Changes

Alopecia - Hair Loss

17,372 bytes added, 10:56, 16 July 2007

/* Minoxidil (Vasodilators) */

* Minoxidil is thought to have a direct mitogenic effect on epidermal cells, as has been observed both in vitro and in vivo. Though the mechanism of its action for causing cell proliferation is not very clear, minoxidil is thought to prevent intracellular calcium entry. Calcium normally enhances epidermal growth factors to inhibit hair growth, and Minoxidil by getting converted to minoxidil sulfate acts as a potassium channel agonist and enhances potassium ion permeability to prevent calcium ions from entering into cells. ([http://www.hairtransplantadvice.com/medical-hair-restoration.php Source])

* Minoxidil sulfate (MS) appears to be the active metabolite responsible for hair growth stimulation.

==== Functions of Vasodilators ====

[[Image:minoxidil1.jpg|thumb|center|500px|Functions of Monoxidil [http://www.nurseminerva.co.uk/diagrams.htm#Diagram%201 source]]]

==== IP Map for Vasodilators ====

{| border="1" cellpadding="2"

!width="120" bgcolor=DodgerBlue|'''Pat/Pub#'''

!width="75" bgcolor=DodgerBlue|'''Nature'''

!width="600" bgcolor=DodgerBlue|'''Composition'''

!width="300" bgcolor=DodgerBlue|'''Composition action'''

|- style="height:100px"

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220040157856%22.PGNR.&OS=DN/20040157856&RS=DN/20040157856 US20040157856]

WARNER LAMBERT(2002)

|bgcolor=LightCyan|Organic compound

|bgcolor=LightCyan|Benzopyran compounds

|bgcolor=LightCyan|Rapidly metabolizes, and causes reduced cardiovascular effects as compared to other known potassium channel openers

|- style="height:100px"

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220050053572%22.PGNR.&OS=DN/20050053572&RS=DN/20050053572 US20050053572]

LG HOUSEHOLD & HEALTH CARE(2001)

|bgcolor=LightCyan|Natural extracts

|bgcolor=LightCyan|Sophora flavescens extract (alkaloids & flavonoids, luteolin-7-glucose and cytosine) Hinokitiol (Taiwan hinoki oil, Aomori, Western Red Cedar oil) and Nicotinamide (Vitamin B complex)

|bgcolor=LightCyan|Promotes function of cell activity and dilates blood vessels

|}

=== Double action (Anti-androgen + Vasodilator) ===

* Combination of Vasodilator + Anti-androgen (double action) composition for effective treatment of Male-Pattern Baldness.

'''What is the problem with using only Anti-androgen therapy?'''

* Anti-androgen is not effective in addressing the issue of vasocontriction around hair follicles due to sebum oil build up.

* Anti-androgen only prevents binding of DHT to androgen receptors. However, the effects of improper oxygen and nutrient supply to the brain due to vasocontriction still remains and gradually causes hair loss.

'''What is the problem with using only Vasodilator (or Minoxidil only) therapy?'''

* Vasodilator or Minoxidil-based products are generally not effective in stopping hair loss as vasodilators (or Minoxidil) do not block the harmful effects of DHT in the scalp and hair follicles.

* Vasodilators or Minoxidil simply dilate blood vessels in the scalp. However, the harmful DHT still gets produced in the body, enters the scalp and hair follicles causing hair loss.

'''How is the combination of Anti-androgens and Vasodilator (or Minoxidil) effective?'''

* Anti-androgens target the problem of DHT binding to androgen receptors and prevents follicle miniaturization.

* Vasodilators like Minoxidil cause vasodilation and therefore improve supply of oxygen and nutrients to the hair follicle and roots.

* Combination therapy therefore proves to be much more effective than individual therapy.

