1242156-55-3Relevant articles and documents
Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis
Kawahata, Wataru,Asami, Tokiko,Kiyoi, Takao,Irie, Takayuki,Taniguchi, Haruka,Asamitsu, Yuko,Inoue, Tomoko,Miyake, Takahiro,Sawa, Masaaki
supporting information, p. 8917 - 8933 (2018/10/09)
Bruton's tyrosine kinase (BTK) is a promising drug target for the treatment of multiple diseases, such as B-cell malignances, asthma, and rheumatoid arthritis. A series of novel aminotriazines were identified as highly selective inhibitors of BTK by a scaffold-hopping approach. Subsequent SAR studies of this series using two conformationally different BTK proteins, an activated form of BTK and an unactivated form of BTK, led to the discovery of a highly selective BTK inhibitor, 4b. With significant efficacy in models in vivo and good ADME and safety profiles, 4b was advanced into preclinical studies.
NOVEL TRIAZINE DERIVATIVE
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Paragraph 0088; 0089, (2016/07/05)
The purpose of the present invention is to provide a novel triazine derivative of the formula (I): wherein R1 represents a substituted or unsubstituted lower alkyl group,R2 represents a hydrogen atom or a substituted or unsubstituted lower alkyl group,A represents a nitrogen atom or C—R3,R3 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, andR4 represents a substituted or unsubstituted lower alkyl group,or a substituted or unsubstituted cycloalkyl group,or a pharmaceutically acceptable salt thereof.
NOVEL 2,6-DIAMINOPYRIMIDINE DERIVATIVE
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Page/Page column 9, (2016/08/17)
To provide a novel 2,6-diaminopyrimidine derivative by the following formula (I): A 2,6-diaminopyrimidine derivative is represented by the formula (I): wherein R1 represents a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted alkoxy group, Ar represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group, Z1 and Z2 represent carbon atoms, or either 1 or 2 of the Z1 and Z2 represent nitrogen atoms, Q is selected from a structure (a) or (b) described below: R2 represents a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group, R3 represents a hydrogen atom or a halogen atom, Y represents a nitrogen atom or a carbon atom, and the bond drawn with a dotted line parallel to a solid line on structure (a) represents either double bond or single bond.