发明名称 PRODRUGS OF METHYL HYDROGEN FUMARATE, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE
摘要 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: (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, bis-(2-methoxyethylamino)carbamoyl]methyl methyl (2E)but-2-ene-1,4-dioate, 1-{ 2-{ (2E)-3-(methoxycarbonyl)prop-2-enoyloxy]acetyl} (2S)pyrrolidine-2-carboxylic acid, (N-{ [tert-butyl)oxycarbonyl]methyl} -N-methylcarbamoyl)methyl methyl (2E)but-2ene1,4-dioate, and (1S)-1-[N,N-bis(2-methoxyethyl)carbamoyl]ethyl methyl (2E)but-2-ene-1,4-dioate. 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.
申请公布号 NZ590746(A) 申请公布日期 2012.10.26
申请号 NZ20090590746 申请日期 2009.08.19
申请人 XENOPORT, INC. 发明人 GANGAKHEDKAR, ARCHANA;DAI, XUEDONG;ZERANGUE, NOA;VIRSIK, PETER A
分类号 A61P9/10;A61K31/16;A61P17/06;A61P19/02;C07C69/60;C07C69/96 主分类号 A61P9/10
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