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公开(公告)号：US20240018113A1
公开(公告)日：2024-01-18
申请号：US18372771
申请日：2023-09-26
发明人： Junko Maeda , Ikumi Kuriwaki , Kai Kitamura , Yumi Yamashita , Kenichi Kakefuda , Akio Kamikawa , Kenji Negoro , Wataru Hamaguchi , Ryushi Seo , Jeffrey Ciavarri
IPC分类号： C07D295/16 , C07D213/56 , C07D231/12 , C07D205/04 , C07D307/22 , C07D207/273 , C07D305/08 , C07D333/48 , C07D405/10 , C07D207/16 , C07D211/48 , C07C237/42 , C07C311/46 , C07C311/13 , C07D207/12 , C07D211/62 , C07C233/22 , C07D295/195 , C07C233/69 , C07C235/42 , C07D309/14 , C07D213/75 , C07D231/40 , C07D403/06 , C07C233/81 , C07D209/08 , C07D295/155 , C07D487/10 , C07D403/10 , C07D401/06 , C07D279/12 , C07D239/26
CPC分类号： C07D295/16 , C07D213/56 , C07D231/12 , C07D205/04 , C07D307/22 , C07D207/273 , C07D305/08 , C07D333/48 , C07D405/10 , C07D207/16 , C07D211/48 , C07C237/42 , C07C311/46 , C07C311/13 , C07D207/12 , C07D211/62 , C07C233/22 , C07D295/195 , C07C233/69 , C07C235/42 , C07D309/14 , C07D213/75 , C07D231/40 , C07D403/06 , C07C233/81 , C07D209/08 , C07D295/155 , C07D487/10 , C07D403/10 , C07D401/06 , C07D279/12 , C07D239/26
摘要： [Problem] A compound which is useful as a STING inhibitor is provided.
[Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.-
公开(公告)号：US11702424B2
公开(公告)日：2023-07-18
申请号：US16996117
申请日：2020-08-18
申请人： Pfizer Inc.
发明人： John David Trzupek , Katherine Lin Lee , Mark Edward Bunnage , Seungil Han , David Hepworth , Frank Eldridge Lovering , John Paul Mathias , Nikolaos Papaioannou , Betsy Susan Pierce , Joseph Walter Strohbach , Stephen Wayne Wright , Christoph Wolfgang Zapf , Lori Krim Gavrin , Arthur Lee , David Randolph Anderson , Kevin Joseph Curran , Christoph Martin Dehnhardt , Eddine Saiah , Joel Adam Goldberg , Xiaolun Wang , Horng-Chih Huang , Richard Vargas , Michael Dennis Lowe , Akshay Patny
IPC分类号： C07D491/056 , C07F7/18 , C07D401/14 , C07D405/14 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D207/273 , C07D498/04 , C07D209/52 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , C07C69/94 , A61K31/541 , A61K45/06 , C07D207/26 , C07D215/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , A61K31/40 , C07D207/08 , C07D207/267
CPC分类号： C07D491/056 , A61K31/40 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C69/94 , C07D207/08 , C07D207/26 , C07D207/267 , C07D207/273 , C07D209/52 , C07D215/48 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07F7/1804
摘要： Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.-
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：US20220363640A1
公开(公告)日：2022-11-17
申请号：US17208964
申请日：2021-03-22
发明人： Guangyi WANG , Leonid BEIGELMAN , Anh TRUONG , Carmela NAPOLITANO , Daniele ANDREOTTI , Haiying HE , Karin Ann STEIN
IPC分类号： C07D213/40 , C07D409/04 , C07D495/14 , C07D401/04 , C07D413/04 , C07D417/04 , C07D239/34 , C07D471/04 , C07D213/65 , C07D401/12 , C07D491/048 , C07D233/64 , C07D409/14 , C07D417/06 , C07D413/12 , C07D413/06 , C07D401/06 , C07D405/12 , C07D417/12 , C07D207/273 , C07D491/052 , A61K31/4436 , A61K31/4418 , A61K31/4178 , A61K31/4439 , A61K31/4365 , A61K31/422 , A61K31/4196 , A61K31/427 , A61K31/505 , A61K31/437 , A61K45/06 , A61K31/4355 , A61K31/444 , A61K31/4709
摘要： Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
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公开(公告)号：US20220363633A1
公开(公告)日：2022-11-17
申请号：US17733513
申请日：2022-04-29
发明人： Gary E. Schiltz , Jindan Yu
IPC分类号： C07D207/273 , C07D207/27
摘要： Disclosed are substituted pyrrolidones and piperidones which may be utilized as EZH2 targeting agents. The substituted pyrrolidones and piperidones may include substituted 2-pyrrolidones and 2-piperidones. The disclosed pyrrolidones and piperidones may be used in pharmaceutical compositions and methods for treating cell proliferative disorders such as cancer.
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公开(公告)号：US20220332683A1
公开(公告)日：2022-10-20
申请号：US17724125
申请日：2022-04-19
发明人： Jun Wang
IPC分类号： C07D207/273 , C07D207/46 , A61K31/16 , A61P11/00 , A61P31/14 , C07D209/02 , A61K9/00
摘要： This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a pyrrolidinone-acetamide (or similar) structure (e.g., Formula I) which function as inhibitors of the SARS-CoV-2 papain-like protease (PLpro), which function as inhibitors of the SARS-CoV-2 related viral 3CL protease (MPpro), which function as therapeutics for the treatment of viral infection characterized with PLPpro and/or Mpro protease activity and/or expression (e.g., COVID-19), and which function as therapeutics for the treatment of other conditions characterized with PLPpro and/or Mpro protease activity and/or expression.
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公开(公告)号：US11365191B2
公开(公告)日：2022-06-21
申请号：US16976363
申请日：2019-02-26
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 , C07D213/38 , C07C255/46 , C07D211/76 , C07D207/14 , C07D207/273 , C07C211/40 , C07D211/58 , C07D309/14 , C07D401/12 , C07C237/24 , C07D211/96 , A61P25/28
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.
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公开(公告)号：US20220177418A1
公开(公告)日：2022-06-09
申请号：US17599083
申请日：2020-03-27
申请人： The Regents of the University of California , The United States Government represented by the Department of Veterans Affairs
IPC分类号： C07C233/13 , C07C233/40 , C07C233/91 , C07C235/76 , C07C255/46 , C07C307/04 , C07C49/537 , C07C49/697 , C07C69/618 , C07D207/273 , C07D207/38 , C07D211/70 , C07D213/46 , C07D307/46 , C07D303/32 , C07D263/32
摘要： The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
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公开(公告)号：US11180490B2
公开(公告)日：2021-11-23
申请号：US16619961
申请日：2018-06-08
发明人： Joanne M. Smallheer , Nicholas R. Wurtz , Meriah Neissel Valente , Karen A. Rossi , Ellen K. Kick
IPC分类号： C07D207/273 , C07D401/12 , C07D401/14 , C07D403/12 , C07D407/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D405/12 , C07D405/14 , C07D409/12
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, and related diseases.
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公开(公告)号：US11124503B2
公开(公告)日：2021-09-21
申请号：US16055559
申请日：2018-08-06
IPC分类号： C07D409/06 , C07D207/27 , C07D207/273 , C07D207/277
摘要： This disclosure provides methods for intermolecular enantioselective C-acylation of lactams with quaternary stereogenic centers by applying a chiral Ni catalyst. The methods comprise treating a lactam of formula (IIa): with a chiral Ni catalyst, an aryl nitrile, and an aryl halide to provide compounds of formula (Ia):
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