CGRP antagonists - Why is this one website so far ahead of everyone else?

[Guest guest]

I did a little research on CGRP antagonists on the web. I didnt find a whole

lot, but I found this website at the U.S. patent office or something.

http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=/\

netahtml/srchnum.htm&r=1&f=G&l=50&s1='5932215'.WKU.&OS=PN/5932215&RS=PN/5932215

Not sure if the link will work. Anyway, it talks about CGRP has been shown in

studies to be effective for treating cea and erythema for many of the

reasons that have already been discussed on here. It talks about how cea

has no cure, and how products like Metronidazole, antibiotics, etc, are

primarily ineffective at treating certain aspects of cea because they dont

go after the cause of the disorder. This patent talks about a topical

CGRP-blocker, possibly mixed with a substance-P blocker, or antiinflammatory

substances, or even with antibiotics. It seems like something that was actually

put together like this would blow every other cea treatment currently

available right out of the water. At the end they give seven examples of how to

make a succesful CGRP-blocking topical:

" EXAMPLE 1

Face cream (oil-in-water emulsion):

______________________________________

CGRP 8-37 0.5%

Glyceryl stearate 2%

Polysorbate 60 (Tween 60

1%

marketed by ICI)

Stearic acid 1.4%

Triethanolamine 0.7%

Carbomer 0.4%

Cyclomethicone 8%

Sunflower Oil 12%

Antioxidant 0.05%

Preservative 0.3%

Water qs 100%

EXAMPLE 5 Cream (oil-in-water emulsion):

______________________________________

Glyceryl stearate 2%

CGRP 8-37 0.02%

Polysorbate 60 (Tween 60

1%

marketed by ICI)

Stearic acid 1.4%

Metronidazole 0.5%

Triethanolamine 0.7%

Carbomer 0.4%

Cyclomethicone 8%

Sunflower oil 10%

Antioxidant 0.05%

Preservative 0.3%

Water qs 100%The website made it sound like the technology

already exists to make this happen, so my question is, why hasnt it happened

yet?Adam

[Guest guest]

Hi,

L'Oreal holds patents on CGRP antagonists as well as many others

(substance P antagonists, TNF-alpha antagonists, etc) for rosacea.

They also hold patents related to strontium nitrate and rosacea /

sensitive skin (as does Dr. Hahn of Cosmederm).

One person in particular, Dr. OLIVIER DE LACHARRIERE has filed many

patents directly applicable to rosacea for L'Oreal and others. Most

recently he has filed the following patent for NO synthase

inhibitors and rosacea (see link below).

http://appft1.uspto.gov/netacgi/nph-Parser?

Sect1=PTO2&Sect2=HITOFF&p=1&u=/netahtml/PTO/search-

bool.html&r=8&f=G&l=50&co1=AND&d=PG01&s1=rosacea&OS=rosacea&RS=rosace

a

As anyone who has worked with patent law will attest, it is a vast

and complex area. The fact that many of these patents will state

that " complete clearance " of redness has been achieved one must

treat with some caution; many times a company will simply take out

extremely similar patents on a host of similar technologies. In

L'Oreal's case they have patents across a wide range of antagonists

that block actions of mediators in the facial skin... This is how

patent law works; an initial " invention " is made applicable to the

widest possible means of use or relative uses. Will this stop us

being able to have NO inhibitors or CGRP antagonists made up for us

as part of a trial with a research doctor? The answer is almost

certainly not. Patents are often kept as a form of " insurance " (if

one company claims patent infringement on another, there is

invariably a counter-claim) and are indeed not guaranteed to

be " valid " unless they have been tested in a court of law. In other

words, companies hedge their bets by patenting " inventions " which

*MAY* work... rather than ones which they have finalised or tested

to perfection. From what I understand talking to researchers, CGRP

(8-37) as mentioned in the patent below, is NOT a good drug to apply

topically. But the patent has been written as patents always are

and claims coverage of any CGRP antagonists applied to rosacea (i.e.

current or future).

There is no doubt in my mind however that a *combined* CGRP and NO

inhibitor would be extremely beneficial for rosacea sufferers.