==== Functions of (Anti-androgen + Vasodilators) ====

[http://www.revivogen.com/revivogen/work.html Anti-androgen ]and [http://www.xandrox.net/articles/article01.htm Minoxidil]

[[Image:Doubleaction1.jpg|thumb|center|500px|Functions of (Anti-androgen + Vasodilators)]]

==== IP Map for (Anti-androgen + Vasodilators) ====

{| border="1" cellpadding="3"

!width="120" bgcolor=DodgerBlue|'''Pat/Pub#'''

!width="75" bgcolor=DodgerBlue|'''Nature'''

!width="500" bgcolor=DodgerBlue|'''Composition'''

!width="500" bgcolor=DodgerBlue|'''Composition action'''

|- style="height:100px"

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220060052405%22.PGNR.&OS=DN/20060052405&RS=DN/20060052405 US20060052405]

N/A(2000)

|bgcolor=LightCyan|Peptides

|bgcolor=LightCyan|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

|bgcolor=LightCyan|Inhibits 5.alpha.-reductase activity (block DHT) and increase blood flow on the scalp

|- style="height:100px"

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220050123577%22.PGNR.&OS=DN/20050123577&RS=DN/20050123577 US20050123577]

L'OREAL(2000)

|bgcolor=LightCyan|Peptides

|bgcolor=LightCyan|Prostaglandin (polyunsaturated fatty acids) EP-2, EP-3 EP-4 receptor agonist with Minoxidil, 2,4-diaminopyrimidine 3-oxide, and Aminexil, cyclic AMP

|bgcolor=LightCyan|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

|- style="height:100px"

|bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=6447762.PN.&OS=PN/6447762&RS=PN/6447762 US6447762]

COLOMER GROUP(1999)

|bgcolor=LightCyan|Natural extract

|bgcolor=LightCyan|Hop extract (oil contains terpenes and humulene), Rosemary extract (hydroalcohol), Swertia extract (glycol with a swertiamarin), Silanodiol salicylate (biologically active silicon compound)

|bgcolor=LightCyan|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 ===

Hair matrix cell activator is a substance that acts at the matrix cells in the hair follicle preventing their degradation.

'''What causes hair loss?'''

* Stem cells are interspersed within the basal layer of the outer root sheath and in an area called the bulge.

* Stem cells migrate to hair matrix where they start to divide and differentiate, under the influence of substances produced by cells of the dermal papilla.

* Perifollicular matrix cells undergo slow degradation which prevents follicle stimulation.

* Hair follicle activation is required for hair growth and thus inhibition of follicle activation eventually leads to hair loss.

'''How does hair cell matrix activator treat hair loss?'''

* Hair cell matrix activator slows down and inhibits degradation of the perifollicular matrix.

* This leads to an increase in hair follicle matrix cells that differentiate from progenitor stem cells.

* Matrix activator allows activation of hair matrix cells and therefore follicle stimulation leading to hair growth.

==== Functions of Hair matrix cell activator ====

[http://www.ijdb.ehu.es/fullaccess/fulltext.04023/ft163.pdf Hair matrix cell activator]

[[Image:Hair matrix.jpg|thumb|center|500px|Functions of Hair matrix cell activator ]]

==== IP Map for Hair matrix cell activator ====

{| border="1" cellpadding="2"

!width="120" bgcolor=DodgerBlue|'''Pat/Pub#'''

!width="100" bgcolor=DodgerBlue|'''Nature'''

!width="200" bgcolor=DodgerBlue|'''Composition'''

!width="600" bgcolor=DodgerBlue|'''Composition action'''

|- style="height:50px"

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220020052498%22.PGNR.&OS=DN/20020052498&RS=DN/20020052498 US20020052498]

SHISEIDO(1999)

|bgcolor=LightCyan|Organic compound

|bgcolor=LightCyan|(2-substituted oxyphenyl) alkanamide derivative and its salt

|bgcolor=LightCyan|Mechanism of action has not been made clear, having excellent hair follicle activating action and regrowth promoting effect

|- style="height:50px"

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220040071647%22.PGNR.&OS=DN/20040071647&RS=DN/20040071647 US20040071647]

L'OREAL(1998)

|bgcolor=LightCyan|Peptides

|bgcolor=LightCyan|Metalloprotease (MMP-9) inhibitor (thiol or a hydroxamate) other than chelating calcium ions

|bgcolor=LightCyan|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)

|}

== Technology mapping based on patents analyzed ==

=== IPMap: Composition nature matrix ===

{| border="1" cellpadding="11", style="#008080"

