MXPA00002847A - Reduction of hair growth - Google Patents

Reduction of hair growth

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Publication number
MXPA00002847A
MXPA00002847A MXPA/A/2000/002847A MXPA00002847A MXPA00002847A MX PA00002847 A MXPA00002847 A MX PA00002847A MX PA00002847 A MXPA00002847 A MX PA00002847A MX PA00002847 A MXPA00002847 A MX PA00002847A
Authority
MX
Mexico
Prior art keywords
aminoacyl
inhibitor
trna synthetase
hair growth
amino
Prior art date
Application number
MXPA/A/2000/002847A
Other languages
Spanish (es)
Inventor
Gillette Company The
James P Henry
Gurpreet S Ahluwalia
Original Assignee
Gillette Company The
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Publication date
Application filed by Gillette Company The filed Critical Gillette Company The
Publication of MXPA00002847A publication Critical patent/MXPA00002847A/en

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Abstract

Mammalian hair growth is reduced by applying an inhibitor of aminoacyl-tRNA synthetase to the skin.

Description

REDUCTION OF HAIR GROWTH The invention relates to the reduction of hair growth in mammals. A major function of hair in mammals is to provide protection against the environment. However, this function has been lost in humans in essentially, in which the hair is preserved or removed from various parts of the body essentially for aesthetic reasons. For example, it is generally preferred to have hair on the scalp but not on the face. Several procedures have been used to remove unwanted hair, including shaving, electrolysis, waxing creams or lotions, waxing, tearing, and therapeutic antiandrogens. These conventional methods generally have disadvantages associated therewith. Shaving, for example, can cause scratches and cuts, and may leave a perception of an increase in growth in the proportion of hair regrowth. Shaving can also leave an undesirable wall. Electrolysis, on the other hand, can in a treated area keep it free of hair for "" long periods of time, but it can be expensive, painful, and sometimes scarring. Hair removal creams, REF .: 33176 Although very effective, they are typically not recommended for frequent use due to their high potential irritation. The waxing and tearing can cause pain, discomfort, and poor hair removal. Finally, antiandrogens - which have to be used to treat female hirsutism - can have unwanted side effects.
It has previously been revealed that the proportion and type of hair growth can be changed by the application of the inhibitor of certain enzymes on the skin. These inhibitors include the inhibitors of 5-alpha reductase, ornithine decarboxylase, s-adenosylmethionine decarboxylase, gamma-glutamyl transpeptidase, and transglutaminase. See, for example, Breuer et al., U.S. Pat. No. 4,885,289; Shander, U.S. Pat. No. 4,720,489; Ahluwalia, U.S. Pat. 5,095,007; Ahluwalia et al., U.S. Pat. No. 5,096,911; Shander et al.], U.S. Pat No. 5,132,293; and Shander et al, U.S. Pat. No. 5,143,925.
Aminoacyl-tRNA synthetases are a family of enzymes that are involved in the synthesis of cellular protein. In particular, the enzymes involved in the activation of amino acids and the subsequent binding of amino acids to the corresponding tRNA. There is at least one inoperable-tRNA for each of the twenty natural amino acids that protein molecules make. Aminoacyl-tRNA synthetase are described, for example, in P, Schi mel (1987) Ann. Rev. Biochem. 65: 125-158.
It has now been found that unwanted hair growth in mammals (including man) - hair growth particularly stimulated by androgen - can be reduced by the application of a dermatologically acceptable skin composition including an aminoacyl-tRNA inhibitor. synthetase in an effective amount to reduce hair growth. The growth of unwanted hair which is reduced may be normal hair growth, or hair growth as a result of an abnormality or a condition of a disease.
