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Heterocyclic glucocorticoid receptor modulators, AP-1 activity and / or NFKB activity, and use thereof
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
YANG, BINGWEI
申请号:
ES06718214
公开号:
ES2381278T3
申请日:
2006.01.13
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound having the structure: (i) (ii) or one of its stereoisomers of (i) or one of its tautomers of (i) or a pharmaceutically acceptable salt of (i), in which: R is hydrogen , NHR6, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, aryl, arylalkyl, aryloxy, heteroaryl, cycloheteroalkyl, heteroarylalkyl, cycloheteroalkylalkyl, cycloalkyl, cycloalkylalkyl, cyanoalkyl, aminoalkyl, hydroxyalkyl, aryloxyalkyl; R2 is selected from: R4 is selected from cyano, nitro, CH2NH2, CHO, COOH, CO2alkyl, OCORe, OCOtRf, CONReRf and NRg-COtR¡; R6 is hydrogen, S (O) tRh or C (O) tRh; Ra and Rb are independently hydrogen, methyl, bromine, chlorine, nitro or cyano; Re and Rf are independently selected at each occurrence from hydrogen, aryl, alkyl, alkenyl, alkynyl, alkoxy, amino, substituted amino, alkoxyalkyl, alkylaminoalkyl, dialkylaminoalkyl, heteroaryl, cycloheteroalkyl, heteroarylalkyl, cycloheteroalkylalkyl, cycloalkyl and cycloalkylalkyl, Re and Rf are not both alkoxy or amino; or Re and Rf, at each occurrence, can be taken together with the nitrogen to which they are attached to form a 5, 6 or 7-membered heteroaryl or cycloheteroalkyl ring containing 1, 2 or 3 heteroatoms that can be N, O or S ; Rg, Rh and R¡ are independently selected from hydrogen, aryl, alkyl, alkenyl, alkynyl, alkoxy, amino, substituted amino, alkoxyalkyl, alkylaminoalkyl, dialkylaminoalkyl, heteroaryl, cycloheteroalkyl, heteroarylalkyl, cycloheteroalkylalkyl, and cycloalkyl; Rm is selected from hydrogen, CO2alkyl, naphthyl, quinolinyl or -C (R7) (R8) -T, in which the naphthyl or quinolinyl group is substituted with one or more substituents selected from the group consisting of hydrogen, amino, hydroxyl, C1-4 alkyl, C1-4 alkoxy, C1-4 alkyl substituted with perfluoro, cyano, nitro and halogen; Rn is hydrogen, bromine or chlorine; T is a cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl or heteroaryl ring in which each ring is substituted with 0-4 R9 and 0-1 R10; R7 and R8 are independently at each occurrence hydro
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来源网址:
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