14 results about "Dihydropyrimidinuria" patented technology

The present disclosure relates to dihydropyrimidine-2, 4 (1H, 3H) -dione-containing polycyclic compounds, or pharmaceutically acceptable salts thereof, and compositions thereof which are effective to reduce or modulate widely interspaced zinc finger motifs (WIZ) protein expression levels and / or induce fetal hemoglobin (HbF) expression, and also relates to methods of their preparation and their use in treatment of subjects in need.

The present disclosure relates to dihydropyrimidine-2,4(1H,3H)-dione-containing polycyclic compounds, or pharmaceutically acceptable salts thereof, and compositions thereof which are effective to reduce or modulate widely interspaced zinc finger motifs (WIZ) protein expression levels and / or induce fetal hemoglobin (HbF) expression, and also relates to methods of their preparation and their use in treatment of subjects in need.

Disclosed are a dihydropyrimidine based compound, a preparation method therefor and an application thereof, belonging to the technical field of pharmaceutical chemistry. The present invention relates to a dihydropyrimidine based compound, the structure of which is shown in formula I. Also provided in the present invention is an application of the compound represented by formula I, or a salt, solvate, isomer, metabolite, nitrogen oxide and prodrug thereof, in the preparation of a medicament for treating or preventing P2X3 and / or P2X2 / 3 receptor-related diseases. The dihydropyrimidine based compound of the present invention has good P2X3 receptor antagonist activity and improved safety.

The application belongs to the technical field of chemical medicine, and particularly relates to a kind of 2,3-dihydropyrimidino [4,5-d] pyrimidine-4 (1H) -ketone derivatives and preparation method and purposes thereof.The existing Wee1 small molecule inhibitors still have one or more defects in activity, safety or pharmacokinetic properties, and a new generation of Wee1 small molecule inhibitors with novel structure, low toxicity, high efficiency and excellent pharmacokinetic properties needs to be developed.The application provides a kind of 2,3-dihydropyrimidino [4,5-d] pyrimidine-4 (1H) -ketone derivatives, specifically including 95 new compounds, or pharmaceutically acceptable salt thereof, or stereoisomer thereof.Experiments show that the compound of formula (I) disclosed in the application has good inhibitory activity on Wee1, and therefore the compound of the application can be used for treating diseases caused by abnormal Wee1 activity.

The invention relates to a group of dihydropyrimidone compounds, a preparation method of the dihydropyrimidone compounds, a pharmaceutical composition containing the dihydropyrimidone compounds and application of the dihydropyrimidone compounds in pharmacy. Specifically, the compound has structures shown in general formulas (I) and (II), is used for preparing a PCSK9 inhibitor and an LDLR up-regulating agent, and has an excellent treatment effect on hyperlipidemia, fatty liver, atherosclerosis and cardiovascular and cerebrovascular diseases. The invention also relates to a pharmaceutical composition of the compound and a pharmaceutical composition for treating and / or preventing the application. The pharmaceutical composition contains an active component with a therapeutically effective amount and an optional pharmaceutically acceptable carrier.

This disclosure relates to dihydropyrimidine-2,4(1H,3H)-dione-containing polycyclic compounds or pharmaceutically acceptable salts thereof and compositions thereof that effectively reduce or regulate the expression level of broad-space zinc finger motif (WIZ) proteins and / or induce the expression of fetal hemoglobin (HbF), as well as methods for preparing them and their use in the treatment of subjects requiring them.

The invention discloses a dihydropyrimidone-coumarin derivative and a preparation method thereof, and belongs to the technical field of dihydropyrimidone-coumarin derivates. The preparation method comprises the steps that firstly, aromatic aldehyde with different substituent groups and containing hydroxyl, urea and a beta-dicarbonyl compound are subjected to a reaction under the conditions that DES serves as a solvent and p-toluenesulfonic acid monohydrate serves as a catalyst; dihydropyrimidone compounds are obtained through Biginelli condensation, and the dihydropyrimidone compounds and bromomethyl coumarin are synthesized into a series of target compounds through a Williamson ether synthesis method. According to the method, a series of target products capable of efficiently removing DPPH free radicals are obtained, the reaction process is simple, and the used catalyst is non-toxic, harmless, low in price and free of burden on the environment; the structural diversity of the target compound is enriched, and a certain theoretical basis is provided for subsequent development of novel coumarin drugs.

The application discloses a 3,4-dihydropyrimidine-2(1H)-one compound and a preparation method and application thereof. The compound has the structure shown in the formula I. X is selected from halogen. The application provides a series of 3,4-dihydropyrimidine-2(1H)-one compounds with novel structures. The compounds have unique dual-site pH response characteristics and excitation wavelength-dependent luminescence performance, and show high sensitivity and high selectivity to volatile organic amine gas.

The application discloses a dihydropyrimidine[4,5-d]pyrimidine-2(H)-ketone Nrf2 activator and a preparation method and application thereof. The compound has the following structural general formula: experiments prove that the compound can effectively activate the Nrf2 signal pathway to produce an antioxidative stress effect, thereby protecting nerve cells, and can be used for preventing and / or treating neurodegenerative diseases.

The invention discloses dihydropyrimidine (thio) ketone as shown in a general formula I or pharmaceutically acceptable salt thereof, and preparation and antiviral application of the dihydropyrimidine (thio) ketone or the pharmaceutically acceptable salt thereof. The compound has the effects of inhibiting PEDV virus replication and reducing virus titer, is used for preventing and treating PED in the pig breeding industry, and reduces the incidence rate and case fatality rate of PED. # imgabs0 #

The invention provides a dihydropyrimidine derivative containing bithiazolinone, the chemical structural formula of the dihydropyrimidine derivative is as shown in formula (I), in the formula (I), substituent R is H, C1-6 alkyl, F, Cl, Br, I, alkoxy, hydroxyl, nitrile group, nitryl, carboxyl, ester group, amino or sulfonic acid group. The bithiazolinone-containing dihydropyrimidine derivative has certain inhibitory activity on tumor cells, the synthesis method is simple, materials are easy to obtain, and the bithiazolinone-containing dihydropyrimidine derivative can be used for preparing antitumor drugs. # imgabs0 #

The invention provides a dihydropyrimidine compound and a preparation method and application thereof, a dihydropyrimidine derivative and application thereof, and a pharmaceutical composition and application thereof, and relates to the technical field of biological medicines. The dihydropyrimidine compound provided by the invention is high in antiviral activity, particularly high in anti-HBV activity and low in toxicity, can be used for preparing antiviral drugs, and particularly has a very good application prospect when being used for preparing HBV inhibitors.

The present disclosure relates to polycyclic compounds comprising dihydropyrimidine-2, 4 (1H, 3H)-dione, or pharmaceutically acceptable salts thereof, and compositions thereof, which are effective to reduce or modulate the expression level of the widely spaced zinc finger structure motif (WIZ) protein and / or to induce the expression of fetal hemoglobin (HbF), it also relates to methods of their preparation and their use in the treatment of subjects in need thereof.

A compound of formula Ior 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.