公开(公告)号：US12129259B1

公开(公告)日：2024-10-29

申请号：US18635375

申请日：2024-04-15

申请人： KING FAISAL UNIVERSITY

发明人： Michelyne Haroun ,  Christophe Tratrat

IPC分类号： C07D487/22 ,  A61K31/4375 ,  A61P35/00

CPC分类号： C07D487/22 ,  A61K31/4375 ,  A61P35/00

摘要： Novel pyrazino[1′,2′:1,5]pyrazolo[4,3-b][1,6]naphthyridine, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrazino[1′,2′:1,5]pyrazolo[4,3-b][1,6]naphthyridine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

公开(公告)号：US20240352040A1

公开(公告)日：2024-10-24

申请号：US18293374

申请日：2022-08-02

申请人： GENFLEET THERAPEUTICS (SHANGHAI) INC. ,  ZHEJIANG GENFLEET THERAPEUTICS CO., LTD.

发明人： Fusheng ZHOU ,  Yuanzhi TAO ,  Jinzhu ZHAO ,  Jiong LAN

IPC分类号： C07D519/00 ,  A61K31/185 ,  A61K31/194 ,  A61K31/4375 ,  C07C55/22 ,  C07C57/145 ,  C07C57/15 ,  C07C309/04 ,  C07C309/23 ,  C07C309/24

CPC分类号： C07D519/00 ,  A61K31/185 ,  A61K31/194 ,  A61K31/4375 ,  C07C55/22 ,  C07C57/145 ,  C07C57/15 ,  C07C309/04 ,  C07C309/23 ,  C07C309/24 ,  C07B2200/13 ,  C07C2601/14 ,  C07C2601/16

摘要： Disclosed are a crystal form of a RIPK1 inhibitor, an acid salt thereof, and a crystal form of an acid salt thereof. The crystal form of the RIPK1 inhibitor, the acid salt thereof, and the crystal form of the acid salt thereof have advantages of good stability and low hygroscopicity, and same have good pharmaceutical prospects.

公开(公告)号：US12116363B2

公开(公告)日：2024-10-15

申请号：US16657477

申请日：2019-10-18

申请人： SENHWA BIOSCIENCES, INC.

发明人： John Soong

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61K31/7068 ,  A61K33/243 ,  A61K45/06 ,  A61P35/00 ,  A61P35/04 ,  C07K16/28

CPC分类号： C07D471/04 ,  A61P35/00 ,  A61K45/06

摘要： The present disclosure provides a method for treating a cancer or refractory cancer and/or inhibiting cancer metastasis, recurrence or progression in a subject or increasing the likelihood of survival over a relevant period in a subject diagnosed with a cancer, comprising administering to a subject a combination of an anti-cancer agent, a CK2 inhibitor and optionally an immune checkpoint inhibitor. The method of the present disclosure increases the number of T cells and activated T cells in the tumor microenvironment and thus can modulate immune in cancer therapy.

公开(公告)号：US20240335433A1

公开(公告)日：2024-10-10

申请号：US18627617

申请日：2024-04-05

申请人： Dennis W. Stacey

发明人： Dennis W. Stacey

IPC分类号： A61K31/4375 ,  A61K9/00 ,  A61P35/00

CPC分类号： A61K31/4375 ,  A61K9/0019 ,  A61P35/00

摘要： A normal cell cycle synchronization process includes repeated administration of a drug specifically toxic for a single cell cycle phase to selectively synchronize normal cells. The selective synchronization of normal cells allows for the selective targeting of abnormal cells with cell cycle phase specific toxins. Such selective targeting may be useful in the treatment of a number of medical conditions.

公开(公告)号：US20240317708A1

公开(公告)日：2024-09-26

申请号：US18573802

申请日：2022-06-30

申请人： ZEDIRA GMBH

发明人： Ralf PASTERNACK ,  Christian BÜCHOLD ,  Martin HILS ,  Martin STIELER ,  Uwe GERLACH

IPC分类号： C07D401/12 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4748 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  C07D213/75 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

CPC分类号： C07D401/12 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4748 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  C07D213/75 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

摘要： The invention relates to the compound of general formula (I) as novel inhibitors of transglutaminases, to methods for producing the inventive compounds, to pharmaceutical compositions containing said inventive compounds and to their use for the prophylaxis and treatment of diseases associated with transglutaminases, in particular transglutaminase 2.

公开(公告)号：US12091397B2

公开(公告)日：2024-09-17

申请号：US17878753

申请日：2022-08-01

申请人： C4 Therapeutics, Inc.

