Both men and women lose hair for similar reasons. Hair loss in men is often more dramatic, and follows a specific pattern of loss, one of which has been termed ?Male Pattern Baldness" or "Androgenetic Alopecia".
Main causes
Some facts from Japan
(JICST-EPlus - Japanese Science & Technology)
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Assignees currently active with more than 5 patents to their credit during 2000-2005.
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Composition of treatment for causes are identified and categorized as follows:
Cause | Treatment approach | Pathways affected |
---|---|---|
Hormonal effect of androgen | Anti-androgens | Testosterone pathway |
Reduction of blood circulation around hair follicle | Vasodilators (eg. Minoxidil) | NO/cGMP Pathway |
Deactivation of hair matrix cells | Hair matrix cells activator |
|
What causes hair loss?
How do anti-androgens treat hair loss?
Pat/Pub# | Nature | Composition | Composition action |
---|---|---|---|
US20060009430
BLOTECH (2004) |
Natural extracts | Palmetto berry extract (fatty acids & sterols), Pumpkin seed extract (Vitamins-B, alpha-linolenic acid, amino acids and phytosterols), Quercetin (Flavonoids) and Beta-sitosterol (Rice bran, wheat germ, corn oils and soybeans) | Fatty acids ? Inhibit testosterone
Sterols - Mechanism of action unknown. Quercetin results in cell growth cycle. Beta-sitosterol reduce inflammation on scalp |
US20060009427
WARNER LAMBERT(2004) |
Organic compound | New class of 4-cycloalkoxy benzonitrile derivatives and salts | Acts as androgen receptor modulator and blocks formation of DHT. |
US20050085467
WARNER LAMBERT(2004) |
Organic compound | New class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives. | The compounds inhibit, or decrease, activation of androgen receptor by androgens. |
US20050118282
APHIOS Corp (2003) |
Natural extracts | Supercritical fluid isolate of Saw Palmetto and Sperol (Serenoa repens berry) and their analogs or derivatives. | Modulates androgenic activity by inhibiting 5.alpha.-reductase activity. |
US20060009429
Fundacion Pablo Cassara (2003) |
Nucleotide | Pharmacologically active oligonucleotides (encompass both DNA and S-DNA bond) | Oligonucleotides inhibit androgen receptor (AR) expression at very low concentrations in skin and hair follicle |
US20030007941
PFIZER INC (2001) |
Organic compound | Thyromimetic compounds (structurally similar to thyronine) with finasteride, or cyproterone acetate | Activates thyroid hormone receptors in hair follicle which in turn promote elasticisation of follicle walls and hair follicle |
US20030073616
N/A (1995) |
Peptides/nucleic acid | Bradykinin antagonist (peptide of plasma origin from kininogen precursor-kallikrein) | Inhibits synthesis of bradykinin receptors or compounds by binding to B2 receptor |
EP0279010
KAO Corp (1987) |
Natural extracts | Walnut extract (leaves/pericarps) with an organic solvent | Blocks formation of DHT |
What causes hair loss?
How does Minoxidil treat hair loss?
Pat/Pub# | Nature | Composition | Composition action |
---|---|---|---|
US20040157856
WARNER LAMBERT(2002) |
Organic compound | Benzopyran compounds | Rapidly metabolizes, and causes reduced cardiovascular effects as compared to other known potassium channel openers |
US20050053572
LG HOUSEHOLD & HEALTH CARE(2001) |
Natural extracts | Sophora flavescens extract (alkaloids & flavonoids, luteolin-7-glucose and cytosine) Hinokitiol (Taiwan hinoki oil, Aomori, Western Red Cedar oil) and Nicotinamide (Vitamin B complex) | Promotes function of cell activity and dilates blood vessels |
What is the problem with using only Anti-androgen therapy?
What is the problem with using only Vasodilator (or Minoxidil only) therapy?
How is the combination of Anti-androgens and Vasodilator (or Minoxidil) effective?
