公开(公告)号：US20120329743A1

公开(公告)日：2012-12-27

申请号：US13523354

申请日：2012-06-14

申请人： Xianhai Huang ,  Jason Brubaker ,  Scott L. Peterson ,  John W. Butcher ,  Joshua T. Close ,  Michelle Martinez ,  Rachel Nicola MacCoss ,  Joon O. Jung ,  Phieng Siliphaivanh ,  Hongjun Zhang ,  Robert G. Aslanian ,  Purakkattle Johny Biju ,  Li Dong ,  Ying Huang ,  Kevin D. McCormick ,  Anandan Palani ,  Ning Shao ,  Wei Zhou

发明人： Xianhai Huang ,  Jason Brubaker ,  Scott L. Peterson ,  John W. Butcher ,  Joshua T. Close ,  Michelle Martinez ,  Rachel Nicola MacCoss ,  Joon O. Jung ,  Phieng Siliphaivanh ,  Hongjun Zhang ,  Robert G. Aslanian ,  Purakkattle Johny Biju ,  Li Dong ,  Ying Huang ,  Kevin D. McCormick ,  Anandan Palani ,  Ning Shao ,  Wei Zhou

IPC分类号： C07D221/16 ,  C07D413/10 ,  A61K31/5377 ,  C07D401/10 ,  A61P11/00 ,  A61K31/501 ,  C07H15/26 ,  A61K31/706 ,  A61P11/06 ,  A61P37/08 ,  A61K31/473 ,  A61K31/506

CPC分类号： C07D221/16 ,  A61K31/473 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

摘要： The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.

摘要翻译： 本发明提供一些式（I）的环烷基稠合的四氢喹啉及其药学上可接受的盐和酯，其中R1，R2，R7，R8，R8a，E，Y，Z，n，u和t如本文所定义 。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。

公开(公告)号：US20140128367A1

公开(公告)日：2014-05-08

申请号：US14126579

申请日：2012-06-14

申请人： Xianhai Huang ,  Jason Brubaker ,  Scott L. Peterson ,  John W. Butcher ,  Joshua T. Close ,  Michelle Martinez ,  Rachel Nicola MacCoss ,  Joon O. Jung ,  Phieng Siliphaivanh ,  Hongjun Zhang ,  Robert G. Aslanian ,  Purakkattle Johny Biju ,  Li Dong ,  Ying Huang ,  Kevin D. McCormick ,  Anandan Palani ,  Ning Shao ,  Wei Zhou

发明人： Xianhai Huang ,  Jason Brubaker ,  Scott L. Peterson ,  John W. Butcher ,  Joshua T. Close ,  Michelle Martinez ,  Rachel Nicola MacCoss ,  Joon O. Jung ,  Phieng Siliphaivanh ,  Hongjun Zhang ,  Robert G. Aslanian ,  Purakkattle Johny Biju ,  Li Dong ,  Ying Huang ,  Kevin D. McCormick ,  Anandan Palani ,  Ning Shao ,  Wei Zhou

IPC分类号： C07D221/16 ,  A61K31/5377 ,  C07D401/12 ,  A61K31/506 ,  A61K31/501 ,  A61K31/473 ,  C07D401/10

CPC分类号： C07D221/16 ,  A61K31/473 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

摘要： The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.

摘要翻译： 本发明提供一些式（I）的环烷基稠合的四氢喹啉及其药学上可接受的盐和酯，其中R1，R2，R7，R8a，E，Y，Z，n，u和t如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。

公开(公告)号：US08592383B2

公开(公告)日：2013-11-26

申请号：US13523354

申请日：2012-06-14

申请人： Xianhai Huang ,  Jason Brubaker ,  Scott L. Peterson ,  John W. Butcher ,  Joshua T. Close ,  Michelle Martinez ,  Rachel Nicola MacCoss ,  Joon O. Jung ,  Phieng Siliphaivanh ,  Hongjun Zhang ,  Robert G. Aslanian ,  Purakkattle Johny Biju ,  Li Dong ,  Ying Huang ,  Kevin D. McCormick ,  Anandan Palani ,  Ning Shao ,  Wei Zhou

