Patent classifications
C07C49/835
CHALCONES AND DERIVATIVES FOR USE IN MEDICAMENTS AND NUTRACEUTICALS
Provided herein are means and methods for inhibiting processes and/or facilitating processes in cells by means of a compound of structural formula I
##STR00001##
wherein R1, R2, R3, R4, R5 and R6 are each independently H, OH, CH3, OCH3, a monosaccharide, an oligosaccharide or Cl; with the proviso that at least two of R1-R6 are H; and at least one other of R1-R6 is OH. The compound can be used among others in the prophylactic or curative treatment of an elevated blood interleukin-1β level and/or the treatment of low grade inflammation in an animal subject in need thereof. Also provided is a method for increasing longevity or increasing the health span in a non-diseased animal subject, the method including administering to the animal subject an effective amount of a hydroxychalcone of formula I as indicated herein. Also provided are food and food supplements including a compound of formula I as indicated herein.
Notch inhibitors for use in the treatment of t-cell acute lymphoblastic leukemia
Compounds of formula (I) in the capacity of compounds with anti-tumor activity for the treatment of T-cell acute lymphoblastic leukemia (T-ALL). ##STR00001##
Notch inhibitors for use in the treatment of t-cell acute lymphoblastic leukemia
Compounds of formula (I) in the capacity of compounds with anti-tumor activity for the treatment of T-cell acute lymphoblastic leukemia (T-ALL). ##STR00001##
SUBSTITUTED ALKYLPHENOLS AS HCN1 ANTAGONISTS
Provided herein are compounds (e.g., compounds of Formula (I) and Formula (II), that modulate HCN channels, intermembrane proteins that serve as nonselective voltage-gated cation channels in the plasma membranes of heart and brain cells. Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating HCN-related disorders (e.g., pain) with the compounds in a subject, by administering the compounds and/or compositions described herein.
Isopentenyl chalcone compound and preparation method thereof
A method for preparing 2,2′,4,4′-tetrahydroxy-3′-(2″,3″-dihydroxy-3″-methylbutyl)chalcone includes the following steps: subjecting a Morus alba leaf to extraction with an aqueous solution of methanol or ethanol having a volume fraction of 40%-100%, concentrating an extract to remove methanol or ethanol and dissolving in water, subjecting to extraction with petroleum ether and ethyl acetate successively, and concentrating an ethyl acetate extract to obtain a paste; chromatographing the paste over a silica gel column using chloroform-methanol, collecting an eluate where the volume ratio of chloroform-methanol is 95/5; chromatographing the eluate over a reversed-phase column using acetonitrile-water, collecting an eluate where the volume ratio of acetonitrile-water is 33/67, and thereby the compound is obtained.
Isopentenyl chalcone compound and preparation method thereof
A method for preparing 2,2′,4,4′-tetrahydroxy-3′-(2″,3″-dihydroxy-3″-methylbutyl)chalcone includes the following steps: subjecting a Morus alba leaf to extraction with an aqueous solution of methanol or ethanol having a volume fraction of 40%-100%, concentrating an extract to remove methanol or ethanol and dissolving in water, subjecting to extraction with petroleum ether and ethyl acetate successively, and concentrating an ethyl acetate extract to obtain a paste; chromatographing the paste over a silica gel column using chloroform-methanol, collecting an eluate where the volume ratio of chloroform-methanol is 95/5; chromatographing the eluate over a reversed-phase column using acetonitrile-water, collecting an eluate where the volume ratio of acetonitrile-water is 33/67, and thereby the compound is obtained.
Anti-fungal compounds
The present disclosure provides compounds of the formula (I), (II), (III), wherein the variables are as defined herein for use in the treatment of fungal infections. In some embodiments, the fungal infection is an infection of Cryptococcus neojormans fungus. Also provided herein are compositions comprising a compound of formula I, II, or III and a second anti-fungal agent. ##STR00001##
Anti-fungal compounds
The present disclosure provides compounds of the formula (I), (II), (III), wherein the variables are as defined herein for use in the treatment of fungal infections. In some embodiments, the fungal infection is an infection of Cryptococcus neojormans fungus. Also provided herein are compositions comprising a compound of formula I, II, or III and a second anti-fungal agent. ##STR00001##
STREPTOCOCCUS MUTANS GLUCOSYL TRANSFERASE INHIBITORS FOR DENTAL CARIES THERAPY
The present invention is related to the inhibition of the formation of Streptococci biofilms through the inhibition of glucosyl transferase (Gtf). Compounds, compositions and methods for inhibiting Streptococcus biofilm formation, as well as for preventing, inhibiting and/or treating the formation of dental caries, and methods of identifying compounds that prevent, inhibit and/or treat the formation of dental caries are provided.
DIARYLALKANES AS POTENT INHIBITORS OF BINUCLEAR ENZYMES
The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compoundsdiarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.