Examples of aminoacyl-tRNA inhibitors include S-trityl-L-cysteine: L-asparaginamide; 4-aza-DL-leucine; DL-serine hydroxamate; proflavine (hemisulfate salt); L-isoleucinol; N-phenylglycine; L-leucinol; L-methioninol; fe-leu-amide; tyramine; L-isoleucinol; 3, 4-dehydro-DL-proline; S-carbamyl-L-cysteine; α-methyl-DL-methionine; chlorine-L-alanine; cis-hydroxy proline; L-prolinol; L-histidonol; L-tirprofan hydroxamate; DL-4-thiaisoleucine; DL-amino-e-caprolactam; L-aspartic acid amide; DL-β-hydroxynorvaline; cis-4-fluoro-L-proline; trans-4-fluoro-L-carboxylic acid; α-methyl-DL-histidine; N-formyl-L-histidine; L-2-amino-3-sulfamoylpropinoic acid; ß-hydroxamate of L-aspartic acid; β-cyano-L-alanine; selenocistamine; 4-amino-n-butyric acid amide; DL-5-hydroxylysine; L-lisinhydroxamate; 3- (N-phenylacetyl) amino-2,6-piperidinedione (antineoplaston A10); 4-amino-4-phosphonobutyric acid; ethionamide; 1,2-diamino-3 (4-imidazolyl) propane (histidinamine); ct-methylhistidine; (S) -2-methylbutylamine; L-O-methyl threonine; DL-armentomycin (2-amino-4,4-dichlorobutyric acid); DL-3-dehydroarmentomycin; DL-3-dihydroxyleucine; 5, 5, 5-trifluoro-DL-leucine; β- (3-aminocyclohexyl) -DL-alanine; DL-p-chloroamphetamine; trans-2,6-diaminohex-4-enoic acid; DL-2, 6-diftali idocaproic acid methyl ester; DL-5-hydroxylysine; L-lisinhydroxamate; DL-4-oxalisin; DL-4-selenalysin; L-methioninamide; 2-amino-4-methylhex-4-enoic acid; (SS, 2S) -2-amino-1-phenyl-1,3-propanediol; N-benzyl-D-amphetamine; N-benzyl-L-phenylamine; N-benzyl-D-phenylethylamine; 1,3-bis (acetoxy) -2-nitro-l-phenylpropane (phenytopane); 1,2-diamino-3- (2,6-dichloro-phenyl) propane; 1,2-diamino-3-hydroxy-5-phenylpentane; 1,2-diamino-3-phenylpropane; N- (2,6-dichlorobenzylidene) -2-phenylethylamine; N- (2,6-dichlorobenzyl) 2-phenylostylamine; N- (4-fluorobenzyl) -L-phenylalanine; DL-2-fluorophenylalanine; 2-hydroxyethyl-2-phenylammonium sulfate; α- and β-methyl-DL-phenylalanine; L-phenylalaninol; L-a-phenylglycerin; DL-threo-β-phenylserine; β-2-thienyl-DL-alanine; cyclohexyl ester of N-trifluoroacetyl-L-phenylalanine; oxalate 2-amj inomethyl-4-isopropyloxypyrrolidine; 2-amino-methylpyrrolidine; L-4-thiaproline; N-benzylethanolamine; N- (2,6-dichlorobenzyl) ethanolamine; N- (2,6-dichloro-benzylidone) ethanolamine; DL-ßP-hydroxyleucine; 1,2-diamino-5-phenyl-3-pentanol; DL-7-azatriptofan; DL-4- and DL-6-fluorotriptofan; 5-hydroxy-tryptamine; L-5-hydroxytryptophan; DL-a-methyltriptamine; α- and β-methyl-DL-tryptophan; Tryptamine; DL-2-amino-1- (4-hydroxyphenyl) -1-propanol; DL-3-fluoro-tyrosine; 3-iodine-L-tyrosine; 3-nitro-L-tyrosine; L-tyrosinol-HCl; L-threo-2-amino-3-chlorobutyric acid; hexafluoro-DL-valine; DL-norvaline; L-4-tialisine; DL-ethionine; N, N'-di-CBZ-L-lysine; DL-3-fluorophenylalanine; DL-4-fluorophenyl-alanine; and DL-3,4-dihydroxyphenylalanine. These compounds are known-s-.
Many of the examples of aminoacyl-tRNA inhibitors are amino acids and inhibit the aminoacyl-tRNA synthetase associated with the amino acid analogs, although a particular inhibitor can sometimes inhibit the aminoacyl-tRNA synthetase associated with more than one amino acid. The term "The inhibitor of [amino acid name] aminoacyl-RNAt synthetase" is used herein, a compound that inhibits at least the aminoacyl-tRNA associated with the amino acid. The amino acid can be one of the 20 naturally occurring amino acids (e.g. leucine, serine etc), or some other amino acid. As used herein, "Aminoacyl-RNAT synthetase inhibitors" and an "Aminoacyl-tRNA synthetase inhibitor" means a compound that inhibits one or more aminoacyl-tRNA synthetase.
