Phosphotetrahydropyran compounds for the treatment of wounds and fibrotic disorders
AssigneePharmaxis Pty Limited
InventorsAlan D. Robertson, Diego Silva, Ian Alexander McDonald
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Abstract
Methods of using phosphotetrahydropyran compounds for treatment of fibrotic and scarring disorders, e.g. pulmonary fibrosis, fibrosis associated with surgical procedures, wound healing disorders, scar formation, sclerotic disorders, ocular fibrotic disorders, ocular healing disorders, ocular fibrosis after surgery, glaucoma, tendon scarring disorders, joint scarring disorders, kidney interstitial fibrosis and glomerular fibrosis and tubular fibrosis of the kidney.
Claims20
A method to modulate wound healing processes in a subject, said method comprising the administration of a composition containing an effective amount of a phosphonate prodrug of a phosphonotetrahydropyran compound of a compound of Formula I, and an acceptable pharmaceutical carrier,
- wherein the phosphonate prodrug is a mono- or di-ester of the phosphonic acid functionality;
- and
- wherein n is an integer from 0 to 3, the —O(CH2)nR group is in an axial or equatorial position, and R is lower alkyl, or optionally substituted heteroaryl or optionally substituted aryl wherein the substituent is selected from the group consisting of —Cl, —F, CF3, CH3, CH2CH3, —OCH3, —OCF3, —(CH2)mCO2R1, —(CH2)mOR2, —(CH2)mCONHR2, —(CH2)mNHR2, and —(CH2)mCONR2R3, wherein m is an integer from 0 to 3;
- R1 is selected from the group of consisting of H, alkyl and aryl;
- and R2 and R3 are independently selected from the group consisting of H, alkyl, aryl and acyl.
A method of treating pulmonary fibrosis, comprising administering to a subject in need of treatment, an effective amount of a composition comprising a phosphonate prodrug of a phosphonotetrahydropyran compound of Formula I:
- wherein the phosphonate prodrug is a mono- or di-ester of the phosphonic acid functionality;
- and
- wherein n is an integer from 0 to 3, the —O(CH2)nR group is in an axial or equatorial position, and R is lower alkyl, or optionally substituted heteroaryl or optionally substituted aryl wherein the substituent is selected from the group consisting of —Cl, —F, CF3, CH3, CH2CH3, —OCH3, —OCF3, —(CH2)mCO2R1, —(CH2)mOR2, —(CH2)mCONHR2, —(CH2)mNHR2, and —(CH2)mCONR2R3, wherein m is an integer from 0 to 3;
- R1 is selected from the group of consisting of H, alkyl and aryl;
- and R2 and R3 are independently selected from the group consisting of H, alkyl, aryl and acyl.
A pharmaceutical composition for modulating wound healing processes or treating pulmonary fibrosis in a subject, comprising a phosphonate prodrug of a phosphonotetrahydropyran compound of a compound of Formula I:
- and an acceptable pharmaceutical carrier
- wherein the phosphonate prodrug is a mono- or di-ester of the phosphonic acid functionality;
- and
- wherein n is an integer from 0 to 3, the —O(CH2)nR group is in an axial or equatorial position, and R is lower alkyl, or optionally substituted heteroaryl or optionally substituted aryl wherein the substituent is selected from the group consisting of —Cl, —F, CF3, CH3, CH2CH3, —OCH3, —OCF3, —(CH2)mCO2R1, —(CH2)mOR2, —(CH2)mCONHR2, —(CH2)mNHR2, and —(CH2)mCONR2R3, wherein m is an integer from 0 to 3;
- R1 is selected from the group of consisting of H, alkyl and aryl;
- and R2 and R3 are independently selected from the group consisting of H, alkyl, aryl and acyl.
Dependencies are inferred from the claim text.