DERIVATIVES OF 5-FLUORO-N- (PIRIDIN-2-IL) PIRIDIN-2-AMINA CONTAINING A SULFOXIMINE GROUP
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Abstract
5-Fluoro-N- (pyridin-2-yl) -pyridin-2-amine derivatives containing a sulfoximin group and having the general formula (1), as described and defined herein. Methods to prepare them. Its use in the treatment and / or prophylaxis of various disorders, particularly hyperproliferative disorders, infectious diseases induced by viruses and / or cardiovascular diseases. Intermediate compounds useful for preparing the compounds of the general formula (1). Claim 1: A compound of the general formula (1) wherein R¹ represents a group selected from C alquilo alkyl, C ciclo cycloalkyl, heterocyclyl, phenyl, heteroaryl, phenyl-C₁₋₃ alkyl or heteroaryl-C₁₋₃ alkyl, wherein said group is optionally substituted with one or two or three substituents, identically or differently, selected from the group consisting of hydroxy, cyano, halogen, halo C₁₋₃ alkyl, C alkoxy, C₁₋₃ fluoroalkoxy, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl-N-acetylamino, cyclic amines, -OP (O) (OH) ₂, -C (O) OH, -C (O) NH₂; R² represents a group selected from the group of formulas (2); R³, R⁴ independently represent each other, a group selected from a hydrogen atom, fluorine atom, chlorine atom, bromine atom, cyano, C₁₋₃ alkyl, C₁₋₃ alkoxy, halo-C₁₋₃ alkyl , C₁₋₃ fluoroalkoxy; R⁵ represents a group selected from a hydrogen atom, cyano, -C (O) R⁹, -C (O) OR⁹, -S (O) ₂R⁹, -C (O) NR¹⁰R¹¹, -P (O) (OR¹²) ₂ , -CH₂OP (OR¹²) ₂, C₁₋₆ alkyl, C₃₋₇ cycloalkyl, heterocyclyl, phenyl, heteroaryl, wherein said C₁₋₆ alkyl group, C₃₋₇ cycloalkyl, heterocyclyl, phenyl or heteroaryl is optionally substituted with one, two or three substituents, identically or differently, selected from halogen, hydroxy, cyano, C₁₋₃ alkyl, C₁₋₃ alkoxy, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl-N-acetylamino, cyclic amines, halo-alkyl C₁₋₃, Coro fluoroalkoxy; R⁶, R⁷ independently represent each other, a group selected from a hydrogen atom, fluorine atom, chlorine atom, C₁₋₃ alkyl, C₁₋₃ alkoxy, halo C₁₋₃ alkyl, C₁₋ fluoroalkoxy ₃; R⁸ represents a group selected from a) a C₁₋₆ alkyl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from halogen, hydroxy, -NH₂, alkylamino, dialkylamino, acetylamino, N- methyl-N-acetylamino, cyclic amines, cyano, C₁₋₃ alkyl, halo C₁₋₃ alkyl, Coro fluoroalkoxy, C₁₋₃ alkoxy, C₂₋₃ alkenyl, C₂₋₃ alkynyl, C₃₋₇ cycloalkyl, heterocyclyl, phenyl, heteroaryl, wherein said C₃₋₇ cycloalkyl, heterocyclyl, phenyl or heteroaryl group is optionally substituted with one, two or three substituents, identically or differently, selected from halogen, hydroxy, C₁₋₃ alkyl, C₁₋ alkoxy ₃, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl-N-acetylamino cyclic amines, halo-C₁₋₃ alkyl, fluoro-C₁₋₃ alkoxy; b) a C₃₋₇ cycloalkyl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group consisting of halogen, hydroxy, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl -N-acetylamino, cyclic amines, cyano, C₁₋₃ alkyl, halo C₁₋₃ alkyl, Coro fluoroalkoxy, C₁₋₃ alkoxy, C₂₋₃ alkenyl, C₂₋₃ alkynyl; c) a heterocyclyl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group consisting of halogen, hydroxy, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl -N- acetylamino, cyclic amines, cyano, C₁₋₃ alkyl, halo C₁₋₃ alkyl, Coro fluoroalkoxy, C₁₋₃ alkoxy, C₂₋₃ alkenyl, C₂₋₃ alkynyl; d) a phenyl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group