公开(公告)号：US20240327353A1

公开(公告)日：2024-10-03

申请号：US18578066

申请日：2022-07-14

申请人： Northeastern University

发明人： Raymond BOOTH

IPC分类号： C07D213/38 ,  A61K31/135 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4409 ,  C07C211/42 ,  C07C211/49 ,  C07D307/52 ,  C07D333/20

CPC分类号： C07D213/38 ,  A61K31/135 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4409 ,  C07C211/42 ,  C07C211/49 ,  C07D307/52 ,  C07D333/20 ,  C07C2602/10

摘要： 4-phenyl-2-dimethylaminotetralin compounds, formulations, and methods are provided for selective modulation of serotonin 5-HT2A and 5-HT2C receptors without causing sedation at doses that are antipsychotic. Mechanisms for selective modulation are shown to involve inverse agonism at one or more of the 5-HT2A-2C receptors based on stereochemistry and substituents. The technology can be targeted to receptors inside or outside the central nervous system.

公开(公告)号：US20240262812A1

公开(公告)日：2024-08-08

申请号：US18570783

申请日：2022-06-10

申请人： Shanghai Leado Pharmatech Co., Ltd.

发明人： Youxin WANG ,  Lingling ZHANG ,  Qiang DING

IPC分类号： C07D409/12 ,  A61K31/341 ,  A61K31/343 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/426 ,  A61K31/443 ,  A61P1/00 ,  A61P29/00 ,  C07D207/335 ,  C07D231/12 ,  C07D233/64 ,  C07D249/06 ,  C07D261/08 ,  C07D277/28 ,  C07D307/52 ,  C07D307/54 ,  C07D307/79 ,  C07D333/20 ,  C07D333/34 ,  C07D405/12 ,  C07D417/12

CPC分类号： C07D409/12 ,  A61K31/341 ,  A61K31/343 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/426 ,  A61K31/443 ,  A61P1/00 ,  A61P29/00 ,  C07D207/335 ,  C07D231/12 ,  C07D233/64 ,  C07D249/06 ,  C07D261/08 ,  C07D277/28 ,  C07D307/52 ,  C07D307/54 ,  C07D307/79 ,  C07D333/20 ,  C07D333/34 ,  C07D405/12 ,  C07D417/12

摘要： The present invention relates to an N-substituted phenylsulfonamide compound and a use thereof. Specifically, the present invention provides a compound represented by formula I, or an optical isomer thereof, or a racemate thereof, or a pharmaceutically acceptable salt thereof. The compound described in the present invention has an excellent inhibitory effect on transient receptor potential channel proteins, and has an excellent therapeutic effect on transient receptor potential channel protein-related diseases, such as inflammatory bowel disease, irritable bowel syndrome, pain, and inflammation.

公开(公告)号：US20240173307A1

公开(公告)日：2024-05-30

申请号：US18330171

申请日：2023-06-06

申请人： Calico Life Sciences LLC ,  AbbVie Inc.

发明人： Kathleen Ann Martin ,  Carmela Sidrauski ,  Marina Pliushchev ,  Jennifer M. Frost ,  Yunsong Tong ,  Xiangdong Xu ,  Lei Shi ,  Qingwei Zhang ,  Zhaoming Xiong ,  Ramzi Farah Sweis ,  Michael J. Dart ,  Kathleen J. Murauski

IPC分类号： A61K31/44 ,  A61K31/165 ,  A61K31/18 ,  A61K31/341 ,  A61K31/35 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/443 ,  A61K31/444 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K45/06 ,  A61P25/28 ,  C07C237/24 ,  C07C311/46 ,  C07C323/40 ,  C07D213/40 ,  C07D213/64 ,  C07D213/71 ,  C07D213/75 ,  C07D213/85 ,  C07D231/12 ,  C07D233/64 ,  C07D235/14 ,  C07D237/14 ,  C07D239/34 ,  C07D239/47 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/28 ,  C07D307/52 ,  C07D333/20 ,  C07D401/12 ,  C07D405/12 ,  C07D471/04 ,  C07D471/08 ,  C07D493/08

