公开(公告)号：EP3359194A2

公开(公告)日：2018-08-15

申请号：EP16854112.6

申请日：2016-09-30

申请人： Merck Sharp & Dohme Corp. ,  Ambrx, Inc.

发明人： BRANDISH, Philip, E. ,  GARBACCIO, Robert, M. ,  KERN, Jeffrey ,  LIANG, Linda ,  SHAH, Sanjiv ,  ZALLER, Dennis ,  BECK, Andrew ,  GATELY, Dennis ,  KNUDSEN, Nick ,  MANIBUSAN, Anthony ,  WANG, Jianing ,  SUN, Ying

IPC分类号： A61K39/44 ,  C07K17/06 ,  A61K47/24 ,  A61K39/395

CPC分类号： C07K16/2833 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6889 ,  C07K16/2866 ,  C07K16/2875

摘要： Antibody drug conjugates (ADCs) comprising an antibody conjugated to an anti-inflammatory therapeutic agent via a phosphate-based linker with tunable extracellular and intracellular stability are described.

公开(公告)号：EP3359191A1

公开(公告)日：2018-08-15

申请号：EP16854155.5

申请日：2016-10-04

申请人： Merck Sharp & Dohme Corp. ,  Ambrx, Inc.

发明人： GARBACCIO, Robert, M. ,  CARRINGTON, Paul, E. ,  SEGHEZZI, Wolfgang ,  ERMAKOV, Grigori ,  BIANCHI, Elisabetta ,  ORVIETO, Federica ,  KNUDSEN, Nick ,  MANIBUSAN, Anthony ,  GATELY, Dennis

IPC分类号： A61K39/395 ,  C07K16/08 ,  C07K16/10 ,  C07K19/00 ,  C07K14/605 ,  C07K14/575 ,  A61P3/10 ,  A61P3/08

CPC分类号： C07K14/605 ,  A61K47/6811 ,  A61K47/6843 ,  A61K2039/505 ,  C07K16/26 ,  C07K16/2869 ,  C07K2317/75 ,  C07K2319/00

摘要： Described are antibody peptide conjugates (APCs) comprising an antibody conjugated to a peptide analog of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have agonist activity at the glucagon (GCG) receptor and the glucagon-like peptide 1 (GLP-1) receptor and the use of such APCs for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

公开(公告)号：EP2470527A1

公开(公告)日：2012-07-04

申请号：EP10810431.6

申请日：2010-08-16

申请人： Merck Sharp & Dohme Corp.

发明人： DUDKIN, Vadim, Y. ,  FRALEY, Mark, E. ,  WANG, Cheng ,  GARBACCIO, Robert, M. ,  BESHORE, Douglas, C. ,  KUDUK, Scott, D. ,  SKUDLAREK, Jason, W.

IPC分类号： C07D403/00

CPC分类号： C07D417/14 ,  A61K31/4192 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  C07D249/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D495/04 ,  C07D498/04

摘要： The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.

公开(公告)号：EP3407916A2

公开(公告)日：2018-12-05

申请号：EP17744740.6

申请日：2017-01-24

申请人： Merck Sharp & Dohme Corp.

发明人： GARBACCIO, Robert, M. ,  KERN, Jeffrey, C. ,  MULHEARN, James, J. ,  BRANDISH, Philip, E.

IPC分类号： A61K47/00 ,  A61K47/06 ,  A61K47/24

CPC分类号： A61K47/6849 ,  A61K47/6803 ,  A61K47/6889

摘要： Phosphonate linkers and their use for delivering compounds with passive cell permeability into a cell wherein the phosphonate group facilitateS cellular retention of the compound are described.

公开(公告)号：EP2640400A1

公开(公告)日：2013-09-25

申请号：EP11841433.3

申请日：2011-11-16

申请人： Merck Sharp & Dohme Corp.