Pat/Pub# | Nature | Composition | Composition action |
---|---|---|---|
US20060052405
N/A(2000) |
Peptides | Testosterone blocker or vascular toner (Flutamide, cyproterone acetate, spironolactone, progesterone, or analogs or derivatives) and minoxidil mixed along with non-retinoid penetration enhancer and sunscreen | Inhibits 5.alpha.-reductase activity (block DHT) and increase blood flow on the scalp |
US20050123577
L'OREAL(2000) |
Peptides | Prostaglandin (polyunsaturated fatty acids) EP-2, EP-3 EP-4 receptor agonist with Minoxidil, 2,4-diaminopyrimidine 3-oxide, and Aminexil, cyclic AMP | Minoxidil (designed to mimic nitric oxide's effects) grows hair via prostaglandin-H synthase stimulation. EP-3 and EP-4 are expressed in anagen hair follicles which induce a reduction in the level of cAMP |
US6447762
COLOMER GROUP(1999) |
Natural extract | Hop extract (oil contains terpenes and humulene), Rosemary extract (hydroalcohol), Swertia extract (glycol with a swertiamarin), Silanodiol salicylate (biologically active silicon compound) | Inhibits activity of 5-alpha-reductase, protects follicular cell membranes by neutralizing action of oxidation reaction in tissues, stimulates hair follicles and blood circulation to the hair root, supplies oxygen and nutrients to base of follicle, retains humidity, avoids dehydration of scalp |
Hair matrix cell activator is a substance that acts at the matrix cells in the hair follicle preventing their degradation.
What causes hair loss?
How does hair cell matrix activator treat hair loss?
Pat/Pub# | Nature | Composition | Composition action |
---|---|---|---|
US20020052498
SHISEIDO(1999) |
Organic compound | (2-substituted oxyphenyl) alkanamide derivative and its salt | Mechanism of action has not been made clear, having excellent hair follicle activating action and regrowth promoting effect |
US20040071647
L'OREAL(1998) |
Peptides | Metalloprotease (MMP-9) inhibitor (thiol or a hydroxamate) other than chelating calcium ions | Reducing the expression of MMPs (Metalloproteases) in the scalp - slows down or inhibits the degradation of the perifollicular matrix (extracellular matrix surrounding the hair follicle) |
Year | Organic Compound | Natural extracts | Peptides | Nucleotides | Natural extract + Organic comp |
---|---|---|---|---|---|
2005 | .... | .... | .... | .... | UNILEVER (1) |
2004 | WARNER (1) | BLOTECH (1) | .... | .... | KAO (1) |
2003 | WARNER (1) | APHIOS (1) | .... | FUNDACION (1) | .... |
2002 | WARNER (1) | .... | .... | .... | .... |
2001 | PFIZER (1) | LG HEALTH-CARE (1) | .... | .... | .... |
2000 | .... | .... | L?OREAL (1) / N/A (1) | .... | .... |
1999 | SHISEDIO (1) | COLOMER (1) | .... | .... | .... |
1998 | .... | .... | L?OREAL (1) | .... | .... |
1995 | .... | .... | N/A (1) | .... | .... |
1987 | .... | KAO (1) | .... | .... | .... |
1982 | UNILEVER (1) | .... | .... | .... | .... |
Focus of patents | Patent no. | Rec. no. |
---|---|---|
2-substituted oxyphenyl alkanamide derivative having excellent hair growth effect. | US20020052498 | 1 |
Thyromimetic compounds, and its role in treating hair loss | US20030007941 | 2 |
Saw Palmetto berry extract, pumpkin seed extract, sitosterol and quercetin for the treatment and prevention of the biologically detrimental effects of DHT | US20060009430 | 3 |
4-cycloalkoxy benzonitriles and its use as androgen receptor modulators | US20060009427 | 4 |
