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US 5,508,383 AGranted
Cyclic peptide LHRH antagonists
AssigneeTap Holdings Inc.
InventorsDaryl R. Sauer, Fortuna Haviv
Life of this patent
Estimating the term…
Abstract
A class of cyclic peptides are effective inhibitors of LHRH and are useful in the treatment of disease conditions which are mediated by sex hormones including prostate cancer, endometriosis, uterine fibroids, and precocious puberty.
Claims1
A cyclic peptide antagonist of LHRH or a pharmaceutically acceptable salt thereof selected from the group consisting of:
- AcD2Nal-D4ClPhe-c-{DLys-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopro pyl)-Pro-DGlu}-NH.sub.2 ;
- AcD2Nal-D4ClPhe-c-{DLys-Ser-Tyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopropyl )-Pro-Glu}-NH.sub.2 ;
- AcD2Nal-D4ClPhe-c-{Lys-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isoprop yl)-Pro-DGlu}-NH.sub.2 ;
- AcD2Nal-D4ClPhe-c-{DLys-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopro pyl)-Pro-Glu}-NH.sub.2 ;
- AcD2Nal-D4ClPhe-c-{Lys-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isoprop yl)-Pro-Glu}-NH.sub.2 ;
- AcD2Nal-D4ClPhe-c-{Glu-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isoprop yl)-Pro-DOrn}-NH.sub.2 ;
- AcD2Nal-D4ClPhe-c-{DGlu-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopro pyl)-Pro-DLys}-NH.sub.2 ;
- AcD2Nal-D4ClPhe-c-{DLys-Ser-Tyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopropyl )-Pro-DGlu}-NH.sub.2 ;
- 4F-Phenylacetyl-c-{DLys-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopro pyl)-Pro-DGlu}-NH.sub.2 ;
- Ac-c-{DGlu-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopropyl)-Pro-DLys }-NH.sub.2 ;
- AcD2Nal-D4ClPhe-c-{DGlu-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopro pyl)-Pro-DGlu}-NH.sub.2 ;
- 4-ClPhenylpropionyl-c-{DLys-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Is opropyl)-Pro-DGlu}-NH.sub.2 ;
- AcD2Nal-D4ClPhe-c-{DOrn-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopro pyl)-Pro-DGlu}-NH.sub.2 ;
- 4Cl-Phenylpropionyl-c-{DLys-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Is opropyl)-Gly-DGlu}-NH.sub.2 ;
- AcD2Nal-D4ClPhe-c-{DLys-Gly-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopro pyl)-Gly-DGlu}-NH.sub.2 ;
- Ac-c-{DLys-Ser-NMeTyr-DLys(Nicotinyl)-Leu-Lys(N-epsilon-Isopropyl)-Pro-DGlu }-NH.sub.2.
13 more elements
Dependencies are inferred from the claim text.