1185428-32-3Relevant articles and documents
3-amido pyrrolopyrazine JAK kinase inhibitors: Development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models
Soth, Michael,Hermann, Johannes C.,Yee, Calvin,Alam, Muzaffar,Barnett, Jim W.,Berry, Pamela,Browner, Michelle F.,Frank, Karl,Frauchiger, Sandra,Harris, Seth,He, Yang,Hekmat-Nejad, Mohammad,Hendricks, Than,Henningsen, Robert,Hilgenkamp, Ramona,Ho, Hoangdung,Hoffman, Ann,Hsu, Pei-Yuan,Hu, Dong-Qing,Itano, Andrea,Jaime-Figueroa, Saul,Jahangir, Alam,Jin, Sue,Kuglstatter, Andreas,Kutach, Alan K.,Liao, Cheng,Lynch, Stephen,Menke, John,Niu, Linghao,Patel, Vaishali,Railkar, Aruna,Roy, Douglas,Shao, Ada,Shaw, David,Steiner, Sandra,Sun, Yongliang,Tan, Seng-Lai,Wang, Sandra,Vu, Minh Diem
, p. 345 - 356 (2013)
The Janus kinases (JAKs) are involved in multiple signaling networks relevant to inflammatory diseases, and inhibition of one or more members of this class may modulate disease activity or progression. We optimized a new inhibitor scaffold, 3-amido-5-cycl
PYRROLOPYRIMIDINE ITK INHIBITORS
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Paragraph 0686; 0687; 0688, (2020/02/27)
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.
PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL, PYRROLO[2,3-B]PYRIDINYL ACRYLAMIDES AND EPOXIDES THEREOF
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Page/Page column 30, (2016/11/21)
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
PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL AND PYR-ROLO[2,3-D]PYRIDINYL ACRYLAMIDES
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Paragraph 0650, (2015/06/17)
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.
DIARYL MACROCYCLES AS MODULATORS OF PROTEIN KINASES
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Paragraph 0359, (2015/11/27)
The present invention relates to certain diaryl macrocyclic compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
Its use as an inhibitor and JAK and SYK deriv. pyrroropyrazine
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Paragraph 0127; 0131, (2016/11/07)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q, R2, R3, and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
AZAINDOLE DERIVATIVES AS JAK3 INHIBITORS
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Page/Page column 34, (2014/06/11)
The present disclosure provides compounds that are JAK3 inhibitors and therefore useful for the treatment of diseases treatable by inhibition of JAK3 such as cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
PYRROLO[2,3-B]PYRAZINES AS SYK INHIBITORS
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Page/Page column 38; 39, (2014/03/25)
The present invention relates to the use of novel pyrrolo[2,3- b]]pyrazines wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors
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.
, p. 1677 - 1692 (2013/04/10)
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.
PYRROLOPYRAZINE KINASE INHIBITORS
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Page/Page column 48, (2013/03/28)
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.