1446200-63-0Relevant articles and documents
BIFLUORODIOXALANE-AMINO-BENZIMIDAZOLE KINASE INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNEINFLAMMATION AND CNS DISORDERS
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, (2014/01/17)
The invention relates to a compound of the general formula (I) or a physiologically functional derivative, solvate or salt thereof, (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-, *-S02N(R"')-, -S02, or *-N(R"')-SO2-, 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)-alkyI-, *-alkyl-N(RN)-, *-N(RN)CON(RN)-, *-CO-, *-S02-, alkyl, *-alkyl-0-alkyl-, *-NCO-CH=CH-, *-CH=CH-CONH-, * -S02N(RN)-, *-N(RN)S02-, 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 RN 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.
2-Benzamido-N-(1H-benzo[d]imidazol-2-yl)thiazole-4-carboxamide derivatives as potent inhibitors of CK1δ/ε
Bischof, Joachim,Leban, Johann,Zaja, Mirko,Grothey, Arnhild,Radunsky, Barbara,Othersen, Olaf,Strobl, Stefan,Vitt, Daniel,Knippschild, Uwe
, p. 1577 - 1591 (2013/01/14)
In this study we identified two heterocyclic compounds (5 and 6) as potent and specific inhibitors of CK1δ (IC50 = 0.040 and 0.042 μM, respectively). Whereas compound 5 exhibited fivefold higher affinity towards CK1δ than to CK1ε (IC50/su
