STYRYL QUINAZOLINE DERIVATIVES AS PHARMACEUTICALLY ACTIVE AGENTS

摘要

The present invention relates to styryl quinazoline derivatives of the general formula (I) and pharmaceutically acceptable solvates, hydrates, salts, regioisomeric and polymorphic forms thereof as well as pharmaceutical compositions containing at least one of the described compounds as pharmaceutically active agent. The compounds have been identified as new drug candidates for the prevention and/or treatment of diseases related to disfunction(s) of hematopoiesis and cancer or any other form of neo- or hyperplasias related to Fms-like tyrosine kinase 3 (FLT3) containing Internal Tandem Duplications (ITD), especially in the case of myeloid leukemia. The compounds have been also identified as new drug candidates as antibacterial agents (having bactericidal or bacteriostatic activity) which can be used for the prevention and/or treatment of bacterial infectious diseases.

主权项

1. Compounds of general formula (I) and pharmaceutically acceptable salts, solvates, hydrates, regioisomeric and polymorphic forms thereof, Wherein R1 is N(R5)(R6), wherein R5 and R6 are independently selected from the group of hydrogen, alkyl or ALK-N(R7)(R8), wherein
ALK is an alkanediyl group andR7 and R8 are independently selected from the group of hydrogen, alkyl, alkylcarbonyl and alkoxycarbonyl; orR7 and R8 taken together with the adjacent N form a saturated heterocyclyl which is optionally substituted with alkyl; or R5 and R6 taken together with the adjacent N may form a heterocyclyl optionally substituted heterocyclyl-alkyl or a cycloketal group is joined to it; R2 is hydrogen or halogen; R3 and R4 are independently selected from the group of hydrogen, halogen, alkoxy or nitro group; or R3 and R4 together with the carbon atoms they attached to may form an aryl fused to the quinazoline ring; Q is aryl optionally mono or polysubstituted with halogen, alkyl, dialkylamine, alkoxy, alkylsulfanyl, alkylsulfinyl, or alkylsulfonyl; or heteroaryl group.