Supercritical fluid isolate of Saw Palmetto, Sperol for inhibition of 5-.alpha.-reductase activity | US20050118282 | 5 |
New class of quinolin-2-ones and chromen-2-ones andtheir use as androgen receptor antagonists | US20050085467 | 6 |
Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders | US20060009429 | 7 |
Bradykinin antagonists for stimulating or inducing hair growth and/or arresting hair loss | US20030073616 | 8 |
Extract from walnut leaves and/or pericarps as 5 alpha -reductase inhibitor | EP0279010 | 9 |
Stimulating hair growth using benzopyrans | US20040157856 | 10 |
Sophora flavescens extract, Coicis semen extract, clove extract, etc for promoting hair growth, function of cell activity and dilating peripheral blood vessels. | US20050053572 | 11 |
Compositions to prevent or reduce hair loss | US20060052405 | 12 |
Prostaglandin EP-3 receptor antagonists for reducing hair loss | US20050123577 | 13 |
Synergic effect arising from the interaction of active ingredients, consisting of three plant extracts and a synthetic organosilicic compound for prevent hair loss and stimulate hair growth | US6447762 | 14 |
Metalloprotease inhibitors to induce and/or stimulate the growth | US20040071647 | 15 |
Method of decreasing sebum production and pore size | US20050277699 | 16 |
Method for reducing sebum on the hair and skin | US4529587 | 17 |
Target disease/ disorder | Patent no. | Rec. no. |
---|---|---|
Alopecia areata, alopecia pityrodes or alopecia seborrheica, or androgenic alopecia (i.e. male pattern baldness) | US20020052498 | 1 |
Alopecia areata, male pattern baldness and female pattern baldness | US20030007941 | 2 |
Androgenic alopecia (i.e. male pattern baldness), prostatic hyperplasia or both. | US20060009430 | 3 |
Inappropriate activation of the androgen receptor, acne, oily skin, alopecia | US20060009427 | 4 |
Prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity | US20050118282 | 5 |
Alopecia, acne, oily skin, prostrate cancer, hirsutism, and benign prostate hyperplasia | US20050085467 | 6 |
Androgen-associated hair loss and androgen-skin related disorders. | US20060009429 | 7 |
Androgenetic or androgenic alopecia or androgeno-genetic alopecia | US20030073616 | 8 |
Diseases caused by testosterone (male-pattern alopecia) | EP0279010 | 9 |
Alopecia areata, female pattern hair loss, hair loss secondary to chemotherapy or radiation treatment, stress-related hair loss, self-induced hair loss, scarring alopecia, and alopecia in non-human mammal | US20040157856 | 10 |
Male pattern alopecia | US20050053572 | 11 |
Alopecia, androgenic alopecia | US20060052405 | 12 |
Hair loss | US20050123577 | 13 |
Male pattern alopecia | US6447762 | 14 |
Androgenetic, androgenic or androgenogenetic alopecia | US20040071647 | 15 |
Curing other scalp related problems | US20050244362 | 16 |
Molecular mediators of hair follicle embryogenesis: Identification of the molecular pathways controlling differentiation and proliferation in mammalian hair follicles provides the crucial link to understanding the regulation of normal hair growth, the basis of hereditary hair loss diseases, and the origin of follicle-based tumors. Homeobox (hox), hedgehog (hh), patched (ptc), wingless (wg}/wnt, disheveled (dsh), engrailed (en), Notch 1 and armadillo/B-catenin genes are all critical for hair follicle.
