公开(公告)号：US11034661B2

公开(公告)日：2021-06-15

申请号：US16495883

申请日：2018-03-23

申请人： Merck Sharp & Dohme Corp. ,  Liangqin Guo ,  Yongxin Han ,  Kun Liu ,  Shuwen He ,  Joseph Kozlowski ,  Ravi Nargund ,  Wensheng Yu ,  Hongjun Zhang ,  Qinglin Pu ,  Derun Li ,  Abdelghani Achab ,  Guoqing Li

发明人： Liangqin Guo ,  Yongxin Han ,  Kun Liu ,  Shuwen He ,  Joseph Kozlowski ,  Ravi Nargund ,  Wensheng Yu ,  Hongjun Zhang ,  Qinglin Pu ,  Derun Li ,  Abdelghani Achab ,  Guoqing Li

IPC分类号： C07D271/08 ,  C07D413/12

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：US10927086B2

公开(公告)日：2021-02-23

申请号：US16483957

申请日：2018-02-19

申请人： Merck Sharp & Dohme Corp. ,  Kun Liu ,  Dane Clausen ,  Liangqin Guo ,  Yongxin Han ,  Shuwen He ,  Joseph Kozlowski ,  Derun Li ,  Qinglin Pu ,  Wensheng Yu ,  Hongjun Zhang

发明人： Kun Liu ,  Dane Clausen ,  Liangqin Guo ,  Yongxin Han ,  Shuwen He ,  Joseph Kozlowski ,  Derun Li ,  Qinglin Pu ,  Wensheng Yu ,  Hongjun Zhang

IPC分类号： C07D271/08 ,  C07D413/12

摘要： Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). 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：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：US09828365B2

公开(公告)日：2017-11-28

申请号：US15104584

申请日：2014-12-15

申请人： MERCK SHARP & DOHME CORP. ,  Joseph Kozlowski ,  Craig Coburn ,  Wensheng Yu ,  Ling Tong ,  Bin Hu ,  Bin Zhong ,  Jinglai Hao ,  Dahai Wang ,  Tao Ji

发明人： Joseph Kozlowski ,  Craig Coburn ,  Wensheng Yu ,  Ling Tong ,  Bin Hu ,  Bin Zhong ,  Jinglai Hao ,  Dahai Wang ,  Tao Ji

IPC分类号： C07D493/04 ,  C07D405/14 ,  A61K45/06 ,  A61K31/4985 ,  A61K31/7072 ,  A61K31/4178

CPC分类号： C07D405/14 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4985 ,  A61K31/7072 ,  A61K45/06 ,  C07D493/04 ,  A61K2300/00

摘要： The present invention relates to novel Fused Tetracyclic Heterocyclic Compounds of Formula I: (I), wherein A, A′, R2A, R2B, R7, R8, R9, and R10 are defined herein. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The present invention also relates to pharmaceutical compositions comprising at least one Fused Tetracyclic Heterocyclic Compound, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines, and methods of using the Fused Tetracyclic Heterocyclic Compounds for treating or preventing HCV infection in a patient.

公开(公告)号：US20150258074A1

公开(公告)日：2015-09-17

申请号：US14431485

申请日：2013-09-26

申请人： Kevin J. WILSON ,  David J. WITTER ,  Matthew H. DANIELS ,  Angie R. ANGELES ,  Phieng SILIPHAIVANH ,  David L. SLOMAN ,  Brendan O'BOYLE ,  Danielle FALCONE ,  Catherine WHITE ,  Ron FERGUSON ,  Wei ZHOU ,  Kathryn LIPFORD ,  Umar Faruk MANSOOR ,  Salem FEVRIRE ,  Xianhai HUANG ,  Ravi KURUKULASURIYA ,  Judson E. RICHARD ,  Shuyi TANG ,  Christopher BOYCE ,  Joseph KOZLOWSKI ,  Raman Kumar BAKSHI ,  Ganesh Babu UNAKARAN ,  Merck Sharp & Dohme Corp.

发明人： Kevin J. Wilson ,  David J. Witter ,  Matthew H. Daniels ,  Angie R. Angeles ,  Phieng Siliphaivanh ,  David Sloman ,  Brendan O'Boyle ,  Danielle Falcone ,  Catherine White ,  Ron Ferguson ,  Wei Zhou ,  Kathryn Lipford ,  Umar Faruk Mansoor ,  Salem Fevrier ,  Xianhai Huang ,  Ravi Kurukulasuriya ,  Judson E. Richard ,  Shuyi Tang ,  Christopher Boyce ,  Joseph Kozlowski ,  Raman Kumar Bakshi ,  Ganesh Babu Karunakaran

IPC分类号： A61K31/437 ,  A61K45/06 ,  A61K31/4545 ,  C07D471/04

CPC分类号： A61K31/437 ,  A61K31/4545 ,  A61K45/06 ,  C07D471/04

摘要： Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).

