公开(公告)号：US20240300905A1

公开(公告)日：2024-09-12

申请号：US18583526

申请日：2024-02-21

申请人： Prosetta Biosciences, Inc.

发明人： Dennis Solas ,  Anuradha F. Lingappa ,  Vishwanath R. Lingappa

IPC分类号： C07D239/94 ,  A61P31/18 ,  A61P33/06 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14

CPC分类号： C07D239/94 ,  A61P31/18 ,  A61P33/06 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14

摘要： Disclosed are novel heterocyclic compounds such as novel quinazoline compounds and pharmaceutical compositions thereof which may be used to treat or prevent malaria, HIV infection and cancer.

公开(公告)号：US12071424B2

公开(公告)日：2024-08-27

申请号：US18176362

申请日：2023-02-28

申请人： Cornell University

发明人： Joseph P. Vacca ,  Dansu Li ,  Sarah Elizabeth Bettigole

IPC分类号： C07D401/04 ,  A61K31/517 ,  A61P35/00 ,  C07D217/22 ,  C07D239/74 ,  C07D239/84 ,  C07D239/94 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D413/04 ,  C07D417/04

CPC分类号： C07D401/10 ,  A61P35/00 ,  C07D217/22 ,  C07D239/84 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D413/04 ,  C07D417/04

摘要： Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.

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：US20240239749A1

公开(公告)日：2024-07-18

申请号：US18497879

申请日：2023-10-30

申请人： Escient Pharmaceuticals, Inc.

发明人： Marion Lanier ,  Marcus Boehm ,  Liming Huang ,  Esther Martinborough ,  Marcos Sainz ,  Brandon Selfridge ,  Adam Yeager

IPC分类号： C07D213/73 ,  C07C255/60 ,  C07D209/08 ,  C07D231/14 ,  C07D239/48 ,  C07D239/94 ,  C07D277/56 ,  C07D277/62 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D471/04

CPC分类号： C07D213/73 ,  C07C255/60 ,  C07D209/08 ,  C07D231/14 ,  C07D239/48 ,  C07D239/94 ,  C07D277/56 ,  C07D277/62 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D471/04

摘要： Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 dependent condition more specifically, by contacting the MRGPRX2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I):






or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein D, W, Z, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

公开(公告)号：US12030857B2

公开(公告)日：2024-07-09

申请号：US16973941

申请日：2019-06-25

申请人： Kadmon Corporation, LLC

发明人： Kevin G. Liu ,  Kellen L. Olszewski ,  Ji-In Kim ,  Masha V. Poyurovsky ,  Koi Morris ,  Xuemei Yu ,  Christophe Lamarque

IPC分类号： C07D239/42 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/34 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07D519/00

CPC分类号： C07D239/42 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/34 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07D519/00

摘要： This invention provides compounds that modulate glucose uptake activity and cellular transport/uptake of glucose, and particularly GLUTS3, but also including but not limited to GLUT1-14 (SLC2A1-SLC2A14). Compounds of the invention are useful for treating diseases, including cancer, autoimmune diseases and inflammation, infectious diseases, and metabolic diseases.

公开(公告)号：US20240150317A1

公开(公告)日：2024-05-09

申请号：US18118549

申请日：2023-03-07

申请人： Genzyme Corporation

发明人： Jorgen Blixt ,  Michael David Golden ,  Philip John Hogan ,  David Michael Glanville Martin ,  Francis Joseph Montgomery ,  Zakariya Patel ,  John David Pittam ,  George Joseph Sependa ,  Christopher John Squire ,  Nicholas Cartwright Alexander Wright

IPC分类号： C07D401/12 ,  C07D211/16 ,  C07D239/94

CPC分类号： C07D401/12 ,  C07D211/16 ,  C07D239/94

摘要： The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.

公开(公告)号：US20240025863A1

公开(公告)日：2024-01-25

申请号：US18245125

申请日：2021-09-16

申请人： BioTheryX, Inc.

发明人： Kyle W.H. Chan ,  Aparajita Hoskote Chourasia ,  Paul E. Erdman ,  Leah M. Fung ,  David Aaron Hecht ,  Imelda Lam ,  Patrick Papa ,  Angela Schoolmeesters ,  Eduardo Torres

IPC分类号： C07D239/94 ,  C07D409/12 ,  C07D487/04 ,  C07D471/04 ,  C07D403/14 ,  C07D401/14 ,  A61P35/00

CPC分类号： C07D239/94 ,  C07D409/12 ,  C07D487/04 ,  A61P35/00 ,  C07D403/14 ,  C07D401/14 ,  C07D471/04

摘要： Provided herein are SOS1 protein degraders, for example, a compound of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of an SOS1-mediated disorder, disease, or condition.

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：US20230271936A1

公开(公告)日：2023-08-31

申请号：US18040598

申请日：2021-08-09

申请人： Abbisko Therapeutics Co., Ltd

发明人： Fei Yang ,  Shuqun Yang ,  Hongping Yu ,  Zhui Chen ,  Yaochang Xu

IPC分类号： C07D401/12 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D401/14 ,  C07D405/14

CPC分类号： C07D401/12 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D401/14 ,  C07D405/14

摘要： An EGFR inhibitor having the structure of formula (I), a preparation method therefor, a pharmaceutical composition containing same, a use of same as an EGFR inhibitor, and a use of same in preparing a drug for treating and/or preventing a cancer, a tumor, or a metastatic disease at least partially related to an EGFR exon 20 insertion, deletion, or other mutation, and in particular a use in preparing a drug for treating and/or preventing a hyperproliferative disease and an induced cell death disorder. Each substituent of formula (I) has the same definition as in the description.