LXR modulators with bicyclic core moiety

Inventors

Gege, Christian • Kinzel, Olaf • Hambruch, Eva • Birkel, Manfred • Kremoser, Claus • Deuschle, Ulrich

Assignees

Phenex Pharmaceuticals AG • Orsobio Inc

Abstract

The present invention relates to bicyclic compounds (e.g. indoles) containing a sulfonyl moiety, which bind to the liver X receptor (LXRa and/or LXKJ3) and act preferably as inverse agonists of LXR.

Core Innovation

The disclosure concerns compounds of Formula (I), including preferred structural features and substitution patterns. The description includes extensive definitional material for substituent concepts used in the Formula (I) framework, together with tautomerism, solvate forms, isotopic labeling, and deuterated analogs.

Carboxylic acid-containing variants of the Formula (I) compounds are specifically addressed, including optional conjugates. The disclosure indicates carboxylic acid moiety variants optionally conjugated with glycine or tauro, described as glycine conjugate and tauro conjugate. Representative compound selections consistent with Formula (I) include exemplified carboxylic acid structures, and the disclosure frames the compounds as LXR-modulator compounds.

The patent content also provides examples and analytical characterization for related substituted heteroaromatic compounds, including indole-based biphenyl carboxylates/sulfonamides, fluorinated sulfonamide-containing aromatic compounds, brominated/halogenated sulfonyl-indole derivatives, and other labeled intermediates and final compounds. The described examples include 1H NMR and MS data, structural depictions, stereochemical forms, atropisomers, pharmaceutically acceptable salts, and multiple sequences progressing through intermediates to final compounds.

Claims Coverage

The provided independent claims are broad and are directed to a compound or a pharmaceutically acceptable salt thereof. Across the supplied claim excerpts, no additional inventive feature limitations are explicitly stated beyond the compound/salt scope.

Across the provided claim text, the claimed subject matter is defined at the level of a compound and pharmaceutically acceptable salt forms, without further extractable structural or functional limitations in the independent claims shown.

Stated Advantages

Documented Applications