公开(公告)号：US20110257156A1

公开(公告)日：2011-10-20

申请号：US13126056

申请日：2009-11-05

申请人： Zhaoning Zhu ,  William J. Greenlee ,  David James Cole ,  Dmitri A. Pissarnitski ,  Gioconda V. Gallo ,  Hongmei Li ,  Hubert B. Josien ,  Jun Qin ,  Chad E. Knutson ,  Mihirbaran Mandal ,  Monica L. Vicarel ,  Murali Rajagopalan ,  Pawan Kumar Dhondi ,  Ruo Xu ,  Zhong-Yue Sun ,  Thomas A. Bara ,  Xianhai Huang ,  Xiaohong Zhu ,  Zhiqiang Zhao ,  John W. Clader ,  Anandan Palani ,  Theodros Asberom ,  Troy McCracken ,  Chad E. Bennett

发明人： Zhaoning Zhu ,  William J. Greenlee ,  David James Cole ,  Dmitri A. Pissarnitski ,  Gioconda V. Gallo ,  Hongmei Li ,  Hubert B. Josien ,  Jun Qin ,  Chad E. Knutson ,  Mihirbaran Mandal ,  Monica L. Vicarel ,  Murali Rajagopalan ,  Pawan Kumar Dhondi ,  Ruo Xu ,  Zhong-Yue Sun ,  Thomas A. Bara ,  Xianhai Huang ,  Xiaohong Zhu ,  Zhiqiang Zhao ,  John W. Clader ,  Anandan Palani ,  Theodros Asberom ,  Troy McCracken ,  Chad E. Bennett

IPC分类号： A61K31/55 ,  A61K31/5383 ,  A61K31/5377 ,  A61K31/501 ,  A61K31/497 ,  A61K31/506 ,  A61K31/438 ,  A61K31/437 ,  C07D413/10 ,  C07D498/20 ,  C07D498/04 ,  A61P25/00 ,  A61P25/28 ,  A61K31/4245 ,  A61K31/5386

CPC分类号： C07D471/04 ,  C07D413/10 ,  C07D498/04 ,  C07D498/20 ,  C07F7/0812

摘要： In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, 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 diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了新颖的杂环化合物作为γ-分泌酶的调节剂，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，以及治疗方法， 使用这种化合物或药物组合物预防，抑制或改善与中枢神经系统相关的一种或多种疾病。

公开(公告)号：US20110082153A1

公开(公告)日：2011-04-07

申请号：US12673858

申请日：2008-09-04

申请人： Robert G. Aslanian ,  Xianhai Huang ,  Anandan Palani ,  JUn Qin ,  Wei Zhou ,  Xiaohong Zhu ,  Robert Mazzola ,  Pawan Dhondi ,  William J. Greenlee

发明人： Robert G. Aslanian ,  Xianhai Huang ,  Anandan Palani ,  JUn Qin ,  Wei Zhou ,  Xiaohong Zhu ,  Robert Mazzola ,  Pawan Dhondi ,  William J. Greenlee

IPC分类号： A61K31/501 ,  C07D403/12 ,  C07D237/14 ,  A61K31/50 ,  C07D401/12 ,  A61K31/4439 ,  C07D403/14 ,  A61P25/28 ,  A61P27/06 ,  A61P9/00 ,  A61P29/00

CPC分类号： C07D403/12 ,  C07D237/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).

摘要翻译： 本发明提供了作为γ分泌酶调节剂的新型化合物。 化合物具有式（I）。 还公开了使用式（I）化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。

公开(公告)号：US20110015190A1

公开(公告)日：2011-01-20

申请号：US12746041

申请日：2008-12-04

申请人： Xianhai Huang ,  Anandan Palani ,  Jun Qin ,  Robert Aslanian ,  Zhaoning Zhu ,  William Greenlee ,  Hubert Josien ,  Wei Zhou ,  Xiaohong Zhou ,  Chad E. Bennett ,  Dmitri Pissarnitski ,  Mihirbaran Mandal ,  Pawan Dhondi ,  Troy McCracken ,  Thomas Bara ,  Zhiqiang Zhao ,  Duane Burnett ,  John Clader

发明人： Xianhai Huang ,  Anandan Palani ,  Jun Qin ,  Robert Aslanian ,  Zhaoning Zhu ,  William Greenlee ,  Hubert Josien ,  Wei Zhou ,  Xiaohong Zhou ,  Chad E. Bennett ,  Dmitri Pissarnitski ,  Mihirbaran Mandal ,  Pawan Dhondi ,  Troy McCracken ,  Thomas Bara ,  Zhiqiang Zhao ,  Duane Burnett ,  John Clader

IPC分类号： A61K31/5383 ,  C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C07D498/04 ,  C07D403/02 ,  A61K31/4178 ,  A61P25/28

CPC分类号： C07D471/04 ,  C07D403/10 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).

