C07D209/26

CYCLOPROPENIUM COMPOUNDS, PROCESS FOR THEIR PREPARATION AND USE
20230373900 · 2023-11-23 ·

The present invention relates to a cyclopropenium salt bearing an electron withdrawing group suitable for use as a reagent in cyclopropenylation reactions of formula (I). The invention also relates to a process for their preparation, the use thereof as cyclopropenylation reagent, to an electrophilic aromatic substitution process of cyclopropenylation, and to a process for cyclopropenylation of organometallic substrates using said reagents.

##STR00001##

CYCLOPROPENIUM COMPOUNDS, PROCESS FOR THEIR PREPARATION AND USE
20230373900 · 2023-11-23 ·

The present invention relates to a cyclopropenium salt bearing an electron withdrawing group suitable for use as a reagent in cyclopropenylation reactions of formula (I). The invention also relates to a process for their preparation, the use thereof as cyclopropenylation reagent, to an electrophilic aromatic substitution process of cyclopropenylation, and to a process for cyclopropenylation of organometallic substrates using said reagents.

##STR00001##

Compositions and methods for modulating hair growth

The present disclosure relates to compounds that are capable of inhibiting the mitochondrial pyruvate carrier and promoting hair growth. The disclosure further relates to methods of promoting hair growth or treating conditions or disorders affecting hair growth, such as baldness or alopecia.

Indole compounds and their use

The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.

Indole compounds and their use

The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.

COMPOSITIONS AND METHODS FOR MODULATING HAIR GROWTH

The present disclosure relates to compounds that are capable of inhibiting the mitochondrial pyruvate carrier and promoting hair growth. The disclosure further relates to methods of promoting hair growth or treating conditions or disorders affecting hair growth, such as baldness or alopecia.

NOVEL INDOLE DERIVATIVE AND ANTI-CANCER CONPOSITION CONTAINING SAME

The present invention relates to: an indole derivative, which is a novel cell mitosis inhibitor; a stereoisomer thereof or a pharmaceutically acceptable salt thereof; a use thereof as a therapeutic agent; a composition containing the same and a treatment method using the composition; and a preparation method therefor. According to the present invention, the indole derivative, the stereoisomer thereof or the pharmaceutically acceptable salt thereof, inhibits the tubulin polymerization during mitosis so as to induce apoptosis, and has an excellent anti-cancer effect also in cancer cells having multiple drug resistance.

INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured. The variables shown in Formula AA are as defined in the claims. The compounds of formula AA are NLRP3 activity modulators and, as such, can be used in the treatment of metabolic disorders (e.g. Type 2 diabetes, atherosclerosis, obesity or gout), a disease of the central nervous system (e.g. Alzheimer's disease, multiple sclerosis, Amyotrophic Lateral Sclerosis or Parkinson's disease), lung disease (e.g. asthma, COPD or pulmonary idiopathic fibrosis), liver disease (e.g. NASH syndrome, viral hepatitis or cirrhosis), pancreatic disease (e.g. acute pancreatitis or chronic pancreatitis), kidney disease (e.g. acute kidney injury or chronic kidney injury), intestinal disease (e.g. Crohn's disease or Ulcerative Colitis), skin disease (e.g. psoriasis), musculoskeletal disease (e.g. scleroderma), a vessel disorder (e.g. giant cell arteritis), a disorder of the bones (e.g. osteoarthritis, osteoporosis or osteopetrosis disorders), eye disease (e.g. glaucoma or macular degeneration), a disease caused by viral infection (e.g. HIV or AIDS), an autoimmune disease (e.g. Rheumatoid Arthritis, Systemic Lupus Erythematosus or Autoimmune Thyroiditis), cancer or aging.

##STR00001##