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公开(公告)号:US20240293362A1
公开(公告)日:2024-09-05
申请号:US18634344
申请日:2024-04-12
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.
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公开(公告)号:US11993576B2
公开(公告)日:2024-05-28
申请号:US17424292
申请日:2020-01-21
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.
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公开(公告)号:US20230348426A1
公开(公告)日:2023-11-02
申请号:US18004731
申请日:2021-07-08
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.
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公开(公告)号:US20230312499A1
公开(公告)日:2023-10-05
申请号:US18053582
申请日:2022-11-08
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.
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公开(公告)号:US20230242548A1
公开(公告)日:2023-08-03
申请号:US18058655
申请日:2022-11-23
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.
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公开(公告)号:US11708327B2
公开(公告)日:2023-07-25
申请号:US17400421
申请日:2021-08-12
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.
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公开(公告)号:US20230144411A1
公开(公告)日:2023-05-11
申请号:US17841570
申请日:2022-06-15
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:US20180251443A9
公开(公告)日:2018-09-06
申请号:US15537283
申请日:2015-12-16
发明人: Gary A. PIAZZA , Xi CHEN , Adam B. KEETON , Michael R. BOYD
IPC分类号: C07D317/64 , C07D307/54 , C07C235/32 , C07D207/14 , C07D213/75 , C07D211/56 , A61K31/341 , A61K31/36 , A61K31/401 , A61K31/40 , A61K31/44 , A61K31/445 , C07D307/52 , C07D307/38 , C07D213/24 , C07C233/58 , C07D405/12 , C07D235/30 , C07C237/20 , C07D207/337
CPC分类号: C07D317/64 , A61K31/165 , A61K31/167 , A61K31/216 , A61K31/341 , A61K31/36 , A61K31/40 , A61K31/401 , A61K31/421 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/445 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K45/06 , A61K2300/00 , C07C233/58 , C07C235/32 , C07C235/34 , C07C237/20 , C07C311/29 , C07C2601/02 , C07C2602/08 , C07D207/14 , C07D207/335 , C07D207/337 , C07D211/56 , C07D213/24 , C07D213/40 , C07D213/75 , C07D235/30 , C07D307/38 , C07D307/52 , C07D307/54 , C07D405/12 , G01N33/5748 , A61K2800/00
摘要: Disclosed are compounds, for example, a compound of formula I, wherein R, R0, R1-R8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition for example, cancer, mediated by the ras gene.
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公开(公告)号:US20180221514A1
公开(公告)日:2018-08-09
申请号:US15748556
申请日:2016-08-17
IPC分类号: A61K49/20 , A61K31/015 , A61K31/05 , A61K31/353 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/53
CPC分类号: A61K49/20 , A61K31/015 , A61K31/05 , A61K31/353 , A61K31/4015 , A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/53 , C07D207/14 , C07D207/20 , C07D207/273 , C07D491/052
摘要: The present invention provides methods of using nitroxide spin-labeled amyloid beta-binding compounds to image amyloid. The present invention also provides nitroxide spin-labeled amyloid beta-binding compounds
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公开(公告)号:US20180194718A1
公开(公告)日:2018-07-12
申请号:US15806722
申请日:2017-11-08
发明人: Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号: C07C243/38 , C07D493/10 , C07D491/107 , A61K31/192 , C07D405/06 , C07D401/04 , C07D309/08 , C07D307/68 , C07D295/32 , C07D265/30 , C07D261/04 , C07D261/02 , C07D239/36 , C07D233/06 , C07D213/87 , C07D213/86 , C07D213/75 , C07D213/65 , C07D213/61 , C07D213/56 , C07D211/62 , C07D211/60 , C07D211/48 , C07D211/46 , C07D211/42 , C07D211/38 , C07D211/22 , C07D207/16 , C07D207/14 , C07D207/12 , C07D207/09 , C07D207/08 , C07D205/04 , C07C259/04 , C07C243/32 , C07C243/24 , C07C235/80 , C07C235/78 , C07C235/74 , C07C235/34 , C07C235/20 , C07C235/12 , C07C233/56 , A61K45/06 , A61K31/5375 , A61K31/495 , A61K31/4409 , A61K31/4406 , A61K31/44 , A61K31/42 , A61K31/4015 , A61K31/40 , A61K31/397 , A61K31/341 , A61K31/197
CPC分类号: C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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