83878-89-1Relevant articles and documents
TYK2 INHIBITORS AND USES THEREOF
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Paragraph 00496, (2020/06/10)
Described herein are compounds that are useful in treating a TYK2-mediated disorder. In some embodiments, the TYK2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.
Using ovality to predict nonmutagenic, orally efficacious pyridazine amides as cell specific spleen tyrosine kinase inhibitors
Lucas, Matthew C.,Bhagirath, Niala,Chiao, Eric,Goldstein, David M.,Hermann, Johannes C.,Hsu, Pei-Yuan,Kirchner, Stephan,Kennedy-Smith, Joshua J.,Kuglstatter, Andreas,Lukacs, Christine,Menke, John,Niu, Linghao,Padilla, Fernando,Peng, Ying,Polonchuk, Liudmila,Railkar, Aruna,Slade, Michelle,Soth, Michael,Xu, Daigen,Yadava, Preeti,Yee, Calvin,Zhou, Mingyan,Liao, Cheng
supporting information, p. 2683 - 2691 (2014/04/17)
Inhibition of spleen tyrosine kinase has attracted much attention as a mechanism for the treatment of cancers and autoimmune diseases such as asthma, rheumatoid arthritis, and systemic lupus erythematous. We report the structure-guided optimization of pyridazine amide spleen tyrosine kinase inhibitors. Early representatives of this scaffold were highly potent and selective but mutagenic in an Ames assay. An approach that led to the successful identification of nonmutagenic examples, as well as further optimization to compounds with reduced cardiovascular liabilities is described. Select pharmacokinetic and in vivo efficacy data are presented.
PYRIDAZINE AMIDE COMPOUNDS
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Paragraph 0297; 0298, (2013/07/19)
The present invention relates to the use of novel triazolopyridine derivatives of formula I: 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.
