公开(公告)号：EP2744331A1

公开(公告)日：2014-06-25

申请号：EP12825726.8

申请日：2012-08-16

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

发明人： YASUDA, Nobuyoshi ,  KUETHE, Jeffrey,T. ,  HUMPHREY, Guy ,  BEUTNER, Gregory, L. ,  ZHONG, Yong-Li ,  CLEATOR, Edward ,  BAXTER, Carl

IPC分类号： A01N43/04 ,  A61K31/70 ,  A01N43/42 ,  A61K31/44

CPC分类号： C07C35/04 ,  A61K38/00 ,  C07C67/14 ,  C07C69/013 ,  C07C69/12 ,  C07C269/04 ,  C07C271/34 ,  C07D403/12 ,  C07D498/16 ,  C07K5/0808 ,  C07K5/126

摘要： The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applica

公开(公告)号：EP2635265A2

公开(公告)日：2013-09-11

申请号：EP11838596.2

申请日：2011-10-31

申请人： Merck Sharp & Dohme Corp.

发明人： STANTON, Matthew, G. ,  BEUTNER, Gregory, L.

IPC分类号： A61K9/50 ,  A61K9/127 ,  A61K31/41

CPC分类号： C12N15/1137 ,  A61K9/5123 ,  C07D207/12 ,  C07D211/40 ,  C07D223/08 ,  C12N15/113 ,  C12N2310/14 ,  C12N2320/32

摘要： The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

公开(公告)号：EP2605772A2

公开(公告)日：2013-06-26

申请号：EP11818552.9

申请日：2011-08-08

申请人： Merck Sharp & Dohme Corp.

发明人： LIMANTO, John ,  BEUTNER, Gregory, L. ,  YIN, Jingjun ,  KLAPARS, Artis ,  ASHLEY, Eric, R. ,  STROTMAN, Hallena, R. ,  TRUPPO, Matthew, D. ,  CHUNG, Cheol, K. ,  HUGHES, Gregory ,  LIU, Zhijian ,  GRAU, Brendan ,  JANEY, Jacob

IPC分类号： A61K31/275

CPC分类号： C07D207/12 ,  C07C217/52 ,  C07D207/416 ,  C12P17/10

摘要： The present invention relates to a process for preparing aminocyclohexyl ether compounds of Formula I: or the pharmaceutically acceptable salts and esters thereof. In particular, the instant invention is directed towards a process for preparing (1R,2R)-2-[(3R)-Hydroxypyrrolidinyl]-1-(3,4-dimethoxyphenethoxy)-cyclohexane as well as various intermediates.