公开(公告)号：US20220259227A1

公开(公告)日：2022-08-18

申请号：US17670689

申请日：2022-02-14

Applicant: Merck Sharp & Dohme Corp.

Inventor： Timothy John Hartingh ,  John A. McCauley ,  Tao Yu ,  Yonglian Zhang

IPC: C07D498/22 ,  A61K45/06

Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula and pharmaceutically acceptable salts or prodrug thereof, wherein R1 is 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.

公开(公告)号：US20190322666A1

公开(公告)日：2019-10-24

申请号：US16454857

申请日：2019-06-27

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Tao Yu ,  Sherman T. Waddell ,  Thomas H. Graham ,  Yonglian Zhang ,  John A. McCauley ,  Andrew W. Stamford ,  Jiaqiang Cai ,  Zhiqi Qi

IPC: C07D471/16 ,  A61K31/635 ,  A61K31/427 ,  A61K31/513 ,  A61K31/5365 ,  A61K31/4402 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/52 ,  A61K31/683

Abstract: The present invention relates to Fused Tricyclic Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocyclic Compound, and methods of using the Fused Tricyclic Heterocyclic Compounds for treating or preventing HIV infection in a subject.

公开(公告)号：US10201533B2

公开(公告)日：2019-02-12

申请号：US15725407

申请日：2017-10-05

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Tao Yu ,  Yonglian Zhang ,  Sherman Tim Waddell ,  John M. Sanders ,  Thomas H. Graham ,  Hong Li

IPC: C07D491/00 ,  A61K31/44 ,  A61K31/4375 ,  C07D455/02 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/505 ,  A61K31/513 ,  A61K31/52 ,  A61K31/635 ,  A61K31/675 ,  C07D455/00 ,  C07D455/04 ,  C07D471/14 ,  C07D491/147 ,  A61K45/06 ,  C07D519/00

Abstract: The present invention relates to 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 Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.

公开(公告)号：US20180099967A1

公开(公告)日：2018-04-12

申请号：US15840017

申请日：2017-12-13

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Tao Yu ,  Sherman T. Waddell ,  Thomas H. Graham ,  Yonglian Zhang ,  John A. McCauley ,  Andrew W. Stamford ,  Jiaqiang Cai ,  Zhiqi Qi

IPC: C07D471/16 ,  A61K31/52 ,  A61K31/4402 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/427 ,  A61K31/5365 ,  A61K31/635 ,  A61K31/683 ,  A61K31/513

CPC classification number: C07D471/16 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/513 ,  A61K31/52 ,  A61K31/5365 ,  A61K31/635 ,  A61K31/683

Abstract: The present invention relates to Fused Tricyclic Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocyclic Compound, and methods of using the Fused Tricyclic Heterocyclic Compounds for treating or preventing HIV infection in a subject.

公开(公告)号：US20180051043A1

公开(公告)日：2018-02-22

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: C07F9/6561 ,  A61K31/683 ,  A61K31/675

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.

公开(公告)号：US09676780B2

公开(公告)日：2017-06-13

申请号：US14655572

申请日：2013-12-20

Applicant: MERCK SHARP & DOHME CORP. ,  Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Michael Berlin ,  Pauline Ting ,  Gang Zhou ,  Tao Yu ,  Christopher Boyce ,  Joseph Michael Kelly ,  Jayaram R. Tagat ,  Junying Zheng ,  Xianhai Huang ,  Wei Zhou ,  Jae-Hun Kim ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Rajan Anand ,  Qiaolin Deng

Inventor： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Michael Berlin ,  Pauline Ting ,  Gang Zhou ,  Tao Yu ,  Christopher Boyce ,  Joseph Michael Kelly ,  Jayaram R. Tagat ,  Junying Zheng ,  Xianhai Huang ,  Wei Zhou ,  Jae-Hun Kim ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Rajan Anand ,  Qiaolin Deng

IPC: C07D487/04 ,  A61K31/519 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

CPC classification number: C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

Abstract: Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

公开(公告)号：US20190365727A1

公开(公告)日：2019-12-05

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 ,  C07D491/147 ,  A61K31/5365 ,  A61K31/506 ,  A61K31/7068 ,  A61K31/7076 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/675 ,  A61K31/47

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.

公开(公告)号：US10138212B2

公开(公告)日：2018-11-27

申请号：US15549242

申请日：2016-02-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Amjad Ali ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Pauline C. Ting ,  Purakkattle Biju ,  Manuel de Lera Ruiz ,  Sylvia J. Degrado ,  Alexander L. Tung ,  Timothy J. Henderson ,  Liwu Hong ,  Jae-Hun Kim ,  Dong Won-Shik Kim ,  Joe Lee ,  Jie Wu ,  Heping Wu ,  Yushi Xiao ,  Tao Yu ,  Gang Zhou ,  Xiaohong Zhu ,  Kevin D. McCormick ,  Jayaram R. Tagat ,  Dong Xiao ,  Tanweer Khan ,  Jianhua Cao ,  Michael Berlin ,  Yonglian Zhang

IPC: C07D239/84 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61P25/14 ,  A61K31/517

Abstract: The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.

公开(公告)号：US20180325927A1

公开(公告)日：2018-11-15

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 ,  Wengsheng Liu ,  Jay A. Grobler ,  Libo Xu

IPC: A61K31/675 ,  A61K31/683 ,  A61P31/18

CPC classification number: A61K31/675 ,  A61K31/34 ,  A61K31/426 ,  A61K31/44 ,  A61K31/513 ,  A61K31/52 ,  A61K31/535 ,  A61K31/683 ,  A61K31/7068 ,  A61K45/06 ,  A61K2300/00 ,  A61P31/18 ,  C07D471/04 ,  C07F9/6561

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.

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.