公开(公告)号：US20240360146A1

公开(公告)日：2024-10-31

申请号：US18574511

申请日：2022-06-30

Applicant: HANGZHOU HEALZEN THERAPEUTICS CO., LTD. ,  SHANGHAI INSTITTUTE OF MATERIA, CHINESE ACADEMY OF SCCIENCES

Inventor： Xinglu ZHOU ,  Jia LI ,  Xingguo LIU ,  Yubo ZHOU ,  Miao HU ,  Xiaomin LUO ,  Jiangfeng XIE ,  Weijuan KAN ,  Mingbo SU ,  Yizhe WU

IPC: C07D491/048 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61K31/675 ,  A61K47/55 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07F9/6558

CPC classification number: C07D491/048 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61K31/675 ,  A61K47/55 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07F9/65583

Abstract: Disclosed are a Bruton's tyrosine kinase and a mutant degrader thereof; or a stereoisomer thereof, or a stereoisomer mixture thereof or a pharmaceutically acceptable salt thereof, and an application thereof in the preparation of a drug for treating diseases, disorders or conditions that would benefit from the degradation of the Bruton's tyrosine kinase and the mutant thereof. The compound of the present invention can degrade BTK protein, can degrade BTKC481S protein, has an anti-proliferation inhibiting effect on tumor cell strains Mino and OCI-LY10, shows good anti-tumor activity in an OCI-LY10 subcutaneous transplantation tumor model, has an inhibiting effect on B cell activation, and can be applied to B cell or plasma cell proliferative diseases and autoimmune diseases. The compound of the present invention has good oral absorption properties, and can be applied to oral treatment of human or animal B cell or plasma cell proliferative diseases and autoimmune diseases.

公开(公告)号：US20240360129A1

公开(公告)日：2024-10-31

申请号：US18763258

申请日：2024-07-03

Applicant: Ventus Therapeutics U.S., Inc.

Inventor： Stéphane DORICH ,  Jason BURCH ,  Miguel ST-ONGE ,  Amandine CHEFSON ,  Alexandre CÔTÉ ,  Ramsay BEVERIDGE ,  Stéphane CIBLAT

IPC: C07D471/04 ,  A61K31/501 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/5377 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/501 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/5377 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

Abstract: The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein and having the Formula (I):

公开(公告)号：US20240360128A1

公开(公告)日：2024-10-31

申请号：US18763243

申请日：2024-07-03

Applicant: Ventus Therapeutics U.S., Inc.

Inventor： Stéphane DORICH ,  Jason BURCH ,  Miguel ST-ONGE ,  Amandine CHEFSON ,  Alexandre CÔTÉ

IPC: C07D471/04 ,  A61K31/501 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/5377 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/501 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/5377 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

Abstract: The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein and having the Formula (I):

公开(公告)号：US20240357923A1

公开(公告)日：2024-10-24

申请号：US18757110

申请日：2024-06-27

Applicant: IDEMITSU KOSAN CO., LTD.

Inventor： TOMOKI KATO ,  Nobuhiro Yabunouchi ,  Takahiro Fujiyama

IPC: H10K85/60 ,  C07D405/10 ,  C07D405/14 ,  C07D457/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C09B57/00 ,  C09B69/00 ,  C09K11/06 ,  H05B33/20 ,  H10K50/11 ,  H10K85/30

CPC classification number: H10K85/615 ,  C07D405/10 ,  C07D405/14 ,  C07D457/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C09B57/00 ,  C09B69/008 ,  C09K11/06 ,  H05B33/20 ,  H10K85/657 ,  H10K85/6572 ,  H10K85/6574 ,  C09K2211/1007 ,  C09K2211/1029 ,  C09K2211/1033 ,  C09K2211/1044 ,  C09K2211/1059 ,  C09K2211/1092 ,  C09K2211/185 ,  H10K50/11 ,  H10K85/342 ,  H10K85/631

Abstract: A nitrogen-containing aromatic heterocyclic derivative in which a nitrogen atom of an indenocarbazole skeleton optionally having a hetero atom or an indenoindole skeleton optionally having a hetero atom is bonded to a dibenzofuran or a dibenzothiophene directly or indirectly. The derivative realizes an organic EL device with a high emission efficiency and a long lifetime.

公开(公告)号：US20240352026A1

公开(公告)日：2024-10-24

申请号：US18612147

申请日：2024-03-21

Applicant: AcuraStem Incorporated

Inventor： Martin SMRCINA ,  Ronghua LI ,  Anil NAIR ,  Paul August ,  Kirsten BJERGARDE

IPC: C07D491/048 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D491/048 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention relates to compounds of formula (I) (shown below) useful as inhibitors of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) as well as their use for treating diseases and disorders associated with PIKfyve.