!width="120" bgcolor=DodgerBlue|'''Year'''

!width="200" bgcolor=DodgerBlue|'''Organic Compound'''

!width="200" bgcolor=DodgerBlue|'''Natural extracts'''

!width="200" bgcolor=DodgerBlue|'''Peptides'''

!width="200" bgcolor=DodgerBlue|'''Nucleotides'''

!width="200" bgcolor=DodgerBlue|'''Natural extract + Organic comp'''

|- style="height:10px"

|bgcolor=LightCyan|2005

|bgcolor=LightCyan|....

|bgcolor=LightCyan|UNILEVER (1)

|-

|bgcolor=LightCyan|2004

|bgcolor=LightCyan|WARNER (1)

|bgcolor=LightCyan|BLOTECH (1)

|bgcolor=LightCyan|....

|bgcolor=LightCyan|KAO (1)

|-

|bgcolor=LightCyan|2003

|bgcolor=LightCyan|WARNER (1)

|bgcolor=LightCyan|APHIOS (1)

|bgcolor=LightCyan|....

|bgcolor=LightCyan|FUNDACION (1)

|bgcolor=LightCyan|....

|-

|bgcolor=LightCyan|2002

|bgcolor=LightCyan|WARNER (1)

|bgcolor=LightCyan|....

|-

|bgcolor=LightCyan|2001

|bgcolor=LightCyan |PFIZER (1)

|bgcolor=LightCyan|LG HEALTH-CARE (1)

|bgcolor=LightCyan|....

|-

|bgcolor=LightCyan|2000

|bgcolor=LightCyan|....

|bgcolor=LightCyan|L’OREAL (1) / N/A (1)

|bgcolor=LightCyan|....

|-

|bgcolor=LightCyan|1999

|bgcolor=LightCyan|SHISEDIO (1)

|bgcolor=LightCyan|COLOMER (1)

|bgcolor=LightCyan|....

|-

|bgcolor=LightCyan|1998

|bgcolor=LightCyan|....

|bgcolor=LightCyan|L’OREAL (1)

|bgcolor=LightCyan|....

|-

|bgcolor=LightCyan|1995

|bgcolor=LightCyan|....

|bgcolor=LightCyan|N/A (1)

|bgcolor=LightCyan|....

|-

|bgcolor=LightCyan|1987

|bgcolor=LightCyan|....

|bgcolor=LightCyan|KAO (1)

|bgcolor=LightCyan|....

|-

|bgcolor=LightCyan|1982

|bgcolor=LightCyan|UNILEVER (1)

|bgcolor=LightCyan|....

|}

=== Focus of patents ===

{| border="1" cellpadding="17", style="#008080"

!width="800" bgcolor=DodgerBlue|'''Focus of patents'''

!width="150" bgcolor=DodgerBlue|'''Patent no.'''

!width="100" bgcolor=DodgerBlue|'''Rec. no.'''

|-

|bgcolor=LightCyan|2-substituted oxyphenyl alkanamide derivative having excellent hair growth effect.

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220020052498%22.PGNR.&OS=DN/20020052498&RS=DN/20020052498 US20020052498]

|bgcolor=LightCyan|1

|-

|bgcolor=LightCyan|Thyromimetic compounds, and its role in treating hair loss

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220030007941%22.PGNR.&OS=DN/20030007941&RS=DN/20030007941 US20030007941]

|bgcolor=LightCyan|2

|-

|bgcolor=LightCyan|Saw Palmetto berry extract, pumpkin seed extract, sitosterol and quercetin for the treatment and prevention of the biologically detrimental effects of DHT

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220060009430%22.PGNR.&OS=DN/20060009430&RS=DN/20060009430 US20060009430]

|bgcolor=LightCyan|3

|-

|bgcolor=LightCyan|4-cycloalkoxy benzonitriles and its use as androgen receptor modulators

