Patent classifications
C07D233/68
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.
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.
SUBSTITUTED 4-AMINO-1H-IMIDAZO[4,5-c]QUINOLINE COMPOUNDS AND IMPROVED METHODS FOR THEIR PREPARATION
Improved methods and intermediates thereof for preparing substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds are described. These compounds are useful as NLRP3 modulators.
SUBSTITUTED 4-AMINO-1H-IMIDAZO[4,5-c]QUINOLINE COMPOUNDS AND IMPROVED METHODS FOR THEIR PREPARATION
Improved methods and intermediates thereof for preparing substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds are described. These compounds are useful as NLRP3 modulators.
Flexible piezoelectric and ferroelectric haloimidazole crystals
Provided herein are substituted haloimidazole crystals, the substituted haloimidazole crystal comprising a substituted haloimidazole compound wherein the substituents are selected from the group consisting of hydrogen, an alkyl, and a halogen. The substituted haloimidazole crystals may further comprise second substituted haloimidazole. The substituted haloimidazole crystals may be piezoelectric, ferroelectric, flexible, or any combination thereof. Also provided herein are methods for preparing substituted haloimidazole crystals.
Flexible piezoelectric and ferroelectric haloimidazole crystals
Provided herein are substituted haloimidazole crystals, the substituted haloimidazole crystal comprising a substituted haloimidazole compound wherein the substituents are selected from the group consisting of hydrogen, an alkyl, and a halogen. The substituted haloimidazole crystals may further comprise second substituted haloimidazole. The substituted haloimidazole crystals may be piezoelectric, ferroelectric, flexible, or any combination thereof. Also provided herein are methods for preparing substituted haloimidazole crystals.
SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF
- Jean-Christophe Andrez ,
- Paul Robert Bichler ,
- Chien-An CHEN ,
- Sultan Chowdhury ,
- Shannon Marie Decker ,
- Christoph Martin Dehnhardt ,
- Thilo Focken ,
- Michael Edward Grimwood ,
- Ivan William HEMEON ,
- Qi Jia ,
- Jun LI ,
- Zhiguo Liu ,
- Daniel F. ORTWINE ,
- Brian Salvatore Safina ,
- Daniel SUTHERLIN ,
- Tao SHENG ,
- Shaoyi Sun ,
- Andrew D. WHITE ,
- Michael Scott Wilson ,
- Alla Yurevna Zenova ,
- Jiuxiang Zhu
The invention provides compounds having the general formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables R.sup.A, R.sup.AA, subscript n, ring A, X.sup.2, L, subscript m, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.N have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Alpha-cinnamide compounds and compositions as HDAC8 inhibitors
The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
Alpha-cinnamide compounds and compositions as HDAC8 inhibitors
The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
Heterocyclic Lipoxin Analogs and Uses Thereof
The present invention relates to a compound of formula (I): wherein L is an optionally substituted heterocyclic group excluding unsubstituted monocyclic pyridine groups; wherein a is 0, 1 or 2; wherein R.sup.1 is H or with R.sup.2 is a bond; wherein R.sup.2 is an optionally substituted alkoxy or aryloxy group, or with R.sup.1 forms a bond; wherein R.sup.3 is an optionally substituted alkyl group; and wherein R.sup.4 is CH.sub.2, CMe.sub.2 or O. Such compounds may be used in the treatment or prophylaxis of a disease or condition in which inhibition of acute inflammation and/or promotion of its resolution and/or suppression of fibrosis.
##STR00001##