Patents Assigned to Jiangsu Hengrui Medicine Co., Ltd.
  • 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: 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: 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: 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
  • Publication number: 20180237438
    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: Application
    Filed: September 9, 2015
    Publication date: August 23, 2018
    Applicants: Jiangsu Hengrui Medicine Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Piaoyang SUN, Guaili WU, Xiaohui GAO, Yongjiang CHEN, Lingjia SHEN
  • Patent number: 10030018
    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. Therefore, the crystal form I can be used in improved clinical therapy.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: July 24, 2018
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili Wu, Xiaohui Gao, Junlei Jia
  • Patent number: 10022365
    Abstract: A liposome of irinotecan or irinotecan hydrochloride and its preparation method are disclosed. The liposome contains irinotecan or irinotecan hydrochloride, neutral phospholipid and cholesterol, wherein the weight ratio of the cholesterol to the neutral phospholipid is 1:3 to 1:5. The liposome is prepared by an ion gradient method.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: July 17, 2018
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Xinyong Tong, Guofeng Lei, Chengxia Yu, Liang Chen
  • Patent number: 10005781
    Abstract: Pyrazolopyrimidone and pyrrolotriazone derivatives, methods of preparation thereof, and pharmaceutical uses thereof are described. Specifically, pyrazolopyrimidone and pyrrolotriazone derivatives represented by the general formula (I) and pharmaceutically acceptable salts thereof are described. The pyrazolopyrimidone and pyrrolotriazone derivatives are useful as gonadotropin releasing hormone (GnRH) antagonists, such as for therapeutic agents for endometriosis. The definitions of the substituents in the general formula (I) are the same as the definitions in the specification.
    Type: Grant
    Filed: September 30, 2014
    Date of Patent: June 26, 2018
    Assignees: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Hejun Lu, Piaoyang Sun, Bin Gui, Qing Dong
  • Publication number: 20180118715
    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: Application
    Filed: March 8, 2016
    Publication date: May 3, 2018
    Applicant: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili WU, Xiaohui GAO, Lin BIAN, Junlei JIA
  • Publication number: 20180118750
    Abstract: The present invention relates to an imidazo isoindole derivative, a preparation method therefor and a medical use thereof. In particular, the present invention relates to the imidazo isoindole derivative as shown in the formula (I), a preparation method and pharmaceutical composition containing the derivative, and a use thereof for treating diseases with a pathological characteristic of the IDO-mediated tryptophan metabolic pathways. The diseases comprise cancers, Alzheimer's disease, autoimmune diseases, depression, anxiety disorders, cataracts, psychological disorders and AIDS, wherein the substituents in the formula (I) are the same as those defined in the specification.
    Type: Application
    Filed: April 12, 2016
    Publication date: May 3, 2018
    Applicants: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Wangyang TU, Guoji XU, Haitang ZHANG, Jiangtao CHI, Qing DONG
  • Patent number: 9951077
    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: April 24, 2018
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Dong Liu, Minsheng Zhang, Qiyue Hu
  • Publication number: 20180099046
    Abstract: Provided is a humanized antibody and chimeric antibody that specifically binds human sclerostin. The antibodies can be used for treating human bone metabolism related diseases such as osteoporosis (OP).
    Type: Application
    Filed: February 16, 2016
    Publication date: April 12, 2018
    Applicants: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Jiajian LIU, Yayuan FU, Haoying ZHANG, Yifang WANG, Zhen ZHANG, Ling ZHANG, Dongbing CUI, Lianshan ZHANG, Weikang TAO
  • Patent number: 9914703
    Abstract: Pyridone derivatives, methods of preparing the pyridone derivatives, and methods of using the pyridone derivatives are provided. In particular, pyridone derivatives of formula (I), and pharmaceutical salts thereof are provided. The pyridone derivatives are useful as mitogen-activated protein kinase kinase (MEK) inhibitors, and can be used as therapeutic agents for treating cancer.
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: March 13, 2018
    Assignees: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Wangyang Tu, Haitang Zhang, Guoji Xu, Jiangtao Chi
  • Patent number: 9895355
    Abstract: Methods for treating androgen receptor-mediated diseases, such as breast cancer, with imidazoline derivatives of formula (I) are provided:
    Type: Grant
    Filed: January 20, 2017
    Date of Patent: February 20, 2018
    Assignees: Shanghai Hengru Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Hejun Lu, Piaoyang Sun, Hongbo Fei, Hongjian Jiang, Haowei Wang, Qing Dong