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.

公开(公告)号：US20110224136A1

公开(公告)日：2011-09-15

申请号：US13129830

申请日：2009-11-17

申请人： Pauline C. Ting ,  Robert Aslanian ,  Mary Ann Caplen ,  Jianhua Cao ,  David Kim ,  Hyunjin Kim ,  Rongze Kuang ,  Joe F. Lee ,  John Schwerdt ,  Heping Wu ,  Gang Zhou ,  Nicolas Zorn

发明人： Pauline C. Ting ,  Robert Aslanian ,  Mary Ann Caplen ,  Jianhua Cao ,  David Kim ,  Hyunjin Kim ,  Rongze Kuang ,  Joe F. Lee ,  John Schwerdt ,  Heping Wu ,  Gang Zhou ,  Nicolas Zorn

IPC分类号： A61K38/28 ,  C07D409/14 ,  C07D413/14 ,  C07D401/14 ,  C07D211/32 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.

摘要翻译： 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖症或肥胖相关障碍的化合物的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本发明的说明性化合物如下所示。

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：US20170044183A1

公开(公告)日：2017-02-16

申请号：US15305421

申请日：2015-04-21

申请人： Yeon-Hee Lim ,  Zhuyan Guo ,  Amjad Ali ,  Scott D. Edmondson ,  Weiguo Liu ,  Giocanda V. Gallo-Etienne ,  Heping Wu ,  Ying-Duo Gao ,  Andrew W. Stamford ,  Younong Yu ,  Nancy J. Kevin ,  Rajan Anand ,  Deyou Sha ,  Santhosh F. Neelamkavil ,  Zahid Hussain ,  Puneet Kumar ,  Remond Moningka ,  Joseph L. Duffy ,  Jiayi Xu ,  Yu Jiang ,  Anjan Chakrabarti ,  Hiroki Sone

发明人： Yeon-Hee Lim ,  Zhuyan Guo ,  Amjad Ali ,  Scott D. Edmondson ,  Weiguo Liu ,  Giocanda V. Gallo-Etienne ,  Heping Wu ,  Ying-Duo Gao ,  Andrew W. Stamford ,  Younong Yu ,  Nancy J. Kevin ,  Rajan Anand ,  Deyou Sha ,  Santhosh F. Neelamkavil ,  Zahid Hussain ,  Puneet Kumar ,  Remond Moningka ,  Joseph L. Duffy ,  Jiayi Xu ,  Yu Jiang ,  Anjan Chakrabarti ,  Hiroki Sone

IPC分类号： C07D498/20 ,  C07F9/6561 ,  C07D487/10 ,  C07D498/10 ,  C07D471/10

CPC分类号： C07D498/20 ,  C07D471/10 ,  C07D487/10 ,  C07D498/10 ,  C07F9/6561

摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

摘要翻译： 本发明提供式（I）的化合物和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维变化的方法。 该化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。

公开(公告)号：US08232274B2

公开(公告)日：2012-07-31

申请号：US12046755

申请日：2008-03-12

申请人： Pauline C. Ting ,  Robert G. Aslanian ,  Jianhua Cao ,  David Won-Shik Kim ,  Rongze Kuang ,  Gang Zhou ,  Robert Jason Herr ,  Andrew John Zych ,  Jinhai Yang ,  Heping Wu ,  Nicolas Zorn

发明人： Pauline C. Ting ,  Robert G. Aslanian ,  Jianhua Cao ,  David Won-Shik Kim ,  Rongze Kuang ,  Gang Zhou ,  Robert Jason Herr ,  Andrew John Zych ,  Jinhai Yang ,  Heping Wu ,  Nicolas Zorn

IPC分类号： A61K31/501 ,  A61K31/5377 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  A61P31/00

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/08 ,  C07D515/22

摘要： Disclosed is a set of compounds useful as glucan synthase inhibitors having the generic structure of Formula I: wherein the various moieties A, D, R6, etc., are as defined in the specification. These compounds are useful in treating or preventing fungal infections in a patient.

