Patent classifications
C07D273/00
Dipeptide mimics, libraries combining two dipeptide mimics with a third group, and methods for production thereof
Monovalent compounds having moieties comprising at least one amino acid side chain are bound to a core molecule, which also comprises a nucleophilic moiety bound to said core molecule. Monovalent compounds also comprise a macrocyclic ring, a nucleophilic moiety, and a spacer group. Monovalent compounds may be combined into bivalent and trivalent compounds, some of which may have a labeling tag. Methods of production of bivalent compounds and contemplated uses thereof are disclosed.
Dipeptide mimics, libraries combining two dipeptide mimics with a third group, and methods for production thereof
Monovalent compounds having moieties comprising at least one amino acid side chain are bound to a core molecule, which also comprises a nucleophilic moiety bound to said core molecule. Monovalent compounds also comprise a macrocyclic ring, a nucleophilic moiety, and a spacer group. Monovalent compounds may be combined into bivalent and trivalent compounds, some of which may have a labeling tag. Methods of production of bivalent compounds and contemplated uses thereof are disclosed.
ANTHELMINTIC DEPSIPEPTIDE COMPOUNDS
The present invention provides cyclic depsipeptide compounds of formula (I) and 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) and 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) and 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.
GUANINE-RICH OLIGONUCLEOTIDES
This invention relates to methods for oligonucleotide synthesis, specifically the synthesis of oligonucleotides that contain a high content of guanine monomers. In more detail, the invention relates to a method for coupling a nucleoside phosphoramidite during the synthesis of an oligonucleotide to a universal support, to a first nucleoside, or to an extending oligonucleotide.
GUANINE-RICH OLIGONUCLEOTIDES
This invention relates to methods for oligonucleotide synthesis, specifically the synthesis of oligonucleotides that contain a high content of guanine monomers. In more detail, the invention relates to a method for coupling a nucleoside phosphoramidite during the synthesis of an oligonucleotide to a universal support, to a first nucleoside, or to an extending oligonucleotide.
Conjugated lipomers and uses thereof
The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as conjugated lipomers or lipomers) containing one or more groups of the formula (iii): ##STR00001##
wherein R.sup.3 and R.sup.4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.
Conjugated lipomers and uses thereof
The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as conjugated lipomers or lipomers) containing one or more groups of the formula (iii): ##STR00001##
wherein R.sup.3 and R.sup.4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.
Macrocycles comprising a 4-amido-2,4-pentadienoate moiety for the treatment of hypoxic cancers
The present disclosure provides macrocyclic compounds comprising a 4-amido-2,4-pentadienoate (APD) moiety. The compounds exhibit toxicity that is selective to the hypoxic micro-environments often found in cancerous tissues. The disclosed compounds are therefore suitable for treatment of hypoxic cancer cells.