Fused thiophene and thiazole derivatives as ROR gamma modulators

Fused thiophene and thiazole derivatives are developed to modulate RORγ activity, addressing the limitations of existing agents by specifically inhibiting RORγ and reducing IL-17 production, offering a promising treatment for autoimmune and inflammatory diseases.

WO2015101928A1 Publication Date: 2015-07-09AURIGENE ONCOLOGY LIMITED
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Patent Information

Application Number
PCT/IB2014/067408
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2014-01-21
Filing Date
2014-12-30
Publication Date
2015-07-09

AI Technical Summary

Technical Problem

Current therapeutic agents are inadequate for effectively modulating the activity of Retinoic acid receptor-related orphan receptor gamma (RORγ), which is a key mediator in various autoimmune and inflammatory diseases, including rheumatoid arthritis, psoriasis, and asthma, due to limited selectivity and efficacy.

Method used

Development of fused thiophene and thiazole derivatives that act as RORγ modulators, specifically designed to inhibit the activity of RORγ, thereby reducing the production of inflammatory cytokines like IL-17, which are involved in the pathogenesis of these diseases.

Benefits of technology

The fused thiophene and thiazole derivatives effectively inhibit RORγ activity, providing a therapeutic benefit in treating autoimmune and inflammatory disorders by reducing IL-17 levels, thus offering a new approach for managing conditions such as rheumatoid arthritis, psoriasis, and asthma.

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Abstract

The present invention provides fused thiophene and thiazole derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; in which R1, R2, R3, R4, R5, R6, R7, X1, X2, L, m, n and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in disease(s) or disorder(s) where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the fused thiophene and thiazole derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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