发明人： BARRETT, Stephanie, E. ,  BUSUEK, Marina ,  COLLETTI, Steven, L. ,  GARBACCIO, Robert, M. ,  GUIDRY, Erin, N. ,  KOWTONIUK, Robert, A. ,  LIAO, Jing ,  PARISH, Craig, A. ,  PARMAR, Rubina, G. ,  PEI, Tao ,  SCHLOSSER, Kevin, M. ,  TELLERS, David, M. ,  TOBIAS, Sandra, C. ,  THUONG, Quang, T. ,  WALDMAN, Jacob, H. ,  WANG, Weimin ,  WILLIAMS, J. Michael

IPC分类号： A61K31/7088

CPC分类号： A61K47/48092 ,  A61K47/549 ,  C08G69/10 ,  C08G73/028 ,  C08L79/02

摘要： The present invention provides poly(amide) polymers, polyconjugates, compositions and methods for the delivery of oligonucleotides for therapeutic purposes.

公开(公告)号：EP2291078A1

公开(公告)日：2011-03-09

申请号：EP09747248.4

申请日：2009-05-08

申请人： Merck Sharp & Dohme Corp.

发明人： BRNARDIC, Edward, J. ,  CONVERSO, Antonella ,  FRALEY, Mark, E. ,  GARBACCIO, Robert, M. ,  HUANG, Shaei, Y.

IPC分类号： A01N43/50 ,  A01N43/76 ,  A61K31/42

CPC分类号： C07D498/04

摘要： The present invention is directed to oxazolobenzimidazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.

摘要翻译： 本发明涉及作为代谢型谷氨酸受体增效剂的恶唑并苯并咪唑衍生物，特别是mGluR2受体，其可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及涉及代谢型谷氨酸受体的疾病。 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代谢型谷氨酸受体的疾病中的用途。

公开(公告)号：EP2257161A1

公开(公告)日：2010-12-08

申请号：EP09714617.9

申请日：2009-02-18

申请人： Merck Sharp & Dohme Corp.

发明人： GARBACCIO, Robert, M. ,  CONVERSO, Antonella ,  FRALEY, Mark, E. ,  HARTINGH, Timothy, J.

IPC分类号： A01N43/00 ,  A61K31/495

CPC分类号： C07D487/04

摘要： The present invention is directed to AHCY inhibitors of formula (I) which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels.

公开(公告)号：EP2257161B1

公开(公告)日：2012-04-25

申请号：EP09714617.9

申请日：2009-02-18

申请人： Merck Sharp & Dohme Corp.

发明人： GARBACCIO, Robert, M. ,  CONVERSO, Antonella ,  FRALEY, Mark, E. ,  HARTINGH, Timothy, J.

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： The present invention is directed to AHCY inhibitors of formula (I) which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels.

公开(公告)号：EP2279532A2

公开(公告)日：2011-02-02

申请号：EP09747251.8

申请日：2009-05-08

申请人： Merck Sharp & Dohme Corp.

发明人： BRNARDIC, Edward, J. ,  FRALEY, Mark, E. ,  GARBACCIO, Robert, M.

IPC分类号： H01L31/06

CPC分类号： C07D498/04

摘要： The present invention is directed to oxazolobenzimidazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.

公开(公告)号：EP1765830B1

公开(公告)日：2010-09-22

申请号：EP05786157.7

申请日：2005-06-27

申请人： Merck Sharp & Dohme Corp.

发明人： BERGMAN, Jeffrey, M. ,  COLEMAN, Paul, J. ,  FRALEY, Mark, E. ,  GARBACCIO, Robert, M. ,  HARTMAN, George, D. ,  LI, Chunze ,  NEILSON, Lou Anne ,  OLSON, Christy, M. ,  TASBER, Edward, S.

IPC分类号： C07D498/04 ,  C07D519/00 ,  A61K31/5383 ,  A61P35/00

CPC分类号： C07D498/04 ,  C07D519/00

摘要： The present invention relates to tricyclic pyrazoles according to Formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

摘要翻译： 本发明涉及根据式（I）的三环吡唑，其可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。