公开(公告)号：US20240360151A1

公开(公告)日：2024-10-31

申请号：US18602519

申请日：2024-03-12

申请人： SANOFI

发明人： Jean-Philippe LETALLEC ,  Franck Marguet ,  Fréderic Petit ,  Baptiste Ronan ,  Corinne Terrier

IPC分类号： C07D498/10 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/553 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/04

CPC分类号： C07D498/10 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/553 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/04

摘要： The present invention relates to a compound of formula (I) wherein n is 1 or 2, R1 is halogen, (C1-C4)alkyl, halo(C1-C4)alkyl, (C1-C4)alkoxy, halo(C1-C4)alkoxy, ethynyl, propargyl, or (C3-C6)cycloalkyl, or two R1 form a cyclopentane ring fused to the phenol; R2 and R3 represent H, cyano, ethynyl, propargyl, (C1-C4)alkyl, hydroxy(C1-C4)alkyl or a halo(C1-C4)alkyl, or R2 and R3 form together with the atoms connecting them a (C5-C6)carbocyclic ring fused to the pyridazine ring; R4 and R5 form together with N to which they are attached an optionally substituted 3-7 membered monocyclic heterocycloalkyl ring, 8-11 membered bicyclic heterocycloalkyl ring or 7-12 membered bicyclic heterocyclic spiro ring. The present invention also relates to a medicament and a pharmaceutical composition comprising said compound of formula (I), as well as their therapeutic uses, in particular as inhibitor of NOD-like receptor protein 3 inflammasome for treating for example Parkinson's disease or frontotemporal Dementia.

公开(公告)号：US20240351986A1

公开(公告)日：2024-10-24

申请号：US18683623

申请日：2022-07-26

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Youhong HU ,  Yi CHEN ,  Zhicheng XIE ,  Jian DING ,  Xin LI ,  Yanfen FANG ,  Qianqian SHEN

IPC分类号： C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

CPC分类号： C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

摘要： The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.

公开(公告)号：US20240317775A1

公开(公告)日：2024-09-26

申请号：US18257413

申请日：2021-12-14

申请人： HEPTARES THERAPEUTICS LIMITED

发明人： Giles Albert BROWN ,  Miles Sturt CONGREVE ,  Barry TEOBALD ,  Nigel Alan SWAIN ,  Charlootte FIELDHOUSE ,  Mark PICKWORTH ,  Malken BAYRAKDARIAN ,  Delphine KARILA ,  Danail BEAUDION

IPC分类号： C07D498/04 ,  A61K31/5383 ,  A61K31/553 ,  C07D498/14

CPC分类号： C07D498/04 ,  A61K31/5383 ,  A61K31/553 ,  C07D498/14

摘要： The disclosures herein relate to novel compounds of formula (1):




and salts thereof, wherein Y, Z, R1, R2, R3, R4, R5 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with H4 receptors.

公开(公告)号：US20240287022A1

公开(公告)日：2024-08-29

申请号：US18569352

申请日：2022-06-23

申请人： Merck Sharp & Dohme LLC

发明人： BRANDON D. CASH ,  GEORGE MADALIN GIAMBASU ,  ANDREW M. HAIDLE ,  BRETT A. HOPKINS ,  MATTHEW A. LARSEN ,  CHARLES A. LESBURG ,  PING LIU ,  RYAN QUIROZ ,  SULAGNA SANYAL ,  CATHERINE M. WHITE ,  XIN YAN ,  XIAO MEI ZHENG

IPC分类号： C07D401/06 ,  A61K31/4375 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/538 ,  A61K31/5383 ,  C07D215/227 ,  C07D401/10 ,  C07D401/12 ,  C07D405/10 ,  C07D405/14 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D471/06 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D401/06 ,  A61K31/4375 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/538 ,  A61K31/5383 ,  C07D215/227 ,  C07D401/10 ,  C07D401/12 ,  C07D405/10 ,  C07D405/14 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D471/06 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

摘要： Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof wherein A, E, U, X, Y, Z, R1, R2 and n are as defined herein. The compounds of Formula I act as IL4I1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for IL4I1-related diseases. Also provided herein are pharmaceutical compositions comprising the compounds of the invention, or their pharmaceutically acceptable salts, and a pharmaceutically acceptable carrier and methods of treatment with the compounds of the invention.

公开(公告)号：US20240285643A1

公开(公告)日：2024-08-29

申请号：US18602656

申请日：2024-03-12

申请人： Shionogi & Co., Ltd. ,  F. HOFFMANN-LA ROCHE AG

发明人： Takeki UEHARA ,  Toru ISHIBASHI ,  Takao SHISHIDO ,  Keita FUKAO ,  Motoyasu OONISHI ,  Barry CLINCH ,  Jaspinder RANDHAWA

IPC分类号： A61K31/5383 ,  A61K31/215 ,  A61P31/16

CPC分类号： A61K31/5383 ,  A61K31/215 ,  A61P31/16

摘要： A method for treating an influenza virus infection is described. The disclosed method generally involves administering an effective amount of a compound (A), for example baloxavir marboxil, and a compound (B), for example a neuraminidase inhibor, to a subject that (1) has an influenza virus infection, (2) has been symptomatic of the influenza virus infection for no more than 96 hours, and (3) further has at least one severe influenza condition selected from the following: (a) being hospitalized due to severe influenza virus infection, (b) requiring an extension of hospitalization because of the influenza virus infection during the hospitalization, (c) having a National Early Warning Score 2 of four or more, (d) being on support for respiration, and (e) having at least one complication attributable to the influenza virus infection that necessitates hospitalization.

