LEAD PHARMA CEL MODELS IP B.V.;ЛИД ФАРМА СЕЛ МОДЕЛЗ АйПи Б.В.
发明人:
Joseph, Maria, Gerardus, Barbara,Йосеф Мария Герардус Барбара,Sander, Bernardus,Сандер Бернардус
申请号：
EA201691173
公开号：
EA030393B1
申请日:
2014.12.03
申请国别(地区):
EA
年份:
2018
代理人:
摘要：
The present invention relates to compounds according to Formula Iwherein 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 C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, di-C1-6alkylamino, di-C3-6cycloalkylamino or di-(C3-6cycloalkylC1-3alkyl)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 are carbonyl, all alkyl groups, if present, optionally being substituted with one or more F； R4 is H or C1-6alkyl； R5 is H, hydroxyethyl, methoxyethyl, C1-6alkyl, C6-10aryl, C6-10arylC1-3alkyl, C1-9heteroaryl, C1-9heteroarylC1-3alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, C2-5heterocycloalkyl or C2-5heterocycloalkylC1-3alkyl, all groups optionally substituted with one or more substituents selected from F, Cl, C1-2alkyl, C1-2alkoxy or cyano； the sulfonyl group with R1 is represented by one of R7, R8 or R9； the remaining R6-R14 are independently H, halogen, C1-3alkoxy, di-C1-3alkylamino or C1-6alkyl, all of the alkyl groups optionally being substituted with one or more F； and R15 and R16 are independently H, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, C6-10aryl, C6-10arylC1-3alkyl, C1-9heteroaryl, C1-9heteroarylC1-3alkyl, C2-5heterocycloalkyl or C2-5heterocycloalkylC1-3alkyl, all groups optionally substituted with one or more substituents selected from F, Cl, C1-2alkyl, C1-2alkoxy or cyano. The compounds can be used as inhibitors of RORγ and are useful for the treatment of RORγ mediated diseases.Изобретение относится к соединениям формулы Iгде A11-A14 представляют собой N или CR11, CR12, CR13, CR14 соответственно при условии, что не более чем в двух положениях из четырех A могут одновременно представлять собой N； R1 представляет собой C1-6алкил, C3-6ци
