Patent classifications
C07D207/08
Treprostinil derivative compounds and methods of using same
Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
ADO-resistant cysteamine analogs and uses thereof
The present disclosure is directed to methods for treating diseases for which cysteamine is indicated and compounds useful in such methods.
ADO-resistant cysteamine analogs and uses thereof
The present disclosure is directed to methods for treating diseases for which cysteamine is indicated and compounds useful in such methods.
Biphenyl derivatives and methods for preparing same
Provided are biphenyl derivatives having the structure of Formula 1: ##STR00001##
stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein R.sub.1 is hydrogen, halogen, hydroxy, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or C.sub.1-C.sub.6 alkoxy; R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, halogen, substituted or unsubstituted amino, nitro, cyano, hydroxy, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, substituted or unsubstituted C.sub.1-C.sub.6 alkoxy, or —C(O)R.sub.6; R.sub.5 is hydrogen or C.sub.1-C.sub.6 alkyl; n is 0 or 1; and R.sub.6 is hydrogen or amino, methods for preparing the same, and a pharmaceutical composition containing the same. The biphenyl derivatives having the structure of Formula 1 act as muscarinic M3 receptor antagonists, and thus are useful for the prevention or treatment of a disease selected from among chronic obstructive pulmonary disease, asthma, irritable bowel syndrome, urinary incontinence, rhinitis, spasmodic colitis, chronic cystitis, Alzheimer's disease, senile dementia, glaucoma, schizophrenia, gastroesophageal reflux disease, cardiac arrhythmia, and hyper-salivation syndromes.
Biphenyl derivatives and methods for preparing same
Provided are biphenyl derivatives having the structure of Formula 1: ##STR00001##
stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein R.sub.1 is hydrogen, halogen, hydroxy, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or C.sub.1-C.sub.6 alkoxy; R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, halogen, substituted or unsubstituted amino, nitro, cyano, hydroxy, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, substituted or unsubstituted C.sub.1-C.sub.6 alkoxy, or —C(O)R.sub.6; R.sub.5 is hydrogen or C.sub.1-C.sub.6 alkyl; n is 0 or 1; and R.sub.6 is hydrogen or amino, methods for preparing the same, and a pharmaceutical composition containing the same. The biphenyl derivatives having the structure of Formula 1 act as muscarinic M3 receptor antagonists, and thus are useful for the prevention or treatment of a disease selected from among chronic obstructive pulmonary disease, asthma, irritable bowel syndrome, urinary incontinence, rhinitis, spasmodic colitis, chronic cystitis, Alzheimer's disease, senile dementia, glaucoma, schizophrenia, gastroesophageal reflux disease, cardiac arrhythmia, and hyper-salivation syndromes.
Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
TWO-PHOTON ABSORBING FLUOROPHORES AND METHOD FOR CELLULAR IMAGING USING THE SAME
The present invention relates to new one-photon or two-photon absorbing fluorophores, a method for preparing the same, and a method for cellular imaging using the same, and more particularly, to new two-photon absorbing fluorophores having higher fluorescence quantum yield and two-photon absorption cross-section value than those of the conventional two-photon absorbing fluorophore, acedan, and thus are promisingly applicable in bioimaging. The design strategy and the compounds according to the present invention may practically utilized for developing new D-π-A fluorophores.
TWO-PHOTON ABSORBING FLUOROPHORES AND METHOD FOR CELLULAR IMAGING USING THE SAME
The present invention relates to new one-photon or two-photon absorbing fluorophores, a method for preparing the same, and a method for cellular imaging using the same, and more particularly, to new two-photon absorbing fluorophores having higher fluorescence quantum yield and two-photon absorption cross-section value than those of the conventional two-photon absorbing fluorophore, acedan, and thus are promisingly applicable in bioimaging. The design strategy and the compounds according to the present invention may practically utilized for developing new D-π-A fluorophores.
COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES
The present disclosure relates to novel compounds, pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurodegerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed.