Claims Analysis
Total Claims: 52
Claim 1
Independent Claim
447 words
A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth which comprises: (i) a first chemical inhibitor chosen from proteoglycanase inhibitors, glycosaminoglycanase inhibitors, glycosaminoglycan chain cellular uptake inhibitors or mixtures thereof; and (ii) a cosmetically acceptable vehicle for the chemical inhibitor; provided that when the first chemical inhibitor is a weak inhibitor, such that a 1 mM aqueous solution of the inhibitor reduces proteoglycanase activity, glycosaminoglycanase activity or cellular uptake of glycosaminoglycan chains, by from 5 to 50%, in accordance with at least one of the assay tests as herein described, then there is also present in the composition a second chemical inhibitor and/or an activity enhancer; provided also that when minoxidil is the sole chemical inhibitor then the .activity enhancer is a penetration enhancer chosen from: Dioctyl adipate Dicapryl adipate Diisopropyl adipate Diisopropyl sebacate Dibutyl sebacate Diethyl sebacate Dimethyl sebacate Dioctyl sebacate Dibutyl suberate Dioctyl azelate Debenzyl sebacate Dibutyl phthalate Dibutyl azelate Ethyl myristate Dimethyl azelate Butyl myristate Dibutyl succinate Didecyl phthalate Decyl oleate Ethyl caproate Ethyl salicylate Isopropyl palmitate Ethyl laurate 2-ethyl-hexyl pelargonate Isopropyl isostearate Butyl laurate Benzyl benzoate Butyl benzoate Hexyl laurate Ethyl caprate Ethyl caprylate Butyl stearate Benzyl salicylate 2-hydroxypropanoic acid 2-hyroxyoctanoic acid, esters of pyroglutamic acid having the structure: where R is C 1 to C 30 alkyl, or and where R' and R" are the same or different and are each represented by H or the grouping: [(CH 3 ) u , (CH 2 OH) v , (CH 2 ) w , (CH 3 CH 2 ) x , (CH = CH) z] - (2) where u is zero or 1 v is zero, or the integer 1 or 2, w is zero, or an integer of from 1 to 21 x is zero, or an integer of from 1 to 4, y is zero, or the integer 1 or 2, z is zero, or an integer of from 1 to 22, and u + v + w + x + y + z is an integer of from 1 to 22; provided that when the subgrouping (CH = CH) is present, then the total number of carbon atoms in said grouping is from 10 to 22; and/or a cationic polymer chosen from: Guar Hydroxypropyltrimonium chloride Quaternium-19 Quaternium-23 Quaternium-40 Quaternium-57 Poly(dipropyldiallylammonium chloride) Poly(methyl-β-propaniodiallylammonium chloride) Poly(diallylpiperidinium chloride) Poly(vinyl pyridinium chloride) Quaternised poly (vinyl alcohol) and Quaternised poly (dimethylaminoethylmethacrylate): the total amount of chemical inhibitor present in the composition being sufficient to increase hair growth in the rat, when said composition is applied topically thereto, by at least 10% more than that obtainable using a control composition from which the said inhibitors have been omitted.
