Pharmacologically active 5-oxo-1-imidazolidine acetamide compounds
申请人:Societe I.S.F. S.p.A.
公开号:US04719222A1
公开(公告)日:1988-01-12
The invention relates to 5-oxo-1-imidazolidineacetamide derivatives which help restore learning and memory difficulties associated with ageing. A compound of the invention is 2,2-dimethyl-5-oxo-1-imidazolidineacetamide.
The Partial Molar Volume and Heat Capacity of the Glycyl Group in Aqueous Solution at 25^C
作者:Nessha M. Wise、Gavin R. Hedwig
DOI:10.1007/s10953-006-9038-9
日期:2006.7
e, where x=0 to 2, in aqueous solution at 25^C. Values for V2^ at 25°C have also been determined for two neutral peptide derivatives N-acetylglycylglycinamide and N-acetylglycylglycylglycinamide. These V2°; and Cp,2°; results were used to estimate the partial molar volume and heat capacity of the backbone glycyl group, CH2CONH, of proteins in aqueous solution at 25°;C. The results obtained are compared
An anti-EGFR nanobody was labeled at the C-terminus with a lysosome-sorting NPGY (Asn-Pro-Gly-Tyr) motifviasortase-mediated ligation to enhance the clathrin-mediated endocytosis.
Compounds of Structure (1)
in which
R1 is H, Cl-5 alkyl (straight or branched), or a phenyl or benzyl group optionally substituted by C1-5 alkyl (straight or branched), C1-4 alkoxy (straight or branched) or hydroxy;
R2 is H, OH, Cl-5 alkyl (straight or branched), aryl or acyl;
R3 is H, C1-5 alkyl (straight or branched) or phenyl and R4 is Cl-5 alkyl (straight or branched) or phenyl, or R3 and R4 can together form a 1,4-butylene or 1,5-pentylene group;
R5 is H or C1-5 alkyl (straight or branched);
R6 is H, C1-5 alkyl (straight or branched), -CHR8CONH2 or -CHR8CONHCHR9CONH2; where R8 and R9 (which can be the same or different) are H or C1-5 alkyl (straight or branched); and
R7 is H or Cl-5 alkyl (straight or branched), and pharmaceutically acceptable salts thereof, processes and intermediates for making them, pharmaceutical compositions containing them and their use as nootropic agents.
As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the formula: L1-L2-LP-NH-(CH2)n1-La-Lb-Lc or -L1-L2-LP-wherein the anti-HER2 antibody is connected to the terminal L1, and the antitumor compound is connected to the terminal Lc or LP with the nitrogen atom of the amino group at position 1 as the connecting position.