公开(公告)号：US20240360146A1

公开(公告)日：2024-10-31

申请号：US18574511

申请日：2022-06-30

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

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

IPC分类号： 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分类号： 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

摘要： 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：US20240343704A1

公开(公告)日：2024-10-17

申请号：US18288213

申请日：2022-05-02

申请人： Ontario Institute for Cancer Research (OICR)

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

IPC分类号： 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分类号： 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

摘要： 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：US12116375B2

公开(公告)日：2024-10-15

申请号：US18490700

申请日：2023-10-19

申请人： The Regents of the University of California

发明人： Jonathan Ostrem ,  Ulf Peters ,  Kevan M. Shokat

IPC分类号： C07D409/04 ,  A61K38/17 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/185 ,  C07D295/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D495/04 ,  C12N9/14 ,  C12Q1/6886

CPC分类号： C07D495/04 ,  A61K38/1709 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/185 ,  C07D295/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C12N9/14 ,  C12Q1/6886 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Y306/05002 ,  G01N2500/04

摘要： K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

公开(公告)号：US20240336611A1

公开(公告)日：2024-10-10

申请号：US18547190

申请日：2022-02-23

申请人： Insilico Medicine IP Limited

发明人： Aleksandrs ZAVORONKOVS ,  Aleksandr ALIPER ,  Vladimir ALADINSKIY ,  Andrey KUKHARENKO ,  Luoheng QUIN ,  Xin CHENG

IPC分类号： C07D471/08 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4995 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/10

CPC分类号： C07D471/08 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4995 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/10

摘要： Provided are TNIK and/or MAP4K4 kinases inhibitors for the treatment of disease. In one aspect, disclosed herein are kinase inhibitors having a structure of Formulas (A), (A*), (I), (II), (AA), (B), (C), (D), (B*), (C*) and (D*). Further described herein are pharmaceutical composition comprising these compounds and methods of using these compounds. In one aspect, disclosed herein are methods of treating a disease or condition by administering the kinases inhibitors described herein.

公开(公告)号：US20240309002A1

公开(公告)日：2024-09-19

申请号：US18665923

申请日：2024-05-16

申请人： Shionogi & Co., Ltd.

发明人： Kouhei NODU ,  Yusuke Tateno ,  Kengo Masuda ,  Yuji Nishiura ,  Yoshikazu Sasaki ,  Yu Hinata

IPC分类号： C07D471/20 ,  A61K31/438 ,  A61K31/444 ,  C07D471/10 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

CPC分类号： C07D471/20 ,  A61K31/438 ,  A61K31/444 ,  C07D471/10 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

摘要： The present invention provides the compound represented by the following formula (I):






wherein a moiety represented by formula:








or the like;

y is 0 or 1; R1 is hydrogen or the like; R2a and R2b are taken together with an adjacent carbon atom to form ring B; ring B is a substituted or unsubstituted non-aromatic carbocycle or the like; R3a is hydrogen or the like; R3b is hydrogen or the like; R4a is represented by formula:





L1 is a single bond or the like; L2 is —C(═O)— or the like; La is a single bond or the like; R7 is substituted or unsubstituted alkyl or the like; R4b is substituted or unsubstituted alkyl or the like; R4c is each independently halogen or the like.

公开(公告)号：US20240285614A1

公开(公告)日：2024-08-29

申请号：US18433734

申请日：2024-02-06

申请人： Boundless Bio, Inc.

发明人： Anthony B. PINKERTON ,  Jacques MAUGER ,  Yen Pham Hong TRUONG ,  Camille REMEUR ,  Jérôme TOUM ,  Olivier MIRGUET

IPC分类号： A61K31/496 ,  A61K31/404 ,  A61K31/435 ,  A61K31/438 ,  A61K31/454 ,  A61K31/4995 ,  A61K45/06 ,  C07D207/12 ,  C07D209/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08

CPC分类号： A61K31/496 ,  A61K31/404 ,  A61K31/435 ,  A61K31/438 ,  A61K31/454 ,  A61K31/4995 ,  A61K45/06 ,  C07D207/12 ,  C07D209/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08

摘要： Provided herein are compounds and methods for the treatment of cancer. The methods include administering to a subject in need a therapeutically effective amount of a cyclic sulfonamide RNR inhibitor disclosed herein.

公开(公告)号：US12065440B2

公开(公告)日：2024-08-20

申请号：US17850198

申请日：2022-06-27

申请人： Cassava Sciences, Inc.

发明人： Michael Zamloot ,  Lindsay Burns Barbier ,  Shawn Anthony Kucera

IPC分类号： C07D471/10

CPC分类号： C07D471/10 ,  C07B2200/13

摘要： The preparation and properties of crystalline polymorphs and solvates of 1-benzyl-8-methyl-1,4,8-triazaspiro-[4.5]-decan-2-one free base and of the mono- and dihydrochloride salts and solvates thereof are disclosed, as is an amorphous polymorph of the dihydrochloride. A pharmaceutical composition containing one or more polymorphs and a method of using that composition are also disclosed.

公开(公告)号：US20240270739A1

公开(公告)日：2024-08-15

申请号：US18512625

申请日：2023-11-17

申请人： Incyte Corporation

发明人： Ming Xiang ,  Joshua Hummel ,  Shaoqun Qian ,  Shicheng Shi ,  Xiaozhao Wang

IPC分类号： C07D417/14 ,  A61K31/438 ,  A61K31/501 ,  A61K31/5386 ,  C07D471/10 ,  C07D498/10

CPC分类号： C07D417/14 ,  A61K31/438 ,  A61K31/501 ,  A61K31/5386 ,  C07D471/10 ,  C07D498/10

摘要： The present application provides heteroaryl fluoroalkene compounds that modulate the activity of diacylglycerol kinase (DGK), which are useful in the treatment of various diseases, including cancer.

公开(公告)号：US20240262815A1

公开(公告)日：2024-08-08

申请号：US18559542

申请日：2022-04-08

申请人： VORONOI INC.

发明人： Younho LEE ,  Seonah HWANG ,  Woomi DO ,  Inseob SHIM ,  Hwa LEE ,  Jungbeom SON ,  Namdoo KIM ,  Sunghwan KIM ,  Hongryul JUNG ,  Jihye YOO

IPC分类号： C07D413/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  A61P35/00 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107 ,  C07D498/08

CPC分类号： C07D413/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  A61P35/00 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107 ,  C07D498/08

摘要： The present invention relates to an isoxazolidin-2-yl-substituted heteroaryl derivative and a pharmaceutical composition for cancer prevention or treatment, comprising the compound as an active ingredient. The compound exhibits high inhibitory activity against the wild type or mutants of at least one of ErbB2 and ErbB4 and thus can be useful for treating cancers in which ErbB2 and ErbB4 are expressed.

公开(公告)号：US12048748B2

公开(公告)日：2024-07-30

申请号：US17524558

申请日：2021-11-11

申请人： C4 Therapeutics, Inc.

发明人： Andrew J. Phillips ,  Christopher G. Nasveschuk ,  James A. Henderson ,  Yanke Liang ,  Kiel Lazarski ,  Ryan E. Michael

IPC分类号： A61K31/435 ,  A61K31/438 ,  A61K47/54 ,  C07D471/10 ,  C07D498/20 ,  C07D519/00

CPC分类号： A61K47/545 ,  A61K31/435 ,  A61K31/438 ,  A61K47/554 ,  C07D471/10 ,  C07D498/20 ,  C07D519/00

摘要： This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.