(19) TZZ _ __T (11) EP 2 512 418 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61Q 7/00 (2006.01) A61K 8/36 (2006.01) 01.11.2017 Bulletin 2017/44 A61K 8/67 (2006.01) A61K 8/92 (2006.01) A61K 31/19 (2006.01) A61K 31/201 (2006.01) (2006.01) (2006.01) (21) Application number: 10795533.8 A61K 31/505 A61K 31/20 (22) Date of filing: 13.12.2010 (86) International application number: PCT/US2010/060005 (87) International publication number: WO 2011/081862 (07.07.2011 Gazette 2011/27) (54) METHODS OF REDUCING HAIR LOSS AND / OR FACILITATING HAIR GROWTH AND / OR REGROWTH VERFAHREN ZUR HEMMUNG VON HAARAUSFALL UND/ODER ZUR FÖRDERUNG DES HAARWUCHSES UN/ODER DES NACHWACHSENS VON HAAREN. MÉTHODE POUR FREINER LA PERTE DE CHEVEUX OU/ET FAVORISER LEUR POUSSE OU REPOUSSE. (84) Designated Contracting States: • MINERVA, Josephine, A. AL AT BE BG CH CY CZ DE DK EE ES FI FR GB Parsippany GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO NJ 07054-1445 (US) PL PT RO RS SE SI SK SM TR • WENDLING, Susan Annandale (30) Priority: 15.12.2009 US 638142 NJ 08801 (US) (43) Date of publication of application: (74) Representative: Kirsch, Susan Edith 24.10.2012 Bulletin 2012/43 Carpmaels & Ransford LLP One Southampton Row (73) Proprietor: Johnson & Johnson Consumer Inc. London WC1B 5HA (GB) Skillman, NJ 08558 (US) (56) References cited: (72) Inventors: DE-A1- 3 133 132 DE-A1- 3 246 265 • HU, Longsheng DE-A1- 4 113 346 FR-A1- 2 167 407 Piscataway FR-A1- 2 569 347 FR-A1- 2 909 870 NJ 08854 (US) GB-A- 2 341 317 JP-A- 3 167 111 • GOLDMAN, Virginia, Streusand US-B1- 7 357 923 ZA-A- 9 505 409 Morris Plains NJ 07950 (US) Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. Notice of opposition shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention). EP 2 512 418 B1 Printed by Jouve, 75001 PARIS (FR) EP 2 512 418 B1 Description Technical Field 5 [0001] The present disclosure relates to methods of retarding hair loss or facilitating hair growth and/or regrowth. More specifically, the present disclosure relates to methods of using the disclosed compositions to increase the rate of terminal hair growth in a mammal. Background of the Present Invention 10 [0002] Alopecia, or hair loss, in its various forms is an ongoing problem afflicting mankind and animals. Men, woman and children can all suffer from alopecia, which can result of one, or a combination of, of factors including genetic factors, hormonal factors, surgery, trauma and stress. The universality of the occurrence of alopecia has led to continuing efforts throughout history to discover compositions for stimulating hair growth and preventing hair loss. 15 [0003] A number of "natural" remedies for alopecia based solely on herbs and plant extracts have been proposed. However, such compounds have proved to have very little if any effect. [0004] Accordingly, an aspect of the present invention is to provide a non-therapeutic method for reducing hair loss and facilitate hair growth and/or regrowth and/or providing a thicker or richer hair coat as described in the claims. [0005] Another aspect of the present disclosure is concerned with therapeutic methods of using compositions com- 20 prising at least one acid, at least one antioxidant and a select fatty acid mixture as described in the claims. [0006] The disclosed compositions can be used to accelerate the onset of the anagen phase of hair growth in a mammal. [0007] DE 32 46 265 A1 discloses a therapeutic agent for promoting hair growth based on a mixture of waxes, animal and vegetable fats and oils, paraffin oil and glycerin, and, as additional active substance-containing components, a citrus fruit juice, a fungus juice and a vitamin E concentrate, as well as optionally conventional diluents, additives, perfumes 25 and/or auxiliaries. [0008] FR 2 909 870 A1 discloses topical use of mono-unsaturated fatty acid, its salts or esters to prevent and/or treat scalp damages. Also disclosed is a cosmetic process to improve the quality of hair and capillary fibers, comprising the application of a composition comprising a mono-unsaturated fatty acid, its salt and/or its ester on the scalp and/or hair. 30 Summary of the Invention [0009] The present application is related to methods for reducing hair loss and/or facilitating hair growth or hair regrowth as described in the claims. More specifically, the methods of this disclosure exhibit enhanced ability to decrease hair loss and/or promote hair growth or regrowth. 