Medical studies already exist that show combined NO inhibitors and

CGRP antagonists have a cumulative effect on *decreasing* blood

flow. Here is the relevant study (note that the drugs were injected

cutaneously rather than applied topically):

" Calcitonin gene-related peptide, substance P and nitric oxide are

involved in cutaneous inflammation following ultraviolet

irradiation. "

Key finding:

" The inhibitor of NO synthase NG-nitro-L-arginine methyl ester

hydrochloride (L-NAME, 25 nmol in 25 microliters, s.c.) attenuated

skin blood flow by 38%. Concurrent injections s.c. of CGRP-(8-37)

(1.5 nmol in 12.5 microliters) and L-NAME (25 nmol in 12.5

microliters) demonstrated an ***augmentive*** effect in attenuating

skin blood flow. "

(stars added by me for **emphasis**)

If we have any French readers of rosacea-support who could contact

Dr. LACHARRIERE it would be extremely interesting to hear the

studies he has conducted.

Just my thoughts,

.

> I did a little research on CGRP antagonists on the web. I didnt

find a whole lot, but I found this website at the U.S. patent office

or something.

>

> http://patft.uspto.gov/netacgi/nph-Parser?

Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=/netahtml/srchnum.htm&r=1&f=G&l=

50&s1='5932215'.WKU.&OS=PN/5932215&RS=PN/5932215

>

> Not sure if the link will work. Anyway, it talks about CGRP has

been shown in studies to be effective for treating cea and

erythema for many of the reasons that have already been discussed on

here. It talks about how cea has no cure, and how products like

Metronidazole, antibiotics, etc, are primarily ineffective at

treating certain aspects of cea because they dont go after the

cause of the disorder. This patent talks about a topical CGRP-

blocker, possibly mixed with a substance-P blocker, or

antiinflammatory substances, or even with antibiotics. It seems

like something that was actually put together like this would blow

every other cea treatment currently available right out of the

water. At the end they give seven examples of how to make a

succesful CGRP-blocking topical:

>

> " EXAMPLE 1

>

> Face cream (oil-in-water emulsion):

>

>

> ______________________________________

> CGRP 8-37 0.5%

> Glyceryl stearate 2%

> Polysorbate 60 (Tween 60

> 1%

> marketed by ICI)

> Stearic acid 1.4%

> Triethanolamine 0.7%

> Carbomer 0.4%

> Cyclomethicone 8%

> Sunflower Oil 12%

> Antioxidant 0.05%

> Preservative 0.3%

> Water qs 100%

>

> EXAMPLE 5 Cream (oil-in-water emulsion):

______________________________________

> Glyceryl stearate 2%

> CGRP 8-37 0.02%

> Polysorbate 60 (Tween 60

> 1%

> marketed by ICI)

> Stearic acid 1.4%

> Metronidazole 0.5%

> Triethanolamine 0.7%

> Carbomer 0.4%

> Cyclomethicone 8%

> Sunflower oil 10%

> Antioxidant 0.05%

> Preservative 0.3%

> Water qs 100%The website made it sound like

the technology already exists to make this happen, so my question

is, why hasnt it happened yet?Adam

>

>

>

>

[Guest guest]

Hi,

L'Oreal holds patents on CGRP antagonists as well as many others

(substance P antagonists, TNF-alpha antagonists, etc) for rosacea.

They also hold patents related to strontium nitrate and rosacea /

sensitive skin (as does Dr. Hahn of Cosmederm).

One person in particular, Dr. OLIVIER DE LACHARRIERE has filed many

patents directly applicable to rosacea for L'Oreal and others. Most

recently he has filed the following patent for NO synthase

inhibitors and rosacea (see link below).

http://appft1.uspto.gov/netacgi/nph-Parser?

Sect1=PTO2&Sect2=HITOFF&p=1&u=/netahtml/PTO/search-

bool.html&r=8&f=G&l=50&co1=AND&d=PG01&s1=rosacea&OS=rosacea&RS=rosace

a

As anyone who has worked with patent law will attest, it is a vast

and complex area. The fact that many of these patents will state

that " complete clearance " of redness has been achieved one must

treat with some caution; many times a company will simply take out

extremely similar patents on a host of similar technologies. In

L'Oreal's case they have patents across a wide range of antagonists

that block actions of mediators in the facial skin... This is how

patent law works; an initial " invention " is made applicable to the

widest possible means of use or relative uses. Will this stop us

being able to have NO inhibitors or CGRP antagonists made up for us

as part of a trial with a research doctor? The answer is almost

certainly not. Patents are often kept as a form of " insurance " (if

one company claims patent infringement on another, there is

invariably a counter-claim) and are indeed not guaranteed to

be " valid " unless they have been tested in a court of law. In other

words, companies hedge their bets by patenting " inventions " which

*MAY* work... rather than ones which they have finalised or tested

to perfection. From what I understand talking to researchers, CGRP

(8-37) as mentioned in the patent below, is NOT a good drug to apply

topically. But the patent has been written as patents always are

and claims coverage of any CGRP antagonists applied to rosacea (i.e.

current or future).

