Hair growth and/or regrowth compositions

Abstract

The present disclosure relates to compositions containing certain pyrimidine compounds such as minoxidil and/or certain pyrimidine sulfate (inner salt) compounds such as minoxidil sulfate and especially compositions containing pyrimidine compounds in combination with an admixtures comprising at least one antioxidant, at least one organic acid and a select fatty acid mixture. The present disclosure also relates to use of the compositions to grow and/or regrow hair and/or prevent hair loss in mammals and particularly in humans.

1 . A hair growth and/or regrowth compositions comprising;
 a. at least one compound selected from the group consisting of compounds represented by the formulae:   
       
         
           
           
               
               
           
         
         
           and mixtures thereof, 
           wherein R 1  is a moiety selected from the group consisting of moieties of the formula —N(R 3 )(R 4 ), 
           wherein R 3  and R 4  are selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl, and lower cycloalkyl, and taken together R 3  and R 4  may be a heterocyclic moiety selected from the group consisting of aziridinyl, azetidinyl, pyrrolidinyl, piperidino, hexahydroazepinyl, heptamethylenimino, octamethylenimino, morpholino, and 4-lower-alkylpiperazinyl, each of said heterocyclic moieties having attached as substituents on the carbon atoms 0 to 3 lower alkyl groups, hydroxy or alkoxy; and wherein R 2  is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkoxyalkyl, lower cycloalkyl, lower aryl, lower aralkyl, lower alkaryl, lower alkaralkyl, lower alkoxyaralkyl, and lower haloaralkyl and the pharmacologically acceptable acid addition salts thereof; and 
         
         b. from about 0.1% to about 99% by weight of an admixture, comprising:
 i. from about 0.01% to about 99.98% by weight of the admixture of an acid selected from the group consisting of intermediates of the Kreb cycle, non-Kreb cycle intermediate alpha-keto acid, derivatives thereof, salts thereof and mixtures thereof; 
 ii. from about 0.01% to about 99.98% by weight of the admixture of an antioxidant; and 
 iii. from about 0.01% to about 99.98% by weight of the admixture of a fatty acid mixture or fatty acid mixture source comprising at least 7 unsaturated or saturated fatty acids selected from the group consisting of butyric acid, caproic acid, caprylic acid, capric acid, lauric acid, myristic acid, myristoleic acid, palmitic acid, palmitoleic acid, stearic acid, oleic acid, linoleic acid, linolenic acid, arachidic acid, gadoleic acid, pentadecanoic acid, margaric acid, margaroleic acid, behenic acid, dihomolinoleic acid, arachidonic acid and lignoceric acid. 
 
       
     
     
         2 . The composition of  claim 1 , wherein the compound is minoxidil. 
     
     
         3 . The composition of  claim 2 , wherein the compound is minoxidil sulfate. 
     
     
         4 . The composition of  claim 1 , wherein the acid is an alpha-keto acid. 
     
     
         5 . The composition of  claim 4 , wherein the alpha-keto acid is selected from the group consisting of pyruvic acid, alpha-ketoglutaric acid, alpha-ketoisovaleric acid, alpha-ketoisocaproic acid, salts thereof and mixtures thereof. 
     
     
         6 . The composition according to  claim 5 , wherein the alpha-keto acid is a pyruvic acid selected from the group consisting of pyruvic acid, lithium pyruvate, sodium pyruvate, potassium pyruvate, magnesium pyruvate, calcium pyruvate, zinc pyruvate, manganese pyruvate, methyl pyruvate, salts thereof, prodrugs thereof, and mixtures thereof. 
     
     
         7 . The composition according to  claim 6 , wherein the pyruvic acid is sodium pyruvate. 
     
     
         8 . The composition according to  claim 1 , wherein the antioxidant is selected from the group consisting of a Vitamin A; Vitamin C; a tocopherol; a prodrugs of Vitamin A, a prodrugs of Vitamin C, and a prodrugs of Vitamin E; salts of Vitamin A, salts of Vitamin C, and salts of Vitamin E; flavonoids; polyphenols; and mixtures thereof. 
     
     
         9 . The composition according to  claim 8 , wherein the antioxidant is a Vitamin E selected from the group consisting of alpha-tocopherol, beta-tocopherol, gamma-tocopherol, delta-tocopherol, tocoquinone, tocotrienol, esters thereof and mixtures thereof. 
     
     
         10 . The composition according to  claim 9 , wherein the Vitamin E is selected from the group consisting of esters of tocopherol, esters of beta-tocopherol, esters of gamma-tocopherol, esters of delta-tocopherol, esters of tocoquinone, esters of tocotrienol and mixtures thereof. 
     
