公开(公告)号：US20240246910A1

公开(公告)日：2024-07-25

申请号：US18405058

申请日：2024-01-05

申请人： Sensorium Therapeutics, Inc.

发明人： Jacob M. Hooker ,  Michael S. Placzek

IPC分类号： C07D209/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D475/04 ,  C07D491/113 ,  C07D491/20 ,  C07D495/04 ,  C07D495/10 ,  C07D497/10 ,  C07D498/10 ,  C07D519/00 ,  C07F7/18

CPC分类号： C07D209/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D475/04 ,  C07D491/113 ,  C07D491/20 ,  C07D495/04 ,  C07D495/10 ,  C07D497/10 ,  C07D498/10 ,  C07D519/00 ,  C07F7/1804

摘要： Disclosed are prodrug compounds that can be converted to mesembrine under biologically relevant conditions, such as hydrolysis in vivo; and related methods of preparing and using these compounds. Stable preparations of isolated mesembrine stereoisomers are also provided.

公开(公告)号：US20240239805A1

公开(公告)日：2024-07-18

申请号：US18541565

申请日：2023-12-15

申请人： University of Kansas

发明人： Manvendra Pal Singh ,  Zarko Boskovic ,  Bryce Gaskins

IPC分类号： C07D491/20 ,  C07D471/04

CPC分类号： C07D491/20 ,  C07D471/04

摘要： The present disclosure is directed to a compound of Formula I, Formula II, Formula III, Formula IV, or Formula V




or a pharmaceutically acceptable salt and/or solvate thereof.

公开(公告)号：US11964986B1

公开(公告)日：2024-04-23

申请号：US18217914

申请日：2023-07-03

申请人： REJUVERON TELOMERE THERAPEUTICS AG

发明人： Patrick Schnider ,  Fedor Romanov Michailidis ,  Chien-Chi Hsiao

IPC分类号： C07D491/20 ,  C07D491/147

CPC分类号： C07D491/147

摘要： The present invention relates to 9-oxo-9,10-dihydro-6H-pyrano[3,2-b:4,5-b′]dipyridine-8-carboxylic acid derivatives, their manufacture, pharmaceutical compositions containing them and their use as a medicament.

公开(公告)号：US20240124443A1

公开(公告)日：2024-04-18

申请号：US18264310

申请日：2022-01-28

申请人： SCINNOHUB PHARMACEUTICAL CO., LTD

发明人： Anle YANG ,  Sen JI ,  Zhi WANG ,  Hao WANG ,  Dewei ZHANG ,  Xiao WANG ,  Huan SHEN ,  Jie XIANG ,  Jialing XIAN ,  Yan WANG ,  Xiao HU ,  Xiaodong ZHANG ,  Jun TANG

IPC分类号： C07D471/04 ,  A61P7/04 ,  C07D491/20

CPC分类号： C07D471/04 ,  A61P7/04 ,  C07D491/20

摘要： The present invention relates to a compound of formula (I) capable of inhibiting plasmin activity and having blood coagulation and hemostasis activity, and a pharmaceutically acceptable salt, hydrate, isomer, prodrug and mixture thereof, wherein R1 to R3 are as defined in the description.

公开(公告)号：US11939335B2

公开(公告)日：2024-03-26

申请号：US18199900

申请日：2023-05-19

申请人： 858 Therapeutics, Inc.

发明人： James M. Veal ,  Jeffrey A. Stafford ,  Donald S. Karanewsky ,  Shyama Herath

IPC分类号： A61K31/519 ,  C07D487/04 ,  C07D487/14 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00

CPC分类号： C07D487/04 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00 ,  C07B2200/05

摘要： Provided herein are inhibitors of PARG, pharmaceutical compositions comprising the inhibitory compounds, and methods for using the PARG inhibitory compounds for the treatment of disease. Said inhibitors of PARG have the structure provided in Formula (I):




as represented, for example, by Example 1:

公开(公告)号：US20230374022A1

公开(公告)日：2023-11-23

申请号：US18199900

申请日：2023-05-19

申请人： 858 Therapeutics, Inc.

发明人： James M. VEAL ,  Jeffrey A. STAFFORD ,  Donald S. KARANEWSKY ,  Shyama HERATH

IPC分类号： C07D487/04 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00

CPC分类号： C07D487/04 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00 ,  C07B2200/05

摘要： Provided herein are inhibitors of PARG, pharmaceutical compositions comprising the inhibitory compounds, and methods for using the PARG inhibitory compounds for the treatment of disease.

