ANELLATED CABAMOYLAZAHETEROCYCLES, FOCUSED LIBRARY, PHARMACEUTICAL COMPOSITION AND METHOD FOR ITS PREPARING

• Main Authors: IVASHCHENKO ALEKSANDR VASIL'EVICH, KHVAT ALEKSANDR VIKTOROVICH, KISEL' VLADIMIR MIKHAJLOVICH, TSYRUL'NIKOV SERGEJ ALEKSANDROVICH, LOSEVA MARINA VASIL'EVNA, PARCHINSKIJ VLADISLAV ZENONOVICH, TKACHENKO SERGEJ EVGEN'EVICH, RYZHOVA ELENA ALEKSANDROVNA, IL'IN ALEKSEJ PETROVICH, OKUN' IL'JA MATUSOVICH, VVEDENSKIJ VLADIMIR JUR'EVICH, KISELEV ALEKSANDR SERGEEVICH, KRAVCHENKO DMITRIJ VLADIMIROVICH
• Format: Patent
• Language: English; Russian
• Published: 20.08.2006
• Subjects: 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

FIELD: organic chemistry, biochemistry, medicine, pharmacy. ^ SUBSTANCE: invention relates to novel anellated carbamoylazaheterocycles of the general formula (1) that possess inhibitory property of kinase activity and eliciting, for example, an anticancer activity. Also, compounds can be used as agonists, antagonists, receptor modulating agents, antiparasitic and antibacterial agents. Also, invention relates to a method for synthesis of compounds of the formula (1), a pharmaceutical composition based on thereof and a focused library for assay of leader-compounds. In compounds of the general formula (1) W represents 6-oxopiperazine, [1,4]-thiazepane, [1,4]-oxazepane or [1,4]-diazepane cycle anellated with at least one optionally substituted and optionally condensed heterocycle or carbocycle Q; Q represents optionally substituted thiophene, optionally substituted pyrrole, optionally substituted imidazole, optionally substituted thiazole, optionally substituted pyrrolidine, optionally substituted indole, optionally substituted benzofuran, optionally substituted pyridine, optionally substituted quinoline, optionally substituted benzene or optionally substituted naphthalene cycle; R1, R2 and R represent independently of each another hydrogen atom, inert substitute, optionally substituted (C1-C6)-alkyl, optionally substituted (C3-C8)-cycloalkyl, optionally substituted phenyl, optionally substituted aryl, optionally substituted heterocyclyl. ^ EFFECT: improved preparing method, valuable biological and medicinal properties of compounds and pharmaceutical composition. ^ 15 cl, 5 tbl, 6 ex