BERTHEL STEVEN JOSEPH,BILLEDEAU ROLAND J.,BROTHERTON-PLEISS CHRISTINE E.,FIROOZNIA FARIBORZ,GABRIEL STEPHEN DEEMS,HAN XIAOCHUN,HILGENKAMP RAMONA,JAIME-FIGUEROA SAUL,KOCER BRULENT,LOPEZ-TAPIA FRANCISCO
申请号：
ARP110102870
公开号：
AR082590A1
申请日:
2011.08.08
申请国别(地区):
AR
年份:
2012
代理人:
摘要：
These compounds help regulate Btk activity and treat diseases related to Btk overactivity. These compounds also contribute to the treatment of inflammatory and autoimmune diseases, such as rheumatoid arthritis, associated with the abnormal spread of B cells. The composition 1: formula (1) compound containing formula (1) compound and at least one vehicle, diluent or precursor compound is also described,in which - - - - - is a single link or a double link； X is CH, CH2 or N； R is H, -R1, -R1-R2-R3, -R1-R3 or -R2-R3； R1 is aryl, heteroaryl, bicyclic heteroaryl, cycloalkyl or heterocycloalkyl, each of which is optionally substituted by one or more lower alkyl, hydroxy, hydroxyalkyl lower, lower alkoxy, halogen, nitro, amino, amido, cyano, oxo or lower haloalkyl； R2 is -C (= O),-C (= O) or C (= O) NR2 RSQE；,-NHC (= O) O, -C (R2) 2, -O, -S, -C (= NH) NR2 or -S (= O) 2； each R2 is independently H or lower alkyl； R3 is H or R4； R4 is lower alkyl, lower haloalkyl, lower alkoxy, amino, (lower alkyl) -amino, cycloalkylamino, di (lower alkyl) -amino, aryl, arylalkyl, alkylaryl, heteroaryl, alkyl-heteroaryl, heteroaryl-alkyl, cycloalkyl, alkyl- cycloalkyl, cycloalkyl-alkyl, heterocycloalkyl, alkyl-heterocycloalkyl, heterocycloalkyl-alkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, spirocycloalkyl, spiroheterocycloalkyl, or bicyclic spiroheterocycloalkyl,Each of these substances can be replaced by one or more lower tar, halogen (lower tar) - amino, di (lower tar) - amino, hydroxy, lower hydroxide, lower alkane, halogen, nitrogen, amino, acylamine, acylamine, acid, cyanogen, oxo, sulfur, sulfosalkylhydrazide, lower tar, guandino, hydroxyamino, carboxi. Carbamate, carbamate, low halo propyl ester, isocyclopropyl or low haloalkyl； two groups of lower asphalt can form a ring when they are combined； Y4 is y4a, y4b, y4c or y4d； y4a is h or halogen； y4b is lower asphalt, which can be replaced by one or more substitutes selected from the lower halogenated coke oil and halogen grou
