32 results about "Dihydropyrimidinuria" patented technology

The present invention is directed in part towards methods of modulating the function of calcium channels with pyrimidine-based compounds. In addition, the invention describes methods of preventing and treating calcium channel-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyrimidine-based compounds and pharmaceutical compositions comprising these compounds.

Provided herein are dihydropyrimidine compounds and their pharmaceutical applications, especially for use in treating and preventing HBV diseases. Specifically, provided herein are compounds having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, wherein the variables of the formulas are as defined in the specification. Also provided herein is the use of the compounds having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof for treating and preventing HBV diseases.

Disclosed are salts of dihydropyrimidine derivative and uses thereof in medicine. Specifically, it relates to citric acid complex, acid addition salt of 3-((R)-4-(((R)-6-(2-bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic acid or tautomer thereof, or crystalline form thereof, and pharmaceutically compositions thereof.

The invention discloses a dihydropyrimidine-sulfonamide derivative, a preparation method and application thereof. The compound has the structure shown in formula I. The present invention also relates to a preparation method containing the compound of formula I, a pharmaceutical composition and the application of the above compound in the preparation of anti-HBV medicines.

A dihydropyrimidine compound and a pharmaceutical application thereof, especially the application used for treating and preventing HBV diseases. Specifically, a compound having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, wherein the variables of the formulas are as defined in the specification. Also, use of the compound having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof as a medicine, especially for treating and preventing HBV diseases.

Disclosed are a solid form of (E)-3-((R)-4-(((R)-6-(2-chloro-4-fluorophenyl)-5-(methoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)acrylic acid, a preparation method therefor, a pharmaceutical composition comprising same, and the use thereof in the preparation of drugs for preventing or treating viral diseases.

The invention discloses a dihydropyrimidine-triazole derivative, a preparation method therefor and an application of the dihydropyrimidine-triazole derivative. The compound has a structure represented by a formula I shown in the description. The invention further relates to the preparation method for the compound with the structure represented by the formula I and a pharmaceutical composition and provides the application of the compound in preparation of anti-HBV drugs.

Provided herein are dihydropyrimidine derivatives which are useful in the treatment of HBV infection or HBV-induced diseases, as well as pharmaceutical or medical applications thereof.

The invention discloses a dihydropyrimidine compound, a preparation method and an application thereof, and belongs to the technical field of medicinal chemistry. The structure of the dihydropyrimidine compounds provided by the present invention is shown in Formula I. The invention also discloses a preparation method of the dihydropyrimidine compound. The present invention provides the application of the compound represented by formula I or its salt, solvate, isomer, metabolite, nitrogen oxide and prodrug in the preparation of medicines for treating or preventing P2X3 and / or / P2X2 / 3 receptor-related diseases . The antitussive action time of the compound of the present invention is significantly longer than that of the compound of Comparative Example 1; the inhibitory activity to P2X3 is better than that of the compound of Comparative Example 1 and the positive control drug gefapixant, and it has almost no effect on the taste of mice under 10mg / kg intravenous administration, which is comparable to that of the compound of Comparative Example 1. The positive control drug gefapixant had a statistically significant difference.

The present invention provides a pharmaceutical composition, as an effective ingredient, a urea compound having a protein kinase inhibitory activity and containing a 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one skeleton, and a pharmaceutically acceptable salt thereof.

The present invention provides a composition containing orlistat and dihydropyrimidine compounds, and the specific definition of the dihydropyrimidine compounds is shown in the specification: the results of in vitro tests show that orlistat and the dihydropyrimidine compounds of the present invention The pyrimidine compounds can synergistically inhibit the replication of HBV DNA in Hep G2.2.15 cells within the stated molar ratio (combination index CI<1).

The invention provides a dihydropyrimidine-spiro derivative and its preparation method and application. The compound has the structure shown in formula I. The present invention also relates to a preparation method containing the compound of formula I, a pharmaceutical composition and the application of the above compound in the preparation of anti-HBV medicines.

A compound of formula (I) or a pharmaceutically acceptable salt thereof. The compound is useful in therapy, e.g. for the treatment of cancers, inflammation, autoimmune diseases and graft-versus host diseases (e.g. in transplantation patients). A pharmaceutical composition comprising the compound or its salt and a method for preparing the compound.

The present invention proposes a FGFR4 inhibitor with 3,4-dihydropyrimidin[4,5-d]pyrimidin-2(1H)-one as the core and a covalent structure. The embodiment gives 9 specific compounds and tested the kinase inhibitory activity of these 9 compounds, wherein the half-inhibitory concentration of LX08 to the FGFR4 kinase inhibitory activity is only 7nM, which is lower than the FIIN-2 of the active control, and has potential application prospects . In addition, by performing MALDI-TOF mass spectrometry binding experiments on the synthesized compounds, we found that compounds such as LX01, LX05, LX06, LX07, and LX08 can only covalently bind to Cys552 in FGFR4, but cannot covalently bind to Cys477 in FGFR4, while LX09 is a FGFR4 inhibitor that can covalently bind to two cysteines Cys552 and Cys477 in FGFR4.