发明名称 PEPTOID OLIGOMERS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME
摘要 Novel peptoid oligomers are disclosed that have a formula represented by the following formula I:;;The peptoids demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present cyclic and linear peptoids are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provoked by standard antibiotics.
申请公布号 US2015011465(A1) 申请公布日期 2015.01.08
申请号 US201414481148 申请日期 2014.09.09
申请人 Kirshenbaum Kent;Shin Sung Bin 发明人 Kirshenbaum Kent;Shin Sung Bin
分类号 C07K7/66;C07K7/64;A01N43/713;A01N47/44;A01N37/26;A01N43/90;C07K7/06;A01N43/36 主分类号 C07K7/66
代理机构 代理人
主权项 1. A peptoid oligomer according to formula Ia or Ib: comprised of one or more monomers according to formula IIa, IIb, IIc, or IId: wherein each R1 is independently substituted or unsubstituted alkyl; each R2 is independently hydrogen, or substituted or unsubstituted alkyl; or each R1 and R2 are join together to form a 4-7 membered heterocyclic ring; each R1a is independently unsubstituted alkyl; each R1b is independently aminoalkyl, guanidinoalkyl (H2N—C(═NH)—NH-alkyl), or N-containing heteroarylalkyl; each R1c is independently substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted diarylalkyl; each m is 0, 1, 2, or 3; X is H, or substituted or unsubstituted acyl; Y is NH2, OH, acylamino, or acyloxy; n is an integer between 2-20, when the peptoid oligomer is of formula Ia; and n is an integer between 4-20, when the peptoid oligomer is of formula Ib; or a salt thereof; and stereoisomers, isotopic variants and tautomers thereof; provided that: vi) the peptoid oligomer may comprise one, two, three or all four, IIa, IIb, IIe and IId, of monomers;vii) at least one of the monomers in the peptoid oligomer is of formula IIb;viii) each R1 in the peptoid oligomer may be the same or different;ix) each R2 in the peptoid oligomer may be the same or different; andx) when the peptoid oligomer is of formula Ia and R1b is 4-aminobutyl or 2-imidazol-4-ylethyl, then X is other than H; or a pharmaceutically acceptable salt, solvate or prodrug thereof; and stereoisomers, isotopic variants and tautomers thereof.
地址 New York NY US