MORTENSEN, DEBORAH SUE,MEDEROS, MARIA MERCEDES DELGADO,SAPIENZA, JOHN JOSEPH,ALBERS, RONALD J.,LEE, BRANDEN G.,HUANG, DEHUA,SCHWARZ, KIMBERLY LYN,PARNES, JASON SIMON,RIGGS, JENNIFER R.,PAPA, PATRICK W
申请号:
ES07861468
公开号:
ES2383370T3
申请日:
2007.10.18
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound having the following formula: and its pharmaceutically acceptable salts, wherein: R 1 is substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl or substituted or unsubstituted heterocycloalkyl .-XABY- together form -N (R2) CH2C (O) NH-, -N (R2) C (O) CH2NH-, -N (R2) C (O) NH -, - N (R2) CH>; = N-, or -C (R2)>; = CHNH-; L is a direct bond, NH or O; R2 is C1-8 substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl substituted or substituted or unsubstituted heterocycloalkyl; and R3 and R4 are independently H or C1-8 alkyl, where the groups that are substituted are substituted with one or more halogens; C 1-8 alkyl; C 2-8 alkenyl; C2-8 alkynyl; hydroxyl; C1-8 alkoxy; Not me; nitro; thiol; thioether; imine; cyano; amido; phosphonate; phosphine; carboxyl; thiocarbonyl; sulfonyl; sulfonamide; ketone; aldehyde; ester; carbonyl; haloalkyl; B (OH) 2; carbocyclic cycloalkyl, heterocycloalkyl, aryl or monocyclic or fused or polycyclic heteroaryl not fused; amino; O-lower alkyl; O-aryl, aryl; aryl-lower alkyl; CO2CH3; CONH2; OCH2CONH2; NH2; SO2NH2; OCHF2; CF3; or OCF3 groups, where each of these groups is optionally substituted, where aryl denotes an unsaturated aromatic carbocyclic group of 6 to 14 carbon atoms having a single ring or multiple condensed rings; heteroaryl denotes an aryl ring system that has one four heteroatoms selected from O, S and N as ring atoms where the rest of the ring atoms are carbon atoms; cycloalkyl denotes a saturated or unsaturated unsaturated carbocyclic ring; and heterocycloalkyl denotes a non-aromatic cycloalkyl where one to four of the ring carbon atoms are independently replaced with a heteroatom selected from O, S and N; with the proviso that R2 is not a substituted or unsubstituted furanoside and that the compound other than 8,9-