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公开(公告)号：US09738661B2
公开(公告)日：2017-08-22
申请号：US14638733
申请日：2015-04-03
Applicant: Merck Sharp & Dohme Corp. , MSD Italia S.R.L.
Inventor： Nigel J. Liverton , Vincenzo Summa , Steven Harper , John A. McCauley , Joseph J. Romano , Michael T. Rudd
IPC: A61K31/519 , C07D498/22 , C07D498/08 , C07D498/18 , C07K5/083 , C07K5/087 , A61K31/407 , A61K31/4192 , A61K31/437 , A61K31/439 , A61K45/06 , A61K38/00
CPC classification number: C07D498/22 , A61K31/407 , A61K31/4192 , A61K31/437 , A61K31/439 , A61K38/00 , A61K45/06 , C07D498/08 , C07D498/18 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/0812
Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
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公开(公告)号：US20150266897A1
公开(公告)日：2015-09-24
申请号：US14638733
申请日：2015-04-03
Applicant: Merck Sharp & Dohme Corp. , MSD Italia S.R.L.
Inventor： Nigel J. Liverton , Vincenzo Summa , Maria Emilia Di Francesco , Marco Ferrara , Kevin F. Gilbert , Steven Harper , John A. McCauley , Charles J. McIntyre , Alessia Petrocchi , Marco Pompei , Joseph J. Romano , Michael T. Rudd , John W. Butcher , M. Katharine Holloway
IPC: C07D498/22 , A61K31/437 , A61K31/439 , C07D498/08 , A61K31/407 , A61K31/4192 , C07D498/18 , A61K45/06
CPC classification number: C07D498/22 , A61K31/407 , A61K31/4192 , A61K31/437 , A61K31/439 , A61K38/00 , A61K45/06 , C07D498/08 , C07D498/18 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/0812
Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。
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公开(公告)号：US20190315769A1
公开(公告)日：2019-10-17
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: C07D498/22 , A61P31/18 , C07D498/16 , C07D487/16 , A61K31/553 , A61K31/4188 , A61K31/407 , A61K31/5365 , A61K31/4985 , C07D471/22
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：US20180325926A1
公开(公告)日：2018-11-15
申请号：US15775871
申请日：2016-11-11
Applicant: Merck Sharp & Dohme Corp.
Inventor： Thomas H. Graham , Tao Yu , Sherman T. Waddell , John A. McCauley , Andrew Stamford , Wengsheng Liu , Jay A. Grobler , Libo Xu
IPC: A61K31/675 , A61P31/18
CPC classification number: A61K31/675 , A61K31/426 , A61K31/513 , A61K31/52 , A61K2300/00 , A61P31/18 , C07D491/20 , C07F9/6561
Abstract: The present invention relates to Spirocyclic Pyridotriazine Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R16 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Pyridotriazine Derivative, and methods of using the Spirocyclic Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
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公开(公告)号：US09834526B2
公开(公告)日：2017-12-05
申请号：US15104510
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 , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Satyanarayana Tummanapalli , Vouy Linh Truong , Peter D. Williams
IPC: A61K31/535 , C07D265/28 , C07D265/30 , A61K45/06 , A61K31/5375 , A61K31/5377 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
CPC classification number: C07D265/30 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
Abstract: The present invention is directed to 2,5,6-substituted morpholine 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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Patent Agency Ranking
公开(公告)号：US10934312B2
公开(公告)日：2021-03-02
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: A61K31/53 , A61P31/18 , C07D471/16 , C07D498/16 , C07D491/22 , A61K45/06
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：US10786488B2
公开(公告)日：2020-09-29
申请号：US16479997
申请日：2018-01-23
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Tao Yu , John A. McCauley , Alan Whitehead , James M. Apgar , Izzat T. Raheem , Guizhen Dong , Sherman T. Waddell , Hong Li
IPC: A61K31/4375 , A61K31/427 , A61K31/4402 , A61K31/47 , A61K31/506 , A61K31/5365 , A61K31/675 , A61K31/7068 , A61K31/7076 , C07D491/147
Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
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公开(公告)号：US10548910B2
公开(公告)日：2020-02-04
申请号：US15775966
申请日：2016-11-11
Applicant: Merck Sharp & Dohme Corp.
Inventor： Thomas H. Graham , Tao Yu , Sherman T. Waddell , John A. McCauley , Andrew Stamford , Wensheng Liu , Jay A. Grobler , Libo Xu
IPC: A61K31/675 , A61P31/18 , A61K31/683 , A61K31/34 , A61K31/426 , A61K31/44 , A61K31/513 , A61K31/52 , A61K31/535 , A61K31/7068
Abstract: The present invention relates to Amido-Substituted Pyridotriazine Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein B, X, Y, R, R1, R2 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Pyridotriazine Derivative, and methods of using the Amido-Substituted Pyridotriazine Derivatives for treating or preventing HIV infection in a subject.
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公开(公告)号：US10081647B2
公开(公告)日：2018-09-25
申请号：US15560896
申请日：2016-03-25
Applicant: Merck Sharp & Dohme Corp.
Inventor： Tao Yu , Sherman T. Waddell , John A. McCauley , Thomas H. Graham , Hong Li , Izzat Raheem , Jay A. Grobler
IPC: A61K31/675 , C07F9/6561 , A61K31/683
CPC classification number: C07F9/6561 , A61K31/427 , A61K31/4402 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/635 , A61K31/675 , A61K31/683 , A61K2300/00
Abstract: The present invention relates to Phosphate Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Phosphate Substituted Quinolizine Derivative, and methods of using the Phosphate Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
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公开(公告)号：US20160296527A1
公开(公告)日：2016-10-13
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 , C07D413/14 , C07D471/04 , C07D487/04 , A61K45/06 , C07D413/04
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.
Abstract translation: 本发明涉及5-杂芳基吗啉衍生物及其用于抑制HIV蛋白酶，HIV复制的抑制，HIV预防感染，HIV感染治疗以及预防，治疗和延迟的用途 艾滋病的发病或进展。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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