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1. 发明公开

US20240239807A1 SARS-COV2 MAIN PROTEASE INHIBITORS 审中-公开
公开(公告)号：US20240239807A1
公开(公告)日：2024-07-18
申请号：US18365919
申请日：2023-08-04
申请人： Gilead Sciences, Inc.
发明人： Stephen E. Ammann , Xinpei Cai , Eda Y. Canales , Weng K. Chang , Gregory F. Chin , Henok H. Kinfe , Scott E. Lazerwith , Jessica L. McKinley , Michael R. Mish , Devan Naduthambi , Jason K. Perry , Kevin X. Rodriguez , Scott D. Schroeder , Christopher J. Swank , Joshua J. Van Veldhuizen
IPC分类号： C07D495/04 , A61P31/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/107 , C07D491/113 , C07D498/04 , C07D513/04 , C07D519/00
CPC分类号： C07D495/04 , A61P31/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/107 , C07D491/113 , C07D498/04 , C07D513/04 , C07D519/00
摘要： The present disclosure relates to compounds of Formula I:

and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, useful in the treatment of treating viral infections, for example, coronaviridae infections.

2. 发明授权

US11993583B2 Therapeutic compounds 有权
公开(公告)号：US11993583B2
公开(公告)日：2024-05-28
申请号：US16694332
申请日：2019-11-25
申请人： Gilead Sciences, Inc.
发明人： Michael Graupe , John O. Link , Roland D. Saito , Scott D. Schroeder , Dimitrios Stefanidis , Winston C. Tse , Jennifer R. Zhang
IPC分类号： C07D487/00 , A61K31/4439 , A61K31/537 , A61K31/675 , A61K31/7076 , A61K45/06 , C07C317/08 , C07D231/54 , C07D231/56 , C07D401/14 , C07F5/02
CPC分类号： C07D401/14 , A61K31/4439 , A61K31/537 , A61K31/675 , A61K31/7076 , A61K45/06 , C07C317/08 , C07D231/54 , C07F5/025 , A61K31/4439 , A61K2300/00
摘要： The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb):

which are useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

3. 发明公开

US20230391747A1 GLP-1R MODULATING COMPOUNDS 审中-公开
公开(公告)号：US20230391747A1
公开(公告)日：2023-12-07
申请号：US18195767
申请日：2023-05-10
申请人： Gilead Sciences, Inc.
发明人： Stephen E. Ammann , Gediminas J. Brizgys , James S. Cassidy , Elbert Chin , Chienhung Chou , Jeromy J. Cottell , Michael Graupe , Chao-I Hung , Kavoos Kolahdouzan , Scott D. Schroeder , Nathan D. Shapiro , Daniel G. Shore , Suzanne M. Szewczyk , James G. Taylor , Rhiannon Thomas-Tran , Nathan E. Wright , Zheng-Yu Yang , Sheila M. Zipfel
IPC分类号： C07D401/14 , A61K45/06 , C07D235/16 , C07D401/10 , C07D403/06 , C07D405/14 , C07D409/14 , C07D471/04 , C07D493/08 , C07D413/14 , C07D417/14
CPC分类号： C07D401/14 , A61K45/06 , C07D235/16 , C07D401/10 , C07D403/06 , C07D405/14 , C07D409/14 , C07D471/04 , C07D493/08 , C07D413/14 , C07D417/14
摘要： The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.

