C07C225/30

COMPOUNDS AND METHODS FOR THE TREATMENT OF PARASITIC INFECTIONS

Cryptosporidium parvum is a highly prevalent zoonotic and anthroponotic protozoan parasite that causes a diarrheal syndrome in children and neonatal livestock, culminating in growth retardation and mortalities. Disclosed herein are inhibitors against the enzymatic activity of recombinant CpLDH protein that were identified. The inhibitors were tested for anti-Cryptosporidium effect using in vitro infection assays of HCT-8 cells monolayers. Compounds NSC158011 and NSC10447 were identified to inhibit the proliferation of intracellular C. parvum in vitro, with IC50 values of 14.88 and 72.65 μM, respectively. At doses tolerable in mice, both NSC158011 and NSC10447 significantly reduced the shedding of C. parvum oocysts in infected immunocompromised mice's feces and prevented intestinal villous atrophy as well as mucosal erosion due to C. parvum. These findings have unveiled anti-Cryptosporidium drug candidates that can be explored further for the development of therapeutic agents against C. parvum infections.

COMPOUNDS AND METHODS FOR THE TREATMENT OF PARASITIC INFECTIONS

Cryptosporidium parvum is a highly prevalent zoonotic and anthroponotic protozoan parasite that causes a diarrheal syndrome in children and neonatal livestock, culminating in growth retardation and mortalities. Disclosed herein are inhibitors against the enzymatic activity of recombinant CpLDH protein that were identified. The inhibitors were tested for anti-Cryptosporidium effect using in vitro infection assays of HCT-8 cells monolayers. Compounds NSC158011 and NSC10447 were identified to inhibit the proliferation of intracellular C. parvum in vitro, with IC50 values of 14.88 and 72.65 μM, respectively. At doses tolerable in mice, both NSC158011 and NSC10447 significantly reduced the shedding of C. parvum oocysts in infected immunocompromised mice's feces and prevented intestinal villous atrophy as well as mucosal erosion due to C. parvum. These findings have unveiled anti-Cryptosporidium drug candidates that can be explored further for the development of therapeutic agents against C. parvum infections.

COMPOSITIONS AND METHODS FOR TREATMENT OF PROSTATE CARCINOMA

Disclosed herein are 1,4-naphthoquinone analogs, pharmaceutical compositions that include one or more of such 1,4-naphthoquinone analogs, and methods of treating and/or ameliorating diseases and/or conditions associated with a cancer, such as prostate cancer with such 1,4-naphthoquinone analogs. Also included are combination therapies wherein a 1,4-naphthoquinone analog disclosed herein, and a hormone therapy agent are provided to a subject suffering from a condition such as cancer.

COMPOSITIONS AND METHODS FOR TREATMENT OF PROSTATE CARCINOMA

Disclosed herein are 1,4-naphthoquinone analogs, pharmaceutical compositions that include one or more of such 1,4-naphthoquinone analogs, and methods of treating and/or ameliorating diseases and/or conditions associated with a cancer, such as prostate cancer with such 1,4-naphthoquinone analogs. Also included are combination therapies wherein a 1,4-naphthoquinone analog disclosed herein, and a hormone therapy agent are provided to a subject suffering from a condition such as cancer.

WATER-SOLUBLE NAPHTHOQUINONE DERIVATIVE COMPOSITION AND METHOD FOR PRODUCING SAME, WATER-SOLUBLE COMPOSITION FOR CONTROLLING HARMFUL ALGAE, METHOD FOR CONTROLLING LARGE-SCALE HARMFUL ALGAE, AND AUTOMATION SYSTEM FOR AI-MONITORING, REMOVING, AND PREVENTING LARGE-SCALE HARMFUL ALGAE
20220144752 · 2022-05-12 ·

Provided are a water-soluble naphthoquinone derivative composition and a method for preparing the same, a water-soluble composition for controlling harmful algae, a method of controlling large-scale harmful algae, and an automated system for artificial intelligence monitoring, removal, and prevention of large-scale harmful algae. According to one embodiment, a method of preparing a water-soluble naphthoquinone derivative composition includes reacting a 1,4-naphthoquinone compound with N,N-diethylethylenediamine to obtain an intermediate product of [Chemical Formula 2]; and reacting an intermediate product of [Chemical Formula 2] with hydrochloric acid to obtain a compound of [Chemical Formula 1]. In addition, the water-soluble naphthoquinone derivative composition represented by the following [Chemical Formula 1] is proposed. In addition, a water-soluble composition is proposed for controlling harmful algae, a method for controlling large-scale harmful algae using the water-soluble composition for controlling harmful algae, and an automated system for artificial intelligence monitoring, removal, and prevention of large-scale harmful algae.

