1257294-51-1Relevant articles and documents
MACROCYCLIC COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
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Page/Page column 453; 489; 490, (2020/03/29)
Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce excessive activation of complement.
ASK1 inhibitor and applications thereof
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Paragraph 0252-0254, (2020/06/17)
The invention relates to the technical field of medicines, specifically to a compound represented by a formula (I), a pharmaceutically acceptable salt, ester or stereoisomer thereof, a pharmaceuticalcomposition and a preparation containing the compound, the pharmaceutically acceptable salt, the ester or the isomer thereof, a method for preparing the compound, the pharmaceutically acceptable salt,the ester or the isomer thereof, and applications of the compound, the pharmaceutically acceptable salt, the ester or the isomer thereof in preparation of drugs for treating and/or preventing ASK1-mediated diseases and related diseases.
MUSCARINIC ACETYLCHOLINE M1 RECEPTOR ANTAGONISTS
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Paragraph 00402; 00403, (2020/01/08)
Provided herein are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.
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.
INHIBITORS OF SYK
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Page/Page column 97-98, (2014/05/07)
The present invention relates to the use of novel compounds 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.
PYRIDAZINE AMIDE COMPOUNDS
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Paragraph 0495; 0496, (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.