C07C235/64

METAL (HYDR)OXIDE COMPOSITE COMPRISING POORLY SOLUBLE DRUG, METHOD FOR MANUFACTURING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

The present invention relates to a metal (hydr)oxide composite comprising a poorly soluble drug, a method for manufacturing same, and a pharmaceutical composition comprising same.

COCRYSTAL COMPRISING CAMOSTAT AND NICLOSAMIDE, PHARMACEUTICAL COMPOSITION COMPRISING SAME AND PREPARATION METHOD THEREFOR
20230233502 · 2023-07-27 ·

The present invention relates to a novel cocrystal, a pharmaceutical composition comprising same and a preparation method therefor. By using the cocrystal of the present invention, cancers, inflammatory diseases, or viral infection diseases may be effectively prevented and/or treated.

DUAL ANDROGEN RECEPTOR/AKR1C3 INHIBITORS

The present invention provides benzamide compounds, compositions containing the benzamides, and use of the benzamides for inhibiting androgen receptor (AR) and/or aldo-keto reductase family 1 member C3 (AKR1C3). Also described herein methods for the treatment of hormone-mediated diseases and conditions, including hormone-related cancers such as castration resistant prostate cancer.

DUAL ANDROGEN RECEPTOR/AKR1C3 INHIBITORS

The present invention provides benzamide compounds, compositions containing the benzamides, and use of the benzamides for inhibiting androgen receptor (AR) and/or aldo-keto reductase family 1 member C3 (AKR1C3). Also described herein methods for the treatment of hormone-mediated diseases and conditions, including hormone-related cancers such as castration resistant prostate cancer.

Compounds and compositions for the treatment of neurodegenerative and inflammatory diseases

The invention relates to compounds exhibiting kallikrein inhibitory activity, and to compositions comprising at least one of these compounds for use in the treatment of diseases or disorders in which kallikrein activity is dysregulated, particularly neurodegenerative and inflammatory diseases.

COMPOUNDS AND METHODS FOR POTENTIATING COLISTIN ACTIVITY

Infections caused by multidrug-resistant (MDR) bacteria, particularly Gram-negative bacteria, are an escalating global t health threat. Often clinicians are forced to administer the last resort antibiotic colistin, however colistin resistance is becoming increasingly prevalent, giving rise to the potential for a situation in which there are no treatment options for MDR Gram-negative infections. The development of adjuvants that circumvent bacterial resistance mechanisms is a promising orthogonal approach to the development of new antibiotics. We recently disclosed that the known IKK-13 inhibitor IMD-0354 potently suppresses colistin resistance in several Gram-negative strains. In this disclosure, we explore the structure activity relationship (SAR) between the IMD-0354 scaffold and colistin resistance suppression, and identify several compounds with more potent activity than the parent against highly colistin resistant strains of Acinetobacter baumannii and Klebsiella pneumoniae.

COMPOUNDS AND METHODS FOR POTENTIATING COLISTIN ACTIVITY

Infections caused by multidrug-resistant (MDR) bacteria, particularly Gram-negative bacteria, are an escalating global t health threat. Often clinicians are forced to administer the last resort antibiotic colistin, however colistin resistance is becoming increasingly prevalent, giving rise to the potential for a situation in which there are no treatment options for MDR Gram-negative infections. The development of adjuvants that circumvent bacterial resistance mechanisms is a promising orthogonal approach to the development of new antibiotics. We recently disclosed that the known IKK-13 inhibitor IMD-0354 potently suppresses colistin resistance in several Gram-negative strains. In this disclosure, we explore the structure activity relationship (SAR) between the IMD-0354 scaffold and colistin resistance suppression, and identify several compounds with more potent activity than the parent against highly colistin resistant strains of Acinetobacter baumannii and Klebsiella pneumoniae.

Pharmaceutical compositions with antiflaviviral activity

Provided is a method of inhibiting viral replication, including contacting one or more cells that has been infected or contacted with a flavivirus with an effective amount of niclosamide, temoporfin, nitazoxanide, tizoxanide, erythrosin B, methylene blue. Contacting one or more cells that have been infected with a flavivirus may include administering the compound to a mammal, a human, or other subject. The flavivirus may be Dengue virus serotype 1, Dengue virus serotype 2, Dengue virus serotype 3, Dengue virus serotype 4, yellow fever virus, West Nile virus, Zika virus, Japanese encephalitis virus, tick-born encephalitis virus, Powassan virus, St. Louis encephalitis virus, or other flavivirus.

Pharmaceutical compositions with antiflaviviral activity

Provided is a method of inhibiting viral replication, including contacting one or more cells that has been infected or contacted with a flavivirus with an effective amount of niclosamide, temoporfin, nitazoxanide, tizoxanide, erythrosin B, methylene blue. Contacting one or more cells that have been infected with a flavivirus may include administering the compound to a mammal, a human, or other subject. The flavivirus may be Dengue virus serotype 1, Dengue virus serotype 2, Dengue virus serotype 3, Dengue virus serotype 4, yellow fever virus, West Nile virus, Zika virus, Japanese encephalitis virus, tick-born encephalitis virus, Powassan virus, St. Louis encephalitis virus, or other flavivirus.

PHARMACEUTICAL COMPOSITIONS WITH ANTIFLAVIVIRAL ACTIVITY

Provided is a method of inhibiting viral replication, including contacting one or more cells that has been infected or contacted with a flavivirus with an effective amount of niclosamide, temoporfin, nitazoxanide, tizoxanide, erythrosin B, methylene blue. Contacting one or more cells that have been infected with a flavivirus may include administering the compound to a mammal, a human, or other subject. The flavivirus may be Dengue virus serotype 1, Dengue virus serotype 2, Dengue virus serotype 3, Dengue virus serotype 4, yellow fever virus, West Nile virus, Zika virus, Japanese encephalitis virus, tick-born encephalitis virus, Powassan virus, St. Louis encephalitis virus, or other flavivirus.