5177-27-5Relevant articles and documents
Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing
Chen, Bailing,Feru, Frederic,Feutrill, John,Gero, Thomas W.,Gray, Nathanael S.,Groendyke, Brian J.,Li, Bin,Li, Zhengnian,Powell, Chelsea E.,Scott, David A.,Szabo, Hilary
, (2020/08/07)
The protein kinase TNK2 (ACK1) is an emerging drug target for a variety of indications, in particular for cancer where it plays a key role transmitting cell survival, growth and proliferative signals via modification of multiple downstream effectors by unique tyrosine phosphorylation events. Scaffold morphing based on our previous TNK2 inhibitor XMD8-87 identified urea 17 from which we developed the potent and selective compound 32. A co-crystal structure was obtained showing 32 interacting primarily with the main chain atoms of an alanine residue of the hinge region. Additional H-bonds exist between the urea NHs and the Thr205 and Asp270 residues.
TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 64, (2015/12/30)
The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
PURINE COMPOUNDS FOR TREATING AUTOIMMUNE AND DEMYELINATING DISEASES
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Page/Page column 83; 84; 101; 102, (2011/09/30)
A compound of Formula (I), or a pharmaceutically acceptable salt thereof. Values and preferred values of variables A1, A2 and R1 are provided herein.
