Glutamine antagonists and their use for treating oncological, immunological, and neurological diseases are disclosed. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder, the method comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof. Also disclosed are methods of enhancing the effects of an immune checkpoint inhibitor, enabling a subject to respond to an immune checkpoint inhibitor, or enabling the toxicity or the dose or number of treatments with an immune checkpoint inhibitor to be reduced, comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof, and an immune checkpoint inhibitor. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder that is refractory to checkpoint inhibitor therapy, the method comprising administering to a subject in need thereof, and having the refractory disease or disorder, a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof.

Glutamine antagonists and their use for treating oncological, immunological, and neurological diseases are disclosed. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder, the method comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof. Also disclosed are methods of enhancing the effects of an immune checkpoint inhibitor, enabling a subject to respond to an immune checkpoint inhibitor, or enabling the toxicity or the dose or number of treatments with an immune checkpoint inhibitor to be reduced, comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof, and an immune checkpoint inhibitor. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder that is refractory to checkpoint inhibitor therapy, the method comprising administering to a subject in need thereof, and having the refractory disease or disorder, a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof.

The present invention provides a new building block for peptide synthesis, which introduces a cleavage site that can be used to generate cleavable fragments subsequent to a peptide sequence.

The present invention provides a new building block for peptide synthesis, which introduces a cleavage site that can be used to generate cleavable fragments subsequent to a peptide sequence.

The invention relates to an aqueous coating composition comprising a compound having reactive groups A, and a quaternary ammonium compound according to Formula I, II or III

##STR00001## wherein R.sup.1 is an alkyl, alkenyl, alkylaryl or arylalkyl group having from 5 to 50 carbon atoms; R.sup.2 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.3 and R.sup.4 are alkylene groups having from 1 to 4 carbon atoms; R.sup.5 and R.sup.6 are H or C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.7 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.8 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.9 is H or a methyl group; Z is a substituent containing at least one reactive group B which is capable of reacting with the reactive group A; X.sup.− is an anion; y is 0 or 1; a is 0 or 1; and the sum of y and a is 1 or 2 and m is an integer from 1 to 30, preferably between 1 and 10, or between 2 and 6 n is an integer from 0-30, preferably between 1 and 10, or 2 and 6 T is a monomer unit; U is a monomer unit; V is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing hetero atoms; d is an integer between 1 and 5, preferably 1; e is an integer between 1 and 1000, preferably between 5 and 100; g is an integer between 1 and 100, preferably between 2 and 10; h is an integer between 1 and 5, preferably 2 or 3.

The invention relates to an aqueous coating composition comprising a compound having reactive groups A, and a quaternary ammonium compound according to Formula I, II or III

##STR00001## wherein R.sup.1 is an alkyl, alkenyl, alkylaryl or arylalkyl group having from 5 to 50 carbon atoms; R.sup.2 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.3 and R.sup.4 are alkylene groups having from 1 to 4 carbon atoms; R.sup.5 and R.sup.6 are H or C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.7 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.8 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.9 is H or a methyl group; Z is a substituent containing at least one reactive group B which is capable of reacting with the reactive group A; X.sup.− is an anion; y is 0 or 1; a is 0 or 1; and the sum of y and a is 1 or 2 and m is an integer from 1 to 30, preferably between 1 and 10, or between 2 and 6 n is an integer from 0-30, preferably between 1 and 10, or 2 and 6 T is a monomer unit; U is a monomer unit; V is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing hetero atoms; d is an integer between 1 and 5, preferably 1; e is an integer between 1 and 1000, preferably between 5 and 100; g is an integer between 1 and 100, preferably between 2 and 10; h is an integer between 1 and 5, preferably 2 or 3.

This disclosure relates to picolinamides of Formula I and their use as fungicides.

##STR00001##

This disclosure relates to picolinamides of Formula I and their use as fungicides.

##STR00001##

A fungicidal 4-methoxy-3-acetyloxypicolinamide may be conveniently prepared in processes that include the coupling together of 4-methoxy-3-acetyloxypicolinic acid or 4-methoxy-3-hydroxypicolinic acid with a key 2-aminopropanoate ester derived from a 1,1-bis(4-fluorophenyl)propane-1,2-diol.

A fungicidal 4-methoxy-3-acetyloxypicolinamide may be conveniently prepared in processes that include the coupling together of 4-methoxy-3-acetyloxypicolinic acid or 4-methoxy-3-hydroxypicolinic acid with a key 2-aminopropanoate ester derived from a 1,1-bis(4-fluorophenyl)propane-1,2-diol.