Anti-fibrotic compounds and use thereof
AssigneeHadasit Medical Research Services and Development Ltd.
InventorsShulamit Richter-Dayan, Raphael Breuer, Rotem Sertchook
Life of this patent
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Abstract
The present invention relates to compounds, compositions and methods for treating fibrosis. In particular, compounds that inhibit or downregulate Sirtuin 1 (SIRT1) activity, which are particularly useful in the treatment of Idiopathic Pulmonary Fibrosis (IPF) are provided.
Claims16
A method of treating or inhibiting pulmonary fibrosis in a subject in need thereof, the method comprising administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula X, or salts, hydrates, solvates, polymorphs, optical isomers, geometrical isomers, enantiomers, diastereomers, or mixtures thereof:
- wherein L is a linker selected from the group consisting of:
- C1-C10 alkylene, C2-C10 alkenylene, and C2-C10 alkynylene, and
- Ar is selected from the group consisting of:
- phenyl substituted with at least one of methyl, methoxy, amido, amino, and nitro;
- C10-C18 fused bicyclic aryl optionally substituted with at least one of hydroxy, amido, alkylamido, amino, alkylamino, carboxyl, CH2CH2OH, and CH2CH2OCH2CH2OH;
- and
- C5-C9 fused bicyclic heteroaryl optionally substituted with at least one of hydroxy, amido, alkylamido, amino, alkylamino, carboxyl, C1-C4 alkyl, C1-C4 alkoxy, halogen, haloalkyl, nitro, cyano, CH2CH2OH, and CH2CH2OCH2CH2OH, provided that when Ar is C5-C9 fused bicyclic heteroaryl substituted with methoxy and amino, then the amino is not an aniline group.
A method of treating a condition associated with pulmonary fibrosis in a subject in need thereof, the method comprising administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by the structure of Formula X, or salts, hydrates, solvates, polymorphs, optical isomers, enantiomers, diastereomers, or mixtures thereof:
- wherein L is a C2-C6 alkylene, and Ar is a C5-C9 fused bicyclic heteroaryl optionally substituted with at least one of hydroxy, amido, alkylamido, amino, alkylamino, carboxyl, C1-C4 alkyl, C1-C4 alkoxy, halogen, haloalkyl, nitro, cyano, CH2CH2OH, and CH2CH2OCH2CH2OH, provided that when Ar is substituted with methoxy and amino, then the amino is not an aniline group.
A method of treating a condition associated with pulmonary fibrosis in a subject in need thereof, the method comprising administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound selected from the group consisting of:
- or salts, hydrates, solvates, polymorphs, or mixtures thereof.
Dependencies are inferred from the claim text.