New fumaric acid monoalkylesters, useful to treat e.g. psoriasis, psoriatic arthritis, neurodermatitis, atopic dermatitis, inflammatory bowel disease, autoimmune diseases, pain, sarcoidosis, necrobiosis lipoidica and lupus nephritis

Henrik Nilsson (Inventor), Jens Enevold Thaulov Andersen (Inventor), B./W. Mueller (Inventor), B. Mueller (Inventor), B./W. Mueller (Inventor)

Research output: Patent

Abstract

Are useful to fight against tissue degenerative processes; and to treat psoriasis, psoriatic arthritis, neurodermatitis, atopic dermatitis, inflammatory bowel disease, autoimmune diseases, pain, sarcoidosis, necrobiosis lipoidica, lupus nephritis, myasthenia gravis, uveitis, refractory uveitis, vernal conjunctivitis, pemphigus vulgaris, scleroderma, multiple sclerosis and/or granuloma annulare; and/or to prevent organ transplant rejection (claimed). ADVANTAGE - (I) Provide an alternative and potentially improved treatment e.g. with a reduction in flushing and/or gastrointestinal related side effects and/or flush side effects with increased bioavailability. The gastrointestinal related side effect of (I) was tested in caco-2 cell monolayers using biological assay. The results showed that (I) caused no damage to the cell monolayers. DETAILED DESCRIPTION - Fumaric acid monoalkylesters of formula R1-O-C(O)-CH=COO-X+ (I) and their enantiomers or racemic mixtures, are new. R1 = 1-5C alkyl; and X+ = a protonated form of an amino acid. An INDEPENDENT CLAIM is also included for a pharmaceutical composition comprising (I).
Original languageEnglish
Patent numberWO2007006307-A2
Publication statusPublished - 2007
Externally publishedYes

Bibliographical note

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No.: IN200800534-P2


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No.: EP1915334-A2


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No.: US2008227847-A1

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