公开(公告)号：US12037324B2

公开(公告)日：2024-07-16

申请号：US17861809

申请日：2022-07-11

申请人： Université de Montréal ,  Bristol-Myers Squibb Company

发明人： Eldon Scott Priestley ,  Samuel Kaye Reznik ,  Edward H. Ruediger ,  James R. Gillard ,  Oz Scott Halpern ,  Wen Jiang ,  Jeremy Richter ,  Rejean Ruel ,  Sasmita Tripathy ,  Wu Yang ,  Xiaojun Zhang

IPC分类号： C07D401/14 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61P9/04 ,  C07D233/90 ,  C07D235/26 ,  C07D239/20 ,  C07D257/04 ,  C07D271/07 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/10

CPC分类号： C07D401/14 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61P9/04 ,  C07D233/90 ,  C07D235/26 ,  C07D239/20 ,  C07D257/04 ,  C07D271/07 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/10

摘要： The present invention provides compounds of Formula (I):




wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are biased agonists, or β-Arrestin agonists of the angiotensin II receptor, which may be used as medicaments.

公开(公告)号：US12030876B2

公开(公告)日：2024-07-09

申请号：US18166689

申请日：2023-02-09

申请人： Ikena Oncology, Inc.

发明人： Alfredo C. Castro ,  Karen J. McGovern ,  Michael Burke

IPC分类号： A61K31/426 ,  A61P1/00 ,  A61P29/00 ,  C07D235/00 ,  C07D249/14 ,  C07D263/48 ,  C07D271/07 ,  C07D271/113 ,  C07D277/42 ,  C07D277/48 ,  C07D285/135 ,  C07D333/36 ,  C07D417/04 ,  C07D417/12

CPC分类号： C07D417/04 ,  A61K31/426 ,  A61P1/00 ,  A61P29/00 ,  C07D235/00 ,  C07D249/14 ,  C07D263/48 ,  C07D271/07 ,  C07D271/113 ,  C07D277/42 ,  C07D277/48 ,  C07D285/135 ,  C07D333/36 ,  C07D417/12

摘要： The present invention provides AHR agonists, compositions thereof, and methods of using the same.

公开(公告)号：US20220249447A1

公开(公告)日：2022-08-11

申请号：US17606720

申请日：2020-04-24

申请人： Purdue Research Foundation

发明人： Herman O. Sintim ,  George Naclerio

IPC分类号： A61K31/4245 ,  C07D413/04 ,  C07D417/14 ,  C07D413/14 ,  C07D271/113 ,  C07D409/04 ,  C07D271/07 ,  C07D413/12 ,  C07D277/46 ,  C07D231/40 ,  C07D257/06 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4196 ,  A61K31/433 ,  A61K31/426 ,  A61K31/415 ,  A61K31/41 ,  A61K45/06

摘要： The present invention generally relates to compounds as a new antibiotic to treat various infections, including infections caused by methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate and vancomycin-resistant S. aureus (VISA and VRSA respectively) vancomycin-resistant Enterococcusfaecalis (VRE), and Clostridioides difficile. Pharmaceutical compositions and methods for treating those infection diseases are within the scope of this invention.

公开(公告)号：US11384060B2

公开(公告)日：2022-07-12

申请号：US16477072

申请日：2018-01-22

申请人： ALPHALA CO., LTD.

发明人： Cheng-Ho Chung ,  Shi-Liang Tseng ,  Yung-Ning Yang ,  Yen-Fu Chen

IPC分类号： C07D233/92 ,  C07D257/04 ,  C07D277/66 ,  C07D471/04 ,  C07D417/04 ,  C07D307/81 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D263/57 ,  C07D213/56 ,  C07D491/04 ,  C07D271/06 ,  C07D271/10 ,  C07D271/113 ,  C07D401/04 ,  C07D401/12 ,  C07D231/18 ,  C07D403/04 ,  C07D239/34 ,  C07D237/14 ,  C07D333/60 ,  A61P3/10 ,  C07D307/79 ,  C07C233/92 ,  C07D209/08 ,  C07D213/90 ,  C07D271/07

摘要： Disclosed are compounds of formula (I) below and pharmaceutically acceptable salts thereof: (I), in which each of variables R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Y is defined herein. Also disclosed are methods for reducing the glycemic level and treating glucagon-associated disorders with a compound of formula (I) or a salt thereof and a pharmaceutical composition containing same.

