CAS: 1448232-80-1; (R)-5-((1-Acryloylpyrrolidin-3-yl)Oxy)-6-Ethyl-3-((4-(4-(4-Methylpiperazin-1-yl)Piperidin-1-yl)Phenyl)Amino)Pyrazine-2-Carboxamide

专利信息

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:WO-2024258613-A9
优先权日:2023-06-16
标题:Tetrachlorovancomycin and derivatives
发明人：BOGER DALE
权利人:SCRIPPS RESEARCH INST
摘要:A total synthesis of a new class of vancomycin analogues of reduced synthetic complexity was developed. The synthesis, achieved by the addition of two aryl chloride substituents to provide tetrachlorovancomcyin aglycon (Compound II), tetrachlorovancomcyin (Compound I ), and their derivatives, permitted a streamlined total synthesis of the new class of glycopeptide antibiotics by removing atropisomer stereochemical control and enabled the simultaneous and further activated SNAr macrocyclizations that establish the tricyclic skeleton of Compound I. In addition to the antimicrobial evaluation of tetrachlorovancomycin (Compound I), the preparation of key binding pocket and peripherally-modi fied derivatives, which overcome vancomycin resistance and introduce independent and synergistic mechanisms of action, revealed their exceptional antimicrobial potency and provide the foundation for use of this new class of synthetic glycopeptide analogues. Also disclosed are a pharmaceutical composition containing bactericidal amount of tetrachlorovancomycin, a derivative thereof or a salt of either dissolved or dispersed in a pharmaceutically acceptable diluent.