公开(公告)号：US10011615B2

公开(公告)日：2018-07-03

申请号：US15423238

申请日：2017-02-02

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： A01N43/00 ,  A01N43/46 ,  C07D519/00 ,  C07D487/04

CPC分类号： C07D519/00 ,  C07D487/04

摘要： 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：US09688654B2

公开(公告)日：2017-06-27

申请号：US14772525

申请日：2014-02-27

申请人： Merck Sharp & Dohme Corp.

发明人： Michael Miller ,  Kallol Basu ,  Duane DeMong ,  Jack Scott ,  Hong Liu ,  Xing Dai ,  Andrew Stamford ,  Marc Poirier ,  Paul Tempest

IPC分类号： C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D491/08 ,  C07D495/08 ,  C07D498/04 ,  C07D498/08

CPC分类号： C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D491/08 ,  C07D495/08 ,  C07D498/04 ,  C07D498/08

摘要： The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK2 kinase is involved.

公开(公告)号：US09676780B2

公开(公告)日：2017-06-13

申请号：US14655572

申请日：2013-12-20

申请人： 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

发明人： 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分类号： C07D487/04 ,  A61K31/519 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

CPC分类号： C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

摘要： 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：US20180325926A1

公开(公告)日：2018-11-15

申请号：US15775871

申请日：2016-11-11

申请人： Merck Sharp & Dohme Corp.

发明人： Thomas H. Graham ,  Tao Yu ,  Sherman T. Waddell ,  John A. McCauley ,  Andrew Stamford ,  Wengsheng Liu ,  Jay A. Grobler ,  Libo Xu

IPC分类号： A61K31/675 ,  A61P31/18

CPC分类号： A61K31/675 ,  A61K31/426 ,  A61K31/513 ,  A61K31/52 ,  A61K2300/00 ,  A61P31/18 ,  C07D491/20 ,  C07F9/6561

摘要： 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.

公开(公告)号：US20180028509A1

公开(公告)日：2018-02-01

申请号：US15725407

申请日：2017-10-05

申请人： MERCK SHARP & DOHME CORP.

发明人： Tao Yu ,  Yonglian Zhang ,  Sherman Tim Waddell ,  Andrew Stamford ,  John S. Wai ,  Paul J. Coleman ,  John M. Sanders ,  Ronald Ferguson ,  Thomas H. Graham ,  Hong Li

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

CPC分类号： A61K31/4375 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/505 ,  A61K31/513 ,  A61K31/52 ,  A61K31/635 ,  A61K31/675 ,  A61K45/06 ,  C07D455/00 ,  C07D455/02 ,  C07D455/04 ,  C07D471/14 ,  C07D491/147 ,  C07D519/00 ,  A61K2300/00

摘要： 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：US09861620B2

公开(公告)日：2018-01-09

申请号：US15025038

申请日：2014-09-26

申请人： MERCK SHARP & DOHME CORP.

发明人： Tao Yu ,  Yonglian Zhang ,  Sherman Tim Waddell ,  Andrew Stamford ,  John S. Wai ,  Paul J. Coleman ,  John M. Sanders ,  Ronald Ferguson ,  Thomas H. Graham ,  Hong Li

IPC分类号： A61K31/44 ,  C07D491/02 ,  C07D491/00 ,  C07D221/00 ,  C07D453/00 ,  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

CPC分类号： A61K31/4375 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/505 ,  A61K31/513 ,  A61K31/52 ,  A61K31/635 ,  A61K31/675 ,  A61K45/06 ,  C07D455/00 ,  C07D455/02 ,  C07D455/04 ,  C07D471/14 ,  C07D491/147 ,  C07D519/00 ,  A61K2300/00

摘要： 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：US20170197991A1

公开(公告)日：2017-07-13

申请号：US15423238

申请日：2017-02-02

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： C07D519/00 ,  C07D487/04

CPC分类号： C07D519/00 ,  C07D487/04

摘要： 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：US09511052B2

公开(公告)日：2016-12-06

申请号：US14415210

申请日：2013-07-15

申请人： Merck Sharp & Dohme Corp.

发明人： Timothy A. Cernak ,  Kevin D. Dykstra ,  Dong-Ming Shen ,  Kun Liu ,  Andrew Stamford ,  John Qiang Tan

IPC分类号： C07D231/56 ,  A61K31/416 ,  A61K45/06

CPC分类号： A61K31/416 ,  A61K45/06 ,  C07D231/56 ,  A61K2300/00

摘要： The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.

公开(公告)号：US09493440B2

公开(公告)日：2016-11-15

申请号：US14772295

申请日：2014-02-27

申请人： Merck Sharp & Dohme Corp.

发明人： Michael Miller ,  Kallol Basu ,  Duane DeMong ,  Jack Scott ,  Wei Li ,  Andrew Stamford ,  Marc Poirer ,  Paul Tempest

IPC分类号： C07D403/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08 ,  C07D498/10

CPC分类号： C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08 ,  C07D498/10

摘要： The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

公开(公告)号：US20160289207A1

公开(公告)日：2016-10-06

申请号：US15035255

申请日：2014-11-10

申请人： MERCK SHARP & DOHME CORP.

发明人： Duane DeMong ,  Michael Miller ,  Hong Liu ,  Xing Dai ,  Thomas Greshock ,  Andrew Stamford ,  Ravi Nargund

IPC分类号： C07D401/04 ,  C07D401/14

CPC分类号： C07D401/04 ,  C07D231/56 ,  C07D401/14

摘要： The present invention is directed to substituted indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

摘要翻译： 本发明涉及取代的吲唑化合物，其是LRRK2激酶的有效抑制剂并且可用于治疗或预防涉及LRRK2激酶的疾病，例如帕金森病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及LRRK-2激酶的疾病中的用途。