Patent classifications
C07C235/64
Methods of treating cardiac edema, neuromyelitis optica, and hyponatremia
The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g., neurosurgery, endovascular clot removal, spinal tap, aneurysm repair, or deep brain stimulation, as well as retinal edema), as well as hyponatremia and excess fluid retention, and diseases such as epilepsy, retinal ischemia and other diseases of the eye associated with abnormalities in intraocular pressure and/or tissue hydration, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines, as well as to novel assays for identifying aquaporin inhibitors.
Methods of treating cardiac edema, neuromyelitis optica, and hyponatremia
The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g., neurosurgery, endovascular clot removal, spinal tap, aneurysm repair, or deep brain stimulation, as well as retinal edema), as well as hyponatremia and excess fluid retention, and diseases such as epilepsy, retinal ischemia and other diseases of the eye associated with abnormalities in intraocular pressure and/or tissue hydration, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines, as well as to novel assays for identifying aquaporin inhibitors.
CARBOXAMIDES AS MODULATORS OF SODIUM CHANNELS
Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
CARBOXAMIDES AS MODULATORS OF SODIUM CHANNELS
Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
PHARMACEUTICAL FORMULATIONS
This disclosure features niclosamide compounds (or pharmaceutically acceptable salts and/or co-crystals thereof, e.g., niclosamide), having one or more properties that include, but are not limited to: a particular purity (e.g., a chemical purity of greater than about 99.0%) and a particular particle size (e.g., a particular particle size distribution and/or a particular particle size range and/or a specific surface area range). In an aspect, the niclosamide compounds described herein (e.g., niclosamide) can form part of compositions, dosage forms (e.g., unit dosage forms), and the like, which are suitable for oral administration. This disclosure also features methods of making and using the same.
PHARMACEUTICAL FORMULATIONS
This disclosure features niclosamide compounds (or pharmaceutically acceptable salts and/or co-crystals thereof, e.g., niclosamide), having one or more properties that include, but are not limited to: a particular purity (e.g., a chemical purity of greater than about 99.0%) and a particular particle size (e.g., a particular particle size distribution and/or a particular particle size range and/or a specific surface area range). In an aspect, the niclosamide compounds described herein (e.g., niclosamide) can form part of compositions, dosage forms (e.g., unit dosage forms), and the like, which are suitable for oral administration. This disclosure also features methods of making and using the same.
COMPOUNDS AND METHODS OF INHIBITING BACTERIAL CHAPERONIN SYSTEMS
The present disclosure relates to compounds and methods of killing or inhibiting the growth of bacteria by disrupting chaperonin-mediated refolding of proteins.
COMPOUNDS AND METHODS OF INHIBITING BACTERIAL CHAPERONIN SYSTEMS
The present disclosure relates to compounds and methods of killing or inhibiting the growth of bacteria by disrupting chaperonin-mediated refolding of proteins.
NOVEL ANTIMICROBIAL COMPOUND AND USE THEREOF
The present invention relates to: coralmycin A and B, which are novel compounds exhibiting antimicrobial activity, an isomer thereof, a derivative thereof or a pharmaceutically acceptable salt thereof; a microorganism of the genus Corallococcus producing the same; and an antimicrobial use thereof.
The coralmycin A and B have very strong antimicrobial activity against antibiotic-resistant bacteria such as MRSA, QRSA, VRE, VISA, etc.; Acinetobacter baumannii, which is a multidrug-resistant microorganism; and also against gram-positive microorganisms and gram-negative microorganisms. Therefore, the present invention can be very useful for prevention, treatment and alleviation of various microbial infections, and thus can be widely applied to the medical supply, quasi-drug, food, and feed industries.
NOVEL ANTIMICROBIAL COMPOUND AND USE THEREOF
The present invention relates to: coralmycin A and B, which are novel compounds exhibiting antimicrobial activity, an isomer thereof, a derivative thereof or a pharmaceutically acceptable salt thereof; a microorganism of the genus Corallococcus producing the same; and an antimicrobial use thereof.
The coralmycin A and B have very strong antimicrobial activity against antibiotic-resistant bacteria such as MRSA, QRSA, VRE, VISA, etc.; Acinetobacter baumannii, which is a multidrug-resistant microorganism; and also against gram-positive microorganisms and gram-negative microorganisms. Therefore, the present invention can be very useful for prevention, treatment and alleviation of various microbial infections, and thus can be widely applied to the medical supply, quasi-drug, food, and feed industries.