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US 5,013,722 AGranted
Cholecystokinin analogs for controlling appetite
AssigneeHoffmann-LaRoche Inc.
InventorsWaleed Danho, Vincent S. Madison, Joseph Triscari
Life of this patent
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Abstract
Cholecystokinin analogs useful for suppressing food intake in mammals and humans.
Claims22
A peptide of the formula
- X--(R).sub.n --Tyr(SO.sub.3 H)--R.sub.1 --R.sub.2 --R.sub.3 --R.sub.4 --R.sub.5 --N--methyl--Phe--Y
- wherein ##STR5## R=Asp or Aeg R.sub.1 =Met, Nle, Leu, Ile, or a bond
- R.sub.2 =Gly, Ala, D-Ala, or .alpha.-Ala
- R.sub.3 =Trp or Trp(For)
- R.sub.4 =Met, Nle, or Nva
- R.sub.5 =Thr(SO.sub.3 H), Ser(SO.sub.3 H), or Hyp(SO.sub.3 H)
- R.sub.6 =H or C.sub.1-3 alkyl
- R.sub.7 =H, C.sub.1-3 alkyl, or C.sub.1-3 haloalkyl
- R.sub.8 =H or C.sub.1-3 alkyl
- Y=OR.sub.8 or NR.sub.9 R.sub.10
- R.sub.9 =H or C.sub.1-3 alkyl
- R.sub.10 =H or C.sub.1-3 alkyl
- n=0 or 1
- m=1-14
- or the pharmaceutically acceptable salt.
12 more elements
A method for suppressing food intake in mammals comprising administering to said mammal an effective food intake suppressing amount of a peptide of the formula:
- X--(R).sub.n --Tyr(SO.sub.3 H)--R.sub.1 --R.sub.2 --R.sub.3 --R.sub.4 --R.sub.5 --N--methyl--Phe--Y
- wherein ##STR6## R=Asp or Aeg R.sub.1 =Met, Nle, Leu, Ile, or a bond
- R.sub.2 =Gly, Ala, D-Ala, of .beta.-Ala
- R.sub.3 =Trp or Trp(For)
- R.sub.4 =Met, Nle, or Nva
- R.sub.5 =Thr(SO.sub.3 H), Ser(SO.sub.3 H), or Hyp(SO.sub.3 H)
- R.sub.6 =H or C.sub.1-3 alkyl
- R.sub.7 =H, C.sub.1-3 alkyl, or C.sub.1-3 haloalkyl
- R.sub.8 .dbd.H or C.sub.1-3 alkyl
- Y.dbd.OR.sub.8 or NR.sub.9 R.sub.10
- R.sub.9 .dbd.H or C.sub.1-3 alkyl
- R.sub.10 .dbd.H or C.sub.1-3 alkyl
- n.dbd.0 or 1
- m.dbd.1-4
- or the pharmaceutically acceptable salt.
12 more elements
Dependencies are inferred from the claim text.