公开(公告)号：US20240365662A1

公开(公告)日：2024-10-31

申请号：US18681320

申请日：2022-08-05

Applicant: SUMITOMO CHEMICAL CO., LTD.

Inventor： Michal Maciejczyk ,  Nir Yaacobi-Gross ,  Florence Bourcet ,  Ben Gardner ,  Yuki Yokoi

IPC: H10K85/60 ,  C07D519/00 ,  C08G61/12 ,  H10K30/30 ,  H10K85/10

CPC classification number: H10K85/657 ,  C07D519/00 ,  C08G61/126 ,  H10K85/113 ,  H10K85/151 ,  H10K85/626 ,  H10K85/655 ,  H10K85/6576 ,  C08G2261/124 ,  C08G2261/1412 ,  C08G2261/149 ,  C08G2261/18 ,  C08G2261/228 ,  C08G2261/324 ,  C08G2261/3246 ,  C08G2261/94 ,  H10K30/30

Abstract: A compound of formula (I), D1 and D2 are electron-donating groups; A2 and A3 are electron-accepting groups; B1 and B2 are bridging groups; x1 and x2 are 0, 1, 2 or 3; y1 and y2 are at least 1; z1 and z2 are 0, 1, 2 or 3; and A1 is a group of formula (II) wherein Ar1 is an aromatic or heteroaromatic group; and Y is O, S, NR4 or R1-C═C—R1 wherein R1 in each occurrence is independently H or a substituent wherein two substituents R1 may be linked to form a monocyclic or polycyclic ring and R4 is H or a substituent. The compound may be used as an electron-accepting material with an electron-donating material in an organic photodetector.

公开(公告)号：US20240360133A1

公开(公告)日：2024-10-31

申请号：US18254375

申请日：2021-11-26

Applicant: Jiangsu Hengrui Pharmaceuticals Co., Ltd. ,  Shanghai Hengrui Pharmaceutical Co., Ltd.

Inventor： Xiaomin Zhang ,  Weimin Hu ,  Feng He ,  Weikang Tao

IPC: C07D471/14 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/496 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D471/14 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/496 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to a fused tricyclic compound, a preparation method therefor, and an application thereof in medicine. Specifically, the present invention relates to a fused tricyclic compound represented by general formula (1), a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof as a therapeutic agent, particularly a use as a TLR7/8/9 inhibitor and a use in preparing a drug for the treatment and/or prevention of inflammatory and autoimmune diseases. The definition of each group in general formula (1) is as defined in the description.

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：US12129266B2

公开(公告)日：2024-10-29

申请号：US17299999

申请日：2019-12-03

Applicant: Shenzhen TargetRx, Inc.

Inventor： Yihan Wang ,  Xingye Ren

IPC: C07D519/00 ,  C07D471/04

CPC classification number: C07D519/00 ,  C07D471/04

Abstract: The present disclosure provides a substituted pyrazolo[1,5-a]pyridine compound, a composition including the same, and a use thereof. The substituted pyrazolo[1,5-a]pyridine compounds is a compound represented by formula (I) or the tautomers, stereoisomers, prodrugs, crystal forms, pharmaceutically acceptable salts, hydrates or solvates thereof. The compound of the present disclosure and composition thereof are useful for treating RET kinase-mediated diseases or conditions and have more excellent pharmacokinetic properties.

公开(公告)号：US12129263B2

公开(公告)日：2024-10-29

申请号：US17511193

申请日：2021-10-26

Applicant: Denali Therapeutics Inc.

Inventor： Javier de Vicente Fidalgo ,  Anthony A. Estrada ,  Jianwen A. Feng ,  Brian Fox ,  Cinzia Maria Francini ,  Christopher R. H. Hale ,  Cheng Hu ,  Colin Philip Leslie ,  Maksim Osipov ,  Elena Serra ,  Zachary K. Sweeney ,  Arun Thottumkara

IPC: C07D498/04 ,  A61K31/553 ,  A61P3/10 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P27/02 ,  A61P37/00 ,  A61P43/00 ,  C07D223/16 ,  C07D267/04 ,  C07D267/14 ,  C07D413/14 ,  C07D498/10 ,  C07D519/00

CPC classification number: C07D498/04 ,  C07D223/16 ,  C07D267/04 ,  C07D267/14 ,  C07D413/14 ,  C07D519/00

Abstract: The present disclosure relates generally to compounds and compositions, intermediates, processes for their preparation, and their use as kinase inhibitors.

公开(公告)号：US20240357926A1

公开(公告)日：2024-10-24

申请号：US17414758

申请日：2019-12-17

Applicant: Merck Patent GmbH

Inventor： Amir PARHAM ,  Jonas KROEBER ,  Christian EHRENEICH ,  Jonas ENGELHART ,  Christian EICKHOFF ,  Jens PFALZGRAF

IPC: H10K85/60 ,  C07D471/06 ,  C07D519/00 ,  C09K11/06 ,  H10K50/12

CPC classification number: H10K85/6572 ,  C07D471/06 ,  C07D519/00 ,  C09K11/06 ,  H10K85/615 ,  H10K85/657 ,  H10K85/6574 ,  H10K85/6576 ,  C09K2211/1018 ,  H10K50/12

Abstract: The present invention relates to compounds suitable for use in electronic devices, and to electronic devices, especially organic electroluminescent devices, comprising these compounds.

