公开(公告)号：US20150225365A1

公开(公告)日：2015-08-13

申请号：US14433441

申请日：2013-10-02

申请人： Amjad ALI ,  Man-Chu Michael ,  Edward METZGER ,  Lina YIN ,  Rolf HARTMANN ,  Qingzhong HU ,  Ralf HEIM ,  Christina ZIMMER ,  MERCK SHARP & DOHME CORP. ,  ELEXOPHARM GMBH

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Edward Metzger ,  Lina Yin ,  Rolf Hartmann ,  Qingzhong Hu ,  Ralf Heim ,  Christina Zimmer

IPC分类号： C07D401/04 ,  C07D409/14

CPC分类号： C07D401/04 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K45/06 ,  C07D409/14 ,  A61K2300/00

摘要： This invention relates to indo line compounds of the structural formula I, or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

摘要翻译： 本发明涉及结构式I的吲哚类化合物或其药学上可接受的盐，其中变量在本文中定义。 本发明化合物选择性地抑制醛固酮合酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗改善或预防可通过抑制醛固酮合酶治疗的病症的方法。

公开(公告)号：US09550750B2

公开(公告)日：2017-01-24

申请号：US14433441

申请日：2013-10-02

申请人： Merck Sharp & Dohme Corp. ,  ElexoPharm GmbH ,  Amjad Ali ,  Michael Man-Chu Lo ,  Edward Metzger ,  Lina Yin ,  Rolf Hartmann ,  Qingzhong Hu ,  Ralf Heim ,  Christina Zimmer

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Edward Metzger ,  Lina Yin ,  Rolf Hartmann ,  Qingzhong Hu ,  Ralf Heim ,  Christina Zimmer

IPC分类号： C07D401/04 ,  A61K31/4439 ,  A61K45/06 ,  A61K31/4709 ,  C07D409/14

CPC分类号： C07D401/04 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K45/06 ,  C07D409/14 ,  A61K2300/00

摘要： This invention relates to indo line compounds of the structural formula I, or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

摘要翻译： 本发明涉及结构式I的吲哚类化合物或其药学上可接受的盐，其中变量在本文中定义。 本发明化合物选择性地抑制醛固酮合酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗改善或预防可通过抑制醛固酮合酶治疗的病症的方法。

公开(公告)号：US09073929B2

公开(公告)日：2015-07-07

申请号：US14112945

申请日：2012-04-20

申请人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

发明人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/41 ,  A61K45/06

CPC分类号： C07D487/04 ,  A61K31/41 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

摘要： This invention relates to tricyclic triazole analogs of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.

摘要翻译： 本发明涉及式I的三环三唑类似物或其药学上可接受的盐，其中该变量在本文中定义。 本发明化合物选择性地抑制醛固酮合成酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及用于治疗，改善或预防可通过抑制醛固酮合成酶治疗的病症的方法。

公开(公告)号：US20140045819A1

公开(公告)日：2014-02-13

申请号：US14112945

申请日：2012-04-20

申请人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

发明人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

IPC分类号： C07D487/04 ,  C07D471/04

CPC分类号： C07D487/04 ,  A61K31/41 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

摘要： This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.

摘要翻译： 本发明涉及式I的三环三唑类似物或其药学上可接受的盐，其中该变量在本文中定义。 本发明化合物选择性地抑制醛固酮合成酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及用于治疗，改善或预防可通过抑制醛固酮合成酶治疗的病症的方法。

公开(公告)号：US20160214997A1

公开(公告)日：2016-07-28

申请号：US14914843

申请日：2014-08-25

申请人： Amjad ALI ,  Gioconda V. GALLO ,  Timothy J. HENDERSON ,  Rongze KUANG ,  Yeon-Hee LIM ,  Michael Man-Chu LO ,  Edward METZGER ,  Manuel de Lera RUIZ ,  Andrew STAMFORD ,  Paul TEMPEST ,  Brent WHITEHEAD ,  Heping WU ,  MERCK SHARP & DOHME CORP.

发明人： Ali Amjad ,  Gioconda V. Gallo ,  Timothy J. Henderson ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Edward Metzger ,  Manuel de Lera Ruiz ,  Andrew Stamford ,  Paul Tempest ,  Brent Whitehead ,  Heping Wu

IPC分类号： C07D519/00 ,  C07D491/147

CPC分类号： C07D519/00 ,  C07D491/147

摘要： The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

摘要翻译： 本发明涉及作为A2A受体拮抗剂的2,2-二氟二氧代己基化合物。 本发明还涉及本文所述的2,2-二氟二氧代环戊基化合物在涉及A2A受体的神经障碍和疾病的潜在治疗或预防中的用途。 本发明还涉及包含这些化合物的药物组合物以及这些药物组合物用于预防或治疗其中涉及A2A受体的疾病的用途。

公开(公告)号：US09745282B2

公开(公告)日：2017-08-29

申请号：US15197957

申请日：2016-06-30

申请人： Merck Sharp & Dohme Corp. ,  ElexoPharm GmbH

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Edward Metzger ,  Lina Yin ,  Rolf Hartmann ,  Qingzhong Hu ,  Ralf Heim ,  Christina Zimmer

IPC分类号： C07D401/04 ,  A61K31/4709 ,  A61K31/4439 ,  A61K45/06 ,  C07D409/14 ,  A61K31/4725

CPC分类号： C07D401/04 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K45/06 ,  C07D409/14 ,  A61K2300/00

摘要： This invention relates to indoline compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

公开(公告)号：US20160304486A1

公开(公告)日：2016-10-20

申请号：US15197957

申请日：2016-06-30

申请人： Merck Sharp & Dohme Corp. ,  ElexoPharm GmbH

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Edward Metzger ,  Lina Yin ,  Rolf Hartmann ,  Qingzhong Hu ,  Ralf Heim ,  Christina Zimmer

IPC分类号： C07D401/04 ,  A61K31/4439 ,  C07D409/14 ,  A61K31/4725

CPC分类号： C07D401/04 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K45/06 ,  C07D409/14 ,  A61K2300/00

摘要： This invention relates to indoline compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

摘要翻译： 或其药学上可接受的盐，其中变量在本文中定义。 本发明化合物选择性地抑制醛固酮合酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗，改善或预防可通过抑制醛固酮合酶治疗的病症的方法。

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：US20160194330A1

公开(公告)日：2016-07-07

申请号：US14655572

申请日：2013-12-20

申请人： 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 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.

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 ,  C07D487/18 ,  C07D487/08 ,  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.

摘要翻译： 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：US11046714B2

公开(公告)日：2021-06-29

申请号：US14914843

申请日：2014-08-25

申请人： Merck Sharp & Dohme Corp. ,  Ali Amjad ,  Gioconda V. Gallo ,  Timothy J. Henderson ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Edward Metzger ,  Manuel de Lera Ruiz ,  Andrew Stamford ,  Paul Tempest ,  Brent Whitehead ,  Heping Wu

发明人： Ali Amjad ,  Gioconda V. Gallo ,  Timothy J. Henderson ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Edward Metzger ,  Manuel de Lera Ruiz ,  Andrew Stamford ,  Paul Tempest ,  Brent Whitehead ,  Heping Wu

IPC分类号： C07D519/00 ,  C07D491/147

摘要： The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.