Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Reexamination Certificate
2002-02-12
2003-05-13
Reamer, James H (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
C514S120000, C514S121000, C514S134000
Reexamination Certificate
active
06562803
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to a hair-growing agent comprising a phosphatidic acid as an active ingredient.
A known example of a cosmetic or drug relating to hair which comprises a phosphatidic acid is a hair-nourishing agent comprising a phosphatidic acid having straight-chain fatty acid residues having an odd number of carbon atoms, that is, a phosphatidic acid represented by formula (II):
(wherein R
2
and R
3
each represents an aliphatic hydrocarbon group; and at least one of R
2
and R
3
is a straight-chain aliphatic hydrocarbon group having an even number of carbon atoms) (Japanese Published Examined Patent Application No. 41363/88). Japanese Published Unexamined Patent Application No. 7205/86 describes a cell activator comprising a phosphatidic acid having two branched-chain fatty acid residues as an active ingredient. However, there has not been known a hair-growing agent comprising a phosphatidic acid wherein all fatty acid residues are straight-chain fatty acid residues having an even number of carbon atoms and which has an acetyl group at the 2-position of the glycerin residue. Japanese Published Unexamined Patent Application No. 15809/86 describes a cell activator comprising a fatty acid having an odd number of carbon atoms, and biotin or vitamin B12 as active ingredients.
It is known that a phosphatidic acid is used as a vehicle for liposome preparation added to minoxidil which is a hair growth-activating component (U.S. Pat. No. 5,030,442), though not as an active ingredient of a hair-growing agent.
A mixture of some phospholipids including a phosphatidic acid is known to have hair loss-inhibiting activity (WO 97/09989). Also known is a hair-growing agent comprising a phospholipid mixture (DE 3222016, DE 4113346).
WO 96/00561 describes a hair-growing agent comprising proanthocyanidin. It is known that tocopherol [“Ke no Igaku” (Medical Science of Hair), p. 283, Bunkodo (1987); Hair Science, p. 80, Japan Hair Science Association (1986)], pantothenic acid and biotin [Fragrance Journal, p. 95-103, Fragrance Journal (1989)], and a protein kinase C-specific inhibitor [Skin Pharmacology and Applied Skin Physiology, 13, 133-142 (2000)] each have hair-growing activity. However, there is no report on a hair-growing agent comprising, as active ingredients, a phosphatidic acid, and one or more members selected from the group consisting of proanthocyanidin, tocopherol, derivatives of tocopherol, pantothenic acid, derivatives of pantothenic acid, protein kinase C-specific inhibitors or pharmaceutically acceptable salts thereof and biotin.
SUMMARY OF THE INVENTION
The present invention provides a hair-growing agent comprising a phosphatidic acid as an active ingredient, which has an excellent hair-growing effect, and a hair-growing agent comprising, as active ingredients, a phosphatidic acid, and one or more members selected from the group consisting of proanthocyanidin, tocopherol, derivatives of tocopherol, pantothenic acid, derivatives of pantothenic acid, protein kinase C-specific inhibitors or pharmaceutically acceptable salts thereof and biotin.
The present invention relates to the following subject matters.
(1) A hair-growing agent comprising, as an active ingredient, a phosphatidic acid represented by formula (I):
(wherein R
1
represents straight-chain alkyl having an odd number of carbon atoms, straight-chain alkenyl having an odd number of carbon atoms, or straight-chain alkynyl having an odd number of carbon atoms).
(2) The hair-growing agent according to the above (1), wherein the straight-chain alkyl having an odd number of carbon atoms is undecyl, tridecyl, pentadecyl or heptadecyl, and the straight-chain alkenyl having an odd number of carbon atoms is pentadecenyl or heptadecenyl.
(3) A hair-growing agent comprising, as active ingredients, the phosphatidic acid according to the above (1) or (2), and one or more members selected from the group consisting of proanthocyanidin, tocopherol, derivatives of tocopherol, pantothenic acid, derivatives of pantothenic acid, protein kinase C-specific inhibitors or pharmaceutically acceptable salts thereof and biotin.
(4) The hair-growing agent according to the above (1) or (2), further comprising proanthocyanidin.
