Galderma Patent Portfolio: Dipyridyl Compounds

Written by on December 30, 2012 in Galderma, patents with 2 Comments

The pharmaceutical giant Galderma continues to build its war chest of rosacea patents. A newly surfaced patent covers treating rosacea with a dipyrdyl compound.

A brief online search for Galderma-assigned patents that mention rosacea reveals almost 2000 matches, with about 11,000 patents being assigned to Galderma Research & Development overall. These numbers are likely to be conservative.

The list of potential rosacea treatments is lengthy and exotic including such compounds as idrocilamidepicketprofenavermectines and fepradinol.

Who Cares?

A recent example of how Galderma patent filings are important is the new drug in development by Galderma called CD5024.

This product, 1% Topical Ivermectin appears to be covered by several Galderma assigned patents, and may result in a new drug to treat rosacea.

Rosacea sufferers need well funded pharmaceutical companies to be able to afford the rigorous campaign that is required to create novel treatments.

Dipyridyl Patent

Here are some extracts from this recent filing, to give a flavour of what is being protected as an invention.

Use of a dipyridyl compound for treating rosacea

Agent: Galderma Research & Development – Biot, FR
Inventors: Irina Safonova, Jean-Dominique Pierret
USPTO Applicaton #: #20120322829

Furthermore, research, in particular clinical research, tends to suggest that rosacea is an inflammatory pathology.

An over-regulation of proinflammatory cytokines and matrix metalloproteinases (MMPs) contributes to a chronic vasodilatation and to a continuous degradation of the dermal matrix. Many studies describe increased expression and activity of MMPs, such as MMP-8 and MMP-9, in patients suffering from rosacea.

A reduction in the expression and/or activity of certain MMPs has been associated with a therapeutic benefit in the case of rosacea.

Tetracycline derivatives, which include doxycycline, possess not only an antibiotic activity, but also anti-inflammatory properties. These anti-inflammatory effects due to doxycycline include a reduction in the production of proinflammatory cytokines, an inhibition of the expression of the NO synthase enzyme, and a reduction in the expression and/or the activity of certain MMPs, such as MMP-1, MMP-2, MMP-8, MMP-9, MMP-12 and MMP-13.

The objective of the present invention is, in particular, to propose an effective treatment of rosacea, which limits the effects. Preferably, this treatment is carried out topically, which avoids any systemic side effect.

One subject of the present invention is therefore compounds of formula (I) below:


in which R1, R2, R3, R′1, R′2 and R′3 each independently represent a hydrogen atom or a linear or branched alkyl radical having from 1 to 6 carbon atoms, or the pharmaceutically acceptable salts thereof, for the use thereof in the treatment of rosacea.

The results of this study indicate that

  • 4,4′-dimethyl-2,2′-dipyridyl,
  • 5,5′-dimethyl-2,2′-dipyridyl and
  • 6,6′-dimethyl-2,2′-dipyridyl

were able to inhibit the activity of the MMPs. The compounds tested particularly inhibit MMP-8 and MMP-9, matrix metalloproteinases known for being upregulated in patients suffering from rosacea. These compounds were less active on certain other MMPs, such as MMP-1, MMP-2, MMP-12, MMP-14 and MMP-13. These MMPs, the inhibition of which by tetracycline derivatives, such as doxycycline, has been demonstrated, tetracyclines being known for being effective in the treatment of rosacea. Moreover, the compounds had no activity on TACE (TNF-alpha converting enzyme), the matrix metalloproteinase not being known for being involved in rosacea.

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Read more about: Galderma, patents

About the Author

About the Author: David Pascoe started the Rosacea Support Group in October 1998. .

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2 Reader Comments

  1. maggie doud says:

    rosacea in face, eyes puffy, now reaching to hairline with red, tiny tiny blistering. using metrogel for th epast 4 days =- what else can i do?

  2. Brady Barrows says:

    Your cryptic ‘Who Cares?’ is at the very least fun and interesting to muse about. Other than the fact that someone needs to be a chemist or a scientific expert in interpreting the compounds of the formula into layman’s terms it appears that the drug is to reduce certain matrix metalloproteinases (MMPs) which are are zinc-dependent endopeptidases. MMPs were first described in vertebrates (1962) but are now known to be in invertebrates and plants. Endopeptidases break peptide bonds of nonterminal amino acids. Richard Gallo, et. al, announced the news in 2007 that “found that
    small proteins called anti-microbial peptides caused the same skin symptoms that are seen in rosacea. The peptides are part of the body’s immune system … A precursor form of these peptides known as cathelicidin normally helps protect the skin from infection. Indeed, some skin problems occur when there is toolittle cathelicidin. But it turned out that people with rosacea had too much cathelicidin … Rosacea patients
    also had high levels of stratum corneum tryptic enzymes (SCTE), the precursor of the disease-causing peptide…”

    When you consider that understanding all this is good news if once can comprehend it, we need to pause and reflect that it has been now over five years since Gallo’s team announced these findings. Galderma is trying to make a prescription treatment to knock out certain MMPs that a lot of trial and errors have to occur before we see the results that are wanted. Huge amounts of money are spent on all this. All we can do is hope and wait. And a few rosaceans may make the clinical trials.

    I appreciate you keeping up with all this since it is a job in itself just to post such information as this. Kudos to Dave Pascoe.

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