QUINOLINE DERIVATIVES Russian patent published in 2012 - IPC C07D401/12 C07D215/22 C07D403/12 C07D417/12 C07D413/12 A61K31/4709 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to quinoline derivatives of formula I

, or to its pharmaceutically acceptable salts, wherein X¹ represents O; p represents 0, 1 or 2; each group R¹ which can be identical or different and which can be located only in positions of 6- and/or 7-quinoline ring, specified in halogen, cyano, carboxy, (1-6C)alkoxycarbonyl, carbamoyl, (1-6C)alkoxy, N-(1-6C)alkylcarbamoyl, N,N-di-[(1-6C)alkyl]carbamoyl, or in a group of formula: Q¹-X²-, wherein X² represents CO and Q¹ represents pyrrolidine, q represents 0 or 1; R² represents (1-6C)alkoxy; R³ represents hydrogen or (1-6C)alkyl; R⁴ represents hydrogen; R⁵ represents hydrogen, methyl, ethyl, propyl, allyl, 2-propynyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, 3-fluoropropyl, 3,3-difluoropropyl, 3,3,3-trifluoropropyl, 2-hydroxyethyl, 3-hydroxypropyl, 2-methoxyethyl, 3-methoxypropyl, cyanomethyl, 2-cyanoethyl or 3-cyanopropyl; the ring A represents a 5-membor monocyclic heteroaryl ring with up to three ring heteroatoms specified in oxygen, nitrogen and sulphur; r represents 0, 1 or 2; and each group R⁶ which can be identical or different is specified in amino, (1-6C)alkyl, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, or in a group of formula: -X⁶-R¹⁵ wherein X⁶ represents a single link and R¹⁵ represents (1-6C)alkoxy-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(1-6C)alkyl or in a group of formula: -X⁷-Q³ wherein X⁷ represents C(R¹⁷)₂N(R¹⁷) wherein each R¹⁷ represents hydrogen and Q³ represents (3-8C)cycloalkyl, and wherein any CH₂ group within the R⁶ group optionally carries a hydroxy group on each said group. Also, the invention refers to methods for making the compound of formula I, to a pharmaceutical composition on the basis of the compound of formula I, to applying the compound of formula I and the combinations on the basis of the compound of formula I and additional anticancer drugs.

EFFECT: there are produced new quinoline derivatives effective in treating diabetic retinopathy and disturbed cell proliferation.

15 cl, 6 tbl, 32 ex