4. 发明公开

US20230212148A1 THERAPEUTIC COMPOUNDS FOR HIV VIRUS INFECTION 审中-公开
公开(公告)号：US20230212148A1
公开(公告)日：2023-07-06
申请号：US18061150
申请日：2022-12-02
申请人： Gilead Sciences, Inc.
发明人： Gediminas J. Brizgys , Chienhung Chou , Hang Chu , Julie Farand , Michael Graupe , Tezcan Guney , Darryl Kato , Jiayao Li , John O. Link , James B.C. Mack , Dong Min Mun , Scott D. Schroeder , William J. Watkins , Qiaoyin Wu , Jennifer R. Zhang
IPC分类号： C07D401/14 , C07F9/6558 , A61K45/06
CPC分类号： C07D401/14 , C07F9/65583 , A61K45/06
摘要： Background: HIV capsid (CA) is an emerging target for antiretroviral treatment PF-3450074 (P74) is a small-molecule CA binder that has been proposed to inhibit reverse transcription (RT) by accelerating HIV core uncoating. PF74 antiviral potency can depend on cyclophilin A (CypA) binding to CA in some cells and it shares a CA binding site with the host nuclear transport factor CPSF6, which restrict HIV infection when mislocalized to the cell cytoplasm. Here we further interrogate the mechanism of action (MOA) for PF74 in human T cells and clarify its potential dependence on CypA and CPSF6.
Methodology: HIV reporter viruses were produced in HEK293T cells and used to infect MT2 cells and primary CD4+ T cells to determine the antiviral effect of PF74. Compound exposure was controlled by staggered addition and cell washing at various times post-infection. DNA products of infection were analyzed by qPCR. CypA and CPSF6 levels were varied in MT2 cells by overexpression and shRNA knockdown. CA (P90A, N74D) and CPSF6 (FG50,AA) mutations were used to eliminate CypA or CPSF6 binding to the viral capsid. CPSF6 binding to CA was tested using a CA-NO pull down assay.
Results: PF74 efficiently inhibited late (EC50=795 nM) and early (EC50=264 nM) post-entry stages of HIV-1 replication in single-round infectivity assays and stabilized CA-NC polymers in vitro. Stable CypA knockdown or mutation of the CypA binding site of CA (P90A) had no effect on HIV infectivity or PF74 antiviral potency in T cells. CypA-independence of PF74 MOA was confirmed in PBMCs using HIV isolates unable to bind CypA due to CA polymorphisms. Drug washout studies showed that at high concentrations (100× EC50), PF74 inactivates cell-free virus via core disassembly and also acts concomitant with the RT step in infected cells. At 10× EC50, however, PF74 acted post-RT and was not virucidal, suggesting antiviral mechanism(s) beyond capsid destabilization. In time-of-addition studies, PF74 (10× EC50) remained active when added after RT but before vDNA integration, and normal levels of late-RT products but reduced 2-LTR circles were observed under these conditions. In contrast, reduced late-RT products were detected at higher compound concentrations. Although PF74 did compete with CPSF6 binding to CA in vitro, it remained active against the N740 mutant virus that does not bind CPSF6, suggesting a CPSF6-independent MOA.
Conclusions: Although PF74 can accelerate viral capsid disassembly at high concentrations, our results indicate that this compound primarly acts after the RT step, but prior to 2-LTR circle accumulation in human T cells, via a CypA- and CPSF6-independent MOA. We propose that by directly stabilizing the viral capsid at lower drug concentrations, PF74 may interfere with nuclear targeting of the pre-integration complex.

5. 发明申请

US20220267302A1 THERAPEUTIC COMPOUNDS 有权
公开(公告)号：US20220267302A1
公开(公告)日：2022-08-25
申请号：US17584643
申请日：2022-01-26
申请人： Gilead Sciences, Inc.
发明人： Gediminas Brizgys , Eda Canales , Chienhung Chou , Michael Graupe , Jiayao Li , Roland D. Saito , Scott D. Schroeder , Winston C. Tse , Qiaoyin Wu , Jennifer R. Zhang
IPC分类号： C07D401/14 , A61P31/18 , C07D405/14 , C07D413/14
摘要： The invention provides compounds having Formula (I): or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising the same, processes for their preparation, and methods of treating and preventing HIV infection by their administration.

6. 发明申请

US20210009555A1 THERAPEUTIC COMPOUNDS 有权
公开(公告)号：US20210009555A1
公开(公告)日：2021-01-14
申请号：US16882804
申请日：2020-05-26
申请人： Gilead Sciences, Inc.
发明人： Gediminas Brizgys , Eda Canales , Chien-Hung Chou , Michael Graupe , Randall L. Halcomb , Yunfeng Eric Hu , Scott E. Lazerwith , John O. Link , Qi Liu , Yafan Lu , Roland D. Saito , Scott D. Schroeder , John R. Somoza , Winston C. Tse , Jennifer R. Zhang
IPC分类号： C07D401/12 , C07D401/14 , C07D403/14 , C07D471/04 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K45/06 , C07D491/052 , C07D401/04 , C07D413/14 , C07D417/14 , C07D487/04
摘要： Compounds of formula (I) or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

