Use of cyclosporine analogues for treating fibrosis
AssigneeHepion Pharmaceuticals, Inc.
InventorsDaren R. Ure, Daniel J. Trepanier, Patrick R. Mayo, Robert T. Foster
Life of this patent
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Abstract
Disclosed herein include methods, compositions, and kits suitable for use in preventing, treating or reverse fibrosis. The methods comprise administering to a subject in need thereof a composition comprising a cyclosporine analogue (for example, CRV431), or a pharmaceutically acceptable salt, solvate, stereoisomer thereof. The compositions and kits comprise a cyclosporine analogue (for example, CRV431), or a pharmaceutically acceptable salt, solvate, stereoisomer thereof.
Claims28
A method for treating non-liver fibrosis, comprising administering to a subject in need thereof a composition comprising cyclosporine analogue of Formula L, or a pharmaceutically acceptable salt, solvate, stereoisomer thereof,
- wherein:
- a. R′ is H or acetyl;
- b. R1 is a saturated or unsaturated straight or branched aliphatic carbon chain from 2 to 15 carbon atoms in length;
- c. R2 is selected from the group consisting of:
- i. H;
- ii. an unsubstituted, N-substituted, or N,N-disubstituted amide;
- iii. a N-substituted or unsubstituted acyl protected amine;
- iv. a N-substituted or unsubstituted amine;
- v. a carboxylic acid;
- vi. a nitrile;
- vii. an ester;
- viii. a ketone;
- ix. a hydroxy, dihydroxy, trihydroxy, or polyhydroxy alkyl;
- and
- x. a substituted or unsubstituted aryl;
- xi. a saturated or unsaturated. straight or branched aliphatic chain optionally containing a substituent selected from the group consisting of a hydrogen, a ketone, a hydroxyl, a nitrile, a carboxylic acid, an ester, a 1,3-dioxolane, a halogen, and an oxo;
- xii. an aromatic group containing a substituent selected from the group consisting of a halogen, an ester, and a nitro;
- and
- xiii. a combination of the saturated or unsaturated, straight or branched aliphatic chain of (xi) and the aromatic group of (xii);
- and
- d. R23 is a saturated or unsaturated straight chain or branched optionally substituted aliphatic carbon chain.
(canceled)
(canceled)
A method for preventing or delaying the onset of fibrosis, comprising administering to a subject in need thereof a composition comprising cyclosporine analogue of Formula L, or a pharmaceutically acceptable salt, solvate, stereoisomer thereof,
- wherein:
- a. R′ is H or acetyl;
- b. R1 is a saturated or unsaturated straight or branched aliphatic carbon chain from 2 to 15 carbon atoms in length;
- c. R2 is selected from the group consisting of:
- i. H;
- ii. an unsubstituted, N-substituted, or N,N-disubstituted amide;
- iii. a N-substituted or unsubstituted acyl protected amine;
- iv. a N-substituted or unsubstituted amine;
- v. a carboxylic acid;
- vi. a nitrile;
- vii. an ester;
- viii. a ketone;
- ix. a hydroxy, dihydroxy, trihydroxy, or polyhydroxy alkyl;
- and
- x. a substituted or unsubstituted aryl;
- xi. a saturated or unsaturated. straight or branched aliphatic chain optionally containing a substituent selected from the group consisting of a hydrogen, a ketone, a hydroxyl, a nitrile, a carboxylic acid, an ester, a 1,3-dioxolane, a halogen, and an oxo;
- xii. an aromatic group containing a substituent selected from the group consisting of a halogen, an ester, and a nitro;
- and
- xiii. a combination of the saturated or unsaturated, straight or branched aliphatic chain of (xi) and the aromatic group of (xii);
- and
- d. R23 is a saturated or unsaturated straight chain or branched optionally substituted aliphatic carbon chain.
-14. (canceled)
A method for reducing fibrosis or reversing fibrosis, comprising administering to a subject in need thereof a composition comprising cyclosporine analogue of Formula L, or a pharmaceutically acceptable salt, solvate, stereoisomer thereof,
- wherein:
- a. R′ is H or acetyl;
- b. R1 is a saturated or unsaturated straight or branched aliphatic carbon chain from 2 to 15 carbon atoms in length;
- c. R2 is selected from the group consisting of:
- i. H;
- ii. an unsubstituted, N-substituted, or N,N-disubstituted amide;
- iii. a N-substituted or unsubstituted acyl protected amine;
- iv. a N-substituted or unsubstituted amine;
- v. a carboxylic acid;
- vi. a nitrile;
- vii. an ester;
- viii. a ketone;
- ix. a hydroxy, dihydroxy, trihydroxy, or polyhydroxy alkyl;
- and
- x. a substituted or unsubstituted aryl;
- xi. a saturated or unsaturated. straight or branched aliphatic chain optionally containing a substituent selected from the group consisting of a hydrogen, a ketone, a hydroxyl, a nitrile, a carboxylic acid, an ester, a 1,3-dioxolane, a halogen, and an oxo;
- xii. an aromatic group containing a substituent selected from the group consisting of a halogen, an ester, and a nitro;
- and
- xiii. a combination of the saturated or unsaturated, straight or branched aliphatic chain of (xi) and the aromatic group of (xii);
- and
- d. R23 is a saturated or unsaturated straight chain or branched optionally substituted aliphatic carbon chain.
-21. (canceled)
(canceled)
-31. (canceled)
-37. (canceled)
-51. (canceled)
Dependencies are inferred from the claim text.