公开(公告)号：US20230271936A1

公开(公告)日：2023-08-31

申请号：US18040598

申请日：2021-08-09

Applicant: Abbisko Therapeutics Co., Ltd

Inventor： Fei Yang ,  Shuqun Yang ,  Hongping Yu ,  Zhui Chen ,  Yaochang Xu

IPC: C07D401/12 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D401/12 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D401/14 ,  C07D405/14

Abstract: An EGFR inhibitor having the structure of formula (I), a preparation method therefor, a pharmaceutical composition containing same, a use of same as an EGFR inhibitor, and a use of same in preparing a drug for treating and/or preventing a cancer, a tumor, or a metastatic disease at least partially related to an EGFR exon 20 insertion, deletion, or other mutation, and in particular a use in preparing a drug for treating and/or preventing a hyperproliferative disease and an induced cell death disorder. Each substituent of formula (I) has the same definition as in the description.

公开(公告)号：US20240317710A1

公开(公告)日：2024-09-26

申请号：US18290102

申请日：2022-05-23

Applicant: Abbisko Therapeutics Co. Ltd.

Inventor： Lei ZHANG ,  Baowei ZHAO ,  Hongping YU

IPC: C07D401/14

CPC classification number: C07D401/14

Abstract: Provided are an acid salt of a crystalline CSF-1R inhibitor, and a preparation method therefor and the use thereof, wherein the CSF-1R inhibitor is the compound 3,3-dimethyl-N-(6-methyl-5-((2-(1-methyl-iH-pyrazol-4-yl)pyridin-4-yl)oxy)pyridin-2-yl)-2-oxopyrrolidine-1-carboxamide having the structure of formula (I). The crystalline acid salt compound can greatly improve the physicochemical properties such as solubility, hygroscopicity and chemical stability of the compound of formula (I) in a free state, and meet the requirements for industrial production and clinical drug preparation development. The crystalline acid salt compound can be widely used in the preparation of a drug for treating cancers, tumors, autoimmune diseases, metabolic diseases or metastatic diseases.

公开(公告)号：US20220162253A1

公开(公告)日：2022-05-26

申请号：US17438770

申请日：2020-04-27

Applicant: Abbisko Therapeutics Co., Ltd.

Inventor： Haibing DENG ,  Hongping YU ,  Zhui CHEN ,  Yaochang XU

IPC: C07H19/207

Abstract: A CD73 inhibitor having the structure represented by formula (I), a preparation method therefor and an application thereof are provided. The series of compounds can be widely applied in the preparation of drugs for treating cancers or tumors that are at least partially mediated by CD73, autoimmune diseases and disorders and metabolic diseases, in particular drugs for treating melanoma, colon cancer, pancreatic cancer, breast cancer, prostate cancer, lung cancer, leukemia, brain tumor, lymphoma, ovarian cancer and Kaposi's sarcoma. A new generation of CD73 inhibitor drugs is expected to be developed.

公开(公告)号：US20220009894A1

公开(公告)日：2022-01-13

申请号：US17289709

申请日：2019-09-12

Applicant: Abbisko Therapeutics Co., Ltd.

Inventor： Baowei ZHAO ,  Guoliang XUN ,  Yuan ZHAO ,  Tao FENG ,  Hongping YU ,  Zhui CHEN ,  Yaochang XU

IPC: C07D241/50 ,  C07D487/04

Abstract: A 1,2,3,4-tetrahydroquinoxaline derivative having a structure as represented by formula (I), preparation method therefor and application thereof. These compounds can be widely applied to preparation of drugs for treating one or more tumors, cancers, metabolic diseases, autoimmune diseases or disorders, and a new generation of RORγt agonist drugs is expected to be developed.

公开(公告)号：US20210261544A1

公开(公告)日：2021-08-26

申请号：US17253113

申请日：2019-07-23

Applicant: Abbisko Therapeutics Co., Ltd.

Inventor： Haibing DENG ,  Hongping YU ,  Zhui CHEN ,  Yaochang XU

IPC: C07D471/04 ,  C07D519/00 ,  A61P35/00

Abstract: A compound having a structure of formula (I) and a preparation method therefor, and a use of the compound serving as an FGFR inhibitor for treating tumors, cancers, myeloproliferative diseases, bone or chondrocyte disorders, and hypophosphatemia.

公开(公告)号：US20210130323A1

公开(公告)日：2021-05-06

申请号：US16633254

申请日：2018-08-01

Applicant: Abbisko Therapeutics Co., Ltd.