Claim 2
Dependent Claim
447 words
A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth which comprises: (i) a first chemical inhibitor chosen from proteoglycanase inhibitors, glycosaminoglycanase inhibitors, glycosaminoglycan chain cellular uptake inhibitors or mixtures thereof; and (ii) a cosmetically acceptable vehicle for the chemical inhibitor; provided that when the first chemical inhibitor is a weak inhibitor, such that a 1 mM aqueous solution of the inhibitor reduces proteoglycanase activity, glycosaminoglycanase activity or cellular uptake of glycosaminoglycan chains, by from 5 to 50%, in accordance with at least one of the assay tests as herein described, then there is also present in the composition a second chemical inhibitor and/or an activity enhancer; provided also that when minoxidil is the sole chemical inhibitor then the .activity enhancer is a penetration enhancer chosen from: Dioctyl adipate Dicapryl adipate Diisopropyl adipate Diisopropyl sebacate Dibutyl sebacate Diethyl sebacate Dimethyl sebacate Dioctyl sebacate Dibutyl suberate Dioctyl azelate Debenzyl sebacate Dibutyl phthalate Dibutyl azelate Ethyl myristate Dimethyl azelate Butyl myristate Dibutyl succinate Didecyl phthalate Decyl oleate Ethyl caproate Ethyl salicylate Isopropyl palmitate Ethyl laurate 2-ethyl-hexyl pelargonate Isopropyl isostearate Butyl laurate Benzyl benzoate Butyl benzoate Hexyl laurate Ethyl caprate Ethyl caprylate Butyl stearate Benzyl salicylate 2-hydroxypropanoic acid 2-hyroxyoctanoic acid, esters of pyroglutamic acid having the structure: where R is C 1 to C 30 alkyl, or and where R' and R" are the same or different and are each represented by H or the grouping: [(CH 3 ) u , (CH 2 OH) v , (CH 2 ) w , (CH 3 CH 2 ) x , (CH = CH) z] - (2) where u is zero or 1 v is zero, or the integer 1 or 2, w is zero, or an integer of from 1 to 21 x is zero, or an integer of from 1 to 4, y is zero, or the integer 1 or 2, z is zero, or an integer of from 1 to 22, and u + v + w + x + y + z is an integer of from 1 to 22; provided that when the subgrouping (CH = CH) is present, then the total number of carbon atoms in said grouping is from 10 to 22; and/or a cationic polymer chosen from: Guar Hydroxypropyltrimonium chloride Quaternium-19 Quaternium-23 Quaternium-40 Quaternium-57 Poly(dipropyldiallylammonium chloride) Poly(methyl-β-propaniodiallylammonium chloride) Poly(diallylpiperidinium chloride) Poly(vinyl pyridinium chloride) Quaternised poly (vinyl alcohol) and Quaternised poly (dimethylaminoethylmethacrylate): the total amount of chemical inhibitor present in the composition being sufficient to increase hair growth in the rat, when said composition is applied topically thereto, by at least 10% more than that obtainable using a control composition from which the said inhibitors have been omitted.
Claim 3
Dependent Claim
15 words
A composition according to claim 1, in which the chemical inhibitor is a proteoglycanase inhibitor.
Claim 4
Dependent Claim
60 words
A composition according to claim 2, in which the proteoglycanase inhibitor is a direct proteoglycanase inhibitor chosen from: 1,10-Phenanthroline AcetylPhe-LeuSH AcetyISer-LeuSH AcetyiTrp-LeuSH AcetyIPhe-Phe-LeuSH HSCH 2 CH(i-Butyl)COPheNH 2 HSCH 2 CH(i-Butyl)COLeu-PheNH 2 AcetylTrp-IIeSH AcetylPhe-IleSH HOOCCH(i-Butyl)Leu-Leu-LeuOCH 3 HOOCCH(i-Butyl)Leu-Leu-AlaNH 2 HOOCCH(i-Butyl)Leu-Leu-PheNH 2 HOOCCH(i-Butyl)Leu-Leu-Leu-AlaNH 2 HONHCOCH 2 CH(n-Pentyl)COLeu-PheNH 2 HONHCOCH 2 CH(n-Pentyl)COLeu-AlaNH 2 HONHCOCH 2 CH(i-Butyl)COLeu-PheNH 2 HONHCOCH 2 CH(n-Pentyl)COVal-AlaNH 2 and mixtures thereof
Claim 5
Dependent Claim
20 words
A composition according to claim 2, in which the proteoglycanase inhibitor is an indirect proteoglycanase inhibitor chosen from cationic oligomers
Claim 6
Dependent Claim
21 words
A composition according to claim 4, in which the cationic oligomer is chosen from; Arg-Arg-Arg, Cys-Arg-Arg-Arg-Lys-Arg-Arg, Pro-Arg-Arg-Arg-Arg, Arg-Pro-Val-Arg-Arg-Arg-Arg-Arg-Pro-Val, and mixtures thereof.
Claim 7
Dependent Claim
15 words
A composition according to claim 1, in which the glycosaminoglycanase inhibitor is an exoglycosdase inhibitor.
