公开(公告)号：US11478461B2

公开(公告)日：2022-10-25

申请号：US17047247

申请日：2019-04-15

申请人： Merck Sharp & Dohme Corp.

发明人： Liangqin Guo ,  Hongjun Zhang ,  Ping Chen ,  Dane Clausen ,  Xavier Fradera ,  Yongxin Han ,  Shuwen He ,  Xianhai Huang ,  Alexander Pasternak ,  Qinglin Pu ,  Li Xiao ,  Feng Ye

IPC分类号： A61K31/44 ,  A61K45/06 ,  C07C237/22 ,  C07C255/60 ,  C07D213/75 ,  C07C271/36 ,  C07C233/78 ,  C07C271/24 ,  C07C233/79 ,  C07D213/81 ,  C07D271/06 ,  C07D239/28 ,  C07D215/48 ,  C07C275/30 ,  C07C275/28 ,  C07D239/42 ,  C07D305/06 ,  C07D261/08 ,  C07D471/04 ,  C07D261/20 ,  C07D209/34 ,  C07D277/56 ,  C07D217/02 ,  C07D231/14 ,  C07D237/28 ,  C07D241/24 ,  C07D217/26 ,  A61K31/167 ,  A61K31/27 ,  A61K31/4245 ,  A61K31/47 ,  A61K31/17 ,  A61K31/505 ,  A61K31/337 ,  A61K31/437 ,  A61K31/42 ,  A61K31/426 ,  A61K31/472 ,  A61K31/415 ,  A61K31/4965

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：US10968210B2

公开(公告)日：2021-04-06

申请号：US16345913

申请日：2017-11-13

申请人： Merck Sharp & Dohme Corp. ,  Thomas J. Greshock ,  James Mulhearn ,  Anthony J. Roecker ,  Tianying Jian ,  Gang Zhou ,  Liangqin Guo ,  Walter Won ,  Ting Zhang ,  Rajan Anand ,  John E. Stelmach ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Christopher S. Burgey ,  Philippe G. Nantermet

发明人： Thomas J. Greshock ,  James Mulhearn ,  Anthony J. Roecker ,  Tianying Jian ,  Gang Zhou ,  Liangqin Guo ,  Walter Won ,  Ting Zhang ,  Rajan Anand ,  John E. Stelmach ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Christopher S. Burgey ,  Philippe G. Nantermet

IPC分类号： C07D417/12 ,  C07D417/14 ,  C07D277/52 ,  C07D471/04 ,  C07D487/10 ,  C07D401/12 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

摘要： Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.

公开(公告)号：US10519147B2

公开(公告)日：2019-12-31

申请号：US16061815

申请日：2016-12-15

申请人： Merck Sharp & Dohme Corp. ,  Thomas J. Greshock ,  James Mulhearn ,  Liangqin Guo ,  Ting Zhang ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Michael J. Kelly, III ,  Rajan Anand ,  Philippe Nantermet ,  Tianying Jian ,  Anthony J. Roecker ,  Walter Won ,  Gang Zhou

发明人： Thomas J. Greshock ,  James Mulhearn ,  Liangqin Guo ,  Ting Zhang ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Michael J. Kelly, III ,  Rajan Anand ,  Philippe Nantermet ,  Tianying Jian ,  Anthony J. Roecker ,  Walter Won ,  Gang Zhou

IPC分类号： C07D417/12 ,  A61K45/06 ,  C07D277/52 ,  C07D285/135 ,  A61P25/02 ,  A61P25/04 ,  A61P11/14 ,  A61P17/04

摘要： Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.

公开(公告)号：US09708308B2

公开(公告)日：2017-07-18

申请号：US14652237

申请日：2013-12-16

申请人： Merck Sharp & Dohme Corp. ,  Mochida Pharmaceutical Co., Ltd.

发明人： Cameron James Smith ,  John Qiang Tan ,  Ting Zhang ,  James Balkovec ,  William John Greenlee ,  Liangqin Guo ,  Yi-Heng Chen ,  Yili Chen ,  Jiayi Xu ,  Samuel Chackalamannil ,  Tomokazu Hirabayashi ,  Hiroshi Nagasue ,  Kouki Ogawa

IPC分类号： C07D471/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04

CPC分类号： C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.

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：US10221167B2

公开(公告)日：2019-03-05

申请号：US15378465

申请日：2016-12-14

申请人： Merck Sharp & Dohme Corp.

