公开(公告)号：US20250066389A1

公开(公告)日：2025-02-27

申请号：US18710312

申请日：2022-11-18

Applicant: Rgenta Therapeutics, Inc.

Inventor： Travis T. Wager ,  Zhiping Weng ,  Hualin Simon Xi

IPC: C07D519/00 ,  A61K31/416 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D495/04 ,  C07D498/10

Abstract: The present disclosure relates to compounds of Formula (I), and subformulas thereof, and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds of the present disclosure may act as small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded genes, and methods of use of the compounds for modulating splicing and treating related diseases and conditions. The compounds disclosed herein may possess activity toward various genetic pathways and are accordingly useful in methods of treatment of diseases or disorders of the human or animal body.

公开(公告)号：US20250051321A1

公开(公告)日：2025-02-13

申请号：US18713633

申请日：2022-11-25

Applicant: SHANGHAI JEMINCARE PHARMACEUTICAL CO., LTD.

Inventor： Gang DENG ,  Shuchun GUO ,  Jun FAN ,  Zhitao ZHANG ,  Nan WU ,  Wenqiang SHI ,  Zhihua FANG ,  Jianbo FENG ,  Jianbiao PENG ,  Haibing GUO

IPC: C07D417/14 ,  A61K31/4375 ,  A61K31/473 ,  A61K31/4741 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/4995 ,  C07D471/04 ,  C07D471/10 ,  C07D471/14 ,  C07D487/10 ,  C07D491/048 ,  C07D491/107 ,  C07D491/147 ,  C07D495/10 ,  C07D498/04 ,  C07D519/00

Abstract: Disclosed are a tricyclic derivative and a preparation method therefor and an application thereof. Specifically, disclosed are a compound shown in formula (I) and an optical isomer thereof or a pharmaceutically acceptable salt thereof, and an application of the compound as an Autotaxin inhibitor.

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：US20250034116A1

公开(公告)日：2025-01-30

申请号：US18898598

申请日：2024-09-26

Applicant: BeBetter Med Inc.

Inventor： Xiong CAI ,  Yuanhui QING ,  Qijie HE ,  Yiting LIU ,  Shaobin WU ,  Yaonan HE ,  Huichen TAN ,  Yunwo WENG ,  Bin LIU ,  Mingsheng LIN ,  Xinlan DENG ,  Junling ZHU ,  Qiao FENG ,  Changgeng QIAN

IPC: C07D401/14 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K38/26 ,  A61P3/04 ,  A61P3/10 ,  C07D401/08 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10

Abstract: The present invention disclosed a 1,4-diheterocyclic substituted aromatic ring or aromatic heterocyclic compound represented by formula (I). The compound can effectively inhibit the generation of 20-HETE, and has high activity, high selectivity and good pharmacokinetic characteristics. By means of the inhibition on the generation of 20-HETE, the compound can be used for treating various diseases related to 20-HETE, and thus has a great application value.

公开(公告)号：US20250026761A1

公开(公告)日：2025-01-23

申请号：US18700339

申请日：2022-10-07

Applicant: VASA THERAPEUTICS SPÓLKA Z OGRANICZONA ODPOWIEDZIALNOSCIA

Inventor： Benjamin Anthony Pratt ,  Piotr Jakub Lipinski

IPC: C07D487/08 ,  A61K31/4995 ,  A61K31/5377

Abstract: Provided herein are compounds that are MMP inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in treating a disease, disorder or condition selected from cardiovascular disorders, lung disorders, renal disorders, hepatic disorders, and scleroderma pigmentosum. Formula (I)

公开(公告)号：US20240425498A1

公开(公告)日：2024-12-26

申请号：US18698137

申请日：2022-10-03

Applicant: FORX THERAPEUTICS AG

Inventor： Ulrich Luecking ,  Andreas Goutopoulos ,  Jin Tian ,  Sotirios Sotiriou ,  Luca Iacovino ,  Alena Freudenmann ,  Olivier Querolle

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/438 ,  A61K31/439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/499 ,  A61K31/4995 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61K31/675 ,  C07D519/00 ,  C07F9/6561

Abstract: The present invention relates to a compound of formula (I) or an enantiomer, diastereoisomer, tautomer, pharmaceutically acceptable solvate, pharmaceutically acceptable crystal form, pharmaceutically acceptable salt or a prodrug thereof. The present invention further relates to the compound of formula (I) of the present invention for use in therapy. Instant compounds are particularly useful as PARC inhibitors, and can be used in a method of treatment of a proliferative disorder, preferably of cancer.