Inventor： Haibing DENG ,  Fei YANG ,  Hongping YU ,  Zhui CHEN ,  Yaochang XU

IPC: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D491/107 ,  A61P35/00

Abstract: Formylpyridine derivatives having FGFR4 inhibitory activities, a preparation method therefor and use thereof are described. In particular, the formylpyridine derivatives have a structure of formula (I), and the definition of each substituent in the formula are described in the description and claims. The series of compounds of the formula (I) have very strong inhibitory effects on FGFR4 kinases and very high selectivity, and can be widely used in the preparation of medicaments for treating cancers, particularly prostate cancer, liver cancer, pancreatic cancer, esophageal cancer, stomach cancer, lung cancer, breast cancer, ovarian cancer, colon cancer, skin cancer, neuroglioblastoma or rhabdomyosarcoma, and prospectively will be further developed to become a new generation of FGFR4 inhibitors.

公开(公告)号：US12157755B2

公开(公告)日：2024-12-03

申请号：US17438770

申请日：2020-04-27

Applicant: Abbisko Therapeutics Co., Ltd.

Inventor： Haibing Deng ,  Hongping Yu ,  Zhui Chen ,  Yaochang Xu

IPC: C07H19/207

Abstract: A CD73 inhibitor having the structure represented by formula (I), a preparation method therefor and an application thereof are provided. The series of compounds can be widely applied in the preparation of drugs for treating cancers or tumors that are at least partially mediated by CD73, autoimmune diseases and disorders and metabolic diseases, in particular drugs for treating melanoma, colon cancer, pancreatic cancer, breast cancer, prostate cancer, lung cancer, leukemia, brain tumor, lymphoma, ovarian cancer and Kaposi's sarcoma. A new generation of CD73 inhibitor drugs is expected to be developed.

公开(公告)号：US20240360102A1

公开(公告)日：2024-10-31

申请号：US18571418

申请日：2022-07-28

Applicant: Abbisko Therapeutics Co., Ltd.

Inventor： Fei YANG ,  Shuqun YANG ,  Hongping YU ,  Zhui CHEN ,  Yaochang XU

IPC: C07D401/14 ,  A61K31/506 ,  A61K31/5377

CPC classification number: C07D401/14 ,  A61K31/506 ,  A61K31/5377

Abstract: The present invention relates to a pyrimidine-4,6-diamine derivative, a preparation method therefor, and a pharmaceutical application thereof. Particularly, the present invention relates to a pyrimidine-4,6-diamine derivative having the structure of formula (I), a preparation method therefor, a pharmaceutical composition containing same, and a use of same as an EGFR inhibitor and a use of same in the preparation of drugs for the treatment and/or prevention of cancers, tumors, or metastatic diseases at least partially related to EGFR Del19 mutation, EGFR L858R mutation, EGFR L858R/C797S double mutation or EGFRDel19/C797S double mutation, in particular a use of same in the preparation of drugs for the treatment and/or prevention of hyperproliferative diseases and induced cell death disorders. The definition of each substituent in formula (I) is the same as that in the description.

公开(公告)号：US20240101573A1

公开(公告)日：2024-03-28

申请号：US18267664

申请日：2021-10-18

Applicant: Abbisko Therapeutics Co., Ltd.

Inventor： Guoliang XUN ,  Hongping YU ,  Zhui CHEN ,  Yaochang XU

IPC: C07D498/22

CPC classification number: C07D498/22

Abstract: A macrocyclic K-RAS G12C inhibitor, a preparation method therefor and use thereof. The inhibitor can be widely used in preparation of a drug for treating cancer or tumor which is at least partially mediated by a K-RAS G12C mutation, particularly a drug for treating lung, liver, gastrointestinal tract, blood system, skin, bone, genitourinary tract, nervous system, gynecological, and adrenal related malignant tumor or cancer.

公开(公告)号：US20230303575A1

公开(公告)日：2023-09-28

申请号：US18014095

申请日：2021-08-11

Applicant: Abbisko Therapeutics Co., Ltd.

Inventor： Haibing DENG ,  Haiyan YING ,  Hongping YU ,  Zhui CHEN ,  Yaochang XU

IPC: C07D487/04 ,  C07D519/00 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D519/00 ,  A61P35/00

Abstract: Provided are an FGFR and a mutation inhibitor thereof, and a preparation method therefor and the use thereof. In particular, provided are an FGFR having a structure of formula (I) and a mutation inhibitor thereof, a preparation method therefor, a pharmaceutical composition containing same, the use thereof as an FGFR and a mutation inhibitor thereof and the use thereof in the preparation of a drug for treating and/or preventing tumors or cancers mediated at least in part by means of an FGFR kinase and for treating a tumor patient having resistance to an FGFR inhibitor, and in particular, the use thereof in the preparation of a drug for treating and/or preventing a tumor patient with mutations at V561, V565, N550, N540, V555, E566, K660 and/or V550 of an FGFR signaling pathway. Each substituent of formula (I) has the same definition as in the description.