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МОДУЛЯТОРИ ROR-ГAMMA (RORγ)
专利权人:
LEAD PHARMA HOLDING B.V.
发明人:
Cals, Joseph Maria Gerardus Barbara,Nabuurs, Sander Bernardus
申请号:
UAA201607189
公开号:
UA117941C2
申请日:
2014.12.03
申请国别(地区):
UA
年份:
2018
代理人:
摘要:
The present invention relates to compounds according to Formula I: Wherein: A11-A14 are N or CR11, CR12, CR13, CR14, respectively, with the proviso that no more than two of the four positions A can be simultaneously N; R1 is C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, (di)C(1-6)alkylamino, (di)C(3-6)cycloalkylamino or (di)(C(3-6)cycloalkylC(l-3)alkyl)amino, with all carbon atoms of alkyl groups optionally substituted with one or more F and all carbon atoms of cycloalkyl groups optionally substituted with one or more F or methyl; R2 and R3 are independently H, F, methyl, ethyl, hydroxy, methoxy or R2 and R3 together is carbonyl, all alkyl groups, if present, optionally being substituted with one or more F; R4 is Η or C(l-6)alkyl; R5 is H, hydroxyethyl, methoxyethyl, C(l-6)alkyl, C(6-10)aryl, C(6-10)arylC(l-3)alkyl, C(l-9)heteroaryl, C(l-9)heteroarylC(l-3)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(l-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(l-3)alkyl, all groups optionally substituted with one or more F, CI, C(l-2)alkyl, C(l-2)alkoxy or cyano; the sulfonyl group with R1 is represented by one of R7, R8 or R9; the remaining R6-RH are independently H, halogen, C(l-3)alkoxy, (di)C(l-3)alkylamino or C(l-6)alkyl, all of the alkyl groups optionally being substituted with one or more F; and Ri5 and Ri6 are independently H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(l-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(l-3)alkyl, C(2-5)het-erocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl, all groups optionally substituted with one or more F, CI, C(1-2)alkyl, C(1-2)alkoxy or cyano. The compounds can be used as inhibitors of RORy and are useful for the treatment of RORy mediated diseases.Даний винахід стосується сполук формули І Мета або параФормула І,де А11-А14 являють собою N або CR11, CR12, CR13, CR14, відповідно, за умови, що не більше ніж в двох положеннях з чотирьох А можуть одночасно являти собою N; R1
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