公开(公告)号：US20240343704A1

公开(公告)日：2024-10-17

申请号：US18288213

申请日：2022-05-02

Applicant: Ontario Institute for Cancer Research (OICR)

Inventor： Anh Chau ,  Methvin Isaac ,  Babu Joseph ,  Radek Laufer ,  Gennady Poda ,  Michael Prakesch ,  Pandiaraju Subramanian ,  David Uehling ,  Iain Watson ,  Brian Wilson ,  Tao Xin

IPC: C07D401/04 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/695 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D491/107 ,  C07D491/113 ,  C07D495/04 ,  C07D498/04 ,  C07D498/10 ,  C07F7/08

CPC classification number: C07D401/04 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/695 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D491/107 ,  C07D491/113 ,  C07D495/04 ,  C07D498/04 ,  C07D498/10 ,  C07F7/0836

Abstract: The present application relates to halo-substituted heterocyclic compounds of Formula (I): or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer.

公开(公告)号：US20240342186A1

公开(公告)日：2024-10-17

申请号：US18734077

申请日：2024-06-05

Applicant: Boehringer Ingelheim International GmbH

Inventor： Annekatrin Charlotte HEIMANN ,  Sandra Ruth HANDSCHUH ,  Christoph HOENKE ,  Cédrickx GODBOUT ,  Christian GNAMM ,  Patrick GROSS ,  Marc Alexander GRUNDL ,  Joerg Thomas KLEY ,  Christian Andreas KUTTRUFF ,  Dirk REINART ,  Raphael STUBER ,  Theodor THEIS

IPC: A61K31/5386 ,  A61K31/4412 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61K39/395 ,  A61K45/06 ,  A61P37/06 ,  C07D491/048 ,  C07D519/00

CPC classification number: A61K31/5386 ,  A61K31/4412 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61K39/3955 ,  A61K45/06 ,  A61P37/06 ,  C07D491/048 ,  C07D519/00

Abstract: The invention relates to new proline derivatives of formula (I) as cGAS inhibitors,






wherein
wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and G are defined as in claim 1,
and prodrugs or pharmaceutically acceptable salts of these compounds
for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), non-alcoholic steatotic hepatitis (NASH), interstitial lung disease (ILD) and idiopathic pulmonary fibrosis (IPF).

公开(公告)号：US12116367B2

公开(公告)日：2024-10-15

申请号：US18306236

申请日：2023-04-25

Applicant: FUJIAN AKEYLINK BIOTECHNOLOGY CO., LTD.

Inventor： Shuhui Chen ,  Yaxun Yang ,  Jianchen Zhang ,  Peng Li ,  Haiying He ,  Zheng Wang ,  Jian Li

IPC: C07D403/12 ,  A61P31/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04

CPC classification number: C07D471/08 ,  A61P31/14 ,  C07D403/12 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04

Abstract: Disclosed are a ring-modified proline short peptide compound and the use thereof, and specifically disclosed is a compound represented by formula (X) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US12098145B2

公开(公告)日：2024-09-24

申请号：US18543599

申请日：2023-12-18

Applicant: Libra Therapeutics, Inc.

Inventor： James Guy Breitenbucher ,  Maria Pia Catalani ,  Ali Munaim Yousif

IPC: C07D263/48 ,  A61K31/422 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D491/048 ,  C07D491/056 ,  C07D491/08 ,  C07D491/107 ,  C07D495/10 ,  C07D498/04

CPC classification number: C07D413/04 ,  C07D263/48 ,  C07D413/12 ,  C07D413/14 ,  C07D491/048 ,  C07D491/056 ,  C07D491/08 ,  C07D491/107 ,  C07D495/10 ,  C07D498/04

Abstract: Described herein are oxazole TRPML1 agonists and pharmaceutical compositions comprising said agonists. The subject compounds and compositions are useful for the treatment of TRPML1-mediated disorders or diseases.

公开(公告)号：US20240298538A1

公开(公告)日：2024-09-05

申请号：US18564003

申请日：2021-09-24

Applicant: KYULUX, INC.

Inventor： Yong Joo CHO ,  Yoshitake SUZUKI ,  Masataka YAMASHITA ,  Naomi SHIMAMURA ,  Yu YAMANE ,  Satoshi OHNO ,  Shinhyung CHOI ,  Noboru SANADA

IPC: H10K85/60 ,  C07D491/048 ,  C07D495/04 ,  C09K11/02 ,  C09K11/06 ,  H10K50/12

CPC classification number: H10K85/6572 ,  C07D491/048 ,  C07D495/04 ,  C09K11/02 ,  C09K11/06 ,  H10K85/657 ,  C09K2211/1007 ,  C09K2211/1018 ,  H10K50/12

Abstract: A compound represented by the following general formula is an excellent light emitting material. R1 to R5 each represent a hydrogen atom, a deuterium atom, or a substituent other than a cyano group, but one or more of R1 to R5 is an aryl group or a pyridyl group, two or more of R1 to R5 are donor groups, and one or more of them are a substituted ring-fused indol-1-yl group (the number of rings constituting the fused ring is 4 or more).