Angiogenesis inhibitors and pharmaceutical/cosmetic applications thereof
AssigneesGalderma Research & Development, Cnrs
InventorsJacques Eustache, Pierre Van De Weghe, Vincent Rodeschini, Celine Tarnus
Life of this patent
Estimating the term…
Abstract
Novel derivatives of fumagalone have the general formula (I): and are useful angiogenes is inhibitors; these can be formulated into pharmaceutical compositions suited for human or veterinary medicine, or can be formulated into cosmetic compositions.
Claims11
A compound having the following formula (I):
- in which:
- R1 is a radical of structure (a) or of structure (b):
- wherein R5, R6 and R7 are as defined below;
- R2 is a lower alkyl radical having 1 to 5 carbon atoms;
- R3 is a lower alkyl radical having 1 to 5 carbon atoms;
- R4 is a radical of structure (c), bound by a single bond to the cyclohexane from which it depends:
- or R4 is an oxygen atom bound by a double bond to the cyclohexane from which it depends;
- R5 is a hydrogen atom or a methyl radical or a trifluoromethyl radical;
- and
- R6 and R7 represent, independently of each other, a hydrogen atom or a trifluoromethyl radical, or salt or isomer thereof.
A method for the inhibition of angiogenesis comprising administering to a subject in need of such inhibition, an effective angiogenesis-inhibiting amount of a pharmaceutical composition comprising at least one compound having the following formula (I):
- in which:
- R1 is a radical of structure (a) or of structure (b):
- wherein R5, R6 and R7 are as defined below
- R2 is a lower alkyl radical having 1 to 5 carbon atoms;
- R3 is a lower alkyl radical having 1 to 5 carbon atoms;
- R4 is a radical of structure (c), bound to the cyclohexane from which it depends;
- or R4 is an oxygen atom bound by a double bond to the cyclohexane from which it depends;
- R5 is a hydrogen atom or a methyl radical or a trifluromethyl radical;
- and
- R6 and R7 represent independently of each other, a hydrogen atom or a trifluoromethyl radical, or salt or isomer thereof;
- formulated into a pharmaceutically acceptable carrier therefor.
A method for the inhibition of the angiogenesis of rosacea comprising administering to a subject in need of such inhibition an effective angiogenesis-inhibiting amount of a pharmaceutical composition comprising at least one compound having the following formula (I):
- in which:
- R1 is a radical of structure (a) or of structure (b):
- wherein R5, R6 and R7 are as defined below
- R2 is a lower alkyl radical having 1 to 5 carbon atoms;
- R3 is a lower alkyl radical having 1 to 5 carbon atoms;
- R4 is a radical of structure (c), bound to the cyclohexane from which it depends;
- or R4 is an oxygen atom bound by a double bond to the cyclohexane from which it depends;
- R5 is a hydrogen atom or a methyl radical or a trifluromethyl radical;
- and
- R6 and R7 represent independently of each other, a hydrogen atom or a trifluoromethyl radical, or salt or isomer thereof;
- formulated into a pharmaceutically acceptable carrier therefor.
A method for the inhibition of angiogenesis in the skin or scalp of a subject in need of such inhibition comprising topically applying to said skin or scalp an effective angiogenesis-inhibiting amount of a cosmetic composition comprising at least one compound having the following formula (I):
- in which:
- R1 is a radical of structure (a) or of structure (b):
- wherein R5, R6 and R7 are as defined below;
- R2 is a lower alkyl radical having 1 to 5 carbon atoms;
- R3 is a lower alkyl radical having 1 to 5 carbon atoms;
- R4 is a radical of structure (c), bound to the cyclohexane from which it depends;
- or R4 is an oxygen atom bound by a double bond to the cyclohexane from which it depends;
- R5 is a hydrogen atom or a methyl radical or a trifluromethyl radical;
- and
- R6 and R7 represent independently of each other, a hydrogen atom or a trifluoromethyl radical, or salt or isomer thereof;
- formulated into a cosmetically acceptable carrier therefor.
Dependencies are inferred from the claim text.