- DIARYL MACROCYCLES AS MODULATORS OF PROTEIN KINASES
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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.
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Paragraph 0358
(2015/11/27)
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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 0649
(2015/06/17)
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- Its use as an inhibitor and JAK and SYK deriv. pyrroropyrazine
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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.
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Paragraph 0127; 0130
(2016/11/07)
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- PYRROLO[2,3-B]PYRAZINES AS SYK INHIBITORS
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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.
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Page/Page column 38
(2014/03/25)
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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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- 3-amido pyrrolopyrazine JAK kinase inhibitors: Development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models
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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
- 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
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p. 345 - 356
(2013/02/23)
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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 47; 48
(2013/03/28)
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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 n, p, q, Q, X, X′ and Y 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 54; 56
(2011/10/10)
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- PYRROLOPYRAZINE DERIVATIVES AS SYK AND JAK INHIBITORS
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The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables Q and R1 and R2 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 36
(2011/12/04)
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- PYRROLO [2, 3 - B] PYRAZINE - 7 - CARBOXAMIDE DERIVATIVES AND THEIR USE AS JAK AND SYK INHIBITORS
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The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables Q and R, R2, and R3 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 98
(2011/12/04)
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