公开(公告)号：US20230348482A1

公开(公告)日：2023-11-02

申请号：US18027990

申请日：2022-01-13

申请人： Universidad Autonoma De Madrid ,  Consejo Superior De Investigaciones Cientificas ,  Universidad Miguel Hernandez De Elche ,  Fundacion De Investigacion Biomedica Del Hospital Universitario De La Princesa

发明人： Antonio Cuadrado Pastor ,  Raquel Fernandez Gines ,  Jose Antonio Encinar ,  Rafael Leon Martinez ,  Juan Felipe Franco Gonzalez ,  Manuela Garcia Lopez ,  Maria Isabe Rodriguez Franco ,  Ana Isabel Rojo Sanchis

IPC分类号： C07D487/20 ,  A61P1/16 ,  G01N33/50

CPC分类号： C07D487/20 ,  A61P1/16 ,  G01N33/5008

摘要： The present invention relates to NRF2-βTrCP interaction inhibitors with general formula I and its derivate salts for use in the treatment of NRF2-related diseases caused by chronic inflammation and oxidative stress. More specifically the present invention relates to NRF2-βTrCP interaction inhibitors with specific formula I and its derivate salts for treating diseases of the liver related with chronic inflammation and oxidative stress, such as fatty liver disease.

公开(公告)号：US11629150B2

公开(公告)日：2023-04-18

申请号：US17121392

申请日：2020-12-14

申请人： G1 Therapeutics, Inc.

发明人： Alexander Smith ,  Hannah S. White ,  Francis Xavier Tavares ,  Sergiy Krasutsky ,  Jian-Xie Chen ,  Roberta L. Dorrow ,  Hua Zhong

IPC分类号： C07D487/20 ,  C07D487/14 ,  C07D403/04 ,  A61P35/00

摘要： This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.

公开(公告)号：US11466013B2

公开(公告)日：2022-10-11

申请号：US16973335

申请日：2019-06-06

申请人： Betta Pharmaceuticals Co., LTD

发明人： Hao Wu ,  Wei Gu ,  Xiaojing Tang ,  Wei Wang ,  Bo Zhan ,  Dongjie Feng ,  Yongxin Ke ,  Zhongyan Chen ,  Yifei Shen ,  Wenmao Wu ,  Xintao Zhao ,  Hong Lan ,  Jiabing Wang ,  Lieming Ding

IPC分类号： C07D487/04 ,  A61P35/00 ,  C07D401/04 ,  C07D403/14 ,  C07D417/04 ,  C07D487/20 ,  C07D491/20 ,  C07D513/04 ,  C07D519/00

摘要： Disclosed are a compound (as shown in formula I) as an extracellular signal-regulated kinase (ERK) inhibitor, a pharmaceutical composition thereof, a preparation method therefor, and use thereof in treating ERK-mediated diseases. Said compound plays a role by regulating a plurality of processes such as cell proliferation, apoptosis, migration and angiogenesis.

公开(公告)号：US20220306644A1

公开(公告)日：2022-09-29

申请号：US17742315

申请日：2022-05-11

申请人： G1 Therapeutics, Inc.

发明人： Jay Copeland Strum

IPC分类号： C07D487/20 ,  C07D487/04

摘要： This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.

公开(公告)号：US20210395259A1

公开(公告)日：2021-12-23

申请号：US17153516

申请日：2021-01-20

申请人： G1 Therapeutics, Inc.

发明人： Francis X. Tavares ,  Jay Copeland Strum

IPC分类号： C07D487/14 ,  C07D487/20 ,  A61K31/499 ,  A61K31/527 ,  C07D498/14 ,  C07D519/00

摘要： Compounds of Formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

公开(公告)号：US11174267B2

公开(公告)日：2021-11-16

申请号：US15735873

申请日：2016-06-13

申请人： The Regents of the University of California

发明人： David Lee Van Vranken ,  Haoping Liu ,  Ilandari Dewage Udara Anulal Premachandra ,  Fuqiang Wang ,  Chengtian Shen ,  Kevin Andre Scott ,  Shelley Ren-An Lane ,  Aaron David Mood ,  Stanley Chungsing Hiew

IPC分类号： C07D487/20 ,  A61P31/10 ,  C07D487/14 ,  A61K45/06

摘要： Small molecules comprised of spiroindolinone analogues are provided. Some spiroindolinones are provided with a particular relative stereochemistry in which the indolone carbonyl and all three hydrogens are on the same face of the central pyrrolidine ring. A stereoselective method of synthesis is provided for making some of the spiroindolinones described above. Formulations and medicaments are also provided that are directed to the treatment of disease, such as, for example, fungal infections. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.

公开(公告)号：US20210077498A1

公开(公告)日：2021-03-18

申请号：US17102311

申请日：2020-11-23

申请人： G1 Therapeutics, Inc.

发明人： Jay Copeland Strum ,  John Emerson Bisi ,  Patrick Joseph Roberts ,  Francis Xavier Tavares

IPC分类号： A61K31/527 ,  A61K45/06 ,  C07D487/20 ,  A61K38/18 ,  A61K38/19 ,  A61K38/20 ,  A61K31/202 ,  A61K31/702 ,  A61K31/519 ,  A61N5/10

摘要： This invention is in the area of improved compounds and methods for transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC), from the damage associated with ionizing radiation (IR) exposure using selective radioprotectants.

公开(公告)号：US20200277300A1

公开(公告)日：2020-09-03

申请号：US15931330

申请日：2020-05-13

申请人： G1 Therapeutics, Inc.

发明人： Francis X. Tavares ,  Jay Copeland Strum

IPC分类号： C07D487/14 ,  C07D487/20 ,  A61K31/499 ,  C07D498/14 ,  C07D519/00

摘要： Compounds of Formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

公开(公告)号：US10696682B2

公开(公告)日：2020-06-30

申请号：US16226430

申请日：2018-12-19

申请人： G1 Therapeutics, Inc.

发明人： Francis X. Tavares ,  Jay Copeland Strum

IPC分类号： A61K31/519 ,  C07D487/14 ,  C07D487/20 ,  A61K31/499 ,  C07D498/14 ,  C07D519/00

摘要： Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

公开(公告)号：US20190135820A1

公开(公告)日：2019-05-09

申请号：US16230381

申请日：2018-12-21

申请人： G1 Therapeutics, Inc.

发明人： Alexander Smith ,  Hannah S. White ,  francis Xavier Tavares ,  Sergiy Krasutsky ,  Jian-Xie Chen ,  Roberta L. Dorrow ,  Hua Zhong

IPC分类号： C07D487/20 ,  C07D403/04

摘要： This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.