摘要翻译： 公开了具有吡唑并吡啶基结构的式（1.0）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1.0）化合物治疗癌症的方法。

公开(公告)号：US20150266895A1

公开(公告)日：2015-09-24

申请号：US14431462

申请日：2013-09-26

申请人： Kevin J. WILSON ,  David J. WITTER ,  Phieng SILIPHAIVANH ,  Kathryn KIPFORD ,  David SLOMAN ,  Danielle FALCONE ,  Brendan O'BOYLE ,  Umar Faruk MANSOOR ,  Jongwon LIM ,  Joey L. METHOT ,  Christopher BOYCE ,  Lei CHEN ,  Matthew H. DANIELS ,  Salem FEVRIER ,  Xianhai HUANG ,  Ravi KURUKULASURIYA ,  Ling TONG ,  Wei ZHOU ,  Joseph KOZLOWSKI ,  Milana M. MALETIC ,  Bidhan A. SHINKRE ,  Jayanth Thiruvellore THATAI ,  Raman Kumar BAKSHI ,  Ganesh Babu KARUNAKARAN ,  MERCK SHARP & DOHME CORP.

发明人： Kevin J. Wilson ,  David J. Witter ,  Phieng Siliphaivanh ,  Kathryn Lipford ,  David Sloman ,  Danielle Falcone ,  Brendan O'Boyle ,  Umar Faruk Mansoor ,  Jongwon Lim ,  Joey L. Methot ,  Christopher Boyce ,  Lei Chen ,  Matthew H. Daniels ,  Salem Fevrier ,  Xianhai Huang ,  Ravi Kurukulasuriya ,  Ling Tong ,  Wei Zhou ,  Joseph Kozlowski ,  Milana M. Maletic ,  Bidhan A. Shinkre ,  Jayanth Thiruvellore Thatai ,  Raman Kumar Bakshi ,  Ganesh Babu Karunakaran

IPC分类号： C07D498/18 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/496 ,  A61K45/06 ,  A61K31/4375 ,  C07D498/14 ,  A61K31/553 ,  C07D519/00 ,  C07D471/04 ,  C07D471/14

CPC分类号： C07D498/18 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/553 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/16 ,  C07D498/14 ,  C07D498/16 ,  C07D519/00 ,  A61K2300/00

摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).

摘要翻译： 公开了式（1）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1）的化合物治疗癌症的方法。

公开(公告)号：US20170217940A1

公开(公告)日：2017-08-03

申请号：US15104584

申请日：2014-12-15

申请人： Joseph KOZLOWSKI ,  Craig COBURN ,  Wensheng YU ,  Bin HU ,  Bin ZHONG ,  Jinglai HAO ,  Dahai WANG ,  Tao JI ,  MERCL SHARP & DOHME CORP.

发明人： Joseph Kozlowski ,  Craig Coburn ,  Wensheng Yu ,  Ling Tong ,  Bin Hu ,  Bin Zhong ,  Jinglai Hao ,  Dahai Wang ,  Tao Ji

IPC分类号： C07D405/14 ,  A61K31/4178 ,  A61K31/7072 ,  A61K45/06 ,  A61K31/4985

CPC分类号： C07D405/14 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4985 ,  A61K31/7072 ,  A61K45/06 ,  C07D493/04 ,  A61K2300/00

摘要： The present invention relates to novel Fused Tetracyclic Heterocyclic Compounds of Formula I: (I), wherein A, A′, R2A, R2B, R7, R8, R9, and R10 are defined herein. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The present invention also relates to pharmaceutical compositions comprising at least one Fused Tetracyclic Heterocyclic Compound, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines, and methods of using the Fused Tetracyclic Heterocyclic Compounds for treating or preventing HCV infection in a patient.

