公开(公告)号：US20140088124A1

公开(公告)日：2014-03-27

申请号：US14123246

申请日：2012-06-01

Applicant: Robert J. DeVita ,  QingMei Hong ,  Zhong Lai ,  Kevin D. Dykstra ,  Yang Yu ,  Jian Liu ,  Donald M. Sperbeck ,  Tianying Jian ,  Deodial Guiadeen ,  Ginger Xu-qiang Yang ,  Zhicai Wu ,  Shuwen He ,  Pauline C. Ting ,  Robert Aslanian ,  Jeffrey T. Kuethe ,  James Balkovec ,  Rongze Kuang ,  Gang Zhou ,  Heping Wu

Inventor： Robert J. DeVita ,  QingMei Hong ,  Zhong Lai ,  Kevin D. Dykstra ,  Yang Yu ,  Jian Liu ,  Donald M. Sperbeck ,  Tianying Jian ,  Deodial Guiadeen ,  Ginger Xu-qiang Yang ,  Zhicai Wu ,  Shuwen He ,  Pauline C. Ting ,  Robert Aslanian ,  Jeffrey T. Kuethe ,  James Balkovec ,  Rongze Kuang ,  Gang Zhou ,  Heping Wu

IPC: C07D401/14 ,  C07D417/14 ,  C07D493/04 ,  C07D471/04

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04

Abstract: Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

Abstract translation: 本文描述的是式（I）的化合物。式I化合物作为DGAT1抑制剂，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的补救剂。

公开(公告)号：US20230416227A1

公开(公告)日：2023-12-28

申请号：US18043357

申请日：2021-09-09

Applicant: Merck Sharp & Dohme LLC ,  Anthony Ken OGAWA ,  Christopher J. SINZ ,  Jacqueline D. HICKS ,  Alan C. CHENG ,  Song YANG ,  Jianming BAO ,  Donna A. A. W. HAYES ,  Simon B. LANG ,  Maoqun TIAN ,  Salman JABRI ,  Galen Paul SHEARN-NANCE ,  Rongze KUANG ,  Zhiqiang ZHAO ,  Zhicai WU

Inventor： Anthony Ken Ogawa ,  Christopher J. Sinz ,  Jacqueline D. Hicks ,  Alan C. Cheng ,  Song Yang ,  Jianming Bao ,  Donna A. A. W. Hayes ,  Simon B. Lang ,  Maoqun Tian ,  Salman Jabri ,  Galen Paul Shearn-Nance ,  Rongze Kuang ,  Zhiqiang Zhao ,  Zhicai Wu

IPC: C07D401/14 ,  A61K45/06 ,  A61P9/10

CPC classification number: C07D401/14 ,  A61P9/10 ,  A61K45/06

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 one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

公开(公告)号：US11046714B2

公开(公告)日：2021-06-29

申请号：US14914843

申请日：2014-08-25

Applicant: 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

Inventor： 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: C07D519/00 ,  C07D491/147

Abstract: 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：US08324213B2

公开(公告)日：2012-12-04

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 ,  Youngong Yu ,  Jianhua Chao ,  Walter S. Won ,  Ashwin U. Rao ,  Rongze Kuang ,  Pauline C. Ting ,  Xianhai Huang ,  Ning Shao ,  Anandan 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 ,  Youngong Yu ,  Jianhua Chao ,  Walter S. Won ,  Ashwin U. Rao ,  Rongze Kuang ,  Pauline C. Ting ,  Xianhai Huang ,  Ning Shao ,  Anandan Palani ,  Michael Y. Berlin ,  Robert G. Aslanian

IPC: A61K31/501 ,  A61K31/497 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/423 ,  C07D235/02 ,  C07D405/02 ,  C07D409/02 ,  C07D413/02 ,  C07D263/52

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：US20110224136A1

公开(公告)日：2011-09-15

申请号：US13129830

申请日：2009-11-17

Applicant: 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

Inventor： 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: 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 classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

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。

公开(公告)号：US20060106062A1

公开(公告)日：2006-05-18

申请号：US11130359

申请日：2005-05-16

Applicant: Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John Schwerdt ,  Pauline Ting ,  Shing-Chun Wong ,  Li Xiao

Inventor： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John Schwerdt ,  Pauline Ting ,  Shing-Chun Wong ,  Li Xiao

IPC: A61K31/4709 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

CPC classification number: C07D405/14 ,  C07D401/04 ,  C07D405/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH2F, —CHF2, —CF3, —C(O)alkyl or —C(O)NR18R19; R3 and R4H, alkyl, hydroxyalkyl or —C(O)Oalkyl; R5 and R6 are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, —CH2F, —CHF2, —CF3, —C(O)OH or —C(O)Oalkyl; R7 is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or —CH2—C(O)—O-alkyl; and R8 comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.

Abstract translation: 本发明要求具有下式的化合物其中是5元杂芳基; X是S或O; R 1是H，烷基，环烷基，环烷基烷基 - ，-CH 2 F，-CHF 2，-CF 3， -C（O）烷基或-C（O）NR 18 R 19; R 3和R 4 H，烷基，羟烷基或-C（O）O烷基; R 5和R 6是H，烷基，羟基烷基，烷氧基烷基，巯基烷基，-CH 2 F 2，-CHF 2， -CF 3，-C（O）OH或-C（O）O烷基; R 7是H，烷基，烯基，羟基烷基，环烷基，烷氧基烷基，氨基烷基，（R 17 - 苯基）烷基或-CH 2 - C（O）-O-烷基; 和R 8包括烷基，杂芳基，苯基或环烷基，或杂环烷基，全部被取代，或环烷基 - 或杂环烷基取代的酰胺; 或R 7和R 8和它们所连接的氮一起形成任选取代的环; 其余变量如本说明书中所定义。 还要求保护的是药物组合物，化合物作为PDE4抑制剂的用途，以及与其它活性物质的组合。

公开(公告)号：US06420401B1

公开(公告)日：2002-07-16

申请号：US08916693

申请日：1997-08-22

Applicant: William C. Groutas ,  Rongze Kuang

Inventor： William C. Groutas ,  Rongze Kuang

IPC: A61K3141

CPC classification number: C07D285/10 ,  C07K5/06139

Abstract: Substituted derivatives of 1,2,5-thiadiazolidin-3-one 1,1-dioxides, oligomers containing them, and methods of using them.

Abstract translation: 1,2,5-噻二唑烷-3-酮1,1-二氧化物的取代衍生物，含有它们的低聚物及其使用方法。

公开(公告)号：US20160214997A1

公开(公告)日：2016-07-28

申请号：US14914843

申请日：2014-08-25

Applicant: 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.

Inventor： 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: C07D519/00 ,  C07D491/147

CPC classification number: C07D519/00 ,  C07D491/147

Abstract: 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.

Abstract translation: 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

Applicant: 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

Inventor： 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: A61K31/5513 ,  C07D413/14 ,  A61K31/4545 ,  A61K31/497 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P3/08

CPC classification number: 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

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 with this abstract.

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

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: 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 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: formula (I).

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：式（I）。