Patent classifications
C07C235/64
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 cyclic and heterocyclic anilide rings and their synthetic precursors, and mono-, di-, or multi-substituted N-heterocyclic rings, R-isomers, non-hydroxylated and/or non-chiral propanamides in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, 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.
STAT3 TRANSCRIPTION FACTOR INHIBITORS AND METHODS OF USING THE SAME
Compounds that inhibit the activity of Signal transducer and activator of transcription 3 (STAT3), or pharmaceutically acceptable salts or prodrugs thereof, and methods of using these compounds to treat cancer and other diseases.
STAT3 TRANSCRIPTION FACTOR INHIBITORS AND METHODS OF USING THE SAME
Compounds that inhibit the activity of Signal transducer and activator of transcription 3 (STAT3), or pharmaceutically acceptable salts or prodrugs thereof, and methods of using these compounds to treat cancer and other diseases.
Albicidin derivatives, their use and synthesis
A chemical compound is provided according to general formula (1): ##STR00001##
Albicidin derivatives, their use and synthesis
A chemical compound is provided according to general formula (1): ##STR00001##
STABLE HEAVY ISOTOPES IN AMIDE FUNCTIONAL GROUPS AND USES THEREOF
There are provided isotope-enriched compounds containing stable heavy isotope-enriched amide functional groups for modulating the pharmacokinetic profile, metabolic profile, and/or delivery efficiency of a drug or prodrug, as well as its therapeutic or prophylactic efficacy and/or adverse effects. Use of the isotope-enriched amide-containing drugs and prodrugs for the treatment or prevention of disease states and conditions is also provided.
##STR00001##
CARBOXAMIDES AS MODULATORS OF SODIUM CHANNELS
Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
CARBOXAMIDES AS MODULATORS OF SODIUM CHANNELS
Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
2,5- OR 2,6-DISUBSTITUTED HYDROQUINONE DERIVATIVES WITH AT LEAST ONE CARBOXY, SULFO OR AMIDO GROUP USEFUL AS MEDICAMENTS
The present invention provides novel hydroquinone derivatives of formula (I), processes of preparation, as well as pharmaceutical compositions and methods of treating and/or preventing e.g. autoimmune, immunological, rheumatology, vascular disorders, ophthalmologic disorders, fibrotic disorders, metabolic and gastrointestinal disorders, neuroinflammatory and neurodegenerative diseases, neoplasms and cancer associated disorders, hormone related diseases and immunological disorders resulting from viral and bacterial infectious diseases and complications thereof. wherein R.sub.1 is COOR.sub.4, (CH.sub.2)nCOOR.sub.4, SO.sub.3H, (CH.sub.2)nSO.sub.3H or CONH—R.sub.10; one of R.sub.2 and R.sub.3 is H and the other is R.sub.5.
##STR00001##
2,5- OR 2,6-DISUBSTITUTED HYDROQUINONE DERIVATIVES WITH AT LEAST ONE CARBOXY, SULFO OR AMIDO GROUP USEFUL AS MEDICAMENTS
The present invention provides novel hydroquinone derivatives of formula (I), processes of preparation, as well as pharmaceutical compositions and methods of treating and/or preventing e.g. autoimmune, immunological, rheumatology, vascular disorders, ophthalmologic disorders, fibrotic disorders, metabolic and gastrointestinal disorders, neuroinflammatory and neurodegenerative diseases, neoplasms and cancer associated disorders, hormone related diseases and immunological disorders resulting from viral and bacterial infectious diseases and complications thereof. wherein R.sub.1 is COOR.sub.4, (CH.sub.2)nCOOR.sub.4, SO.sub.3H, (CH.sub.2)nSO.sub.3H or CONH—R.sub.10; one of R.sub.2 and R.sub.3 is H and the other is R.sub.5.
##STR00001##