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：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：US08232274B2

公开(公告)日：2012-07-31

申请号：US12046755

申请日：2008-03-12

Applicant: 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

Inventor： 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: A61K31/501 ,  A61K31/5377 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  A61P31/00

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/08 ,  C07D515/22

Abstract: 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.

Abstract translation: 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：US20110251207A1

公开(公告)日：2011-10-13

申请号：US13122679

申请日：2009-10-06

Applicant: Kevin D. McCormick ,  Li Dong ,  Christopher W. Boyce ,  Manuel de Lera Ruiz ,  Salem Fevrier ,  Jie Wu ,  Junying Zheng ,  Younong Yu ,  Jianhua Chao ,  Walter S. Won ,  Ashwin U. Rao ,  Rongze Kuang ,  Pauline C. Ting ,  Xianhai Huang ,  Ning Shao ,  Adandan Palani ,  Michael Y. Berlin ,  Robert G. Aslanian

Inventor： Kevin D. McCormick ,  Li Dong ,  Christopher W. Boyce ,  Manuel de Lera Ruiz ,  Salem Fevrier ,  Jie Wu ,  Junying Zheng ,  Younong Yu ,  Jianhua Chao ,  Walter S. Won ,  Ashwin U. Rao ,  Rongze Kuang ,  Pauline C. Ting ,  Xianhai Huang ,  Ning Shao ,  Adandan Palani ,  Michael Y. Berlin ,  Robert G. Aslanian

IPC: A61K31/501 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/497 ,  C07D263/52 ,  A61K31/423 ,  C07D235/02 ,  A61K31/4184 ,  C07D405/10 ,  C07D409/10 ,  A61K31/422 ,  C07D403/10 ,  A61P27/06 ,  A61P25/22 ,  A61P21/02 ,  A61P9/00 ,  A61P25/18 ,  A61P25/06 ,  A61P25/28 ,  A61P3/10 ,  A61P11/02 ,  C07D413/10

CPC classification number: A61K31/5377 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506 ,  A61K31/537 ,  C07D235/02 ,  C07D263/52 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/10 ,  C07D519/00

Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的作为α2C肾上腺素能受体激动剂的调节剂的生物二螺吡喃恶唑啉类似物，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法 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α2C肾上腺素能受体相关的一种或多种病症的方法。

公开(公告)号：US20090170861A1

公开(公告)日：2009-07-02

申请号：US12046755

申请日：2008-03-12

Applicant: 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

Inventor： 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: A61K31/501 ,  C07D403/04 ,  A01N43/58 ,  A01P3/00 ,  A61P31/10

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/08 ,  C07D515/22

Abstract: 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.

Abstract translation: 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：US20080108818A1

公开(公告)日：2008-05-08

申请号：US11891351

申请日：2007-08-10

Applicant: Xiaoming Chen ,  Xiao Chen ,  Jianguo Yin ,  Xiaoyong Fu ,  David Blythin ,  Rongze Kuang ,  Ho-Jane Shue ,  Scott Trzaska ,  Chee-Wah Tang ,  Vincenzo Liotta ,  Zaher Shabani

Inventor： Xiaoming Chen ,  Xiao Chen ,  Jianguo Yin ,  Xiaoyong Fu ,  David Blythin ,  Rongze Kuang ,  Ho-Jane Shue ,  Scott Trzaska ,  Chee-Wah Tang ,  Vincenzo Liotta ,  Zaher Shabani

IPC: C07D413/02

CPC classification number: C07D413/04

Abstract: Disclosed are maleate, tosylate, fumarate, and oxalate salts of the compound 5-(1(S)-Amino-2-Hydroxyethyl)-N-[(2,4-Difluorophenyl)-Methyl]-2-[8-Methoxy-2-(Trifluoromethyl)-5-Quinoline]-4-Oxazolecarboxamide, represented by Formula I, and methods of preparing the same.

Abstract translation: 公开了化合物5-（1（S） - 氨基-2-羟乙基）-N - [（2,4-二氟苯基） - 甲基] -2- [8-甲氧基 - 由式I表示的2-（三氟甲基）-5-喹啉啉-4-氧杂二甲酰胺及其制备方法。

公开(公告)号：US20230167085A1

公开(公告)日：2023-06-01

申请号：US17920943

申请日：2021-05-07

Applicant: Wei LAN ,  John S. Debenham ,  Amjad Ali ,  Ying-Duo Gao ,  Lan Wei ,  Dexi Yang ,  Rongze Kuang ,  Alan Hruza ,  Peter Nizner ,  Daniel A. Tatosian ,  Merck Sharp & Dohme LLC

Inventor： Jacqueline D. HICKS ,  John S. Debenham ,  Amjad Ali ,  Ying-Duo Gao ,  Lan Wei ,  Dexi Yang ,  Rongze Kuang ,  Alan Hruza ,  Peter Nizner ,  Daniel A. Tatosian

IPC: C07D401/14 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D417/14

Abstract: 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 XI activation inhibitors.

公开(公告)号：US20210395255A1

公开(公告)日：2021-12-23

申请号：US17292511

申请日：2019-11-15

Applicant: Zachary G. BRILL ,  Amjad ALI ,  Jared CUMMING ,  Duane DEMONG ,  Qiaolin DENG ,  Thomas H. GRAHAM ,  Rongze KUANG ,  Yeon-Hee LIM ,  Christopher W. PLUMMER ,  Jenny Lorena RICO DUQUE ,  Huijun WANG ,  Yonglian ZHANG ,  Kake ZHAO ,  Merck Sharp & Dohme Corp.

Inventor： Zachary G. Brill ,  Amjad Ali ,  Jared Cumming ,  Duane DeMong ,  Qiaolin Deng ,  Thomas H. Graham ,  Rongze Kuang ,  Yeon-Hee Lim ,  Christopher W. Plummer ,  Jenny Lorena Rico Duque ,  Huijun Wang ,  Yonglian Zhang ,  Kake Zhao

IPC: C07D487/04 ,  C07K16/28

Abstract: In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): or and pharmaceutically acceptable salts thereof, wherein, R1, R2, and R3 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US20150361098A1

公开(公告)日：2015-12-17

申请号：US14655648

申请日：2013-12-20

Applicant: 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 ,  Gloconda GALLO ,  Walter WON ,  Heping WU ,  MERCH 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 (structurally represented): 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.

Abstract translation: 公开了式G1（结构表示）的化合物：其中“RG3”“Rd1”至“Rd4”，“n”，“m”，“p”，“W”，“X”，“Y”和“Z “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：US08716312B2

公开(公告)日：2014-05-06

申请号：US13129843

申请日：2009-11-17

Applicant: 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

Inventor： 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: A61P3/00 ,  A61P9/00 ,  A61K31/445 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D413/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04

Abstract: 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:

Abstract translation: 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：