公开(公告)号：US12049461B2

公开(公告)日：2024-07-30

申请号：US16950654

申请日：2020-11-17

申请人： Gilead Sciences, Inc.

发明人： Ling-Jie Gao ,  Piet Andre Maurits Maria Herdewijn ,  Steven Cesar Alfons De Jonghe ,  William John Watkins ,  Lee Shun Chong

IPC分类号： A61K31/517 ,  A61K31/5375 ,  A61K31/5377 ,  A61P31/14 ,  C07D239/72 ,  C07D239/78 ,  C07D239/86 ,  C07D239/88 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04

CPC分类号： C07D413/04 ,  A61K31/517 ,  A61K31/5375 ,  A61K31/5377 ,  A61P31/14 ,  C07D239/72 ,  C07D239/78 ,  C07D239/86 ,  C07D239/88 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04

摘要： This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR′R″, C1-7alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

公开(公告)号：US11932634B2

公开(公告)日：2024-03-19

申请号：US17845469

申请日：2022-06-21

申请人： Gilead Sciences, Inc.

发明人： Michael Graupe ,  Juan A. Guerrero ,  Stephen D. Holmbo ,  Jesse M. Jacobsen ,  Tetsuya Kobayashi ,  Leena B. Patel ,  Heath A. Weaver ,  Jie Xu ,  Suet C. Yeung

IPC分类号： C07D413/14 ,  C07D239/95 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D413/14 ,  C07D239/95 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D417/12 ,  C07D471/04 ,  C07B2200/05

摘要： The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.

公开(公告)号：US20230322726A1

公开(公告)日：2023-10-12

申请号：US18125826

申请日：2023-03-24

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： James A. Johnson ,  John Lloyd ,  Heather Finlay ,  James Neels ,  Naveen Kumar Dhondi ,  Prashantha Gunaga ,  Abhisek Banerjee ,  Ashokkumar Adisechan

IPC分类号： C07D401/14 ,  C07D239/95 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D407/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/549 ,  A61K45/06 ,  C07D239/94 ,  C07D405/12 ,  C07D471/04 ,  C07D513/04

CPC分类号： C07D401/14 ,  A61K31/517 ,  A61K31/549 ,  A61K31/5377 ,  A61K45/06 ,  C07D239/94 ,  C07D239/95 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

摘要： A compound of formula I





wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

公开(公告)号：US20230303586A1

公开(公告)日：2023-09-28

申请号：US18178452

申请日：2023-03-03

申请人： Araxes Pharma LLC

发明人： Liansheng LI ,  Jun FENG ,  Tao WU ,  Pingda REN ,  Yi LIU ,  Yuan Liu ,  Yun Oliver Long

IPC分类号： C07D495/04 ,  C07D239/94 ,  C07D401/12 ,  C07D217/22 ,  C07D215/46 ,  C07D215/54 ,  C07D239/84 ,  C07D487/04 ,  C07D239/95 ,  C07D403/04 ,  C07D241/44 ,  C07D401/04 ,  C07D409/04

CPC分类号： C07D495/04 ,  C07D215/46 ,  C07D215/54 ,  C07D217/22 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D241/44 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D409/04 ,  C07D487/04

摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):





or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

公开(公告)号：US11597704B2

公开(公告)日：2023-03-07

申请号：US16977043

申请日：2019-02-28

申请人： Janssen Sciences Ireland Unlimited Company

发明人： David Craig Mc Gowan ,  Werner Constant Johan Embrechts ,  Jérôme Émile Georges Guillemont ,  Ludwig Paul Cooymans ,  Tim Hugo Maria Jonckers ,  Pierre Jean-Marie Raboisson