(5) The hair-growing agent according to the above (4), wherein the proanthocyanidin is one or more members selected from the group consisting of procyanidin B-1, procyanidin B-2, procyanidin B-3, procyanidin C-1 and procyanidin C-2.
(6) The hair-growing agent according to any of the above (1), (2), (4) and (5), further comprising tocopherol or a derivative of tocopherol.
(7) The hair-growing agent according to the above (6), wherein the tocopherol or the derivative of tocopherol is one or more members selected from the group consisting of dl-&agr;-tocopherol, d-&agr;-tocopherol, dl-&agr;-tocopherol acetate, d-&agr;-tocopherol acetate and dl-&agr;-tocopherol nicotinate.
(8) The hair-growing agent according to any of the above (1), (2) and (4) to (7), further comprising pantothenic acid or a derivative of pantothenic acid.
(9) The hair-growing agent according to the above (8), wherein the pantothenic acid or the derivative of pantothenic acid is one or more members selected from the group consisting of calcium pantothenate, sodium pantothenate, D-pantothenyl alcohol, DL-pantothenyl alcohol and pantothenyl ethyl ether.
(10) The hair-growing agent according to any of the above (1), (2) and (4) to (9), further comprising a protein kinase C-specific inhibitor or a pharmaceutically acceptable salt thereof.
(11) The hair-growing agent according to the above (10), wherein the protein kinase C-specific inhibitor is one or more members selected from the group consisting of calphostin C, hexadecylphosphocholine, palmitoyl-DL-carnitine and polymyxin B.
(12) The hair-growing agent according to any of the above (1), (2) and (4) to (11), further comprising biotin.
(13) The hair-growing agent according to any of the above (1) to (12), which does not substantially comprise minoxidil.
(14) A method for stimulating hair growth in a mammal, which comprises applying to the skin of said mammal a phosphatidic acid represented by formula (I):
(wherein R
1
represents straight-chain alkyl having an odd number of carbon atoms, straight-chain alkenyl having an odd number of carbon atoms, or straight-chain alkynyl having an odd number of carbon atoms).
(15) A method for stimulating hair growth in a mammal, which comprises applying to the skin of said mammal the phosphatidic acid according to the above (14), and one or more members selected from the group consisting of proanthocyanidin, tocopherol, derivatives of tocopherol, pantothenic acid, derivatives of pantothenic acid, protein kinase C-specific inhibitors or pharmaceutically acceptable salts thereof and biotin.
DETAILED DESCRIPTION OF THE INVENTION
In the definition of each group in formula (I), the straight-chain alkyl having an odd number of carbon atoms includes those having 1 to 23, preferably 7 to 19 carbon atoms, such as methyl, propyl, pentyl, heptyl, nonyl, undecyl, tridecyl, pentadecyl, heptadecyl, nonadecyl, heneicosyl and tricosyl. Preferred are undecyl, tridecyl, pentadecyl and heptadecyl. The straight-chain alkenyl having an odd number of carbon atoms includes those having 3 to 23, preferably 7 to 19 carbon atoms, such as allyl, 1-propenyl, 2-pentenyl, 4-pentenyl, pentadienyl, heptenyl, nonenyl, undecenyl, tridecenyl, pentadecenyl, heptadecenyl, nonadecenyl, heneicosenyl and tricosenyl. Preferred are pentadecenyl and heptadecenyl. The straight-chain alkynyl having an odd number of carbon atoms includes those having 3 to 23, preferably 7 to 19 carbon atoms, such as propynyl, pentynyl, heptynyl, nonyl, undecynyl, tridecynyl, pentadecynyl, heptadecynyl, nonadecynyl, heneicosynyl and tricosynyl. The number and position of unsaturated bonds in the alkenyl and the alkynyl are not specifically restricted.
The phosphatidic acids to be used in the present invention can be obtained mainly by chemical synthesis [ref
Honda Shinkichi
Kamimura Ayako
Mimura Takashi
Takahashi Tomoya
Fitzpatrick ,Cella, Harper & Scinto
Kyowa Hakko Kogyo Co. Ltd.
Reamer James H
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