5177-27-5Relevant academic research and scientific papers
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.
As tyrosine kinase inhibitors containing nitrogen and ring compound
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Paragraph 0357; 0358; 0359; 0360, (2017/04/26)
The invention belongs to the technical field of medicine, particularly relates to a heterocyclic nitrogen compound which acts as a tyrosine kinase inhibitor and is represented by a general formula (I) as well as a deuterated material, pharmaceutically acc
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.
Bicyclic Kinase Inhibitors
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Page/Page column 17, (2011/08/22)
New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
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.
CRF receptor antagonists and methods relating thereto
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, (2008/06/13)
CRF receptor antagonists are disclosed. Such receptor antagonists are thiadiazole-, pyrimidine-, triazine-, and triazole-containing compounds substituted with both a C3-C14 monocyclic or fused, homoaryl or heteroaryl group and a substituted amine group. The CFR receptor antagonists have utility in the treatment of a variety of disorders, including disorders associated with the hypersecretion of CRF.
