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US 6,444,709 B1Granted
Heteroethylene compounds and pharmaceutical and cosmetic compositions containing same
AssigneeGalderma Research & Development, S.N.C.
InventorsPhilippe Diaz, Jean-Michel Bernardon
Life of this patent
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Abstract
The invention relates to novel heteroethynylenic compounds having the general formula (I): as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.
Claims16
Heteroethynylenic compounds, corresponding to formula (I) below:
- in which:
- R1 represents:
- (i) a —CH3 radical
- (ii) a radical —CH2—O—R5
- (iii) radical —COR6
- R5 and R6 having the meanings given below,
- X represents:
- O, Se, S(O)n, n being 0, 1 or 2,
- Y represents a divalent radical which has the formula:
- R7, R8, R9 and R10 having the meanings given below,
- R2 and R3, taken together, form, with the adjacent aromatic ring, a 5- or 6-membered ring optionally substituted with methyl groups and/or optionally interrupted by an oxygen or sulphur atom,
- or R2 and R3 independently, which may be identical or different, can represent:
- a) a hydrogen atom,
- b) a radical comprising
- tert-butyl,
- 1-methylcyclohexyl, or
- 1-adamantyl,
- c) a radical —OR11
- d) a polyether radical
- e) a halogen atom
- R11 having the meaning given below, it being understood that at least one of the substituents R2 and R3 represents (b),
- R4 represents a hydrogen atom, a lower alkyl radical, a radical OR12, a polyether radical, a radical COR13 or a halogen atom,
- R12 and R13 having the meanings given below,
- R′4 represents a hydrogen atom or a halogen atom,
- R5 represents a hydrogen atom or a lower alkyl radical,
- R6 represents:
- (i) a hydrogen atom
- (ii) a lower alkyl radical
- (iii) a radical OR14
- R14 having the meaning given below,
- (iv) a radical of formula
- R′ and R″ having the meanings given below,
- R7, R8, R9 and R10, which may be identical or different, represent a hydrogen atom, a lower alkyl radical or an aryl radical,
- R11 and R12, which may be identical or different, represent a hydrogen atom, a lower alkyl radical, an optionally substituted aryl radical, an optionally substituted aralkyl radical, a monohydroxyalkyl or polyhydroxyalkyl radical or a lower acyl radical,
- R13 represents a lower alkyl radical, a radical OR15 or a radical
- R15, R′ and R″ having the meanings given below,
- R14 and R15 which may be identical or different, represent a hydrogen atom, a lower alkyl radical, an aryl radical, an optionally substituted aralkyl radical, a monohydroxyalkyl radical or a polyhydroxyalkyl radical,
- R′ and R″, which may be identical or different, represent a hydrogen atom, a lower alkyl radical, a mono- or polyhydroxyalkyl radical, an optionally substituted aryl radical or an amino acid residue, or alternatively, taken together with the nitrogen atom, form a heterocycle,
- as well as the salts thereof and the optical and geometrical isomers thereof.
36 more elements
Dependencies are inferred from the claim text.