WATER-SOLUBLE NAPHTHOQUINONE DERIVATIVE COMPOSITION AND METHOD FOR PRODUCING SAME, WATER-SOLUBLE COMPOSITION FOR CONTROLLING HARMFUL ALGAE, METHOD FOR CONTROLLING LARGE-SCALE HARMFUL ALGAE, AND AUTOMATION SYSTEM FOR AI-MONITORING, REMOVING, AND PREVENTING LARGE-SCALE HARMFUL ALGAE
20220144752 · 2022-05-12 ·

Provided are a water-soluble naphthoquinone derivative composition and a method for preparing the same, a water-soluble composition for controlling harmful algae, a method of controlling large-scale harmful algae, and an automated system for artificial intelligence monitoring, removal, and prevention of large-scale harmful algae. According to one embodiment, a method of preparing a water-soluble naphthoquinone derivative composition includes reacting a 1,4-naphthoquinone compound with N,N-diethylethylenediamine to obtain an intermediate product of [Chemical Formula 2]; and reacting an intermediate product of [Chemical Formula 2] with hydrochloric acid to obtain a compound of [Chemical Formula 1]. In addition, the water-soluble naphthoquinone derivative composition represented by the following [Chemical Formula 1] is proposed. In addition, a water-soluble composition is proposed for controlling harmful algae, a method for controlling large-scale harmful algae using the water-soluble composition for controlling harmful algae, and an automated system for artificial intelligence monitoring, removal, and prevention of large-scale harmful algae.

WATER-SOLUBLE NAPHTHOQUINONE DERIVATIVE COMPOSITION AND METHOD FOR PRODUCING SAME, WATER-SOLUBLE COMPOSITION FOR CONTROLLING HARMFUL ALGAE, METHOD FOR CONTROLLING LARGE-SCALE HARMFUL ALGAE, AND AUTOMATION SYSTEM FOR AI-MONITORING, REMOVING, AND PREVENTING LARGE-SCALE HARMFUL ALGAE
20220144752 · 2022-05-12 ·

Provided are a water-soluble naphthoquinone derivative composition and a method for preparing the same, a water-soluble composition for controlling harmful algae, a method of controlling large-scale harmful algae, and an automated system for artificial intelligence monitoring, removal, and prevention of large-scale harmful algae. According to one embodiment, a method of preparing a water-soluble naphthoquinone derivative composition includes reacting a 1,4-naphthoquinone compound with N,N-diethylethylenediamine to obtain an intermediate product of [Chemical Formula 2]; and reacting an intermediate product of [Chemical Formula 2] with hydrochloric acid to obtain a compound of [Chemical Formula 1]. In addition, the water-soluble naphthoquinone derivative composition represented by the following [Chemical Formula 1] is proposed. In addition, a water-soluble composition is proposed for controlling harmful algae, a method for controlling large-scale harmful algae using the water-soluble composition for controlling harmful algae, and an automated system for artificial intelligence monitoring, removal, and prevention of large-scale harmful algae.

Aziridinyl and amino dimeric naphthoquinone compounds and use for acute myeloid leukemia

The invention relates to new amino dimeric naphthoquinone compounds with antileukemic activity. Compounds of the invention demonstrated increased aqueous solubility compared to previously available dimeric naphthoquinones and potent nanomolar inhibition of cell survival in AML cells. Preferred compounds contained an aziridine or a secondary amino alcohol pharmacophore.

Aziridinyl and amino dimeric naphthoquinone compounds and use for acute myeloid leukemia

The invention relates to new amino dimeric naphthoquinone compounds with antileukemic activity. Compounds of the invention demonstrated increased aqueous solubility compared to previously available dimeric naphthoquinones and potent nanomolar inhibition of cell survival in AML cells. Preferred compounds contained an aziridine or a secondary amino alcohol pharmacophore.

Compounds and pharmaceutical composition associated with ubiquitination-proteasome system

The invention relates to new compounds with low cytotoxicity for blocking ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of treating disorders including, but not limited to, cancers, neurodegenerative diseases, inflammatory disorders and autoimmune disorders and metabolic disorders.