796845-64-2Relevant academic research and scientific papers
Kilogram-Scale Preparation of an Aminopyrazole Building Block via Copper-Catalyzed Aryl Amidation
Baldwin, Aaron F.,Caporello, Michaella A.,Chen, Guoyong,Goetz, Adam E.,Hu, Weifeng,Jin, Chengfeng,Knopf, Kevin M.,Li, Zhifeng,Lu, Cuong V.,Monfette, Sebastien,Puchlopek-Dermenci, Angela L. A.,Shi, Feng
supporting information, p. 1065 - 1073 (2021/05/04)
We describe a scalable method for preparing an aminopyrazole building block using copper-catalyzed amidation with acetamide as an ammonia surrogate. This procedure provides an alternative to the standard nitration/reduction sequence and avoids energetic intermediates, specialized hydrogenation equipment, and potentially genotoxic impurities that arise from nitro reduction. The chemistry has been successfully scaled to produce >50 kg of the target compound and demonstrate the viability of this alternative route.
SULFONYLUREA DERIVATIVES AND USES THEREOF
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Paragraph 01473-01474, (2020/12/30)
The present disclosure relates to compounds of Formula (I) and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
SULPHONYL UREA DERIVATIVES AS NLRP3 INFLAMMASOME MODULATORS
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Paragraph 01022, (2019/07/13)
The present disclosure relates to compounds of Formula (I): (I) and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
A convenient synthesis method of 5-oxopyrazolo[4,3-b]pyridine-6-carboxylic acids and their nitriles
Yakovenko, Georgiy G.,Lukianov, Oleh А.,Bol’but, Andriy V.,Vovk, Mikhailo V.
, p. 1211 - 1216 (2020/01/08)
[Figure not available: see fulltext.] N-Boc-protected 5-formyl-1H-pyrazol-4-amines react with malonic acid in pyridine in the presence of pyrrolidine at 45–50°С or with malonic acid monomethyl ether in the presence of pyrrolidine in AcOH under reflux with
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Paragraph 001221, (2016/12/22)
Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are describeded, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
CEPHEM COMPOUNDS
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Page 32, (2010/02/09)
The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl which may have suitable substituent(s), R2 is amino, protected amino or guanidino, R3 is carboxy or protected carboxy, R4 /sup
