| abstract |
Claim 1: A compound of the formula (1), wherein n is selected from 0, 1 and 2; m is selected from 0, 1 and 2; X is selected from O and NR⁶; wherein R⁶ is C₁₋₄ alkyl; Y¹ is selected from N and CR⁷; wherein R⁷ is selected from hydrogen and C₁₋₄ alkyl; R¹ is hydrogen; R² is selected from hydrogen and halo; R³ is selected from -CH₂CH₂R⁸ᵇ and -CR⁸ᵃ = CR⁸ᵃR⁸ᵇ; wherein each R⁸ᵃ is independently selected from hydrogen, fluorine and C₁₋₄ alkyl; and R⁸ᵇ is selected from -C (O) OR⁹ᵃ, -C (O) NR⁹ᵃR⁹ᵇ, -C (O) NHOR⁹ᵃ, -C (O) X²R⁹ᵃ and a 5-6 membered heteroaryl selected from the group of formulas ( 2) where the dotted line indicates the fixation point with -CH₂CH₂ or -CR⁸ᵃ = CR⁸ᵃ of R³; wherein X² is C₁₋₄ alkylene; R⁹ᵃ and R⁹ᵇ are independently selected from hydrogen, C₁₋₄ alkyl, C₁₋₄ hydroxyl-substituted alkyl, C₁₋₄ halo-substituted alkyl and -X⁴R¹⁰; wherein X⁴ is selected from a bond and C₁₋₃ alkylene; and R¹⁰ is a 4-6 membered saturated ring containing 1 to 3 atoms independently selected from O, N and S; wherein said R⁸ᵇ heteroaryl is unsubstituted or substituted by 1 to 3 groups independently selected from C₁₋₄ alkyl and C₃₋₈ cycloalkyl; R⁴ is selected from hydrogen, C₁₋₄ alkyl, halo and C₁₋₃ alkoxy; R⁵ is selected from C₆₋₁₀ aryl and a 5-6 membered heteroaryl selected from the group of formulas (3) wherein the dotted line indicates the point of fixation with the benzothiophene core; wherein said C₆₋₁₀ aryl or R⁵ heteroaryl is substituted by 1 to 3 groups selected from -X³-R⁵ᵃ and R⁵ᵃ; wherein X³ is methylene; R⁵ᵃ is selected from hydroxyl, amino, C₁₋₄ alkyl, halo, nitro, cyano, halo-substituted C₁₋₄ alkyl, C₁₋₄ cyano-substituted alkyl, C₁₋₄ hydroxyl-substituted alkyl, C₁₋₄ halo alkoxy -substituted, C₁₋₄ alkoxy, -SF₅, -NR¹¹ᵃR¹¹ᵇ, -C (O) R¹¹ᵃ, C₃₋₈ cycloalkyl and a saturated, unsaturated or partially saturated 4-7 membered ring containing one to 4 heteroatoms or groups selected from from O, NH, C (O) and S (O) ₀₋₂; wherein R¹¹ᵃ and R¹¹ᵇ are independently selected from hydrogen and C₁₋₄ alkyl; or R¹¹ᵃ and R¹¹ᵇ together with the nitrogen to which they are attached form a 4-7 membered saturated ring containing another heteroatom or group selected from O, NH, and S (O) ₀₋₂; wherein said 4-7 R anillo member ring may be unsubstituted or substituted by C₁₋₄ alkyl; or a pharmaceutically acceptable salt thereof. |