公开(公告)号：US12234244B2

公开(公告)日：2025-02-25

申请号：US17716707

申请日：2022-04-08

Applicant: Araxes Pharma LLC

Inventor： Liansheng Li ,  Jun Feng ,  Tao Wu ,  Pingda Ren ,  Yi Liu ,  Yuan Liu ,  Yun Oliver Long

IPC: A61K31/517 ,  C07D215/46 ,  C07D215/54 ,  C07D217/22 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D241/44 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D409/04 ,  C07D487/04 ,  C07D495/04

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, have the following structure: wherein A, L1, L2, Q, R1, R2a, R3a, R3b, R4a, R4b, R9, R10, Y, and Z are as exemplified herein. Pharmaceutical compositions comprising such compounds, methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, and methods associated with preparation of such compounds are also provided.

公开(公告)号：US20240376058A1

公开(公告)日：2024-11-14

申请号：US18408956

申请日：2024-01-10

Applicant: Deciphera Pharmaceuticals, LLC

Inventor： Daniel L. Flynn ,  Patrick Kearney ,  Jeffery Zwicker ,  Gada Al-Ani ,  Salim Javed ,  Yu Mi Ahn ,  Kristen Stoltz ,  Bertrand Le Bourdonnec

IPC: C07D239/84 ,  A61P35/00 ,  C07D401/12 ,  C07D471/04

Abstract: Described herein are compounds that are inhibitors of GCN2 kinase or PERK kinase, and methods of treating diseases, including diseases associated with GCN2 kinase or PERK kinase, with said compounds.

公开(公告)号：US12071424B2

公开(公告)日：2024-08-27

申请号：US18176362

申请日：2023-02-28

Applicant: Cornell University

Inventor： Joseph P. Vacca ,  Dansu Li ,  Sarah Elizabeth Bettigole

IPC: C07D401/04 ,  A61K31/517 ,  A61P35/00 ,  C07D217/22 ,  C07D239/74 ,  C07D239/84 ,  C07D239/94 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D401/10 ,  A61P35/00 ,  C07D217/22 ,  C07D239/84 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D413/04 ,  C07D417/04

Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.

公开(公告)号：US11912668B2

公开(公告)日：2024-02-27

申请号：US17528478

申请日：2021-11-17

Applicant: Deciphera Pharmaceuticals, LLC

Inventor： Daniel L. Flynn ,  Patrick Kearney ,  Jeffery Zwicker ,  Gada Al-Ani ,  Salim Javed ,  Yu Mi Ahn ,  Kristen Stoltz ,  Bertrand Le Bourdonnec

IPC: C07D471/04 ,  C07D239/84 ,  A61P35/00 ,  C07D401/12

CPC classification number: C07D239/84 ,  A61P35/00 ,  C07D401/12 ,  C07D471/04

Abstract: Described herein are compounds, such as compounds represented by Formula I-R:




and pharmaceutically acceptable salts, enantiomers, stereoisomers, and tautomers thereof, that are inhibitors of GCN2 kinase or PERK kinase, and methods of treating diseases, including diseases associated with GCN2 kinase or PERK kinase, with said compounds.

公开(公告)号：US20230303586A1

公开(公告)日：2023-09-28

申请号：US18178452

申请日：2023-03-03

Applicant: Araxes Pharma LLC

Inventor： Liansheng LI ,  Jun FENG ,  Tao WU ,  Pingda REN ,  Yi LIU ,  Yuan Liu ,  Yun Oliver Long

IPC: C07D495/04 ,  C07D239/94 ,  C07D401/12 ,  C07D217/22 ,  C07D215/46 ,  C07D215/54 ,  C07D239/84 ,  C07D487/04 ,  C07D239/95 ,  C07D403/04 ,  C07D241/44 ,  C07D401/04 ,  C07D409/04

CPC classification number: C07D495/04 ,  C07D215/46 ,  C07D215/54 ,  C07D217/22 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D241/44 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D409/04 ,  C07D487/04