公开(公告)号：US20070265299A1

公开(公告)日：2007-11-15

申请号：US11653798

申请日：2007-01-16

申请人： Brian Lavey ,  Joseph Kozlowski ,  Guowei Zhou ,  Ling Tong ,  Wensheng Yu ,  Michael Wong ,  Bandarpalle Shankar ,  Neng-Yang Shih ,  M. Siddiqui ,  Kristin Rosner ,  Chaoyang Dai ,  Janeta Popovici-Muller ,  Vinay Girijavallabhan ,  Dansu Li ,  Aneta Micula ,  Seong-Heon Kim ,  De-Yi Yang ,  Razia Rizvi

发明人： Brian Lavey ,  Joseph Kozlowski ,  Guowei Zhou ,  Ling Tong ,  Wensheng Yu ,  Michael Wong ,  Bandarpalle Shankar ,  Neng-Yang Shih ,  M. Siddiqui ,  Kristin Rosner ,  Chaoyang Dai ,  Janeta Popovici-Muller ,  Vinay Girijavallabhan ,  Dansu Li ,  Aneta Micula ,  Seong-Heon Kim ,  De-Yi Yang ,  Razia Rizvi

IPC分类号： A61K31/44 ,  A61K31/4152 ,  A61K31/4412 ,  A61K31/4709 ,  A61K35/00 ,  A61P11/00 ,  A61P11/08 ,  A61P17/06 ,  A61P3/14 ,  A61P37/00 ,  A61P37/08 ,  A61P9/00 ,  A61P9/10 ,  C07D215/06 ,  C07D233/02 ,  C07D401/06 ,  C07D471/02

CPC分类号： C07D403/14 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00

摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPS, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.

摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，溶剂化物或异构体，其可用于治疗由MMPS，ADAM，TACE，聚集蛋白聚糖蛋白酶，TNF-α或其组合介导的疾病或病症 。

公开(公告)号：US20070219218A1

公开(公告)日：2007-09-20

申请号：US11653676

申请日：2007-01-16

申请人： Wensheng Yu ,  Ling Tong ,  Lei Chen ,  Joseph Kozlowski ,  Brian Lavey ,  Neng-Yang Shih ,  Vincent Madison ,  Guowei Zhou ,  Peter Orth ,  Zhuyan Guo ,  Michael Wong ,  De-Yi Yang ,  Seong Kim ,  Bandarpalle Shankar ,  M. Siddiqui ,  Kristin Rosner ,  Chaoyang Dai ,  Janeta Popovici-Muller ,  Vinay Girijavallabhan ,  Dansu Li ,  Razia Rizvi ,  Aneta Micula ,  Robert Feltz

发明人： Wensheng Yu ,  Ling Tong ,  Lei Chen ,  Joseph Kozlowski ,  Brian Lavey ,  Neng-Yang Shih ,  Vincent Madison ,  Guowei Zhou ,  Peter Orth ,  Zhuyan Guo ,  Michael Wong ,  De-Yi Yang ,  Seong Kim ,  Bandarpalle Shankar ,  M. Siddiqui ,  Kristin Rosner ,  Chaoyang Dai ,  Janeta Popovici-Muller ,  Vinay Girijavallabhan ,  Dansu Li ,  Razia Rizvi ,  Aneta Micula ,  Robert Feltz

IPC分类号： A61K31/497 ,  A61K31/506 ,  A61K31/4709 ,  A61K31/4741 ,  A61K31/4745 ,  A61K31/4178 ,  C07D403/14 ,  C07D491/02 ,  C07D471/02

CPC分类号： C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D473/34 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.

摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，溶剂化物，酯或异构体，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖酶，TNF-或组合介导的疾病或病症 其中。

公开(公告)号：US20060205797A1

公开(公告)日：2006-09-14

申请号：US11180863

申请日：2005-07-13

申请人： Wensheng Yu ,  Ling Tong ,  Lei Chen ,  Joseph Kozlowski ,  Brian Lavey ,  Neng-Yang Shih ,  Vincent Madison ,  Guowei Zhou ,  Peter Orth ,  Zhuyan Guo ,  Michael Wong ,  De-Yi Yang ,  Seong Kim ,  Bandarpalle Shankar

发明人： Wensheng Yu ,  Ling Tong ,  Lei Chen ,  Joseph Kozlowski ,  Brian Lavey ,  Neng-Yang Shih ,  Vincent Madison ,  Guowei Zhou ,  Peter Orth ,  Zhuyan Guo ,  Michael Wong ,  De-Yi Yang ,  Seong Kim ,  Bandarpalle Shankar

IPC分类号： A61K31/425 ,  A61K31/4178 ,  C07D417/02 ,  C07D403/02

CPC分类号： C07D401/14 ,  C07D403/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF—combinations thereof.

摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，TNF-组合介导的疾病或病症。