公开(公告)号：EP3526196A1

公开(公告)日：2019-08-21

申请号：EP17860988.9

申请日：2017-10-09

申请人： Merck Sharp & Dohme Corp.

发明人： RUDD, Michael, T. ,  MENG, Zhaoyang ,  WAI, Jenny ,  BENNETT, David Jonathan ,  BRNARDIC, Edward, J. ,  LIVERTON, Nigel, J. ,  STACHEL, Shawn, J. ,  HAN, Yongxin ,  TEMPEST, Paul ,  ZHU, Jiuxiang ,  XU, Xuewang ,  ZHU, Bin

IPC分类号： C07D211/08 ,  C07D211/14 ,  C07D401/02

公开(公告)号：EP2945632B1

公开(公告)日：2018-03-07

申请号：EP13866588.0

申请日：2013-12-20

申请人： Merck Sharp & Dohme Corp.

发明人： ALI, Amjad ,  LO, Michael Man-Chu ,  LIM, Yeon-Hee ,  STAMFORD, Andrew ,  KUANG, Rongze ,  TEMPEST, Paul ,  YU, Younong ,  HUANG, Xianhai ,  HENDERSON, Timothy, J. ,  KIM, Jae-Hun ,  BOYCE, Christopher ,  TING, Pauline ,  ZHENG, Junying ,  METZGER, Edward ,  ZORN, Nicolas ,  XIAO, Dong ,  GALLO, Gioconda, V. ,  WON, Walter ,  WU, Heping ,  DENG, Qiaolin

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/519 ,  A61P25/16

CPC分类号： C07D519/00 ,  C07D487/04

摘要： where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

公开(公告)号：EP2938344A1

公开(公告)日：2015-11-04

申请号：EP13867977.4

申请日：2013-12-20

申请人： Merck Sharp & Dohme Corp.

发明人： ALI, Amjad ,  LO, Michael Man-Chu ,  LIM, Yeon-Hee ,  STAMFORD, Andrew ,  KUANG, Rongze ,  TEMPEST, Paul ,  YU, Younong ,  BERLIN, Michael ,  TING, Pauline ,  ZHOU, Gang ,  YU, Tao ,  BOYCE, Christopher ,  KELLY, Joseph Michael ,  TAGAT, Jayaram, R. ,  ZHENG, Junying ,  HUANG, Xianhai ,  ZHOU, Wei ,  KIM, Jae-Hun ,  ZORN, Nicolas ,  XIAO, Dong ,  GALLO, Gioconda, V. ,  WON, Walter ,  WU, Heping ,  ANAND, Rajan ,  DENG, Qiaolin

IPC分类号： A61K31/4985 ,  A61K31/519

CPC分类号： C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

摘要： Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

摘要翻译： 公开了式A化合物：（结构上表示）其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

公开(公告)号：EP2032141B1

公开(公告)日：2012-10-31

申请号：EP07795763.7

申请日：2007-06-05

申请人： Merck Sharp & Dohme Corp.

发明人： YOUNG, Jonathan, R. ,  HAIDLE, Andrew ,  TEMPEST, Paul ,  MACHACEK, Michelle

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P35/02

CPC分类号： C07D471/04

公开(公告)号：EP2205070A1

公开(公告)日：2010-07-14

申请号：EP08836352.8

申请日：2008-09-30

申请人： Merck Sharp & Dohme Corp.

发明人： KATTAR, Solomon ,  MILLER, Thomas, A. ,  OTTE, Karin, M. ,  SILIPHAIVANH, Phieng ,  SURDI, Laura ,  TEMPEST, Paul ,  ZABIEREK, Anna, A.

IPC分类号： A01N37/18 ,  A61K31/16

CPC分类号： C07D319/18 ,  C07C259/10 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/323 ,  C07D207/335 ,  C07D213/40 ,  C07D231/56 ,  C07D233/61 ,  C07D261/08 ,  C07D265/30 ,  C07D277/28 ,  C07D307/14 ,  C07D307/52 ,  C07D307/81 ,  C07D409/04 ,  C07D417/04 ,  C07D471/04

摘要： The present invention relates to a novel class of N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can be used to treat cancer. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives in vivo.

公开(公告)号：EP2166846A1

公开(公告)日：2010-03-31

申请号：EP08768504.6

申请日：2008-06-16

申请人： Merck Sharp & Dohme Corp.

发明人： ALTMAN, Michael ,  CHRISTOPHER, Matthew ,  GRIMM, Jonathan, B. ,  HAIDLE, Andrew ,  KONRAD, Kaleen ,  LIM, Jongwon ,  MACCOSS, Rachel, N. ,  MACHACEK, Michelle ,  OSIMBONI, Ekundayo ,  OTTE, Ryan, D. ,  SIU, Tony ,  SPENCER, Kerrie ,  TAOKA, Brandon ,  TEMPEST, Paul ,  WILSON, Kevin ,  WOO, Hyun Chong ,  YOUNG, Jonathan ,  ZABIEREK, Anna

IPC分类号： A01N43/06 ,  A61K31/38 ,  A61K31/535

CPC分类号： C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/10 ,  C07F9/65586 ,  C07F9/65685

摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.