C07D455/03

Bioorthogonal turn-on probes

This present application relates to fluorescent tetrazine-containing compounds consisting of a single pi-system. For example, a compound of Formula (I): or a salt thereof, wherein: F is a fluorophore, L is a conjugated linker, and Tz is a substituted or unsubstituted tetrazine; wherein the linker bridges the Tz and F moieties in a single conjugated pi-system. Also provided herein are methods of using the compounds provided herein for biomedical imaging.

ISOQUINOLINONE COMPOUNDS AND USE THEREOF IN PREPARATION OF ANTIVIRAL DRUGS
20190381014 · 2019-12-19 ·

Disclosed is an isoquinolinone compound as shown in Formula (I) or a stereoisomer, pharmaceutically acceptable salt, solvate or crystal thereof, and a preparation method thereof, and use thereof in the preparation of drugs for treating or preventing viral infectious diseases caused by the hepatitis B virus (HBV) and other viruses, in particular, use thereof in drugs as HBV surface antigen inhibitors and HBV DNA production inhibitors. The compound has a significant activity in inhibiting hepatitis B surface antigen and hepatitis B DNA, and is possible to significantly improve the probability of curing hepatitis B by administration in combination with nucleoside drugs or other drugs in the future, and has good clinical application prospects.

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CRYSTAL FORM OF COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention discloses a crystal form A of a compound, where the compound is S-()-2,3-methylenedioxy-5,8,13,13a-tetrahydro-10,11-dimethoxy-6H-dibenzo[a,g]quinolizine, and an X-ray powder diffraction pattern of the crystal form A includes three or more 2 values selected from the group consisting of: 12.210.2, 13.3810.2, 15.1810.2, 16.1710.2, 17.1010.2, 19.8010.2, 21.5110.2, 24.3910.2, and 25.3210.2. The crystal form A of the compound of the present invention does not contain water and a solvent, has high stability and low hygroscopicity, and is suitable for patent medicine.

COMPOUND, LIGHT EMITTING MATERIAL AND ORGANIC LIGHT EMITTING ELEMENT

A compound having a structure, represented by the following general formula is useful as a light emitting material. At least one of R.sup.1 to R.sup.9 is a substituent; Y.sup.1 to Y.sup.3 each are a methylene group, a carbonyl group, a thiocarbonyl group, an imino group, an oxygen atom, a sulfur atom or a sulfonyl group; Z is a nitrogen atom, a boron atom or a phosphine oxide group.

Crystal form of compound, and preparation method therefor and use thereof

The present invention discloses a crystal form A of a compound, where the compound is S-(?)-2,3-methylenedioxy-5,8,13,13a-tetrahydro-10,11-dimethoxy-6H-dibenzo[a, g]quinolizine, and an X-ray powder diffraction pattern of the crystal form A includes three or more 2? values selected from the group consisting of: 12.21?0.2?, 13.381?0.2?, 15.181?0.2?, 16.171?0.2?, 17.101?0.2?, 19.801?0.2?, 21.511?0.2?, 24.391?0.2?, and 25.321?0.2?. The crystal form A of the compound of the present invention does not contain water and a solvent, has high stability and low hygroscopicity, and is suitable for patent medicine.

COMPOSITION FOR PREVENTING OR TREATING DISEASES CAUSED BY MITOCHONDRIAL DYSFUNCTION, CONTAINING ISOQUINOLINE DERIVATIVE COMPOUND AS ACTIVE INGREDIENT

The present invention relates to a composition for preventing or treating diseases caused by mitochondrial dysfunction, containing, as an active ingredient, an isoquinoline derivative compound represented by chemical formula 1, or a pharmaceutically acceptable salt thereof, and does not induce mitochondrial damage, unlike conventional mitochondrial toxins such as CCCP, and specifically and excellently promotes the activity of mitophagy to alleviate mitochondrial disfunction, and thus can be effectively used in the treatment of diseases caused by mitochondrial dysfunction.

COMPOSITION FOR PREVENTING OR TREATING DISEASES CAUSED BY MITOCHONDRIAL DYSFUNCTION, CONTAINING ISOQUINOLINE DERIVATIVE COMPOUND AS ACTIVE INGREDIENT

The present invention relates to a composition for preventing or treating diseases caused by mitochondrial dysfunction, containing, as an active ingredient, an isoquinoline derivative compound represented by chemical formula 1, or a pharmaceutically acceptable salt thereof, and does not induce mitochondrial damage, unlike conventional mitochondrial toxins such as CCCP, and specifically and excellently promotes the activity of mitophagy to alleviate mitochondrial disfunction, and thus can be effectively used in the treatment of diseases caused by mitochondrial dysfunction.

Pharmaceutical composition comprising berberine and ursodeoxycholic acid for the treatment of various diseases or disorders

The invention provides various novel compositions of berberine in combination with pharmacologically active organic acids, and related methods of their use in treating various diseases or disorders. The invention further provides various novel compounds prepared from berberine and pharmacologically active organic acids and prepared from ursodeoxycholic acid and pharmacologically active organic bases, and pharmaceutical compositions thereof, and methods of their preparation and therapeutic use in treating and/or preventing various diseases or disorders. The compounds and pharmaceutical compositions of the invention can be utilized to treat various diseases or disorders, such as diabetes, diabetic complications, dyslipidemia, hyperlipidemia, obesity, metabolic syndromes, pre-diabetes, atherosclerosis, heart diseases, neurodegenerative diseases, sarcopenia, muscle atrophy, inflammation, cancer and liver diseases and conditions such as fatty liver, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, cholestatic liver diseases or graft-versus-host disease of the liver. The compounds of this invention are also useful in improving liver functions in chronic viral associated liver diseases and alcohol-related liver diseases.

Pharmaceutical composition comprising berberine and ursodeoxycholic acid for the treatment of various diseases or disorders

The invention provides various novel compositions of berberine in combination with pharmacologically active organic acids, and related methods of their use in treating various diseases or disorders. The invention further provides various novel compounds prepared from berberine and pharmacologically active organic acids and prepared from ursodeoxycholic acid and pharmacologically active organic bases, and pharmaceutical compositions thereof, and methods of their preparation and therapeutic use in treating and/or preventing various diseases or disorders. The compounds and pharmaceutical compositions of the invention can be utilized to treat various diseases or disorders, such as diabetes, diabetic complications, dyslipidemia, hyperlipidemia, obesity, metabolic syndromes, pre-diabetes, atherosclerosis, heart diseases, neurodegenerative diseases, sarcopenia, muscle atrophy, inflammation, cancer and liver diseases and conditions such as fatty liver, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, cholestatic liver diseases or graft-versus-host disease of the liver. The compounds of this invention are also useful in improving liver functions in chronic viral associated liver diseases and alcohol-related liver diseases.

DEUTERATED COMPOUNDS AND MEDICAL USES THEREOF
20190240204 · 2019-08-08 ·

The present disclosure relates to a compound of Formula I or a non-toxic pharmaceutically acceptable salt or solvate thereof, wherein each R1, R2, R3, and R4 is independently selected from methyl (CH.sub.3) and trideuteromethyl (CD.sub.3), at least one of R1, R2, R3, and R4 is selected from trideuteromethyl (CD.sub.3).

The compound is a deuterated derivative of L-tetrahydropalmatine, which not only markedly improves pharmacological effects, but also significantly reduces cardiac side effects, liver toxicity, and remarkably decreases individual differences.

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