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):





or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

公开(公告)号：US11655239B2

公开(公告)日：2023-05-23

申请号：US17628246

申请日：2020-07-17

Applicant: SHANGHAI INSTITUTE OF MATERIAL MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Bing Xiong ,  Jia Li ,  Meiyu Geng ,  Jingkang Shen ,  Yi Zang ,  Jing Ai ,  Danqi Chen ,  Qi Wang ,  Ying Dong ,  Xia Peng ,  Yinchun Ji ,  Qian Tan

IPC: C07D239/84 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14 ,  A61P11/00 ,  A61K31/517 ,  A61K45/06 ,  C07D403/14

CPC classification number: C07D403/12 ,  A61K31/517 ,  A61K45/06 ,  A61P11/00 ,  C07D239/84 ,  C07D401/14 ,  C07D403/14 ,  C07D417/14

Abstract: The present disclosure relates to a fused ring pyrimidine amino compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically disclosed in the present disclosure are the compound shown in formula I, a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof. The fused ring pyrimidine amino compound of the present application has good inhibitory activity against DDRs, particularly DDR2, and has a good therapeutic effect on tumors and fibrotic diseases, especially pulmonary inflammation and pulmonary fibrosis. Also disclosed in the present disclosure are a preparation method for the compound shown in formula I, and a use thereof.

公开(公告)号：US11649224B2

公开(公告)日：2023-05-16

申请号：US17313688

申请日：2021-05-06

Applicant: Cornell University

Inventor： Joseph P. Vacca ,  Dansu Li ,  Sarah Bettigole

IPC: C07D401/04 ,  C07D403/04 ,  A61P35/00 ,  C07D239/84 ,  C07D413/04 ,  C07D217/22 ,  C07D401/12 ,  C07D417/04 ,  A61K31/517

CPC classification number: C07D403/04 ,  A61K31/517 ,  A61P35/00 ,  C07D217/22 ,  C07D239/84 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D417/04

Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.

公开(公告)号：US20230043970A1

公开(公告)日：2023-02-09

申请号：US17506367

申请日：2021-10-20

Applicant: NEUPHARMA, INC

Inventor： Xiangping QIAN ,  Yong-Liang ZHU

IPC: C07D239/74 ,  C07D403/12 ,  A61K45/06 ,  C07D403/04 ,  C07D239/84 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D471/04 ,  C07D473/32 ,  C07D487/04

Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.

公开(公告)号：US20220249487A1

公开(公告)日：2022-08-11

申请号：US17643623

申请日：2021-12-10

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Georgette Castanedo ,  Paul Gibbons ,  Joachim Rudolph ,  Yao Wu ,  Guosheng Wu

IPC: A61K31/517 ,  C07D401/12 ,  C07D239/84 ,  C07D401/04 ,  C07D401/14 ,  A61K31/573 ,  A61K38/07 ,  A61K31/69 ,  A61K31/454 ,  A61K39/395 ,  C07D405/14

Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof useful in the treatment of IRE1-related diseases and disorders described herein.

公开(公告)号：US11339132B2

公开(公告)日：2022-05-24

申请号：US16071233

申请日：2016-12-30

Applicant: DUK SAN NEOLUX CO., LTD.

Inventor： Soung Yun Mun ,  Sun-Hee Lee ,  Bumsung Lee ,  Junghwan Park ,  Gyu Min Lee

IPC: C07D239/84 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D403/12 ,  C07D403/14 ,  C07D491/048 ,  H01L51/00 ,  H01L51/50 ,  C07D403/04

Abstract: The present invention provides the compound represented by Formula 1, an organic electric element comprising a first electrode, a second electrode, and an organic material layer formed between the first electrode and the second electrode, and electronic device thereof, and by comprising the compound represented by Formula 1 in the organic material layer, the driving voltage of the organic electronic device can be lowered, and the luminous efficiency and life time of the organic electronic device can be improved.