| abstract |
These compounds are selective inhibitors of the LPA receptor. Claim 1: A compound characterized by the formula (1), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein R² is independently selected from H and C₁₋₄ alkyl substituted with 1 - 5 R⁹; R¹³ is independently selected from H, D and C₁₋₄ alkyl substituted with 1-3 R⁹; R³ and R⁴ are independently selected from H, C₁₋₇ alkyl substituted with 1-3 R⁹, - (CR⁷R⁷) ʳ-C₃₋₈ cycloalkyl substituted with 1-3 R⁸, - (CR⁷R⁷) ʳ-aryl substituted with 1-3 R⁸ , C₂₋₇ alkenyl substituted with 1-3 R⁹, heterocyclic ring - (CR⁷R⁷) ʳ 5-6 members substituted with 1-3 R⁹, heteroaryl ring - (CR⁷R⁷) ʳ 5-6 members substituted with 1-3 R⁸ , or R³ and R⁴ combine with the N to which they are attached to form a 4-9 membered heterocyclic ring substituted with 1-3 R⁸; X¹, X², X³ and X⁴ are independently selected from CR⁵ and N; provided that no more than two of X¹, X², X³ or X⁴ are N; R⁵ is independently selected from H, F, Cl, OR⁷, CN, N (R⁷) ₂, C₁₋₄, alkyl substituted with 1-5 R⁹, C₁₋₄ alkoxy substituted with 1-5 R⁹ and C₁₋₄ heteroalkyl substituted with 1-5 R⁹; R⁶ is C₃₋₈ cycloalkyl which is substituted with R¹⁰ and (-CH₂) ₀₋₁R¹¹; R⁷ is independently selected from H, C₁₋₄ alkyl and C₃₋₆ cycloalkyl; or R⁷ and R⁷, together with the carbon atom to which they are attached, form a C₃₋₆ cycloalkyl ring; R⁸ is independently selected from H, D, C₁₋₆ alkyl substituted with 1-5 R⁹, C₂₋₆ alkenyl, C₂₋₆ alkynyl, phenyl, - (CH₂) ʳ-C₃₋₆ cycloalkyl, F, Cl, Br, CN , COOH and C₁₋₄ alkoxy; R⁹ is independently selected from H, D, F, Cl, NH₂, OH, OC₁₋₅ alkyl, C₁₋₅ alkyl, C₁₋₅ heteroalkyl C₃₋₆ cycloalkyl and phenyl, wherein when R⁹ is Cl, NH₂ or OH, no it is substituted in C₁ of the alkyl to which it is attached; R¹⁰ is independently selected from H, D, C₁₋₄ alkyl, F, Cl, Br, OR⁷, NHC (= O) OR⁷ and NHC (= O) OR⁷; R¹¹ is independently selected from H, CN, -C (= O) R¹², tetrazolyl, a moiety of formula (2) and a moiety of formula (3); R¹² is independently selected from OH, OC₁₋₄ alkyl, NH₂, NHCH₂CH₂SO₃H and NHSO₂C₁₋₄ alkyl; r is independently selected from 0, 1, 2, 3 and 4; and n is selected from 1, 2, 3 or 4. |