Claim 8
Dependent Claim
99 words
A composition according to claim 6, in which the exoglycosidase inhibitor is chosen from aldonolactones and esterified aldonolactones having the structure: where A 1 and A 6 are -H, B is OR" or a lactone linkage to position 1 or 6, or -NHCOCHs and where R is -H or C 2 to C 8 alkyl, R' is the remainder of the molecule joined through another C atom at positions 2 to 5 to form a lactone, R" is -is or C 2 (ie acetyl) to C 4 acyl of either configuration with respect to the backbone of this molecule.
Claim 9
Dependent Claim
29 words
A composition according to claim 7, in which the aldonolactone is chosen from: L-Galactonic acid-y-lactone L-Arabino-1,5-lactone D-Fucono-1,5-lactone D-Glucaro-1,4-lactone D-Glucurono-6,3-lactone Galactaric acid lactone 2-Acetamido-2-deoxygluconolactone 2-Acetamido-2-deoxygalactonolactone D-Glucaro-1,4:6,3-dilactone L-ldaro-1,4-lactone, and mixtures thereof.
Claim 10
Dependent Claim
19 words
A composition according to claim 7, in which the esterified aldonolactone is chosen from: 2,3,5,-Tri-O-acetyl-D-glucaro-1,4-lactone 2,5-Di-0-acetyl-D-glucaro-1,4:6,3-dilactone, and mixtures thereof.
Claim 11
Dependent Claim
54 words
A composition according to claim 6, in which the exoglycosidase inhibitor is chosen from monosaccharides and esterified monosaccharides having the structure: where A is -OR or -NHCOCH 3 R is -H, -SO 3 M, C 2 (ie acetyl) to C 4 acyl R' is -H or -OR M is -H or a metal cation
Claim 12
Dependent Claim
19 words
A composition according to claim 10, in which the monosaccharide is chosen from: N-Acetylglucosamine N-Acetylgalactosamine D-Galactosamine, and mixtures thereof
Claim 13
Dependent Claim
57 words
A composition according to claim 6, in which the exoglycosidase inhibitor is chosen from piperidines having the structure: where A is -H, -OR' or R is -H, C 2 to C 8 alkyl or diamino-pyrimidine N-oxide R' is -H or C 2 (ie acetyl) to C 4 acyl, the substituent groups A being the same or different
Claim 14
Dependent Claim
12 words
A composition according to claim 12, in which the piperidine is 2(S)-Carboxy-3(R),4(R),5(S)-trihydroxypiperidine.
Claim 15
Dependent Claim
12 words
A composition according to claim 12, in which the piperidine is minoxidil.
Claim 16
Dependent Claim
40 words
A composition according to claim 14, which further comprises in addition to minoxidil, one more chemical inhibitor chosen from: Zinc gluconate magnesium sulphate D-glucaro-1,4-lactone 1,10-phenanthroline D-glucosamine-3-sulphate L-idaro-1,4-lactone L-galactono-1,4-lactone 2-acetamido-2-deoxygluconolactone D-glucaro-1,4:6,3-dilactone 2,3,5-tri-0-acetyl-D-glucaro-1,4-lactone N-acetylglucosamine N-acetylmannosamine phosphorylated hesperidin glucuronic acid, and mixtures thereof
Claim 17
Dependent Claim
19 words
A composition according to claim 12, in which the piperidine is minoxidil, the composition also comprising an activity enhancer.
Claim 18
Dependent Claim
15 words
A composition according to claim 1, in which the glycosaminoglycanase inhibitor is an endoglycosidase inhibitor.
Claim 19
Dependent Claim
24 words
A composition according to claim 17, in which the endoglycosidase inhibitor is chosen from: phosphorylated hesperidin sodium aurothlomalate substitued thiosemicarbazone indoles, and mixtures thereof
Claim 20
Dependent Claim
39 words
A composition according to claim 1, in which the sulphatase inhibitor is chosen from the anions sulphate sulphite pyrophosphate fluoride borate chloride gluconate, and mixtures thereof, each anion being in the form of a water-soluble metal or ammonium salt.
Claim 21
Dependent Claim
18 words
A composition according to claim 19, in which the salt is chosen from magnesium sulphate or zinc gluconate.
