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Alopecia - Hair Loss

2,754 bytes added, 11:04, 4 December 2014
/* Structure-Activity Relationships(SARs) */
{{TOCrightEx}}
== Rationale ==
* "Medication for men plagued by hair loss has become a topic of interest in Japan since a drug company began marketing it at the end of last year." March 5th, 2006 – [http://stophair.setupmyblog.com/?p=55 sourceSource] * "An increasing number of companies are apparently turning the Chinese fear of a bald spot into big bucks with some doing so well they are branching out into other countries." February 16, 2006 – [http://stophair.setupmyblog.com/Source] * "There is something in the air, or should we say in the hair, these days. Scientific research into hair loss remedies has never been more active or more exciting." June 7, 2006 - [http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=109&STORY=/www/story/06-07-2005/0003821470&EDATE=Source]<br><br> == Alopecia IPMap == [http://www.dolcera.com/client/d8r3/hairloss_map.htm Dolcera IPMap for Alopecia]<br>
== Introduction ==
* Hair is made up of a protein called keratin.
* Each shaft of hair is made of two or three inter-twined layers of keratin which grow from a follicle beneath the skin.
* Hair Structure - [http://www.pg.com/science/haircare/hair_twh_12.htmSource]* Hair Cycle - [http://www.follicle.com/hair-structure-life-cycle.htmlSource]
[[Image:Hairbasics.jpg|center|400px|Structure of Hair root and Hair bulb]]
[[Image:Facts.jpg|thumb|right|250px|Survey results from Japan]]
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".
 
=== Types of alopecia===
== Major players ==
[[Image:players.jpg|thumb|left|400px500px|Assignees with more than 20 patents ]][[Image:players1.jpg|thumb|center|400px500px|Assignees with fewer than 20 patents ]]<br>
* '''Active assignees'''
[[Image:Active.jpg|thumb|center|500px|Active Assignees]]
== Taxonomy ==
 
[[Image:Alopecia toxonomy.jpg|thumb|center|800px]]
 
== Interactive Taxonomy ==
''Use the mouse(click and drag/scroll up or down/click on nodes) to explore nodes in the detailed taxonomy'' <br>
''Click on the red arrow on the side of a node name to view the content for that particular node in the dashboard''
<mm>[[Map12.mm]]</mm>
== Treatment Approaches==
!width="400" bgcolor=DodgerBlue|'''Composition action'''
|- style="height:20px"
|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]]
BLOTECH (2004)
|bgcolor=LightCyan|Natural extracts
|bgcolor=LightCyan|....
|}
 
=== Focus of patents ===
=== Technology focus===
[[Image:Technologyfocus2.jpg|thumb|center|700px|Technology focus]]
 
=== Distribution of patents ===
==== Target species ====
[[Image:Species.jpg|thumb|center|700px|Target species]]
 
|}
==== Patents by application ====
[[Image:application.jpg|thumb|center|700px|Distribution of patents based on application]]
==== [[List of patents]] ====
==== [[List of patents]] ====
== Pathways and linkages ==
=== Pathways associated with Anti Androgen===
[[Image:Slide1Slide3.GIF|thumbgif|center|700 720 px|Alopecia pathways]]
==== Players of Wnt WNT inhibition Pathway ====
[[Image:wnt.jpg|thumb|right|200 px|Wnt inhibition]]
{| border="1" cellpadding="15", style="#008080"
|bgcolor=LightCyan|[http://v3.espacenet.com/textdoc?DB=EPODOC&IDX=WO03011287&F=0 WO2003011287]
|bgcolor=LightCyan|Pyrazolon derivatives
|bgcolor=LightCyan|GSK3, βß-catenin
|-
|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=6924141.PN.&OS=PN/6924141&RS=PN/6924141 US6924141]
|bgcolor=LightCyan|Lithium chloride, Wnt3/4/ 7
|bgcolor=LightCyan|βß-catenin, GSK3, Wnt
|-
|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=6706685.PN.&OS=PN/6706685&RS=PN/6706685 US6706685]
|bgcolor=LightCyan|Peptide sequence
|bgcolor=LightCyan|βß-catenin
|-
|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=6683048.PN.&OS=PN/6683048&RS=PN/6683048 US6683048]
|bgcolor=LightCyan|Peptide sequence
|bgcolor=LightCyan|αa-catenin, βß-catenin
|-
|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=6677116.PN.&OS=PN/6677116&RS=PN/6677116 US6677116]
|bgcolor=LightCyan|Peptide sequence LXXLL
|bgcolor=LightCyan|βß-catenin
|-
|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=6303576.PN.&OS=PN/6303576&RS=PN/6303576 US6303576]
|bgcolor=LightCyan|Peptide sequence LXXLL
|bgcolor=LightCyan|βß-catenin
|}
'''Pyrazole'''
* '''Pyrazole''' (C3H4N2) refers both to the class of simple aromatic ring organic compounds of the heterocyclic series characterized by a 5-membered ring structure composed of three carbon atoms and two nitrogen atoms in adjacent positions and to the unsubstituted parent compound. Being so composed and having pharmacological effects on humans, they are classified as alkaloids although they are not known to occur in nature.
* Pyrazoles are produced synthetically through the reaction of αa,βß-unsaturated aldehydes with hydrazine and subsequent dehydrogenation
[[Image:pyrazole1.jpg|thumb|center|500px|Pyrazole (C3H4N2)]]
* Pyrazoles are used for their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxing, psychoanaleptic, anticonvulsant, monoamineoxidase inhibiting, antidiabetic and antibacterial activities.
** Binds to androgen receptor on susceptible hair follicles
* Hormone-receptor complex activates genes responsible for gradual transformation of large terminal follicles to miniaturized (progressive diminution of hair shaft diameter and length in response to systemic androgens) follicles
 