CPC分类号： A61K31/44 ,  A61K31/165 ,  A61K31/18 ,  A61K31/341 ,  A61K31/35 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/443 ,  A61K31/444 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K45/06 ,  A61P25/28 ,  C07C237/24 ,  C07C311/46 ,  C07C323/40 ,  C07D213/40 ,  C07D213/64 ,  C07D213/71 ,  C07D213/75 ,  C07D213/85 ,  C07D231/12 ,  C07D233/64 ,  C07D235/14 ,  C07D237/14 ,  C07D239/34 ,  C07D239/47 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/28 ,  C07D307/52 ,  C07D333/20 ,  C07D401/12 ,  C07D405/12 ,  C07D471/04 ,  C07D471/08 ,  C07D493/08

摘要： Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

公开(公告)号：US20240166598A1

公开(公告)日：2024-05-23

申请号：US18264109

申请日：2022-02-02

申请人： Arizona Board of Regents on Behalf of the University of Arizona ,  The Board of Trustees of the University of Illinois

发明人： Gregory R. Thatcher ,  Zhengnan Shen ,  Rui Xiong ,  Kiira Ratia ,  Lijun Rong ,  Laura Cooper

IPC分类号： C07D205/04 ,  A61K39/215 ,  A61K39/39 ,  A61K45/06 ,  A61P31/14 ,  C07C211/49 ,  C07C237/30 ,  C07D209/08 ,  C07D209/14 ,  C07D211/58 ,  C07D211/62 ,  C07D213/81 ,  C07D215/12 ,  C07D333/20 ,  C07D333/58 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07H19/067

CPC分类号： C07D205/04 ,  A61K39/215 ,  A61K39/39 ,  A61K45/06 ,  A61P31/14 ,  C07C211/49 ,  C07C237/30 ,  C07D209/08 ,  C07D209/14 ,  C07D211/58 ,  C07D211/62 ,  C07D213/81 ,  C07D215/12 ,  C07D333/20 ,  C07D333/58 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07H19/067

摘要： Provided herein are PLpro inhibitors and methods of treating and/or preventing an infection caused by a coronavirus by administration of one or more of said PLpro inhibitors to a subject in need thereof, as well as pharmaceutical formulations and kits for use in these methods.

公开(公告)号：US11839147B2

公开(公告)日：2023-12-05

申请号：US16101565

申请日：2018-08-13

申请人： BEIJING SUMMER SPROUT TECHNOLOGY CO., LTD.

发明人： Chuanjun Xia

IPC分类号： C07C211/54 ,  C07C211/58 ,  C07C211/61 ,  C07C255/31 ,  C07C255/34 ,  C07C255/37 ,  C07C255/51 ,  C07C321/26 ,  C07C381/00 ,  C07D209/86 ,  C07D209/88 ,  C07D307/52 ,  C07D307/91 ,  C07D333/20 ,  C07D333/76 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D471/14 ,  C07D487/04 ,  C07D487/06 ,  C07D487/14 ,  C09K11/06 ,  H10K50/11 ,  H10K50/13 ,  H10K50/15 ,  H10K50/17 ,  H10K85/60

CPC分类号： H10K85/624 ,  C07C255/34 ,  C07C255/37 ,  C07C255/51 ,  C07C381/00 ,  H10K50/13 ,  H10K85/611 ,  H10K85/633 ,  H10K85/636 ,  H10K85/6572 ,  C07C2603/54 ,  H10K50/17 ,  H10K85/631

摘要： Hole injection layer and charge generation layer containing a truxene based compound are disclosed for organic electronic devices. By applying the truxene based compound for the hole injection layer, low driving voltage, high efficiency and long lifetime of the device can be achieved. In addition, a P-type charge generation layer comprising the truxene based compound can be used in tandem OLEDs structure and can further improve the voltage, efficiency and lifetime of the device.

公开(公告)号：US20230167101A1

公开(公告)日：2023-06-01

申请号：US17918074

申请日：2021-04-08

申请人： BAYLOR COLLEGE OF MEDICINE

发明人： Yongcheng Song ,  Fangrui Wu ,  Shenyou Nie ,  Yuanda Hua ,  Yi-Lun Lin ,  Salma Kaochar ,  Nicholas Mitsiades

IPC分类号： C07D409/12 ,  A61P35/00 ,  C07D405/14 ,  C07D409/14 ,  C07D333/20 ,  C07D405/12 ,  C07D417/12

CPC分类号： C07D409/12 ,  A61P35/00 ,  C07D333/20 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12

摘要： Embodiments of the present disclosure pertain to compositions that include a compound that inhibits the histone acetyl transferase activity of a protein, such as p300 and/or CBP. Further embodiments of the present disclosure pertain to methods of inhibiting the histone acetyl transferase activity of a protein by exposing the protein to a composition that contains one or more of the compounds of the present disclosure. The compositions of the present disclosure may be exposed to a protein in vitro or in vivo. Additional embodiments of the present disclosure pertain to methods of treating a cancer in a subject by administering a composition of the present disclosure to the subject in order to treat the cancer.

