[EN] CARBAMOYL COMPOUNDS AS DGAT1 INHIBITORS 190<br/>[FR] COMPOSÉS CARBAMOYLES COMME INHIBITEURS DE DGAT1 190
申请人:ASTRAZENECA AB
公开号:WO2009081195A1
公开(公告)日:2009-07-02
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, Ring A is optionally substituted 2,6-pyrazindiyl; X is =O; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or -O-; Y2 is -(CH 2) 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.
DGAT-1抑制剂化合物公式(I),药用可接受的盐和前药,以及药物组合物、制造它们的过程以及它们在治疗例如肥胖症中的用途,其中,例如,环A是可选取代的2,6-吡嗪二基;X是=O;环B是可选取代的1,4-苯基;Y1是直接键或-O-;Y2是-(CH2)r-,其中r是2或3;n是0或当Y1是环B和环C之间的直接键并且当环B是1,4-苯基和环C是(4-6C)环烷时,n是1;环C是可选取代的(4-6C)环烷、(7-10C)双环烷、(8-12C)三环烷、苯基或吡啶二基;L是直接键或-O-;p是0、1或2,并且当p是1或2时,RA1和RA2各自独立地为氢或(1-4C)烷基;Z是羧酸或其模拟物或生物等排体。