198995-91-4Relevant articles and documents
PYRAZOLO[1,5-D][1,2,4]TRIAZINE-5(4H)-ACETAMIDES AS INHIBITORS OF THE NLRP3 INFLAMMASOME PATHWAY
-
Page/Page column 93, (2021/10/22)
The invention relates to novel compounds for use as inhibitors of NLRP3 inflammasone production, wherein such compounds are as defined by compounds of formula (I) and wherein the integers R1, R2 and R3 are defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of a disease or disorder that is associated with NLRP3 inflammasome activity.
Diastereoselective Synthesis of a cis-1,3-Disubstituted Cyclobutane Carboxylic Acid Scaffold for TAK-828F, a Potent Retinoic Acid Receptor-Related Orphan Receptor (ROR)-γt Inverse Agonist
Majima, Keisuke,Yamano, Mitsuhisa
, p. 11464 - 11471 (2021/09/02)
A scalable synthesis of the cis-1,3-disubstituted cyclobutane carboxylic acid scaffold of TAK-828F (1) has been developed, featuring the diastereoselective reduction of a cyclobutylidene Meldrum's acid derivative with NaBH4. Controlling acidic impurities was crucial for improving the diastereomeric ratio by recrystallization. Furthermore, reaction optimization and the streamlining of several steps established a scalable synthetic method free from column chromatography purification with an overall yield improved from 23 to 39%.
METHOD FOR PRODUCING HETEROCYCLIC COMPOUND
-
Paragraph 0124-0126, (2020/10/16)
PROBLEM TO BE SOLVED: To provide a production method suitable for industrial production of a compound (A). SOLUTION: A compound (A) or a salt thereof is produced in an increased total yield and at low cost, with a reduced number of steps, and without requiring cryogenic reaction conditions or complex operation such as column purification or chiral column purification [where each symbol is as described in the specifications]. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPO&INPIT