The aminoacyl-tRNA synthetase inhibitor is preferably incorporated into a topical composition that includes a non-toxic dermatologically acceptable carrier or carrier or a carrier which is adapted to be expanded on the skin. Examples of suitable carriers are acetones, alcohols, or a cream, lotion, or gel which can effectively deliver the active compound. A vehicle is disclosed in U.S. Pat. No. 5,648,394. In sum, a better penetration can be added to the vehicle to encourage the increase in the effectiveness of the formulation.
The concentration of the inhibitor in the composition can vary over a wide range to the saturated solution, preferably from 0.1% to 30% by weight or even more; The reduction in hair growth increases with the increase in the amount of inhibitor applied per unit area of skin. The maximum amount applied effectively is limited only by the proportion of the inhibitor which penetrates the skin. The effective amounts may vary, for example, from 10 to 3000 micrograms or more per square centimeter of skin.
A composition may include more than one aminoacyl-tRNA synthetase inhibitor. For example, the composition may include two inhibitors of an aminoacyl-tRNA synthetase associated with a particular amino acid, or may include an inhibitor of an aminoacyl-tRNA synthetase associated with a first amino acid and an inhibitor of an associated aminoacyl-RNAt synthetase with a second amino acid. The composition may optionally also include another compound that are known to reduce hair growth where they are typically applied.
The composition should be topically applied in a selected area of the body in which it is desired to reduce hair growth. For example; the composition can be applied to the face, particularly in the area of the face beard, i.e., the cheek, the neck, the upper lip, and the chin. The composition can also be applied on the legs, arms, torso and armpits. The composition is particularly suitable for reducing unwanted hair growth in women victims of irsutism or in other conditions. The duration of treatment may vary depending on how the reduction of hair growth is perceived, for example, the separation and location of unwanted hair. In humans, the composition, for example, can be applied once or twice a day, or even more frequently, from two weeks to six months (e.g. three months) to achieve the realization of the reduction of hair growth. The reduction in hair growth is demonstrated when the frequency or removal of the hair is reduced, or the subject perceives less hair at the treated site, or quantitatively, when the hair weight removed by shaving (ie, the hair mass) It is reduced. ~ Golden Syrian intact male hamsters are considered acceptable models for the growth of human hair on lateral sides that have oval shaped bodies, one on each side, each in a diameter greater than approximately 8 mm, whose thickness Black grows and coarse hair is similar to the hair of the human beard. These organs produce hair in response to androgens in the hamster. To evaluate the effectiveness of a composition that includes an aminoacyl-tRNA synthetase inhibitor, the ijar organs of each of a Hamster group are shaved. For an organ of each animal 10 μl of vehicle was applied only once a day, while the other organ of each animal was applied an equal amount of vehicle containing an aminoacyl-tRNA inhibitor. After thirteen applications (one application per day for five days a week), the ijar organs are shaved and the amount of hair recovered (the hair mass) of each is heavy. The percentage of hair growth reduction is calculated by subtracting the value of the hair mass (mg) from the treated side of the test compound from the value of the hair mass of the treated side of the vehicle; and the delta value obtained is then divided by the value of the hair mass of the treated side of the vehicle, and the resulting number is multiplied by 100.
