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Publication Number
US-11311541-B2
Publication Date
2022-04-26
Expiration Date
Abstract
The invention relates to treatment of graft versus host disease (GVHD) using compounds that inhibit ROCK2. In preferred aspects, the present invention provides methods for the treatment of GVHD, including chronic GVHD (cGVHD) using compounds having the formulae 1-XXV, as set forth herein.
Core Innovation
The invention relates to ROCK2-inhibiting chemical compounds and their use for treating graft versus host disease (GVHD), including chronic GVHD (cGVHD) and sclerodermatous chronic graft versus host disease. The compounds are defined by broad structural formulas with extensive variable definitions for substituents and ring systems, including indazol-5-amine, pyrimidinyl, isoindolinyl, and related heteroaryl and heterocyclic scaffold elements.
The disclosed chemical scope includes multiple named formulas and specific example scaffold formulas, together with pharmaceutically acceptable salts and stereoisomer embodiments. The examples describe substituted pyrimidinyl–indazole–phenoxy acetamide analogs, indazolyl–pyrimidinyl–isoindolinyl series, and related halogenated or substituted pyrimidine variants.
The invention provides a method of treating sclerodermatous chronic graft versus host disease in a subject in need thereof by administering an effective amount of a compound of Formula, or a pharmaceutically acceptable salt thereof. The document also describes pharmacological characterization and immunological/therapeutic outcomes in connection with the disease context, including cytokine secretion and signaling pathway changes and effects on chronic GVHD-related pathology and pulmonary dysfunction in murine models.
Claims Coverage
The provided material identifies one independent claim directed to treatment of sclerodermatous chronic graft versus host disease, with one dependent refinement. The independent claim uses one inventive feature: administering an effective amount of a Formula compound, or a pharmaceutically acceptable salt, and the dependent refinement adds co-administration with a second agent.
Treating sclerodermatous chronic graft versus host disease by administering a compound of formula
A method of treating sclerodermatous chronic graft versus host disease in a subject in need thereof by administering an effective amount of a compound of Formula or a pharmaceutically acceptable salt thereof.
Co-administration with a second agent
The method further specifies administering the compound together with a second agent.
The claim coverage centers on administering an effective amount of a compound of Formula or a pharmaceutically acceptable salt to treat sclerodermatous chronic graft versus host disease, with a dependent refinement adding co-administration with a second agent.
Stated Advantages
Treating graft versus host disease (GVHD), including chronic GVHD (cGVHD).
Treating sclerodermatous chronic graft versus host disease (cGVHD).
Documented Applications
Treatment of graft versus host disease (GVHD), including chronic GVHD (cGVHD), and sclerodermatous cGVHD.
Treatment of sclerodermatous chronic graft-versus-host disease in a subject, including reversal or blockade of chronic GVHD-related pathology and pulmonary dysfunction in murine models.
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