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Kinase inhibitor with novel structure

A solvate, C1-C8 technology, applied in the field of kinase inhibitors with novel structures, can solve problems such as easy tolerability of side effects

Active Publication Date: 2015-08-19
PRECEDO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, Dasatinib in the treatment of Imatinib-resistant chronic myelogenous leukemia CML can almost inhibit 9 kinases of the SRC family (and many other tyrosine kinases), but compared with traditional cell chemotherapy, its side effects are still easy to tolerate

Method used

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  • Kinase inhibitor with novel structure
  • Kinase inhibitor with novel structure
  • Kinase inhibitor with novel structure

Examples

Experimental program
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Effect test

preparation example Construction

[0093] Compound preparation

[0094] Compounds of formula (I) may be synthesized using standard synthetic techniques known to those skilled in the art or using methods known in the art in combination with the methods described herein. Additionally, solvents, temperatures and other reaction conditions given herein may be varied according to the skill in the art. As a further guide, the following synthetic methods can also be utilized.

[0095] The reactions can be used sequentially to provide the compounds described herein; or they can be used to synthesize fragments which are subsequently added by methods described herein and / or methods known in the art.

[0096] In certain embodiments, provided herein are methods of making and methods of using the tyrosine kinase inhibitor compounds described herein. In certain embodiments, the compounds described herein can be synthesized using the following synthetic schemes. Compounds can be synthesized using methods similar to those ...

Embodiment 1

[0148] Synthesis of (4-methyl-3-(N-(4(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(propynamidomethyl)benzamide compound 1

[0149] With 0.05mmol 4-(methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide k reaction temperature down Zero degrees Celsius, 0.05mmol of N-(4-methyl-3-(piperidine-4-oxyl)phenyl)-4-((4-methylpiperazin-1-yl)methyl)-3- (Trifluoromethyl)benzamide trihydrochloride h, 0.05mmol propiolic acid, 0.3mmol N,N-diisopropylethylamine (DIPEA) and 1 ml N,N-dimethylformamide (DMF ) into a 5-milliliter round-bottomed flask successively, and 0.06 mmol of 2-(7-azobenzotriazole)-N, N, N', N'-tetramethyluronium hexafluorophosphate ( HATU). The reaction system was stirred at room temperature for 2 hours. The reaction system was extracted with ethyl acetate, dried over anhydrous sodium sulfate; the solvent was removed by a rotary evaporator, and the crude product was separated by a silica gel column to obtain the target compound 1 (yield: 38%). Exa...

Embodiment 2

[0151] (E)-(4-(4-(Dimethylamino)-2-acrylamide)methyl)-(4-methyl-3-(4-(3-pyridyl)pyrimidin-2-yl)amino) Synthesis of phenyl)benzamide compound 2

[0152] Synthesis of Compound 2 was accomplished using a procedure similar to that described in Example 1. Exact Mass (calculated value): 521.25; MS (ESI) m / z (M+1) + : 522.27.

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Abstract

The invention provides compounds of a novel kinase inhibitor as shown in the formula (I) or pharmaceutically acceptable salts, solvates, esters, acids, metabolites, combination drugs or prodrugs thereof. The compounds independently combines with at least one variety of other therapeutic agents and can be used to prevent or treat illnesses, disorders or diseases, and autoimmune diseases which are regulated by tyrosine kinase activity or affected by the tyrosine kinase activity or related to the tyrosine kinase activity, and specifically cancers and other cellular proliferative diseases.

Description

technical field [0001] The present invention relates to novel compounds and their tautomers and stereoisomers and pharmaceutically acceptable salts, esters, acids, metabolites or prodrugs thereof, compositions of these novel compounds with pharmaceutically acceptable carriers, and These novel compounds alone in combination with at least one additional therapeutic agent in the prevention or treatment of diseases, disorders or conditions, autoimmune diseases which are modulated by or affected by tyrosine kinase activity or in which tyrosine kinase activity is involved Uses, especially in cancer and other cell proliferative diseases. Background technique [0002] Tyrosine kinase is a kind of kinase that catalyzes the transfer of γ-phosphate on ATP to protein tyrosine residues. It can catalyze the phosphorylation of protein tyrosine residues on various substrates, and plays an important role in cell growth, proliferation and differentiation. effect. Dysfunctional kinases have ...

Claims

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Application Information

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IPC IPC(8): C07D401/04C07D211/46C07D207/12C07D205/04C07D401/14C07D401/12C07D211/96C07D473/34C07D405/06C07D401/06A61K31/506A61K31/496A61K31/445A61K31/4545A61K31/454A61K31/52A61K31/498A61K31/517A61P35/00A61P35/02A61P29/00A61P19/02A61P17/00A61P37/00A61P37/06A61P11/00A61P25/28A61P17/06A61P3/10A61P21/04A61P25/00A61P27/02A61P7/06A61P17/14A61P1/16A61P9/00A61P15/00A61P13/10A61P15/02
CPCC07D205/04C07D207/12C07D211/46C07D211/96C07D401/04C07D401/06C07D401/12C07D401/14C07D405/06C07D473/34
Inventor 刘青松刘静王强刘飞扬王蓓蕾王傲莉王文超胡晨陈程赵铮吴宏王黎
Owner PRECEDO PHARMA CO LTD
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