METHYL MODIFYING ENZYME MODULATORS, COMPOSITIONS AND USES THEREOF

Abstract

Claim 1: A compound of formula (1), or a pharmaceutically acceptable salt thereof, characterized in that: R¹ is halo, -SC₁₋₄ alkyl, -SC₃₋₇ cycloalkyl, or -S[halo-C₁₋₄ alkyl]; X is CH or N; R² is hydrogen, halo, C₁₋₄ alkyl, or halo-C₁₋₄ alkyl; R³ is halo, C₁₋₄ alkyl, or halo-C₁₋₄ alkyl; R⁴ is a 4-7 membered C₃₋₇ cycloalkyl or heterocyclyl, each of which is optionally substituted with 1 to 3 groups selected from halo, C₁₋₄ alkyl, halo-C₁₋₄ alkyl, C₁₋₄ alkoxy, halo-C₁₋₄ alkoxy and -NRᵃRᵇ; Rᵃ is hydrogen, C₁₋₄ alkyl, or halo-C₁₋₄ alkyl; Rᵇ is C₁₋₄ alkyl, halo-C₁₋₄ alkyl, or 4-7 membered heterocyclyl, wherein the heterocyclyl is optionally substituted with 1 to 3 groups selected from halo, C₁₋₄ alkyl, halo-C₁₋₄ alkyl, C₁₋₄ alkoxy, and halo-C₁₋₄ alkoxy;or Rᵃ and Rᵇ together with the nitrogen atom to which they are attached form a 4-7 membered heterocycle optionally substituted with 1 to 3 groups selected from halo, C₁₋₄ alkyl, halo-C₁₋₄ alkyl and -ORᶜ; Rᶜ is C₁₋₄ alkyl, halo-C₁₋₄ alkyl, or C₃₋₇ cycloalkyl; and R⁵ is halo, C₁₋₄ alkyl, or halo-C₁₋₄ alkyl.;

Claims

1. A compound of Formula I: FORMULA 1, or a pharmaceutically acceptable salt thereof, characterized in that: R1 is halo, -S(C1-4)alkyl, -S(C3-7)cycloalkyl, or -S[halo(C1-4)alkyl]; X is CH or N; R2 is hydrogen, halo, (C1-4)alkyl, or halo(C1-4)alkyl; R3 is halo, (C1-4)alkyl, or halo(C1-4)alkyl; R4 is (C3-7)cycloalkyl or 4-7 membered heterocyclyl, each of which is optionally substituted with 1 to 3 groups selected from halo, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkoxy, halo(C1-4)alkoxy and -NR to R b ; R a is hydrogen, (C1-4)alkyl, or halo(C1-4)alkyl; R b is (C1-4)alkyl, halo(C1-4)alkyl, or 4-7 membered heterocyclyl, wherein the heterocyclyl is optionally substituted with 1 to 3 groups selected from halo, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkoxy, and halo(C1-4)alkoxy;or R a and R b together with the nitrogen atom to which they are attached form a 4-7 membered heterocycle optionally substituted with 1 to 3 groups selected from halo, (C1-4)alkyl, halo(C1-4)alkyl and -OR c; R c is (C1-4)alkyl, halo(C1-4)alkyl, or (C3-7)cycloalkyl; and R 5 is halo, (C1-4)alkyl, or halo(C1-4)alkyl. 26 Claims follow;