consisting of halogen, hydroxy, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl-N- acetylamino, cyclic amines, cyano, C₁₋₃ alkyl, halo-C₁₋₃ alkyl, fluoro-C₁₋₃ alkoxy, C₁₋₃ alkoxy; e) a heteroaryl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group consisting of halogen, hydroxy, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl-N- acetylamino, cyclic amines, cyano, C₁₋₃ alkyl, halo-C₁₋₃ alkyl, fluoro-C₁₋₃ alkoxy, C₁₋₃ alkoxy; f) a phenyl-C₁₋₃ alkyl group, where the phenyl group thereof is optionally substituted with one or two or three substituents, identically or differently, selected from the group consisting of halogen, hydroxy, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl-N acetylamino, cyclic amines, cyano, C₁₋₃ alkyl, halo-C₁₋₃ alkyl, fluoro-C₁₋₃ alkoxy, C₁₋₃ alkoxy; g) a heteroaryl-cyc3alkyl group wherein the heteroaryl group thereof is optionally substituted with one or two or three substituents, identically or differently, selected from the group consisting of halogen, hydroxy, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl-N-acetylamino cyclic amines, cyano, C₁₋₃ alkyl, halo-C₁₋₃ alkyl, fluoro-C₁₋₃ alkoxy, C₁₋₃ alkoxy; h) a C₃₋₆-C₁₋₃ cycloalkyl group where the C₃₋₆ cycloalkyl group thereof is optionally substituted with one or two or three Substituents identically or differently, selected from halogen, C₁₋₃ alkyl, C₁₋ alkoxy ₃, halo-C₁₋₃ -alkyl fluoro-C₁₋₃-alkoxy; i) a heterocyclyl-C₁₋₃ alkyl group, wherein the heterocyclyl group thereof is optionally substituted with one or two or three substituents, identically or differently, selected from halogen, C₁₋₃ alkyl, C₁₋₃ alkoxy, halo- C₁₋₃ alkyl, Coro fluoro-alkoxy; R⁹ represents a group selected from C₁₋₆ alkyl, halo-C₁₋₃ alkyl C₃₋₇ cycloalkyl, heterocyclyl, phenyl, benzyl or heteroaryl, wherein said group is optionally substituted with one, two or three substituents, identically or differently, selected from halogen, hydroxy, C₁₋₃ alkyl, C₁₋₃ alkoxy, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl-N-acetylamino, cyclic amines, halo C₁₋₃ alkyl, fluoro-C₁₋₃ alkoxy; R¹⁰, R¹¹ independently represent each other, a group selected from hydrogen, C₁₋₆ alkyl, C₃₋₇ cycloalkyl, heterocyclyl, phenyl, benzyl or heteroaryl, wherein said C₁₋₆ alkyl group, C₃₋₇ cycloalkyl, heterocyclyl, phenyl, benzyl or heteroaryl is optionally substituted with one, two or three substituents, identically or differently, selected from halogen, hydroxy, C₁₋₃ alkyl, C₁₋₃ alkoxy, -NH₂, alkylamino, dialkylamino, acetylamino, N-methyl -N-acetylamino, cyclic amines, halo-C₁₋₃ alkyl, fluoro-C₁₋₃ alkoxy, or R¹⁰ and R¹¹, together with the nitrogen atom to which they are attached, form a cyclic amine; R² represents a group selected from hydrogen, C₁₋₄ alkyl or benzyl; and the enantiomers, diasteromers, salts, solvates or solvate salts thereof.

First Claim
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Patent Owner(s)
Patent Owner | Address |
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BAYER PHARMA AG | DELEVERKUSEN GERMANY LEVERKUSEN NORTH RHINE-WESTPHALIA |
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Inventor(s)
Inventor Name | Address |
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GERHARD DR SIEMEISTER | DE |
PHILIP DR LIENAU | DE |
DIRK DR KOSEMUND | DE |
ULRICH DR LCKING | DE |
NIELS DR BHNKE | DE |
ARNE DR SCHOLZ | DE |
ULF DR BMER | DE |
ROLF DR BOHLMANN | DE |
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