1448348-15-9Relevant academic research and scientific papers
KIF18A INHIBITORS
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Paragraph 0189; 0252; 0255, (2021/02/12)
Compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.
PYRIDINE DERIVATIVES AS KIF18A INHIBITORS
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Paragraph 0288, (2021/02/12)
Amide compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers
Popovici-Muller, Janeta,Lemieux, René M.,Artin, Erin,Saunders, Jeffrey O.,Salituro, Francesco G.,Travins, Jeremy,Cianchetta, Giovanni,Cai, Zhenwei,Zhou, Ding,Cui, Dawei,Chen, Ping,Straley, Kimberly,Tobin, Erica,Wang, Fang,David, Muriel D.,Penard-Lacronique, Virginie,Quivoron, Cyril,Saada, Véronique,De Botton, Stéphane,Gross, Stefan,Dang, Lenny,Yang, Hua,Utley, Luke,Chen, Yue,Kim, Hyeryun,Jin, Shengfang,Gu, Zhiwei,Yao, Gui,Luo, Zhiyong,Lv, Xiaobing,Fang, Cheng,Yan, Liping,Olaharski, Andrew,Silverman, Lee,Biller, Scott,Su, Shin-San M.,Yen, Katharine
supporting information, p. 300 - 305 (2018/04/20)
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.
THERAPEUTICALLY ACTIVE COMPOUNDS AND USE THEREOF
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Page/Page column 159; 160, (2015/02/19)
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.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column 160-161, (2015/02/19)
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.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column, (2015/02/19)
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.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column 160; 161, (2013/07/31)
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.
THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE
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Page/Page column, (2013/07/31)
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.