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220060009427%22.PGNR.&OS=DN/20060009427&RS=DN/20060009427 US20060009427]

|bgcolor=LightCyan|4

|-

|bgcolor=LightCyan|Supercritical fluid isolate of Saw Palmetto, Sperol for inhibition of 5-.alpha.-reductase activity

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220050118282%22.PGNR.&OS=DN/20050118282&RS=DN/20050118282 US20050118282]

|bgcolor=LightCyan|5

|-

|bgcolor=LightCyan|New class of quinolin-2-ones and chromen-2-ones andtheir use as androgen receptor antagonists

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220050085467%22.PGNR.&OS=DN/20050085467&RS=DN/20050085467 US20050085467]

|bgcolor=LightCyan|6

|-

|bgcolor=LightCyan|Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220060009429%22.PGNR.&OS=DN/20060009429&RS=DN/20060009429 US20060009429]

|bgcolor=LightCyan|7

|-

|bgcolor=LightCyan|Bradykinin antagonists for stimulating or inducing hair growth and/or arresting hair loss

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220030073616%22.PGNR.&OS=DN/20030073616&RS=DN/20030073616 US20030073616]

|bgcolor=LightCyan|8

|-

|bgcolor=LightCyan|Extract from walnut leaves and/or pericarps as 5 alpha -reductase inhibitor

|bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&IDX=EP0279010&F=0 EP0279010]

|bgcolor=LightCyan|9

|-

|bgcolor=LightCyan|Stimulating hair growth using benzopyrans

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220040157856%22.PGNR.&OS=DN/20040157856&RS=DN/20040157856 US20040157856]

|bgcolor=LightCyan|10

|-

|bgcolor=LightCyan|Sophora flavescens extract, Coicis semen extract, clove extract, etc for promoting hair growth, function of cell activity and dilating peripheral blood vessels.

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220050053572%22.PGNR.&OS=DN/20050053572&RS=DN/20050053572 US20050053572]

|bgcolor=LightCyan|11

|-

|bgcolor=LightCyan|Compositions to prevent or reduce hair loss

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220060052405%22.PGNR.&OS=DN/20060052405&RS=DN/20060052405 US20060052405]

|bgcolor=LightCyan|12

|-

|bgcolor=LightCyan|Prostaglandin EP-3 receptor antagonists for reducing hair loss

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220050123577%22.PGNR.&OS=DN/20050123577&RS=DN/20050123577 US20050123577]

|bgcolor=LightCyan|13

|-

|bgcolor=LightCyan|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

|bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=6447762.PN.&OS=PN/6447762&RS=PN/6447762 US6447762]

|bgcolor=LightCyan|14

|-

|bgcolor=LightCyan|Metalloprotease inhibitors to induce and/or stimulate the growth

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220040071647%22.PGNR.&OS=DN/20040071647&RS=DN/20040071647 US20040071647]

|bgcolor=LightCyan|15

|-

|bgcolor=LightCyan|Method of decreasing sebum production and pore size

|bgcolor=LightCyan|[http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.html&r=1&f=G&l=50&s1=%2220050277699%22.PGNR.&OS=DN/20050277699&RS=DN/20050277699 US20050277699 ]

|bgcolor=LightCyan|16

|-

|bgcolor=LightCyan|Method for reducing sebum on the hair and skin

|bgcolor=LightCyan|[http://patft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=4529587.PN.&OS=PN/4529587&RS=PN/4529587 US4529587]

|bgcolor=LightCyan|17

|}

=== Technology focus===

[[Image:Technologyfocus2.jpg|thumb|center|700px|Technology focus]]

=== Distribution of patents ===

==== By patent types ====

[[Image:Didtribution.jpg|thumb|center|700px|Distribution based on patent types ]]

==== By key ingredients ====

[[Image:key1.jpg|thumb|center|700px|Distribution of key ingredients]]

==== By target disease ====

[[Image:target.jpg|thumb|center|700px|Distribution based on target diseases]]

==== Key ingredients vs. Target disease ====

[[Image:key&target1.jpg|thumb|center|1000px|Key ingredients vs. Target disease]]

==== Target species ====

[[Image:Species.jpg|thumb|center|700px|Target species]]

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Changes

Alopecia - Hair Loss

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