Patents Assigned to Jiangsu Hengrui Medicine Co., Ltd.
  • Patent number: 10344034
    Abstract: Methods of preparation and pharmaceutical uses of pyrazolopyrimidone derivatives are described. Specifically, methods of preparation and pharmaceutical uses of pyrazolopyrimidone derivatives represented by the general formula (II) and pharmaceutically acceptable salts thereof are described, wherein the definitions of substituents in the general formula (II) are the same as the definitions in the specification. The pyrazolopyrimidone derivatives are useful as gonadotropin releasing hormone (GnRH) antagonists, such as for therapeutic agents for endometriosis.
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: July 9, 2019
    Assignees: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Hejun Lu, Piaoyang Sun, Bin Gui, Qing Dong
  • Patent number: 10323037
    Abstract: The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: June 18, 2019
    Assignee: JIANGSU HENGRUI MEDICINE CO., LTD.
    Inventors: Dong Liu, Minsheng Zhang, Qiyue Hu
  • Publication number: 20190169257
    Abstract: Provided is an acylated derivative of human insulin or an analogue thereof. Specifically disclosed is an acylated derivative of a human insulin analogue, or zinc complex thereof; said acylated derivative is longer-lasting than existing insulin analogues and acylated derivatives thereof, its blood glucose reduction is more steady, and it is more stable in storage.
    Type: Application
    Filed: August 1, 2017
    Publication date: June 6, 2019
    Applicant: JIANGSU HENGRUI MEDICINE CO., LTD.
    Inventors: Deyu LIU, Hongwei WANG, Liang ZHAO, Feifei WANG, Xiang ZENG, Tao WANG, Yali WANG, Yulu DAI
  • Patent number: 10301344
    Abstract: Provided are an L-proline complex of a sodium-glucose cotransporter 2 inhibitor, and a monohydrate and a crystal of the L-proline complex. Specifically, provided are 1,6-dehydrated-1-C{4-chloro-3-[(3-fluoro-4-ethoxyphenyl)methyl]phenyl}-5-C-(hydroxymethyl)-?-L-idopyranose L-proline (a compound of formula (I)), a monohydrate and a type A crystal thereof, and a preparation method therefor. The obtained type A crystal of the compound of formula (I) has good chemical stability and crystal stability, and the crystallization solvent used has low toxicity and low residue, so the type A crystal can be better used in clinical treatment.
    Type: Grant
    Filed: September 8, 2015
    Date of Patent: May 28, 2019
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Piaoyang Sun, Guaili Wu, Changshan Guo, Yun Lu, Yuxia Wu, Lingjia Shen
  • Patent number: 10258584
    Abstract: Disclosed is a pregabalin sustained-release preparation, wherein the sustained-release tablet contains a pharmaceutically active ingredient containing pregabalin or a salt or hydrate thereof, a gel framework material containing alginic acid, and a swellable material containing polyoxyethylene.
    Type: Grant
    Filed: September 24, 2015
    Date of Patent: April 16, 2019
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Yun Lu, Jiajia Xu, Hao Chen
  • Publication number: 20190070264
    Abstract: An interleukin 15 (IL-15) protein complex is provided. The IL-15 protein complex includes soluble fusion proteins (I) and (II), wherein the fusion protein (I) is an IL-15 polypeptide or a functional fragment thereof, and the soluble fusion protein (II) is an IL-15R? polypeptide or a functional fragment thereof. The soluble fusion protein (I) has at least one amino acid residue mutated to a cysteine (Cys) residue, which pairs with a corresponding mutated Cys residue on the soluble fusion protein (II), or vice versa, to form one or more disulfide bonds. The IL-15 protein complex can be used for tumor therapy.
    Type: Application
    Filed: November 17, 2015
    Publication date: March 7, 2019
    Applicants: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Xiangdong QU, Xin YE, Qiyue HU, Dongbing CUI, Weikang TAO, Lianshan ZHANG, Piaoyang SUN
  • Publication number: 20190054025
    Abstract: The present invention provides a method for preparing a pharmaceutical composition containing a quinoline derivative or a salt thereof. Specifically, the invention provides a method for preparing 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. The method uses a wetting agent containing at least one organic solvent for a wet granulation in a preparation process of the pharmaceutical composition. The pharmaceutical composition prepared using the method has a uniform distribution of grain sizes during the preparation process and a property of rapid and uniform dissolution.
