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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:
TW105117767
公开号:
TW201710240A
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 is NR1 or CR1, with R1 is as described herein; - the cyclopropyl moiety can be optionally substituted with one or more methyl and one or more F; - A2-A5 are N or CR2-CR5, respectively, with the proviso that no more than two of the four positions A in A2-A5 can be simultaneously N; - R2-R5 are as described herein; - R6 and R7 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R6 and R7 together is carbonyl, all alkyl groups, if present, optionally being substituted with one or more F; - R8 is H or C(1-6)alkyl; - A9-A12 are N or CR9-CR12, respectively, with the proviso that no more than two of the four positions A in A9-A12 can be simultaneously N; - R9-R12 are as described herein; - R13 and R14 are as described herein; - 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係NR1或CR1,其中R1係如本文所述;- 環丙基部分可視情況經一或多個甲基及一或多個F取代;- A2至A5分別係N或CR2至CR5,條件係A2至A5中之4個位置A中之不多於2者可同時係N;- R2至R5係如本文所述;- R6及R7獨立地係H、F、甲基、乙基、羥基或甲氧基或R6及R7一起係羰基,所有烷基(若存在)視情況經一或多個F取代;- R8係H或C(1-6)烷基;- A9至A12分別係N或CR9至CR12,條件係A9至A12中之4個位置A中之不多於2者可同時係N;- R9至R12係如本文所述;- R13及R14係如本文所述;- 或藉由將為C(1-6)烷基或C(2-6)烯基之R13與在R14定義內之獨立取代基接合來使R13及R14融合且形成具有5至7個原子之環,所有基團視情況經一或多個鹵素、胺基、羥基、氰基、C(1-3)烷氧基、C(1-3)烷氧基羰基、(二)C(1-3)烷基胺基或C(1-3)烷基取代。該等化合物可用作RORγ之抑制劑且用於治療RORγ介導之疾病。
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