公开(公告)号：US12091409B2

公开(公告)日：2024-09-17

申请号：US17350183

申请日：2021-06-17

申请人： ASTEX THERAPEUTICS LIMITED

发明人： Anthony William James Cooper ,  Nicole Cathleen Goodwin ,  Charlotte Mary Griffiths-Jones ,  Thomas Daniel Heightman ,  Jeffrey K. Kerns ,  Hendrika Maria Gerarda Willems ,  Hongxing Yan

IPC分类号： C07D249/04 ,  A61K31/4192 ,  A61K31/4402 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61P9/04 ,  A61P11/00 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D419/12 ,  C07D419/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D419/12 ,  C07D249/04 ,  C07D401/12 ,  C07D419/14 ,  C07D498/04 ,  C07D513/04

摘要： The present invention relates to ether-linked triazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators. In particular, the invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof:

公开(公告)号：US12084517B2

公开(公告)日：2024-09-10

申请号：US18206937

申请日：2023-06-07

申请人： YALE UNIVERSITY

发明人： David Spiegel ,  Ryan Murelli ,  Andrew Zhang

IPC分类号： C07K16/44 ,  A61K9/00 ,  A61K31/4192 ,  A61K45/06 ,  A61K47/54 ,  A61K47/55 ,  A61K47/64 ,  A61K47/68 ,  C07D249/04 ,  C07K16/30

CPC分类号： C07K16/44 ,  A61K9/0019 ,  A61K31/4192 ,  A61K45/06 ,  A61K47/54 ,  A61K47/549 ,  A61K47/55 ,  A61K47/646 ,  A61K47/68 ,  A61K47/6803 ,  A61K47/6869 ,  A61K47/6873 ,  A61K47/6891 ,  C07D249/04 ,  C07K16/3069 ,  C07K2317/31

摘要： The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.

公开(公告)号：US12012392B2

公开(公告)日：2024-06-18

申请号：US16761993

申请日：2018-11-09

申请人： Inflazome Limited

发明人： Matthew Cooper ,  David Miller ,  Angus Macleod ,  Stephen Thom ,  Stephen St-Gallay ,  Jonathan Shannon ,  Ian Strutt

IPC分类号： C07D401/06 ,  A61P29/00 ,  C07D231/18 ,  C07D233/84 ,  C07D249/04 ,  C07D249/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06

CPC分类号： C07D401/06 ,  A61P29/00 ,  C07D231/18 ,  C07D233/84 ,  C07D249/04 ,  C07D249/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06

摘要： The present invention relates to sulfonylureas and sulfonylthioureas comprising as-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with at least one group containing an oxygen atom, and wherein said oxygen atom is attached to the heteroaryl ring via at least two other atoms. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

公开(公告)号：US12000846B2

公开(公告)日：2024-06-04

申请号：US17254922

申请日：2019-06-28

申请人： Rheinische Friedrich-Wilhelms-Universitaet Bonn

发明人： Christoph Thiele

IPC分类号： G01N33/92 ,  C07C247/04 ,  C07D249/04 ,  C07D487/04 ,  G01N1/40

CPC分类号： G01N33/92 ,  C07C247/04 ,  C07D249/04 ,  C07D487/04 ,  G01N1/4022 ,  C07B2200/05 ,  G01N2001/4027 ,  G01N2458/15 ,  G01N2560/00 ,  G01N2570/00

摘要： Nitrogen containing compounds may have formulas (I), (II) and (IV), and such compounds may be suitable for detecting alkyne group containing organic compounds by mass spectrometry. Furthermore, methods may also include synthesizing these compounds, detecting of organic compounds containing the specific compounds, uses of the compounds in mass spectrometry for determining enzyme activity or monitoring the lipid metabolism in a cell, and a kit which contains at least one of these compounds and at least one internal standard.

公开(公告)号：US20240002354A1

公开(公告)日：2024-01-04

申请号：US18040596

申请日：2021-07-30

申请人： REZUBIO PHARMACEUTICALS CO., LTD

发明人： Yusheng XIONG ,  Hongping GUAN

IPC分类号： C07D249/04 ,  C07D405/14 ,  C07D405/04 ,  A61K45/06

CPC分类号： C07D249/04 ,  A61K45/06 ,  C07D405/04 ,  C07D405/14

摘要： Provided herein are novel compounds (e.g., Formula I), pharmaceutical compositions, and methods of using related to GPR40. The compounds herein are typically GPR40 agonists, which can be used for treating a variety of disorders, conditions or diseases such as Type 2 diabetes.

