123344-02-5Relevant articles and documents
Pyrimidine heterocyclic compounds, preparation method and application thereof
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Paragraph 0168-0171, (2018/03/25)
The present invention relates to compounds of a formula (I) shown in the description, and pharmaceutically acceptable salts, prodrugs and solvates thereof, and the compounds are useful for treating cancer and inflammation in mammals. The invention also discloses a preparation method for the compounds of the formula (I) and a pharmaceutical composition containing the compound.
Amino pyrimidine compound and preparation method and application thereof
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Paragraph 1043; 1049; 1050; 1051, (2018/11/22)
The invention relates to an amino pyrimidine compound and a preparation method and application thereof. The amino pyrimidine compound has a structure as shown in a formula I. The formula is shown in the description. The compound is an inhibitor of an epidermal growth factor receptor (EGFR) kinase. The invention further relates to a medicine composition comprising the compound, a preparation methodand application thereof in preparation of anti-tumor medicines.
Design, Synthesis, and Biological Evaluation of Novel Type I1/2 p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine
Walter, Niklas M.,Wentsch, Heike K.,Bührmann, Mike,Bauer, Silke M.,D?ring, Eva,Mayer-Wrangowski, Svenja,Sievers-Engler, Adrian,Willemsen-Seegers, Nicole,Zaman, Guido,Buijsman, Rogier,L?mmerhofer, Michael,Rauh, Daniel,Laufer, Stefan A.
supporting information, p. 8027 - 8054 (2017/10/18)
We recently reported 1a (skepinone-L) as a type I p38α MAP kinase inhibitor with high potency and excellent selectivity in vitro and in vivo. However, as a type I inhibitor, it is entirely ATP-competitive and shows just a moderate residence time. Thus, the scope was to develop a new class of advanced compounds maintaining the structural binding features of skepinone-L scaffold like inducing a glycine flip at the hinge region and occupying both hydrophobic regions I and II. Extending this scaffold with suitable residues resulted in an interference with the kinase's R-Spine. By synthesizing 69 compounds, we could significantly prolong the target residence time with one example to 3663 s, along with an excellent selectivity score of 0.006 and an outstanding potency of 1.0 nM. This new binding mode was validated by cocrystallization, showing all binding interactions typifying type I1/2 binding. Moreover, microsomal studies showed convenient metabolic stability of the most potent, herein reported representatives.
HETEROARYL COMPOUNDS AS IRAK INHIBITORS AND USES THEREOF
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Paragraph 00205, (2017/05/02)
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
SUBSTITUTED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
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Paragraph 000178, (2015/03/13)
The present disclosure relates to pyrimidine compounds of formula (I), their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to process of preparation of these pyrimidine compounds, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders mediated by epidermal growth factor receptor (EGFR) family kinases.
THIENO (2, 3B) PYRAZINE COMPOUNDS AS B-RAF INHIBITORS
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Paragraph 0249, (2013/04/10)
The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer.
Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity
Fischer, Stefan,Wentsch, Heike K.,Mayer-Wrangowski, Svenja C.,Zimmermann, Markus,Bauer, Silke M.,Storch, Kirsten,Niess, Raimund,Koeberle, Solveigh C.,Grütter, Christian,Boeckler, Frank M.,Rauh, Daniel,Laufer, Stefan A.
supporting information, p. 241 - 253 (2013/03/13)
p38α mitogen-activated protein (MAP) kinase is a main target in drug research concerning inflammatory diseases. Nevertheless, no inhibitor of p38α MAP kinase has been introduced to the market. This might be attributed to the fact that there is no inhibitor which combines outstanding activity in biological systems and selectivity. Herein an approach to the development of such inhibitors on the basis of the highly selective molecular probe Skepinone-L is described. Introduction of a "deep pocket" moiety addressing the DFG motif led to an increased activity of the compounds. Hydrophilic moieties, addressing the solvent-exposed area adjacent to hydrophilic region II, conserved a high activity of the compounds in a whole blood assay. Combined with their outstanding selectivity and low ATP competitiveness, these inhibitors are very interesting candidates for use in biological systems and in therapy.
TRICYCLIC COMPOUNDS AS TEC KINASE INHIBITORS
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Page/Page column 47-48; 71, (2013/11/05)
The present invention is directed to tricyclic compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermed
THIENO (2, 3B) PYRAZINE COMPOUNDS AS B - RAF INHIBITORS
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Page/Page column 75-76, (2011/12/14)
The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer.
8-(1H-imidazol-1-yl)-7-nitro-4(5H)-imidazo[1,2-a]quinoxalinone and related compounds: Synthesis and structure-activity relationships for the AMPA-type non-NMDA receptor
Ohmori, Junya,Shimizu-Sasamata, Masao,Okada, Masamichi,Sakamoto, Shuichi
, p. 2053 - 2063 (2007/10/03)
As a part of our program to discover novel antagonists for the AMPA subtype of EAA receptors, we designed and synthesized a series of heterocyclic-fused imidazolylquinoxalinones 5a-c, 9, 11, 14a-e, and 18 which led from 6-(1H-imidazol-1-yl)-7-nitro-2,3(1H