C07D207/08

COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES

The present disclosure relates to novel compounds, pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurodegerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed.

Inhibitors of the N-terminal domain of the androgen receptor

The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.

Inhibitors of the N-terminal domain of the androgen receptor

The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.

Fluorene derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition comprising same as effective ingredient for preventing or treating HCV-related disease

The present invention relates to a fluorene derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition comprising the same as an effective ingredient for preventing or treating HCV-related disease. A fluorene derivative according to the present invention is identified to exhibit an antiviral performance against not only HCV, but also highly against HCV mutants, particularly double mutants and thus can be used in a pharmaceutical composition for prevention or treatment of HCV-caused liver disease, such as acute hepatitis C, chronic hepatitis C, liver cirrhosis, hepatocellular cancer, etc., particularly, liver disease caused by mutants of HCV. The derivative can be useful in a pharmaceutical composition for prevention or treatment of HCV-related liver disease by which the problem of resistant mutation against conventional therapeutic agents is solved.

Drug-conjugates, conjugation methods, and uses thereof

In certain aspects, compounds and uses thereof are provided. In certain aspects, compound-conjugates and uses thereof are provided.

Drug-conjugates, conjugation methods, and uses thereof

In certain aspects, compounds and uses thereof are provided. In certain aspects, compound-conjugates and uses thereof are provided.

Necrosis Inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives

Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology use.

Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives

Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology use.

GLP-1 receptor modulators

Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “custom character” represents either or both the R and S form of the compound): ##STR00001##
where A, B, C, Y.sub.1, Y.sub.2, Z, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, W.sub.1, n, p and q are as defined herein.