A61K31/4192

Methods of treating eye diseases associated with inflammation and vascular proliferation
11583535 · 2023-02-21 · ·

Methods for treating eye diseases associated with inflammation and/or vascular proliferation in subjects are disclosed. The methods include administering therapeutically effective amounts of a tranilast compound, in particular (E)-2-[[3-(3-Methoxy-4-propargyloxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid or (E)-2-[[3,4-Bis(difluoromethoxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid or pharmaceutically acceptable salts or solvates thereof.

Methods of treating eye diseases associated with inflammation and vascular proliferation
11583535 · 2023-02-21 · ·

Methods for treating eye diseases associated with inflammation and/or vascular proliferation in subjects are disclosed. The methods include administering therapeutically effective amounts of a tranilast compound, in particular (E)-2-[[3-(3-Methoxy-4-propargyloxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid or (E)-2-[[3,4-Bis(difluoromethoxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid or pharmaceutically acceptable salts or solvates thereof.

METHOD FOR TREATMENT OF PANCREATITIS

A composition for preventing and/or treating pancreatitis and a method of prevention and/or treatment of pancreatitis are disclosed. The composition include an aryl ethene compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, as an active ingredient. Also disclosed is a use of the aryl ethene compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, in manufacturing a medicament for preventing and/or treating pancreatitis or for treating one or more symptoms of pancreatitis in a patient. The method of prevention and/or treatment of pancreatitis includes administering the aryl ethene compound, an isomer, a pharmaceutically acceptable salt thereof, or a solvate thereof, in an effective amount to a subject in need thereof.

PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF INFLAMMATORY DISEASES COMPRISING NAPHTHOQUINONE DERIVATIVE
20220354825 · 2022-11-10 · ·

Provided is a method for the prevention or treatment of inflammatory diseases using a naphthoquinone or benzoindazole compound which increases the ratio of NAD.sup.+ and NAD.sup.+/NADH through activity in NQO1 in vivo, and through this, activates mitochondria, thereby inducing the metabolism of macrophages towards mitochondrial OXPHOS, which is the major metabolic pathway of M2 phenotype macrophages, such that the macrophages are polarized into an anti-inflammatory macrophage M2 phenotype, and consequently is able to inhibit the expression and activity of inflammatory cytokines, or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, diasteromer, tautomer, or prodrug thereof.

PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF INFLAMMATORY DISEASES COMPRISING NAPHTHOQUINONE DERIVATIVE
20220354825 · 2022-11-10 · ·

Provided is a method for the prevention or treatment of inflammatory diseases using a naphthoquinone or benzoindazole compound which increases the ratio of NAD.sup.+ and NAD.sup.+/NADH through activity in NQO1 in vivo, and through this, activates mitochondria, thereby inducing the metabolism of macrophages towards mitochondrial OXPHOS, which is the major metabolic pathway of M2 phenotype macrophages, such that the macrophages are polarized into an anti-inflammatory macrophage M2 phenotype, and consequently is able to inhibit the expression and activity of inflammatory cytokines, or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, diasteromer, tautomer, or prodrug thereof.

SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/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 provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

Amide derivatives useful in the treatment of HBV infection or HBV-induced diseases

The application relates to amide derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their uses, more particularly their uses in treating chronic hepatitis B virus (HBV) infection: ##STR00001##

Amide derivatives useful in the treatment of HBV infection or HBV-induced diseases

The application relates to amide derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their uses, more particularly their uses in treating chronic hepatitis B virus (HBV) infection: ##STR00001##

MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS

Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.