     
         11 . The composition according to  claim 10 , wherein the Vitamin E is selected from the group consisting of an acetate ester of tocopherol, acetate ester of beta-tocopherol, acetate ester of gamma-tocopherol, acetate ester of delta-tocopherol, acetate ester of tocoquinone, acetate ester of tocotrienol and mixtures thereof. 
     
     
         12 . The composition according to  claim 1 , which further comprises a lactate. 
     
     
         13 . The composition according to  claim 1 , being in the form of a suitable topical carrier. 
     
     
         14 . The compositions according to  claim 13 , wherein the topical carrier is in the form of an ointment, paste, gel, jelly, serum, aerosol spray, non-aerosol spray, foam, cream, lotion, solution, or suspension. 
     
     
         15 . A hair growth or regrowth composition comprising;
 a. at least one compound selected from the group consisting of compounds represented by the formulae:   
       
         
           
           
               
               
           
         
         
           and mixtures thereof, 
           wherein R 1  is a moiety selected from the group consisting of moieties of the formula —N(R 3 )(R 4 ), 
           wherein R 3  and R 4  are selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl, and lower cycloalkyl, and taken together R 3  and R 4  may be a heterocyclic moiety selected from the group consisting of aziridinyl, azetidinyl, pyrrolidinyl, piperidino, hexahydroazepinyl, heptamethylenimino, octamethylenimino, morpholino, and 4-lower-alkylpiperazinyl, each of said heterocyclic moieties having attached as substituents on the carbon atoms 0 to 3 lower alkyl groups, hydroxy or alkoxy; and wherein R 2  is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkoxyalkyl, lower cycloalkyl, lower aryl, lower aralkyl, lower alkaryl, lower alkaralkyl, lower alkoxyaralkyl, and lower haloaralkyl and the pharmacologically acceptable acid addition salts thereof; and 
         
         b. from about 5% to about 50% of an admixture, comprising:
 i) from about 0.01% to about 99.98% by weight of the admixture of an acid selected from the group consisting of pyruvic acid, a salt thereof and mixtures thereof; 
 ii) from about 0.01% to about 99.98% by weight of the admixture of an antioxidant; and 
 iii) from about 0.01% to about 99.98% by weight of the admixture of a fatty acid mixture or fatty acid mixture source 
 
         wherein the ratio of the pyruvic acid component to the fatty acid mixture is from 0.01:1 (or about 0.01:1) to 1:0.01 (about 1:0.01); the ratio of the pyruvic acid component to the antioxidant component is from 0.01:1 (or about 0.01:1) to 1:0.01 (or about 1:1.01); and the ratio of the fatty acid mixture component to the antioxidant component is from 0.01:1 (or about 0.01:1) to 1:0.01 (or about 1:0.01). 
       
     
     
         16 . The composition of according to  claim 15  wherein the ratio of the pyruvic acid component or the fatty acid component to the antioxidant component is from 1:1 to 1:0.5. 
     
     
         17 . A hair growth and/or regrowth compositions comprising;
 a. at least one compound selected from the group consisting of compounds represented by the formulae:   
       
         
           
           
               
               
           
         
         
           and mixtures thereof, 
           wherein R 1  is a moiety selected from the group consisting of moieties of the formula —N(R 3 )(R 4 ), 
           wherein R 3  and R 4  are selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl, and lower cycloalkyl, and taken together R 3  and R 4  may be a heterocyclic moiety selected from the group consisting of aziridinyl, azetidinyl, pyrrolidinyl, piperidino, hexahydroazepinyl, heptamethylenimino, octamethylenimino, morpholino, and 4-lower-alkylpiperazinyl, each of said heterocyclic moieties having attached as substituents on the carbon atoms 0 to 3 lower alkyl groups, hydroxy or alkoxy; and wherein R 2  is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkoxyalkyl, lower cycloalkyl, lower aryl, lower aralkyl, lower alkaryl, lower alkaralkyl, lower alkoxyaralkyl, and lower haloaralkyl and the pharmacologically acceptable acid addition salts thereof; and 
         
         b. from about 0.1% to about 99% of an admixture, comprising:
 i. from about 0.01% to about 99.98% by weight of the admixture of an acid selected from the group consisting of pyruvic acid, a salt thereof and mixtures thereof; 
 ii. from about 0.01% to about 99.98% by weight of the admixture of a tocopherol or an ester thereof; and 
 iii. from about 0.01% to about 99.98% by weight of the admixture of a fatty acid mixture source, wherein the fatty acid mixture is an oil mixture comprising:
 1. from about 0.01% to about 99.98% by weight of the fatty acid mixture of olive oil; 
 2. from about 0.01% to about 99.98% by weight of the fatty acid mixture of cocoa butter; and 
 3. from about 0.01% to about 99.98% by weight of the fatty acid mixture of cottonseed oil. 
 
 
       
     
     
         18 - 25 . (canceled)