| abstract |
Claim 1: A compound of formula (1) wherein R¹ᵃ and R¹ᵇ are independently from each other C₁₋₆ alkyl optionally substituted with between 1 and 5 R²⁰ groups; R²ᵃ and R²ᵇ are independently of each other H or halo; R³ is boronic acid or halo; or -C (O) ORᵃ, -NHC (O) ORᵃ, -NHS (O) ₂Rᵃ, or -S (O) ₂NRᵃRᵇ; or is selected from the group consisting of C₁₋₁₀ alkyl, C₁₋₁₀ alkoxy, amino, C₅₋₁₀ aryl, C₆₋₂₀ arylalkyl, C₁₋₁₀ heteroalkyl, C₅₋₁₀ heteroaryl, and C₆₋₁₀ heteroarylalkyl, each of which is optionally substituted with between 1 and 5 R²⁰ groups; one of R⁴ᵃ and R⁴ᵇ is selected from the group consisting of H and C₁₋₆ alkyl optionally substituted with between 1 and 5 R²⁰ groups, and the other is absent; R⁵ is -C (O) ORᵃ, -NHC (O) ORᵃ, -NHS (O) ₂Rᵃ, or -S (O) ₂NRᵃRᵇ; or is selected from the group consisting of H, C₁₋₁₀ alkyl, C₁₋₁₀ haloalkyl, C₁₋₁₀ alkoxy, amino, C₅₋₁₀ aryl, C₆₋₂₀ arylalkyl, C₁₋₁₀ heteroalkyl, C₅₋₁₀ heteroaryl, and heteroarylalkyl C₆₋₂₀, each of which is optionally substituted with between 1 and 5 R²⁰ groups; each Rᵃ and Rᵇ is independently selected from the group consisting of H, C₁₋₁₀ alkyl, C₅₋₁₀ aryl, C₆₋₂₀ arylalkyl, C₁₋₁₀ heteroalkyl, C₁₋₁₀ heteroaryl, and C₆₋₂₀ heteroarylalkyl, each of which it is optionally substituted with between 1 and 5 R²⁰ groups; and each R²⁰ is independently selected from the group consisting of acyl, C₁₋₁₀ alkyl, C₁₋₁₀ alkoxy, amino, amido, amidino, C₅₋₁₀ aryl, C₆₋₂₀ arylalkyl, azido, carbamoyl, carboxyl, ester of carboxyl, cyano, guanidino, halo, C₁₋₁₀ haloalkyl, C hetero heteroalkyl, C hetero heteroaryl, C₆₋₂₀ heteroarylalkyl, hydroxy, hydrazino, hydroxyl, imino, oxo, nitro, sulfinyl, sulfonic acid, sulfonyl, thiocyanate, thiol , and tiona; wherein the groups C₁₋₁₀ alkyl, C₅₋₁₀ aryl, C₆₋₂₀ arylalkyl, C₁₋₁₀ heteroalkyl, C₅₋₁₀ heteroaryl, and C₆₋₂₀ heteroarylalkyl are optionally substituted with between 1 and 3 substituents independently selected from C₁₋ alkyl ₆, C₅₋₁₀ aryl, halo, C₁₋₆ haloalkyl, cyano, hydroxyl, and C₁₋₆ alkoxy; or a pharmaceutically acceptable salt thereof. |