公开(公告)号：EP1954135A2

公开(公告)日：2008-08-13

申请号：EP06837498.2

申请日：2006-11-14

申请人： Merck and Co., Inc.

发明人： BELL, Ian, M. ,  SELNICK, Harold, G. ,  WOOD, Michael, R. ,  THEBERGE, Cory, R. ,  STUMP, Craig, A. ,  GALLICCHIO, Steven, N. ,  ZARTMAN, C., Blair

IPC分类号： A01N43/42 ,  A61K31/44

CPC分类号： C07D471/20 ,  C07D519/00

摘要： Compounds of formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, E1, E2, E3, E4, E5, G1, G2, J and K are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

公开(公告)号：EP1947936A2

公开(公告)日：2008-07-30

申请号：EP06827515.5

申请日：2006-11-03

申请人： Merck and Co., Inc.

发明人： FRANKEL, Stanley ,  DEUTSCH, Paul ,  RANDOLPH, Sophia ,  FINE, Bernard

IPC分类号： A01N37/18

CPC分类号： A61K31/167 ,  A61K31/19 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/69 ,  A61K2300/00

摘要： The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Bortezomib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.

公开(公告)号：EP1942907A2

公开(公告)日：2008-07-16

申请号：EP06836951.1

申请日：2006-11-03

申请人： Merck and Co., Inc. ,  The Regents of the University of Colorado

发明人： BUNN, Paul ,  WITTA, Samir ,  RICHON, Victoria, M. ,  FRANKEL, Stanley ,  DEUTSCH, Paul ,  RANDOLPH, Sophia

IPC分类号： A61K31/70

CPC分类号： A61K31/167 ,  A61K31/19 ,  A61K31/517 ,  A61K2300/00

摘要： The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Erlotinib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.

公开(公告)号：EP1940406A2

公开(公告)日：2008-07-09

申请号：EP06816998.6

申请日：2006-10-17

申请人： Merck and Co., Inc.

发明人： TROTTER, Wesley, B. ,  NANDA, Kausik, K. ,  WOLKENBERG, Scott ,  NOLT, Brad, M. ,  MANLEY, Peter ,  KETT, Nathan, R. ,  BILODEAU, Mark, T.

IPC分类号： A61K31/47

CPC分类号： C07D401/14 ,  C07D213/38 ,  C07D213/57 ,  C07D213/74

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

公开(公告)号：EP1934364A2

公开(公告)日：2008-06-25

申请号：EP06804139.1

申请日：2006-09-26

申请人： Merck and Co., Inc.

发明人： KANE, Stefanie, A. ,  MALLEE, John, J. ,  SALVATORE, Christopher ,  WANG, Jixin

IPC分类号： C12P21/06 ,  C12N1/12 ,  C12N1/20 ,  C12N15/00 ,  C12N15/09 ,  C12N15/63 ,  C12N15/70

CPC分类号： C07K14/705

摘要： The subject invention relates to the rhesus monkey P2X3 receptor, nucleic acids encoding this receptor, methods of modulating the activity of a target purinergic receptor using the P2X3 receptor and to uses of these methods. In particular, such methods may be used, for example, to accelerate the rate of resensitization of a desensitized receptor.

公开(公告)号：EP1758594A1

公开(公告)日：2007-03-07

申请号：EP04776045.9

申请日：2004-05-19

申请人： Merck and Co., Inc.

发明人： DAIFOTIS, Anastasia, G. ,  DENKER, Andrew ,  IKEDA, Craig ,  MATUSZEWSKI, Bogdan, K. ,  MAZEL, Sid ,  PORRAS, Arturo, G. ,  SANTORA, Art ,  SEBURG, Randal, Alan ,  ZHU, Limin ,  YATES, John ,  KIRSCH, John, D.

IPC分类号： A61K31/663 ,  A61K31/69 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  G01N33/82

CPC分类号： A61K31/59 ,  A61K31/593 ,  A61K31/663 ,  A61K31/69 ,  Y02A50/401 ,  A61K2300/00

摘要： Disclosed are compositions and methods for preventing, inhibiting, reducing and treating conditions and diseases associated with abnormal bone resorption in mammals, including for example osteoporosis. Embodiments of compositions of the invention comprise a pharmaceutically effective amount of alendronate and vitamin D3 suitable for once-weekly dosing. Compositions and methods of the invention provide vitamin D nutrition during bisphosphonate treatment to facilitate normal bone formation and mineralization while minimizing the occurrence of or potential for the complications associated with vitamin D insufficiency, such as hypocalcaemia and osteomalacia. Also disclosed are methods for manufacturing compositions of the present invention, for measuring stability and degradation of those compositions, and for measuring blood plasma levels of vitamin D.