Patent no. | Key compound | Players of inhibition |
---|---|---|
US6664247 | Pyrazole compounds | GSK3 |
US6989385 | Pyrazole compounds | GSK3 |
WO2005012256 | Pyrazole compounds | CDK,GSK3 |
US6974819 | Pyrimidine derivative | GSK3 |
US6743791 | Heterocyclic compounds | AKT3, GSK-3, ERK2 |
US20050277773 | Pyrrolo[3,2-d]pyrimidine derivatives | GSK3 |
US20040072836 | Aza-oxindole derivatives | GSK3, AKT, PKC |
EP1477489 | Pyrrolopyrimidine derivatives | GSK3 |
WO0056710 | 3-(Anilinomethylene) oxindoles | GSK3, AKT, PKC |
WO2003011287 | Pyrazolon derivatives | GSK3, ß-catenin |
US6924141 | Lithium chloride, Wnt3/4/ 7 | ß-catenin, GSK3, Wnt |
US6706685 | Peptide sequence | ß-catenin |
US6683048 | Peptide sequence | a-catenin, ß-catenin |
US6677116 | Peptide sequence LXXLL | ß-catenin |
US6303576 | Peptide sequence LXXLL | ß-catenin |
Pyrazole
US6989385 | US6664247 | WO2005012256 |
---|---|---|
R1=T-Ring D, wherein
T is a valence bond and Ring D = 5-6 membered aryl or heteroaryl ring; R2 = hydrogen or C1-4 aliphatic and R2'= hydrogen; R3 = -R, -OR, or -N(R4)2, wherein R = hydrogen, C1-6 aliphatic, 5-6 membered heterocyclyl, phenyl, or 5-6 membered heteroaryl, and L is -O-, -S-, or -NH-; and Ring D is substituted by up to three substituents selected from -halo, -CN, -NO2, -N(R4)2, optionally substituted C1-6 aliphatic group, -OR, -C(O)R, -CO2R, -CONH(R<4>), -N(R4)COR, -N(R4)CO2R, -SO2N(R4)2, -N(R4)SO2R, -N(R6)COCH2N(R4)2, -N(R6)COCH2CH2N(R4)2, or -N(R6)COCH2CH2CH2N(R4)2, wherein R = hydrogen, C1-6 aliphatic, phenyl, 5-6 membered heteroaryl ring, or 5-6 membered heterocyclic ring |
X = R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length;
R1 is hydrogen; carbocyclic or heterocyclic group having from 3 to 12 ring members; or C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S02; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy). |
X is a groupR1-A-NR4-or a 5-or 6-membered carbocyclic or heterocyclic ring;
A is a bond,SO2, C=O, NRg (C=O) or O(C=O) wherein Rg is hydrogen orC14 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy;Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length;R'is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e. g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono-ordi-Cl 4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected fromO, S, NH, SO, SO2 ;R2 is hydrogen; halogen;C14 alkoxy (e. g. methoxy); or aC14 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl orC14 alkoxy (e. g. methoxy);R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; andR4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e. g. fluorine), hydroxyl or C1-4 alkoxy (e. g. methoxy). |
Patent Number: US6989385 Applicant: Vertex Pharmaceuticals Incorporated Title: Pyrazole compounds useful as protein kinase inhibitors
Basic Structure:
Derivatives of pyrimidine-pyrazole amine disclosed in US6989385 patent
Patent Number: US7008948 Applicant: Vertex Pharmaceuticals Incorporated Title: Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors
Basic Structure
Derivatives of pyrimidine-pyrazole amine disclosed in US7008948 patent
Patent Number: US6977262 Assignee: Mitsubishi Pharma Corporation Title: Dihydropyrazolopyridine compounds and pharmaceutical use thereof
Basic Structure:
Derivatives of pyrimidine-pyrazole amine disclosed in US6977262 patent
Patent Number: US6664247 Assignee: Vertex Pharmaceuticals Incorporated Title: Pyrazole compounds useful as protein kinase inhibitors
Basic Structure:
Derivatives of pyrimidine-pyrazole amine disclosed in US6664247 patent
Patent Number: US2004224944 Assignee: VERTEX PHARMACEUTICALS INC Title: Pyrazole compounds useful as protein kinase inhibitors
Basic Structure:
Derivatives of pyrimidine-pyrazole amine disclosed in US2004224944 patent
Key points
GK3 Inhibition:
Serine - pyrazole reaction
Proposed mechanisms to regulate GSK-3 source
Key Finding
Minoxidil is a well know drug used for the treatment of alopecia. A co-relation between Sesquiterpene lactone (Helenalin) produced from Arnica montana and Minoxidil is illustrated in the figure below. Arnica montana, a Vasodilator, acts on the NO/cGMP Pathway through T-cells, B-cells and epithelial cells & abrogates kappa B-driven gene expression.
