SUBSTITUTED 5-SULFO-2-OXO-1,2-DIHYDROQUINOLINE 4-CARBOXYLIC ACIDS AND THEIR DERIVATIVES (VARIANTS) AND FOCUSED LIBRARY Russian patent published in 2005 - IPC

FIELD: organic chemistry, chemical technology, biochemistry.

SUBSTANCE: invention relates to new substituted 6-sulfo-2-oxo-1,2-dihydroquinoline 4-carboxylic acids and their derivatives of the general formula (1):

eliciting physiological activity, in particular, capacity to inhibit activity of protein kinase, and also to intermediate compounds for their preparing and to the focused library, for search compound-leaders and medicinal candidates obtaining on the basis of screening combinatory libraries. In compounds of the general formula (1) R¹ represents hydrogen atom or electrophilic substitute; R² represents hydrogen atom or inert substitute; R³ represents optionally substituted hydroxyl group, optionally substituted amino-group and optionally substituted azaheterocycle; R⁴ represents optionally substituted amino-group and optionally substituted azaheterocycle. Also, invention relates to compounds of the general formula (1.1):

wherein R¹, R² and R³ have above given values; R⁵ represents hydroxyl or chlorine atom, and to their applying for preparing compounds of the general formula (1.2):

and (1.3):

wherein R¹, R² and R⁴ have above given values.

EFFECT: valuable medicinal and biochemical properties of compounds.

6 cl, 4 tbl, 5 ex