发明人： Xianhai Huang ,  Jason Brubaker ,  Scott L. Peterson ,  John W. Butcher ,  Joshua T. Close ,  Michelle Martinez ,  Rachel Nicola MacCoss ,  Joon O. Jung ,  Phieng Siliphaivanh ,  Hongjun Zhang ,  Robert G. Aslanian ,  Purakkattle Johny Biju ,  Li Dong ,  Ying Huang ,  Kevin D. McCormick ,  Anandan Palani ,  Ning Shao ,  Wei Zhou

IPC分类号： C07D221/16 ,  C07D401/10 ,  C07D413/10 ,  A61K31/473 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/706 ,  A61P11/00 ,  A61P11/06 ,  A61P37/08 ,  C07H15/26

CPC分类号： C07D221/16 ,  A61K31/473 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

摘要： The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.

摘要翻译： 本发明提供一些式（I）的环烷基稠合的四氢喹啉及其药学上可接受的盐和酯，其中R1，R2，R7，R8，R8a，E，Y，Z，n，u和t如本文所定义 。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。

公开(公告)号：US10442819B2

公开(公告)日：2019-10-15

申请号：US15532549

申请日：2015-12-01

申请人： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Qingmei Hong ,  Chunhui Huang ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Ryan D. Otte ,  Dann L. Parker, Jr. ,  Michael Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Feroze Ujjainwalla ,  Catherine White ,  Zhicai Wu ,  Yang Yu ,  Kake Zhao ,  Craig Gibeau ,  Tesfaye Biftu ,  Purakkattle Biju ,  Lei Chen ,  Joshua Close ,  Peter H. Fuller ,  Xianhai Huang ,  Min K. Park ,  Valdimir Simov ,  David J. Witter ,  Hongjun Zhang

发明人： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Qingmei Hong ,  Chunhui Huang ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Ryan D. Otte ,  Dann L. Parker, Jr. ,  Michael Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Feroze Ujjainwalla ,  Catherine White ,  Zhicai Wu ,  Yang Yu ,  Kake Zhao ,  Craig Gibeau ,  Tesfaye Biftu ,  Purakkattle Biju ,  Lei Chen ,  Joshua Close ,  Peter H. Fuller ,  Xianhai Huang ,  Min K. Park ,  Valdimir Simov ,  David J. Witter ,  Hongjun Zhang

IPC分类号： A61K31/351 ,  A61K31/4353 ,  A61K31/5355 ,  A61K31/551 ,  C07D471/04 ,  C07D471/14 ,  C07D498/08 ,  C07D471/08 ,  C07D498/04 ,  C07D498/10 ,  A01N43/00

摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

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：US20130079271A1

公开(公告)日：2013-03-28

申请号：US13499071

申请日：2010-09-22

申请人： Kevin D. McCormick ,  Ning Shao ,  Younong Yu ,  Xianhai Huang ,  Manuel De Lera Ruiz ,  Anandan Palani ,  Junying Zheng ,  Christopher W. Boyce ,  Robert G. Aslanian ,  Jianhua Chao

发明人： Kevin D. McCormick ,  Ning Shao ,  Younong Yu ,  Xianhai Huang ,  Manuel De Lera Ruiz ,  Anandan Palani ,  Junying Zheng ,  Christopher W. Boyce ,  Robert G. Aslanian ,  Jianhua Chao

IPC分类号： C07D413/10 ,  A61K31/537 ,  A61K31/4245 ,  A61K38/02 ,  A61K31/423 ,  A61K31/4439 ,  A61K31/56 ,  A61K31/506 ,  C07D263/52

CPC分类号： C07D413/10 ,  A61K31/42 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/537 ,  A61K31/56 ,  A61K38/02 ,  A61K45/06 ,  C07D263/52 ,  C07D413/04 ,  C07D417/04 ,  A61K2300/00

摘要： In its many embodiments, the present invention provides a novel class of biaryl 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联芳基螺氨基恶唑啉类似物作为α2C肾上腺素能受体激动剂的调节剂，制备此类化合物的方法，含有一种或多种此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：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：US20150353498A1

公开(公告)日：2015-12-10

申请号：US14432462

申请日：2013-09-26

申请人： Xianhai HUANG ,  Anandan PALANI ,  Ashwin U. RAO ,  Hongjun ZHANG ,  Wei ZHOU ,  MERCK SHARP & DOHME CORP.

