公开(公告)号：US20120108602A1

公开(公告)日：2012-05-03

申请号：US13101926

申请日：2011-05-05

申请人： Udo Andreas BAUER ,  Jonas Gunnar BARLIND ,  Petra JOHANNESSON ,  Jan Magnus JOHANSSON ,  Alexander Tobias NOESKE ,  Annika Ulrika PETERSSON ,  Alan Martin BIRCH ,  Roger John BUTLIN ,  Clive GREEN ,  Andrew LEACH ,  Ragnar HOVLAND

发明人： Udo Andreas BAUER ,  Jonas Gunnar BARLIND ,  Petra JOHANNESSON ,  Jan Magnus JOHANSSON ,  Alexander Tobias NOESKE ,  Annika Ulrika PETERSSON ,  Alan Martin BIRCH ,  Roger John BUTLIN ,  Clive GREEN ,  Andrew LEACH ,  Ragnar HOVLAND

IPC分类号： A61K31/4965 ,  C07D401/04 ,  A61K31/497 ,  A61P3/10 ,  A61K31/4425 ,  C07D213/81 ,  A61K31/4418 ,  C07D403/10 ,  C07D241/24 ,  C07D213/89

CPC分类号： C07D213/81 ,  C07D213/82 ,  C07D241/24 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10

摘要： DGAT-1 inhibitor compounds of formula (1), 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, Ring A is optionally substituted 2,6-pyrazindiyl; X is ═0; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or —O—; Y2 is —(CH2)r— wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.

摘要翻译： 与药物组合物一起描述式（1）的DGAT-1抑制剂化合物，其药学上可接受的盐和前药与制备它们的方法及其用于治疗例如肥胖症的用途，其中例如环A为 任选取代的2,6-吡嗪二基; X为═0; 环B为任选取代的1,4-亚苯基; Y1是直接键或-O-键; Y2是 - （CH2）r-，其中r是2或3; 当Y 1是环B和环C之间的直接键，当环B是1,4-亚苯基且环C是（4-6C）环烷烃时，n是0或n是1; 环C是任选取代的（4-6C）环烷烃，（7-10C）双环烷烃，（8-12C）三环烷烃，亚苯基或辛基二辛基; L是直接键或-O-键; p为0,1或2，当p为1或2时，RA1和RA2各自独立地为氢或（1-4C）烷基; Z是羧基或其模拟物或生物电子等排体。