There is no doubt in my mind however that a *combined* CGRP and NO

inhibitor would be extremely beneficial for rosacea sufferers.

Medical studies already exist that show combined NO inhibitors and

CGRP antagonists have a cumulative effect on *decreasing* blood

flow. Here is the relevant study (note that the drugs were injected

cutaneously rather than applied topically):

" Calcitonin gene-related peptide, substance P and nitric oxide are

involved in cutaneous inflammation following ultraviolet

irradiation. "

Key finding:

" The inhibitor of NO synthase NG-nitro-L-arginine methyl ester

hydrochloride (L-NAME, 25 nmol in 25 microliters, s.c.) attenuated

skin blood flow by 38%. Concurrent injections s.c. of CGRP-(8-37)

(1.5 nmol in 12.5 microliters) and L-NAME (25 nmol in 12.5

microliters) demonstrated an ***augmentive*** effect in attenuating

skin blood flow. "

(stars added by me for **emphasis**)

If we have any French readers of rosacea-support who could contact

Dr. LACHARRIERE it would be extremely interesting to hear the

studies he has conducted.

Just my thoughts,

.

> I did a little research on CGRP antagonists on the web. I didnt

find a whole lot, but I found this website at the U.S. patent office

or something.

>

> http://patft.uspto.gov/netacgi/nph-Parser?

Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=/netahtml/srchnum.htm&r=1&f=G&l=

50&s1='5932215'.WKU.&OS=PN/5932215&RS=PN/5932215

>

> Not sure if the link will work. Anyway, it talks about CGRP has

been shown in studies to be effective for treating cea and

erythema for many of the reasons that have already been discussed on

here. It talks about how cea has no cure, and how products like

Metronidazole, antibiotics, etc, are primarily ineffective at

treating certain aspects of cea because they dont go after the

cause of the disorder. This patent talks about a topical CGRP-

blocker, possibly mixed with a substance-P blocker, or

antiinflammatory substances, or even with antibiotics. It seems

like something that was actually put together like this would blow

every other cea treatment currently available right out of the

water. At the end they give seven examples of how to make a

succesful CGRP-blocking topical:

>

> " EXAMPLE 1

>

> Face cream (oil-in-water emulsion):

>

>

> ______________________________________

> CGRP 8-37 0.5%

> Glyceryl stearate 2%

> Polysorbate 60 (Tween 60

> 1%

> marketed by ICI)

> Stearic acid 1.4%

> Triethanolamine 0.7%

> Carbomer 0.4%

> Cyclomethicone 8%

> Sunflower Oil 12%

> Antioxidant 0.05%

> Preservative 0.3%

> Water qs 100%

>

> EXAMPLE 5 Cream (oil-in-water emulsion):

______________________________________

> Glyceryl stearate 2%

> CGRP 8-37 0.02%

> Polysorbate 60 (Tween 60

> 1%

> marketed by ICI)

> Stearic acid 1.4%

> Metronidazole 0.5%

> Triethanolamine 0.7%

> Carbomer 0.4%

> Cyclomethicone 8%

> Sunflower oil 10%

> Antioxidant 0.05%

> Preservative 0.3%

> Water qs 100%The website made it sound like

the technology already exists to make this happen, so my question

is, why hasnt it happened yet?Adam

>

>

>

>

[Guest guest]

Hi,

L'Oreal holds patents on CGRP antagonists as well as many others

(substance P antagonists, TNF-alpha antagonists, etc) for rosacea.

They also hold patents related to strontium nitrate and rosacea /

sensitive skin (as does Dr. Hahn of Cosmederm).

One person in particular, Dr. OLIVIER DE LACHARRIERE has filed many

patents directly applicable to rosacea for L'Oreal and others. Most

recently he has filed the following patent for NO synthase

inhibitors and rosacea (see link below).

http://appft1.uspto.gov/netacgi/nph-Parser?

