公开(公告)号：EP2349276B1

公开(公告)日：2019-11-27

申请号：EP09740569.0

申请日：2009-10-02

申请人： Merck Sharp & Dohme Corp.

发明人： ISAACS, Richard, C. A. ,  THOMPSON, Wayne, J. ,  WILLIAMS, Peter, D. ,  SU, Dai-Shi ,  VENKATRAMAN, Shankar ,  EMBREY, Mark, W. ,  FISHER, Thorsten, E. ,  WAI, John, S. ,  DUBOST, David, C. ,  BALL, Richard, G. ,  CHOI, Eric, J. ,  PEI, Tao ,  TRICE, Sarah, L. ,  CAMPBELL, Neil ,  MADDESS, Matthew ,  MALIGRES, Peter, E. ,  SHEVLIN, Michael ,  SONG, Zhiguo Jake ,  STEINHUEBEL, Dietrich, P. ,  STROTMAN, Neil, A. ,  YIN, Jingjun

IPC分类号： A61K31/553 ,  C07D487/04 ,  C07D281/10 ,  A61K31/55 ,  A61P31/18

公开(公告)号：EP2231621B1

公开(公告)日：2016-11-02

申请号：EP08869559.8

申请日：2008-12-22

申请人： Merck Sharp & Dohme Corp.

发明人： HUMPHREY, Guy, R. ,  MILLER, Ross, A. ,  MALIGRES, Peter, E. ,  WEISSMAN, Steven

IPC分类号： C07D239/52 ,  C07D413/12

CPC分类号： C07D413/12 ,  C07D239/52 ,  Y02P20/55

公开(公告)号：EP2773210A1

公开(公告)日：2014-09-10

申请号：EP12846651.3

申请日：2012-10-26

申请人： Merck Sharp & Dohme Corp.

发明人： CHUNG, Cheol ,  HUMPHREY, Guy ,  MALIGRES, Peter, E. ,  WRIGHT, Timothy, J.

IPC分类号： A01N43/76

CPC分类号： C07C41/18 ,  C07C41/30 ,  C07D263/20 ,  C07C43/23 ,  C07C43/225

摘要： An efficient process is disclosed for producing the compound of formula I, which is the CETP inhibitor anacetrapib, which raises HDL-cholesterol and reduces LDL-cholesterol in human patients and may be effective for treating or reducing the risk of developing atherosclerosis:.

摘要翻译： 公开了一种用于制备式I化合物的有效方法，其是CETP抑制剂anacetrapib，其提高人类患者中的HDL-胆固醇并降低LDL-胆固醇，并且可以有效治疗或降低发生动脉粥样硬化的风险。

公开(公告)号：EP2231621A1

公开(公告)日：2010-09-29

申请号：EP08869559.8

申请日：2008-12-22

申请人： Merck Sharp & Dohme Corp.

发明人： HUMPHREY, Guy, R. ,  MILLER, Ross, A. ,  MALIGRES, Peter, E. ,  WEISSMAN, Steven

IPC分类号： C07D239/52 ,  C07D413/12

CPC分类号： C07D413/12 ,  C07D239/52 ,  Y02P20/55

摘要： Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl- 5-hydroxy -6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)- 2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.

摘要翻译： 公开了制备某些N-芳基烷基-1-（烷基或芳烷基）-2-酰氨基烷基-5-羟基-6-氧代-1,6-二氢嘧啶-4-甲酰胺的方法。 在一个实施方案中，该方法包括酰化相应的N-芳基烷基-1-（烷基或芳烷基）-2-氨基烷基-5-酯保护的羟基-6-氧代-1,6-二氢嘧啶-4-甲酰胺中的游离胺和 然后通过碱水解将5-羟基脱保护。 该方法的羟基嘧啶酮甲酰胺产物是HTV整合酶抑制剂，其可用于治疗HIV感染，治疗AIDS或延迟AIDS的发作或进展。 也公开了可用作方法中间体的某些酯化N-芳基烷基羟基嘧啶酮甲酰胺。

公开(公告)号：EP3356332A1

公开(公告)日：2018-08-08

申请号：EP16852356.1

申请日：2016-09-26

申请人： Merck Sharp & Dohme Corp. ,  Merck Sharp & Dohme Limited

发明人： CHEN, Qinghao ,  SCOTT, Jeremy ,  KRSKA, Shane, W. ,  BAXTER, Carl ,  STEWART, Gavin William ,  TAN, Lushi ,  GIBB, Andrew ,  MALIGRES, Peter, E.

IPC分类号： C07D239/70 ,  A61K31/517 ,  A61P25/28 ,  C07D401/10

CPC分类号： C07D401/06 ,  A61K31/517

摘要： This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.

公开(公告)号：EP2349276A2

公开(公告)日：2011-08-03

申请号：EP09740569.0

申请日：2009-10-02

申请人： Merck Sharp & Dohme Corp.

发明人： ISAACS, Richard, C. A. ,  THOMPSON, Wayne, J. ,  WILLIAMS, Peter, D. ,  SU, Dai-Shi ,  VENKATRAMAN, Shankar ,  EMBREY, Mark, W. ,  FISHER, Thorsten, E. ,  WAI, John, S. ,  DUBOST, David, C. ,  BALL, Richard, G. ,  CHOI, Eric, J. ,  PEI, Tao ,  TRICE, Sarah, L. ,  CAMPBELL, Neil ,  MADDESS, Matthew ,  MALIGRES, Peter, E. ,  SHEVLIN, Michael ,  SONG, Zhiguo Jake ,  STEINHUEBEL, Dietrich, P. ,  STROTMAN, Neil, A. ,  YIN, Jingjun

IPC分类号： A61K31/553 ,  C07D487/04 ,  C07D281/10 ,  A61K31/55 ,  A61P31/18

CPC分类号： C07D498/04 ,  C07D487/04 ,  H01L2924/0002 ,  H01L2924/00

摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.

摘要翻译： 式I化合物是HIV整合酶抑制剂和HIV复制抑制剂：其中X1，X2，Y，R1A，R1B，R2和R3如本文所定义。 该化合物可用于预防或治疗HIV感染以及预防，治疗或延迟AIDS的发作或进展。 这些化合物作为化合物本身（或其水合物或溶剂合物）或以药学上可接受的盐的形式用于抗HIV感染和AIDS。 化合物及其盐可以用作药物组合物中的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 还描述了制备式I化合物及其中间体的方法。