C07K11/00

VERTICILIDE ENANTIOMER AND METHODS OF INHIBITING CARDIAC RYANODINE RECEPTOR-MEDIATED INTRACELLULAR CALCIUM RELEASE

The non-natural enantiomer (ent-(+)-verticilide) and uses for treatment of RyR2-mediated spontaneous Ca.sup.2+ leak, arrhythmia and memory loss.

Process for the preparation of cyclic depsipeptides

Processes for preparing compounds of Formula (1) and Formula (2) are described, wherein X, Y, Z, R.sub.1-R.sub.7, L and n are defined herein. Intermediates useful in the preparation of the compounds of Formula (1) and Formula (2) are also described. ##STR00001##

Process for the preparation of cyclic depsipeptides

Processes for preparing compounds of Formula (1) and Formula (2) are described, wherein X, Y, Z, R.sub.1-R.sub.7, L and n are defined herein. Intermediates useful in the preparation of the compounds of Formula (1) and Formula (2) are also described. ##STR00001##

PEPTIDES AND NEMATICIDAL COMPOSITIONS
20200123208 · 2020-04-23 ·

Peptides, nematicidal compositions, transgenic microorganisms for expressing the peptides and methods of treating plant parasitic nematodes, the method comprising providing either a peptide or a nematicidal composition or a transgenic microorganism for expressing the peptide on or adjacent the plant parasitic nematodes.

PEPTIDES AND NEMATICIDAL COMPOSITIONS
20200123208 · 2020-04-23 ·

Peptides, nematicidal compositions, transgenic microorganisms for expressing the peptides and methods of treating plant parasitic nematodes, the method comprising providing either a peptide or a nematicidal composition or a transgenic microorganism for expressing the peptide on or adjacent the plant parasitic nematodes.

NOVEL PEPTIDIC LINKERS AND CRYPTOPHYCIN CONJUGATES, THEIR PREPARATION AND THEIR THERAPEUTIC USE
20200093934 · 2020-03-26 ·

The present disclosure relates to compounds of formula (I): RCG1-L-P (I) wherein RCG1 represents a reactive chemical group being reactive towards a chemical group present on a polypeptide such as an antibody; P represents H, OH or an activated O; and L represents a specific linker. The disclosure also relates to cryptophycin payloads, as well as to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these conjugates.

NOVEL PEPTIDIC LINKERS AND CRYPTOPHYCIN CONJUGATES, THEIR PREPARATION AND THEIR THERAPEUTIC USE
20200093934 · 2020-03-26 ·

The present disclosure relates to compounds of formula (I): RCG1-L-P (I) wherein RCG1 represents a reactive chemical group being reactive towards a chemical group present on a polypeptide such as an antibody; P represents H, OH or an activated O; and L represents a specific linker. The disclosure also relates to cryptophycin payloads, as well as to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these conjugates.

TAILORED CYCLODEPSIPEPTIDES AS POTENT NON-COVALENT SERINE PROTEASE INHIBITORS

The present invention pertains to an improved chemical synthesis method for Ahp-cyclodepsipeptides which allows straight forward and easy synthesis of tailor-made Ahp-cyclodepsipeptides. The invention further provides Ahp-cyclodepsipeptides for use as HTRA protease inhibitors and their medical use.

NOVEL PAENIBACILLUS STRAIN, ANTIFUNGAL COMPOUNDS, AND METHODS FOR THEIR USE

The present invention relates to a composition comprising a biologically pure culture of a fungicidal Paenibacillus sp. strain comprising a variant fusaricidin synthetase lacking a functional adenylation domain in the third module. The present invention also provides a composition comprising a biologically pure culture of a fungicidal Paenibacillus sp. strain or a cell-free extract thereof comprising at least one Paeniserine and at least one Paeniprolixin. Also provided are isolated compounds and methods of treating a plant to control a plant disease with the disclosed compositions and compounds.

NOVEL PEPTIDIC LINKERS AND CRYPTOPHYCIN CONJUGATES, THEIR PREPARATION AND THEIR THERAPEUTIC USE
20200054760 · 2020-02-20 ·

The present disclosure relates to compounds of formula (I):


RCG1-L-P(I)

wherein RCG1 represents a reactive chemical group being reactive towards a chemical group present on a polypeptide such as an antibody; P represents H, OH or an activated O; and L represents a specific linker. The disclosure also relates to cryptophycin payloads, as well as to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these conjugates.