摘要：【中文】本发明涉及一种稠合三环类化合物及其在药物中的应用，尤其是作为用于治疗和/或预防乙型肝炎的药物的应用。具体地说，本发明涉及通式(I)所示化合物或其立体异构体、互变异构体、氮氧化物、溶剂化物、代谢产物、药学上可接受的盐或它的前药，其中各变量如说明书所定义。本发明还涉及通式(I)所示化合物或其立体异构体、互变异构体、氮氧化物、溶剂化物、代谢产物、药学上可接受的盐或它的前药作为药物的用途，尤其是作为用于治疗和/或预防乙型肝炎的药物的用途。 【EN】The invention relates to a fused tricyclic compound and application thereof in medicines, in particular to application of the fused tricyclic compound as a medicine for treating and/or preventing hepatitis B. Specifically, the invention relates to a compound shown in a general formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein variables are defined in the specification. The invention also relates to a compound shown in the general formula (I) or a stereoisomer and a tautomer thereofThe use of a construct, nitrogen oxide, solvate, metabolite, pharmaceutically acceptable salt or prodrug thereof as a medicament, in particular for the treatment and/or prevention of hepatitis b.

摘要：【中文】本发明涉及一种巴洛沙韦中间体的制备方法，属于药物化学领域。所述制备方法包括采用式(A)化合物作为起始物料，经过卤代反应、格氏反应、卤代反应、亲核取代、傅克酰基化扣环等步骤得到式(G)化合物。本发明提供的制备方法具有成本低、安全、环境友好、收率高、纯度高等优点，适合工业化放大生产。 【EN】The invention relates to a preparation method of a baroxavir intermediate, belonging to the field of pharmaceutical chemistry. The preparation method comprises the steps of adopting the compound of the formula (A) as a starting material, and carrying out halogenation reaction, Grignard reaction, halogenation reaction, nucleophilic substitution, Friedel-crafts acylation retaining ring and the likeTo obtain the compound of formula (G). The preparation method provided by the invention has the advantages of low cost, safety, environmental friendliness, high yield, high purity and the like, and is suitable for industrial large-scale production.

摘要：【中文】本发明提供了一种奎宁酮衍生物的制备方法，属于医药化工领域；本发明所述方法通过将二乙醇胺衍生物为起始物料，经过氯代或者甲磺酸、与丙二酸二乙酯环合、Dieckmann Condensation、得到3‑奎宁酮衍生物。该方法生产得到的产物纯度高，收率高，成本低，操作简单，工艺稳定的特点。 【EN】The invention provides a preparation method of a quininone derivative, belonging to the field of pharmaceutical chemicals; according to the method, a diethanolamine derivative is taken as a starting material, and the 3-quininone derivative is obtained through cyclization with diethyl malonate by chloro or methanesulfonic acid and Dieckmann Condensation. The method has the advantages of high product purity, high yield, low cost, simple operation, and stable process.

摘要：【中文】本发明涉及苯甲酰氨基吡啶衍生物的晶型及其用途。本发明还涉及包含所述晶型的药物组合物，以及所述晶型或所述药物组合物在制备用于预防、治疗或减轻患者由ASK1调节的疾病的药物中的用途。 【EN】The invention relates to a crystal form of a benzoylaminopyridine derivative and application thereof. The invention also relates to a pharmaceutical composition containing the crystal form, and application of the crystal form or the pharmaceutical composition in preparing a medicament for preventing, treating or relieving the ASK 1-regulated diseases of patients.

摘要：【中文】本发明涉及一种美托洛尔缓释组合物及其制备方法，属于药物制剂领域。所述组合物，含有美托洛尔或其药学上可接受的盐和控释材料，任选地含有润滑剂和/或增塑剂。所述组合物可以采用热熔挤出制备。所述组合物易于制备，制备方法，简便易行，工序少，时间短，成本低，适于工业化生产。 【EN】The invention relates to a metoprolol sustained-release composition and a preparation method thereof, belonging to the field of pharmaceutical preparations. The composition comprises metoprolol or pharmaceutically acceptable salt thereof and a controlled release material, and optionally comprises a lubricant and/or a plasticizer. The composition may be prepared by hot melt extrusion. The composition is easy to prepare, the preparation method is simple and easy to implement, the working procedures are few, the time is short, the cost is low, and the composition is suitable for industrial production.

