A NEW CRYSTAL 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]OXAZINE-3(4H)-ONE FOR HUMAN USE

A NEW CRYSTAL 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]OXAZINE-3(4H)-ONE FOR HUMAN USE

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, s...

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Hauptverfasser: NEBOLSIN, VLADIMIR EVGENIEVICH, CHILOV, GERMES GRIGORIEVICH, STROILOV, VIKTOR SERGEEVICH, STROGANOV, OLEG VALENTINOVICH, TITOV, ILYA YURIEVICH, NOVIKOV, FEDOR NIKOLAEVICH
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Zusammenfassung: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, and polymorphic 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. L'invention concerne la chimie des composés organiques, la pharmacologie et la médecine humaine et concerne le traitement et la prévention des maladies des humains et des animaux associées aux troubles du métabolisme des tissus osseux et/ou cartilagineux et notamment des maladies de l'appareil locomoteur telles que l'ostéoarthrite ou l'ostéoporose, avec une nouvelle formule de sel 2,2-diméthyl-6-((4-((3,4,5-triméthoxyphényl)amino)-1,3,5-triazin-2-yl)amino)-2H-pyrido[3,2-B][1,4]oxazin-3(4H)-on. Le sel de ce composé avec un acide 4-méthylbenzolsulphonique (I), y compris ses hydrates, solvates et modifications polymorphes de sels, hydrates et solvates est caractérisé par une efficacité plus élevée en termes d'inhibitions de kinases des familles de kinases Src et Syk et d'autres kinases thérapeutiquement efficaces ainsi que des paramètres pharmacocinétiques acceptables. La présente invention concerne également des compositions pharmaceutiques contenant une quantité thérapeutiquement efficace de sel de l'invention.