Methods of Treatment of Fibrotic Diseases
AssigneesPhost’in Therapeutics, RD Nephrologie
InventorsLudovic CLARION, Karine CHORRO, Séverine LOISEAU, Bernard PAU, Angel ARGILES, Nathalie GAYRARD
Life of this patent
Estimating the term…
Abstract
The present invention relates to the use of heterocyclic phosphonic compounds or compositions comprising the same for the treatment of fibrotic diseases. In particular, the present invention relates to compounds of general formula (1) as claimed herein or compositions comprising the same for use in the treatment of fibrotic diseases.
Claims20
A method of treating a fibrotic disease, the method comprising administering an effective amount of a compound of formula (1) to a subject in need thereof, for wherein the compound has the following formula (1):
- wherein Y represents an oxygen, a sulfur or a selenium atom,
- Z represents O, S, Se, NH or a NR6 group, wherein R6 is an aryl or an optionally substituted alkyl group,
- R1 represents a hydrogen atom, an optionally substituted alkyl group or an aryl group,
- R2a represents a hydrogen atom, halogen, azide (N3), a carbonate or dithiocarbonate group, a 1H-[1,2,3]triazolyl group or a group —X—R2, wherein
- X represents an oxygen, a sulfur, a selenium atom, a NH or NR7 group, R7 being an optionally substituted aryl or alkyl group;
- and;
- R2 represents an aryl group, an optionally substituted alkyl group, a hydrogen atom, a trichloroacetimidate group (—C(═NH)CCl3), an acyl, formyl, sulfonyl, sulfinyl, tert-butyldiphenylsilyl, allyl group, a saccharyl, ester, amide, thioamide, sulfonamide group, or X—R2 represents a P(O)R2R6 group, in which R2 and R6 represent independently from each other an aryl group, an optionally substituted alkyl group, OH, an alkoxy or an aryloxy group,
- R3 and R4 represent independently from each other an aryl, an optionally substituted alkyl group, an hydrogen atom, a trichloroacetimidate group, an acyl, formyl, sulfonyl, sulfinyl, tert-butyldiphenylsilyl group, an allyl, ester, amide, thioamide, sulfonamide group, or R3 and R4 taken together form a divalent radical of formula —R3—R4—,
- R5 represents a hydrogen atom or a hydrocarbon group comprising one or more heteroatoms.
A kit comprising a compound of formula (1), and instructions for use in the treatment of fibrosis diseases,
- wherein the compound has the following formula (1):
- wherein Y represents an oxygen, a sulfur or a selenium atom,
- Z represents O, S, Se, NH or a NR6 group, wherein R6 is an aryl or an optionally substituted alkyl group,
- R1 represents a hydrogen atom, an optionally substituted alkyl group or an aryl group,
- R2a represents a hydrogen atom, halogen, azide (N3), a carbonate or dithiocarbonate group, a 1H-[1,2,3]triazolyl group or a group —X—R2, wherein
- X represents an oxygen, a sulfur, a selenium atom, a NH or NR7 group, R7 being an optionally substituted aryl or alkyl group;
- and;
- R2 represents an aryl group, an optionally substituted alkyl group, a hydrogen atom, a trichloroacetimidate group (—C(═NH)CCl3), an acyl, formyl, sulfonyl, sulfinyl, tert-butyldiphenylsilyl, allyl group, a saccharyl, ester, amide, thioamide, sulfonamide group, or X—R2 represents a P(O)R2R6 group, in which R2 and R6 represent independently from each other an aryl group, an optionally substituted alkyl group, OH, an alkoxy or an aryloxy group,
- R3 and R4 represent independently from each other an aryl, an optionally substituted alkyl group, an hydrogen atom, a trichloroacetimidate group, an acyl, formyl, sulfonyl, sulfinyl, tert-butyldiphenylsilyl group, an allyl, ester, amide, thioamide, sulfonamide group, or R3 and R4 taken together form a divalent radical of formula —R3—R4—,
- R5 represents a hydrogen atom or a hydrocarbon group comprising one or more heteroatoms.
Dependencies are inferred from the claim text.