公开(公告)号：US12122791B2

公开(公告)日：2024-10-22

申请号：US17842612

申请日：2022-06-16

Applicant: Hoffmann-La Roche Inc.

Inventor： Jean-Michel Adam ,  Serena Maria Fantasia ,  Daniel Vincent Fishlock ,  Fabienne Hoffmann-Emery ,  Gerard Moine ,  Christophe Pfleger ,  Christian Moessner

IPC: C07D519/00 ,  B01J23/44 ,  B01J23/755

CPC classification number: C07D519/00 ,  B01J23/44 ,  B01J23/755

Abstract: The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.

公开(公告)号：US20240343742A1

公开(公告)日：2024-10-17

申请号：US18643536

申请日：2024-04-23

Applicant: INCYTE CORPORATION

Inventor： Peter Carlsen ,  Xiaozhao Wang ,  Alexander Sokolsky ,  Pei Gan ,  Rocco Policarpo ,  Wenqing Yao

IPC: C07D519/00 ,  A61P35/00 ,  C07D455/02 ,  C07D487/02

CPC classification number: C07D519/00 ,  A61P35/00 ,  C07D455/02 ,  C07D487/02

Abstract: Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.

公开(公告)号：US20240343733A1

公开(公告)日：2024-10-17

申请号：US18576940

申请日：2022-07-07

Applicant: BIOGEN MA INC. ,  C4 THRAPEUTICS, INC.

Inventor： Kevin M. Guckian ,  Emily Anne Peterson ,  Fang Gao ,  Ryan Evans ,  Eric Stefan ,  Jeremy L. Yap ,  Corey Don Anderson ,  Morgan Welzel O'Shea ,  Jae Young M. Ahn ,  Christopher G. Nasveschuk ,  James A. Henderson

IPC: C07D487/04 ,  A61K31/4545 ,  A61K31/513 ,  A61K31/519 ,  C07D401/14 ,  C07D471/04 ,  C07D487/10 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/4545 ,  A61K31/513 ,  A61K31/519 ,  C07D401/14 ,  C07D471/04 ,  C07D487/10 ,  C07D519/00

Abstract: This disclosure relates to compounds of Formula (A): IRAK-L-DSM (A), or a pharmaceutically acceptable salt thereof, wherein DSM is a degradation signaling moiety that is covalently attached to the linker L, L is a linker that covalently attaches IRAK to DSM; and IRAK is an IRAK4 binding moiety represented by Formula (I) that is covalently attached to linker L; in which all of the variables are as defined in the application. Compounds or pharmaceutically acceptable salts thereof as described herein are capable of activating the selective ubiqitination of IRAK4 proteins via the ubiquitin-proteasome pathways (UPP) and cause degradation of IRAK4 proteins. The present disclosure also provides methods of treating disorders responsive to modulation of IRAK4 activity and/or degradation of IRAK4 with at least one compound described herein.

公开(公告)号：US20240336614A1

公开(公告)日：2024-10-10

申请号：US18487690

申请日：2023-10-16

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Upul Keerthi BANDARAGE ,  Cavan McKeon BLIGH ,  Diane BOUCHER ,  Michael John BOYD ,  Michael Aaron BRODNEY ,  Michael Philip CLARK ,  Veronique DAMAGNEZ ,  Lev Tyler Dewey FANNING ,  Robert Francis FIMOGNARI ,  Gabrielle Simone FLEMING ,  Kevin James GAGNON ,  Pedro Manuel GARCIA BARRANTES ,  Robert Daniel GIACOMETTI ,  Simon GIROUX ,  Ronald Lee GREY, JR. ,  Samantha GUIDO ,  Amy Beth HALL ,  Sarah Carol HOOD ,  Dennis James HURLEY ,  Mac Arthur JOHNSON, JR. ,  Peter Jones ,  Sarathy KESAVAN ,  Mei-Hsiu LAI ,  Siying LIU ,  Adam LOOKER ,  Brad MAXWELL ,  John Patrick MAXWELL ,  Ales MEDEK ,  Philippe Marcel NUHANT ,  Kirk Alan OVERHOFF ,  Setu RODAY ,  Stefanie ROEPER ,  Steven M. RONKIN ,  Rupa SAWANT ,  Yi SHI ,  Muna SHRESTHA ,  Marisa SPOSATO ,  Kathy STAVROPOULOS ,  Rebecca Jane SWETT ,  Timothy Lewis TAPLEY ,  Qing TANG ,  Stephen THOMSON ,  Jinwang XU ,  Mariam ZAKY ,  Kevin Michael COTTRELL

IPC: C07D487/04 ,  A61K9/16 ,  A61K31/4162 ,  C07D491/18 ,  C07D513/04 ,  C07D519/00 ,  C07F9/6561 ,  C07H15/26

CPC classification number: C07D487/04 ,  A61K9/1635 ,  A61K9/1652 ,  A61K31/4162 ,  C07D491/18 ,  C07D513/04 ,  C07D519/00 ,  C07F9/6561 ,  C07H15/26 ,  C07B2200/13

Abstract: The disclosure provides compounds useful for treating alpha-1 antitrypsin deficiency (AATD), according to formula (I):




tautomers thereof, pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable salts of the tautomers, deuterated derivatives of the compounds, deuterated derivatives of the tautomers, and deuterated derivatives of the salts, solid forms of those compounds and processes for making those compounds.