    Type: Application
    Filed: January 23, 2017
    Publication date: February 21, 2019
    Applicant: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Yun LU, Xinhua ZHANG, Chenyang WANG
  • Patent number: 10206980
    Abstract: Provided is an IL-15 heterodimeric protein, such as an IL-15/IL-15R? heterodimeric protein. The IL-15 heterodimeric protein contains protein (I) and protein (II). Protein (I) is recombinantly produced by combining IL-15 or a variant thereof with a first Fc variant, and protein (II) is a second Fc variant, or recombinantly produced by combining IL-15R? or a variant thereof with a second Fc variant. The first Fc variant and the second Fc variant are preferably linked via a “Knob-into-Hole” mode. Also provided are methods of using the IL-15 heterodimeric proteins to modulate an immune response. The provided IL-15 heterodimeric proteins have significant anti-tumor activity, better biological activity and prolonged in vivo half-life compared to the IL-15 molecule alone.
    Type: Grant
    Filed: December 25, 2014
    Date of Patent: February 19, 2019
    Assignees: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Xiangdong Qu, Xin Ye, Jijun Yuan, Lei Zhang, Kan Chen, Lianshan Zhang, Guoqing Cao, Zhibin Xu, Weikang Tao
  • Patent number: 10196361
    Abstract: Provided are a sodium salt of a uric acid transporter inhibitor and a crystalline form thereof, In particular, provided are a uric acid transporter (URAT1) inhibitor 1-((6-bromo-quinoline-4-yl)thio)cyclobutyl sodium formate (the compound of formula (I)), a crystal form I, and preparation method thereof. The obtained crystal form I of the compound of formula (I) has a good crystal form stability and chemical stability, and the crystallization solvent used has a low toxicity and low residue, and can be better used in clinical treatment.
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: February 5, 2019
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili Wu, Zhenjun Qiu, Yunpeng Su, Xi Lu
  • Publication number: 20190010161
    Abstract: The present invention relates to a crystalline form of a BTK kinase inhibitor and the preparation method thereof. In particular, the present invention relates to a crystal form I of (R)-4-amino-1-(1-(but-2-ynoyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1H-pyrrolo[2,3-d]pyridazin-7(6H)-one (the compound of formula (I)) and the preparation method thereof. The crystal form I of the compound of formula (I) obtained by the present invention has a good crystalline stability and chemical stability, and the crystallization solvent used has a low toxicity and low residue, thus making it more suitable for use in clinical treatment.
    Type: Application
    Filed: December 20, 2016
    Publication date: January 10, 2019
    Applicant: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili WU, Zhenjun QIU, Xi LU, Yun LU
  • Patent number: 10160759
    Abstract: Provided are a hydroxyethyl sulfonate of a cyclin-dependent protein kinase inhibitor, a crystalline form thereof and a preparation method therefor. Specifically, 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydroxyethyl sulfonate (compound of formula (I)), a crystal form I thereof and a preparation method therefor are provided. Crystal form I of the compound of formula (I) has good chemical and crystalline stability, low toxicity, and low residual crystallization solvent. The compound of formula (I) and crystal form I thereof can be used in improved clinical therapy.
    Type: Grant
    Filed: April 13, 2018
    Date of Patent: December 25, 2018
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili Wu, Xiaohui Gao, Junlei Jia
  • Patent number: 10150739
    Abstract: A crystalline form of an androgen receptor inhibitor and its preparation method are provided. In particular, provided are crystal form I of (S)-4-(3-(4-(2,3-dihydroxypropoxy)phenyl)-4,4-dimethyl-5-carbonyl-2-thioimidazolin-2-yl)-2-(trifluoromethyl)benzonitrile (a compound of formula (I)) and its preparation method. The method includes (a) adding any crystal form or amorphous form of the compound of formula (I) to an organic solvent to obtain a solution and heating the solution until it is clear, followed by cooling the solution to precipitate a crystal; and (b) filtering, washing, and drying the crystal. The obtained crystal form I of the compound of formula (I) has good chemical stability and crystal form stability, and the crystallization solvent used has low toxicity and residue, and is thus better for use in clinical treatment.
    Type: Grant
    Filed: August 23, 2016
    Date of Patent: December 11, 2018
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili Wu, Changshan Guo, Liang Zhong, Yun Lu
  • Patent number: 10150770
    Abstract: A crystal form I of a Janus Kinase (JAK) inhibitor (3aR,5s,6aS)—N-(3-methoxyl-1,2,4-thiadiazole-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate of formula (I) is provided. Also provided is a method of preparing the crystal form I of the JAK inhibitor of formula (I). The preparation method includes crystallizing any crystal form or amorphous compound solid of formula (I) in a single organic solvent to obtain the form I crystal. The crystal form I has excellent crystal stability and chemical stability. Additionally, the crystal solvent used to produce the crystal form I has low toxicity and a relatively low content of residual solvent, making the compound better suited for clinical treatment.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: December 11, 2018
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Piaoyang Sun, Guaili Wu, Xiaohui Gao, Yongjiang Chen, Lingjia Shen
  • Patent number: 10144737
    Abstract: The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: December 4, 2018
    Assignee: JIANGSU HENGRUI MEDICINE CO., LTD.
