C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 7/06 (2006.01) A61K 51/08 (2006.01) C07K 14/705 (2006.01) G01N 33/566 (2006.01) G01N 33/58 (2006.01)
Patent
CA 2163996
The radioligands are peptides having at least six amino acids and falling within the following general structure: A-B-C-E-F-Z wherein A = Thr, Ser, Ala, or Gly; B = Phe or Phe or halogenated Phe; C, when F is Tyr(l) or Tyr(I2), = Leu, Val, Cha, Me, Phe, Arg, hArg, or Lys; C, when F is Tyr, = NH-CH(R)CO-, wherein R = (CH2)nNHCO(CH2)2-C6H3IO, (CH2)DNHCO(CH2)2-C6H4IO, CH2-C6H4IO, or CH2-C6H3I2O, wherein n = 2, 3 or 4; D = Leu or Cha; E = Arg, hArg, or Lys; F = Tyr, Tyr(I), or Tyr(I2); and Z = OH, OCH3, or NRR'; wheran RR' = H, alkyl, aryl, or 1-15 amino acids. Thrombin receptor radioligands of the present invention are useful for screening for thrombin receptor antagonists.
Les radioligands sont des peptides ayant au moins six aminoacides et de structure générale suivante: A-B-C-D-E-F-Z, dans laquelle A = Thr, Ser, Ala, ou Gly; B = Phe ou Phe halogéné; C, quand F est Tyr(I) ou Tyr(I2), = Leu, Val, Cha, Nle, Phe, Arg, hArg, ou Lys; C, quand F est Tyr, = NH-CH(R)CO-, où R = (CH2)nNHCO(CH2)2-C6H3IO, (CH2)nNHCO(CH2)2-C6H4IO, CH2-C6H4IO, ou CH2-C6H3I2O, où n = 2,3 ou 4; D = Leu ou Cha; E = Arg, hArg, ou Lys; F = Tyr, Tyr(I), ou Tyr(I2); et Z = OH, OCH3, ou NRR'; où RR' = H, alkyle, aryle, ou 1-15 aminoacides. Les radioligands du récepteur de la thrombine selon la présente invention sont utiles pour le dépistage des antagonistes du récepteur de la thrombine.
Connolly Thomas M.
Feng Dong-Mei
Gould Robert J.
Nutt Ruth F.
Veber Daniel F.
Merck & Co. Inc.
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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