公开(公告)号：US20240351997A1

公开(公告)日：2024-10-24

申请号：US18580154

申请日：2022-07-28

申请人： SHANGHAI QILU PHARMACEUTICAL RESEARCH AND DEVELOPMENT CENTRE LTD.

发明人： Xiaoxia YAN ,  Guanxin HUANG ,  Wei JU ,  Daqing SUN

IPC分类号： C07D401/12 ,  A61K31/444 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  C07D239/42 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

CPC分类号： C07D401/12 ,  A61K31/444 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  C07D239/42 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

摘要： Disclosed are a compound serving as a PARP7 inhibitor, and a use thereof in preparing a drug for treating relevant diseases. Specifically disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof. The compound can be used for treating cancer.

公开(公告)号：US12115157B2

公开(公告)日：2024-10-15

申请号：US17941860

申请日：2022-09-09

申请人： Boehringer Ingelheim International GmbH ,  Arena Pharmaceuticals, Inc.

发明人： Kai Gerlach ,  Daniela Gavina Berta ,  Marco Ferrara ,  Kirsten Gutsche ,  Ursula Mueller-Vieira ,  Scott Hobson ,  Frank Runge ,  Graeme Semple ,  Viktor Vintonyak ,  Yifeng Xiong

IPC分类号： A61K31/497 ,  A61K31/433 ,  A61K45/06 ,  C07D403/14 ,  C07D417/14 ,  C07D487/08

CPC分类号： A61K31/497 ,  A61K31/433 ,  A61K45/06 ,  C07D403/14 ,  C07D417/14 ,  C07D487/08 ,  C07B2200/05 ,  C07B2200/09

摘要： The invention relates to 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases.
In addition, the invention relates to the 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) for use as a medicament, pharmaceutical compositions comprising at least a compound of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

公开(公告)号：US12110296B2

公开(公告)日：2024-10-08

申请号：US17283385

申请日：2019-10-07

申请人： N.E. CHEMCAT CORPORATION ,  OSAKA UNIVERSITY

发明人： Kiyotomi Kaneda ,  Takato Mitsudome ,  Yoshiyuki Wada ,  Yukio Takagi

IPC分类号： C07D487/08 ,  B01J6/00 ,  B01J23/648 ,  B01J23/652 ,  B01J27/18 ,  B01J37/00 ,  B01J37/04

CPC分类号： C07D487/08 ,  B01J6/001 ,  B01J23/6482 ,  B01J23/6525 ,  B01J27/1806 ,  B01J37/0036 ,  B01J37/04

摘要： The present invention provides a method for producing a compound represented by formula (2), comprising at least a step of preparing a compound represented by formula (1) and a step of reacting the compound represented by formula (1) with a hydrogen source using a catalyst,




wherein R1 and R2 are each independently an alkyl group.

公开(公告)号：US20240327354A1

公开(公告)日：2024-10-03

申请号：US18579953

申请日：2022-07-22

申请人： INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE ,  INSTITUT PASTEUR DE LILLE ,  UNIVERSITÉ DE LILLE ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  CHRU DE LILLE ,  JOHANN WOLFGANG GOETHE-UNIVERSITÄT FRANKFURT AM MAIN

发明人： Anaïs VIEIRA DA CRUZ ,  Coline PLÉ ,  Marion FLIPO ,  Nina COMPAGNE ,  Nicolas WILLAND ,  Heng-Keat TAM ,  Juan Carlos JIMÉNEZ CASTELLANOS ,  Klaas Martinus POS ,  Ruben Christiaan HARTKOORN ,  Reinke Tobias MÜLLER

IPC分类号： C07D213/74 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/498 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D213/80 ,  C07D215/38 ,  C07D217/22 ,  C07D241/44 ,  C07D295/073 ,  C07D401/04 ,  C07D413/04 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08

CPC分类号： C07D213/74 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/498 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D213/80 ,  C07D215/38 ,  C07D217/22 ,  C07D241/44 ,  C07D295/073 ,  C07D401/04 ,  C07D413/04 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08

摘要： The present invention concerns novel Gram-negative bacteria efflux pump inhibitors. It further relates to the use of Gram-negative bacteria efflux pump inhibitors to prevent and/or treat antibiotic resistance by potentiating the activity of antibiotics. Infections by multidrug resistant (MDR) Gram-negative bacteria are a major threat to global healthcare. The inventors have discovered a novel class of Resistance Nodulation cell Division-efflux pump inhibitors. The inventors tested the effects of these inhibitors on growth inhibition of different bacteria as well as their impact on the boosting of antibiotic activity in different bacteria. Particularly, the inventors tested the effects of these inhibitors on E. coli, A. baumamnii, K. pneumoniae and P. aeruginosa.

