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：US20220235028A1

公开(公告)日：2022-07-28

申请号：US17615718

申请日：2020-06-08

申请人： Yongxin HAN ,  Yongqi DENG ,  Hua ZHOU ,  Meredeth A. MCGOWAN ,  Hongjun ZHANG ,  Wensheng YU ,  Brett A. HOPKINS ,  Xavier FRADERA ,  Nunzio SCIAMMETTA ,  Merck Sharp & Dohme Corp.

发明人： Yongxin Han ,  Yongqi Deng ,  Hua Zhou ,  Meredeth A. McGowan ,  Hongjun Zhang ,  Wensheng Yu ,  Brett A. Hopkins ,  Xavier Fradera ,  Nunzio Sciammetta

IPC分类号： C07D401/06 ,  C07D401/08 ,  C07D471/04 ,  C07D519/00

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. 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：US11319283B2

公开(公告)日：2022-05-03

申请号：US16753035

申请日：2018-10-04

申请人： MERCK SHARP & DOHME CORP. ,  Meredeth Ann McGowan ,  Abdelghani Achab ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Jongwon Lim ,  Kun Liu ,  Nunzio Sciammetta ,  Catherine M. White ,  Wensheng Yu ,  Hongjun Zhang ,  Hua Zhou

发明人： Meredeth Ann McGowan ,  Abdelghani Achab ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Jongwon Lim ,  Kun Liu ,  Nunzio Sciammetta ,  Catherine M. White ,  Wensheng Yu ,  Hongjun Zhang ,  Hua Zhou

IPC分类号： C07D205/04 ,  C07C237/42 ,  C07D213/75 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D237/20 ,  C07D239/28 ,  C07D241/24 ,  C07D263/34 ,  C07D277/56 ,  C07D285/06 ,  C07D307/14 ,  C07D309/14 ,  C07D487/04

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20200277252A1

公开(公告)日：2020-09-03

申请号：US16753035

申请日：2018-10-04

申请人： Meredeth Ann McGowan ,  Abdelghani Achab ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Jongwon Lim ,  Kun Liu ,  Nunzio Sciammetta ,  Catherine M. White ,  Wensheng Yu ,  Hongjun Zhang ,  Hua Zhou ,  MERCK SHARP & DOHME CORP.

发明人： Meredeth Ann McGowan ,  Abdelghani Achab ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Jongwon Lim ,  Kun Liu ,  Nunzio Sciammetta ,  Catherine M. White ,  Wensheng Yu ,  Hongjun Zhang ,  Hua Zhou

IPC分类号： C07C237/42 ,  C07D241/24 ,  C07D213/82 ,  C07D233/90 ,  C07D263/34 ,  C07D231/14 ,  C07D277/56 ,  C07D239/28 ,  C07D213/75 ,  C07D309/14 ,  C07D237/20 ,  C07D307/14 ,  C07D205/04 ,  C07D285/06 ,  C07D487/04

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20220056051A1

公开(公告)日：2022-02-24

申请号：US17312480

申请日：2019-12-13

申请人： Abdelghani Abe ACHAB ,  Matthew L. CHILDERS ,  Jared N. CUMMING ,  Symon GATHIAKA ,  Charles A. LESBURG ,  Derun LI ,  Min LU ,  Matthew J. MITCHELTREE ,  Anandan PALANI ,  Rachel L. PALTE ,  Hongjun ZHANG ,  Merck Sharp & Dohme Corp.

发明人： Abdelghani Abe Achab ,  Matthew L. Childers ,  Jared N. Cumming ,  Symon Gathiaka ,  Charles A. Lesburg ,  Derun Li ,  Min Lu ,  Matthew J. Mitcheltree ,  Anandan Palani ,  Rachel L. Palte ,  Hongjun Zhang

IPC分类号： C07F5/02

摘要： Described herein are compounds of Formula (I), or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

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：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：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：US20130303517A1

公开(公告)日：2013-11-14

申请号：US13996361

申请日：2011-12-19

申请人： Christopher W. Boyce ,  Sylvia Joanna Degrado ,  Xiao Chen ,  Jun Qin ,  Robert D. Mazzola, JR. ,  Younong Yu ,  Kevin D. McCormick ,  Anandan Palani ,  Dong Xiao ,  Robert George Aslanian ,  Jie Wu ,  Ashwin Umesh Rao ,  Phieng Siliphaivanh ,  Joey L. Methot ,  Hongjun Zhang ,  Elizabeth Helen Kelley ,  William Colby Brown ,  Qin Jiang ,  Jolicia Polivina Gauuan ,  Andrew J. Leyhane ,  Purakkattle Johny Biju ,  Pawan K. Dhondi ,  Li Dong ,  Salem Fevrier ,  Xianhai Huang ,  Henry M. Vaccaro

发明人： Christopher W. Boyce ,  Sylvia Joanna Degrado ,  Xiao Chen ,  Jun Qin ,  Robert D. Mazzola, JR. ,  Younong Yu ,  Kevin D. McCormick ,  Anandan Palani ,  Dong Xiao ,  Robert George Aslanian ,  Jie Wu ,  Ashwin Umesh Rao ,  Phieng Siliphaivanh ,  Joey L. Methot ,  Hongjun Zhang ,  Elizabeth Helen Kelley ,  William Colby Brown ,  Qin Jiang ,  Jolicia Polivina Gauuan ,  Andrew J. Leyhane ,  Purakkattle Johny Biju ,  Pawan K. Dhondi ,  Li Dong ,  Salem Fevrier ,  Xianhai Huang ,  Henry M. Vaccaro

IPC分类号： C07D241/42 ,  C07D401/12 ,  C07D403/06 ,  C07D471/04 ,  A61K31/4985 ,  C07D471/10 ,  C07D405/12 ,  C07D401/14 ,  A61K31/506 ,  A61K31/55 ,  C07D417/12 ,  C07D498/04 ,  C07D491/107 ,  A61K45/06 ,  A61K31/498

CPC分类号： C07D241/42 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/55 ,  A61K45/06 ,  C07D241/38 ,  C07D241/44 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/048 ,  C07D491/107 ,  C07D498/04 ,  C07D498/10

摘要： The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q 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： 本发明提供了式（I）的某些喹喔啉和氮杂 - 喹喔啉及其药学上可接受的盐，其中J1，J2，R1，R2，R3，R22，Ra，Rb，Rc，Rd，X，Y，b，n ，和q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：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。