Sect1=PTO2&Sect2=HITOFF&p=1&u=/netahtml/PTO/search-

bool.html&r=8&f=G&l=50&co1=AND&d=PG01&s1=rosacea&OS=rosacea&RS=rosace

a

As anyone who has worked with patent law will attest, it is a vast

and complex area. The fact that many of these patents will state

that " complete clearance " of redness has been achieved one must

treat with some caution; many times a company will simply take out

extremely similar patents on a host of similar technologies. In

L'Oreal's case they have patents across a wide range of antagonists

that block actions of mediators in the facial skin... This is how

patent law works; an initial " invention " is made applicable to the

widest possible means of use or relative uses. Will this stop us

being able to have NO inhibitors or CGRP antagonists made up for us

as part of a trial with a research doctor? The answer is almost

certainly not. Patents are often kept as a form of " insurance " (if

one company claims patent infringement on another, there is

invariably a counter-claim) and are indeed not guaranteed to

be " valid " unless they have been tested in a court of law. In other

words, companies hedge their bets by patenting " inventions " which

*MAY* work... rather than ones which they have finalised or tested

to perfection. From what I understand talking to researchers, CGRP

(8-37) as mentioned in the patent below, is NOT a good drug to apply

topically. But the patent has been written as patents always are

and claims coverage of any CGRP antagonists applied to rosacea (i.e.

current or future).

There is no doubt in my mind however that a *combined* CGRP and NO

inhibitor would be extremely beneficial for rosacea sufferers.

Medical studies already exist that show combined NO inhibitors and

CGRP antagonists have a cumulative effect on *decreasing* blood

flow. Here is the relevant study (note that the drugs were injected

cutaneously rather than applied topically):

" Calcitonin gene-related peptide, substance P and nitric oxide are

involved in cutaneous inflammation following ultraviolet

irradiation. "

Key finding:

" The inhibitor of NO synthase NG-nitro-L-arginine methyl ester

hydrochloride (L-NAME, 25 nmol in 25 microliters, s.c.) attenuated

skin blood flow by 38%. Concurrent injections s.c. of CGRP-(8-37)

(1.5 nmol in 12.5 microliters) and L-NAME (25 nmol in 12.5

microliters) demonstrated an ***augmentive*** effect in attenuating

skin blood flow. "

(stars added by me for **emphasis**)

If we have any French readers of rosacea-support who could contact

Dr. LACHARRIERE it would be extremely interesting to hear the

studies he has conducted.

Just my thoughts,

.

> I did a little research on CGRP antagonists on the web. I didnt

find a whole lot, but I found this website at the U.S. patent office

or something.

>

> http://patft.uspto.gov/netacgi/nph-Parser?

Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=/netahtml/srchnum.htm&r=1&f=G&l=

50&s1='5932215'.WKU.&OS=PN/5932215&RS=PN/5932215

>

> Not sure if the link will work. Anyway, it talks about CGRP has

been shown in studies to be effective for treating cea and

erythema for many of the reasons that have already been discussed on

here. It talks about how cea has no cure, and how products like

Metronidazole, antibiotics, etc, are primarily ineffective at

treating certain aspects of cea because they dont go after the

cause of the disorder. This patent talks about a topical CGRP-

blocker, possibly mixed with a substance-P blocker, or

antiinflammatory substances, or even with antibiotics. It seems

like something that was actually put together like this would blow

every other cea treatment currently available right out of the

water. At the end they give seven examples of how to make a

succesful CGRP-blocking topical:

>

> " EXAMPLE 1

>

> Face cream (oil-in-water emulsion):

>

>

> ______________________________________

> CGRP 8-37 0.5%

> Glyceryl stearate 2%

> Polysorbate 60 (Tween 60

> 1%

> marketed by ICI)

> Stearic acid 1.4%

> Triethanolamine 0.7%

> Carbomer 0.4%

> Cyclomethicone 8%

> Sunflower Oil 12%

> Antioxidant 0.05%

> Preservative 0.3%

> Water qs 100%

>

> EXAMPLE 5 Cream (oil-in-water emulsion):

______________________________________

> Glyceryl stearate 2%

> CGRP 8-37 0.02%

> Polysorbate 60 (Tween 60

> 1%

> marketed by ICI)

> Stearic acid 1.4%

> Metronidazole 0.5%

> Triethanolamine 0.7%

> Carbomer 0.4%

> Cyclomethicone 8%

> Sunflower oil 10%

> Antioxidant 0.05%

> Preservative 0.3%

> Water qs 100%The website made it sound like

the technology already exists to make this happen, so my question

is, why hasnt it happened yet?Adam

>

>

>

>