公开(公告)号：US20230139975A1

公开(公告)日：2023-05-04

申请号：US17909131

申请日：2021-03-03

申请人： Technische Hochschule Köln

发明人： Sherif EL SHEIKH ,  Henrik WEBER

IPC分类号： C07C211/35 ,  C07D213/16 ,  C07D239/26 ,  C07D237/08 ,  C07D241/12 ,  C07D333/20

摘要： The present invention relates to the technical field of pharmaceutical synthesis and development of drugs, and to a process for preparing cyclic 2-amino-1-one derivatives and to the reaction products and intermediates obtainable by this process. The present invention further relates to pharmaceutical compositions, in particular drugs or medicaments, comprising the cyclic 2-amino-1-one derivatives and to their use as medicaments, in particular in the prophylactic or therapeutic treatment of diseases of the human or animal body, preferably of neurodegenerative diseases or psychiatric disorders.

公开(公告)号：US11596691B2

公开(公告)日：2023-03-07

申请号：US17091863

申请日：2020-11-06

申请人： The General Hospital Corporation

发明人： Ralph Mazitschek ,  Balaram Ghosh ,  James Adam Hendricks ,  Surya Reis ,  Stephen John Haggarty

IPC分类号： C07D333/20 ,  C07D409/14 ,  C07D491/16 ,  C07F5/02 ,  C07C259/06 ,  C07C245/08 ,  C07C259/10 ,  A61K41/00

摘要： This invention relates to photoswitchable inhibitors of histone deacetylases and methods of using the same.

公开(公告)号：US11555012B2

公开(公告)日：2023-01-17

申请号：US16677768

申请日：2019-11-08

申请人： Nimbus Artemis, Inc.

发明人： Silvana Marcel Leit de Moradei ,  Eric Therrien

IPC分类号： C07C311/29 ,  C07C311/21 ,  C07D491/113 ,  C07D295/135 ,  C07D333/20 ,  C07D257/04 ,  C07D295/10 ,  C07D205/04 ,  C07D277/34 ,  C07D209/80 ,  C07D231/38 ,  C07D263/32 ,  C07D401/12 ,  C07D413/06 ,  C07D401/04 ,  C07D409/12 ,  C07D213/04

摘要： The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

公开(公告)号：US20220347176A1

公开(公告)日：2022-11-03

申请号：US17609177

申请日：2020-05-07

申请人： GREY WOLF THERAPEUTICS LIMITED

发明人： Martin QUIBELL ,  Jason John SHIERS ,  Michael SPARENBERG

IPC分类号： A61K31/505 ,  A61K31/192 ,  A61K31/4418 ,  A61K31/381 ,  A61K31/415 ,  A61K31/277 ,  A61K31/341 ,  A61K31/421 ,  A61K31/4196 ,  A61K31/402 ,  A61K31/4164 ,  A61K31/41 ,  A61K31/40 ,  A61K31/426 ,  A61K31/425 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/422 ,  A61K31/50 ,  A61K31/4155 ,  A61K45/06 ,  C07C311/29 ,  C07D213/42 ,  C07D333/20 ,  C07D231/12 ,  C07D307/52 ,  C07D263/32 ,  C07D249/08 ,  C07D207/325 ,  C07D233/64 ,  C07D257/04 ,  C07D213/57 ,  C07D409/10 ,  C07D239/26 ,  C07D207/335 ,  C07D333/24 ,  C07D333/22 ,  C07D333/38 ,  C07D213/56 ,  C07D207/327 ,  C07D277/28 ,  C07D275/02 ,  C07D417/10 ,  C07D401/10 ,  C07D277/30 ,  C07D413/10 ,  C07D237/08 ,  C07D403/10 ,  A61P37/02

摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO2— or —SO2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, C land alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, SO2NR12R13, heteroaryl, CONR10R11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; and R9 is H, alkyl or halo; R10 and R11 are each independently H or alkyl; and R12 and R13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).