C07C323/53

FATTY ACID DERIVATIVE LABELED WITH POSITRON-EMITTING RADIONUCLIDE
20230065079 · 2023-03-02 ·

[Problem] To provide a labeled fatty acid derivative for diagnostic imaging that enables the quantification of myocardial fatty acid metabolic activity. [Solution] The inventors, engaging in diligent research into methods that enable the quantification of fatty acid metabolic activity, discovered that a labeled fatty acid derivative represented by formula (1), in which [.sup.18F] has been substituted at a specific position of a long-chain carboxylic acid compound containing a sulfur atom, or a salt thereof, has good accumulation in the myocardium, and enables imaging of fatty acid metabolic activity via positron emission tomography (PET). Therefore, the labeled fatty acid derivative according to the present invention can be used as a radiotracer for swift and noninvasive quantification of myocardial fatty acid metabolic activity, diagnostic imaging of heart diseases such as ischemic heart disease, diagnostic imaging of the therapeutic effects yielded by a heart disease therapeutic agent, and so forth.

FATTY ACID DERIVATIVE LABELED WITH POSITRON-EMITTING RADIONUCLIDE
20230065079 · 2023-03-02 ·

[Problem] To provide a labeled fatty acid derivative for diagnostic imaging that enables the quantification of myocardial fatty acid metabolic activity. [Solution] The inventors, engaging in diligent research into methods that enable the quantification of fatty acid metabolic activity, discovered that a labeled fatty acid derivative represented by formula (1), in which [.sup.18F] has been substituted at a specific position of a long-chain carboxylic acid compound containing a sulfur atom, or a salt thereof, has good accumulation in the myocardium, and enables imaging of fatty acid metabolic activity via positron emission tomography (PET). Therefore, the labeled fatty acid derivative according to the present invention can be used as a radiotracer for swift and noninvasive quantification of myocardial fatty acid metabolic activity, diagnostic imaging of heart diseases such as ischemic heart disease, diagnostic imaging of the therapeutic effects yielded by a heart disease therapeutic agent, and so forth.

Sulfide alkyl compounds for HBV treatment

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.

Sulfide alkyl compounds for HBV treatment

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.

SULFIDE ALKYL COMPOUNDS FOR HBV TREATMENT

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.

SULFIDE ALKYL COMPOUNDS FOR HBV TREATMENT

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.

UNSATURATED AMINO ACIDS

There is provided a method of producing at least one unsaturated amino acid from at least one amino acid comprising at least two carbonyl groups, the method comprising (a) contacting a recombinant microbial cell with a medium comprising the amino acid comprising the carbonyl groups, wherein the cell is genetically modified to compriseat least a first genetic mutation that increases the expression relative to the wild type cell of an enzyme (E) selected from the CYP152 10 peroxygenase family, andat least a second genetic mutation that increases the expression relative to the wild type cell of at least one NAD(P)+ oxidoreductase (E2) and the corresponding mediator protein.

UNSATURATED AMINO ACIDS

There is provided a method of producing at least one unsaturated amino acid from at least one amino acid comprising at least two carbonyl groups, the method comprising (a) contacting a recombinant microbial cell with a medium comprising the amino acid comprising the carbonyl groups, wherein the cell is genetically modified to compriseat least a first genetic mutation that increases the expression relative to the wild type cell of an enzyme (E) selected from the CYP152 10 peroxygenase family, andat least a second genetic mutation that increases the expression relative to the wild type cell of at least one NAD(P)+ oxidoreductase (E2) and the corresponding mediator protein.

TERTIARY AMIDES AND METHOD OF USE

Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein G.sup.1, G.sup.2, G.sup.3, L.sup.1, L.sup.2, and L.sup.3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by the modulation of lysophosphatidic acid receptor 1. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

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Biaryl derivatives as GPR120 agonists

The present invention relates to biaryl derivatives of Formula 1, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The biaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in the liver or in muscle due to anti-inflammatory action in macrophages, lipocytes, etc., and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, obesity, non-alcoholic fatty liver, steatohepatitis, osteoporosis or inflammation.