    Inventors: Minsheng Zhang, Yinfa Yan
  • Publication number: 20180334504
    Abstract: The present invention relates to a PD-L1 antibody, antigen-binding fragments, and medical application thereof. Further, the present invention relates to chimeric antibodies and humanized antibodies comprising the CDR regions of the present PD-L1 antibody, as well as a pharmaceutical composition comprising the present PD-L1 antibody and the antigen-binding fragments thereof, and their use as anti-cancer drugs. In particular, the present invention relates to a humanized PD-L1 antibody and its use in preparation of a medicament for the treatment of PD-L1 mediated disease or disorder.
    Type: Application
    Filed: November 2, 2016
    Publication date: November 22, 2018
    Applicants: Suzhou Suncadia Biopharmaceuticals Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Xiangdong QU, Qiyue HU, Shaoyu XU, Dongbing CUI, Houcong JIN, Weikang TAO, Lianshan ZHANG, Guoqing CAO, Piaoyang SUN
  • Patent number: 10118911
    Abstract: Disclosed are a p-toluenesulfonate of a MEK kinase inhibitor, and a crystal form thereof and a preparation method thereof. Specifically disclosed are a 2-((2-fluorine-4-iodophenyl)amino)-1-methyl-4-((6-methylpyridine-3-group)oxygroup)-6-carbonyl-1,6-dihydropyridine-3-formamide p-toluenesulfonate (a compound represented by formula (I)), a crystal form I, and a preparation method thereof. The obtained crystal form I of the compound of formula (I) has good crystal form stability and chemical stability, and the crystallization solvent used has low toxicity and low residue, and is more suitable for use in clinical treatment.
    Type: Grant
    Filed: March 8, 2016
    Date of Patent: November 6, 2018
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili Wu, Xiaohui Gao, Lin Bian, Junlei Jia
  • Patent number: 10087191
    Abstract: The present invention relates to a piperidine derivative and the preparation method and a pharmaceutical use thereof. In particular, the present invention relates to the piperidine derivative as shown by general formula (I) and the preparation method thereof and a pharmaceutical composition containing the same, and the use thereof as an estrogen receptor modulator in the treatment of estrogen receptor mediated or dependent diseases or conditions, the diseases preferably being breast cancer. In the abstract, the definition of each substituent of the general formula (I) is the same as that in the description.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: October 2, 2018
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Shanghai Yu, Fanglong Yang, Lei Chen, Jingjing Yan, Xiqian Zhang, Zhichao Xie, Lingxiang Chen, Mingxun He
  • Patent number: 10081629
    Abstract: Amide derivatives and pharmaceutically acceptable salts thereof, preparation method thereof and medicinal application thereof are provided. Specifically, amide derivatives represented by general formula (I) are provided. The amide derivatives represented by general formula (I) can be used as a therapeutic agent, particularly as an inhibitor for microsomal prostaglandin E synthase-1 (mPGES-1), and also to treat and/or prevent diseases or illnesses such as inflammation and/or pain etc. The definition of each substituent group in general formula (I) is the same as the definition in the description.
    Type: Grant
    Filed: March 31, 2015
    Date of Patent: September 25, 2018
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Xin Li, Wei He, Xianbo Liu, Bin Wang, Qiyue Hu, Fangfang Jin, Qing Dong, Piaoyang Sun
  • Publication number: 20180251465
    Abstract: The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.
    Type: Application
    Filed: February 27, 2018
    Publication date: September 6, 2018
    Applicant: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Dong LIU, Minsheng ZHANG, Qiyue HU
  • Patent number: 10064848
    Abstract: Compounds for the preparation of pyridone derivatives are provided. In particular, compounds of formula (IA) are provided, wherein the variable groups are as defined in the specification. The compounds of formula (IA) can be used as intermediates in the preparation of pyridone derivatives useful as mitogen-activated protein kinase kinase (MEK) inhibitors and therapeutic agents for treating cancer.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: September 4, 2018
    Assignees: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Wangyang Tu, Haitang Zhang, Guoji Xu, Jiangtao Chi