THIAZOLYLDIHYDROINDAZOLES Russian patent published in 2010 - IPC C07D513/04 C07D417/06 C07D277/82 A61K31/429 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds which possess inhibiting properties with respect to PI3-kinase of general formula (1), where R¹ is selected from group, including -NHR^C, -NHC(O)R^c, -NHC(O)OR^c, -NHC(O)NR^cR^c and -NHC(O)SR^c, R² stands for residue, optionally substituted with one or two substituents R⁴, selected from group, including C₁-C₆alkyl, C₃-C₈cycloalkyl, 5-6-member heterocycloalkyl with one heteroatom, selected from nitrogen and sulphur, phenyl, benzyl and 5-6-member heteroaryl, including 1-2 nitrogen atoms, R³ stands for optionally substituted with one or several substituents R^e and/or R^f residue, selected from group, including phenyl and 5-6-member heteroaryl with 1-3 heteroatoms, selected from nitrogen and oxygen, R⁴ represents residue, selected from group, including R^a, R^b, and substituted with one or several identical or different substituents R^c and/or R^b , R^a in each case is independently selected from group, including C₁-C₆alkyl, phenyl, 4-7-member heterocycloalkyl with 1-2 heteroatoms, selected from nitrogen and oxygen, and 9-member heteroaryl with one atom of nitrogen as heteroatom, R^b in each case is independently selected from group, including =O, -OR^c, -NR^CR^C, halogen, -CF₃, -CN, -S(O)R^c, -C(O)R^c, -C(O)OR^c, -C(O)NR^cR^c, -C(O)N(R^g)NR^cR^c, -N(R^g)C(O)R^c, -N(R^g)S(O)₂R^c, -N(R^g)S(O)₂NR^cR^c, -N(R^g)C(O)OR^c and -N(R^g)C(O)NR^cR^c, R^C in each case independently represents hydrogen or optionally substituted with one or two identical or different substituents R and/or R^e residue, selected from group, including C₁-C₆alkyl, C₃-C₈cycloalkyl, C₆-C₉aryl, 4-7-member heterocycloalkyl with 1-2 heteroatoms, selected from nitrogen and oxygen, and 5-6-member heteroaryl with 1-2 heteroatoms, selected from nitrogen, oxygen and sulphur, R^d in each case independently represents hydrogen or optionally substituted with one or two identical or different substituents R^e and/or R^f residue, selected from group, including C₁-C₆alkyl, C₃-C₈cycloalkyl, phenyl, 4-7-member heterocycloalkyl with 1-2 heteroatoms, selected from nitrogen and oxygen, and 5-10-member heteroaryl with one atom of nitrogen, R^e in each case is independently selected from group, including =O, -OR^f, -SR^f, -NR^fR^f, -CN, -S(O)₂R^f, -C(O)R^f, -C(O)OR^f, -C(O)NR^fR^f and -OC(O)R^f, R^f in each case independently represents hydrogen or optionally substituted with one or two identical or different substituents R^g residue, selected from group, including C₁-C₆alkyl, C₃-C₈cycloalkyl, phenyl, 4-7-member heterocycloalkyl with 1-2 heteroatoms, selected from nitrogen and oxygen and 5-6-member heteroaryl with one heteroatom, selected from nitrogen and sulphur, R^g in each case independently represents hydrogen, C₁-C₆alkyl, C₃-C₈cycloalkyl and 4-7-member heterocycloalkyl with one nitrogen as heteroatom, as well as to their pharmaceutically harmless acid-additive salts. Invention also relates to compounds, used as intermediate products of synthesis of formula (I) compounds, pharmaceutical composition and application of compounds for preparation of medication, possessing properties of PI3-kinase inhibitor.

EFFECT: elaborated are novel compounds, which possess properties of PI3-kinase inhibitor.

11 cl, 9 ex