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Composition for inducing and stimulating hair growth and retarding its loss, based on nicotinic esters and pyrimidine derivatives

Assignee: L'Oréal SA
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Filing: 1987-09-08
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Granted: 1990-11-06
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Expires: 2007-09-08
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Abstract

Abstract The invention relates to a composition for inducing and stimulating hair growth and retarding its loss, containing, in a cosmetically or pharmaceutically acceptable medium, at least one pyrimidine derivative corresponding to the formula (I): <IMAGE> (I) in which R1 denotes a group <IMAGE> in which R3 and R4 can be chosen from hydrogen, an alkyl group preferably having 1 to 4 carbon atoms, and an alkenyl, alkylaryl or lower cycloalkyl group, and R3 and R4 can also form a heterocyclic ring with the nitrogen atom to which they are attached, it being possible for this heterocyclic ring to be chosen, inter alia, from aziridinyl, azetidinyl, pyrrolidinyl, piperidyl, hexahydroazepinyl, heptamethyleneimine, octamethyleneimine, morpholine and 4-(lower alkyl)piperazidinyl groups, it being possible for the heterocyclic groups to be substituted on the carbon atoms with one to three lower alkyl, hydroxyl or alkoxy groups; the group R2 is chosen from hydrogen and an alkyl, alkenyl, alkylalkoxy, cycloalkyl, aryl, alkylaryl, arylalkyl, alkylarylalkyl, alkoxyarylalkyl and lower haloarylalkyl group, or one of its addition salts with cosmetically or pharmaceutically acceptable acids, and at least one nicotinic ester.

Inventors

  • 👤 Jean F. Grollier

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-29 12:30
CPC Classifications
A; A61; A61K; A61K8/00; A61K8/18; A61K8/30; A61K8/40; A61K8/44; A61K8/49; A61K8/494; A61K8/4953; A61K8/67; A61K8/673; A61K8/675; A61Q; A61Q7/00

