C07D409/06

Aryl hydrocarbon receptor modulators and uses thereof

Provided are compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, stereoisomers, tautomers, isotopically labeled derivatives, polymorphs, and prodrugs thereof, wherein X.sup.1-X.sup.4, R.sup.X, R.sup.C, R.sup.B, n, and Ring A are as defined herein. The compounds may be aryl hydrocarbon receptor agonists or partial aryl hydrocarbon receptor agonists. Also provided are pharmaceutical compositions comprising a compound of Formula (I) and methods of using such compounds for treating diseases and conditions related to the activity of an aryl hydrocarbon receptor, such as, for example, inflammatory diseases, autoimmune diseases, metabolic disorders, and proliferative diseases. ##STR00001##

Organic electro-optic chromophores

Chromophores with large hyperpolarizabilities, films with electro-optic activity comprising the chromophores, and electro-optic devices comprising the chromophores are disclosed.

HETEROCYCLIC AMIDES AS KINASE INHIBITORS

Disclosed are compounds having the formula:

##STR00001## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, and methods of making and using the same.

HETEROCYCLIC AMIDES AS KINASE INHIBITORS

Disclosed are compounds having the formula:

##STR00001## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, and methods of making and using the same.

OX2R Compounds

Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.

OX2R Compounds

Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.

Lymphoid-specific tyrosine phosphatase (LYP) inhibitors

The present disclosure relates to novel lymphoid-specific tyrosine phosphatase (LYP, encoded by the PTPN22 gene) inhibitors, and to methods of making and using the novel LYP inhibitors. Thus, the compounds according to the disclosure may be used for treating diseases or disorders associated with PTPN22 genetic polymorphism, including type 1 diabetes, rheumatoid arthritis, systemic lupus erythematosis, Graves' disease, Addison's disease, vitiligo, juvenile arthritis, Hashimoto thyroiditis, and other rarer diseases. Furthermore, these LYP inhibitors may be served for a novel class of cancer immunotherapy. The compounds can be injected or orally administered.

Lymphoid-specific tyrosine phosphatase (LYP) inhibitors

The present disclosure relates to novel lymphoid-specific tyrosine phosphatase (LYP, encoded by the PTPN22 gene) inhibitors, and to methods of making and using the novel LYP inhibitors. Thus, the compounds according to the disclosure may be used for treating diseases or disorders associated with PTPN22 genetic polymorphism, including type 1 diabetes, rheumatoid arthritis, systemic lupus erythematosis, Graves' disease, Addison's disease, vitiligo, juvenile arthritis, Hashimoto thyroiditis, and other rarer diseases. Furthermore, these LYP inhibitors may be served for a novel class of cancer immunotherapy. The compounds can be injected or orally administered.

SOLID SUPPORTS AND PHOSPHORAMIDITE BUILDING BLOCKS FOR OLIGONUCLEOTIDE CONJUGATES

Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.

SOLID SUPPORTS AND PHOSPHORAMIDITE BUILDING BLOCKS FOR OLIGONUCLEOTIDE CONJUGATES

Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.