1237535-76-0Relevant articles and documents
CHIRAL SYNTHESIS OF FUSED BICYCLIC RAF INHIBITORS
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Paragraph 0402; 0409-0410; 0437; 0451-0453, (2022/02/09)
The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitor enantiomers of formula (I), (Ia), (Ib), (II), (IIa), or (IIb), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, with high enantiomeric excess (%ee). The disclosure also relates to method of using the compound of formula (I), (Ia), (Ib), (II), (IIa), or (IIb), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
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Paragraph 00454, (2020/04/25)
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
Method suitable for large-scale production of B-RAF kinase dimer inhibitor
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Paragraph 0053-0054, (2020/08/18)
The invention relates to a method for large-scale production of a B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-diazanaphthalene-4-yl) oxy)-1a, 6b-dihydro-1H-cyclopropyl [b] benzofuran-1-yl)-3-(2, 4, 5- trifluorophenyl) urea (hereinafter sometimes referred to as a compound 1). The method enables impurities or by-products to be controlled to 0.05% or less without the use of expensive column chromatography operations. Thus, the method greatly reduces cost and is suitable for large-scale production.