A61K31/428

BICYCLIC COMPOUND

Provided is a bicyclic compound having an acetyl-CoA carboxylase inhibitory action. A compound represented by the formula:

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wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an acetyl-CoA carboxylase inhibitory action, is useful for the prophylaxis or treatment of cancer, inflammatory diseases and the like, and has superior efficacy.

Inhibiting Germination of Clostridium Perfringens Spores to Reduce Necrotic Enteritis
20180000793 · 2018-01-04 ·

Provided herein are materials and methods useful for reducing, preventing, and/or inhibiting germination of C. perfringens spores, including methods for inhibiting C. perfringens germination to reduce necrotizing enteritis (NE, also referred to as necrotic enteritis) in animals. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Inhibiting Germination of Clostridium Perfringens Spores to Reduce Necrotic Enteritis
20180000793 · 2018-01-04 ·

Provided herein are materials and methods useful for reducing, preventing, and/or inhibiting germination of C. perfringens spores, including methods for inhibiting C. perfringens germination to reduce necrotizing enteritis (NE, also referred to as necrotic enteritis) in animals. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Mitigation of lung injury

Inhibition of human epidermal growth factor receptor 2, human epidermal growth factor receptor 3, or of the heterodimerization of these proteins has presently been found to mitigate mechanically-induced lung injury or a lung-stretch injury. Provided are methods for treating a mechanically-induced lung injury or a lung-stretch injury, for increasing lung compliance, moderating alveolar epithelial permeability, or both in a subject having a mechanically-induced lung injury or a lung-stretch injury, for protecting a subject against a decrease in lung compliance, an increase in alveolar epithelial permeability, or both, as a result of a mechanically-induced lung injury or a lung-stretch injury, such methods involving the administration of an inhibitor of human epidermal growth factor receptor 2 (HER2) or human epidermal growth factor receptor 3 (HER3), or an inhibitor of the heterodimerization of HER2/HER3.

Mitigation of lung injury

Inhibition of human epidermal growth factor receptor 2, human epidermal growth factor receptor 3, or of the heterodimerization of these proteins has presently been found to mitigate mechanically-induced lung injury or a lung-stretch injury. Provided are methods for treating a mechanically-induced lung injury or a lung-stretch injury, for increasing lung compliance, moderating alveolar epithelial permeability, or both in a subject having a mechanically-induced lung injury or a lung-stretch injury, for protecting a subject against a decrease in lung compliance, an increase in alveolar epithelial permeability, or both, as a result of a mechanically-induced lung injury or a lung-stretch injury, such methods involving the administration of an inhibitor of human epidermal growth factor receptor 2 (HER2) or human epidermal growth factor receptor 3 (HER3), or an inhibitor of the heterodimerization of HER2/HER3.

Small molecule inhibitors for treatment of alpha viruses

An in vitro assay was designed to measure the activity of the alphavirus non-structural protein 2 (nsP2), which is the viral protease and is required for viral replication. By taking advantage of fluorescence-resonance energy transfer between two proteins, a protease cleavage assay was generated. This was utilized for high-throughput screening of 40,000 small molecules. Inhibitors were validated using cell-based assays to measure alphavirus infection and cytotoxicity. Certain compounds were then characterized for anti-viral efficacy in various cell lines in numerous assays. Compounds were tested against Chikungunya virus, Venezuelan Equine Encephalitis virus, Rift Valley Fever virus, and Zika virus. Three compounds (compounds I, II, and III) showed pan-alphavirus anti-viral efficacy at concentrations that did not result in cell toxicity. An additional compound, structure IV, showed broad spectrum inhibition of all viruses tested. Pharmaceutical preparations and methods of treatment including these compounds are provided herein.

Small molecule inhibitors for treatment of alpha viruses

An in vitro assay was designed to measure the activity of the alphavirus non-structural protein 2 (nsP2), which is the viral protease and is required for viral replication. By taking advantage of fluorescence-resonance energy transfer between two proteins, a protease cleavage assay was generated. This was utilized for high-throughput screening of 40,000 small molecules. Inhibitors were validated using cell-based assays to measure alphavirus infection and cytotoxicity. Certain compounds were then characterized for anti-viral efficacy in various cell lines in numerous assays. Compounds were tested against Chikungunya virus, Venezuelan Equine Encephalitis virus, Rift Valley Fever virus, and Zika virus. Three compounds (compounds I, II, and III) showed pan-alphavirus anti-viral efficacy at concentrations that did not result in cell toxicity. An additional compound, structure IV, showed broad spectrum inhibition of all viruses tested. Pharmaceutical preparations and methods of treatment including these compounds are provided herein.

MrgprX2 Antagonists for the Treatment of Inflammatory Disorders

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically or orally acceptable carrier for administration.

MrgprX2 Antagonists for the Treatment of Inflammatory Disorders

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically or orally acceptable carrier for administration.

PHARMACEUTICAL COMPOSITION, COMPLEMENTARY KIT AND APPLICATION THEREOF
20230028539 · 2023-01-26 ·

A pharmaceutical composition, a complementary kit and an application thereof; the pharmaceutical composition comprises pramipexole and safinamide, the mass ratio of pramipexole to safinamide being 1:300-1:30; and the pharmaceutical composition has a good curative effect and has few side effects, and effectively improve the condition of a patient. The capabilities thereof in restoring dopamine levels are better than those from using pramipexole or safinamide alone. In addition, the composition has better neuroprotective activity, and therefore damage to the dopaminergic system and the normal sensitivity of the dopamine system to dopamine agonists are reduced. The composition can restore or balance a potential unbalanced response to “increasing dopaminergic treatment” that is caused by the use of a dopamine agonist alone; the composition can reduce the amount of pramipexole when used alone so as to reduce the risk of side effects and drug resistance.