A61K31/416

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.

CARBOXYLIC ACID AROMATIC AMIDES

The present invention relates to carboxylic acid aromatic amides compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease as a sole agent or in combination with other active ingredients.

CARBOXYLIC ACID AROMATIC AMIDES

The present invention relates to carboxylic acid aromatic amides compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease as a sole agent or in combination with other active ingredients.

Gut microbiota and treatment of cancer

The ubiquitin ligase, RNF5, regulates the gut microbiota composition and influences the immune checkpoint response to tumors. RNF5 deficient animals exhibit significant inhibition of tumor development as well as an altered gut microbiota composition. Methods of treating cancer by administering to a subject one or more selected bacterial species and/or one or more prebiotics that promote the growth of one or more selected bacterial species are disclosed. Also disclosed are methods of treating cancer by administering to a subject one or more selected bacterial species and/or one or more prebiotics that promote the growth of one or more selected bacterial species in combination with one or more anti-cancer agents.

PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR CHRONIC PROSTATITIS/CHRONIC PELVIC PAIN SYNDROME

The present invention relates to a prophylactic and/or therapeutic agent for chronic prostatitis/chronic pelvic pain syndrome, the agent containing an mPGES-1 inhibitor as an active ingredient.

INDAZOLE HYDRAZIDE COMPOUND AND APPLICATION THEREOF

An indazole hydrazide compound, as represented in formula (I); wherein, R is selected from substituted alkyl, substituted alkenyl and substituted phenyl; substituent in the substituted alkyl and substituted alkenyl includes phenyl and/or substituted phenyl; R′ is selected from H and alkyl. Compared with the prior art, the above indole hydrazide compound can be used as integrin avβ3 receptor antagonist. Besides, it has obvious anti-prostate cancer activity and has a significant inhibitory effect on enzalutamide-resistant cell lines. In addition, the above-mentioned compound has obvious anti-tumor angiogenesis activity and can be used in the preparation of anti-tumor angiogenesis drugs to inhibit tumor angiogenesis.

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Compounds and Methods for Treatment of Visceral Pain
20230033510 · 2023-02-02 ·

The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof and their use in methods for the alleviation and/or treatment of visceral pain, for example abdominal pain; pelvic pain; male pelvic pain; pain from an internal organ; bladder pain; painful bladder syndrome; post-surgical abdominal pain (e.g., GI resection, hysterectomy, oophorectomy, C-section, and the like); or pain arising from or related to: pancreatitis (e.g., chronic pancreatitis), prostatitis (e.g., chronic prostatitis), inflammatory bowel disease (e.g., Crohn's disease), endometriosis, interstitial cystitis, prostatitis (e.g., chronic prostatitis), epididymitis (e.g., chronic epididymitis), or post-surgical abdominal lesions. In some embodiments, the visceral pain is consequent to inflammatory bowel disease, for example Crohn's disease.