发明名称 Basic esters of fatty alcohols and their use as anti-inflammatory or immunomodulatory agents
摘要 Basic esters of fatty alcohols of the general formula: R1-O—CO-A or pharmaceutically acceptable salts thereof, wherein R1 is C12-C24 alkyl or C10-C24 alkenyl, and A is a residue containing at least one acyclic or cyclic amino group and/or at least one heteroaromatic ring containing a tertiary or quaternary nitrogen atom, are anti-inflammatory and immunomodulatory agents, useful in the treatment of immunologically-mediated inflammation, as adjuvants for antigens involved in both cellular and humoral responses.
申请公布号 US8987263(B2) 申请公布日期 2015.03.24
申请号 US200310530776 申请日期 2003.10.09
申请人 发明人 Shinitzky Meir;Cohen Irun R.;Margalit Raanan;Herzig Yaacov;Sterling Jeffrey;Toth Gyorgy;Miskolczi Istvan;Rantal Ferenc;Tamas Tivadar
分类号 A61K31/5377;A61K31/495;A61K31/131;C07D295/00;C07C211/01;A61K31/195;A61K31/22;A61K31/221;A61K31/222;A61K31/223;A61K31/44;A61K31/4425;A61K45/06 主分类号 A61K31/5377
代理机构 Cooper & Dunham LLP 代理人 White John P.;Cooper & Dunham LLP
主权项 1. A compound of the general formula: R1-O—CO-A wherein R1 is C20-C24 alkyl or C16-C18 alkenyl and A is a residue of the formula: wherein R2 is H, C1-C6 alkyl, aryl, or aralkyl, wherein any aryl moiety may be unsubstituted or substituted by nitro, cyano, halo, hydroxy, NR6R7, or CR8R8NR6R7; R3 is H, a pair of electrons, or C1-C6 alkyl; R4 and R5 each is H or each is C1-C6 alkyl, or R4 and R5 together with the nitrogen atom to which they are attached form a 5-7 membered saturated ring optionally interrupted by an oxygen atom or by a nitrogen atom optionally substituted by C1-C6 alkyl; and R6, R7 and R8 each independently is H or C1-C6 alkyl,wherein: when R3 is a pair of electrons and R4 and R5 are each H, then R2 is C5-C6 alkyl, aryl, or aralkyl, wherein any aryl moiety may be unsubstituted or substituted by nitro, cyano, halo, NR6R7, or CR8R8NR6R7; and pharmaceutically acceptable salts thereof.
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