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US 5,670,482 AGranted
Neuropeptide Y antagonists
AssigneeGlaxo Wellcome Inc.
InventorsAlejandro Jose Daniels, Dennis Heyer, Antonio Landavazo, Johann Jakob Leban, Andreas Spaltenstein
Life of this patent
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Abstract
The present invention relates to peptides which show improved Neuropeptide Y antagonism to pharmaceutical compositions containing such peptides and their use.
Claims16
A peptide of formula (I), or a multimer thereof or a salt thereof:
- R.sub.1 --X.sub.5 ArgX.sub.6 ArgX.sub.5 --R.sub.2 (I) (SEQ.ID.No:
- 1)
- where
- R.sub.1 =X.sub.1 X.sub.2 X.sub.3 X.sub.4
- in which
- X.sub.1 =Ile, TyrIle, or desNH.sub.2 TyrIle
- X.sub.2 =Asn,Asp,Cys,Dpr,Glu or Gly
- X.sub.3 =Leu,Pro or 3,4-DehydroPro
- X.sub.4 =Aib,Asp,Cys,Dpr,Glu,Gly,Ile,Orn,Tyr or O-MethylThr
- X.sub.5 =Phe,Tyr or O-(2,6-Dichlorobenzyl)Tyr!
- X.sub.6 =Phe or Leu
- where R.sub.2 =--(CH.sub.2).sub.n CH.sub.3, --(CH.sub.2).sub.n NH.sub.2 or ##STR4## in which n=0-4.
9 more elements
A peptide, multimer thereof or salt thereof, the peptide having a structure selected from:
- IleGluProOrnTyrArgLeuArgTyr-NH.sub.2,Cyclic(2,4'),(2',4)-Diamide (SEQ.ID.No:2),
- IleAspProOrnTyrArgLeuArgTyr-NH.sub.2,Cyclic(2,4'),(2',4)-Diamide (SEQ.ID.No:3),
- IleGluProDprTyrArgLeuArgTyr-NH.sub.2,Cyclic(2,4'),(2',4)-Diamide (SEQ.ID.No:4), and
- IleDprProAspTyrArgLeuArgTyr-NH.sub.2,Cyclic(2,4'),(2',4)-Diamide (SEQ.ID.No:5).
1 more element
A peptide, multimer thereof or salt thereof, the peptide having a structure selected from:
- IleCysProCysTyrArgLeuArgTyr-NH.sub.2,Cyclic(2,2'),(4,4')-Disulfide Dimer (SEQ.ID.No:6), and
- IleCysProCysTyrArgLeuArgTyr-NH.sub.2,Cyclic(2,4'),(4,2')-Disulfide Dimer (SEQ.ID.No:6).
Dependencies are inferred from the claim text.