IPC分类号： C07D239/95

摘要： This application relates to quinazoline derivatives of formula (I), pharmaceutical compositions comprising the compounds of formula (I), and the use of the compounds of formula (I) in the treatment or prevention of a viral infection, of a virus-induced disease, of cancer or of an allergy. In formula (I), R1 is a C3-8alkyl, optionally substituted by one or more substituents independently selected from fluorine, hydroxyl, amino, nitrile, ester, amide, C1-3 alkyl, or C1-3 alkoxy, the carbon of R1 bonded to the amine in the 4-position of the quinazoline is in (R)-configuration, R2 is hydrogen, deuterium, fluorine, chlorine, methyl, methoxy, cyclopropyl, trifluoromethyl, or carboxylic amide, wherein each of methyl, methoxy and cyclopropyl is optionally substituted by one or more substituents independently selected from fluorine and nitrile, R3 is hydrogen or deuterium, R4 is hydrogen, deuterium, fluorine, methyl, carboxylic ester, carboxylic amide, nitrile, cyclopropyl, C4-7 heterocycle, or 5-membered heteroaryl group, wherein each of methyl, cyclopropyl, C4-7 heterocycle and 5-membered heteroaryl group is optionally substituted by one or more substituents independently selected from fluorine, hydroxyl, or methyl, R5 is hydrogen, deuterium, fluorine, chlorine, methyl, or methoxy, provided that at least one of R2, R3, R4 and R5 is not hydrogen.

公开(公告)号：US20230060004A1

公开(公告)日：2023-02-23

申请号：US17845469

申请日：2022-06-21

申请人： Gilead Sciences, Inc.

发明人： Michael Graupe ,  Juan A. Guerrero ,  Stephen D. Holmbo ,  Jesse M. Jacobsen ,  Tetsuya Kobayashi ,  Leena B. Patel ,  Heath A. Weaver ,  Jie Xu ,  Suet C. Yeung

IPC分类号： C07D413/14 ,  C07D239/95 ,  C07D401/12 ,  C07D417/12 ,  C07D403/12 ,  C07D401/04 ,  C07D471/04 ,  C07D413/04 ,  C07D401/14

摘要： The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.

公开(公告)号：US20220162172A1

公开(公告)日：2022-05-26

申请号：US17434145

申请日：2020-02-26

申请人： Cerepeut, Inc.

发明人： Bingwei LU

IPC分类号： C07D239/95 ,  A61P35/00

摘要： New quinazolinone compounds are disclosed, as well as pharmaceutical compositions containing quinazolinones and methods for the treatment of diseases and conditions associated with mitochondrial dysfunction.

公开(公告)号：US11318137B2

公开(公告)日：2022-05-03

申请号：US16500369

申请日：2017-05-17

申请人： VANDERBILT UNIVERSITY

发明人： Alex G. Waterson ,  Jason R. Abbott ,  J. Phillip Kennedy ,  Stephen W. Fesik ,  Qi Sun ,  Jason Phan ,  Michael C. Burns ,  Pratiq Patel

IPC分类号： C07D239/95 ,  A61K31/517 ,  A61K31/5377 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D413/14

摘要： The present invention relates to quinazoline compounds and compositions that modulate Ras signaling. Compounds and compositions of the present invention are useful in the treatment of cancers and other disease states associated with Ras dysfunction (e.g., Ras-associated autoimmune leukoproliferative disorder, or certain types of mitochondrial dysfunction) in a subject, for example a mammal or a human.

公开(公告)号：US11304948B2

公开(公告)日：2022-04-19

申请号：US16718311

申请日：2019-12-18

申请人： Gilead Sciences, Inc. ,  Institute of Organic Chemistry and Biochemistry of the AS CR, V.V.I.

发明人： Ondrej Baszczynski ,  Milan Dejmek ,  Yunfeng Eric Hu ,  Petr Jansa ,  Eric Lansdon ,  Richard L. Mackman ,  Petr Simon

IPC分类号： C07D403/12 ,  A61K31/517 ,  C07D401/12 ,  C07D239/94 ,  A61P31/18 ,  A61K45/06 ,  C07D239/84 ,  C07D239/95

摘要： Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.

公开(公告)号：US20220106276A1

公开(公告)日：2022-04-07

申请号：US17311873

申请日：2019-12-09

申请人： IDEAYA BIOSCIENCES, INC.

发明人： Muzaffar ALAM ,  Leah CLEARY ,  Melissa FLEURY ,  Zhonghua PEI ,  Richard STEEL ,  James SUTTON ,  John E. KNOX ,  Zachary E. R. NEWBY

IPC分类号： C07D239/95 ,  C07D401/04 ,  C07D405/12 ,  C07D417/04 ,  C07D403/04 ,  C07D413/04 ,  A61P35/00 ,  C07D239/96 ,  C07D471/04

摘要： Disclosed herein are certain 2-oxoquinazoline derivatives of Formula (IA): that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.