The test described above is attributed here as the essay "The Golden Syrian Hamster". Preferred compositions provide a reduction in hair growth of a little less than 25%, more often a little less than 50% and still more frequently a little less than 60% when examined in the Golden Syrian Hamster test. A number of compositions containing an inhibitor of aminoacyl-tRNA synthetase synthesis was examined in the Golden Syrian Hamster assay; The results are shown in Table 1 : TABLE 1 Inhibitor Dose Vehicle £ H Control Treaty% of () (mg) (mg) inhibition S-trityl-L-cysteine 7.5 A 6.5 0.35 +/- .10 1.64 +/- .14 80 +/- .6 L-asparaginamide 10 B 5 1.00 +/-, .24 2.60 +/- .42 66 +/- 7 4-aza-DL-leucine ° 2HCl 10 B 5.5 0.70 +/- .08 2.02 +/- .27 66 +/- 3 DL-a-amino-e-caprolactam 10 D 6.6 0.90 +/-, .16 2.30 +/- .11 59 +/- 9 hydroxamate DL-serine 10 B 7.5 1.28 +/- .17 2.94 +/- .34 56 +/- 5 Hemisulphate proflavine 10 C 5.5 1.41 +/- .19 3.04 +/- .24 52 +/- 7 L-Isoleucinol 10 B 7.5 1.20 +/- .21 2.40 +/- .38 51 +/- 9 N-phenylglycine 10 D 3.0 1.37 +/- .19 2.84 +/- .22 51 +/- 8 L-leucinol 10 E 8.0 1.55 +/- .22 2.86 +/- .34 46 +/- 4 L-prolinol 10 B 7.5 1.31 +/- .19 2.43 +/- .26 45 +/- 6 L-histidonal 10 D 7.4 1.88 +/- .26 3.46 +/- .18 45 +/- 7 L-methioninol 10 E 7.5 1.55 +/- .14 2.72 +/- .27 42 +/- 3 Fe-leu-amide 10 F 4.5 1.18 +/- .23 1.95 +/- .19 41 +/- 8 Tyramine 10 B 5.0 1.20 +/- .19 2.10 +/- .13 41 +/- 10 3, 4-dehydro-DL-proline 10 B 6.0 1.18 +/- .18 2.00 +/- .11 39 +/- 9 DL-β-hydroxynorvaline 10 B 6.0 0.81 +/- .15 1.40 +/- .11 38 +/- 13 S-carbamyl-L-cysteine 7.5 G 4.5 1.71 +/- .17 2.55 +/- .29 32 +/- 6 -methyl-DL-methionine 15 B 6.5 1.10 +/- .15 1.70 +/- .40 31 +/- 7 L-aspartic amide acid 10 I 6.9 1.38 +/- .14 1.99 +/- .21 30 +/- 5 Chlorine-L-alanine-HLC 10 B 4.5 2.38 +/- .27 3.26 +/- .26 25 +/- 9 Cis-hydroxy-proline 10 B 5.5 1.96 +/- .18 2.60 +/- .22 24 + / - 7 DL-4-thiaisoleucine 10 B 5.0 2.36 +/- .26 3.08 +/- .16 23 +/- 9 Lucinamide 10 B 4.6 2.13 +/- .28 2.77 +/- .26 22 +/- 10 hydroxamate L-tirprofan 10 H 8 0.88 +/- .10 1.10 +/- .15 10 +/- 17 Vehicles: A-90% H20, 6% dipropylene glycol, and 4% ethanol B-68% water, 16% ethanol, 5% propylene glycol; 5% dipropylene glycol, 4% benzyl alcohol, and 2% propylene carbonate. C-92% water, 3% propylene carboan, and 5% benzyl alcohol. D-80% ethanol, 17.5% water, 2% prolylene glycol diperlargonate (Emerest 2388), and 0.5% propylene glycol. t E-50% dipropylene glycol and 50% ethanol. I F-60% ethanol, 25% dimethyl sulfoxide, 13.1% water, 1.5% propylene glycol dipelargonate (Emerest 2388), and 0.38% propylene glycol. G-95.6% water and 4.4% dimethyl sulfoxide. H-100% dimethyl sulfoxide. 1-84% water, 8% ethanol, 2.5% propylene glycol, 2.5% dipropylene glycol, 2% l, benzyl alcohol, and 1% propylene carbonate.
A study of the response to dosing with S-trityl-L-cysteine indicates that an increase in the concentration of the inhibitor in the composition results in an increased reduction in hair growth. The results are shown in Table 2.
TABLE 2 Inhibition response to hair growth by the dosage of S-trityl-L-cysteine Compound Dosage pH Treated Control% inhibition (mg) S-tri-cysteine 7. 5% 6.5 0.35 +/-. 10 1. 64 +/-. 14 80 +/- 6 S-tri-il-cysteine 5% 6. 5 0. 90 +/-. 17 1. 95 +/-. 35 56 +/- 6 S-trityl-cysteine 1% 5. 5 0. 88 +/-. 10 1. 10 +/-. 15 35 +/- 9 10 Vehicle: 90% H20, 6% dipropylene glycol, 4% ethanol.
