C07D307/66

AMIDE COMPOUND OR SALT THEREOF, AGRICULTURAL AND HORTICULTURAL MICROBICIDE COMPRISING THE COMPOUND AND THE SALT, AND METHOD FOR USING THE AGRICULTURAL AND HORTICULTURAL MICROBICIDE

An amide compound represented by the general formula [I]:

##STR00001##

or a salt thereof, an agricultural and horticultural microbicide comprising the compound or the salt as an active ingredient, and a method for using the agricultural and horticultural microbicide.

INHIBITORS OF BETA-HYDROXYLASE FOR TREATMENT OF CANCER

The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

INHIBITORS OF BETA-HYDROXYLASE FOR TREATMENT OF CANCER

The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

COMPOSITIONS AND METHODS FOR VIRAL SENSITIZATION

Provided are compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.

COMPOSITIONS AND METHODS FOR VIRAL SENSITIZATION

Provided are compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.

DERIVATIVES OF KORORMICIN USEFUL AS ANTIBIOTICS
20200345682 · 2020-11-05 ·

Described herein is a process for antibiotic development comprising: (a) generating a compound of formula (III):

##STR00001##

or a salt or stereoisomer or prodrug thereof; wherein R.sup.1-R.sup.3 and R.sup.5-R.sup.10 are independently selected from H, alkyl group, substituted alkyl group, halogen, OH, NH.sub.2, or SH; R.sup.4 is H, alkyl group or substituted alkyl group; X.sup.1-X.sup.2 are independently selected from O, S, NH, H, alkyl, halogen, OH, SH, or NH.sub.2; W is a saturated acyclic hydrocarbon chain of 1 to 15 carbon atoms; and Z is a neutral or positively charged organic group comprising a nitrogen or phosphorus atom; and; and (b) determining efficacy of the compound to inhibit growth of a bacteria. Systems of drug development of these antibiotic compounds are also described.

DERIVATIVES OF KORORMICIN USEFUL AS ANTIBIOTICS
20200345682 · 2020-11-05 ·

Described herein is a process for antibiotic development comprising: (a) generating a compound of formula (III):

##STR00001##

or a salt or stereoisomer or prodrug thereof; wherein R.sup.1-R.sup.3 and R.sup.5-R.sup.10 are independently selected from H, alkyl group, substituted alkyl group, halogen, OH, NH.sub.2, or SH; R.sup.4 is H, alkyl group or substituted alkyl group; X.sup.1-X.sup.2 are independently selected from O, S, NH, H, alkyl, halogen, OH, SH, or NH.sub.2; W is a saturated acyclic hydrocarbon chain of 1 to 15 carbon atoms; and Z is a neutral or positively charged organic group comprising a nitrogen or phosphorus atom; and; and (b) determining efficacy of the compound to inhibit growth of a bacteria. Systems of drug development of these antibiotic compounds are also described.

Inhibitors of beta-hydroxylase for treatment of cancer

The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

Inhibitors of beta-hydroxylase for treatment of cancer

The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

Isotopically-Stabilized Tetronimide Compounds
20200262804 · 2020-08-20 ·

Isotopically-stabilized tetronimide compounds comprising one or more deuterium atoms, derivatives, and intermediates, thereof, including methods for their synthesis, pharmaceutical compositions thereof, and methods of using these compounds to interact with target molecules in cell-free samples, cell- and tissue-based assays, animal models, and in a subject are disclosed. One aspect relates to molecules that modulate the expression or catalytic activity of aspartyl (asparaginyl) -hydroxylase (ASPH) within or on the surface of a cell. Other aspects of the invention relate to use of the molecules disclosed herein to diagnose, ameliorate, or treat cell proliferation disorders and related diseases. Related aspects include uses of the compounds to modulate the activity of viruses, as anti-hyperlipidemia agents, and as agents to ameliorate or treat thrombosis and related cardiovascular and metabolic disorders.