公开(公告)号：US20240277852A1

公开(公告)日：2024-08-22

申请号：US18559655

申请日：2022-05-19

申请人： DANA-FARBER CANCER INSTITUTE, INC. ,  CORNELL UNIVERSITY

发明人： Nathanael S. Gray ,  Mingxing Teng ,  Eric Wang ,  Jie Jiang ,  Tinghu Zhang ,  Lewis C. Cantley ,  Eric S. Fischer ,  Katherine A. Donovan

IPC分类号： A61K47/55 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5383 ,  A61K47/54 ,  C07D239/42 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D409/04 ,  C07D409/10 ,  C07D417/04 ,  C07D498/14

CPC分类号： A61K47/55 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5383 ,  A61K47/545 ,  C07D239/42 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D409/04 ,  C07D409/10 ,  C07D417/04 ,  C07D498/14

摘要： The present invention relates to compounds, compositions, and methods for treating diseases or conditions by modulating (e.g., reducing) the level or activity of at least one of PIP4K2A, PIP4K2B, and PIP4K2C.

公开(公告)号：US20240270747A1

公开(公告)日：2024-08-15

申请号：US18523284

申请日：2023-11-29

申请人： Genentech, Inc.

发明人： James John CRAWFORD ,  Daniel Fred ORTWINE ,  BinQing WEI ,  Wendy B. YOUNG

IPC分类号： C07D487/04 ,  A61K9/20 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  A61P35/00 ,  A61P37/00 ,  C07D471/04 ,  C07D471/14 ,  C07D487/08 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

CPC分类号： C07D487/04 ,  A61K9/20 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  A61P35/00 ,  A61P37/00 ,  C07D471/04 ,  C07D471/14 ,  C07D487/08 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

摘要： Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US20240262807A1

公开(公告)日：2024-08-08

申请号：US18561553

申请日：2022-05-27

申请人： CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.

发明人： Yinsheng ZHANG ,  Xin LIU ,  Hui QIN ,  Jiawei YE ,  Jinan WANG ,  Songsong WU

IPC分类号： C07D401/14 ,  A61K31/407 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61P35/02 ,  C07D213/82 ,  C07D401/04 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08 ,  C07D519/00

CPC分类号： C07D401/14 ,  A61K31/407 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61P35/02 ,  C07D213/82 ,  C07D401/04 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08 ,  C07D519/00

摘要： Provided are a compound used as a BCR-ABL inhibitor, namely a compound of formula (I), or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition comprising the compound. Moreover, the present invention relates to a use of the compound in the preparation of a drug for treating BCR-ABL related diseases.

公开(公告)号：US20240254140A1

公开(公告)日：2024-08-01

申请号：US18609825

申请日：2024-03-19

申请人： Hoffmann-La Roche Inc.

发明人： Daniele ANDREOTTI ,  John G. CUMMING ,  Giacomo FOSSATI ,  Susanna SAMPAOLESI ,  Elena SERRA

IPC分类号： C07D498/04 ,  A61K9/08 ,  A61K9/20 ,  A61K9/48 ,  A61K31/5383 ,  A61K47/10 ,  A61K47/12 ,  A61P31/04 ,  C07D519/00

CPC分类号： C07D498/04 ,  A61K9/08 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/5383 ,  A61K47/10 ,  A61K47/12 ,  A61P31/04 ,  C07D519/00

摘要： The invention provides novel compounds having the general formula (I)




wherein R1, R2, R3a, R3b, R4, A1, A2, A3, A4, A5, A6, B1, B2, B3, B4, and L are as described herein, compositions including the compounds and methods of using the compounds.

公开(公告)号：US20240252506A1

公开(公告)日：2024-08-01

申请号：US18609853

申请日：2024-03-19

申请人： Hoffmann-La Roche Inc.

发明人： Daniele ANDREOTTI ,  John G. CUMMING ,  Bruno FASSARI ,  Giacomo FOSSATI ,  Elena SERRA ,  Silvia PAOLETTA

IPC分类号： A61K31/5383 ,  A61K9/20 ,  A61K9/48 ,  A61P31/04 ,  C07D498/04 ,  C07D519/00

CPC分类号： A61K31/5383 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866 ,  A61P31/04 ,  C07D498/04 ,  C07D519/00

摘要： The invention provides novel compounds having the general formula (I)




wherein R1, R2, A1, A2, A3, A4, A5, A6, L and W are as described herein, compositions including the compounds and methods of using the compounds.