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Novel crystalline salt form of 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazin-2-yl)amino)-2h-pyrido[3,2-b][1,4]oxazin-3(4H)-one for medical application

A trimethoxyphenyl, dimethyl technology, applied in the fields of osteoporosis, salt form of the compound and its crystal form, osteoarthritis and osteochondrosis, can solve the problem of not being able to obtain drugs based on Src kinase inhibitors And other issues

Active Publication Date: 2019-03-26
OBSHCHESTVO S OGRANICHENNOJ OTVETABTVENNOSTJU MOLEKULJARNYE TEKHNOLOGII
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, drugs based on Src kinase inhibitors are not yet available in clinical practice for the treatment of musculoskeletal disorders

Method used

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  • Novel crystalline salt form of 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazin-2-yl)amino)-2h-pyrido[3,2-b][1,4]oxazin-3(4H)-one for medical application
  • Novel crystalline salt form of 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazin-2-yl)amino)-2h-pyrido[3,2-b][1,4]oxazin-3(4H)-one for medical application
  • Novel crystalline salt form of 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazin-2-yl)amino)-2h-pyrido[3,2-b][1,4]oxazin-3(4H)-one for medical application

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Embodiment Construction

[0037] As a result of the research carried out, it was found that 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazine-2 -yl)amino)-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one (hereinafter referred to as compound 1) at the half maximal inhibitory concentration in the nanomolar range to The Src-kinase family, in particular, has regulatory activity on the human c-Src kinase. At the same time, it was determined that the pharmacokinetics of this compound are unacceptable for use in clinical practice as a drug for the treatment of diseases associated with abnormal kinase activity which leads to abnormal bone and cartilage metabolism. Specifically, when administered orally in rats at a dose of 30 mg / kg, pharmacokinetic studies of Compound 1 showed that the maximum concentration in animal plasma was 100-fold lower than the minimum effective concentration determined in efficacy studies (see Example section details).

[0038] This problem was solved by developing and preparing...

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Abstract

The invention relates to the chemistry of organic compounds, to pharmacology and to medicine, and pertains to the prevention and treatment of human and animal diseases associated with metabolic disorders of bone tissues and / or cartilage tissues, particularly diseases of the musculoskeletal system, such as osteoarthritis or osteoporosis, using a novel salt form of 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazin-2-yl)amino)-2H-pyrido[3,2-B][1,4]oxazin-3(4H)-one. A salt of the present compound with 4-methylbenzenesulfonic acid, (I) including the hydrates and solvates thereof, andpolymorphic modifications of the salt, hydrates and solvates, is characterized by increased effectiveness of inhibiting Src-family kinases, Syk kinase and also other therapeutically-significant kinases, and by acceptable pharmacokinetic parameters. The present invention also relates to pharmaceutical compositions containing a therapeutically-effective amount of the salt according to the invention.

Description

technical field [0001] The present invention relates to organic compound chemistry, pharmacology and medicine, namely to salt forms of compounds and their crystalline (polymorphic) forms, which are promising for the treatment of musculoskeletal diseases associated with disorders of bone and / or cartilage metabolism, in particular Osteoporosis, osteoarthritis and osteochondrosis. Background technique [0002] The increasing incidence of musculoskeletal disorders such as osteoporosis, osteoarthritis and osteochondrosis has become increasingly important. Many publications on the subject reflect this. Despite the efforts of experts in different fields, this problem is still far from being solved. [0003] Osteoporosis is the most common human bone disease. It is a chronic systemic disease characterized by decreased bone mass and progressive deterioration of the microarchitecture of bone tissue, which can lead to reduced bone strength and increased risk of pathological fracture...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/04A61K31/5383A61P19/02
CPCA61K31/5383C07D498/04A61P19/00A61P19/02C07B2200/13
Inventor V·E·内博林F·N·诺维科夫G·G·舍勒夫O·V·斯特戈纳夫V·S·斯特罗洛夫I·Y·蒂托夫
Owner OBSHCHESTVO S OGRANICHENNOJ OTVETABTVENNOSTJU MOLEKULJARNYE TEKHNOLOGII
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