- Compound with IDH mutant inhibitory activity, preparation method and application thereof
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The invention belongs to the field of medicines, and particularly relates to a s-triazine compound with structural characteristics of a general formula I or a pharmaceutically acceptable salt thereof,a pharmaceutical composition and a preparation method thereof, and application of the s-triazine compound or the pharmaceutically acceptable salt and the pharmaceutical composition in preparation ofIDH2 mutant inhibitors. According to the invention, pharmacological experiment results show that the compound disclosed by the invention has an obvious inhibition effect on the activity of an IDH2 mutant (mIDH2), can effectively inhibit the process that alpha-ketoglutaric acid is catalyzed by mIDH2 to generate 2-hydroxyglutaric acid, and can be used for preparing drugs for preventing and/or treating various related diseases caused by IDH2 mutation, wherein the diseases comprise cancers carrying IDH2 mutation.
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- 1,3,5-TRIAZINE DERIVATIVE SALT, CRYSTAL, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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The invention discloses a crystal of 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine compound, a mesylate salt and crystal thereof, a preparation method thereof, a composition containing t
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Paragraph 0185; 0192; 0193; 0194
(2019/12/02)
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- Preparation method of triazine IDH inhibitor
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The invention belongs to the field of medicine chemistry, and relates to a preparation method of a triazine IDH inhibitor, and more specifically relates to a preparation method of (S)-3-(trifluoromethyl)-1-(4-(6-(trifluoromethyl)pyridine-2-yl)-6-(2-(trifl
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Paragraph 0068; 0079-0081; 0088; 0093-0095
(2019/08/07)
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- Substituted triazine-based IDH inhibitor optical isomers and applications thereof
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The present invention belongs to the field of medical chemistry, and relates to a class of substituted triazine-based IDH inhibitor optical isomers and applications thereof, and specifically providesoptical isomers represented by a formula I or formula II or hydrates, solvates, crystals or pharmaceutically acceptable salts thereof, and a preparation method thereof, a pharmaceutical composition containing the optical isomers or hydrates, solvates, crystals or pharmaceutically acceptable salts thereof, and uses in treatment of cancer characterized by the presence of mutant isocitrate dehydrogenase 2. According to the present invention, the compounds have good inhibitory activity against IDH2, and can be used as the cancer treatment agents with advantages of high treatment effect and low side effect. The formulas I and II are defined in the specification.
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Paragraph 0051; 0062; 0063; 0064
(2019/02/17)
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- CHEMICAL COMPOUND OF ISOCITRATE DEHYDROGENASE INHIBITOR, AND APPLICATION THEREOF
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Provided are a chemical compound of an isocitrate dehydrogenase inhibitor, and an application thereof, belonging to the field of medicinal chemistry; specifically provided is the chemical compound represented by formula I, or its isomer, pharmaceutically acceptable salt, crystal, solvate, or prodrug, as well as their preparation methods and pharmaceutical compositions containing said chemical compound, and an application of said chemical compound or composition. The chemical compound has very good ability to inhibit mutant IDH2 enzyme activity and to inhibit mutant IDH2 neoplastic cells, and may be used for preventing and/or treating a tumor characterized by the presence of mutant IDH2.
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Paragraph 0065; 0072; 0073
(2019/06/07)
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- Crystal form of triazine IDH inhibitor methanesulfonate (by machine translation)
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The invention belongs to the field, and relates to a crystal form of mesylate of IDH inhibitor and a preparation method, and particularly relates to a crystal form of methanesulfonate of (S)-3 - (trifluoromethyl) pyridin -1 -yl) 4 - (6 - (trifluoromethyl) pyridin -2 - amino) -6 - 2 -4 -triaz -1-yl) pyrrolidine 3 -3 -2 - 5 - alcohol and a preparation method thereof, wherein the mesylate crystal form can be used for preparing a medicament for treating cancers, and a preparation method thereof. (by machine translation)
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Paragraph 0104; 0115-0117
(2019/08/07)
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- Triazine IDH inhibitor pharmaceutical salt, and preparation method thereof
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The invention belongs to the field of medicine chemistry, and relates to a triazine IDH inhibitor pharmaceutical salt or a hydrate, a solvate, or a crystal thereof, and a preparation method and applications, and more specifically relates to a pharmaceutic
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Paragraph 0079; 0090-0092
(2019/08/07)
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- Triazine compound, and preparation method and applications thereof
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The invention belongs to the field of medicine chemistry, and more specifically relates to a triazine compound, a preparation method thereof, and applications of the triazine compound as a reference substance in (S)-3-(trifluoromethyl)-1-(4-(6-(trifluoromethyl)pyridine-2-yl)-6-(2-(trifluoromethyl)pyridine-4-amino)-1, 3, 5-triazine-2-yl)pyrrolidine-3-ol mesylate bulk drug quality study releated impurity qualitative and/or quantitative analysis.
