-02-07

申请人： Merck & Co., Inc.

发明人： MANDALA, Suzanne, M. ,  THORNTON, Rosemary, A.

IPC分类号： C07H21/02 ,  C07H21/04 ,  C12N5/00 ,  C12N5/02 ,  C12N15/00 ,  C12N15/09 ,  C12N15/63 ,  C12N15/70 ,  C12N15/74

CPC分类号： C12N9/16

摘要： The present invention provides polynucleotides and polypeptides of a murine sphingosine-1-phosphate phosphatase, referred to herein as mSPP1. The polynucleotides and polypeptides are used to further provide expression vectors, host cells comprising the vectors, probes and primers, antibodies against the mSPP1 protein and polypeptides thereof, assays for the presence or expression of mSPP1 and assays for the identification of compounds that interact with mSPP1.

公开(公告)号：EP1257264A1

公开(公告)日：2002-11-20

申请号：EP01912748.9

申请日：2001-02-14

申请人： Merck & Co., Inc.

发明人： PARKER, Dann, LeRoy, Jr. ,  RATCLIFFE, Ronald, W. ,  WILKENING, Robert, R. ,  WILDONGER, Kenneth, J.

IPC分类号： A61K31/05 ,  A61K31/15 ,  A61K31/19 ,  A61K31/122 ,  A61K31/277 ,  A61K31/381 ,  A61K31/445 ,  C07C49/543 ,  C07C49/553 ,  C07C39/23 ,  C07C57/03 ,  C07C251/32 ,  C07C255/47 ,  C07D211/06 ,  C07D333/04

CPC分类号： C07D295/088 ,  C07C39/42 ,  C07C45/28 ,  C07C45/46 ,  C07C45/63 ,  C07C45/65 ,  C07C45/68 ,  C07C45/69 ,  C07C45/71 ,  C07C45/72 ,  C07C45/73 ,  C07C45/74 ,  C07C45/75 ,  C07C49/747 ,  C07C49/755 ,  C07C59/90 ,  C07C205/45 ,  C07C251/44 ,  C07C255/47 ,  C07C2603/18 ,  C07D333/22 ,  C07C49/84

摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.