35 [0010] The present invention provides a hair regrowth composition comprising a. a safe and effective amount of at least one hair growth or regrowth active selected from the group consisting of minoxidil; and b. from 0.1% to 99%, optionally from 5% to 50%, and optionally from 10% to 40%, optionally from 15% to 30%, by 40 weight of the composition of an admixture, comprising: i. from 0.01% to 99.98%, or optionally 10% to 90%, or optionally from 20% to 70%, or optionally from 25% to 50% or optionally from 30% to 40%, or optionally about 33%, by weight of the admixture of a pyruvic acid selected from the group consisting of pyruvic acid, lithium pyruvate, sodium pyruvate, potassium pyruvate, 45 magnesium pyruvate, calcium pyruvate, zinc pyruvate, manganese pyruvate, methyl pyruvate, salts thereof, and mixtures thereof; ii. from 0.01% to 99.98%, or optionally 10% to 90%, or optionally from 20% to 70%, or optionally from 25% to 50% or optionally from 30% to 40%, or optionally about 33%, by weight of the admixture of an antioxidant; and 50 iii. from 0.01% to 99.98%, or optionally 10% to 90%, or optionally from 20% to 70%, or optionally from 25% to 50% or optionally from 30% to 40%, or optionally about 33%, by weight of the admixture of a fatty acid mixture comprising at least 7, optionally at least 14, and optionally at least 22, unsaturated or saturated fatty acids selected from the group consisting of, but not limited to, butyric acid, caproic acid, caprylic acid, capric acid, 55 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 EP 2 512 418 B1 [0011] The present invention also provides a hair regrowth composition as described in the claims for use in a thera- peutic method of reducing hair loss and/or facilitating hair growth of regrowth, wherein the composition is applied to the skin of a mammal. [0012] The present invention also provides a non-therapeutic method of reducing hairloss and/or facilitating hair growth 5 or hair regrowth comprising the steps of applying to the skin of a mammal in need of such treatment a composition as described in the claims. [0013] In one embodiment, the compositions of the present invention comprise from 5% to 50%, and optionally from 10% to 40%, optionally from 15% to 30%, by weight of the composition of an admixture, comprising: 10 a. from 0.01% to 99.98%, or optionally 10% to 90%, or optionally from 20% to 70%, or optionally from 25% to 50% or optionally from 30% to 40%, or optionally about 33%, by weight of the admixture of an alpha-keto acid which 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 there- of, and mixtures thereof; 15 b. from 0.01% to 99.98%, or optionally 10% to 90%, or optionally from 20% to 70%, or optionally from 25% to 50% or optionally from 30% to 40%, or optionally about 33%, by weight of the admixture of an antioxidant; and c. from 0.01% to 99.98%, or optionally 10% to 90%, or optionally from 20% to 70%, or optionally from 25% to 50% 20 or optionally from 30% to 40%, or optionally about 33%, by weight of the admixture of a fatty acid mixture comprising at least 7, optionally at least 14, and optionally at least 22, unsaturated or saturated fatty acids selected from the group consisting of, but not limited to, 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 25 acid and lignoceric acid. [0014] In another embodiment, the compositions of the present invention comprise from 5% to 50%, and optionally from 10% to 40%, optionally from 15% to 30%, by weight of the composition of an admixture, comprising: 30 a. from 0.01% to 99.98%, or optionally 10% to 90%, or optionally from 20% to 70%, or optionally from 25% to 50% or optionally from 30% to 40%, or optionally about 33%, by weight of the admixture of an acid which 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, and mixtures thereof: 35 b.