公开(公告)号：US20210094907A1

公开(公告)日：2021-04-01

申请号：US16981654

申请日：2019-03-21

申请人： NORTHWESTERN UNIVERSITY

发明人： Ali Shilatifard ,  Kaivvei Liang ,  Edwin R. Smith ,  Gary E. Schiitz ,  Rama K. Mishra ,  Kristen Stoltz

IPC分类号： C07C235/74 ,  C07C235/78 ,  C07D241/20 ,  C07D213/40 ,  C07D257/06 ,  C07D271/07 ,  C07D277/46 ,  C07D213/75 ,  C07D239/42 ,  C07D261/18 ,  C07D231/14 ,  C07D239/36 ,  A61P35/00

摘要： Disclosed are compounds which may be utilized to inhibit transcription by RNA Polymerase II (Pol II), and in particular to disrupt the Super Elongation Complex (SEC). The compounds may be utilized in pharmaceutical compositions and methods for treating diseases and disorders associated with the biological activity of SEC, and in particular, diseases and disorders that are associated with high levels of expression of genes whose expression is SEC-dependent and that promote, support, or otherwise are required for the disease or disorder such as cancers.

公开(公告)号：US20200262828A1

公开(公告)日：2020-08-20

申请号：US16758495

申请日：2018-10-24

申请人： Yumanity Therapeutics, Inc.

发明人： Matthew LUCAS ,  Bertrand LE BOURDONNEC ,  Iwona WRONA ,  Bhaumik PANDYA ,  Parcharee TIVITMAHAISOON ,  Kerem OZBOYA ,  Benjamin VINCENT ,  Daniel TARDIFF ,  Jeff PIOTROWSKI ,  Eric SOLIS ,  Robert SCANNEVIN ,  Chee-Yeun CHUNG ,  Rebecca ARON ,  Kenneth RHODES

IPC分类号： C07D413/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D271/07 ,  C07D413/10 ,  C07D487/04 ,  C07D487/10

摘要： The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.

公开(公告)号：US10377695B2

公开(公告)日：2019-08-13

申请号：US15820194

申请日：2017-11-21

申请人： Sanford Burnham Prebys Medical Research Institute

发明人： Raveendra Panickar Dhanya ,  Douglas J. Sheffler ,  Nicholas D. P. Cosford

IPC分类号： C07D333/24 ,  C07C65/40 ,  C07D257/04 ,  C07D271/06 ,  C07C259/10 ,  C07C311/51 ,  C07C235/46 ,  C07C235/54 ,  C07D213/79 ,  C07D213/80 ,  C07D239/26 ,  C07D241/12 ,  C07D271/07 ,  C07D285/08 ,  C07D295/108 ,  C07D213/50 ,  C07D213/68 ,  C07D213/70 ,  C07D307/42 ,  C07D307/68 ,  C07F7/02 ,  C07D213/64 ,  C07C49/84 ,  C07C59/90 ,  C07C69/92 ,  C07C251/48 ,  C07C255/56 ,  C07D213/55 ,  C07D241/24 ,  C07D277/24 ,  C07D285/12 ,  C07D295/16 ,  C07D295/26 ,  C07D307/54 ,  C07D311/16 ,  C07F5/02 ,  C07F5/04

摘要： Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

公开(公告)号：US20180044329A1

公开(公告)日：2018-02-15

申请号：US15556805

申请日：2016-03-09

申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED

发明人： Pottayil Govindan Nair Sasikumar ,  Muralidhara Ramachandra ,  Appukkuttan Prasad ,  Seetharamaiah Setty Sudarshan Naremaddepalli

IPC分类号： C07D413/04 ,  A61K45/06 ,  C07D271/07 ,  A61K31/496 ,  C07D413/14 ,  A61K31/4245 ,  A61K31/497 ,  C07D271/06 ,  C07D417/04 ,  A61K31/454 ,  A61K31/55

CPC分类号： C07D413/04 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/55 ,  A61K45/06 ,  C07D271/06 ,  C07D271/07 ,  C07D413/14 ,  C07D417/04

摘要： The present invention relates to 3-substituted-1,2,4-oxadiazole and thiadiazole compounds of formula (I) or formula (II) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.

公开(公告)号：US09873688B2

公开(公告)日：2018-01-23

申请号：US15093486

申请日：2016-04-07

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Ming Tao ,  William Frietze ,  David J. Meloni ,  Lingkai Weng ,  Jiacheng Zhou ,  Yongchun Pan

IPC分类号： C07D413/04 ,  C07D271/08 ,  C07D271/07 ,  C07C307/06 ,  C07D271/04

CPC分类号： C07D413/04 ,  C07C307/06 ,  C07D271/04 ,  C07D271/08

摘要： The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.

公开(公告)号：US20170342039A1

公开(公告)日：2017-11-30

申请号：US15481568

申请日：2017-04-07

申请人： Farmington Pharma Development

发明人： William F. Brubaker

IPC分类号： C07D273/06 ,  C07C279/14 ,  C07C279/24 ,  C07D273/04 ,  C07D271/07

CPC分类号： C07D273/06 ,  C07B2200/05 ,  C07C279/14 ,  C07C279/24 ,  C07D271/07 ,  C07D273/04

摘要： The invention describes membrane permeable creatine prodrugs, pharmaceutical compositions comprising membrane permeable creatine prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine prodrugs or pharmaceutical compositions thereof.