Inhibition of aminoacyl-tRNA synthetase in the hair follicle was determined using a modification of the procedure described by Hampel et al (Aminoacyl-tRNA Synthetase from Cultured CHO Cells (1979) Methods in Enzymology, Vol. LIX .PP 229-234 ). A reaction mixture containing the following was used for each assay; 50mM Tris (pH 7.4), 15mM MgCl2, 0.5mM EDTA (adjusting the pH to 7), 5mM ATP (adjusting the pH to 7, 0.35 mM CTP, 20 μM 14C amino acid and tRNA (50μg / ml). Synthesis of leucine and serine tRNA was attempted with a buffer pH 8.6 and a concentration of 8 mM MgCl2. The reaction mixture was mixed with the hair follicle extract so that the volume of the final assay is 100μL. Typically 90-95μL of the reaction mixture are mixed with -10μL of hair follicle extract. The reaction was carried out at 37 ° C for 60 minutes. The reaction is terminated by removing the reaction mixture and placing it on a piece of filter paper which was wet with 10% trichloroacetic acid. The filter paper was washed three times in 10% trichloroacetic acid and three times in 5% trichloroacetic acid. The filter paper was dried and the insoluble radioactivity corresponding to 14C-aminoacyl-tRNA was counted in a scintillation counter.
The incorporation of the amino acid 1C varies from 178"dpm / mM to 3.093 dpm / mM in the assays of the amino acids mentioned above.Using this assay, the incorporation of leucine into newly inhibited synthesized proteins was found.
In short, the incorporation of serine into synthesized proteins was again inhibited by DL-serine hydroxamate. Other embodiments are within the claims. DECLARATION THAT INCLUDES PROCESS It is stated that in relation to this date, the best method known by the applicant to carry out the aforementioned invention, is that which is clear from the present description of the invention.
Having described the invention as above, the content of the following is claimed as property.

Claims (74)

1. A method for reducing hair growth in mammals characterized in that: it is selected the area of the skin from which it is desired to reduce hair growth; and a dermatologically acceptable composition including an aminoacyl-tRNS synthetase inhibitor in an amount effective to reduce hair growth is applied in said skin area.
2. The method of claim 1, characterized in that said amino acid synthesis includes the alanine aminoacyl-tRNA synthetase.
3. The method of claim 1, characterized in that said synthesis of aminoacyl-tRNA includes that of arginine aminoacyl-tRNA synthetase.
4. The method of claim 1, characterized in that said aminoacyl-tRNA synthetase includes asparagine aminoacyl-tRNA synthetase.
5. The method of claim 1, characterized in that said aminoacyl-tRNA synthetase includes. aspartic acid aminoacyl-tRNA synthetase.
6. The method of claim 1, characterized in that said aminoacyl-tRNA synthetase includes the cysteine aminoacyl-tRNA synthetase.
7. The method of claim 1; characterized in that said aminoacyl-tRNA synthetase includes glutamine aminoacyl-tRNA synthetase.
8. The method of claim 1, characterized in that said aminoacyl-tRNA synthetase includes glutamic acid aminoacyl-tRNA synthetase.
9. The method of claim 1, characterized in that said aminoacyl-tRNA synthetase includes glycine aminoacyl-tRNA synthetase.
10. The method of claim 1, characterized in that said aminoacyl-tRNA synthetase includes the histidine aminoacyl-tRNA synthetase.
11. The method of claim 1, characterized in that said aminoacyl-tRNA synthetase includes isoleucine aminoacyl-tRNA synthetase.
12. The method of claim 1, characterized in that said aminoacyl-tRNA synthetase includes the leucine aminoacyl-tRNA synthetase.
13. The method of claim 1, characterized in that said aminoacyl-tRNA synthetase includes the aminoacyl-tRNA synthetase lysine.
14. The method of claim 1, characterized in that said aminoacyl-tRNA synthetase includes methionine aminoacyl-tRNA synthetase.
15. The method of claim 1, characterized in that the aminoacyl-tRNA synthetase includes the phenylalanine aminoacyl-tRNA synthetase.
16. The method of claim 1, characterized in that the aminoacyl-tRNA synthetase includes the proline aminoacyl-tRNA synthetase.
17. The method of claim 1, characterized in that the aminoacyl-tRNA synthetase includes the serine aminoacyl-tRNA synthetase.
18. The method of claim 1, characterized in that the aminoacyl-tRNA synthetase includes the threonine aminoacyl-tRNA synthetase.
19. The method of claim 1, characterized in that the aminoacyl-tRNA synthetase includes the tryptophan aminoacyl-tRNA synthetase.
20. The method of claim 1, characterized in that the aminoacyl-tRNA synthetase includes the tyrosine aminoacyl-tRNA synthetase.
21. The method of claim 1, characterized in that the aminoacyl-tRNA synthetase includes valine aminoacyl-tRNA synthetase.
