372118-00-8Relevant articles and documents
TYK2 INHIBITORS AND USES THEREOF
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Paragraph 00496-00497, (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.
Imidazol-1-ylmethyl pyridazine derivatives
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Page 18, (2010/02/06)
The invention provides imidazol-1-ylmethyl pyridazine derivatives of the formula: 1 that bind to GABAA receptors. In the above formula, R1, R2 R3, R4, R5, R6 and Ar are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).