C07D235/14

NOVEL SOLUBLE EPOXIDE HYDROLASE INHIBITORS AND METHOD OF USE THEREOF

Novel soluble epoxide hydrolase (sEH) inhibitors are provided, along with methods for their use. The soluble epoxide hydrolase inhibitors are useful in treating and/or preventing sEH-related related diseases, such as Alzheimer's disease and inflammation. Also provided are methods for inhibiting soluble epoxide hydrolase in a cell using the compounds and compositions described herein.

Benzimidazole derivatives and use thereof

The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: ##STR00001##
and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W.sup.1, W.sup.2, W.sup.3, W.sup.4, U, G, m, R.sup.1, and R.sup.2 are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.

Benzimidazole derivatives and use thereof

The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: ##STR00001##
and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W.sup.1, W.sup.2, W.sup.3, W.sup.4, U, G, m, R.sup.1, and R.sup.2 are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.

DERIVATIZED BENZIMIDAZOLE COMPOUNDS, THEIR SALTS, THEIR COMPLEXES, THEIR PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USING THEM FOR ANTIGERIATRIC ACTIONS

Embodiments of the present invention generally concern pharmaceutical formulations and compositions and methods for using the pharmaceutical formulations and compositions which comprise derivatives of benzimidazole compounds, their racemic mixtures, their enantiomers, their complexes, their salts, and combinations thereof which have been found to be novel agonists of imidizoline receptors with surprising life extending efficacies due to their geroprotective (anti-geriatric) actions on pathologies associated with the aging processes in humans and animals.

Labelling agent, and composition for labelling a protein, method for labelling a protein, and method for detecting a protein

Provided are a labelling agent including a compound of the following Formula 1, a labelling composition, a method of labelling a protein with the labelling agent, and a method of detecting the protein using the labelling agent: ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.8 are independently H, substituted or unsubstituted —C.sub.1-10-alkyl-, —C.sub.2-10-alkenyl, or —C.sub.2-10-alkynyl, R.sub.7 is H or —NR.sub.9R.sub.10, R.sub.9 and R.sub.10 are independently H, substituted or unsubstituted —C.sub.1-10-alkyl-, —C.sub.2-10-alkenyl, or —C.sub.2-10-alkynyl, X is —NR.sub.11, —O, or S, R.sub.11 is H, substituted or unsubstituted —C.sub.1-10-alkyl-, —C.sub.2-10-alkenyl, or —C.sub.2-10-alkynyl, Y is —OR.sub.12 or —NR.sub.13R.sub.14, R.sub.12 is H, substituted or unsubstituted —C.sub.1-10-alkyl-, —C.sub.2-10-alkenyl, or —C.sub.2-10-alkynyl, and R.sub.13 and R.sub.14 are independently H, substituted or unsubstituted —C.sub.1-10-alkyl-, —C.sub.2-10-alkenyl, or —C.sub.2-10-alkynyl.

Labelling agent, and composition for labelling a protein, method for labelling a protein, and method for detecting a protein

Provided are a labelling agent including a compound of the following Formula 1, a labelling composition, a method of labelling a protein with the labelling agent, and a method of detecting the protein using the labelling agent: ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.8 are independently H, substituted or unsubstituted —C.sub.1-10-alkyl-, —C.sub.2-10-alkenyl, or —C.sub.2-10-alkynyl, R.sub.7 is H or —NR.sub.9R.sub.10, R.sub.9 and R.sub.10 are independently H, substituted or unsubstituted —C.sub.1-10-alkyl-, —C.sub.2-10-alkenyl, or —C.sub.2-10-alkynyl, X is —NR.sub.11, —O, or S, R.sub.11 is H, substituted or unsubstituted —C.sub.1-10-alkyl-, —C.sub.2-10-alkenyl, or —C.sub.2-10-alkynyl, Y is —OR.sub.12 or —NR.sub.13R.sub.14, R.sub.12 is H, substituted or unsubstituted —C.sub.1-10-alkyl-, —C.sub.2-10-alkenyl, or —C.sub.2-10-alkynyl, and R.sub.13 and R.sub.14 are independently H, substituted or unsubstituted —C.sub.1-10-alkyl-, —C.sub.2-10-alkenyl, or —C.sub.2-10-alkynyl.

PEPTIDOMIMETIC PROTEASOME INHIBITORS

The compounds of the present invention are represented by the following compounds having Formula (I) and Formula (I′):

##STR00001##

where the substituents R, R.sup.1, R.sup.3, R.sup.4, R, W, X, Y, Z, k, and m are as defined herein and

##STR00002##

where the substituents R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, Y, Z, and m are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.

PEPTIDOMIMETIC PROTEASOME INHIBITORS

The compounds of the present invention are represented by the following compounds having Formula (I) and Formula (I′):

##STR00001##

where the substituents R, R.sup.1, R.sup.3, R.sup.4, R, W, X, Y, Z, k, and m are as defined herein and

##STR00002##

where the substituents R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, Y, Z, and m are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.

Benzo five-membered nitrogen heterocyclic piperidine or piperazine derivatives and preparation methods and pharmaceutical compositions thereof

Compounds of formula (I) and its pharmaceutically acceptable salts are described ##STR00001##
wherein R.sub.1, R.sub.2, X, Y, A, B are as defined in the specification. Also disclosed are methods for preparing the compounds of formula (I) or pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the compounds of formula (I) or pharmaceutically acceptable salts thereof.

Benzo five-membered nitrogen heterocyclic piperidine or piperazine derivatives and preparation methods and pharmaceutical compositions thereof

Compounds of formula (I) and its pharmaceutically acceptable salts are described ##STR00001##
wherein R.sub.1, R.sub.2, X, Y, A, B are as defined in the specification. Also disclosed are methods for preparing the compounds of formula (I) or pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the compounds of formula (I) or pharmaceutically acceptable salts thereof.