Patent classifications
A61K31/517
Use of RNAI Inhibiting PARP Activity for the Manufacture of a Medicament for the Treatment of Cancer
The present invention relates to the use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination.
Use of RNAI Inhibiting PARP Activity for the Manufacture of a Medicament for the Treatment of Cancer
The present invention relates to the use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination.
TRICYCLIC HETEROCYCLES AS ANTICANCER AGENTS
Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne. The compounds are of the following and similar genera:
##STR00001##
in which Het is an aromatic heterocyclic ring and Y is a point of attachment of various side chains and rings. An example of such a compound is 4-chloro-N-(3-(10,11-dihydro-5H-benzo[b]pyrido[2,3-f]azepin-5-yl)propyl)benzenesulfonamide:
##STR00002##
TRICYCLIC HETEROCYCLES AS ANTICANCER AGENTS
Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne. The compounds are of the following and similar genera:
##STR00001##
in which Het is an aromatic heterocyclic ring and Y is a point of attachment of various side chains and rings. An example of such a compound is 4-chloro-N-(3-(10,11-dihydro-5H-benzo[b]pyrido[2,3-f]azepin-5-yl)propyl)benzenesulfonamide:
##STR00002##
TRICYCLIC HETEROCYCLES AS ANTICANCER AGENTS
Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne. The compounds are of the following and similar genera:
##STR00001##
in which Het is an aromatic heterocyclic ring and Y is a point of attachment of various side chains and rings. An example of such a compound is 4-chloro-N-(3-(10,11-dihydro-5H-benzo[b]pyrido[2,3-f]azepin-5-yl)propyl)benzenesulfonamide:
##STR00002##
METHODS OF TREATING UROTHELIAL CARCINOMA
Methods and compositions for treating a urothelial and/or a micropapillary carcinoma, such as a micropapillary urothelial carcinoma are disclosed.
METHODS OF TREATING UROTHELIAL CARCINOMA
Methods and compositions for treating a urothelial and/or a micropapillary carcinoma, such as a micropapillary urothelial carcinoma are disclosed.
Tetrazolones as a Carboxylic Acid Bioisosteres
The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
BICYCLIC COMPOUND
Provided is a bicyclic compound having an acetyl-CoA carboxylase inhibitory action. A compound represented by the formula:
##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an acetyl-CoA carboxylase inhibitory action, is useful for the prophylaxis or treatment of cancer, inflammatory diseases and the like, and has superior efficacy.
METHODS FOR INHIBITING ALPHA-V BETA-3 EXPRESSION ON CANCER STEM CELLS AND INHIBITING PROGRESSION TO A CANCER STEM CELL PHENOTYPE
In alternative embodiments, provided are compositions and methods for treating, enhancing the drug sensitivity of, and preventing the formation of cancer stems cells, including preventing or slowing the development or generation of a beta-3 (β3)-expressing, or integrin β3 (ITG-B3)-expressing cancer or tumor cells. In alternative embodiments, provided are methods using histone acetyl transferase inhibitors and/or histone methyl transferase inhibitors to determine therapeutic values in cancer cells that induce an integrin β3 (ITGB3) polypeptide expression. In alternative embodiments, provided are kits, blister packages, lidded blisters or a blister card or packet, clamshells, trays or shrink wraps, comprising at least one compound, composition or formulation used to practice a method as provided herein, and at least one Growth Factor Inhibitor.