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公开(公告)号：US20240239788A1
公开(公告)日：2024-07-18
申请号：US18555640
申请日：2022-04-15
发明人： David L. Sloman , Gianni Chessari , Patrick Schöpf , Steven Howard , Yuichi Kawai , Kazuaki Shibata , Hiroki Asakura , Takao Uno , Takeshi Sagara , Masayuki Nakamura , Yu Kobayakawa , David Jonathan Bennett , Indu Bharathan , Thomas H. Graham , Yongxin Han , Zahid Hussain , Xiaoshen Ma , Mihir Mandal , Ryan D. Otte , Anandan Palani , Uma Swaminathan , Mycah Uehling , Yingchun Ye , Ryan Chau , Alec H. Christian , Symon Gathiaka , Timothy J. Henderson , Elisabeth T. Hennessy , Andrew J. Hoover , Shuhei Kawamura , Igri Kolaj , Thomas W. Lyons , Matthew J. Mitcheltree , Aaron Sather
IPC分类号： C07D451/06 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D471/08 , C07D519/00
CPC分类号： C07D451/06 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D471/08 , C07D519/00
摘要： Compounds or their pharmaceutically acceptable salts can inhibit the G12D mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
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公开(公告)号：US20230143552A1
公开(公告)日：2023-05-11
申请号：US17962346
申请日：2022-10-07
发明人： Edward Holson , Florence Fevrier Wagner , Michel Weiwer , Edward Scolnick , Michelle Palmer , Luka Dordevic , Michael C. Lewis , Jennifer Q. Pan , Yan-Ling Zhang , Qihong Xu
IPC分类号： C07D207/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/10 , C07D491/048 , C07D491/052 , C07D491/056 , C07D491/107 , C07D211/18 , C07D211/38 , C07D211/42 , C07D211/48 , C07D211/58 , C07D211/62 , C07D211/70 , C07D211/22 , A61P25/18 , A61P25/16
CPC分类号： C07D207/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/10 , C07D491/048 , C07D491/052 , C07D491/056 , C07D491/107 , C07D211/18 , C07D211/38 , C07D211/42 , C07D211/48 , C07D211/58 , C07D211/62 , C07D211/70 , C07D211/22 , A61P25/18 , A61P25/16 , C07K14/70571
摘要： The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.
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公开(公告)号：US20230068499A1
公开(公告)日：2023-03-02
申请号：US17388100
申请日：2021-07-29
发明人： MICHAEL LUZZIO , BRIAN LUCAS , TIANSHENG WANG , JUN FENG
IPC分类号： C07D451/14 , C07D451/06 , C07D498/08 , C07D519/00
摘要： Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, pharmaceutical compositions comprising the same, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
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公开(公告)号：US11299490B2
公开(公告)日：2022-04-12
申请号：US16940696
申请日：2020-07-28
发明人： Jean-Christophe Andrez , Kristen Nicole Burford , Sultan Chowdhury , Charles Jay Cohen , Christoph Martin Dehnhardt , Robert Joseph Devita , James Roy Empfield , Thilo Focken , Michael Edward Grimwood , Syed Abid Hasan , James Philip Johnson, Jr. , Alla Yurevna Zenova
IPC分类号： C07D451/06 , C07D403/12 , C07D213/76 , C07D237/20 , C07D239/69 , C07D413/12 , C07D417/12 , C07D261/16 , C07D493/10 , C07D277/52 , C07D285/08 , C07D401/12 , C07D417/14
摘要： This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.
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5.发明申请公开(公告)号：US20210309656A1
公开(公告)日：2021-10-07
申请号：US17265266
申请日：2019-08-06
发明人： Rajiv Sharma , Lambertus Benthem , Robert Judkins
IPC分类号： C07D451/06 , C07D413/12 , C07D261/08
摘要： Provided are compounds that can act as a modulator of a farnesoid X receptor (FXR) and that can be useful in the treatment of diseases and/or disorders associated with the FXR. Compositions including such compounds are also provided along with methods for preparing compounds of the present invention and their use.
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公开(公告)号：US20210147355A1
公开(公告)日：2021-05-20
申请号：US16826028
申请日：2020-03-20
发明人： Edward Holson , Florence Fevrier Wagner , Michel Weiwer , Edward Scolnick , Michelle Palmer , Luka Dordevic , Michael C. Lewis , Jennifer Q. Pan , Yan-Ling Zhang , Qihong Xu
IPC分类号： C07D207/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/10 , C07D491/048 , C07D491/052 , C07D491/056 , C07D491/107 , C07D211/18 , C07D211/38 , C07D211/42 , C07D211/48 , C07D211/58 , C07D211/62 , C07D211/70 , C07D211/22 , A61P25/18 , A61P25/16
摘要： The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.
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公开(公告)号：US20210115057A1
公开(公告)日：2021-04-22
申请号：US17133372
申请日：2020-12-23
发明人： Matthew Cullen , Cecilia M. Bastos , Daniel Parks , Benito Munoz
IPC分类号： C07D487/08 , C07D451/06 , C07F7/08 , C07D491/22
摘要： The present invention is directed to compounds having the Formulae (Ia), (Ib), (Ic), or (Id); or the Formulae (II), (IIa), (IIb), or (IIc); or the Formulae (III), (IIIa), (IIIb), (IIIc), (IIId), or (IIIe), and pharmaceutically acceptable salts, solvates, clathrates and prodrugs of any Formula thereof, compositions thereof, and methods for the treatment of a condition associated with a dysfunction in proteostasis.
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公开(公告)号：US10981926B2
公开(公告)日：2021-04-20
申请号：US16677906
申请日：2019-11-08
发明人： Gilles Bignan , Peter J. Connolly , Ian Hickson , Lieven Meerpoel , Vineet Pande , Zhuming Zhang , Jonathan Branch , Christian Rocaboy , Luis B. Trabalón Escolar
IPC分类号： C07D491/10 , C07D491/107 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D409/14 , C07D451/02 , C07D451/06 , C07D487/04 , C07D491/044 , C07D491/048 , A61K9/00 , A61K31/4439 , A61K31/4545 , A61K31/46 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/573 , A61K31/58
摘要： Disclosed are compounds, compositions and methods for treating of disorders that are affected by the antagonism of one or more androgen receptor types. Such compounds are represented by Formula (I) as follows: wherein R1 and G are defined herein.
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公开(公告)号：US10377742B2
公开(公告)日：2019-08-13
申请号：US15603023
申请日：2017-05-23
发明人： Dane Goff , Donald Payan , Rajinder Singh , Simon Shaw , David Carroll , Yasumichi Hitoshi
IPC分类号： C07D401/14 , C07D213/82 , C07D401/06 , C07D401/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/06 , C07D471/10 , C07D487/04 , C07D495/04 , C07D405/12 , C07D213/81 , C07D213/56 , C07D401/04
摘要： Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
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公开(公告)号：US10358448B2
公开(公告)日：2019-07-23
申请号：US16043829
申请日：2018-07-24
IPC分类号： C07D471/18 , C07D451/04 , C07D451/06 , C07D451/00 , C07D451/10 , C07D451/12
摘要： The invention provides compounds of Formula 1: and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.
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