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    • 1. 发明授权
    • Peptide amides and process for their manufacture
    • 肽酰胺及其制造方法
    • US4459225A
    • 1984-07-10
    • US359242
    • 1982-03-18
    • Volker TeetzRolf GeigerHans G. AlpermannMartin Bickel
    • Volker TeetzRolf GeigerHans G. AlpermannMartin Bickel
    • C07K5/08A61K38/00A61P25/04C07K5/087C07K5/10C07K5/107C07K7/06C07K14/70C07C103/52
    • C07K5/0812C07K14/702C07K5/1016
    • New peptide amides of the formula IH--Tyr--D--Lys(For)--Gly--X (I)whereinFor is formyl,X is alkylamino, dehydro-Phe or Phe-alkylamido having up to 6 carbon atoms in the alkyl moiety, which moiety may be substituted by hydroxy and/or phenyl, Phe-cycloalkylamide or Phe-cycloalkylene amide having up to 8 carbon atoms in the cycloalkyl or cyclalkylene moiety, 1 to 2 CH.sub.2 groups being optionally replaced by --NH--, --O--, --S-- or --CO--, Phe-alkylene-cycloalkylamide having from 5 to 6 ring carbon atoms, which amide may be substituted by carbonamido,N-alkylcarbonamido or alkyl and 1 carbon atom whereof may be replaced by nitrogen, Phe-endo- or exo-norbornylamide or Phe-thiazolamide or Phe-thiazolidine-carboxylic acid amide, which may be substituted by 1 to 4 methyl groups each,and process for their manufacture are disclosed. These peptide amides are distinguished by an analgetic activity and suppress the motility of the ileum of the guinea pig.
    • 式I H-Tyr-D-Lys(For)-Gly-X(I)的新肽酰胺其中For为甲酰基,X为烷基部分中具有至多6个碳原子的烷基氨基,脱氢-Phe或Phe-烷基酰氨基 ,该部分可以被羟基和/或苯基取代,在环烷基或环亚烷基部分具有至多8个碳原子的Phe-环烷基酰胺或Phe-亚环烷基酰胺,1至2个CH 2基团任选地被-NH-,-O- ,具有5至6个环碳原子的-S-或-CO-,Phe-亚烷基 - 环烷基酰胺,该酰胺可以被碳酰氨基取代,N-烷基碳酰氨基或其烷基和碳原子可以被氮取代,Phe-内 - 或外 - 降冰片烷酰胺或Phe-噻唑胺或Phe-噻唑烷 - 羧酸酰胺,其可以各自被1至4个甲基取代,以及其制造方法。 这些肽酰胺通过止痛活性来区分,并抑制豚鼠回肠的动力。