公开(公告)号：US20240317730A1

公开(公告)日：2024-09-26

申请号：US18731285

申请日：2024-06-01

申请人： Voronoi Inc.

发明人： Youn Ho Lee ,  Seon Ah Hwang ,  In Seob Shim ,  Hyeon Ho Jeon ,  Woo Mi Do ,  Hee Sun Ryu ,  Jung Beom Son ,  Nam Doo Kim ,  Sung Hwan Kim ,  Hong Ryul Jung ,  Young Yi Lee

IPC分类号： C07D413/14 ,  C07D413/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D498/04 ,  C07D498/08 ,  C07F9/6584

CPC分类号： C07D413/14 ,  C07D413/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D498/04 ,  C07D498/08 ,  C07F9/6584

摘要： The present disclosure relates to a heteroaryl derivative and uses thereof. The heteroaryl derivative of the present disclosure exhibits excellent inhibitory activity against EGFR and/or HER2, and thus may be usefully employed as a therapeutic agent for EGFR- and/or HER2-related diseases.

公开(公告)号：US20240316043A1

公开(公告)日：2024-09-26

申请号：US18612647

申请日：2024-03-21

申请人： University of Tennessee Research Foundation

发明人： Duane Miller ,  Lawrence Pfeffer ,  Yali He ,  Yinan Wang ,  Chuan Yang

IPC分类号： A61K31/4995 ,  A61K31/495 ,  A61P35/00 ,  C07D487/08

CPC分类号： A61K31/4995 ,  A61K31/495 ,  A61P35/00 ,  C07D487/08

摘要： The present disclosure related to compounds of Formula (I):




stereoisomers thereof, prodrugs thereof, and pharmaceutically acceptable salts thereof. The present disclosure also relates to uses of the compounds, including to treat cancer in a subject.

公开(公告)号：US20240316034A1

公开(公告)日：2024-09-26

申请号：US18655194

申请日：2024-05-03

申请人： Emory University

发明人： Dennis C. Liotta ,  Edgars Jecs ,  Robert James Wilson ,  Huy Hoang Nguyen ,  Michelle Bora Kim ,  Lawrence Wilson ,  Eric Miller ,  Yesim Altas Tahirovic ,  Valarie Truax

IPC分类号： A61K31/4725 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

CPC分类号： A61K31/4725 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

摘要： The disclosure relates to chemokine CXCR4 receptor modulators and uses related thereto. The receptor modulators can be formulated to form pharmaceutical compositions comprising the disclosed compounds or pharmaceutically acceptable salts or prodrugs thereof. The compositions may be used for managing CXCR4 related conditions, typically prevention or treatment of viral infections abnormal cellular proliferation, retinal degeneration, inflammatory diseases, or as an immunostimulant or immunosuppressant or for managing cancer and may be administered with another active ingredient such as an antiviral agent or chemotherapeutic agent.

公开(公告)号：US20240277877A1

公开(公告)日：2024-08-22

申请号：US18597131

申请日：2024-03-06

申请人： Clarity Pharmaceuticals Ltd

发明人： Paul Stephen Donnelly ,  Nicholas Alan Zia

IPC分类号： A61K51/04 ,  C07D487/08

CPC分类号： A61K51/0482 ,  A61K51/044 ,  C07D487/08

摘要： The present invention is directed to sarcophagine based compounds of formula (I). The compounds can complex a radioisotope, such as 64-copper and hence are useful in radioimaging and radiotherapy of cancers, e.g. colorectal cancer. The compounds work via a pre-targeting imaging approach in which the tetrazine reacts via click chemistry with a functional group such as a transcyclooctene which is pre-bound to a ligand such as a tumour specific antibody.

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：US20240245673A1

公开(公告)日：2024-07-25

申请号：US18532424

申请日：2023-12-07

申请人： Pfizer Inc.

发明人： James Matthew Frick ,  Michelle Renee Garnsey ,  Brian Stephen Gerstenberger ,  Xinjun Hou ,  Magdalena Korczynska ,  Alpha Albert Lee ,  Luong Tien Nguyen ,  Usa Reilly ,  Matthew Christopher Robinson ,  Alexandria Paige Taylor ,  Thomas Reynold Vargo ,  Lei Zhang

IPC分类号： A61K31/4709 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D215/38 ,  C07D231/12 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

CPC分类号： A61K31/4709 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D215/38 ,  C07D231/12 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

摘要： The invention relates to compounds of Formula (I)




and pharmaceutically acceptable salts thereof as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may inhibit the activity of papain-like protease (PLpro) and may be useful in the treatment of viral infections, in particular viral infections associated with PLpro activity and/or expression such as coronaviruses infections.