公开(公告)号：US20240352028A1

公开(公告)日：2024-10-24

申请号：US18416739

申请日：2024-01-18

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 ,  C07D215/46 ,  C07D215/54 ,  C07D217/22 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D241/44 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D409/04 ,  C07D487/04

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：US20240140957A1

公开(公告)日：2024-05-02

申请号：US18260649

申请日：2022-01-07

申请人： BeiGene Switzerland GmbH

发明人： Qi JI ,  Chao YU ,  Ce WANG ,  Hanzi sun ,  Hao YUAN ,  Zhiwei WANG

IPC分类号： C07D487/08 ,  C07D239/95 ,  C07D403/04 ,  C07D417/14 ,  C07D471/08 ,  C07D498/08 ,  C07D519/00

CPC分类号： C07D487/08 ,  C07D239/95 ,  C07D403/04 ,  C07D417/14 ,  C07D471/08 ,  C07D498/08 ,  C07D519/00

摘要： Provided herein are Bridged Compounds having the following structures:




wherein R1a, R1b, R1c, R1d, R2a, R2b, R2c, R2d, R3a, R3b, R3c, R3d, R4, R5, R6, R7, R8, m1, m2, m3, n2, n3, n4, q, X1, X2, Y1, Y2, L1 and ring A are as defined herein, compositions comprising an effective amount of a Bridged Compound, and methods for treating or preventing various diseases, e.g., pancreatic cancer, or a condition treatable or preventable by inhibition of the function of KRAS protein. In another aspect, a Bridged Compound is useful for treating or preventing a condition treatable or preventable by inhibition of the function of KRAS protein with G12D mutation. In another aspect, a Bridged Compound is useful for treating or preventing a condition treatable or preventable by inhibition of a RAS/MAPK pathway.

公开(公告)号：US11912669B2

公开(公告)日：2024-02-27

申请号：US17537142

申请日：2021-11-29

申请人： Cerepeut, Inc.

发明人： Bingwei Lu

IPC分类号： A61P9/10 ,  A61P23/00 ,  A61P35/00 ,  C07D239/95

CPC分类号： C07D239/95 ,  A61P9/10 ,  A61P23/00 ,  A61P35/00

摘要： The present invention relates to compositions and methods for the treatment of cancer and other diseases associated with mitochondrial dysfunction, including but not limited to, neurodegenerative disease, brain injuries, and certain non-neurological disorders, using a novel compound, 6-chloro-3-(2,4-dichloro-5-methoxyphenyl)-2-mercapto-7-methoxyquinazolin-4(3H)-one, and derivatives thereof.

公开(公告)号：US11878985B2

公开(公告)日：2024-01-23

申请号：US17125955

申请日：2020-12-17

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： A61K31/517 ,  C07D239/94 ,  C07D495/04 ,  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：US20240002351A1

公开(公告)日：2024-01-04

申请号：US18276532

申请日：2022-03-04

申请人： UNIVERSITEIT ANTWERPEN

发明人： Vincent Frans Maria SEGERS ,  Gilles Willy DE KEULENAER ,  Eline FEYEN ,  Hans Louis Jos DE WINTER

IPC分类号： C07D239/95 ,  C07D495/04 ,  C07D403/12

CPC分类号： C07D239/95 ,  C07D403/12 ,  C07D495/04

摘要： The present invention relates to a compound of formula (I) or a stereoisomer, or tautomer, for use in the prevention or treatment of a disease associated with the activation of receptor tyrosine-protein kinase (erbB4). In formula (I), wherein n, A1, A2, A3, A4, A5, R1, R2, R3, and R4 have the same meaning as that defined in the claims and the description. The present invention also relates uses of such compounds for the prevention and/or treatment of a disease associated with the activation of receptor tyrosine-protein kinase (erbB-4) such as heart failure, metabolic disorders, inflammatory disorders, fibrotic disorders, and cancer. The present invention also provides pharmaceutical compositions comprising such compounds, as well as the use of the compounds as a medicament.

公开(公告)号：US20230339866A1

公开(公告)日：2023-10-26

申请号：US17795515

申请日：2021-02-01

申请人： TROBIO THERAPEUTICS PTY LTD

发明人： Edna HARDEMAN ,  Peter GUNNING ,  Eleanor EIFFE

IPC分类号： C07D239/95 ,  C07D409/04 ,  C07D403/04 ,  C07D405/04 ,  C07D403/12 ,  C07D409/14 ,  C07D403/14 ,  C07D405/12 ,  C07D401/12 ,  C07D409/12 ,  A61P35/00

CPC分类号： C07D239/95 ,  C07D409/04 ,  C07D403/04 ,  C07D405/04 ,  C07D403/12 ,  C07D409/14 ,  C07D403/14 ,  C07D405/12 ,  C07D401/12 ,  C07D409/12 ,  A61P35/00

摘要： The present disclosure relates generally to a class of quinazoline compounds, compositions containing the same and the therapeutic use of the compounds in the treatment of cancer.

