- PYRROLOPYRIMIDINE ITK INHIBITORS
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Disclosed herein are arylpyridinone compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structures of Formulas (I)-(IV): wherein the R groups, m, n, and X are as defined in the detailed description. Methods of inhibition of ITK activity in a human or animal subject are also provided.
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Paragraph 0686; 0687; 0689
(2020/02/27)
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- Heteroaromatic compound and application thereof to drug
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The invention discloses a heteroaromatic compound and application thereof to drug. In particular, the invention provides a heteroaromatic compound or stereoisomers thereof, geometric isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, and a pharmaceutical composition comprising the compound provided by the invention. The invention also discloses application of the compound provided by the invention or the pharmaceutical composition thereofto preparation of a medicine for reatment of autoimmune diseases or proliferative diseases.
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- PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL, PYRROLO[2,3-B]PYRIDINYL ACRYLAMIDES AND EPOXIDES THEREOF
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The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3- b]pyrazinyl,and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides,and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention
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Page/Page column 63; 64
(2016/11/21)
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- PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL AND PYR-ROLO[2,3-D]PYRIDINYL ACRYLAMIDES
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The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
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Paragraph 0651
(2015/06/17)
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- PYRROLOPYRAZINE KINASE INHIBITORS
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The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
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Page/Page column 50; 51
(2013/03/28)
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- Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors
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We describe the discovery of several pyrrolopyrazines as potent and selective Syk inhibitors and the efforts that eventually led to the desired improvements in physicochemical properties and human whole blood potencies. Ultimately, our mouse model revealed unexpected toxicity that precluded us from further advancing this series.
- Padilla, Fernando,Bhagirath, Niala,Chen, Shaoqing,Chiao, Eric,Goldstein, David M.,Hermann, Johannes C.,Hsu, Jonathan,Kennedy-Smith, Joshua J.,Kuglstatter, Andreas,Liao, Cheng,Liu, Wenjian,Lowrie, Lee E.,Luk, Kin Chun,Lynch, Stephen M.,Menke, John,Niu, Linghao,Owens, Timothy D.,O-Yang, Counde,Railkar, Aruna,Schoenfeld, Ryan C.,Slade, Michelle,Steiner, Sandra,Tan, Yun-Chou,Villase?or, Armando G.,Wang, Ce,Wanner, Jutta,Xie, Wenwei,Xu, Daigen,Zhang, Xiaohu,Zhou, Mingyan,Lucas, Matthew C.
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supporting information
p. 1677 - 1692
(2013/04/10)
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