公开(公告)号：US20230312587A1

公开(公告)日：2023-10-05

申请号：US18075270

申请日：2022-12-05

申请人： Vertex Pharmaceutical Incorporated

发明人： David LAUFFER ,  Guy Bemis ,  Michael Boyd ,  David Deininger ,  Hongbo Deng ,  Warren Dorsch ,  Wenxin Gu ,  Russell R. Hoover ,  Mac Arthur Johnson, JR. ,  Mark Willem Ledeboer ,  Brian Ledford ,  Francois Maltais ,  Marina Penney ,  Darin Takemoto ,  Nathan D. Waal ,  Tiansheng Wang ,  Pan Li

IPC分类号： C07D487/04 ,  C07D491/20 ,  C07D487/14 ,  C07D519/00 ,  C07D471/14 ,  C07D498/04 ,  C07D471/04

CPC分类号： C07D487/04 ,  C07D491/20 ,  C07D487/14 ,  C07D519/00 ,  C07D471/14 ,  C07D498/04 ,  C07D471/04

摘要： The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).

公开(公告)号：US11702392B2

公开(公告)日：2023-07-18

申请号：US17181614

申请日：2021-02-22

申请人： MERCK PATENT GMBH

发明人： Catherine Jorand-Lebrun ,  Roch Boivin ,  Theresa Johnson ,  Yanping Wang ,  Yufang Xiao ,  Xiaoling Chen ,  Nina Linde ,  Doreen Musch ,  Deepak Kumar

IPC分类号： C07D239/36 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052 ,  C07D491/107 ,  C07D491/20 ,  A61P35/00

CPC分类号： C07D239/36 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052 ,  C07D491/107 ,  C07D491/20

摘要： The invention relates to pyrimidinone derivatives of the general Formula I,




or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

公开(公告)号：US20230175036A1

公开(公告)日：2023-06-08

申请号：US18161610

申请日：2023-01-30

申请人： Enzo Life Sciences, Inc.

发明人： Irina LEBEDEVA ,  Wayne Forrest PATTON ,  Maciej SZCZEPANIK ,  Yuejun XIANG ,  Praveen PANDE

IPC分类号： C12Q1/26 ,  C07C271/08 ,  C09K11/06 ,  C12Q1/37 ,  C12Q1/44 ,  C12Q1/48 ,  C07D311/08 ,  C07D491/052 ,  C07D491/20 ,  C07D493/10

CPC分类号： C12Q1/26 ,  C07C271/08 ,  C09K11/06 ,  C12Q1/37 ,  C12Q1/44 ,  C12Q1/485 ,  C07D311/08 ,  C07D491/052 ,  C07D491/20 ,  C07D493/10 ,  Y10T436/18 ,  G01N2333/902 ,  G01N2500/00 ,  G01N2333/92 ,  G01N2333/918 ,  C09K2211/1022 ,  C09K2211/1088

摘要： Provided is a compound comprising the structure:


(SIG)-(SI-MOD)m.

In this compound, SIG is a signaling molecule, SI is a self-immolative structure bound to SIG such that SIG has a reduced signal relative to the signal of SIG without SI, MOD is a moiety bound to SI that is subject to modification by an activator, and m is an integer from 1 to about 10. With this compound, when MOD is modified by an activator, SI is destabilized and self-cleaved from SIG such that SIG generates an increased signal. Also provided is a method of determining whether a sample comprises an activator, using the above-described compound. Additionally provided is a method of determining whether a cell comprises a nitroreductase using the above-described compound where nitroreductase is the activator. Further provided is a method of determining whether a mammalian cell is hypoxic using the above-described compound where nitroreductase is the activator. A method of detecting a microorganism that comprises a nitroreductase, using the above-described compound where nitroreductase is the activator, is also provided. Also provided is a method of identifying nitroreductase in a sample, using the above-described compound where nitroreductase is the activator.

公开(公告)号：US11655249B2

公开(公告)日：2023-05-23

申请号：US17239362

申请日：2021-04-23

申请人： Kind Pharmaceutical

发明人： Dong Liu ,  Dongdong Chen ,  Biao Deng ,  Xiangyun Tu ,  Zinan Fang ,  Haohao Wu ,  Danyan Gu

IPC分类号： C07D471/04 ,  A61P7/00 ,  C07D491/20

CPC分类号： C07D471/04 ,  A61P7/00 ,  C07D491/20

摘要： This invention relates to indolizine derivatives and their use in medicine. In particular, the present invention discloses novel substituted indolizine derivatives of formula I, or an isotopically labeled compound thereof, or an optical isomer thereof, a geometric isomer thereof, a tautomer thereof or a mixture of various isomers, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. The invention also relates to the use of these compounds in medicine.