公开(公告)号：WO2012004549A1

公开(公告)日：2012-01-12

申请号：PCT/GB2010/051106

申请日：2010-07-05

Applicant: THE UNIVERSITY OF NOTTINGHAM ,  MISTRY, Shailesh ,  DARAS, Etienne ,  FROMONT, Christophe ,  JADHAV, Gopal ,  FISCHER, Peter Martin ,  KELLAM, Barrie ,  HILL, Stephen John ,  BAKER, Jillian Glenda

Inventor： MISTRY, Shailesh ,  DARAS, Etienne ,  FROMONT, Christophe ,  JADHAV, Gopal ,  FISCHER, Peter Martin ,  KELLAM, Barrie ,  HILL, Stephen John ,  BAKER, Jillian Glenda

IPC: C07C275/40 ,  C07C275/28 ,  C07C235/34 ,  C07C335/20 ,  A61K31/16 ,  A61K31/17 ,  A61P9/04

CPC classification number: C07C217/64 ,  C07C43/23 ,  C07C213/08 ,  C07C217/34 ,  C07C231/12 ,  C07C233/40 ,  C07C233/65 ,  C07C233/78 ,  C07C235/34 ,  C07C235/50 ,  C07C235/60 ,  C07C237/04 ,  C07C237/34 ,  C07C269/06 ,  C07C271/28 ,  C07C273/1854 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C275/36 ,  C07C275/40 ,  C07C275/42 ,  C07C303/40 ,  C07C311/13 ,  C07C335/16 ,  C07C335/20 ,  C07C2601/02 ,  C07C2601/08 ,  C07D303/24

Abstract: A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z 1 is C 1 -C 4 linear or branched alkyl or alkenyl; R 4 is selected from unsubstituted and substituted C 3 -C 8 cycloalkyl, C 1 -C 8 linear or branched alkyl, C 2-5 alkenyl, C 6 -C 10 heteroaryl or aryl, or C 3 -C 8 heterocyclyl which may be part unsaturated, and combinations thereof; is linear C 2-3 alkylene,; X 1 is selected from NH and O; X 2 is selected from unsaturated C and unsaturated S; and X 3 is selected from NH and CH 2 ; or one of X 1 and X 3 is a single bond; or X 1 is O and X 2 and X 3 together are a single bond; and R 7 is selected from oxo, F, Cl, Br, CN, NH 2 , NR 9 2 , NO 2 , CF 3 , OR 9 , COR 9 , OCOR 9 , COOR 9, NR 9 COR 9 , CONR 9 2 SO 2 NR 9 2 , NR 9 SO 2 R 9 ; and R 8 is selected from C 1-5 alkyl, C 1-5 alkoxyl, C 2-5 alkenyl or alkynyl, C 6-10 ) aryl and C 3-8 cycloalkyl and combinations thereof, which may be unsubstituted or f urther substituted by one or more F, Cl, Br, CN, NH 2 , NR 3 2 , NO 2 , CF 3 ; and R 9 is selected from H and a group R 8 as hereinbefore defined; n7 and n8 and the sum thereof are independently selected from zero and the whole number integer 1 to 4; processes for the preparation thereof, compositions and uses.

Abstract translation: 式I-0的化合物及其药学上可接受的盐或盐和生理上可水解的游离形式或盐形式的衍生物：其中Z1是C1-C4直链或支链烷基或烯基; R4选自未取代和取代的C 3 -C 8环烷基，C 1 -C 8直链或支链烷基，C 2-5烯基，C 6 -C 10杂芳基或芳基，或可以是部分不饱和的C 3 -C 8杂环基，及其组合; 是直链C 2-3亚烷基; X1选自NH和O; X2选自不饱和C和不饱和S; 并且X 3选自NH和CH 2; 或者X1和X3中的一个是单键; 或X1为O，X2和X3一起为单键; 并且R 7选自氧代，F，Cl，Br，CN，NH 2，NR 9 2，NO 2，CF 3，OR 9，COR 9，OCOR 9，COOR 9，NR 9 COR 9，CONR 9 2 SO 2 NR 9 2，NR 9 SO 2 R 9; 并且R 8选自C 1-5烷基，C 1-5烷氧基，C 2-5烯基或炔基，C 6-10芳基和C 3-8环烷基及其组合，其可未被取代或被一个或多个F， Cl，Br，CN，NH 2，NR 3 2，NO 2，CF 3; 并且R 9选自H和上文定义的基团R 8; n7和n8，它们的和独立地选自零和整数1至4; 制备方法，组合物和用途。