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Paragraph 0036; 0047-0049
(2019/08/07)
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- TABLET COMPOSITIONS
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Provided herein is a tablet comprising 2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol or a pharmaceutically acceptable salt thereof.
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- COMBINATION THERAPY FOR TREATING MALIGNANCIES
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Provided are methods and compositions for treating AML in patients carrying an IDH2 mutation using a combination of an inhibitor of a mutant IDH2 enzyme and an AML induction and consolidation therapy.
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- 1, 3, 5-TRIAZINE DERIVATIVE AND METHOD OF USING SAME
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Disclosed are compounds having formulae I and II or pharmaceutically acceptable salts or hydrates thereof, a preparation method thereof and pharmaceutical compositions thereof. The compounds having formulae I and II possesses an isocitrate dehydrogenase 2 (IDH2) inhibitory activity and are capable of treating IDH2 mutation-induced cancers.
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Paragraph 0083-0084
(2018/06/15)
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- DEUTERATED COMPOUNDS FOR TREATING HEMATOLOGIC MALIGNANCIES, AND COMPOSITIONS AND METHODS THEREOF
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The invention provides novel chemical compounds useful for treating various hematologic malignancies, or a related disease or disorder thereof, and pharmaceutical composition and methods of preparation and use thereof.
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- METHODS OF PREPARING 6-(ARYL OR HETEROARYL)-1,3,5-TRIAZINE-2,4-DIOLS AND 6-(ARYL OR HETEROARYL)-1,3,5-TRIAZINE-2,4-DIAMINES
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Provided are methods of preparing compounds of formula (VIII) useful for treating cancer and intermediates of formula (I)
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Paragraph 0081; 0085
(2017/02/28)
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- COMBINATION THERAPY FOR TREATING MALIGNANCIES
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Provided are methods and compositions for treating cancers in patients carrying an IDH2 mutation using a combination of an inhibitor of a mutant IDH2 enzyme and a DNA demethylating agent.
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Paragraph 0563
(2017/05/02)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are compounds useful for treating cancer and methods of treating cancer, for example an advanced solid tumor, such as a glioma, or angioimmunoblastic T-cell lymphoma (AITL).
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Paragraph 00273; 00280
(2016/04/26)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are crystalline forms of 2-Methyl-l-[ (4-[ 6-(trifluoromethyl) pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2- yl)amino]propan-2-ol mesylate useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof said compound.
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Page/Page column 74
(2016/09/22)
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- HETEROCYCLIC COMPOUNDS AS IDH2 INHIBITORS
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The present invention is directed to novel heterocyclic compounds, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have IDHs inhibitory activities and are useful for the treatment of Isocitrate dehydrogenases mediated diseases and conditions. Novel heterocyclic compounds disclosed herein include pyrimidines and triazines.
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Paragraph 0045
(2016/11/21)
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- CRYSTALLINE FORMS OF THERAPEUTICALLY ACTIVE COMPOUNDS AND USE THEREOF
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Provided are crystalline forms of 2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{ [2-(trifluoromethyl)pyridin-4-yl]amino }-1, 3, 5-triazin-2-yl)amino]propan-2-ol(COMPOUND 3), 2-methyl-1-[(4- [6-(trifluoromethyl)pyridin-2-yi]-6-{ [2-(trifluoromethyl)pyridin-4- yl]amino }-1,3,5-triazin-2-yl)amino]propan-2-ol methanesulfonate (COMPOUND 1) and use thereof.
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are compounds useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof a compound described herein.
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Page/Page column 68; 69
(2015/02/25)
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- N,6-BIS(ARYL OR HETEROARYL)-1,3,5-TRIAZINE-2,4-DIAMINE COMPOUNDS AS IDH2 MUTANTS INHIBITORS FOR THE TREATMENT OF CANCER
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Provided are compounds of formula (I), Wherein: ring A and ring B are each independently an optionally substituted 5-6 membered monocyclic aryl or heteroaryl. The compounds are inhibitors of isocitrate dehydrogenase 2 (IDH2) mutants useful for treating cancer.
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Page/Page column 55; 56
(2015/02/02)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
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Page/Page column 219; 220
(2013/07/19)
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