摘要：【中文】本发明提供了一种伐度司他的制备方法，属于医药化工领域；本发明所述方法通过将3,5‑二氯‑2‑吡啶甲酸、甲醇和硫酸在一定的温度下混合进行反应后，得到3,5‑二氯‑2‑吡啶甲酸甲酯；然后加入3‑氯苯硼酸，经催化反应，反应完毕后，得到5‑(3‑氯苯基)‑3‑氯吡啶‑甲酸甲酯；将上述5‑(3‑氯苯基)‑3‑氯吡啶‑甲酸甲酯，加入甘氨酸，反应得到5‑(3‑氯苯基)‑3‑氯吡啶‑甲酸甲酯。该方法生产得到的产物纯度高，收率高，成本低，操作简单，工艺稳定的特点。 【EN】The invention provides a preparation method of kovar staphylol, belonging to the field of pharmaceutical chemicals; the method comprises the steps of mixing 3, 5-dichloro-2-picolinic acid, methanol and sulfuric acid at a certain temperature for reaction to obtain 3, 5-dichloro-2-picolinic acid methyl ester; then adding 3-chlorobenzeneboronic acid, and obtaining 5- (3-chlorphenyl) -3-chloropyridine-methyl formate after the reaction is finished through catalytic reaction; and adding glycine into the 5- (3-chlorphenyl) -3-chloropyridine-methyl formate to react to obtain the 5- (3-chlorphenyl) -3-chloropyridine-methyl formate. The method has the advantages of high product purity, high yield, low cost, simple operation, and stable process.

摘要：【中文】本发明提供了一种泰拉霉素的制备方法，属于医药化工领域；本发明所述方法以氮红霉素为原料与氯甲酸苯酯反应保护羟基得到保护的氮红霉素，通过氧化将羟基氧化为酮基，再环氧化、脱保护后，与正丙胺反应得到泰拉霉素。该方法生产得到的产物纯度高，收率高，成本低，操作简单，工艺稳定的特点。 【EN】The invention provides a preparation method of tulathromycin, belonging to the field of pharmaceutical chemicals; the method comprises the steps of reacting erythromycin azoxide serving as a raw material with phenyl chloroformate to protect hydroxyl groups to obtain protected erythromycin azoxide, oxidizing the hydroxyl groups into ketone groups through oxidation, and reacting the ketone groups with n-propylamine to obtain tulathromycin after epoxidation and deprotection. The method has the advantages of high product purity, high yield, low cost, simple operation, and stable process.

摘要：【中文】一种用于抑制氨基脲敏感性氧化酶(SSAO)和/或血管黏附蛋白‑1(VAP‑1)抑制剂的胺类化合物及其在医药上的应用，进一步涉及含有该胺类化合物的药物组合物。所述的化合物及药物组合物可用于治疗炎症和/或炎症相关疾病、糖尿病和/或糖尿病相关疾病、精神病症、缺血性疾病、血管疾病、纤维化或组织移植排斥。 【EN】An amine compound for inhibiting semicarbazide-sensitive oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1) inhibitor and its application in medicine, and further relates to a pharmaceutical composition containing the amine compound. The compounds and pharmaceutical compositions can be used for treating inflammation and/or inflammation-related diseases, diabetes and/or diabetes-related diseases, psychiatric disorders, ischemic diseases, vascular diseases, fibrosis or tissue transplant rejection.

摘要：【中文】本发明主要提供了酰胺衍生物的盐及其制备方法，属于医药化工技术领域。该酰胺衍生物的盐由Ralinepag和氨基丁三醇形成，具有稳定性良好，溶解度大，适于制备药用组合物等优势。另外，该Ralinepag氨基丁三醇盐的制备方法工艺简单，适合工业化生产。 【EN】The invention mainly provides a salt of an amide derivative and a preparation method thereof, belonging to the technical field of pharmaceutical chemicals. The salt of the amide derivative is formed by Ralinetag and tromethamine, has the advantages of good stability, high solubility, suitability for preparing medicinal compositions and the like. In addition, the preparation method of the Ralinetag tromethamine salt is simple in process and suitable for industrial production.

摘要：【中文】本发明涉及一种稠合三环类化合物及其在药物中的应用，尤其是作为用于治疗和/或预防乙型肝炎的药物的应用。具体地说，本发明涉及通式(I)所示化合物或其立体异构体、互变异构体、氮氧化物、溶剂化物、代谢产物、药学上可接受的盐或它的前药，其中各变量如说明书所定义。本发明还涉及通式(I)所示化合物或其立体异构体、互变异构体、氮氧化物、溶剂化物、代谢产物、药学上可接受的盐或它的前药作为药物的用途，尤其是作为用于治疗和/或预防乙型肝炎的药物的用途。 【EN】The invention relates to a fused tricyclic compound and application thereof in medicines, in particular to application of the fused tricyclic compound as a medicine for treating and/or preventing hepatitis B. Specifically, the invention relates to a compound shown in a general formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein variables are defined in the specification. The invention also relates to the application of the compound shown in the general formula (I) or the stereoisomer, the tautomer, the nitrogen oxide, the solvate, the metabolite, the pharmaceutically acceptable salt or the prodrug thereof as a medicament, in particular to the application as a medicament for treating and/or preventing hepatitis B.