发明人： Thomas J. Greshock ,  James Mulhearn ,  Junying Zheng ,  Ronald M. Kim ,  Ting Zhang ,  Anthony J. Roecker ,  Walter Won ,  Philippe Nantermet ,  Rajan Anand ,  Gang Zhou ,  Deping Wang ,  Liangqin Guo

IPC分类号： C07D417/12 ,  C07D285/08 ,  C07D277/52 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4168 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/551 ,  A61K45/06

摘要： Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.

公开(公告)号：US20180362482A1

公开(公告)日：2018-12-20

申请号：US16061597

申请日：2016-12-12

申请人： Merck Sharp & Dohme Corp.

发明人： Yongxin Han ,  Abdelghani Achab ,  Purakkattle Biju ,  Yongqi Deng ,  Xavier Fradera ,  Liangqin Guo ,  Shuwen He ,  Joseph Kozlowski ,  Ravi Kurukulasuriya ,  Kun Liu ,  Meredeth Ann McGowan ,  Qinglin Pu ,  Nunzio Sciammetta ,  Hongjun Zhang ,  Hua Zhou

IPC分类号： C07D271/08 ,  C07D285/10 ,  C07D413/12 ,  A61P25/24 ,  A61P25/28 ,  A61P35/02 ,  A61P31/14 ,  A61P27/12 ,  A61P37/06

CPC分类号： C07D271/08 ,  A61P25/24 ,  A61P25/28 ,  A61P27/12 ,  A61P31/14 ,  A61P35/02 ,  A61P37/06 ,  C07D285/10 ,  C07D413/12 ,  C07D417/12 ,  C07F9/65318

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：US09914727B2

公开(公告)日：2018-03-13

申请号：US14652174

申请日：2013-12-16

申请人： Merck Sharp & Dohme Corp. ,  Mochida Pharmaceutical Co., Ltd.

发明人： Cameron James Smith ,  John Qiang Tan ,  Ting Zhang ,  James Balkovec ,  William John Greenlee ,  Liangqin Guo ,  Yi-Heng Chen ,  Yili Chen ,  Samuel Chackalamannil ,  Tomokazu Hirabayashi ,  Mika Sekioka

IPC分类号： C07D413/14 ,  C07D413/12 ,  C07D513/04

CPC分类号： C07D413/14 ,  C07D413/12 ,  C07D513/04

摘要： The present invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula I, and methods for using compounds of Formula I for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes.

公开(公告)号：US20180030036A1

公开(公告)日：2018-02-01

申请号：US15534029

申请日：2015-12-07

申请人： Ting ZHANG ,  Yi-Heng CHEN ,  Liangqin GUO ,  Alan HARUZA ,  Tianying JIAN ,  Bing LI ,  Dongfang MENG ,  Dann L. PARKER, JR. ,  Edward C. SHERER ,  Harold B. WOOD ,  Isao SAKURADA ,  MERCK SHARP & DOHME CORP. ,  MOCHIDA PHARMACEUTICAL CO., LTD

发明人： Ting Zhang ,  Yi-Heng Chen ,  Liangqin Guo ,  Alan Hruza ,  Tianying Jian ,  Bing Li ,  Dongfang Meng ,  Dann L. Parker ,  Edward C. Sherer ,  Harold B. Wood ,  Isao Sakurada

IPC分类号： C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D471/04

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

摘要： 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 unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.

公开(公告)号：US20220000844A1

公开(公告)日：2022-01-06

申请号：US17296601

申请日：2019-12-02

申请人： Merck Sharp & Dohme Corp.

发明人： Christopher J. Bungard ,  Helen Y. Chen ,  Jason M. Cox ,  Liangqin Guo ,  Michael J. Kelly, III ,  Ronald M. Kim ,  Mark E. Layton ,  Hong Liu ,  Jian Liu ,  Mehul F. Patel ,  James J. Perkins ,  Deping Wang ,  Walter Won ,  Younong Yu ,  Ting Zhang

IPC分类号： A61K31/433 ,  C07D285/08 ,  C07D417/12 ,  C07D239/42 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/167

摘要： Disclosed are compounds of Formula (I), Formula (II), or a salt thereof: Formula (I) Formula (II) which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (I), Formula (II) or their salts, and methods of treating pain disorders, cough, and itch using the same.