Claim 22
Dependent Claim
13 words
A composition according to claim 1, in which the sulphatase inhibitor is D-Glucosamine-3-sulphate
Claim 23
Dependent Claim
37 words
A composition according to claim 1, in which the sulphatamase inhibitor is chosen from the anions: sulphate sulphite pyrophosphate fluoride borate, and mixtures thereof, each anion being in the form of a water-soluble metal or ammonium salt.
Claim 24
Dependent Claim
13 words
A composition according to claim 20, in which the salt is magnesium sulphate.
Claim 25
Dependent Claim
51 words
A composition according to claim 1, in which the glycosaminoglycan chain cellular uptake inhibitor is chosen from an hexuronic acid or esters thereof having the structure: where R is -H, -S0 3 M, C 2 (ie acetyl) to C 4 acyl; R' is -H or C 2 to C 8 alkyl.
Claim 26
Dependent Claim
21 words
A composition according to claim 24, in which the hexuronic acid is chosen from glucuronic acid, iduronic acid and mixtures thereof.
Claim 27
Dependent Claim
50 words
A composition according to any preceding claim, in which the total amount of chemical inhibitor is sufficient to increase hair growth in the rat, when said composition is applied topically thereto, by at least 20% more than that obtainable using a control composition from which said inhibitors have been omitted.
Claim 28
Dependent Claim
50 words
A composition according to any preceding claim, in which the total amount of chemical inhibitor is sufficient to increase hair growth in the rat, when said composition is applied topically thereto, by at least 30% more than that obtainable using a control composition from which said inhibitors have been omitted.
Claim 29
Dependent Claim
50 words
A composition according to any preceding claim, in which the total amount of chemical inhibitor is sufficient to increase hair growth in the rat, when said composition is applied topically thereto, by at least 50% more than that obtainable using a control composition from which said inhibitors have been omitted.
Claim 30
Dependent Claim
22 words
A composition according to any preceding claim, in which the amount of the chemical inhibitor forms from 0.0001 to 99% by weight.
Claim 31
Dependent Claim
22 words
A composition according to any preceding claim, in which the amount of the chemical inhibitor forms from 0.1 to 20% by weight.
Claim 32
Dependent Claim
19 words
A composition according to any preceding claim which additionally comprises from 0.01 to 10% by weight of a perfume.
Claim 33
Dependent Claim
13 words
A composition according to any preceding claim, which additionally comprises an activity enhancer.
Claim 34
Dependent Claim
53 words
A composition according to claim 32, in which the activity enhancer is chosen from the hair growth stimulants: Benzalkonium chloride Benzethonium chloride Phenol Estradiol Diphenhydramine hydrocholoride Chlorpheniramine maleate Chlorophyllin derivatives Cholesterol Salicylic acid Cystine Red pepper tincture Benzyl nicotinate dl-Menthol Peppermint oil Calcium pantothenate Panthenol Castor oil Hinokitiol Prednisolone Resorcinol, and mixtures thereof
Claim 35
Dependent Claim
140 words
A composition according to claim 32, in which the activity enhancer is a hair growth stimulant chosen from a-1,4 esterified dissaccharides having the structure: where Z represents a functional nitrogen group, such as an azide or a group having the structure -NHB, in which B represents -H or a functional group such as acetyl or sulphate as a salt with an organic or mineral cation; M represents -H or SO 3 M 1 where M 1 is an organic or metallic cation, particularly an alkali metal; or an acetyl group; R represents a C 1 to C 4 alkyl radical, especially methyl; or an aryl radical; A represents a functional group such as an acid or -COOR,, where R 1 represents -H or a C 1 to C 4 alkyl radical, especially methyl; or a metal, especially an alkali metal.
Claim 36
Dependent Claim
167 words
A composition according to claim 32, in which the activity enhancer is a hair growth stimulant chosen from esterified oligosaccharides, including at least one esterified disaccharide unit consisting of a uronic acid residue having the structure: and a hexosamine residue having the structure: where R' is -H, C 3 to C 10 alkyl or R" is -H, C 1 to C 4 alkyl, -CO(CH 2 ) m CH 3 , -S0 3 M, R'" is -H, -CO(CH 2 ) m CH 3 , or -SO 3 M, M is -H, or a metallic or organic cation n is 0 or an integer of from 1 to 7, and m is 0 or the integer 1 or 2; the groups designated R" being the same or different, one R" group from each pyranose ring structure being linked by a glycosidic linkage having the configuration a-1,3, a-1,4, β-1,3 or β-1,4; and the -COOR', -CH 2 OR" and -OR" groups being of either configuration with respect to the pyranose rings.