公开(公告)号：EP1747212A2

公开(公告)日：2007-01-31

申请号：EP05804807.5

申请日：2005-05-06

申请人： Merck and Co., Inc.

发明人： DREHER, Spencer, D. ,  IKEMOTO, Norihiro ,  SHULTZ, C. Scott ,  WILLIAMS, J. Michael

IPC分类号： C07D315/00

CPC分类号： C07D315/00 ,  C07C303/40 ,  C07C2601/14 ,  C07D309/04 ,  C07D309/06 ,  C07D309/20 ,  C07C311/13 ,  C07C311/19 ,  C07C311/16 ,  C07C311/29

摘要： This invention relates to a process for preparing optically active α -amino acid substrates which are used to make potent lethal factor (LF) inhibitors for the treatment of anthrax. This invention further relates to a process for synthesis of potent LF-inhibitors for the treatment of anthrax. Specifically, the invention concerns a novel, high-yielding and highly enantioselective asymmetric hydrogenation reaction of a tetrasubstituted ene-sulfonamide acid or ester.

摘要翻译： 本发明涉及用于制备用于治疗炭疽的有效致死因子（LF）抑制剂的光学活性α-氨基酸底物的方法。 本发明还涉及用于合成治疗炭疽的有效的LF抑制剂的方法。 具体地，本发明涉及四取代的烯 - 磺酰胺酸或酯的新颖的高产率和高度对映选择性的不对称氢化反应。

公开(公告)号：EP1729772A2

公开(公告)日：2006-12-13

申请号：EP05726105.9

申请日：2005-03-23

申请人： Merck and Co., Inc. ,  MERCK SHARP & DOHME LTD.

发明人： BLACKABY, Wesley ,  DUGGAN, Mark, E. ,  HALLETT, David ,  HARTMAN, George, D. ,  JENNINGS, Andrew, S. ,  LEISTER, William, H. ,  LEWIS, Richard, T. ,  LINDSLEY, Craig, W. ,  NAYLOR, Elizabeth ,  STREET, Leslie, J. ,  WANG, Yi ,  WISNOSKI, David, D. ,  WOLKENBERG, Scott, E. ,  ZHAO, Zhijian

IPC分类号： A61K31/445 ,  A61K31/505 ,  A61K31/535 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

CPC分类号： C07D409/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

摘要： The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

公开(公告)号：EP1725575A2

公开(公告)日：2006-11-29

申请号：EP05713397.7

申请日：2005-02-14

申请人： Merck and Co., Inc.

发明人： ANDERSON, Annaliesa, S. ,  MONTGOMERY, Donna, L.

IPC分类号： C07K1/00 ,  C07K2/00 ,  A61K39/02 ,  A61K39/00 ,  A61K39/085 ,  A61K39/09

CPC分类号： A61K39/085 ,  A61K39/00 ,  C07K14/31

摘要： The present invention features polypeptides comprising an amino acid sequence structurally related to SEQ ID NO: 1 and uses of such polypeptides. SEQ ID NO: 1 is a truncated derivative of a full length S. aureus polypeptide. The full-length polypeptide is referred to herein as full-length “sai-1”. A His-tagged derivative of SEQ ID NO: 1 was found to produce a protective immune response against S. aureus.

公开(公告)号：EP2150115A1

公开(公告)日：2010-02-10

申请号：EP08754538.0

申请日：2008-05-19

申请人： Merck and Co., Inc.

发明人： COLEMAN, Paul, J. ,  MERCER, Swati, P. ,  ROECKER, Anthony, J.

IPC分类号： A01N43/82 ,  A01N43/78 ,  A61K31/41

CPC分类号： C07D417/14 ,  A61K31/401 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/41 ,  C07D403/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D473/36 ,  C07D498/04

摘要： The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲肽受体拮抗剂的环丙基脯氨酸二酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲素受体的这些疾病中的用途。