Patent classifications
C07D307/66
Isotopically-Stabilized Tetronimide Compounds
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.
Derivatives of korormicin useful as antibiotics
An antibiotic compound of formula (III): ##STR00001##
or a salt or stereoisomer thereof; wherein R.sup.1-R.sup.3 and R.sup.5-R.sup.10 are independently selected from the group consisting of H, alkyl group, substituted alkyl group, halogen, OH, NH.sub.2 and SH; R.sup.4 is H, alkyl group or substituted alkyl group; X.sup.1-X.sup.2 are independently selected from the group consisting of O, S, NH, H, alkyl, halogen, OH, SH and 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. The compounds are useful in treating bacterial diseases.
Derivatives of korormicin useful as antibiotics
An antibiotic compound of formula (III): ##STR00001##
or a salt or stereoisomer thereof; wherein R.sup.1-R.sup.3 and R.sup.5-R.sup.10 are independently selected from the group consisting of H, alkyl group, substituted alkyl group, halogen, OH, NH.sub.2 and SH; R.sup.4 is H, alkyl group or substituted alkyl group; X.sup.1-X.sup.2 are independently selected from the group consisting of O, S, NH, H, alkyl, halogen, OH, SH and 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. The compounds are useful in treating bacterial diseases.
Inhibitors of β-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 β-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.
PHOTOELECTRIC CONVERSION ELEMENT, OPTICAL SENSOR, IMAGING ELEMENT, AND COMPOUND
The invention provides a photoelectric conversion element exhibiting excellent photoelectric conversion efficiency even in a case where the photoelectric conversion film is a thin film. Also, the invention provides an optical sensor and an imaging element including the photoelectric conversion element.
The invention provides a compound applied to the photoelectric conversion element.
The photoelectric conversion element of the invention includes a conductive film, a photoelectric conversion film, and a transparent conductive film, in this order, in which the photoelectric conversion film contains a compound represented by Formula (1).
##STR00001##
PHOTOELECTRIC CONVERSION ELEMENT, OPTICAL SENSOR, IMAGING ELEMENT, AND COMPOUND
The invention provides a photoelectric conversion element exhibiting excellent photoelectric conversion efficiency even in a case where the photoelectric conversion film is a thin film. Also, the invention provides an optical sensor and an imaging element including the photoelectric conversion element.
The invention provides a compound applied to the photoelectric conversion element.
The photoelectric conversion element of the invention includes a conductive film, a photoelectric conversion film, and a transparent conductive film, in this order, in which the photoelectric conversion film contains a compound represented by Formula (1).
##STR00001##
Biguanide compositions and methods of treating metabolic disorders
Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
Biguanide compositions and methods of treating metabolic disorders
Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
Compositions and methods for viral sensitization
Provided are compounds of Formula (II) 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. Compounds of Formula (II): ##STR00001##