Claim 37
Dependent Claim
41 words
A composition according to claim 32, in which the activity enhancer is a hair growth stimulant chosen from: minoxidil glucuronides, minoxidil sulphates, and mixtures thereof. 37. A composition according to claim 32, in which the activity enhancer is a penetration enhancer.
Claim 38
Dependent Claim
87 words
A composition according to claim 37, in which the penetration enhancer is chosen from: Dioctyl adipate Dicapryl adipate Diisopropyl adipate Diisopropyl sebacate Dibutyl sebacate Diethyl sebacate Dimethyl sebacate Dioctyl sebacate Dibutyl suberate Dioctyl azelate Debenzyl sebacate Dibutyl phthalate Dibutyl azelate Ethyl myristate Dimethyl azelate Butyl myristate Dibutyl succinate Didecyl phthalate Decyl oleate Ethyl caproate Ethyl salicylate Isopropyl palmitate Ethyl laurate 2-ethyl-hexyl pelargonate Isopropyl isostearate Butyl laurate Benzyl benzoate Butyl benzoate Hexyl laurate Ethyl caprate Ethyl caprylate Butyl stearate Benzyl salicylate 2-hydroxypropanoic acid 2-hydroxyoctanoic acid, and mixtures thereof.
Claim 39
Dependent Claim
179 words
A composition according to claim 37, in which the penetration enhancer is chosen from esters of pyroglutamic acid having the structure: where R is C 1 to C 30 alkyl, or - and where R' and R" are the same or different and are each represented by H or the grouping: [(CH 3 ) u , (CH 2 0H) v , (CH 2 ) w , (CH 3 CH 2 ) x , (CH = CH),]- (2) where u is zero or 1 v is zero, or the integer 1 or 2, w is zero, or an integer of from 1 to 21 x is zero, or an integer of from 1 to 4, y is zero, or the integer 1 or 2, z is zero, or an integer of from 1 to 22, and u + v + w + x + y + z is an integer of from 1 to 22; provided that when the subgrouping (CH = CH) is present, then the total number of carbon atoms in said grouping is from 10 to 22.
Claim 40
Dependent Claim
111 words
A composition according to claim 39, in which the ester of pyroglutamic acid is chosen from: pyroglutamic acid methyl ester pyroglutamic acid ethyl ester pyroglutamic acid n-propyl ester pyroglutamic acid n-butyl ester pyroglutamic acid n-heptyl ester pyroglutamic acid n-octyl ester pyroglutamic acid n-nonyl ester pyroglutamic acid n-decyl ester pyroglutamic acid n-undecyl ester pyroglutamic acid n-dodecyl ester pyroglutamic acid n-tridecyl ester pyroglutamic acid n-tetradcyl ester pyroglutamic acid n-hexadecyl ester pyroglutamic acid n-octadecyl ester pyroglutamic acid n-eicosyl ester pyroglutamic acid iso-propyl ester pyroglutamic acid 2-methylhexyl ester pyroglutamic acid 2-ethylhexyl ester pyroglutamic acid 3,7-dimethyloctyl ester pyroglutamic acid 2-hexyldecyl ester pyroglutamic acid 2-octyldodecyl ester pyroglutamic acid 2,4,4-trimetyl-1-pentane ester pyroglutamic acid methyloctyl ester, and mixtures thereof.