公开(公告)号：US20230302162A1

公开(公告)日：2023-09-28

申请号：US18061715

申请日：2022-12-05

申请人： INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) ,  UNIVERSITE DE LA REUNION

发明人： Olivier MEILHAC ,  Emmanuelle JESTIN ,  Florian GUIBBAL ,  Sébastien BENARD

IPC分类号： A61K51/04 ,  C07D239/95 ,  C07D403/06 ,  C07D405/12 ,  C07F5/02

CPC分类号： A61K51/0459 ,  C07D239/95 ,  C07D403/06 ,  C07D405/12 ,  C07F5/025 ,  A61K9/0019

摘要： The present inventors have developed new radiolabeled Darapladib and analogs thereof which can be used for the specific detection of vulnerable atherosclerotic plaques by targeting lipoprotein-associated phospholipase A2 (Lp-PLA2) which is a biomarker of choice concerning inflammation and atherosclerosis progression. Thus, the present invention relates to radiolabeled Darapladib and analogs thereof and their use as imaging compounds.

公开(公告)号：US20190092758A1

公开(公告)日：2019-03-28

申请号：US16086926

申请日：2017-03-21

申请人： Council of Scientific & Industrial Research

发明人： Arindam Talukdar ,  Dipyaman Ganguly ,  Barnali Paul ,  Ayan Mukherjee ,  Shounak Roy ,  Swarnali Roy ,  Amrit Raj Ghosh ,  Roopkatha Bhattacharya ,  Oindrila Rahaman ,  Biswajit Kundu

IPC分类号： C07D403/12 ,  A61P37/04 ,  C07D403/04 ,  C07D403/14 ,  C07D401/12 ,  C07D239/95

CPC分类号： C07D403/12 ,  A61P37/04 ,  C07D239/95 ,  C07D401/12 ,  C07D403/04 ,  C07D403/14

摘要： The present invention relates to small molecule4-(piperazin-1-yl)quinazolin-2-amino compounds with formula (I) useful for inhibiting signalling by certain toll-like receptors (TLRs), especially TLR9. Toll-like receptors (TLRs) are members of the larger family of evolutionarily conserved pattern recognition receptors which are critical first line of defence for self-nonself discrimination by the host immune response. Aberrant TLR9 activation is implicated in autoreactive inflammation in different autoimmune diseases. The invention depicts compounds with formula (I), composition and methods can be used in a number of clinical applications, including as pharmaceutical agents and methods for treating conditions involving unwanted immune activity due to TLR9 activation.

公开(公告)号：US09932317B2

公开(公告)日：2018-04-03

申请号：US14385268

申请日：2013-03-19

申请人： Imperial Innovations Limited ,  Emory University

发明人： Robert Brown ,  Matthew John Fuchter ,  Nadine Chapman-Rothe ,  Nitipol Srimongkolpithak ,  Joachim Caron ,  James Snyder ,  Thota Ganesh ,  Jin Liu ,  Aiming Sun

IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/517 ,  C07D239/95 ,  C07D405/14 ,  C07D491/056 ,  C07D403/12 ,  C07D401/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551

CPC分类号： C07D239/95 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D491/056

摘要： This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.

公开(公告)号：US20180009786A1

公开(公告)日：2018-01-11

申请号：US15712978

申请日：2017-09-22

申请人： National Health Research Institutes

发明人： Kak-Shan Shia ,  Jiing-Jyh Jan ,  Lun Kelvin Tsou ,  Chiung-Tong Chen ,  Yu-Sheng Chao

IPC分类号： C07D401/14 ,  C07D473/32 ,  C07D471/04 ,  C07D417/14 ,  C07D403/12 ,  A61K31/4192 ,  C07D403/04 ,  C07D239/95 ,  A61K31/517 ,  A61K31/506 ,  C07F9/6558 ,  C07D403/14

CPC分类号： C07D401/14 ,  A61K31/4192 ,  A61K31/506 ,  A61K31/517 ,  C07D239/95 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/32 ,  C07F9/65583

摘要： Heterocyclic compounds of Formula (I) shown herein. Also disclosed are pharmaceutical compositions containing the heterocyclic compounds and methods of using the heterocyclic compounds to mobilize hematopoietic stem cells and endothelial progenitor cells into the peripheral circulation. Further provided are methods for treating tissue injury, cancer, inflammatory disease, and autoimmune disease with the heterocyclic compounds.