7. 发明申请

US20200262815A1 THERAPEUTIC COMPOUNDS 审中-公开
公开(公告)号：US20200262815A1
公开(公告)日：2020-08-20
申请号：US16694332
申请日：2019-11-25
申请人： Gilead Sciences, Inc.
发明人： Michael Graupe , Steven J. Henry , John O. Link , Charles William Rowe , Roland D. Saito , Scott D. Schroeder , Dimitrios Stefanidis , Winston C. Tse , Jennifer R. Zhang
IPC分类号： C07D401/14 , A61K31/4439 , A61K31/537 , A61K31/675 , A61K31/7076 , A61K45/06 , C07F5/02 , C07C317/08 , C07D231/54
摘要： The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb): which are useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

8. 发明授权

US10316017B2 COT modulators and methods of use thereof 有权
公开(公告)号：US10316017B2
公开(公告)日：2019-06-11
申请号：US15697755
申请日：2017-09-07
申请人： Gilead Sciences, Inc.
发明人： Elizabeth M. Bacon , Gayatri Balan , Chien-Hung Chou , Christopher T. Clark , Jeromy J. Cottell , Musong Kim , Thorsten A. Kirschberg , John O. Link , Gary Phillips , Scott D. Schroeder , Neil H. Squires , Kirk L. Stevens , James G. Taylor , William J. Watkins , Nathan E. Wright , Sheila M. Zipfel
IPC分类号： C07D401/12 , C07D453/02 , C07D417/14 , C07D413/14 , C07D413/12 , C07D409/14 , C07D405/14 , C07D401/14 , C07F7/08
摘要： The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.

9. 发明申请

US20180194746A1 Compounds For the Treatment of HIV 审中-公开
公开(公告)号：US20180194746A1
公开(公告)日：2018-07-12
申请号：US15902883
申请日：2018-02-22
申请人： Gilead Sciences, Inc.
发明人： Steven S. Bondy , Carina E. Cannizzaro , Chien-Hung Chou , Randall L. Halcomb , Yunfeng Eric Hu , John O. Link , Qi Liu , Scott D. Schroeder , Winston C. Tse , Jennifer R. Zhang
IPC分类号： C07D401/12 , A61K31/4545 , C07D213/40 , C07D409/14 , C07D413/14 , A61K31/4439 , A61K31/444 , C07D491/052 , A61K31/4709 , A61K31/4985 , A61K31/50 , A61K31/506 , A61K31/5377 , C07D495/04 , C07D491/04 , C07D487/04 , C07D471/06 , C07D471/04 , C07D405/12 , C07D403/14 , C07D403/12 , C07D401/14 , A61K45/06
CPC分类号： C07D401/12 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4985 , A61K31/50 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/40 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D491/04 , C07D491/052 , C07D495/04
摘要： The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

10. 发明授权

US08822430B2 Antiviral compounds 有权
公开(公告)号：US08822430B2
公开(公告)日：2014-09-02
申请号：US13956195
申请日：2013-07-31
申请人： Gilead Sciences, Inc.
发明人： Elizabeth M. Bacon , Eda Canales , Aesop Cho , Jeromy J. Cottell , Manoj C. Desai , Michael Graupe , Hongyan Guo , Randall L. Halcomb , Darryl Kato , Choung U. Kim , Thorsten A. Kirschberg , Evan S. Krygowski , Scott E. Lazerwith , John O. Link , Hongtao Liu , Qi Liu , Richard L. Mackman , Michael L. Mitchell , Jay P. Parrish , Hyung-Jung Pyun , Joseph H. Saugier , Scott D. Schroeder , Jianyu Sun , James G. Taylor , James D. Trenkle , Winston C. Tse , Randall W. Vivian , William J. Watkins , Lianhong Xu
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D495/04 , A61K31/4178 , A61K31/7068 , A61K31/7052 , A61K31/4184 , A61P1/16 , A61P31/14
CPC分类号： C07D403/14 , A61K31/4025 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/435 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K45/06 , A61P31/12 , C07D207/16 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D491/113 , C07D495/04 , C07F5/025
摘要： The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

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