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.
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.
Here are some extracts from this recent filing, to give a flavour of what is being protected as an invention.
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
- 5,5′-dimethyl-2,2′-dipyridyl and
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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