C07K5/0212

METHOD OF MAKING PRODRUGS AND TARGETED THERAPEUTIC COMPOUNDS

Provided is a method for making the compound of Formula 1. Various compounds utilized in that method are also provided, as are methods of making those compounds. Also provided is a compound having the formula XO—CO—(CH.sub.2).sub.nNH.sub.2, where n is an integer greater than 2. A method of making that compound is additionally provided. Further provided is a method of making a prodrug of a bioactive compound.

Antimicrobial peptidomimetics

The present invention relates to peptidomimetics of the formula (I) or (I)c wherein L.sub.1, L.sub.2, L.sub.3, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, m, Q, X, Z.sub.1 and Z.sub.2 are defined as mentioned in the description and to salts and solvates of each of these compounds and to processes for the preparation thereof, compositions containing them and the uses of such compounds. It has been found that the compounds have a high microbicide activity and are suited to combat resistant bacteria, such as meticillin-resistant Staphylococcus aureus (MRSA) strains, at very low concentrations.

Cholecystokinin 2 receptor targeted NIR imaging and use thereof

Compounds are described herein where CCK2R targeting ligands are attached to an imaging agent through a linker. The compounds can be used in the detection, diagnosis, imaging and treatment of cancer.

Tubulysin derivatives

Novel tubulysin derivatives which may be useful as cytotoxic agents to provide therapeutic benefits in the treatment of various types of cancers, alone, as drug conjugates or in combination with other chemotherapies are provided.

ANTIMICROBIAL PEPTIDOMIMETICS
20180354989 · 2018-12-13 ·

The present invention relates to peptidomimetics of the formula (I) or (I)c wherein L.sub.1, L.sub.2, L.sub.3, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, m, Q, X, Z.sub.1 and Z.sub.2 are defined as mentioned in the description and to salts and solvates of each of these compounds and to processes for the preparation thereof, compositions containing them and the uses of such compounds. It has been found that the compounds have a high microbicide activity and are suited to combat resistant bacteria, such as meticillin-resistant Staphylococcus aureus (MRSA) strains, at very low concentrations.

Antimicrobial peptidomimetics

The present invention relates to peptidomimetics of the formula (I) or (I)c wherein L.sub.1, L.sub.2, L.sub.3, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, m, Q, X, Z.sub.1 and Z.sub.2 are defined as mentioned in the description and to salts and solvates of each of these compounds and to processes for the preparation thereof, compositions containing them and the uses of such compounds. It has been found that the compounds have a high microbicide activity and are suited to combat resistant bacteria, such as meticillin-resistant Staphylococcus aureus (MRSA) strains, at very low concentrations. ##STR00001##

CHOLECYSTOKININ 2 RECEPTOR TARGETED NIR IMAGING AND USE THEREOF
20180071408 · 2018-03-15 ·

Compounds are described herein where CCK2R targeting ligands are attached to an imaging agent through a linker. The compounds can be used in the detection, diagnosis, imaging and treatment of cancer.