公开(公告)号：US20240293362A1

公开(公告)日：2024-09-05

申请号：US18634344

申请日：2024-04-12

申请人： Board of Trustees of Michigan State University

发明人： Edmund L. ELLSWORTH ,  Kin Sing Stephen LEE

IPC分类号： A61K31/40 ,  A61K31/397 ,  A61K31/403 ,  A61K31/407 ,  A61K31/438 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/4468 ,  A61K31/46 ,  A61P25/28 ,  C07D205/04 ,  C07D207/09 ,  C07D207/14 ,  C07D209/52 ,  C07D211/58 ,  C07D221/24 ,  C07D401/12 ,  C07D451/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10

CPC分类号： A61K31/40 ,  A61K31/397 ,  A61K31/403 ,  A61K31/407 ,  A61K31/438 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/4468 ,  A61K31/46 ,  A61P25/28 ,  C07D205/04 ,  C07D207/09 ,  C07D207/14 ,  C07D209/52 ,  C07D211/58 ,  C07D221/24 ,  C07D401/12 ,  C07D451/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10

摘要： Compounds and methods to treat or prevent CNS diseases, such as Alzheimer's disease and brain injury inflammation, are disclosed herein. The compounds are soluble epoxide hydrolase (sEH) inhibitors and have improved physical properties, blood-brain-barrier (BBB) penetration and long drug-target residence time. Pharmaceutical compositions and kits comprising the compounds are also disclosed herein.

公开(公告)号：US11993576B2

公开(公告)日：2024-05-28

申请号：US17424292

申请日：2020-01-21

申请人： Hangzhou Yirui Pharmaceutical Technology Co., Ltd

发明人： Xiaolu Wang ,  Yongzhou Hu ,  Qing Ye ,  Xiuai Hu

IPC分类号： C07D295/205 ,  A61P17/06 ,  C07D207/14 ,  C07D211/46 ,  C07D211/52 ,  C07D211/54 ,  C07D211/58 ,  C07D211/74 ,  C07D211/88 ,  C07D213/42 ,  C07D231/12 ,  C07D233/36 ,  C07D233/64 ,  C07D241/08 ,  C07D277/28 ,  C07D295/155 ,  C07D307/52

CPC分类号： C07D295/205 ,  A61P17/06 ,  C07D207/14 ,  C07D211/46 ,  C07D211/52 ,  C07D211/54 ,  C07D211/58 ,  C07D211/74 ,  C07D211/88 ,  C07D213/42 ,  C07D231/12 ,  C07D233/36 ,  C07D233/64 ,  C07D241/08 ,  C07D277/28 ,  C07D295/155 ,  C07D307/52

摘要： The invention provides an N-benzyl-N-arylsulfonamide derivative, which is an N-benzyl-N-arylsulfonamide compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof. The N-benzyl-N-arylsulfonamide derivative is obtained by condensing a substituted nitrobenzene with 5- or 6-membered nitrogen-containing aliphatic heterocycle (the ring B), reducing the nitro group to an amino group, and subjecting the amino group to reductive amination, sulfonamidation; or by subjecting a substituted nitrobenzene to nitro reduction, reductive amination and sulfonamidation, and condensing the resultant intermediate with 5- or 6-membered nitrogen-containing aliphatic heterocycle (the ring B). It has been experimentally demonstrated that the N-benzyl-N-arylsulfonamide derivative of the invention can specifically bind to Kv1.3 potassium channel and inhibit or decrease its activity, and is useful in the treatment of autoimmune diseases caused by abnormal activation of the Kv1.3 potassium channel in human or animals. The invention further provides a medicament or a pharmaceutical composition comprising the N-benzyl-N-arylsulfonamide derivative.

公开(公告)号：US20230348426A1

公开(公告)日：2023-11-02

申请号：US18004731

申请日：2021-07-08

申请人： Bristol-Myers Squibb Company

发明人： Pravin Sudhakar Shirude ,  Chandrasekhar Reddy Rachamreddy ,  Amit Kumar Chattopadhyay ,  Balaji Seshadri ,  Vishweshwaraiah Baligar ,  Sudhakara Reddy Madduri ,  Ellen K. Kick ,  Nicholas R. Wurtz

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D207/14 ,  C07F9/6558 ,  C07D487/08 ,  C07D413/14 ,  C07D405/14 ,  C07D491/107 ,  C07D491/08 ,  C07D403/04 ,  C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07F9/572

CPC分类号： C07D401/14 ,  C07D207/14 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08 ,  C07D491/107 ,  C07D498/04 ,  C07F9/572 ,  C07F9/65583

摘要： The disclosure relates to compounds of Formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.

公开(公告)号：US20230312499A1

公开(公告)日：2023-10-05

申请号：US18053582

申请日：2022-11-08

申请人： H. Lundbeck A/S ,  THE SCRIPPS RESEARCH INSTITUTE

发明人： Justin S. CISAR ,  Cheryl A. GRICE ,  Todd K. JONES ,  Micah J. NIPHAKIS ,  Jae Won CHANG ,  Kenneth M. LUM ,  Benjamin F. CRAVATT

IPC分类号： C07D295/205 ,  C07C271/12 ,  C07D317/46 ,  C07D317/58 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D241/04 ,  C07D471/04 ,  C07D471/10 ,  C07D261/08 ,  C07D487/04 ,  C07D263/32 ,  C07D205/04 ,  C07D491/107 ,  C07D207/14 ,  C07D271/06 ,  C07D307/79 ,  C07D405/14 ,  C07D215/42 ,  C07D213/40 ,  A61P25/22 ,  C07D295/26 ,  C07D213/55 ,  C07D401/04 ,  C07D407/06 ,  C07D413/06 ,  C07C271/10 ,  C07D207/09 ,  C07D213/38 ,  C07D215/46 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10

CPC分类号： C07D295/205 ,  C07C271/12 ,  C07D317/46 ,  C07D317/58 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D241/04 ,  C07D471/04 ,  C07D471/10 ,  C07D261/08 ,  C07D487/04 ,  C07D263/32 ,  C07D205/04 ,  C07D491/107 ,  C07D207/14 ,  C07D271/06 ,  C07D307/79 ,  C07D405/14 ,  C07D215/42 ,  C07D213/40 ,  A61P25/22 ,  C07D295/26 ,  C07D213/55 ,  C07D401/04 ,  C07D407/06 ,  C07D413/06 ,  C07C271/10 ,  C07D207/09 ,  C07D213/38 ,  C07D215/46 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10

摘要： This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.

