cas 1446507-38-5, 6-(6-(trifluoromethyl)pyridin-2-yl)-1,3,5-triazine-2,4(1H,3H)-dione

Articles about 1446507-38-5Total 23 be found

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Compound with IDH mutant inhibitory activity, preparation method and application thereof
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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(2020/09/23)

IDH2 mutant inhibitor with macrocyclic structure, and medical applications thereof
The present invention discloses a macrocyclic compound with a structure represented by a general formula (I), and a medical use thereof, or a pharmaceutically acceptable salt or solvate thereof, wherein L represents (CRaRb)n, 1-3 CRaRb groups can be replaced by O, NH, S or CH=CH, Z represents CRaRb, O, -NH-C(=O)-, -O-C(=O)- or -NH-, T is CH or N, X represents H, halogen, C3-C6 cycloalkyl, C1-C6 alkyl or C1-C6 haloalkyl, n is 4-10, and Ra and Rb are respectively and independently selected from H, halogen and C1-C6 alkyl. The inhibition effect of the macrocyclic compound provided by the invention on IDH2 is superior to the inhibition effect of the existing drug at a kinase level. According to the invention, the solubility of molecules and the overall fat solubility can be improved, so that the macrocyclic compound has the potential of penetrating through a blood-brain barrier, and is beneficial to solving the problem of brain tumors compared with the prior art.
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Paragraph 0047-0050

(2020/05/29)

Structure-based design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells
The enzymes involved in the metabolic pathways in cancer cells have been demonstrated as important therapeutic targets such as the isocitrate dehydrogenase 2 (IDH2). A series of macrocyclic derivatives was designed based on the marketed IDH2 inhibitor AG-221 by using the conformational restriction strategy. The resulted compounds showed moderate to good inhibitory potential against different IDH2-mutant enzymes. Amongst, compound C6 exhibited better IDH2R140Q inhibitory potency than AG-221, and showed excellent activity of 2-hydroxyglutarate (2-HG) suppression in vitro and its mesylate displayed good pharmacokinetic profiles. Moreover, C6 performed strong binding mode to IDH2R140Q after computational docking and dynamic simulation, which may serve as a good starting point for further development.
Che, Jinxin,Chen, Binhui,Dong, Xiaowu,Gao, Anhui,Gao, Jian,Hu, Xiaobei,Hu, Yongzhou,Huang, Feng,Li, Jia,Qu, Bingxue,Xu, Gaoya,Ying, Huazhou,Zhang, Jianjun,Zhang, Mengmeng,Zhou, Yubo
(2020/07/15)

1,3,5-TRIAZINE DERIVATIVE SALT, CRYSTAL, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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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(2019/12/02)

Substituted triazine-based IDH inhibitor optical isomers and applications thereof
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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(2019/02/17)

CHEMICAL COMPOUND OF ISOCITRATE DEHYDROGENASE INHIBITOR, AND APPLICATION THEREOF
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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(2019/06/07)

Crystal form of triazine IDH inhibitor methanesulfonate (by machine translation)
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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(2019/08/07)

Triazine IDH inhibitor pharmaceutical salt, and preparation method thereof
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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(2019/08/07)

Triazine compound, and preparation method and applications thereof
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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(2019/08/07)

Preparation method of triazine IDH inhibitor
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; 0073-0075

(2019/08/07)

TABLET COMPOSITIONS
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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(2018/03/25)

COMBINATION THERAPY FOR TREATING MALIGNANCIES
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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(2018/11/21)

1, 3, 5-TRIAZINE DERIVATIVE AND METHOD OF USING SAME
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 0079-0080

(2018/06/15)

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
Provided are methods of preparing compounds of formula (VIII) useful for treating cancer and intermediates of formula (I)
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(2017/02/28)

COMBINATION THERAPY FOR TREATING MALIGNANCIES
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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(2017/05/02)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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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(2016/04/26)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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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(2016/09/22)

CRYSTALLINE FORMS OF THERAPEUTICALLY ACTIVE COMPOUNDS AND USE THEREOF
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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(2015/02/25)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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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(2015/02/25)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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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Paragraph 0722-0723

(2015/02/18)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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 156; 157

(2015/02/02)

N,6-BIS(ARYL OR HETEROARYL)-1,3,5-TRIAZINE-2,4-DIAMINE COMPOUNDS AS IDH2 MUTANTS INHIBITORS FOR THE TREATMENT OF CANCER
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 52; 53

(2015/02/02)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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 118

(2013/07/19)