公开(公告)号：US11806337B2

公开(公告)日：2023-11-07

申请号：US17875216

申请日：2022-07-27

申请人： Sanford Burnham Prebys Medical Discovery Institute

发明人： Stephen Gardell ,  Anthony B. Pinkerton ,  Eduard Sergienko ,  Hampton Sessions

IPC分类号： A61K31/4409 ,  A61K31/196 ,  A61K31/245 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/417 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/50 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5386 ,  C07C275/42 ,  C07D213/40 ,  C07D213/56 ,  C07D213/643 ,  C07D213/73 ,  C07D213/74 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D249/04 ,  C07D261/08 ,  C07D263/32 ,  C07D277/28 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D498/08

CPC分类号： A61K31/4409 ,  A61K31/196 ,  A61K31/245 ,  A61K31/415 ,  A61K31/417 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4355 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/443 ,  A61K31/444 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/50 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5386 ,  C07C275/42 ,  C07D213/40 ,  C07D213/56 ,  C07D213/643 ,  C07D213/73 ,  C07D213/74 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D249/04 ,  C07D261/08 ,  C07D263/32 ,  C07D277/28 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D498/08

摘要： Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.

公开(公告)号：US20230303502A1

公开(公告)日：2023-09-28

申请号：US18019664

申请日：2021-08-04

申请人： SIGILON THERAPEUTICS, INC.

发明人： Richard Heidebrecht ,  Christopher P. Hencken ,  Omar De Paolis ,  Weiheng Wang ,  Matthew Buchanan

IPC分类号： C07D249/04 ,  C07D471/04 ,  C07D487/04 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

CPC分类号： C07D249/04 ,  C07D471/04 ,  C07D487/04 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

摘要： Described herein are compounds of Formulas (I), (II), and (III) and pharmaceutically acceptable salts thereof, related compositions and preparations thereof, as well as methods of making and using the same.

公开(公告)号：US20230295070A1

公开(公告)日：2023-09-21

申请号：US18200431

申请日：2023-05-22

申请人： Emory University

发明人： Eric Ortlund ,  Suzanne Mays ,  Nathan Jui ,  Autumn Flynn ,  Michael Dugan

IPC分类号： C07C59/54 ,  C07C35/50 ,  C07C39/23 ,  C07C43/23 ,  C07C49/683 ,  C07C49/83 ,  C07C215/70 ,  C07C255/47 ,  C07C271/34 ,  C07C307/02 ,  C07C309/66 ,  C07D249/04 ,  C07F9/09 ,  C07F9/572

CPC分类号： C07C59/54 ,  C07C35/50 ,  C07C39/23 ,  C07C43/23 ,  C07C49/683 ,  C07C49/83 ,  C07C215/70 ,  C07C255/47 ,  C07C271/34 ,  C07C307/02 ,  C07C309/66 ,  C07D249/04 ,  C07F9/091 ,  C07F9/572 ,  C07C2602/22

摘要： This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.

公开(公告)号：US11691939B2

公开(公告)日：2023-07-04

申请号：US17071382

申请日：2020-10-15

申请人： Emory University

发明人： Eric Ortlund ,  Suzanne Mays ,  Nathan Jui ,  Autumn Flynn ,  Michael Dugan

IPC分类号： C07C59/54 ,  C07C35/50 ,  C07C39/23 ,  C07C43/23 ,  C07C49/683 ,  C07C49/83 ,  C07C215/70 ,  C07C255/47 ,  C07C271/34 ,  C07C307/02 ,  C07C309/66 ,  C07D249/04 ,  C07F9/09 ,  C07F9/572

CPC分类号： C07C59/54 ,  C07C35/50 ,  C07C39/23 ,  C07C43/23 ,  C07C49/683 ,  C07C49/83 ,  C07C215/70 ,  C07C255/47 ,  C07C271/34 ,  C07C307/02 ,  C07C309/66 ,  C07D249/04 ,  C07F9/091 ,  C07F9/572 ,  C07C2602/22

摘要： This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.

公开(公告)号：US20230192757A1

公开(公告)日：2023-06-22

申请号：US18169964

申请日：2023-02-16

申请人： Sage Therapeutics, Inc.

发明人： Gabriel Martinez Botella ,  Francesco G. Salituro ,  Albert Jean Robichaud ,  Boyd L. Harrison

IPC分类号： C07J43/00 ,  C07D249/18 ,  C07D231/14 ,  C07D295/033 ,  C07D249/04 ,  A61P25/00 ,  C07J13/00 ,  C07J75/00 ,  A61K9/00 ,  A61K31/58

CPC分类号： C07J43/003 ,  C07D249/18 ,  C07D231/14 ,  C07D295/033 ,  C07D249/04 ,  A61P25/00 ,  C07J13/007 ,  C07J75/00 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/58

摘要： Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein, R1, R2a, R2b, R3 and A are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.