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公开(公告)号：US10829499B2
公开(公告)日：2020-11-10
申请号：US16447271
申请日：2019-06-20
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Thomas H. Graham , Tao Yu , Yonglian Zhang , John A. McCauley
IPC: A61K31/4985 , C07D498/22 , A61P31/18 , C07D498/16 , A61K31/407 , A61K31/4188 , A61K31/5365 , A61K31/553 , C12N15/113
Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
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公开(公告)号：US20200261421A1
公开(公告)日：2020-08-20
申请号：US16461952
申请日：2017-12-19
Applicant: Merck Sharp & Dohme Corp.
Inventor： Brian McKittrick , John P. Caldwell , John A. McCauley , Henry Vaccaro , Tin-Yau Chan , Hyunjin Kim , Elizabeth Smith , Liwu Hong , Tanweer Khan , Shihong Ying , Hongwu Wang
IPC: A61K31/4168 , A61K45/06 , A61K31/497 , C07D233/72 , C07D403/12 , C07D401/12 , A61P31/18
Abstract: The present invention is directed to compounds of Formula I, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
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公开(公告)号：US10544155B2
公开(公告)日：2020-01-28
申请号：US16061369
申请日：2016-12-12
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Yonglian Zhang , Sherman T. Waddell , Tao Yu , John A. McCauley , Andrew Stamford
IPC: A61K31/4375 , A61K31/502 , A61K31/503 , A61K31/34 , C07D455/02 , C07D491/20 , A61P31/18 , A61K31/427 , A61K31/52 , A61K31/505 , A61K31/506 , A61K31/662
Abstract: The present invention relates to spirocyclic quinolizine derivatives and pharmaceutically acceptable salts or prodrug thereof, compositions comprising at least one spirocyclic quinolizine derivative, and methods of using the spirocyclic quinolizine derivatives for treating or preventing HIV infection in a subject.
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公开(公告)号：US20200017524A1
公开(公告)日：2020-01-16
申请号：US16465614
申请日：2017-12-01
Applicant: Merck Sharp & Dohme Corp.
Inventor： Thomas H. Graham , Tao Yu , Sherman T. Waddell , John A. McCauley
IPC: C07D498/16 , C07D471/16 , C07D491/22 , A61P31/18
Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, Y, Z, R1, R7A, R7B and R8 are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
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公开(公告)号：US10479801B2
公开(公告)日：2019-11-19
申请号：US15826898
申请日：2017-11-30
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Thomas H. Graham , Tao Yu , Yonglian Zhang , John A. McCauley
IPC: A61K31/4985 , C07D498/22 , A61K31/407 , A61K31/4188 , A61K31/5365 , A61K31/553 , C07D471/22 , C07D487/16 , C07D498/16 , A61P31/18 , C12N15/113
Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
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Patent Agency Ranking
公开(公告)号：US10233193B2
公开(公告)日：2019-03-19
申请号：US15575433
申请日：2016-05-20
Applicant: MERCK SHARP & DOHME CORP. , Tao Yu , Thomas H. Graham , Sherman T. Waddell , John A. McCauley , Andrew W. Stamford , John M. Sanders , Lihong Hu , Jiaqiang Cai , Lianyun Zhao
Inventor： Tao Yu , Thomas H. Graham , Sherman T. Waddell , John A. McCauley , Andrew W. Stamford , John M. Sanders , Lihong Hu , Jiaqiang Cai , Lianyun Zhao
IPC: A61K31/4375 , C07D491/147 , A61K31/4355 , A61K31/437 , C07D471/14 , A61K31/427 , A61K31/4402 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/635 , A61K31/675 , A61P31/18
Abstract: The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, m, R1, R2, R3, R3, R3, R4, R5 and R9 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.
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公开(公告)号：US20190040076A1
公开(公告)日：2019-02-07
申请号：US16061369
申请日：2016-12-12
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Yonglian Zhang , Sherman T. Waddell , Tao Yu , John A. McCauley , Andrew Stamford
IPC: C07D491/20 , A61P31/18 , A61K31/4375 , A61K31/506 , A61K31/34 , A61K31/505 , A61K31/52 , A61K31/662 , A61K31/427
CPC classification number: C07D491/20 , A61K31/34 , A61K31/427 , A61K31/4375 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/52 , A61K31/662 , A61K31/675 , A61P31/18 , C07D471/04 , A61K2300/00
Abstract: The present invention relates to spirocyclic quinolizine derivatives and pharmaceutically acceptable salts or prodrug thereof, compositions comprising at least one spirocyclic quinolizine derivative, and methods of using the spirocyclic quinolizine derivatives for treating or preventing HIV infection in a subject.
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公开(公告)号：US20180194774A1
公开(公告)日：2018-07-12
申请号：US15575433
申请日：2016-05-20
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Tao Yu , Thomas H. Graham , Sherman T. Waddell , John A. McCauley , Andrew W. Stamford , John M. Sanders , Lihong Hu , Jiaqiang Cai , Lianyun Zhao
IPC: C07D491/147 , A61K31/4375 , A61P31/18 , C07D471/14
CPC classification number: C07D491/147 , A61K31/427 , A61K31/4355 , A61K31/437 , A61K31/4375 , A61K31/4402 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/635 , A61K31/675 , A61P31/18 , C07D471/14 , A61K2300/00
Abstract: The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, m, R1, R2, R3, R3, R3, R4, R5 and R9 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.
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公开(公告)号：US20180155365A1
公开(公告)日：2018-06-07
申请号：US15826898
申请日：2017-11-30
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Thomas H. Graham , Tao Yu , Yonglian Zhang , John A. McCauley
IPC: C07D498/22 , C07D471/22 , A61K31/553 , A61K31/5365 , A61K31/4985 , A61K31/4188 , A61K31/407
Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula (I). and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
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公开(公告)号：US09737545B2
公开(公告)日：2017-08-22
申请号：US15104782
申请日：2014-12-17
Applicant: MERCK SHARP & DOHME CORP. , MERCK CANADA INC.
Inventor： John A. McCauley , Christian Beaulieu , David Jonathan Bennett , Christopher J. Bungard , Sheldon Crane , Thomas J. Greshock , Katharine M. Holloway , Helen Juteau , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Christian Nadeau , Daniel Simard , Satyanarayana Tummanapalli , Vouy Linh Truong , Karine M. Villeneuve , Peter D. Williams
IPC: A61K31/5377 , C07D417/04 , A61K45/06 , C07D487/04 , C07D471/04 , C07D413/04 , C07D265/30 , C07D413/14
CPC classification number: A61K31/5377 , A61K45/06 , C07D265/30 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
Abstract: The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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