摘要翻译： 公开了一组可用作具有式I的通式结构的葡聚糖合酶抑制剂的化合物：其中各个部分A，D，R 6等如说明书中所定义。 这些化合物可用于治疗或预防患者的真菌感染。

公开(公告)号：US20090170861A1

公开(公告)日：2009-07-02

申请号：US12046755

申请日：2008-03-12

申请人： Pauline C. Ting ,  Robert G. Aslanian ,  Jianhua Cao ,  David Won-Shik Kim ,  Rongze Kuang ,  Gang Zhou ,  Robert Jason Herr ,  Andrew John Zych ,  Jinhai Yang ,  Heping Wu ,  Nicolas Zorn

发明人： Pauline C. Ting ,  Robert G. Aslanian ,  Jianhua Cao ,  David Won-Shik Kim ,  Rongze Kuang ,  Gang Zhou ,  Robert Jason Herr ,  Andrew John Zych ,  Jinhai Yang ,  Heping Wu ,  Nicolas Zorn

IPC分类号： A61K31/501 ,  C07D403/04 ,  A01N43/58 ,  A01P3/00 ,  A61P31/10

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/08 ,  C07D515/22

摘要： In its many embodiments, the present invention provides -substituted pyridazinone compounds as glucan synthase inhibitors, methods of preparing such compounds, pharmaceutical including one or more of such compounds, methods of preparing pharmaceutical formulations including one or more such compounds or one or more such compounds along with other antifungal agents, and methods of treatment, prevention, inhibition, or amelioration of one or more fungal infections associated with glucan synthase using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了作为葡聚糖合酶抑制剂的取代的哒嗪酮化合物，制备这些化合物的方法，包括一种或多种这些化合物的药物，制备药物制剂的方法，包括一种或多种这样的化合物或一种或多种这样的化合物 以及其他抗真菌剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与葡聚糖合酶相关的一种或多种真菌感染的方法。

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：US20110224193A1

公开(公告)日：2011-09-15

申请号：US13129821

申请日：2009-11-17

申请人： Pauline C. Ting ,  Robert Aslanian ,  Jianhua Cao ,  Mary Ann Caplen ,  Tin-Yau Chan ,  Hyunjin Kim ,  Jae-Hun Kim ,  Rongze Kuang ,  Joe F. Lee ,  Heping Wu

发明人： Pauline C. Ting ,  Robert Aslanian ,  Jianhua Cao ,  Mary Ann Caplen ,  Tin-Yau Chan ,  Hyunjin Kim ,  Jae-Hun Kim ,  Rongze Kuang ,  Joe F. Lee ,  Heping Wu

IPC分类号： A61K31/5513 ,  C07D413/14 ,  A61K31/4545 ,  A61K31/497 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P3/08

CPC分类号： C07D413/12 ,  A61K31/422 ,  A61K31/427 ,  C07D213/74 ,  C07D401/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D493/10

摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown with this abstract.

摘要翻译： 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖症或肥胖相关障碍的化合物的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本摘要显示了本发明的说明性化合物。

公开(公告)号：US20110224137A1

公开(公告)日：2011-09-15

申请号：US13129843

申请日：2009-11-17

申请人： Pauline C. Ting ,  Robert Aslanian ,  Mary Ann Caplen ,  Jianhua Cao ,  Tin-Yau Chan ,  David Kim ,  Hyunjin Kim ,  Jae-Hun Kim ,  Rongze Kuang ,  Joe F. Lee ,  John Schwerdt ,  Heping Wu ,  Nicolas Zorn

发明人： Pauline C. Ting ,  Robert Aslanian ,  Mary Ann Caplen ,  Jianhua Cao ,  Tin-Yau Chan ,  David Kim ,  Hyunjin Kim ,  Jae-Hun Kim ,  Rongze Kuang ,  Joe F. Lee ,  John Schwerdt ,  Heping Wu ,  Nicolas Zorn

IPC分类号： A61K38/28 ,  C07D409/14 ,  C07D243/08 ,  C07D401/14 ,  C07D221/00 ,  C07D211/06 ,  A61K31/497 ,  A61K31/551 ,  A61K31/4545 ,  A61K31/438 ,  A61K31/454 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D413/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04

摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).

摘要翻译： 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖症或肥胖相关障碍的化合物的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本发明的说明性化合物如下所示：式（I）。