Prodrugs of methyl, hydrogen fumarate, pharmaceutical compositions thereof, and methods of use

Disclosed are prodrugs of methyl hydrogen fumarate (monomethyl fumarate) according to formula (I), and methods for their preparation. Specific examples of compounds of formula (I) include: (2E)-3-[(2-morpholin-4-yl-2-oxoethyl)oxycarbonyI]prop-2-enoic acid; (2E)-3-{ [(N,N-diethylcarbamoyl)methyI]oxyc...

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Hauptverfasser: ARCHANA GANGAKHEDKAR, NOA ZERANGUE, PETER A VIRSIK, XUEDONG DAI
Format: Patent
Sprache:eng
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Zusammenfassung:Disclosed are prodrugs of methyl hydrogen fumarate (monomethyl fumarate) according to formula (I), and methods for their preparation. Specific examples of compounds of formula (I) include: (2E)-3-[(2-morpholin-4-yl-2-oxoethyl)oxycarbonyI]prop-2-enoic acid; (2E)-3-{ [(N,N-diethylcarbamoyl)methyI]oxycarbonyl} prop-2-enoic acid; (2E)-3-({ [N-benzylcarbamoyI]methyl} oxycarbonyl) prop-2-enoic acid. Compounds of formula (I) are useful for treating psoriasis, asthma, chronic obstructive pulmonary disease, cardiac insufficiency, left ventricular insufficiency, myocardial infarction, angina pectoris, Parkinson's disease, Alzheimer's disease, Huntington's disease, retinopathia pigmentosa, mitochondrial encephalomyopathy, transplantation rejection, multiple sclerosis,ischemia, reperfusion injury, AGE induced genome damage, inflammatory bowel disease, Crohn's disease, or ulcerative colitis.