C07D417/06

TRICYCLIC SULFONES AS ROR GAMMA MODULATORS

There are described RORγ modulators of the formula (I),

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and formula (II)

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or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

TRICYCLIC SULFONES AS ROR GAMMA MODULATORS

There are described RORγ modulators of the formula (I),

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and formula (II)

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or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

COMPOSITIONS OF FATOSTATIN BASED HETEROCYCLIC COMPOUNDS AND USES THEREOF
20180000801 · 2018-01-04 ·

The present invention relates to compounds, pharmaceutical compositions and formulations that have a structure (I). The compounds comprise a heterocyclic ring where W, X, Y, and Z generally and independently are S, N or C with the proviso that at least 2 of these positions in the ring are other than carbon. A pyridine or a substituted pyridine A ring and a phenyl or a substituted phenyl B ring are covalently bonded to the heterocyclic ring. Further provided are methods for treating a metabolic disorder, cell proliferative disease, reducing body weight or increasing thermogenesis during weight loss with the compounds of structure as described or pharmaceutically acceptable salt or stereoisomer thereof or both.

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METHODS AND AGENTS FOR TREATING DISEASE

The present invention provides compounds having the general structural formula (I) [formula should be inserted here] and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving elevated levels of aldosterone or abnormal or excessive fibrosis, such as kidney disease and hypertension.

METHODS AND AGENTS FOR TREATING DISEASE

The present invention provides compounds having the general structural formula (I) [formula should be inserted here] and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving elevated levels of aldosterone or abnormal or excessive fibrosis, such as kidney disease and hypertension.

Fungicidal oxadiazoles

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R.sup.1, L and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. ##STR00001##

SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF

The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.

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SMALL MOLECULE ENHANCEMENT OF 20S PROTEASOME ACTIVITY TARGETS INTRINSICALLY DISORDERED PROTEINS

The disclosure is directed to compounds of the formula (I) and (II) and uses of such compounds to treat, among other conditions, neurodegenerative diseases and cancers.

SMALL MOLECULE ENHANCEMENT OF 20S PROTEASOME ACTIVITY TARGETS INTRINSICALLY DISORDERED PROTEINS

The disclosure is directed to compounds of the formula (I) and (II) and uses of such compounds to treat, among other conditions, neurodegenerative diseases and cancers.

IMINO SULFANONE INHIBITORS OF ENPP1

The present disclosure relates generally to inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions thereof, and methods of using said compounds and compositions thereof. More specifically, the present disclosure relates to sulfoximine-based inhibitors of ENPP1 and methods of their use for treating disease mediated by ENPP1.