Importance

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Abstract

Compounds of formula (I) wherein: X is —O—, —S(O)_r—, —CH₂—, or —NR—, wherein r is 0, 1, or 2; X¹, X², and X⁵ are each independently CR⁷ or N; one of X³ or X⁴ is C and is attached by a single bond to -L-, and the other is CR⁷ or N, provided that no more than three of X¹, X², X³, X or X⁵ are N; Ring A is monocyclic C_5-6scycloalkyl or a 5- to 6-membered monocyclic heterocyclyl comprising from 1 to 5 heteroatoms independently selected from N, S, or O; wherein Ring A is further optionally substituted with from 1 to 3 R⁴; provided that Ring A is not morpholinyl, thiomorpholinyl or tetrahydro-2H-pyranyl; L is a bond, —O—, —NR—, —S(O)_n—, —CH₂—, or —C(O)—, wherein n is 0, 1, or 2; 1 2 L¹ is an C_1-8alkylene, C_3-scycloalkylene, —CH₂-L²-, or a 3- to 8-membered heterocyclylene comprising 1 to 5; R¹ is C_6-20alkyl or a monocyclic C_3-8cycloalkyl; wherein said C_3-8cycloalkyl is substituted with at least one R⁶ and may be optionally substituted with from 1 to 5 additional R⁶ substituents, wherein R⁶ for each occurrence is independently selected; and R² is —C(O)OR³, —C(O)N(R³)—S(O)₂R³, —S(O)₂OR³, —C(O)NHC(O)R³, —Si(O)OH, —B(OH)₂, —N(R³)S(O)₂R³, —S(O)₂N(R³)₂, —O—P(O)(OR³)₂, or —P(O)(OR³)₂, —CN, —S(O)₂NHC(O)R³, —C(O)NHS(O)₂R3, —C(O)NHOH, —C(O)NHCN, —CH(CF₃)OH, —C(CF₃)₂OH, or a selected heteroaryl or heterocyclyl; and pharmaceutically acceptable salts thereof, can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).

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First Claim