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 324 words
Composition for inducing and stimulating hair growth and retarding its loss, in a cosmetically or pharmaceutically acceptable medium, said composition comprising an effective amount for inducing and stimulating hair growth and retarding its loss of at least one pyrimidine derivative corresponding to the formula: ##STR6## wherein R 1 denotes a group ##STR7## wherein R 3 and R 4 are selected from the group consisting of hydrogen, C 1 -C 4 alkyl, C 2 -C 5 alkenyl, C 1 -C 4 alkylaryl and lower cycloalkyl group, the alkyl part of which is a C 1 -C 4 alkyl radical, or R 3 and R 4 together form a heterocyclic ring with the nitrogen atom to which they are attached, this heterocyclic ring being selected from the group consisting of aziridinyl, azetidinyl, pyrrolidinyl, piperidino, hexahydroazepinyl, heptamethyleneimino, octamethyleneimino, morpholino and 4-(lower alkyl)piperazidinyl, the heterocyclic groups being unsubstituted or substituted on the carbon atoms with one to three C 1 -C 4 alkyl, hydroxyl or C 1 -C 4 alkoxy, and wherein R 2 is selected from the group consisting of hydrogen, C 1 -C 4 alkyl, C 2 -C 5 alkenyl, C 1 -C 4 alkoxy C 1 -C 4 alkyl cycloalkyl, C 1 -C 4 aryl, C 1 -C 4 alkylaryl, aryl C 1 -C 4 alkyl, C.sub. 1 -C 4 alkylaryl C 1 -C 4 alkyl, C 1 -C 4 alkoxyaryl C 1 -C 4 alkyl and haloaryl C 1 -C 4 alkyl, or one of its addition salts with cosmetically or pharmaceutically acceptable, acids, the pyrimidine derivative of formula (I) being present in the composition in a proportion of between 0.05 and 6% by weight relative to the total weight of the composition. and an effective amount of at least one C 1 -C 6 linear or branched alkyl nicotinic ester, the nicotinic ester being present in a proportion of between 0.05 and 1% by weight relative to the total weight of the composition.
Claim 2
Dependent Claim 324 words
Composition for inducing and stimulating hair growth and retarding its loss, in a cosmetically or pharmaceutically acceptable medium, said composition comprising an effective amount for inducing and stimulating hair growth and retarding its loss of at least one pyrimidine derivative corresponding to the formula: ##STR6## wherein R 1 denotes a group ##STR7## wherein R 3 and R 4 are selected from the group consisting of hydrogen, C 1 -C 4 alkyl, C 2 -C 5 alkenyl, C 1 -C 4 alkylaryl and lower cycloalkyl group, the alkyl part of which is a C 1 -C 4 alkyl radical, or R 3 and R 4 together form a heterocyclic ring with the nitrogen atom to which they are attached, this heterocyclic ring being selected from the group consisting of aziridinyl, azetidinyl, pyrrolidinyl, piperidino, hexahydroazepinyl, heptamethyleneimino, octamethyleneimino, morpholino and 4-(lower alkyl)piperazidinyl, the heterocyclic groups being unsubstituted or substituted on the carbon atoms with one to three C 1 -C 4 alkyl, hydroxyl or C 1 -C 4 alkoxy, and wherein R 2 is selected from the group consisting of hydrogen, C 1 -C 4 alkyl, C 2 -C 5 alkenyl, C 1 -C 4 alkoxy C 1 -C 4 alkyl cycloalkyl, C 1 -C 4 aryl, C 1 -C 4 alkylaryl, aryl C 1 -C 4 alkyl, C.sub. 1 -C 4 alkylaryl C 1 -C 4 alkyl, C 1 -C 4 alkoxyaryl C 1 -C 4 alkyl and haloaryl C 1 -C 4 alkyl, or one of its addition salts with cosmetically or pharmaceutically acceptable, acids, the pyrimidine derivative of formula (I) being present in the composition in a proportion of between 0.05 and 6% by weight relative to the total weight of the composition. and an effective amount of at least one C 1 -C 6 linear or branched alkyl nicotinic ester, the nicotinic ester being present in a proportion of between 0.05 and 1% by weight relative to the total weight of the composition.
Claim 3
Dependent Claim 41 words
Composition according to claim 1, wherein the pyrimidine derivative of the formula (I) is a compound in which R 2 denotes hydrogen and R 1 , denotes a group ##STR8## in which R 3 and R 4 form a piperidyl ring.
Claim 4
Dependent Claim 14 words
Composition according to claim 1, wherein the pyrimidine derivative of formula (I) is 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine.
Claim 5
Dependent Claim 19 words
Composition according to claim 1, containing, in a cosmetically or pharmaceutically acceptable medium, at least 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine and methyl nicotinate.
Claim 6
Dependent Claim 24 words
Composition according to claim 1, wherein the ratio by weight of the pyrimidine derivative to the nicotinic acid ester is between 2:1 and 10:1.
Claim 7
Dependent Claim 20 words
Composition according to claim 1, wherein the pharmaceutically or cosmetically acceptable medium consists of an unthickened hydroalcoholic or alcoholic medium.
Claim 8
Dependent Claim 19 words
Composition according to claim 1, wherein the cosmetically or pharmaceutically acceptable medium is an aqueous, thickened or gelled medium.
Claim 9
Dependent Claim 9 words
Composition according to claim 1, constituting a hydroalcoholic gel.
Claim 10
Dependent Claim 33 words
Process for inducing and stimulating hair growth and retarding its loss comprising applying a composition as defined in claim 1 to the hair or scalp of a individual in need of said treatment.
Claim 11
Dependent Claim 35 words
Composition according to claim 1, wherein the pyrimidine derivative of formula (I) is present in the composition in a proportion of between 0.1 and 5% by weight relative to the total weight of the composition.
Claim 12
Dependent Claim 30 words
Composition according to claim 1, wherein the nicotinic acid ester is present in a proportion of between 0.1 and 0.6 by weight relative to the total weight of the composition.

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