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Modulators of glucocorticoid receptor activity, AP-1 and / or NF-kappaB and their use
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
YANG, BINGWEI VERA,DOWEYKO, LIDIA M.
申请号:
ES07863677
公开号:
ES2382913T3
申请日:
2007.10.31
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound according to formula (Ia), or an enantiomer, diastereomer or a pharmaceutically salt thereof, wherein: A is thienyl, thiazolyl, isothiazolyl, thiadiazolyl, furanyl, pyrrolyl, pyrazolyl, pyridyl or pyrimidinyl, each group optionally substituted with 1 to 4 groups, R1, R2, R3 and / or R4; Z is selected from Rm and Rn, at each occurrence, they are independently selected from (i) hydrogen, halogen, cycloalkyl, cyano, haloalkyl, thioalkyl, -CO2R23, -NR23R24, -C (= O) R23, -C (O) N (R23) (R24), OR23, C1-4 alkyl, substituted C1-4 alkyl, aryl, heteroaryl and heterocycle; or (ii) Rm and Rn, together with the atoms to which they are attached, combine to form a cycloalkyl, aryl, heteroaryl or heterocyclyl ring, condensed from 5 to 7 members; R1, R2, R3, R4, R1a, R2a, R3a, and R4a are independently selected from (i) hydrogen, halogen, C1-4 alkyl, CN, C2-4 alkenyl, C2-4 alkynyl, SR10, SO2R12, OR10, SOpNR10R11 and NR10R11; and / or (ii) C0-3 alkylene substituted with an optionally substituted group, selected from phenyl and a 5-7 membered heterocycle or heteroaryl; R6 is selected from C1-4 alkyl, substituted C1-4 alkyl, cyano and C3-7 cycloalkyl; R7 is selected from hydrogen, C1-4 alkyl, substituted C1-4 alkyl, nitro, cyano, hydroxy, C1-4 alkoxy and C3-7 cycloalkyl; or R6 and R7 are taken together with the carbon to which they are attached to form a C3-7 cycloalkyl group; R10 and R11, at each occurrence, are independently selected from (i) hydrogen, C1-6 alkyl, substituted C1-6 alkyl and -SO2 (C1-4 alkyl); and / or (ii) C3-7 cycloalkyl, heterocycle, aryl and heteroaryl, each is an optionally substituted group; and / or (iii) R10 is taken together with R11 and the nitrogen atom to which both are attached to form a 4- to 6-membered heteroaryl or heterocycle, each group is optionally substituted; R12, at each occurrence, is independently selected from an optionally substituted group selected from C1-6 alkyl, C3-7 cycloalkyl, heterocycle, aryl and heteroaryl; and R23 and R
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