Patent classifications
C07D239/34
NOVEL HYDRAZONE DERIVATIVE IN WHICH TERMINAL AMINE GROUP IS SUBSTITUTED WITH ARYL GROUP OR HETEROARYL GROUP, AND USE THEREOF
- Ae Nim Pae ,
- Yun Kyung Kim ,
- Sang Min LIM ,
- Sungsu LIM ,
- Jihye SEONG ,
- Jae Wook Lee ,
- Ji Yeon Song ,
- Seulgi SHIN ,
- Hyean Jeong JEONG ,
- Woo Seung SON ,
- Haeun LEE ,
- Da Mi LIM ,
- Seok Kyu KIM ,
- Jee Yun AHN ,
- Chae Won KIM ,
- Ashwini Machhindra LONDHE ,
- Lizaveta GOTINA ,
- Hyojin KIM ,
- Hye Yeon LEE ,
- Nam Gyung KIM ,
- Eunji CHA ,
- Kunhee KIM ,
- Ji Woong LIM
The present invention relates to novel hydrazone derivatives in which a terminal amine group is substituted with an aryl group or a heteroaryl group, and uses thereof.
ANTIVIRAL COMPOUNDS
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
ANTIVIRAL COMPOUNDS
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
OPIOID RECEPTOR MODULATORS
Provided herein are opioid receptor modulators and pharmaceutical compositions comprising said compounds.
Tri-substituted aryl and heteroaryl derivatives as modulators of PI3-kinase and autophagy pathways
The present disclosure relates to tri-substituted aryl and heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for modulating autophagy or preventing, reversing, slowing or inhibiting the PI3K-AKT-MTOR pathway, and methods of treating diseases that are associated with autophagy or the PI3K-AKT-MTOR pathway. ##STR00001##
TRNA SYNTHETASE INHIBITORS
Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.
TRNA SYNTHETASE INHIBITORS
Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.
Carbocyanines for G-quadruplex DNA stabilization and telomerase inhibition
Cyanines which selectively bind to G-quadruplex DNA complexes, particularly quadruplexes expressed in cancer cells, and methods of making and using thereof are described herein. The cyanine can be a symmetrical or unsymmetrical streptocyanine, hemicyanine, closed chain cyanine, or combinations thereof. The cyanine is preferably substituted with one or more groups that minimize or prevent aggregation of the cyanine and/or inhibit binding of the cyanine to duplex DNA. One or more of the cyanines can be formulated with one or more pharmaceutical excipients and/or carrier to prepare pharmaceutical compositions suitable for administration to a patient, particular a human patient. The compounds and compositions described herein can be used to treat diseases or disorders characterized by the expression of G-quadruplex DNA, such as cancer.
Carbocyanines for G-quadruplex DNA stabilization and telomerase inhibition
Cyanines which selectively bind to G-quadruplex DNA complexes, particularly quadruplexes expressed in cancer cells, and methods of making and using thereof are described herein. The cyanine can be a symmetrical or unsymmetrical streptocyanine, hemicyanine, closed chain cyanine, or combinations thereof. The cyanine is preferably substituted with one or more groups that minimize or prevent aggregation of the cyanine and/or inhibit binding of the cyanine to duplex DNA. One or more of the cyanines can be formulated with one or more pharmaceutical excipients and/or carrier to prepare pharmaceutical compositions suitable for administration to a patient, particular a human patient. The compounds and compositions described herein can be used to treat diseases or disorders characterized by the expression of G-quadruplex DNA, such as cancer.
COMPOUNDS AND THEIR USE FOR THE TREATMENT OF ALPHA1-ANTITRYPSIN DEFICIENCY
The invention relates to specified benzamide compounds of formula (1), and pharmaceutical compositions containing the compounds. The compounds may be inducers of α.sub.1-antitrypsin (A1AT), and may be used in the treatment of a disease or disorder such as α.sub.1-antitrypsin deficiency (A1AD or AATD).