专利号:US-7579487-B2 优先权日:2004-05-11 标 题 :Process for making N-sulfonated-amino acid derivatives 发明人:DREHER SPENCER D; IKEMOTO NORIHIRO; SHULTZ C SCOTT; WILLIAMS J MICHAEL 权利人:MERCK & CO INC 摘要:This invention relates to a process for preparing optically active α-amino acid substrates which are used to make potent lethal factor (LF) inhibitors for the treatment of anthrax. This invention further relates to a process for synthesis of potent LF-inhibitors for the treatment of anthrax. Specifically, the invention concerns a novel, high-yielding and highly enantioselective asymmetric hydrogenation reaction of a tetrasubstituted ene-sulfonamide acid or ester.
专利号:US-5998595-A 优先权日:1996-11-05 标题:Azidohalogenobenzyl derivatives, sugar compounds and protection of hydroxy groups 发明人:KUSUMOTO SHOICHI; FUKASE KOICHI 权利人:WAKO PURE CHEM IND LTD 摘要:Azidohalogenobenzyl derivatives of the formula (I) ##STR1## wherein A is a halogen atom, B is a halogen atom or a hydrogen atom, and X is a group reactive with a hydroxy group, methods of protecting hydroxy group(s) using said derivatives, and sugar compounds wherein a hydrogen atom of at least one hydroxy group is substituted by an azidohalogenobenzyl group. According to the present invention, there are provided novel derivatives capable of introducing a group into a compound having hydroxy group(s), which group is useful as a stable hydroxy-protecting group even in solid phase synthesis for the purpose of the extension of sugar chain under continuous acidic conditions and of being removed under mild conditions; sugar compounds protected by using said derivatives; and methods of protecting hydroxy group(s) using said derivatives.
专利号:US-2005026965-A1 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of nicotinanilide-N-oxides
专利号:US-2003004189-A1 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of nicotinanilide-N-oxides
专利号:US-2010063105-A1 优先权日:2000-12-29 标题 :Pharmaceutical uses and synthesis of nicotinanilide-n-oxides
专利号:US-7141590-B2 优先权日:2000-12-29 标题 :Pharmaceutical uses and synthesis of nicotinanilide-N-oxides 发明人:CUTSHALL NEIL S; YAGER KRAIG M 权利人:UCB SA 摘要:Disclosed are nicotinanilide-N-oxide compounds, methods for their production, pharmaceutical compositions which include these compounds, and methods for their use in various therapies.