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18 条记录 (耗时 0.013 秒)

    METHOD FOR PREPARING DEUTERATED IMIDAZOLE DIKETONE COMPOUND
    3.
    发明公开
    METHOD FOR PREPARING DEUTERATED IMIDAZOLE DIKETONE COMPOUND 审中-公开

    公开(公告)号：EP3527556A1

    公开(公告)日：2019-08-21

    申请号：EP16919556.7

    申请日：2016-12-20

    申请人： Hinova Pharmaceuticals Inc.

    发明人： CHEN, Yuanwei ,  DU, Wu ,  KUANG, Tongtao ,  GENG, Xi

    IPC分类号： C07D233/86 ,  C07B59/00

    摘要： The present invention discloses a method for preparation of deuterated imidazole diketone compounds, that includes the following steps: (1) using compound of formula (I) and compounds of formula (II) as starting material, compounds of formula (III) are obtained by a substitution reaction; (2) Compounds of formula (IV) are prepared by esterification of carboxyl in compounds of formula (III); (3) Cyclization of compounds of formula (IV) and compound of formula (V) provides compounds of formula (VI); (4) Compounds of formula (VI) are deesterificated and react to produce compounds of formula (VII); (5) using compounds of formula (VII) and compounds of formula (VIII) as starting material, the deuterated imidazole diketone compounds of formula (IX) are obtained by the condensation reaction of amide. Compared with the methods in the prior art, the method according to the present invention is safer, consuming less solvents, minimizing the waste and the effect on the environment, shortening the production cycle, and improving the throughput and the total yield of the method, with a wide market outlook.

    EP300/CBP INHIBITOR
    4.
    发明公开
    EP300/CBP INHIBITOR 审中-公开

    公开(公告)号：EP4043458A1

    公开(公告)日：2022-08-17

    申请号：EP20868375.5

    申请日：2020-09-25

    申请人： Hinova Pharmaceuticals Inc.

    发明人： FAN, Lei ,  WANG, Fei ,  WU, Xiaoquan ,  XU, Kexin ,  LUO, Tongchuan ,  ZHANG, Shaohua ,  HUO, Yongxu ,  LI, Xinghai ,  CHEN, Yuanwei

    IPC分类号： C07D413/14 ,  C07D471/04 ,  A61K31/422 ,  A61P35/00

    摘要： An EP300/CBP inhibitor; specifically provided is a compound as shown in formula I, or a deuterated product thereof, or a salt thereof, or a conformational isomer thereof, or a crystal form thereof, or a solvate thereof. The compound is highly selective for EP300/CBP, and can effectively inhibit the activity of EP300/CBP; in addition, the compound has an excellent inhibitory effect on various tumor cells including prostate cancer cells, leukemia cells, breast cancer cells and multiple myeloma cells. The compound has broad application prospects in the preparation of an EP300/CBP inhibitor, and drugs for preventing and/or treating tumors, myeloid hematopoietic stem/progenitor cells malignant disease, and regulating regulatory T cells.

    DEUTERATED DEFACTINIB COMPOUND AND USE THEREOF
    5.
    发明公开
    DEUTERATED DEFACTINIB COMPOUND AND USE THEREOF 审中-公开

    公开(公告)号：EP3792257A1

    公开(公告)日：2021-03-17

    申请号：EP19798903.1

    申请日：2019-05-06

    申请人： Hinova Pharmaceuticals Inc.

    发明人： DU, Wu ,  LI, Yu ,  WEN, Kun ,  LI, Xinghai ,  CHEN, Yuanwei

    IPC分类号： C07D403/12 ,  A61K31/506 ,  A61P35/00

    摘要： Provided are a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, hydrates or solvates thereof, wherein R 1 -R I8 are independently selected from hydrogen and deuterium respectively, but not all of them are hydrogen at the same time. The compound and salts, hydrates or solvates thereof can be used as FAK inhibitors, and used in the preparation of anti-cancer drugs, and compared with the non-deuterated control compound Defactinib, the compound has significantly improved metabolic stability and pharmacokinetic properties, while also possessing good application prospects.

    HC-1119 FORMULATION, PREPARATION METHOD AND USE THEREOF
    8.
    发明公开
    HC-1119 FORMULATION, PREPARATION METHOD AND USE THEREOF 审中-公开

    公开(公告)号：EP3795153A1

    公开(公告)日：2021-03-24

    申请号：EP19803519.8

    申请日：2019-05-13

    申请人： Hinova Pharmaceuticals Inc.

    发明人： WEI, Xing ,  QI, Ming ,  DU, Wu ,  LI, Xinghai ,  CHEN, Yuanwei

    IPC分类号： A61K31/4166 ,  A61K9/48 ,  A61P35/00

    摘要： Provided is a formulation of androgen receptor inhibitor HC-1119 prepared from the following raw materials at the weight ratio: 1 to 100 parts of the androgen receptor inhibitor HC-1119, 100 to 1000 parts of a solvent, and 0.11 to 11 parts of an antioxidant. Also provided is a HC-1119 soft capsule and a HC-1119 formulation. The HC-1119 raw material is dissolved in Labrasol so as to significantly improve the solubility of HC-1119, and thus greatly improve the bioavailability, reduce the difference in blood drug concentration and exposure among individuals, and increase the safety of medication. Further, the HC-1119 soft capsule has good stability.