Claim 41
Dependent Claim
49 words
A composition according to claim 39, in which the ester of pyroglutamic acid is chosen from: 2-[pyroglutamoyloxy]-propionic acid methyl-2-[pyroglutamoyloxy-acetate ethyl-2-[pyroglutamoyloxy]-n-propionate ethyl-2-[pyroglutamoyloxy]-n-butyrate ethyl-2-[pyroglutamoyloxy]-iso-butyrate ethyl-2-[pyroglutamoyloxy]-n-valerate ethyl-2-[pyroglutamoyloxy]-n-caproate ethyl-2-[pyroglutamoyloxy]-n-heptylate ethyl-2-[pyroglutamoyloxy]-n-caprylate ethyl-2-(pyroglutamoyloxy]-n-pelargonate ethyl-2-[pyroglutamoyloxy]-3-hydroxybutyrate iso-propyl-2-[pyroglutamoyloxy]-n-propionate iso-propyl-2-[pyroglutamoyloxy]-n-caprylate n-propyl-2-[pyroglutamoyloxy]-n-propionate n-propyl-2-[pyroglutamoyloxy]-n-caprylate stearyl-2-[pyroglutamoyloxy]-n-propionate 12-hydroxystearyl-2-[pyroglutamoyloxy]-n-propionate stearyl-2-[pyroglutamoyloxy]-n-stearate palmityl-2-[pyroglutamoyloxy]-n-propionate linoleyl-2-(pyroglutamoyloxy]-n-propionate linoleyl-2-[pyroglutamoyloxy]-n-caprylate lauryl-2-[pyroglutamoyloxy]-n-caprylate stearyl-2-[pyroglutamoyloxy]-n-caprylate glyceryl mono(2-[pyroglutamoyloxy]-n-propionate) glyceryl mono(2-[pyroglutamoyloxy]-n-caprylate) glyceryl di(2-[pyroglutamoyloxy]-n-propionate), and mixtures thereof
Claim 42
Dependent Claim
35 words
A composition according to claim 37, in which the penetration enhancer is chosen from: Dimethyl sulphoxide N,N-Dimethyl acetamide N,N-Dimethyl formamide 2-Pyrrolidonel-Methyl-2-pyrrolidone 5-Methyl-2-pyrrolidone 1,5-Dimethyl-2-pyrrolidone 1-Ethyl-2-pyrrolidone Phosphine oxides Sugar esters Tetrahydrofurfural alcohol Urea Diethyl-m-toluamide 1-Dodecylazacyloheptan-2-one,.and mixtures thereof.
Claim 43
Dependent Claim
17 words
A composition according to claim 37, in which the penetration enhancer comprises an anionic surface active agent.
Claim 44
Dependent Claim
50 words
A composition according to claim 43, in which the anionic surface active agent is chosen from: metallic or alkanolamine salts of fatty acids alkyl benzene sulpharates alkyl sulphates alkyl ether sulphates sulphosuccinates monoglyceride sulphates isethionates methyl taurides acyl sarcosinates acyl peptides acyl lactylates polyalkoxylated ether glycollates phosphates, and mixtures thereof.
Claim 45
Dependent Claim
27 words
A composition according to claim 37, in which the penetration enhancer comprises a catonic surface active agent chosen from: amine salts quaternary ammonium salts, and mixtures thereof.
Claim 46
Dependent Claim
27 words
A composition according to claim 37, in which the penetration enhancer comprises an amphoteric surface active agent chosen from: imidazol compounds N-alkylamino acids betaines, and mixtures thereof
Claim 47
Dependent Claim
18 words
A composition according to claim 37, in which the penetration enhancer is chosen from nonionic surface active agents.
Claim 48
Dependent Claim
34 words
A composition according to claim 47, in which the nonionic surface active agent is chosen from: fatty acid alkanolamides esters of polyalcohols polyglycerol esters polyalkoxylated compounds ethers ester ethers amine oxides, and mixtures thereof.
Claim 49
Dependent Claim
20 words
A composition according to any preceding claim which is in the form of a lotion, cream, shampoo or hair conditioner.
Claim 50
Dependent Claim
25 words
The use of a chemical inhibitor chosen from proteoglycanase inhibitors, glycosaminoglycanase inhibitors, glycosaminoglycan chain cellular uptake inhibitors and mixtures thereof in the treatment of baldness.
Claim 51
Dependent Claim
25 words
The use of a chemical inhibitor chosen from proteoglycanase inhibitors, glycosaminoglycanase inhibitors, glycosaminoglycan chain cellular uptake inhibitors and mixtures thereof in the treatment of baldness.
Claim 52
Independent Claim
35 words
A method for inducing, maintaining or increasing hair growth in the human subject which comprises applying an effective amount of a composition according to any of claims 1 to 49 to the scalp or hair.