[[Image:5-alpha-reductase inhibition.jpeg|center|500 px]]
==== Structure-Activity Relationships(SARs) ====
[[Image:SAR_map.gif|center|600px720px]]
=== Pathway associated with Minoxidil (vasodilators) ===
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.
[[image:vasodiator-rev.jpg|800 px|center]]
 
== Alopecia IPMap ==
[http://www.dolcera.com/client/d8r3/hairloss_map.htm Dolcera IPMap for Alopecia]
 
 
 
 
== Patent activity in China ==
===Treatment approaches===
{|border="2" cellspacing="0" cellpadding="4" width="100%"
|align = "center"|'''Treatment approach'''
|align = "center"|'''Patent number'''
|align = "center"|'''Priority year'''
|align = "center"|'''Assignee/Inventor'''
|-
|rowspan = "7"|Vasodilators
|[http://search.sipo.gov.cn/sipo/zljs/hyjs-yx-new.jsp?recid=CN200510107497.8&leixin=fmzl&title=治疗瘀血阻滞型脱发的中草药汤剂及制备方法&ipc=A61K36/804(2006.01)I CN1772105]
|2005
|叶明伟
|-
|[http://v3.espacenet.com/textdoc?DB=EPODOC&IDX=CN1772139&F=0 CN1772139]
|2005
|王亚杰
|-
|[http://search.sipo.gov.cn/sipo/zljs/hyjs-yx-new.jsp?recid=CN03139861.8&leixin=fmzl&title=一种可用于治疗脱发、白发的天然中草药提取组合物及应用&ipc=A61K35/78 CN1569080]
|2003
|谈汝标
|-
|[http://search.sipo.gov.cn/sipo/zljs/hyjs-yx-new.jsp?recid=CN02155404.8&leixin=fmzl&title=毛囊激活液&ipc=A61K35/78 CN1506103]
|2002
|赵章光
|-
|[http://search.sipo.gov.cn/sipo/zljs/hyjs-yx-new.jsp?recid=CN01127395.X&leixin=fmzl&title=一种止脱生发药物及其制备方法&ipc=A61K35/78 CN1403100]
|2001
|范希田
|-
|[http://search.sipo.gov.cn/sipo/zljs/hyjs-yx-new.jsp?recid=CN96116925.7&leixin=fmzl&title=免洗养发生发香波&ipc=C11D3/48 CN1165181]
|1996
|殷国健
|-
|[http://search.sipo.gov.cn/sipo/zljs/hyjs-yx-new.jsp?recid=CN88103853.9&leixin=fmzl&title=一种通络生发香波&ipc=A61K7/06 CN1031022]
|1988
|天津市轻工业化学研究所
|-
|Hair matrix activator
|[http://search.sipo.gov.cn/sipo/zljs/hyjs-yx-new.jsp?recid=CN02111941.4&leixin=fmzl&title=一种含中西药复方的育发剂&ipc=A61K7/06 CN1463693]
|2002
|朱静建
|-
|Anti-androgen <nowiki>+</nowiki> Vasodilator
|[http://search.sipo.gov.cn/sipo/zljs/hyjs-yx-new.jsp?recid=CN96109964.X&leixin=fmzl&title=一种治疗脂溢性脱发的高效低副作用外用药物&ipc=A61K35/78 CN1150043]
|1996
|梅晓春
|-
|}
 
=== Details of treatment approaches===
{|border="2" cellspacing="0" cellpadding="4" width="100%" align="left"
|-
|}<br clear="all">
 
 
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<br>
== Conclusions ==
* The top companies are Merck, L’Oreal and Smithkline.
== Questions Contact Dolcera Answers ==
'''What’s hot?'''{| style="border:1px solid #AAA; background:#E9E9E9" align="center"* What compositions/ approaches are the most promising?|-* What can I license?* Can you map blockbuster products to their patents?! style="background:lightgrey" | Contact Dolcera|-| '''Can you save me some time?Email''': [mailto:info@dolcera.com info@dolcera.com]* What combinations/ compounds have already been tried?* Is any empirical data available?* Can you tell me the side effects? '''Where should I focus my R&D investment?'''* What are the most promising approaches?* Where’s the ‘white space’ for me to play in? '''Any hints for research?'''* Are there any combinations I could develop? '''What should I do in this geography?'''* What are my competitors up to in this geography?* What are my strengths/ weaknesses here? '''What’s my competition up to?''' * What’s my top competitor investing in?* Are there any loopholes in their patents?* When are their patents expiring?* Will a competitor emerge from nowhere and surprise me?* What are the crowded areas?|-| '''How do I play defense?Phone''': +1-650-269-7952* What should my blocking/reactive strategies be?|}
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