C07D203/08

Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

POST-CURABLE PRESSURE-SENSITIVE ADHESIVE

The present disclosure is directed to a curable precursor of a pressure sensitive adhesive comprising: a) a (co)polymeric material comprising the reaction product of a (co)polymerizable material comprising a (meth)acrylate ester monomer; and optionally, a co-monomer having an ethylenically unsaturated group and which is different from the (meth)acrylate ester monomer; b) a polyfunctional aziridine curing agent; and c) an acid generating agent.

The present disclosure is also directed to a method of manufacturing such pressure sensitive adhesives and uses thereof.

POST-CURABLE PRESSURE-SENSITIVE ADHESIVE

The present disclosure is directed to a curable precursor of a pressure sensitive adhesive comprising: a) a (co)polymeric material comprising the reaction product of a (co)polymerizable material comprising a (meth)acrylate ester monomer; and optionally, a co-monomer having an ethylenically unsaturated group and which is different from the (meth)acrylate ester monomer; b) a polyfunctional aziridine curing agent; and c) an acid generating agent.

The present disclosure is also directed to a method of manufacturing such pressure sensitive adhesives and uses thereof.

Benzoylglycine Derivatives and Methods of Making and Using Same

Disclosed are compounds of formulae:

##STR00001##

and pharmaceutically acceptable salts thereof, wherein the variables, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, R.sub.17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds.

Benzoylglycine Derivatives and Methods of Making and Using Same

Disclosed are compounds of formulae:

##STR00001##

and pharmaceutically acceptable salts thereof, wherein the variables, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, R.sub.17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds.

NOVEL ARYL ETHENE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERR) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient.

NOVEL ARYL ETHENE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERR) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient.

NOVEL ARYL ETHENE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERR) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient.

Method and catalyst for synthesising aziridine

The present invention relates to methods of synthesizing aziridines including isotopically labelled aziridines, said methods comprising contacting an imine or one or more precursors thereof with a diazo compound in the presence of a phosphoramide or a phosphoramide-derived catalyst. The present invention also relates to aziridines, modified aziridines and aziridine-derived compounds preparable by the aforementioned methods, and to phosphoramide or phosphoramide-derived catalysts suitable for use in such methods.