发明人： Xianhai Huang ,  Anandan Palani ,  Ashwin U. Rao ,  Hongjun Zhang ,  Wei Zhou

IPC分类号： C07D217/24 ,  C07D401/06 ,  C07D413/14 ,  A61K31/4725 ,  C07D413/04 ,  A61K31/472 ,  A61K31/496

CPC分类号： C07D217/24 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/496 ,  A61K45/06 ,  C07D401/06 ,  C07D401/12 ,  C07D413/04 ,  C07D413/14 ,  A61K2300/00

摘要： The invention provides certain substituted isoquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters. The invention also provides pharmaceutical compositions comprising for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.

摘要翻译： 本发明提供某些式（I）的取代的异喹啉及其药学上可接受的盐和酯。 本发明还提供药物组合物，其包含用于治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症。

公开(公告)号：US08598158B2

公开(公告)日：2013-12-03

申请号：US13515638

申请日：2010-12-09

申请人： Dong Xiao ,  Anandan Palani ,  Robert G. Aslanian ,  Sylvia Degrado ,  Xianhai Huang ,  Wei Zhou ,  Michael Sofolarides ,  Xiao Chen

发明人： Dong Xiao ,  Anandan Palani ,  Robert G. Aslanian ,  Sylvia Degrado ,  Xianhai Huang ,  Wei Zhou ,  Michael Sofolarides ,  Xiao Chen

IPC分类号： C07D417/02 ,  C07D417/14 ,  A61K31/55 ,  A61P29/00

CPC分类号： A61K31/55 ,  C07D491/048 ,  C07D495/04

摘要： The present invention relates to certain lactam ring-containing compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein D, E, X1, R1, R2, R3, R4, R9, and R10 are as herein described. In addition, the invention relates to pharmaceutically acceptable compositions comprising at least one such compound, and methods of using the compounds for treating or preventing various inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, asthma, and chronic obstructive pulmonary disorder.

摘要翻译： 本发明涉及式（I）的某些含内酰胺环的化合物及其药学上可接受的盐，其中D，E，X 1，R 1，R 2，R 3，R 4，R 9和R 10如本文所述。 此外，本发明涉及包含至少一种此类化合物的药学上可接受的组合物，以及使用该化合物治疗或预防各种炎性疾病如类风湿性关节炎，炎性肠病，牛皮癣，哮喘和慢性阻塞性肺病的方法。

公开(公告)号：US20110294756A1

公开(公告)日：2011-12-01

申请号：US13128493

申请日：2009-11-12

申请人： Zhaoning Zhu ,  William J. ,  Xianhai Huang ,  Jun Qin ,  XIaoxiang Liu ,  Hongmei Li ,  Wei Zhou ,  Anandan Palani ,  Xiaohong Zhu ,  Monica L. Vicarel ,  Mihirbaran Mandal ,  Zhong-Yue Sun ,  Chad E. Bennett ,  Troy Michael McCracken ,  Gioconda V. Gallo

发明人： Zhaoning Zhu ,  William J. ,  Xianhai Huang ,  Jun Qin ,  XIaoxiang Liu ,  Hongmei Li ,  Wei Zhou ,  Anandan Palani ,  Xiaohong Zhu ,  Monica L. Vicarel ,  Mihirbaran Mandal ,  Zhong-Yue Sun ,  Chad E. Bennett ,  Troy Michael McCracken ,  Gioconda V. Gallo

IPC分类号： A61K31/695 ,  C07D413/10 ,  C07D471/04 ,  A61P25/28 ,  A61K31/519 ,  C07D498/20 ,  C07F7/18 ,  C07D498/04 ,  A61K31/5395

CPC分类号： C07D471/04 ,  C07D498/04

摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of Group A or Group, as defined herein, 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，本发明提供了一类新颖的本文所定义的组A或组的杂环化合物作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物的方法 包含一种或多种这样的化合物的制剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。