公开(公告)号：US11661421B2

公开(公告)日：2023-05-30

申请号：US16978501

申请日：2019-03-05

Applicant: HAIHE BIOPHARMA CO., LTD.

Inventor： Xuxing Chen ,  Yi Chen ,  Ying Huang ,  Meiyu Geng ,  Qiong Zhang ,  Jian Ding ,  Yucai Yao ,  Qianqian Shen ,  Yanyan Shen

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The invention provides an indolizine compound represented by formula I or a pharmaceutically acceptable salt thereof, a preparation method and a use thereof. The indolizine compound has an inhibitory effect on wild-type and/or mutant EZH2 or EZH1, and is expected to be developed into a novel drug for anti-tumor or for the treatment of autoimmune diseases.

公开(公告)号：US20250042857A1

公开(公告)日：2025-02-06

申请号：US18695940

申请日：2022-09-28

Applicant: HAIHE BIOPHARMA CO., LTD.

Inventor： Dongsheng LI ,  Shanyun GAO ,  Cailu LIU ,  Yalei CAI ,  Maozhi YANG ,  Wangyang TU ,  Bing YU ,  Qing XIE ,  Yixiang ZHANG ,  Leping LI

IPC: C07D215/44 ,  A61K31/4375 ,  A61K31/438 ,  A61K31/439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to an SOS1 inhibitor with a pyrido-fused-six-membered ring structure, a preparation method therefor, and use thereof. The SOS1 inhibitor has the structural formula shown in formula (I) and an inhibitory activity on SOS1, and can be used to treat head and neck cancer, lung cancer, a mediastinal tumor, a gastrointestinal tumor, prostate cancer, testicular cancer, a gynecological tumor, breast cancer, renal and bladder cancer, an endocrine tumor, soft tissue sarcoma, osteosarcoma, rhabdomyosarcoma, mesothelioma, skin cancer, a peripheral nerve tumor, a central nervous system tumor, lymphoma, leukemia, Noonan syndrome, cardio-facio-cutaneous syndrome, and hereditary gingival fibromatosis and a related syndrome thereof.

公开(公告)号：US20210078972A1

公开(公告)日：2021-03-18

申请号：US17044322

申请日：2019-03-29

Applicant: HAIHE BIOPHARMA CO., LTD. ,  JINAN UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Ke DING ,  Meiyu GENG ,  Shingpan CHAN ,  Jian DING ,  Li TAN ,  Jing AI ,  Zhang ZHANG ,  Xia PENG ,  Xiaomei REN ,  Yinchun JI ,  Zhengchao TU ,  Yang DAI ,  Xiaoyun LU

IPC: C07D401/12 ,  A61P35/00

Abstract: The present invention relates to quinoline or quinazoline compound represented by the formula (I), a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a prodrug molecule thereof, or a deuterated compound thereof. The compound of the present invention is effective in inhibiting the action of AXL protein kinase and can inhibit proliferation, migration, and invasion of various tumor cells. Further, the quinoline or quinazoline compound of the present invention has excellent metabolic stability, high in vivo antitumor activity, low toxic side effects, and can be used for preparing a drug for preventing hyperproliferative diseases such as tumors in humans and other mammals.

公开(公告)号：US20250032464A1

公开(公告)日：2025-01-30

申请号：US18707240

申请日：2022-11-01

Applicant: HAIHE BIOPHARMA CO., LTD.

Inventor： Yong GAN ,  Miao ZHU ,  Yuanhui MA ,  Lei LIU ,  Shiyan GUO ,  Jingkang SHEN ,  Meiyu GENG ,  Li GAO ,  Bing XIONG

IPC: A61K31/437 ,  A61K9/16 ,  A61K9/20 ,  A61K9/28 ,  A61K9/48

Abstract: A solid dispersion, a preparation method therefor, and a solid formulation comprising same. The solid dispersion comprises compound A and a pharmaceutically acceptable matrix polymer, wherein the pharmaceutically acceptable matrix polymer includes an enteric high-molecular polymer and a non-enteric high-molecular polymer, and the compound A is 1-{(6-[(1-methyl)-4-pyrazolyl]-imidazo[1,2-a]pyridine)-3-sulfonyl}-6-[(1-methyl)-4-pyrazolyl]-1-hydro-pyrazolo[4,3-b]pyridine. The solid dispersion can significantly improve the solubility and dissolution stability of the compound A, prolong the supersaturation maintenance time of a drug, and further improve the bioavailability of the drug. The in vivo bioavailability of a solid formulation prepared from the solid dispersion meets the requirement of oral administration of the compound A.

公开(公告)号：US20240383893A1

公开(公告)日：2024-11-21

申请号：US18690358

申请日：2022-09-09

Applicant: Haihe Biopharma Co., Ltd.

Inventor： Shanyun Gao ,  Jingjing Li ,  Chaobo Zhang ,  Yanxiao Xu ,  Wangyang Tu ,  Bing Yu ,  Yixiang Zhang ,  Leping Li

IPC: C07D471/04 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4706 ,  A61K31/519 ,  A61K45/06 ,  C07D215/22 ,  C07D215/46 ,  C07D498/04

Abstract: The present disclosure involves a compound of formula (I) having ENPP1 inhibitory activity, a pharmaceutical composition thereof, and use thereof. The present disclosure particularly involves a compound of formula (I), as well as a pharmaceutical composition containing the compound and a method for preventing or treating diseases using the compound, particularly for diseases or disorders mediated by ENPP1 abnormal activity.

公开(公告)号：US20240150343A1

公开(公告)日：2024-05-09

申请号：US17766601

申请日：2020-09-24

Applicant: HAIHE BIOPHARMA CO., LTD.

Inventor： Lin XIA ,  Leping LI ,  Haoran YANG

IPC: C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

Abstract: Disclosed in the present invention are a compound having a BRD4 inhibitory activity, a preparation method therefor and the use thereof. The structure of the compound having the BRD4 inhibitory activity of the present invention is as shown in formula I, and the definition of each substituent is as described in the description and claims. The compound of the present invention has a high bromodomain protein inhibitory activity, in particular a BRD4-targeting inhibitory activity, and can be used for the treatment and/or prevention of related diseases mediated by bromodomain proteins.