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Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmune inflammation and CNS disorders
专利权人:
4SC Discovery GmbH
发明人:
Leban, Johann,Zaja, Mirko
申请号:
AU2018201275
公开号:
AU2018201275A1
申请日:
2018.02.22
申请国别(地区):
AU
年份:
2018
代理人:
摘要:
#$%^&*AU2018201275A120180315.pdf#####BIFLUORODIOXALANE-AMINO-BENZIMIDAZOLE KINASE INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNEINFLAMMATION AND CNS DISORDERS Abstract The invention relates to a compound of the general formula (I) or a physiologically functional derivative, solvate or salt thereof, R N Y-L-X - / )F RN 0 R (I) wherein A is a bond, alkyl or alkoxy optionally substituted with one or more R" as defined herein, *-N(R"')CO-, *-CON(R'"..)-, *-N(R"')CON(R"')-, -S-, -SO-, *-N(R"')-, *-N(R'")CO-, *-CON(R"')-, -CO-, *-COO-, *-OOC-, *-SO 2N(R"')-, -SO 2, or *-N(R"')-S02-, wherein R"' is as defined herein and * specifies the point of attachment to X; X is aryl, cycloalkyl, aralkyl, heterocyclyl or heteroaryl, which may be substituted with one or more Rx further described herein; L is a bond or *-N(RN)CO-, *-CON(RN)-, *-N(RN)-, *-C=N(RN)-, *-N(RN)alkyl., *-alkyl-N(RN)-, *-N(RN)CON(RN)-, *-CO-, *-SO2-, alkyl, *-alkyl-O-alkyl-, *-NCO-CH=CH-, *-CH=CH-CONH-, * -SO 2N(RN)-, *-N(RN)SO 2-, or heterocyclyl, wherein * specifies the point of attachment to X; Y is H, alkyl, aryl, aralkyl, cycloalkyl, heterocyclyl or heteroaryl, which may be substituted with one or more RY further described herein; and R and e are further described herein; as well as their use as a medicament, a pharmaceutical composition comprising them, a method of treatment or prevention of a medical condition entailing the administration thereof, and the use thereof in the manufacture of a medicament for the treatment or prevention of a medical condition, particularly autoimmune inflammatory disorders, CNS disorders, sleeping disorders, or proliferative diseases including cancer. The invention further relates to a specific process for the preparation of said compounds.WO 2014/001464 PCT/EP2013/063537 1/1 Figures 1) a 2". b " 200 m40 20 0 b2
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