Abstract: The present disclosure relates to compounds for RNA capping and uses thereof, which belong to the technical field of genetic engineering. Compounds of formula I can result in high levels of capping efficiency, and the capped mRNA exhibits a high transcription level and increased expression.

Abstract: A novel imidazothiazole compound as an Autotaxin inhibitor, a pharmaceutical composition including the compound, and a use thereof in a treatment of a disease with a pathological feature of Autotaxin overexpression in a mammal is provided, wherein the compound has a structure of formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, tautomer, nitrogen oxide, metabolite, prodrug, or mixture thereof; wherein each of R1a, R1c, R2, R3, R6, Cy, Y, Z, and t is defined as described in the present disclosure.

Abstract: A novel tetrahydronaphthalene compound is provided, or a stereoisomer, a solvate, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition including the compound, and a use of the compound or the composition for preparing a medicament in prevention and/or treatment of a central nervous system disease, wherein the compound has a structure of formula (I), wherein each of X, Y, Z, W and R is defined as described in the present disclosure.

Abstract: The present disclosure relates to compounds for RNA capping and uses thereof, which belong to the technical field of genetic engineering. Compounds of formula I can result in high levels of capping efficiency, and the capped mRNA exhibits a high transcription level and increased expression.

Abstract: Provided are novel heteroaromatic compound as an Autotaxin inhibitor, a pharmaceutical composition comprising the compound, and a use thereof in a treatment of a disease with a pathological feature of Autotaxin overexpression in a mammal, wherein the compound is according to formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, tautomer, nitrogen oxide, metabolite, prodrug, or mixture thereof; wherein each of R1, Ar1, Ar2, Ar3, W, Y, Z, and Cy is defined in the present disclosure.

Abstract: Provided are a long-acting prodrug of Rasagiline, which has application in the treatment of Central Nervous System diseases such as Parkinson's disease, preparation method and use thereof. The long-acting prodrug of Rasagiline has a structure of formula (I), wherein T is absent, or T is selected from each of R1 and R2 is independently selected from H, D, and alkyl; W is absent, or W is selected from (CH2)n, wherein n is an integer selected from 1 to 15; X is absent, or X is selected from (CH2)m, wherein m is an integer selected from 1 to 10; Y is absent, or Y is selected from —C(?O)NH—, —NHC(?O)—; R3 is selected from substituted or unsubstituted C1-C30 alkyl, substituted or unsubstituted C2-C30 alkenyl, substituted or unsubstituted C2-C30 alkynyl, substituted or unsubstituted C3-C30 cycloalkyl, cholane aliphatic group, —R3a—C(?O)O—R3b, —R3a—OC(?O)—R3b, —R3a—C(?O)NH—R3b, —R3a—NHC(?O)—R3b, —R3a—S(?O)1-2O—R3b and —R3a—OS(?O)1-2—R3b.

Abstract: Provided are a long-acting prodrug of Entecavir, preparation method and use thereof, wherein the prodrug of Entecavir has a structure of formula I. The prodrug of Entecavir can be released slowly, sustainably and steady, and converted to active compound of Entecavir to achieve a long-acting effect.

Abstract: Provided are novel heteroaromatic compound as an Autotaxin inhibitor, a pharmaceutical composition comprising the compound, and a use thereof in a treatment of a disease with a pathological feature of Autotaxin overexpression in a mammal, wherein the compound is according to formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, tautomer, nitrogen oxide, metabolite, prodrug, or mixture thereof; wherein each of R1, Ar1, Ar2, Ar3, W, Y, Z, and Cy is defined in the present disclosure.

Abstract: A cyclohexene compound and use thereof, which relates to the technical field of pharmaceutical chemistry is provided. The cyclohexene compound is the cyclohexene compound having a structural formula I or a pharmaceutically acceptable salt, an ester group prodrug or a stereoisomer thereof. It is verified by activity assay for influenza NA that the cyclohexene compound has a great inhibiting activity against both wild-typed and drug-resistant influenza viruses, and the inhibiting activity IC50 of some compounds against wild-typed and drug-resistant influenza viruses is lower than 5 nM, showing significant inhibiting effect on influenza viruses. This shows that the cyclohexene compound or a pharmaceutically acceptable salt or a stereoisomer thereof has superior application prospect on preparing anti-influenza drugs, thereby providing a new drug choice for treating influenza clinically.

Abstract: A method for preparing a pyrimidone compound and an important intermediate in which raw materials of the preparation method are cheap, the reaction condition of preparation method is mild, the preparation method is simple to operate, and is safe and controllable, has high total yield, and thus is suitable for industrial production.

