An 8-dihalomethyl berberine-type quaternary ammonium salt compound represented by general formula (I) or (II) and an application thereof in preparing a drug. The compound shows hydrophilicity and has antimicrobial, anti-inflammatory, anti-ulcerative colitis, and antitumor activities, while having no or low toxicity.

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The present invention relates to an application of an isoquinoline compound in tumor treatment. Specifically, the present invention provides a use of a compound of formula I, or an optical isomer or a racemate thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof used for the preparation of a composition or formulation for the prevention and/or treatment of a tumor. The compound of the present invention has significant and exceptional therapeutic effects on tumors with low or no expression of an NNMT gene, high expression of a DNA methylase, high expression of UHRF1, high methylation levels at an NNMT gene nucleotide site, and/or high methylation levels at a DNA CpG site in an NNMT gene region.

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts thereof:

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which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts thereof:

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which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Provided are four crystal forms, A, B, C and D, of demethyleneberberine hydrochloride, and a preparation method therefor, and further provided are X-ray powder diffraction characteristic absorption peaks, infrared absorption peaks and DSC spectra of the four crystal forms. The X-ray powder diffraction characteristic diffraction peaks of the crystal forms are at about 8.205, 8.805, 10.817, 14.835, 15.479, 16.668, 17.492, 18.529, 20.656, 21.536, 23.538, 25.657, 26.192, and 28.808. A preparation method for the four crystal forms of the demethyleneberberine hydrochloride is also involved. The preparation method has a simple process, a high yield and a low cost; and has a high product purity and a stable quality.

Provided are four crystal forms, A, B, C and D, of demethyleneberberine hydrochloride, and a preparation method therefor, and further provided are X-ray powder diffraction characteristic absorption peaks, infrared absorption peaks and DSC spectra of the four crystal forms. The X-ray powder diffraction characteristic diffraction peaks of the crystal forms are at about 8.205, 8.805, 10.817, 14.835, 15.479, 16.668, 17.492, 18.529, 20.656, 21.536, 23.538, 25.657, 26.192, and 28.808. A preparation method for the four crystal forms of the demethyleneberberine hydrochloride is also involved. The preparation method has a simple process, a high yield and a low cost; and has a high product purity and a stable quality.

The present invention provides a tetrahydroprotoberberine compound represented by the formula (I), enantiomers, diastereomers, racemates and mixtures thereof, and pharmaceutically acceptable salts, crystalline hydrates and solvates thereof. The invention also provides a method for preparing the compound and the use thereof in the preparation of a medicament for preventing and/or treating central nervous system diseases.

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The present invention provides a tetrahydroprotoberberine compound represented by the formula (I), enantiomers, diastereomers, racemates and mixtures thereof, and pharmaceutically acceptable salts, crystalline hydrates and solvates thereof. The invention also provides a method for preparing the compound and the use thereof in the preparation of a medicament for preventing and/or treating central nervous system diseases.

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This present application relates to fluorescent tetrazine-containing compounds consisting of a single pi-system. For example, a compound of Formula (I):

F-L-Tz

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.

This present application relates to fluorescent tetrazine-containing compounds consisting of a single pi-system. For example, a compound of Formula (I):

F-L-Tz

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.