摘要翻译： 本发明提供了作为γ分泌酶调节剂的新型化合物。 所述化合物具有式（I），其中R 2是式（II）的稠合双环。 还公开了使用式（I）的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。

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：US20230322785A1

公开(公告)日：2023-10-12

申请号：US18015387

申请日：2022-07-21

申请人： Christopher W. BOYCE ,  Thomas H. GRAHAM ,  Andrew J. HOOVER ,  Xianhai HUANG ,  Rognze KUANG ,  Jae-Hun KIM ,  Joseph M. KELLY ,  Michael Man-Chu LO ,  Jing SU ,  Dong XIAO ,  Xiaohong ZHU ,  Merck Sharp & Dohme LLC

发明人： Amjad Ali ,  Christopher W. Boyce ,  Jared N. Cumming ,  Duane DeMong ,  Thomas H. Graham ,  Subrahmanyam Gudipati ,  Andrew J. Hoover ,  Xianhai Huang ,  Rongze Kuang ,  Jae-Hun Kim ,  Joseph M. Kelly ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Jesus Moreno ,  Jing Su ,  Heping Wu ,  Dong Xiao ,  Younong Yu ,  Xiaohong Zhu

IPC分类号： C07D487/04 ,  C07K16/28 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61P35/00 ,  C07K16/2896

摘要： The present invention provides compounds of the structural Formula (I) and pharmaceutically acceptable salts thereof, wherein, 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 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

申请人： 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 ,  Gloconda GALLO ,  Walter WON ,  Heping WU ,  MERCH SHARP & DOHME CORP.

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 (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.

摘要翻译： 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：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：US20110251207A1

公开(公告)日：2011-10-13

申请号：US13122679

申请日：2009-10-06

申请人： 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

发明人： 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分类号： 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分类号： 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

摘要： 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.

摘要翻译： 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：US20230008022A1

公开(公告)日：2023-01-12

申请号：US17295497

申请日：2019-11-25

申请人： Dane CLAUSEN ,  Ping CHEN ,  Xavier FRADERA ,  Liangqin GUO ,  Yongxin HAN ,  Shuwen HE ,  Xianhai HUANG ,  Joseph KOZLOWSKI ,  Guoqing LI ,  Theodore A. MARTINOT ,  Alexander PASTERNAK ,  Andreas VERRAS ,  Li XIAO ,  Wensheng YU ,  Rui ZHANG ,  Merck Sharp & Dohme Corp.

发明人： Dane Clausen ,  Ping Chen ,  Xavier Fradera ,  Liangqin Guo ,  Yongxin Han ,  Shuwen He ,  Xianhai Huang ,  Joseph Kozlowski ,  Guoqing Li ,  Theodore A. Martinot ,  Alexander Pasternak ,  Andreas Verras ,  Li Xiao ,  Feng Ye ,  Wensheng Yu ,  Rui Zhang

IPC分类号： C07D231/56 ,  C07D491/052 ,  C07D231/54 ,  A61K31/496 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  A61K31/5377 ,  C07D498/10 ,  C07D491/107 ,  C07D498/08 ,  C07D471/10 ,  C07D403/12 ,  C07D405/12 ,  C07D498/04 ,  C07D487/04 ,  C07D487/10 ,  A61K31/541 ,  C07D413/14

摘要： Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20160068532A1

公开(公告)日：2016-03-10

申请号：US14787280

申请日：2014-04-25

申请人： Jongwon LIM ,  Xianhai HUANG ,  Ronald D. FERGUSON ,  Wei ZHOU ,  Christopher W. BOYCE ,  Phieng SILIPHAIVANH ,  David J. WITTER ,  Milana M. MALETIC ,  Joseph A. KOZLOWSKI ,  Kevin J. WILSON ,  MERCK SHARP & DOHME CORP.

发明人： Jongwon Lim ,  Xianhai Huang ,  Ronald D. Ferguson ,  Wei Zhou ,  Christopher W. Boyce ,  Phieng Siliphaivanh ,  David J. Witter ,  Milana M. Maletic ,  Joseph A. Kozlowski ,  Kevin J. Wilson

IPC分类号： C07D487/04 ,  C07D471/14 ,  C07D471/04

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00

摘要： Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I).

摘要翻译： 公开了式（I）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（I）化合物治疗癌症的方法。 本发明还提供了包含有效量的至少一种式（I）化合物和药学上可接受的载体的药物组合物。 本发明还提供一种药物组合物，其包含有效量的至少一种式（I）化合物和有效量的至少一种其它药学活性成分（例如化学治疗剂）和药学上可接受的载体 。 本发明还提供了在需要这种治疗的患者中抑制ERK（即，抑制ERK2的活性）的方法，包括向所述患者施用有效量的至少一种式（I）化合物。