Abstract: Provided are a long-acting prodrug of Rasagiline, which has application in the treatment of Central Nervous System diseases such as Parkinson's disease, preparation method and use thereof. The long-acting prodrug of Rasagiline has a structure of formula (I), wherein T is absent, or T is selected from each of R1 and R2 is independently selected from H, D, and alkyl; W is absent, or W is selected from (CH2)n, wherein n is an integer selected from 1 to 15; X is absent, or X is selected from (CH2)m, wherein m is an integer selected from 1 to 10; Y is absent, or Y is selected from —C(?O)NH—, —NHC(?O)—; R3 is selected from substituted or unsubstituted C1-C30 alkyl, substituted or unsubstituted C2-C30 alkenyl, substituted or unsubstituted C2-C30 alkynyl, substituted or unsubstituted C3-C30 cycloalkyl, cholane aliphatic group, —R3a—C(?O)O—R3b, —R3a—OC(?O)—R3b, —R3a—C(?O)NH—R3b, —R3a—NHC(?O)—R3b, —R3a—S(?O)1-2O—R3b and —R3a—OS(?O)1-2—R3b.

Abstract: Provided are a long-acting prodrug of Entecavir, preparation method and use thereof, wherein the prodrug of Entecavir has a structure of formula I. The prodrug of Entecavir can be released slowly, sustainably and steady, and converted to active compound of Entecavir to achieve a long-acting effect.

Abstract: A method for preparing a pyrimidone compound and an important intermediate in which raw materials of the preparation method are cheap, the reaction condition of preparation method is mild, the preparation method is simple to operate, and is safe and controllable, has high total yield, and thus is suitable for industrial production.

Abstract: Provided are salts of 2,6-dimethylpyrimidone derivatives and uses thereof. Also provided are pharmaceutical compositions containing the salts.

Abstract: The invention relates to capthepsin K inhibitors and uses thereof, specifically relates to a class of compounds having the formula (I) which are used for treating or preventing cathepsin dependent diseases or conditions, specifically, wherein the cathepsin is capthepsin K. The compounds and compositions thereof can be used as bone resorption inhibitors for the treatment of associated diseases.

Abstract: Provided are salts of 2, 6-dimethylpyrimidone derivatives and uses thereof. Also provided are pharmaceutical compositions containing the salts.

Abstract: A cyclohexene compound and use thereof, which relates to the technical field of pharmaceutical chemistry is provided. The cyclohexene compound is the cyclohexene compound having a structural formula I or a pharmaceutically acceptable salt, an ester group prodrug or a stereoisomer thereof. It is verified by activity assay for influenza NA that the cyclohexene compound has a great inhibiting activity against both wild-typed and drug-resistant influenza viruses, and the inhibiting activity IC50 of some compounds against wild-typed and drug-resistant influenza viruses is lower than 5 nM, showing significant inhibiting effect on influenza viruses. This shows that the cyclohexene compound or a pharmaceutically acceptable salt or a stereoisomer thereof has superior application prospect on preparing anti-influenza drugs, thereby providing a new drug choice for treating influenza clinically.

Abstract: A cyclohexene derivative or pharmaceutically acceptable salt thereof and application thereof, which belongs to the technical field of pharmaceutical technology is provided. The cyclohexene derivative of formula I or pharmaceutically acceptable salt thereof is a new broad-spectrum anti-influenza compound, having a great inhibiting effect on influenza viruses, specifically, it has a high activity to virus strains which is drug-resistant to Oseltamivir, and may be used as a broad-spectrum anti-influenza NA inhibitor effective to Tamiflu drug-resistance, for treating the flu caused by influenza viruses, thereby it is a broad-spectrum anti-influenza drug.

Abstract: Provided is a modulator of FXR receptor and preparation and use thereof, which relates to the technical filed of medicinal chemistry. The embodiment provides a modulator of FXR receptor having a structural formula I or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, which can combine with FXR receptor (that is NR1H4) and be acted as a FXR agonist or a partial agonist for preventing and treating the disease mediated by FXR, such as chronic intrahepatic or extrahepatic cholestasis, hepatic fibrosis caused by chronic cholestasis or acute intrahepatic cholestasis, chronic hepatitis B, gallstone, hepatic carcinoma, colon cancer or intestinal inflammatory disease, etc. Specifically, for some chemical compounds, their EC50 for FXR agonist activity reach below 100 nM, which show an excellent FXR agonist activity and an excellent prospect to provide a new pharmaceutical selection in clinical treatment for the disease mediated by FXR.

Abstract: Provided are a nimodipine water-soluble derivative, and a preparation method and a use thereof, belonging to the field of pharmaceutical chemistry. The nimodipine water-soluble derivative has the structural feature of general formula I and has a relatively high water solubility, and can be converted into nimodipine by an internal enzyme in blood or in the body, so that the nimodipine water-soluble derivative can be used as a nimodipine prodrug and a calcium ion antagonist for treating cardiovascular and cerebrovascular diseases.