公开(公告)号：US20240408085A1

公开(公告)日：2024-12-12

申请号：US18688647

申请日：2022-09-01

Applicant: XIZANG HAISCO PHARMACEUTICAL CO., LTD.

Inventor： Chen ZHANG ,  Yuting LIAO ,  Yonghua LU ,  Junbin ZHAO ,  Sijia ZOU ,  Yan YU ,  Pingming TANG ,  Qiu GAO ,  Xinfan CHENG ,  Fei YE ,  Yao LI ,  Jia NI ,  Pangke YAN

IPC: A61K31/4995 ,  A61K31/427 ,  A61K31/454 ,  A61P35/00 ,  C07D211/14 ,  C07D277/22 ,  C07D309/26 ,  C07D487/08

Abstract: A compound of general formula (I) or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt, or a co-crystal thereof, an intermediate thereof, and a use thereof in Bcl-2 family proteins-related diseases such as cancer. B-L-K (I)

公开(公告)号：US20240358688A1

公开(公告)日：2024-10-31

申请号：US18756533

申请日：2024-06-27

Applicant: Boehringer Ingelheim International GmbH

Inventor： Harald ENGELHARDT ,  Mark PETRONCZKI ,  Juergen RAMHARTER ,  Ulrich REISER ,  Heinz STADTMUELLER ,  Dirk SCHARN ,  Tobias WUNBERG

IPC: A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/553 ,  A61P35/00 ,  C07D211/04 ,  C07D519/00

CPC classification number: A61K31/437 ,  A61K31/4545 ,  A61K31/4995 ,  A61K31/553 ,  A61P35/00 ,  C07D211/04 ,  C07D519/00 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541

Abstract: The present invention encompasses compounds of formula (I)




wherein the groups R1 to R4 and X1 to X5 have the meanings given in the claims and specification, their use as inhibitors of mutant EGFR, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

公开(公告)号：US12064421B2

公开(公告)日：2024-08-20

申请号：US17514145

申请日：2021-10-29

Applicant: Boehringer Ingelheim International GmbH

Inventor： Harald Engelhardt ,  Mark Petronczki ,  Juergen Ramharter ,  Ulrich Reiser ,  Heinz Stadtmueller ,  Dirk Scharn ,  Tobias Wunberg

IPC: C07D211/04 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/4995 ,  A61K31/553 ,  A61P35/00 ,  C07D519/00 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541

CPC classification number: A61K31/437 ,  A61K31/4545 ,  A61K31/4995 ,  A61K31/553 ,  A61P35/00 ,  C07D211/04 ,  C07D519/00 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541

Abstract: The present invention encompasses compounds of formula (I)




wherein the groups R1 to R4 and X1 to X5 have the meanings given in the claims and specification, their use as inhibitors of mutant EGFR, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

公开(公告)号：US20240262821A1

公开(公告)日：2024-08-08

申请号：US18557852

申请日：2022-05-06

Applicant: Exscientia Al Limited

Inventor： Peter Ray ,  Anthony Bradley ,  Simon Richards ,  Catarina Santos ,  Jeremy Besnard ,  Jérôme Meneyrol ,  Virginie Suchaud

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/551 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/551 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00

Abstract: Disclosed are compounds, compositions and methods for treating disease, syndromes, conditions and disorders that are affected by the modulation of PKC-theta. Such compounds are represented by Formula I, wherein the variables are defined herein. (I)