Abstract: A method for preparing a tyrosine kinase inhibitor and a derivative thereof are described. In particular, the present method has a short synthesis route, low costs, easy operation, and is suitable for large-scale production.
Type:
Grant
Filed:
August 28, 2020
Date of Patent:
December 14, 2021
Assignee:
Jiangsu Hengrui Medicine Co., Ltd.
Inventors:
Guaili Wu, Quanliang Zhang, Yongxing Cao
Abstract: A salt of a phenylpropionamide derivative and a preparation method therefor is described. Specifically, the salt of the compound of formula (I) has good stability, and can be better used in clinical treatment. The process for preparing the salt of the compound of formula (I) of the present invention is simple and easy to operate.
Abstract: A crystal form of PARP-1 inhibitor and a preparation method therefor are described. Specifically, a crystal form A of 4-[[3-[[2-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[1,5-?]pyrazine-7-yl]carbonyl]-4-fluorophenyl]methyl-1(2H)-phthalazinone (formula I) and a preparation method therefor are described.
Type:
Grant
Filed:
August 23, 2018
Date of Patent:
November 23, 2021
Assignee:
Jiangsu Hengrui Medicine Co., Ltd.
Inventors:
Wenhai Li, Quanliang Zhang, Zhenjun Qiu, Zhengming Li
Abstract: Provided are a crystal form of a maleate of a tyrosine kinase inhibitor and a preparation method therefor. Specifically, provided are I crystal form, a II crystal form, a III crystal form, a IV crystal form and a V crystal form of the compound as shown in formula (I) and a preparation method therefor. The new crystal form has a good stability, thereby making same better to use in clinical treatments.
Type:
Application
Filed:
October 21, 2019
Publication date:
November 18, 2021
Applicant:
JIANGSU HENGRUI MEDICINE CO., LTD.
Inventors:
Zhenjun QIU, Quanliang ZHANG, Yanli WEI, Yongxing CAO, Junran YANG, Yahui MA, Zhenxing DU, Jie WANG
Abstract: The present invention relates to a new crystalline form of obeticholic acid and a preparation method therefor. In particular, the present invention relates to crystal form E of obeticholic acid and a preparation method therefor. The crystalline form is very stable, and the solvent residue is low, and the crystalline form is suitable for industrial production.
Abstract: Provided are a LAG-3 antibody, an antigen-binding fragment thereof, and a pharmaceutical application thereof. Further, provided are a chimeric antibody comprising a CDR of the LAG-3 antibody, a humanized antibody, a pharmaceutical composition comprising the LAG-3 antibody and the antigen-binding fragment thereof, and an application of the pharmaceutical composition as an antineoplastic drug. Particularly, provided is an application of a humanized LAG-3 antibody in preparation of drugs for treatment of diseases involving immune cells.
Abstract: This application describes a crystal of a benzofuran derivative free base and a preparation method. Specifically, this application describes crystal A, crystal B, crystal C, and crystal D of N-((4,6-dimethyl-2-carbonyl-1,2-dihydropyridin-3-yl)methyl)-5-ethyl-6-(ethyl(tetrahydro-2H-pyran)4-yl)amino)-2-(piperidin-1-ylmethyl)benzofuran-4-carboxamide and a preparation method for the crystals. The crystals of the compound of formula (I) have great crystal stability and provides improved uses in clinical treatment.
Type:
Grant
Filed:
May 17, 2018
Date of Patent:
October 26, 2021
Assignee:
Jiangsu Hengrui Medicine Co., Ltd.
Inventors:
Likun Wang, Zhenxing Du, Qiyun Shao, Chao Xu
Abstract: Disclosed are a pyrazolo-heteroaryl derivative, a preparation method and medical use thereof. In particular, this invention relates to a new pyrazolo-heteroaryl derivative as shown in the general formula (I), a preparation method thereof and a pharmaceutical composition containing the derivative and the use thereof as a therapeutic agent, in particular as a TLR7 agonist, wherein each substituent in the general formula (I) is defined in the description.
Abstract: Disclosed is a pharmaceutical composition containing a bicyclo-substituted pyrazolone azo derivative or a salt thereof and a preparation method thereof. In particular, the pharmaceutical composition disclosed in the present invention contains (Z)-5-(2-hydroxyl-3-(2-(3-methyl-5-oxo-1-(5,6,7,8-tetrahydronaphthalene-2-yl)-1H-pyrazol-4(5H)-ylidene)hydrazino)phenyl)furan-2-carboxylic acid or a pharmaceutically acceptable salt thereof, and at least one filler optionally selected from cellulose, microcrystalline cellulose, lactose and starch. The composition has a good stability, dissolution rate and bioavailability, and the preparation process is simple, economical and quick.