发明人： Roger Norcross ,  Adrian Britschgi ,  Fabian Dey ,  Annick Goergler ,  Eric Andre Kusznir ,  Moreno Attilio Wichert

IPC分类号： C07D401/04 ,  A61K31/4375 ,  A61K31/4704 ,  A61K47/55 ,  A61P35/00 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/14 ,  C07D519/00

CPC分类号： C07D401/04 ,  A61K31/4375 ,  A61K31/4704 ,  A61K47/55 ,  A61P35/00 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/14 ,  C07D519/00

摘要： The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

公开(公告)号：US20240299369A1

公开(公告)日：2024-09-12

申请号：US18663025

申请日：2024-05-13

申请人： Allergan Pharmaceuticals International Limited ,  Merck Sharp & Dohme Corp.

发明人： Joel M. Trugman ,  Ramesh Boinpally ,  Abhijeet Jakate ,  Michelle Finnegan ,  Mary Ann Johnson ,  Leonardo Resende Allain ,  W. Mark Eickhoff ,  Craig B. Ikeda ,  Chad D. Brown ,  Francis J. Flanagan, JR. ,  Rebecca Nofsinger ,  Melanie Marota ,  Lisa Lupton ,  Paresh B. Patel ,  Hanmi Xi ,  Wei Xu

IPC分类号： A61K31/4375 ,  A61K31/4545 ,  A61P25/06

CPC分类号： A61K31/4375 ,  A61K31/4545 ,  A61P25/06

摘要： The present disclosure provides methods for the acute treatment of migraine with or without aura, comprising the administration of ubrogepant. In particular, the present disclosure provides methods for the acute treatment of migraine in patients having hepatic impairment; in patients with renal impairment; and in patients concurrently taking CYP3A4 modulators or BCRP and/or P-gp only inhibitors.

公开(公告)号：US12083114B2

公开(公告)日：2024-09-10

申请号：US17413689

申请日：2019-12-18

申请人： Disarm Therapeutics, Inc.

发明人： Todd Bosanac ,  Rajesh Devraj ,  Thomas Engber ,  Robert Owen Hughes ,  Raul Eduardo Krauss

IPC分类号： A61K31/472 ,  A61K31/416 ,  A61K31/425 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4985 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/519

CPC分类号： A61K31/472 ,  A61K31/416 ,  A61K31/425 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4985 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/519

摘要： The present disclosure relates to methods of treating neurodegeneration and neurodegenerative diseases comprising administering to a subject in need thereof a combination of a SARM1 inhibitor and a neuroprotective agent.

公开(公告)号：US20240293392A1

公开(公告)日：2024-09-05

申请号：US18570244

申请日：2022-07-18

申请人： NeoPhore Limited

发明人： Julian Blagg ,  Martin Drysdale ,  David Clark ,  Paul Winship

IPC分类号： A61K31/4725 ,  A61K31/4035 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/501 ,  C07D209/44 ,  C07D217/06 ,  C07D401/12 ,  C07D405/14 ,  C07D471/04

CPC分类号： A61K31/4725 ,  A61K31/4035 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/501 ,  C07D209/44 ,  C07D217/06 ,  C07D401/12 ,  C07D405/14 ,  C07D471/04

摘要： The present invention relates to compounds of Formula (I) that target the MLH1 or MLH1 and PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process: Formula (I) wherein R6, Y1, Y2, A1, A2, A3, A4, R11, R12, R13 and R14 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which MLH1 or MLH1 and PMS2 activity is implicated.

公开(公告)号：US20240287096A1

公开(公告)日：2024-08-29

申请号：US18694010

申请日：2022-05-17

申请人： HITGEN INC.

发明人： Ruizhi GUO ,  Jiansong WANG ,  Zhibo LUO ,  Haiwen HUANG ,  Fei QIN ,  Wei WANG ,  Haihong YE ,  Ribin QIAN

IPC分类号： C07D498/22 ,  A61K31/4375

CPC分类号： C07D498/22 ,  A61K31/4375

摘要： The present invention relates to the technical field of drug synthesis. Disclosed are a crystal form of a macrocyclic compound, and a preparation method therefor and the use thereof. The macrocyclic compound is (6R,16R)-9-fluoro-16-methyl-13-oxa-2,17,21,25-tetraazapentane [16.6.2.02,6.07,12.022,26]dihexadecane-1(25),7,9,11,18(26),19,21,23-octane-19-carbonitrile. The X-ray diffraction pattern of the crystal form has characteristic peaks at 2θ values of 9.49±0.2, 10.60±0.2, 11.54±0.2, 14.10±0.2, 17.09±0.2, 19.15±0.2, 20.30±0.2, 22.85±0.2, 23.89±0.2 and 27.74±0.2. The crystal form is hygroscopicity-free, has a good stability and pharmacokinetic properties.