公开(公告)号：US20230242548A1

公开(公告)日：2023-08-03

申请号：US18058655

申请日：2022-11-23

申请人： The Regents of the University of California

发明人： Jonathan Ostrem ,  Ulf Peters ,  Kevan M. Shokat

IPC分类号： C07D495/04 ,  A61K38/17 ,  C07D231/40 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/10 ,  C07D207/14 ,  C07D211/62 ,  C07D295/185 ,  C07D295/26 ,  C07D211/58 ,  C07D487/04 ,  C12N9/14 ,  C07C235/20 ,  C07C317/08 ,  C12Q1/6886

CPC分类号： C07D495/04 ,  A61K38/1709 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/26 ,  C07D295/185 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C12N9/14 ,  C12Q1/6886 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Y306/05002 ,  G01N2500/04

摘要： K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

公开(公告)号：US11708327B2

公开(公告)日：2023-07-25

申请号：US17400421

申请日：2021-08-12

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Pravin Sudhakar Shirude ,  Vishweshwaraiah Baligar ,  Balaji Seshadri ,  Amit Kumar Chattopadhyay ,  Nicholas R. Wurtz ,  Ellen K. Kick

IPC分类号： C07D207/14 ,  C07D403/10 ,  C07D401/10 ,  C07D401/12 ,  A61P9/10 ,  C07D413/10 ,  C07D409/12 ,  A61P9/04 ,  C07D403/12 ,  C07F9/6558 ,  C07D405/10 ,  C07F9/572 ,  A61P9/00 ,  C07D417/10 ,  C07D413/14 ,  A61K31/4015 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/675

CPC分类号： C07D207/14 ,  A61K31/4015 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/675 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D409/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07F9/572 ,  C07F9/5728 ,  C07F9/65583 ,  C07F9/65586

摘要： The disclosure relates to compounds of Formulae (I)-(IX), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.

公开(公告)号：US20230144411A1

公开(公告)日：2023-05-11

申请号：US17841570

申请日：2022-06-15

申请人： Dart NeuroScience, LLC

发明人： Jillian Basinger Thompson ,  Brett C. Bookser ,  Scott Burley ,  Pablo Garcia-Reynaga ,  Andrew Hudson ,  Marco Peters ,  Benjamin Pratt ,  Aaron Thompson ,  Joe Tran ,  Lino Valdez

IPC分类号： C07D405/12 ,  A61P25/28 ,  C07C211/40 ,  C07C237/24 ,  C07C255/46 ,  C07D207/14 ,  C07D207/273 ,  C07D211/58 ,  C07D211/76 ,  C07D211/96 ,  C07D213/38 ,  C07D309/14 ,  C07D401/12

CPC分类号： C07D405/12 ,  A61P25/28 ,  C07C211/40 ,  C07C237/24 ,  C07C255/46 ,  C07D207/14 ,  C07D207/273 ,  C07D211/58 ,  C07D211/76 ,  C07D211/96 ,  C07D213/38 ,  C07D309/14 ,  C07D401/12 ,  C07C2601/08 ,  C07C2601/16 ,  C07C2601/14

摘要： Substituted cyclohexyl chemical entities of Formula (I):






wherein Ra, G, and Rb have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.

公开(公告)号：US20230040770A1

公开(公告)日：2023-02-09

申请号：US17427490

申请日：2020-01-30

申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED

发明人： Yasushi HATTORI ,  Yuhei MIYANOHANA ,  Tatsuki KAJITA ,  Tatsuki KOIKE ,  Yasutaka HOASHI ,  Norihito TOKUNAGA ,  Alexander Martin PAWLICZEK ,  Tsuneo ODA ,  Tohru MIYAZAKI ,  Yoshiteru ITO ,  Kohei TAKEUCHI ,  Keisuke IMAMURA ,  Takahiro SUGIMOTO

IPC分类号： C07D403/06 ,  C07D207/14

摘要： The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

公开(公告)号：US20230021834A1

公开(公告)日：2023-01-26

申请号：US17320574

申请日：2021-05-14

申请人： Takeda Pharmaceutical Company Limited

发明人： Zacharia Cheruvallath ,  Jason Green ,  Ben Johnson ,  Kristin Schleicher ,  Huikai Sun ,  Mingnam Tang

IPC分类号： A61K31/4439 ,  A61K31/40 ,  A61K31/4355 ,  A61K31/438 ,  A61K31/4468 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  C07D207/14 ,  C07D211/58 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D491/048

摘要： Disclosed are compounds of Formula 1, stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein L, r, s, R5, R6, R7, R9, R10, R11, R12, X1, X2, X3, X4, X13, and X14 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.

公开(公告)号：US20220411368A1

公开(公告)日：2022-12-29

申请号：US17775795

申请日：2020-11-13

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： Hiroyuki NAKAMURA

IPC分类号： C07D207/14

摘要： A benzoic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile is provided. A sorbic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile is also provided.