公开(公告)号：EP2574188A1

公开(公告)日：2013-04-03

申请号：EP11783835.9

申请日：2011-05-19

申请人： Targacept, Inc. ,  AstraZeneca AB

发明人： DULL, Gary Maurice ,  GENUS, John ,  RATILAINEN, Tommi ,  RYBERG, Per Olof ,  HELLSTRÖM, Janna ,  WAHLSTRÖM, Niklas ,  WÄNNMAN, Thomas

IPC分类号： C07C29/40 ,  C07C211/21 ,  C07C231/14 ,  C07D213/65

CPC分类号： C07D213/65 ,  C07C29/36 ,  C07C211/21 ,  C07C269/04 ,  C07C33/03 ,  C07C271/12

摘要： An improved process for the preparation of aryl substituted olefinic amines such as (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine and (2S)-(4E)-N- methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine and new intermediates used in said process.

公开(公告)号：EP2443096A1

公开(公告)日：2012-04-25

申请号：EP10725494.8

申请日：2010-06-17

申请人： AstraZeneca AB

发明人： BIRCH, Alan Martin ,  BUTLIN, Roger John ,  CAMPBELL, Leonie ,  GREEN, Clive ,  LEACH, Andrew ,  MURRAY, Paul Michael ,  RYBERG, Per Olof ,  WARING, Michael James

IPC分类号： C07D241/24 ,  C07D401/12 ,  C07D413/10 ,  A61K31/4965 ,  A61K31/497 ,  A61P3/10

CPC分类号： C07D241/24 ,  C07D401/12 ,  C07D413/10

摘要： DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, r is 0 or 1 and X
1 is linear (1-3C)alkyl; q is 0 or 1 and X
1 is fluoro, chloro or (1-3C)alkyl; Y
1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y
2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y
3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or - CONHSO
2 Me or –CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is –CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.

摘要翻译： 式（I）的DGAT-1抑制剂化合物，其药学上可接受的盐和前药与药物组合物一起描述了它们的制备方法及其在治疗例如肥胖中的用途，其中例如r为0 或1并且X 1是直链（1-3C）烷基; q是0或1且X 1是氟，氯或（1-3C）烷基; Y 1选自氟，氯，溴，氰基，（1-3C）烷基和（1-2C）烷氧基; n是0,1或2且Y 2是氟，氯或（1-3C）烷基; p为0,1或2且Y 3为（1-3C）烷基或形成（3-5C）环烷基环; Z是羧基或 - CONHSO 2 Me或ΣCONRbRc，其中Rb和Rc独立地选自例如氢和（1-4C）烷基或Rb和Rc连接形成吗啉环或（4- 6C）杂环，并且当Z是“CONRbRc”时，Rb和Rc基团可以任选被羧基取代。