1242156-52-0Relevant articles and documents
BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY
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Paragraph 0428-0429, (2021/05/15)
The present invention relates to compounds of formula (I) useful for degrading BTK via a ubiquitin proteolytic pathway. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
NOVEL TRIAZINE DERIVATIVE
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Paragraph 0130; 0131, (2016/10/08)
The purpose of the present invention is to provide a novel triazine derivative of the formula (I): wherein R 1 represents a substituted or unsubstituted lower alkyl group, R 2 represents a hydrogen atom or a substituted or unsubstituted lower alkyl group, A represents a nitrogen atom or C-R 3 , R 3 represents a hydrogen atom, a cyano group, a substituted or unsubstituted acyl group, a substituted or unsubstituted sulfonyl group, or a substituted or unsubstituted carbamoyl group, and R 4 represents a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group, or a pharmaceutically acceptable salt thereof.
Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors
Zhao, Xinge,Xin, Minhang,Huang, Wei,Ren, Yanliang,Jin, Qiu,Tang, Feng,Jiang, Hailong,Wang, Yazhou,Yang, Jie,Mo, Shifu,Xiang, Hua
, p. 348 - 364 (2015/02/05)
A series of novel reversible Btk inhibitors has been designed based on the structure of the recently reported preclinical drug RN486. The synthesis and SAR of these compounds are described. Among these derivatives, compound 16b was identified to be a potent and orally available reversible agent with satisfactory Btk enzymatic and cellular inhibition in vitro, as well as favorable PK properties and inhibition of arthritis in vivo.