公开(公告)号：EP2211619A1

公开(公告)日：2010-08-04

申请号：EP08839447.3

申请日：2008-10-14

申请人： Merck Sharp & Dohme Corp.

发明人： WU, Zhicai ,  HARTNETT, John, C.

IPC分类号： A01N43/82

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

摘要： The present invention relates to compounds represented by Formula (I), Formula (II) and Formula (III) and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.

公开(公告)号：EP2203171A2

公开(公告)日：2010-07-07

申请号：EP08795420.2

申请日：2008-08-18

申请人： Merck Sharp & Dohme Corp.

发明人： WU, Zhicai ,  GREEN, Ahren, I. ,  HARTNETT, John, C.

IPC分类号： A61K31/519

CPC分类号： C07D471/04

摘要： The present invention relates to compounds represented by Formula (I) and Formula (II): or pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.

公开(公告)号：EP2485737B1

公开(公告)日：2014-06-25

申请号：EP10822433.8

申请日：2010-09-28

申请人： Merck Sharp & Dohme Corp.

发明人： BILODEAU, Mark, T. ,  EGBERTSON, Melissa ,  GREEN, Ahren ,  LI, Yiwei ,  HARTNETT, John, C.

IPC分类号： A61K31/555 ,  C07C255/58 ,  C07D215/44 ,  C07D215/38 ,  C07D311/74 ,  C07D311/76 ,  C07D405/04 ,  C07D405/06 ,  C07C215/44

CPC分类号： C07C215/20 ,  A61K31/133 ,  C07C25/02 ,  C07C211/34 ,  C07C215/44 ,  C07C255/58 ,  C07C2602/10 ,  C07D215/38 ,  C07D215/44 ,  C07D311/74 ,  C07D311/76 ,  C07D405/04 ,  C07D405/06

公开(公告)号：EP2485737A1

公开(公告)日：2012-08-15

申请号：EP10822433.8

申请日：2010-09-28

申请人： Merck Sharp & Dohme Corp.

发明人： BILODEAU, Mark, T. ,  EGBERTSON, Melissa ,  GREEN, Ahren ,  LI, Yiwei ,  HARTNETT, John, C.

IPC分类号： A61K31/555

CPC分类号： C07C215/20 ,  A61K31/133 ,  C07C25/02 ,  C07C211/34 ,  C07C215/44 ,  C07C255/58 ,  C07C2602/10 ,  C07D215/38 ,  C07D215/44 ,  C07D311/74 ,  C07D311/76 ,  C07D405/04 ,  C07D405/06

摘要： The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.

公开(公告)号：EP2365749A1

公开(公告)日：2011-09-21

申请号：EP09826566.3

申请日：2009-11-03

申请人： Merck Sharp & Dohme Corp.

发明人： BARROW, James, C. ,  BILODEAU, Mark, T. ,  COX, Christopher, D. ,  HARTNETT, John, C. ,  KETT, Nathan, R. ,  LI, Yiwei ,  MANLEY, Peter ,  MELAMED, Jeffrey ,  SHIPE, William, D. ,  TROTTER, B. Wesley ,  ZARTMAN, Amy, E.

IPC分类号： A01N43/42 ,  A61K31/47

CPC分类号： A61K31/47 ,  C07D401/12 ,  C07D405/12

摘要： The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is 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 the neuropeptide S receptor is involved.

公开(公告)号：EP1622616B1

公开(公告)日：2011-06-15

申请号：EP04760294.1

申请日：2004-04-20

申请人： Merck Sharp & Dohme Corp.

发明人： BILODEAU, Mark, T. ,  DUGGAN, Mark, E. ,  HARTNETT, John, C. ,  LINDSLEY, Craig, W. ,  WU, Zhicai ,  ZHAO, Zhijian

IPC分类号： C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  A61P35/00 ,  C07D401/14

CPC分类号： C07F9/65583 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

摘要： The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.