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Tartrate salt of selective cdk9 inhibitor and its crystal form

A technology of tartrate salt and crystal form, which is applied in the field of chemical pharmacy, can solve the problems of unsalted species, further evaluation of performance, and unprepared, etc., and achieve good crystallinity, easy production scale expansion, and good stability. Effect

Active Publication Date: 2020-03-20
CHANGZHOU QIANHONG BIOPHARMA +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] The Chinese invention patent with the publication number CN103373994A (incorporated herein by reference in its entirety) discloses a class of compounds with CDK-9 inhibitory function and its preparation method, which mentions the pharmaceutically acceptable salts of such compounds, but does not prepare specific The salt of the compound, and no further evaluation was made on the type and performance of the salt

Method used

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  • Tartrate salt of selective cdk9 inhibitor and its crystal form
  • Tartrate salt of selective cdk9 inhibitor and its crystal form
  • Tartrate salt of selective cdk9 inhibitor and its crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1 Salt-forming performance of 3-(5-fluoro-4-(4-methyl-2-(methylamino)thiazol-5-yl)pyrimidin-2-ylamino)-benzenesulfonamide (code LS007)

[0054] 1.1 High-throughput screening of salt formation

[0055] Combined with the pKa value of LS007 and the solubility in different pHs, it can be determined that acids with a pKa value of about 3 or less can be used as acids for salt-forming screening. Therefore, we selected 8 acids: hydrochloric acid, sulfuric acid, aspartic acid, maleic acid, phosphoric acid, glutamic acid, tartaric acid, fumaric acid.

[0056]The drug was dissolved and added to a 96-well plate, and the volume of the added counterion was determined according to the molar amount of the added drug and the number of counterion functional groups. Heating time and temperature can be determined according to specific conditions (generally 40 ℃, 1 hour). In order to ensure a certain pressure during the reaction in the bottle, it is necessary to ensure the absolut...

Embodiment 2

[0072] Example 2 Crystal form of 3-(5-fluoro-4-(4-methyl-2-(methylamino)thiazol-5-yl)pyrimidin-2-ylamino)-benzenesulfonamide tartrate

[0073] In this study, aiming at the polymorphic form of LS007 tartrate, different crystallization conditions and experimental methods were used to systematically screen the possible crystal forms of compound LS007 tartrate. Through nearly 300 crystallization experiments, it was found that LS007 tartrate can exist in two different crystal forms, which are crystal forms A and B respectively. Further characterization found that there was no significant difference in physical and chemical properties between different crystal forms. In the transformation experiment between crystal forms, it was found that Form A is a more stable crystal form, and Form B can be transformed into Form A crystal form under certain conditions.

[0074] (1) Form A

[0075] Columnar crystals, the drug melts and decomposes, with a peak decomposition temperature of 236.8°...

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Abstract

The invention relates to the technical field of chemical pharmacy, and discloses a compound of 3-(5-fluoro-4-(4-methyl-2-(methylamino)thiazol-5-yl)pyrimidin-2-ylamino)-benzenesulfonamide Tartrate and its polymorphs, which are inhibitors of protein kinases, especially cyclin-dependent kinase 9 (CDK9), are useful in the treatment of proliferative disorders such as cancer and other diseases in which protein kinase / CDK activity is implicated.

Description

technical field [0001] The invention relates to the technical field of chemical pharmacy, in particular to 3-(5-fluoro-4-(4-methyl-2-(methylamino)thiazol-5-yl)pyrimidin-2-ylamino)-benzenesulfonate The salt form of the amide and its stable crystal form, which are selective inhibitors of cyclin-dependent kinases (CDK) such as CDK9, can be used for the treatment of cell proliferative diseases such as cancer. Background technique [0002] Proliferative diseases such as cancer are characterized by uncontrolled and deregulated cell proliferation. The protein kinase family is an important class of enzymes that has been the subject of extensive research in this regard. The protein kinase family is one of the largest in the human genome. Most kinases contain a catalytic domain of 250-300 amino acid residues with a conserved core structure. This domain contains the binding pocket for ATP, whose terminal phosphate group is covalently transferred to its macromolecular substrate. Pro...

Claims

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Application Information

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IPC IPC(8): C07D417/04A61K31/506A61P35/00A61P35/02
CPCA61P35/00A61P35/02C07D417/04C07B2200/13C07C59/255A61K31/506
Inventor 王淑东王辉江立群吕锦晨居文建
Owner CHANGZHOU QIANHONG BIOPHARMA
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