22. The method of claim 1, characterized in that said inhibitor includes S-trityl-L-cysteine.
23. The method of claim 1, characterized in that said inhibitor includes L-asparaginamide.
24. The method of claim 1, characterized in that said inhibitor includes 4-aza-DL-leucine.
25. The method of claim 1, characterized in that said inhibitor includes DL-serine hydroxamate.
26. The method of claim 1, characterized in that said inhibitor includes proflavine (hemisulfate salt).
27. The method of claim 1, characterized in that said inhibitor includes L-isoleucinol.
28. The method of claim 1, characterized in that said inhibitor includes N-phenylglycine.
29. The method of claim 1, characterized in that said inhibitor includes L-leucinol.
30. The method of claim 1, characterized in that said inhibitor includes L-methioninol.
31. The method of claim 1, characterized in inhibitor includes phe-leu-amide.
32. The method of claim 1, characterized in inhibitor includes tyramine.
33. The method of claim 1, characterized in inhibitor includes L-isoleucinol.
34. The method of claim 1, characterized in inhibitor includes 3,4-dehydro-DL-proline.
35. The method of claim 1, characterized in inhibitor includes S-carbamyl-L-cysteine.
36. The method of claim 1, characterized in inhibitor includes a-methyl-DL-methionine.
37. The method of claim 1, characterized in inhibitor includes chloro-L-alanine.
38. The method of claim 1, characterized in inhibitor includes cis-hydroxy proline.
39. The method of claim 1, characterized in inhibitor includes L-prolinol.
40. The method of claim 1, characterized in inhibitor includes t-histidonol.
41. The method of claim 1, characterized in inhibitor includes L-tirprofan hydroxamate.
42. The method of claim 1, characterized in inhibitor includes thioisoleucine.
43. The method of claim 1, characterized in inhibitor includes DL-amino-e-caprolatam.
44. The method of claim 1, characterized in inhibitor includes L-aspartic acid amide.
45. The method of claim 1, characterized in inhibitor includes DL-β-hydroxynorvaline.
46. The method of claim 1, characterized in inhibitor is selected from the group consisting of 4-fluoro-L-proline; trans-4-fluoro-L-carboxylic acid; α-methyl-DL-histidine; N-formyl-L-histidine; L-2-amino-3-sulfamoylpropionic acid; L-aspartic acid-β-hydroxamate; β-cyano-L-alanine; selenocitamin; and 4-amino-n-butyric acid amide.
47. The method of claim 1, characterized in that said inhibitor is cleaved from the group consisting of DL-5-hydroxylysine; L-lisinhydroxamate; 3- (N-phenylacetyl) amino-2,6-piperidinedione (antineoplaston A10); 4-amino-4-phosphonobutyric acid; ethionamide; 1,2-diamino-3 (4-imidazolyl) propane (histidinamine); a-methylishisidine; (S) -2-methylbutylamine; L-O-methyl threonine; and DL-armentomicin (2-amino-4, 4-dichlorobutyric acid).
48. The method of claim 1, characterized in that said inhibitor is selected from the group consisting of DL-3-dehydroarmentomycin; DL-3-hydroxyleucine; 5,5,5-trifluoro-DL-leucine; β- (3-aminocyclohexyl) -DL-alanine; DL-p-chloroamphetamine; trans-2,6-diaminohex-4-enoic acid; methyl ester of DL-2, 6-diftalimidocaproic acid; DL-5-hydroxylysine; L-lisinhydroxamate; and DL-4-oxalisin .__
49. The method of claim 1, characterized in that said inhibitor is selected from the group consisting of DL-4-selenalysin; L-methioninamide; 2-amino-4-methylhex-4-enoic acid; (SS, 2S) -2-amino-1-phenyl-1,3-propanediol; N-benzyl-D-amphetamine; N-benzyl-L-phenylalanine; N-benzyl-D-phenylethylamine; 1,3-his (acetoxy) -2-nitro-l-phenylpropane (phenytopane); and 1,2-diamino-3- (2,6-dichlorophenyl) propane.
50. The method of claim 1, characterized in that said inhibitor is selected from the group consisting of 1,2-diamino-3-hydroxy-5-phenylpentane; 1,2-diamino-3-phenylpropane; N- (2,6-dichlorobenzylidene) -2-phenylethylamine; N- (2,6-dichlorobenzyl) -2-phenylethylamine; N- (4-fluorobenzyl) -L-phenylalanine; DL-fluorophenylamine; 2-hydroxyethyl-2-phenylammonium sulfate; methyl-DL-phenylalanine; L-phenylalaninol; and L-a-phenylglycine.
