Patent classifications
A61K31/5375
SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
USE OF PPAR-DELTA AGONISTS IN THE TREATMENT OF DISEASE
Described herein is the use sodium (E)-2-(4-((3-(4-fluorophenyl)-3-(4-(3-morpholinoprop-1-yn-1-yl)phenyl)allyl)oxy)-2-methylphenoxy)acetate in the preparation of pharmaceutical compositions for the treatment of diseases or conditions that would benefit by administration with a PPARδ agonist compound.
USE OF PPAR-DELTA AGONISTS IN THE TREATMENT OF DISEASE
Described herein is the use sodium (E)-2-(4-((3-(4-fluorophenyl)-3-(4-(3-morpholinoprop-1-yn-1-yl)phenyl)allyl)oxy)-2-methylphenoxy)acetate in the preparation of pharmaceutical compositions for the treatment of diseases or conditions that would benefit by administration with a PPARδ agonist compound.
DOSING REGIMEN OF KRAS G12C INHIBITOR
Provided herein are methods of administering a KRAS G12C inhibitor to a cancer subject.
DOSING REGIMEN OF KRAS G12C INHIBITOR
Provided herein are methods of administering a KRAS G12C inhibitor to a cancer subject.
PEPTIDES, COMPOUNDS, COMPOSITIONS AND METHODS FOR INHIBITING SOX9
The present application provides SOX9 inhibitor compounds and compositions and methods of use thereof. In certain aspects, the SOX9 inhibitor is a peptide comprising a portion of the SOX9 dimerization motif. In other aspects, the SOX9 inhibitor is a compound of the general formula I
##STR00001##
where one A is H and the other is:
##STR00002##
and the remaining substituents are as defined in the application.
GLP-1R MODULATING COMPOUNDS
The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.
GLP-1R MODULATING COMPOUNDS
The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.
TOPICAL ANTIBIOTIC
Provided herein is a topical antibiotic composition that includes an external antibiotic agent, one or more pharmaceutically acceptable excipients, and at least one of a cannabinoid, terpene, and flavonoid. Also provided is a method that includes topically administering to a skin surface of a subject (e.g., human) the topical antibiotic composition.