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RORγ調節劑
专利权人:
SANOFI;LEAD PHARMA CEL MODELS IP B. V.
发明人:
CALS, JOSEPH MARIA GERARDUS BARBARA,卡尔斯 约瑟夫 玛莉亚 杰拉德斯 芭芭拉,卡爾斯 約瑟夫 瑪莉亞 傑拉德斯 芭芭拉,DE KIMPE, VERA,德金普 薇拉,NABUURS, SANDER BERNARDUS,那布尔斯 山德 柏那德斯,那布爾斯 山德 柏那德斯,卡尔斯 约瑟夫 玛莉亚 杰拉德斯 芭芭拉,卡爾斯 約瑟夫 瑪莉亞 傑拉德斯 芭芭拉,德金普 薇拉,那布尔斯 山德 柏那德斯,那布爾斯 山德 柏那德斯
申请号:
TW105117766
公开号:
TW201718476A
申请日:
2016.06.04
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
The present invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof wherein - A1-A8 are N or CR1-CR8, respectively, with the proviso that no more than two of the four positions A in A1-A4 can be simultaneously N and that no more than two of the four positions A in A5-A8 can be simultaneously N; - R1-R8 are independently H, halogen, amino, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-6)alkyl; - R9 is C(1-6)alkyl; - R10 and R11 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R10 and R11 together is carbonyl, all alkyl groups, if present, optionally being substituted with one or more F; - R12 is H or C(1-6)alkyl; - R13 is C(3-6)cyoloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(2-5)heterocycloalkyl, C(2-5)heterocycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)hetero-aryl or C(1-9)heteroarylC(1-3)alkyl; - R14 is H, C(1-6)alkyl, C(2-6)alkenyl, C(3-6)oycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(2-5)heterocycloalkyl, C(2-5)heterocycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl or C(1-9)heteroarylC(1-3)alkyl; - or R13 and R14 are fused and form a ring having 5 to 7 atoms by joining R13 being C(1-6)alkyl or C(2-6)alkenyl with an independent substituent within the definition of R14, all groups optionally substituted with one or more halogen, amino, hydroxy, cyano, C(1-3)alkoxy, C(1-3)alkoxycarbonyl, (di)C(1-3)alkylamino or C(1-3)alkyl.The compounds can be used as inhibitors of RORγ and are useful for the treatment of RORγ mediated diseases.本發明係關於式I化合物,或其醫藥上可接受之鹽,其中- A1至A8分別係N或CR1-CR8,條件係A1至A4中之4個位置A中之不多於兩者可同時係N且A5至A8中之4個位置A中之不多於兩者可同時係N;- R1至R8獨立地係H、鹵素、胺基、C(1-3)烷氧基、(二)C(1-3)烷基胺基或C(1-6)烷基;- R9係C(1-6)烷基;- R10及R11獨立地係H、F、甲基、乙基、羥基或甲氧基或R10及R11一起係羰基,所有烷基(若存在)視情況經一或多個F取代;- R12係H或C(1-6)烷基;- R13係C(3-6)環烷基、C(3-6)環烷基C(1-3)烷基、C(2-5)雜環烷基、C(2-5)雜環烷基C(1-3)烷基、C(6-10)芳基、C(6-10)芳基C(1-3)烷基、C(1-9)雜芳基或C(1-9)雜芳基C(1-3)烷基;- R14係H、C(1-6)烷基、C(2-6)烯基、C(3-6)環烷基、C(3-6)環烷基C(1-3)烷基、C(2-5)雜環烷基、C(2-5)雜環烷基C(1-3)烷基、C(6-10
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