New glucofuranose esters and glucopyranose esters of alkyl-fumarates useful for treating psoriasis and other hyperliferative, inflammatory and autoimmune disorders.

Henrik Nilsson (Inventor), Jens Enevold Thaulov Andersen (Inventor)

Research output: Patent

Abstract

In medicine for combating tissue degenerative processes, in the treatment of e.g. psoriasis, psoriatic arthritis, neurodermatitis, atopic dermatitis, inflammatory bowel disease, autoimmune diseases, pain, sarcoidosis, necrobiosis lipoidica, granuloma annulare, lupus nephritis, myasthenia gravis, uveitis, refractory uveitis, vernal conjunctivitis, pemphigus vulgaris, scleroderma, multiple sclerosis; in prevention of rejection following organ transplantation (all claimed); also for treating Crohn's disease, ulcerative colitis, polyarthritis, juvenile-onset diabetes mellitus, Hashimoto's thyroiditis, Grave's disease, systemic lupus erythematosus, Sjogren's syndrome, Pernicious anemia, Chronic active (lupoid) hepatitis, Rheumatoid arthritis (RA), optic neuritis, radicular pain, pain associated with radiculopathy, neuropathic pain and sciatica/sciatic pain, sarcoidosis, necrobiosis lipoidica, granuloma annulare. ADVANTAGE - The compound has increased dissolution rate leading to increased bioavailability in-vivo as compared to administration of monomethyl fumarate; provides improved treatment e.g. with a reduction in flushing and/or a reduction in gastro-intestinal related side effects (e.g. diarrhea, stomach ache, stomach pain, abdominal pain, abdominal cramps, nausea, flatulence, tenesmus, meteorism, an increased frequency of stools, a feeling of fullness and upper abdominal cramps) upon oral administration. DETAILED DESCRIPTION - Glucofuranose esters and glucopyranose esters of alkyl-fumarates of formula (I) and (II) and their enantiomers, racemates, diastereomers, anomers and/or tautomeric forms.
Original languageEnglish
Patent numberWO2007006308-A1; EP1915387-A1; IN200800535-P2; EP1915387-B1
Publication statusPublished - 2007
Externally publishedYes

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