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公开(公告)号:US09745282B2
公开(公告)日:2017-08-29
申请号:US15197957
申请日:2016-06-30
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.
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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。
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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。
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公开(公告)号:US20160304486A1
公开(公告)日:2016-10-20
申请号:US15197957
申请日:2016-06-30
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。
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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.
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6.
公开(公告)号:US20170197991A1
公开(公告)日:2017-07-13
申请号:US15423238
申请日:2017-02-02
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.
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公开(公告)号:US10822338B2
公开(公告)日:2020-11-03
申请号:US15738178
申请日:2016-07-05
发明人: Amjad Ali , Xianhai Huang , Yeon-Hee Lim , Rongze Kuang , Heping Wu , Rajan Anand , Younong Yu , Edward Metzger , Michael Man-Chu Lo , Pauline C. Ting , Andrew W. Stamford , Paul Tempest
IPC分类号: C07D487/04 , C07D491/153
摘要: 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. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
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公开(公告)号:US20180362530A1
公开(公告)日:2018-12-20
申请号:US15738178
申请日:2016-07-05
发明人: Amjad Ali , Xianhai Huang , Yeon-Hee Lim , Rongze Kuang , Heping Wu , Rajan Anand , Younong Yu , Edward Metzger , Michael Man-Chu LO , Pauline C. Ting , Andrew W. Stamford , Paul Tempest
IPC分类号: C07D487/04 , C07D491/153
摘要: 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. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
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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。
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10.
公开(公告)号:US10011615B2
公开(公告)日:2018-07-03
申请号:US15423238
申请日:2017-02-02
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.
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