Abstract: A method for preparing an oxaspirocycle derivative and an intermediate thereof are described. The method reduces reaction steps, improves reaction yield, is simple and easy to operate, and is favorable for industrial large-scale production.
Abstract: A heteroaryl-pyrazole derivative, and a preparation method therefor and a medical application thereof are described. Specifically, a new heteroaryl-pyrazole derivative as shown in formula (I), a preparation method for the derivative, a pharmaceutical composition containing the derivative, and a use of the derivative as a therapeutic agent, in particular as a TLR7 agonist, are described. The substituents in formula (I) have the same definitions as in the description.
Abstract: The present invention relates to an oxopicolinamide derivative, a preparation method therefor and the pharmaceutical use thereof. In particular, the present invention relates to an oxopicolinamide derivative as shown in the general formula (AI), a preparation method therefor and a pharmaceutical composition comprising the derivative, and to the use thereof as a therapeutic agent, in particular as an inhibitor of blood coagulation factor XIa (Factor XIa, FXIa for short) and the use thereof in the preparation of a drug for treating diseases such as thromboembolism, wherein the definition of each substituent in the general formula (AI) is the same as defined in the description.
Abstract: The present invention provides a pharmaceutical composition containing a quinoline derivative or a salt thereof. Specifically, the invention provides a pharmaceutical composition containing (R,E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)-propeneamide or a pharmaceutically acceptable salt thereof, a cross-linked polyvinylpyrrolidone, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition has a property of rapid dissolution.
Abstract: A benzofuran derivative, a preparation method thereof and a use thereof in medicine are described. In particular, a benzofuran derivative as shown by general formula (I), the preparation method thereof, a pharmaceutical composition containing the derivative, and uses thereof as an EZH2 inhibitor and in the prevention and/or treatment of diseases such as tumours and cancers, etc., and in particular, uses thereof in the prevention and/or treatment of non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, follicular lymphoma and synovial sarcoma, are described.
Abstract: A pharmaceutically acceptable salt as a renal outer medullary potassium channel (ROMK) inhibitor, specifically an L-tartrate and a crystal form I and crystal form II thereof, is described. The pharmaceutically acceptable salt of the ROMK inhibitor, specifically the L-tartrate, has improved bioavailability and stability.
Type:
Grant
Filed:
June 6, 2017
Date of Patent:
July 13, 2021
Assignee:
Jiangsu Hengrui Medicine Co., Ltd.
Inventors:
Yun Lu, Qiyun Shao, Guaili Wu, Jun Feng
Abstract: Provided in the present invention is a use of CDK4/6 inhibitor in combination with EGFR inhibitor in the preparation of a medicament for treating tumor diseases. In particular, provided in the invention is a use of a cyclin-dependent kinase 4 and 6 inhibitor (CDK4/6i) in combination with a human epidermal growth factor receptor inhibitor (EGFRi) for the preparation of a medicament for preventing or treating tumor diseases.
Type:
Application
Filed:
May 22, 2019
Publication date:
July 1, 2021
Applicant:
JIANGSU HENGRUI MEDICINE CO., LTD.
Inventors:
Lei ZHANG, Changyong YANG, Cheng LIAO, Lianshan ZHANG
Abstract: Disclosed is a method for preparing a precursor of a recombinant human insulin or an analogue thereof, comprising: a. bacterial fermentation, centrifuging a fermentation broth in a continuous flow to collect a supernatant; b. filtering the supernatant in step (a) by means of a hollow fiber membrane and collecting the filtrate; and c. purifying the filtrate in the step (b) by means of a chromatography column. The method has the advantages of streamlined steps, scalability, no use of organic solvents, high yield, etc. The purity of the insulin precursor can exceed 90%, the host cell protein removal rate exceeds 90%, and the exogenous DNA removal rate is 89% or greater, achieving less than 0.1 ng/mg.
Type:
Application
Filed:
May 23, 2019
Publication date:
July 1, 2021
Applicant:
JIANGSU HENGRUI MEDICINE CO., LTD.
Inventors:
Liangliang ZHAO, Guangjie HAN, Ningning NIU, Na LI, Yanwei LIU, Hongwei WANG
Abstract: The present invention provides a pharmaceutical composition comprising quinoline derivative. Specifically, the present invention provides a process for preparing a pharmaceutical composition comprising (R, E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy) phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidinyl-2-yl)-acrylamide or a pharmacologically acceptable salt thereof. The process for preparing is suitable for large-scale industrial production, and the obtained sample has the characteristics such as rapid and uniform dissolution.
Type:
Application
Filed:
October 23, 2018
Publication date:
June 24, 2021
Applicant:
JIANGSU HENGRUI MEDICINE CO., LTD.
Inventors:
Xinhua ZHANG, Chenyang WANG, Daimei ZHANG, Jianfeng BAI