Patent classifications
C07K11/02
BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR EPHA2
The present invention relates to polypeptides which are covalently bound to non-aromatic molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of the Eph receptor tyrosine kinase A2 (EphA2). The invention also relates to pharmaceutical compositions comprising said peptide ligands and to the use of said peptide ligands in preventing, suppressing or treating a disease or disorder characterised by overexpression of EphA2 in diseased tissue (such as a tumour).
A TEIXOBACTIN ANALOGUE AND USE THEREOF
Pharmaceuticals, and specifically a Teixobactin analogue and use thereof. A pharmaceutical composition having the compound and use of the compound and the pharmaceutical composition thereof inhibits the growth and/or reproduction of Gram-positive bacteria or Mycobacterium tuberculosis. A compound has Formula (Ia) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof,
##STR00001##
A TEIXOBACTIN ANALOGUE AND USE THEREOF
Pharmaceuticals, and specifically a Teixobactin analogue and use thereof. A pharmaceutical composition having the compound and use of the compound and the pharmaceutical composition thereof inhibits the growth and/or reproduction of Gram-positive bacteria or Mycobacterium tuberculosis. A compound has Formula (Ia) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof,
##STR00001##
Endoparasitic Depsipeptides
The present invention provides cyclic depsipeptides of Formula (1), stereoisomers thereof, and veterinary acceptable salts thereof
##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, L.sub.1, and L.sub.2, are as defined herein. The present invention also contemplates compositions and methods of treatment as an endoparasiticide with a Formula (1) compound.
Endoparasitic Depsipeptides
The present invention provides cyclic depsipeptides of Formula (1), stereoisomers thereof, and veterinary acceptable salts thereof
##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, L.sub.1, and L.sub.2, are as defined herein. The present invention also contemplates compositions and methods of treatment as an endoparasiticide with a Formula (1) compound.
Anthelmintic depsipeptide compounds
The present invention provides cyclic depsipeptide compounds of formula (I) wherein the stereochemical configuration of at least one carbon atom bearing the groups Cy.sup.1, Cy.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.a and R.sup.b is inverted compared with the naturally occurring cyclic depsipeptide PF1022A. The invention also provides compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.
Anthelmintic depsipeptide compounds
The present invention provides cyclic depsipeptide compounds of formula (I) wherein the stereochemical configuration of at least one carbon atom bearing the groups Cy.sup.1, Cy.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.a and R.sup.b is inverted compared with the naturally occurring cyclic depsipeptide PF1022A. The invention also provides compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.
HETEROTANDEM BICYCLIC PEPTIDE COMPLEX
The present invention relates to a heterotandem bicyclic peptide complex which comprises a first peptide ligand, which binds to Nectin-4, conjugated via a linker to two second peptide ligands, which bind to CD137. The invention also relates to the use of said heterotandem bicyclic peptide complex in preventing, suppressing or treating cancer.
HETEROTANDEM BICYCLIC PEPTIDE COMPLEXES
The present invention relates to a heterotandem bicyclic peptide complex which comprises a first peptide ligand, which binds to EphA2, conjugated via a linker to two second peptide ligands, which bind to CD137. The invention also relates to the use of said heterotandem bicyclic peptide complex in preventing, suppressing or treating cancer.
Creation of peptide-based anti-tumor agent
An object of the present invention is to provide an echinomycin derivative that has anti-cancer activity equal to or greater than that of echinomycin, and a production method therefor based on a chemical procedure. Provided are an echinomycin derivative represented by formula (I), and a production method therefor based on a chemical procedure.