51. The method of claim 1, characterized in that said inhibitor is selected from the group consisting of DL-threo-β-phenylserine; β-2-thienyl-DL-alanine; cyclohexyl ester of N-trifluoroacetyl-1-phenylalanine; oxalate 2-aminomethyl-4-isopropyloxypyrrolidine; 2-amino-methylpyrrolidine; L-4-thiaproline; N-benzylethanolamine; N- (2,6-dichlorobenzyl) ethanolamine; N- (2,6-dichlorobenzylidone) ethanolamine; and DL-β-hydroxyquinuezine.
52. The method of claim 1, characterized in that said inhibitor is selected from the group consisting of 1,2-diamino-5-phenyl-3-pentanol; DL-7-azatriptofan; DL-fluro-tryptophan; 5-hydroxytryptamine; L-5-hydroxy-tryptophan; DL-a-methyltriptamine; methyl-DL-tryptophan; Tryptamine; DL-2-amino-1- (4-hydroxyphenyl) -1-propanol; and DL-3-fluorotyrosine.
53. The method of claim 1, characterized in that said inhibitor is selected from the group consisting of 3-iodo-L-tyrosine; 3-nitro-L-tyrosine; L-tyrosinol »HCl; L-threo-2-amino-3-chlorobutyric acid; hexafluoro-DL-valine; DL-nornalin; L-4-tialisine; DL-ethionine; N, N'-di-CBZ-L-lysine; DL-3-fluorophenylalanine; DL-4-fluorophenyl-alanine; and DL-3, 4-dihydroxyphenylalanine.
54. The method of claim 1, characterized in that the concentration of said inhibitor in said composition is between 0.1% and 30%.
55. The method of claim 1, characterized in that the composition provides a reduction in hair growth of at least 20% when tested in the Golden Syrian Hamster assay.
56. The method of claim 1, characterized in that the composition provides a reduction in hair growth of at least 50% when tested in the Golden Syrian Hamster assay.
57. The method of claim 1, characterized in that the composition provides a reduction in hair growth of at least 60% when tested in the Golden Syrian Hamster test.
58. The method of claim 1, characterized in that the inhibitor is applied to the skin in an amount of about 10 to 3000 micrograms of said inhibitor per square centimeter of skin.
59. The method of claim 1, characterized in that said mammal includes the human.
60. The method of claim 59, characterized in that said skin area is on the face of the human.
61. The method of claim 59, characterized in that said skin area is on the legs of the human.
62. The method of claim 59, characterized in that said skin area is on an arm of the human.
63. The method of claim 59, characterized in that said skin area is in an armpit of the human.
64. The method of claim 59, characterized in that said area of the skin is on the torso of the human.
65. The method of claim 59, characterized in that said human is a woman victim of hirsutism.
66. The method of claim 1, characterized in that said hair growth includes hair growth stimulated by androgens.
67. A method according to any one of claims 1 to 66, characterized in that said application of said inhibitor has a cosmetic effect.
68. A method for producing a composition for inhibiting hair growth in mammals, characterized in that it comprises selecting an inhibitor of an aminoacyl-tRNA synthetase, and combining the inhibitor, in an amount effective to reduce hair growth, with a carrier or transporter Dermatologically acceptable, non-toxic.
69. A method according to claim 68, characterized in that said vehicle or conveyor is adapted to be spread on the skin of a mammal.
70. A method according to claim 68 or 69, characterized in that a cosmetic composition is produced.
71. A method according to claim 68, characterized in that said inhibitor is as defined in any of claims 2-53.
72. The new use of an aminoacyl-tRNA synthetase inhibitor to reduce hair growth.
73. A composition when used to inhibit hair growth in mammals, characterized in that it includes an inhibitor of an aminoacyl-tRNA synthetase, in an amount effective to reduce hair growth, and a dermatologically acceptable, non-toxic carrier or carrier.
74. A composition according to claim 73, characterized in that said inhibitor is as defined in any of claims 2-53. 75, A composition according to claim 73, characterized in that it is a cosmetic composition.
MXPA/A/2000/002847A 1997-09-22 2000-03-22 Reduction of hair growth MXPA00002847A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/935,181 1997-09-22

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MXPA00002847A true MXPA00002847A (en) 2001-06-26

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