公开(公告)号：US11498923B2

公开(公告)日：2022-11-15

申请号：US16769603

申请日：2018-12-10

Applicant: Merck Sharp & Dohme Corp.

Inventor： Yeon-Hee Lim ,  Gioconda V. Gallo-Etienne ,  Joseph Michael Kelly ,  Michael Berlin ,  Pauline Ting ,  Hongwu Wang

IPC: C07D487/04 ,  C07D519/00

Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof: wherein: “Z” and R1 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：US20160194330A1

公开(公告)日：2016-07-07

申请号：US14655572

申请日：2013-12-20

Applicant: 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 TAGAT ,  Junying ZHENG ,  Xianhai HUANG ,  Wei ZHOU ,  Jae-Hun KIM ,  Nicolas ZORN ,  Dong XIAO ,  Gioconda V. GALLO ,  Walter WON ,  Heping WU ,  Rajan ANAND ,  MERCK SHARP & DOHME CORP.

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 ,  C07D487/18 ,  C07D487/08 ,  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.

Abstract translation: 公开了式A化合物（结构表示），其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

公开(公告)号：US20180193314A1

公开(公告)日：2018-07-12

申请号：US15815212

申请日：2016-06-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Junying Zheng ,  Walter Won ,  Michael Berlin ,  Pauline Ting ,  Guoqing Li ,  Dong Xiao ,  Hongwu Wang ,  Robert Aslanian

IPC: A61K31/4162 ,  A61K31/519 ,  A61K31/497 ,  A61P25/00

CPC classification number: A61K31/4162 ,  A01N43/80 ,  A61K31/497 ,  A61K31/519 ,  A61P25/00 ,  C07D487/04 ,  C07D487/10 ,  A01N25/04

Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof, wherein: “Z”, R1 and R2 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：US10472347B2

公开(公告)日：2019-11-12

申请号：US15525788

申请日：2015-11-13

Applicant: Merck Sharp & Dohme Corp.

Inventor： Rongze Kuang ,  Pauline Ting ,  Amjad Ali ,  Heping Wu ,  Michael Berlin ,  Andrew Stamford ,  Hongwu Wang ,  Gang Zhou ,  David Kim ,  Qiaolin Deng ,  Yeon-Hee Lim ,  Younong Yu

IPC: A61K31/497 ,  C07D401/14 ,  C07D241/26 ,  C07D401/12 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04 ,  A61P25/16

Abstract: Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein “R1”, “RA-1”, “R2”, “R3”, and “Het” are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：US20180327385A1

公开(公告)日：2018-11-15

申请号：US15525788

申请日：2015-11-13

Applicant: Merck Sharp & Dohme Corp.

Inventor： Rongze KUANG ,  Pauline Ting ,  Amjad Ali ,  Heping Wu ,  Michael Berlin ,  Andrew Stamford ,  Hongwu Wang ,  Gang Zhou ,  David Kim ,  Qiaolin Deng ,  Yeon-Hee Lim ,  Younong Yu

IPC: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein “R1”, “RA-1”, “R2”, “R3”, and “Het” are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：US10011615B2

公开(公告)日：2018-07-03

申请号：US15423238

申请日：2017-02-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Xianhai Huang ,  Timothy J. Henderson ,  Jae-Hun Kim ,  Christopher Boyce ,  Pauline Ting ,  Junying Zheng ,  Edward Metzger ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Qiaolin Deng

IPC: A01N43/00 ,  A01N43/46 ,  C07D519/00 ,  C07D487/04

CPC classification number: C07D519/00 ,  C07D487/04

Abstract: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” 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：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：US10688082B2

公开(公告)日：2020-06-23

申请号：US15815212

申请日：2016-06-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Junying Zheng ,  Walter Won ,  Michael Berlin ,  Pauline Ting ,  Guoqing Li ,  Dong Xiao ,  Hongwu Wang ,  Robert Aslanian

IPC: A61K31/4162 ,  A61K31/519 ,  A61K31/497 ,  A61P25/00 ,  A01N43/80 ,  C07D487/04 ,  C07D487/10

Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof, wherein: “Z”, R1 and R2 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：US20170197991A1

公开(公告)日：2017-07-13

申请号：US15423238

申请日：2017-02-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Xianhai Huang ,  Timothy J. Henderson ,  Jae-Hun Kim ,  Christopher Boyce ,  Pauline Ting ,  Junying Zheng ,  Edward Metzger ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Qiaolin Deng

IPC: C07D519/00 ,  C07D487/04

CPC classification number: C07D519/00 ,  C07D487/04

Abstract: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” 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.