IMPROVED PROCESS FOR THE PREPARATION OF (2S)-N-{(1S)-1-(2-CHLOROPHENYL)-2-[(3,3-DIFLUOROCYCLOBUTYL)-AMINO]-2-OXOETHYL}-1-(4-CYANOPYRIDIN-2-YL)-N-(5-FLUOROPYRIDIN-3-YL)-5-OXOPYRROLIDINE-2-CARBOXAMIDE
The present invention relates to improved process for the preparation of (2S)-N-{(1S)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)-amino]-2-oxoethyl}-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide and its pharmaceutically acceptable salts represented by the following structural formula. Formula-1 The present invention relates to novel intermediates useful in the preparation of Ivosidenib of formula-1 and novel process for the preparation of (2S)-N-{(1S)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)-amino]-2-oxoethyl}-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide. The present invention also relates to solid state forms of (2S)-N-{(1S)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)-amino]-2- oxoethyl}-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide.
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(2021/04/30)
A METHOD FOR PREPARING IVOSIDENIB AND AN INTERMEDIATE THEREOF
The present application relates to a method for preparing a substantially and diastereomerically pure crystalline ethanol solvate of Compound IIa and its use for synthesizing Ivosidenib.
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Paragraph 0075; 0049
(2021/02/12)
AN IMPROVED PROCESS OF PREPARATION OF IVOSIDENIB
The present invention relates to an improved process of preparation of Ivosidenib a compound of Formula (I). More particularly, present invention provides process of preparation of intermediates. Also provide process of preparation of amorphous form of Ivosidenib. Further, present invention provides process of preparation of chirally pure Ivosidenib a compound of Formula (I).
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(2021/02/19)
SOLID STATE FORMS OF IVOSIDENIB
Solid state forms of Ivosidenib, processes for preparation thereof, pharmaceutical compositions thereof, and uses thereof are disclosed.
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(2019/06/11)
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers
Somatic point mutations at a key arginine residue (R132) within the active site of the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) confer a novel gain of function in cancer cells, resulting in the production of d-2-hydroxyglutarate (2-HG), an oncometabolite. Elevated 2-HG levels are implicated in epigenetic alterations and impaired cellular differentiation. IDH1 mutations have been described in an array of hematologic malignancies and solid tumors. Here, we report the discovery of AG-120 (ivosidenib), an inhibitor of the IDH1 mutant enzyme that exhibits profound 2-HG lowering in tumor models and the ability to effect differentiation of primary patient AML samples ex vivo. Preliminary data from phase 1 clinical trials enrolling patients with cancers harboring an IDH1 mutation indicate that AG-120 has an acceptable safety profile and clinical activity.
Provided are therapeutically active compounds and the use in manufacture of medicaments for treating a cancer characterized by the presence of a mutant allele of IDH1.
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Page/Page column 94; 96; 108
(2015/02/19)
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column 95-96; 108
(2015/02/19)
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