SUBSTITUTED 7-SULFONYL-BENZO[B][1,4]DIAZEPINES (VARIANTS), METHODS FOR THEIR PREPARING (VARIANTS), FOCUSED LIBRARY AND PHARMACEUTICAL COMPOSITION Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to new substituted 7-sulfonyl-benzo[b][1,4]diazepines of the general formula (1) , their pharmaceutically acceptable salts, N-oxides or hydrates that elicit properties of a protein kinase inhibitor that can be used in pharmaceutical industry. In compounds of the general formula (1) R¹ and R² represent independently of one another hydrogen atom, inert substitute, optionally substituted carboxymethyl group, optionally substituted carbamoylmethyl group; R³ and R⁴ represent independently of one another hydrogen atom or inert substituted, or R³ and R⁴ in common with carbon atom to which they are bound form optionally substituted (C₃-C₇)-cycloalkyl, optionally substituted (C₄-C₇)-heterocyclyl or optionally substituted ethylene group; R⁵ represents optionally substituted amino-group or optionally substituted azaheterocyclyl. Also, invention relates to sulfochlorides of the general formula (2) that are used for preparing compound of the formula (1), and to methods for preparing compounds of general formulae (1) and (2). Also, invention relates to a pharmaceutical composition in form of tablets, capsules or injection formulations placed into pharmaceutically acceptable package, and to the focused library for the search of biologically active compound-leaders.

EFFECT: improved preparing method, valuable medicinal and biochemical properties of compounds.

7 cl, 2 sch, 1 tbl, 3 ex