Treatment approach | Patent number | Priority year | Assignee/Inventor |
Vasodilators | CN1772105 | 2005 | ??? |
CN1772139 | 2005 | ??? | |
CN1569080 | 2003 | ??? | |
CN1506103 | 2002 | ??? | |
CN1403100 | 2001 | ??? | |
CN1165181 | 1996 | ??? | |
CN1031022 | 1988 | ??????????? | |
Hair matrix activator | CN1463693 | 2002 | ??? |
Anti-androgen + Vasodilator | CN1150043 | 1996 | ??? |
Patent number | Patent title | Treatment approach | Composition nature | Composition | Composition action |
CN1772105 YE MINGWEI (CN) ??? (2005) |
Chinese herbal medicine decoction for treating blood stasis obstruction type alopecia and its prepn ???????????????????? |
Vasodilators | Herbal extract | Astragalus root, prepared rhizome of rehmannia, white peony root, angelica, peach kernel and sufflower | Promote blood circulation |
CN1772139 WANG YAJIE (CN) ??? 2005 |
Alopecia areata treating medicine ????????? |
Vasodilators | Herbal extract | Pinellia tuber, fleeceflower root, arborvitae seed, chickení s gizzard membrane, prepared rhizome of rehmannia, Poris cocos, Codonopsis pilosula, etc | Promote blood circulation |
CN1569080 TAN RUBIAO (CN) ??? 2003 |
Natural Chinese herb composition for treating alopecia and leucotrichia and its application ?????????????????????????? |
Vasodilators | Herbal extract | Ginger, Cinnamomum cassia, myrrh, clove, mace nutmeg, Loranthus mulberry mistletoe, rhizoma dioscoreae, ligustrum japonicum, drynaria, fleece-flower root, and black sesame seeds | Enhances the hair growth and healthier hairs |
CN1463693 ??? 2002 |
Hair growing preparation containing compound of Chinese medicine and Western medicine ???????????? |
Hair matrix activator | Mixture of Herbal extracts and western medicine | Persimmon leaf, oriental arbor-vitae leaf, ginseng leaf, yellow qi, fruit of the glossy privet, polygonum multiflorum, Kudzu root, dry ginger; Plus?Minoxidil, Vitamins and derivative, cystine, serine, leucine. | Better and faster hair growth |
CN1506103 ???2002 |
Hair follice activating liquid ????? |
Vasodilators | Herbal extract | Ginseng, twists the stock blue, the licorice, the Sophora flavescens and hot peppers | Activates the hair-follicle and enhances the hair growth. |
CN1403100 ??? 2001 |
Trichogen and its prepn ?????????????? |
Vasodilators | Herbal extract | Ginseng, ganoderma lucidum, Chinese rhubarb, polygonum multiflorum, Chinese prickly ash, ginger, grass seed | Promote blood circulation and enhance hair growth |
CN1165181 ??? 1996 |
Washing free shampoo for nourishing and growing hair ???????? |
Vasodilator | Vitamin composition | Vitamin P (Bioflavonoids), Vitamin B15, Vitamin B2, nicotinic acid, bromo?geramineum | Stimulate hair growth |
CN1150043 ??? 1996 |
Efficient low-side effect external use medicine for curing seborrheic baldness ???????????????????? |
Anti-androgen + Vasodilator | Mixture of Herbal extracts and organic compounds | Polygonum multiflorum, Ligustrum lucidum, Morus alba, Rehmannia glutinosa, Eclipta prostrata, Saliva miltiorrhiza, Carthamus tinctorius, Cnidium monnieri, Sophora flavescens, Dictamnus dasycarpus, Kochia scoparia, and antioxidants | Inhibit the excess secretion of the sebaceous glands, increase the blood circulation on scalp and enhance the hair growth |
CN1031022 ??????????? 1988 |
Channel-stimulating and hair-growing hair shampoo ???????? |
Vasodilators | Herbal extract + detergent | Herbal extracts, Penetration media, Detergents. | Increases the blood circulation under the scalp, reduces the hair los |
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