cas 1231930-33-8, 6-Bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole

Articles about 1231930-33-8Total 14 be found

A 2-aminopyrimidine heterocyclic compound and its applications
The present invention discloses a 2-aminopyrimidine heterocyclic compound having a general formula I structure and its applications, which are kinase CDK4, CDK6 and / or CDK9 inhibitors, can be more widely used in the treatment of a variety of cancers, ha
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Paragraph 0086; 0094; 0102-0104

(2022/01/12)

A piperazine-containing aminopyrimidine derivative and its application
The present invention discloses a piperazine-containing aminopyrimidine derivative having a general formula I. structure, which belongs to kinase CDK4, CDK6 and / or CDK9 inhibitors, can be more widely used in the treatment of a variety of cancers, has gr
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Paragraph 0124; 0131-0133

(2022/01/12)

A pyrimidine compound and its application
The present invention discloses a pyrimidine amine compound having a general formula I structure and its applications, the class of compounds belongs to the kinase CDK4, CDK6 and / or CDK9 inhibitors, can be more widely used in the treatment of a variety
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Paragraph 0084; 0091-0092; 0099-0101

(2022/01/12)

Synthetic method of intermediate of abemaciclib
The invention discloses a synthesis method of an intermediate of abemaciclib, which comprises the following steps: carrying out condensation reaction on 5-bromo-3-fluoro-1,2-phenylenediamine serving as an initial raw material and acetic acid to obtain an intermediate 1, and reacting the intermediate 1 with acetone at 0-80 DEG C under the action of a reducing agent to obtain 6-bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzo[D]imidazole, namely, the abemaciclib intermediate. The reaction route is shown in the specification. The synthetic method disclosed by the invention is simpler to operate, lessin three wastes, more guaranteed in yield and product quality, and more suitable for industrial scale-up production.
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Paragraph 0039; 0041

(2020/12/15)

Synthesis method of 6-bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzo[D]imidazole
The invention discloses a synthesis method of 6-bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzo[D]imidazole. The method comprises the following steps: (1) adding sodium hydride into a reaction bottle, adding an aprotic solvent into the reaction bottle, and carrying out a constant-temperature stirring reaction; (2) dissolving N-(4-bromo-2,6-difluorophenyl)-N'-isopropylacetamidine in the aprotic solvent, slowly dropwise adding the clarified solution into a reaction bottle, heating the reaction system to 40-100 DEG C, and then carrying out a stirring reaction for 4-10 h; (3) cooling to room temperature after the reaction is completed, adding water to prepare a solution, extracting for three times, mixing organic phases, washing the organic phase with a saturated saline solution once, drying withanhydrous sodium sulfate, and filtering; and (4) concentrating the obtained filtrate, adding n-hexane for dissolving, adding deionized water into the reaction system solution, standing overnight, andfiltering and drying after white crystals are separated out to obtain the 6-bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzo[D]imidazole. The synthesis method is short in reaction time and simple in treatment, the labor cost is saved, and the environmental pollution is reduced.
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Paragraph 0019-0053

(2020/05/01)

Novel synthesis method of Abemaciclib mesylate
The invention discloses a synthesis method of Abemaciclib mesylate. The method comprises steps as follows: (1), a compound 9 in the description is subjected to a reaction with a compound 5 in the description under the action of strong base, and a compound
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Paragraph 0049-0051

(2019/06/07)

AMINO PYRIMIDINE COMPOUND FOR INHIBITING PROTEIN TYROSINE KINASE ACTIVITY
An amino pyrimidine compound for inhibiting protein tyrosine kinase activity, a pharmaceutical composition thereof, preparation therefor, and an application thereof. Specifically, an amino pyrimidine compound represented by formula (I), R1, R2, L, Y, R6, W, A, m, and n being defined in the specification, and a pharmaceutically acceptable salt, a stereoisomer, a solvent compound, a hydrate, a polymorphism, a prodrug, or an isotope variant thereof. The compound can be used for treating and/or preventing protein tyrosine kinase-related diseases such as cell proliferative diseases, cancers, and immune diseases.
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Paragraph 0302; 0305

(2019/06/07)

CRYSTALLINE POLYMORPHS OF ABEMACICLIB
The present disclosure provides novel polymorphs of abemaciclib, solid dispersions of abemaciclib with pharmaceutical excipients, and processes for the preparation thereof. The disclosure further provides methods for preparing crystalline abemaciclib form I, amorphous abemaciclib, and methods for synthesizing abemaciclib.
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Page/Page column 39; 40

(2019/06/11)

Application of benzimidazole derivative used as inhibitor of cyclin dependent kinase 4/6
The invention relates to an application of a benzimidazole derivative used as an inhibitor of cyclin dependent kinase 4/6. The benzimidazole derivative provided by the invention has a structure as shown in a formula (I) which is described in the specification. In the formula (I), substituents are described in the description.
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(2018/07/30)

Deuterium-modified Abemaciclib derivative
The invention belongs to the field of medicinal chemistry and specifically relates to a deuterium-modified Abemaciclib derivative, a preparation method of the derivative, a pharmaceutical composition containing the deuterium-modified Abemaciclib derivative, and application of the deuterium-modified Abemaciclib derivative and the pharmaceutical composition in the preparation of a medicine for treating cell proliferative diseases. In comparison with Abemaciclib, some compounds of the invention (especially compounds in the embodiment) have more excellent pharmacokinetic properties. It is expected that clinical dosage will be reduced. Thus, treatment cost is reduced so as to benefit more patients.
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Paragraph 0082; 0083; 0084; 0085; 0086; 0087

(2017/08/02)

Substituted benzimidazole derivatives
The invention belongs to the field of pharmaceutical chemistry, particularly relates to substituted benzimidazole derivatives as well as a preparation method and pharmaceutical composition thereof and further relates to an application of the substituted b
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Paragraph 0042; 0048; 0049

(2018/01/09)

KINASE INHIBITOR AND USE THEREOF
The invention relates to a CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers; a pharmaceutical formulation, pharmaceutical composition and kit comprising said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers, and use of said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers. For example, the compounds of the invention are useful for reducing or inhibiting the activity of CDK4/6 kinase in a cell, and/or treating and/or preventing a cancer-related disease mediated by CDK4/6 kinase.
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Paragraph 0175; 0176

(2016/11/21)

COMBINATION THERAPY FOR CANCER
The present invention provides preparation of medicaments for use in treating and methods of treating non-small cell lung cancer in a patient comprising: [5-(4-ethyl-piperazin-1-ylmethyl)-pyridin-2-yl]-[5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-3H- benzoimidazol-5-yl)-pyrimidin-2-yl]-amine, or a pharmaceutically acceptable salt thereof, in combination, as further described herein, with an anti-VEGFR2 antibody, preferably, ramucirumab.
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(2015/09/28)

PROTEIN KINASE INHIBITORS
The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof which is useful in the treatment of cell proliferative diseases.
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Page/Page column 10

(2010/07/04)