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：US20120010183A1

公开(公告)日：2012-01-12

申请号：US13179587

申请日：2011-07-11

申请人： Andrew Simon Bell ,  Alan Daniel Brown ,  Marcel John De Groot ,  Russell Andrew Lewthwaite ,  Ian Roger Marsh ,  David Simon Millan ,  Manuel Perez Pacheco ,  David James Rawson ,  Nunzio Sciammetta ,  Robert Ian Storer ,  Nigel Alan Swain ,  Steven Matthieu Gaulier

发明人： Andrew Simon Bell ,  Alan Daniel Brown ,  Marcel John De Groot ,  Russell Andrew Lewthwaite ,  Ian Roger Marsh ,  David Simon Millan ,  Manuel Perez Pacheco ,  David James Rawson ,  Nunzio Sciammetta ,  Robert Ian Storer ,  Nigel Alan Swain ,  Steven Matthieu Gaulier

IPC分类号： A61K31/44 ,  C07D401/04 ,  C07D215/20 ,  C07D405/12 ,  C07D231/56 ,  A61P29/00 ,  A61K31/506 ,  A61K31/47 ,  A61K31/4427 ,  A61K31/416 ,  A61K31/4545 ,  A61K31/4439 ,  C07D213/69 ,  C07D401/12

CPC分类号： C07D213/69 ,  C07D213/63 ,  C07D213/64 ,  C07D213/65 ,  C07D213/70 ,  C07D213/74 ,  C07D213/85 ,  C07D215/20 ,  C07D231/56 ,  C07D239/47 ,  C07D401/04 ,  C07D405/12 ,  C07D487/04

摘要： The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Het1, X, R1, R2, R3, R4 and R5 are as defined in the description.Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

摘要翻译： 本发明涉及磺酰胺衍生物，其在医学上的用途，含有它们的组合物，其制备方法以及在这些方法中使用的中间体。 更具体地，本发明涉及式（I）的新的磺酰胺Nav1.7抑制剂：或其药学上可接受的盐，其中Het1，X，R1，R2，R3，R4和R5如说明书中所定义。 Nav 1.7抑制剂可用于治疗各种疾病，特别是疼痛。

公开(公告)号：US20220259188A1

公开(公告)日：2022-08-18

申请号：US17614732

申请日：2020-06-01

申请人： Hua ZHOU ,  John J. ACTON, III ,  Michael J. ARDOLINO ,  Yi-Heng CHEN ,  Peter H. FULLER ,  Anmol GULATI ,  Rebecca Elizabeth JOHNSON ,  William P. KAPLAN ,  Solomon D. KATTAR ,  Mitchell H. KEYLOR ,  Derun LI ,  Kaitlyn Marie LOGAN ,  Min LU ,  Gregori J. MORRIELLO ,  Santhosh F. NEELAMKAVIL ,  Barbara PIO ,  Nunzio SCIAMMETTA ,  Vladimir SIMOV ,  Jing SU ,  Luis TORRES ,  Xin YAN ,  Merck Sharp & Dohme Corp.

发明人： Hua Zhou ,  John J. Acton, III ,  Michael J. Ardolino ,  Yi-Heng Chen ,  Peter H. Fuller ,  Anmol Gulati ,  Rebecca Elizabeth Johnson ,  William P. Kaplan ,  Solomon D. Kattar ,  Mitchell H. Keylor ,  Derun Li ,  Kaitlyn Marie Logan ,  Min Lu ,  Gregori J. Morriello ,  Santhosh F. Neelamkavil ,  Barbara Pio ,  Nunzio Sciammetta ,  Vladimir Simov ,  Jing Su ,  Luis Torres ,  Xin Yan

IPC分类号： C07D405/14 ,  C07D487/08 ,  C07D409/14 ,  C07D403/04 ,  C07D403/14 ,  C07D498/04 ,  C07D498/08 ,  C07D487/10 ,  C07D401/14 ,  C07D471/10 ,  C07D491/107 ,  C07D471/04 ,  C07D487/04 ,  A61P25/16

摘要： The present invention is directed to substituted certain 1-pyrazolyl, 5-, 6-disubstituted indazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, and ring A are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.

公开(公告)号：US08685977B2

公开(公告)日：2014-04-01

申请号：US13179585

申请日：2011-07-11

申请人： Andrew Simon Bell ,  Alan Daniel Brown ,  Russell Andrew Lewthwaite ,  Ian Roger Marsh ,  David Simon Millan ,  Manuel Perez Pacheco ,  David James Rawson ,  Nunzio Sciammetta ,  Robert Ian Storer ,  Paul Anthony Stupple ,  Nigel Alan Swain ,  Marcel John De Groot

发明人： Andrew Simon Bell ,  Alan Daniel Brown ,  Russell Andrew Lewthwaite ,  Ian Roger Marsh ,  David Simon Millan ,  Manuel Perez Pacheco ,  David James Rawson ,  Nunzio Sciammetta ,  Robert Ian Storer ,  Paul Anthony Stupple ,  Nigel Alan Swain ,  Marcel John De Groot

IPC分类号： A01N43/58 ,  A61K31/50 ,  A01N43/40 ,  A61K31/435 ,  A01N43/56 ,  A61K31/415 ,  A01N43/36 ,  A61K31/40

CPC分类号： C07C311/51 ,  C07C2601/02 ,  C07D231/12 ,  C07D233/60 ,  C07D237/08

摘要： The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Ar1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

摘要翻译： 本发明涉及磺酰胺衍生物，其在医学上的用途，含有它们的组合物，其制备方法以及在这些方法中使用的中间体。 更具体地，本发明涉及式（I）的新的磺酰胺Nav1.7抑制剂：或其药学上可接受的盐，其中Ar1，X，R1，R2，R3，R4和R5如说明书中所定义。 Nav 1.7抑制剂可用于治疗各种疾病，特别是疼痛。

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：US08592629B2

公开(公告)日：2013-11-26

申请号：US13179587

申请日：2011-07-11

申请人： Andrew Simon Bell ,  Alan Daniel Brown ,  Marcel John De Groot ,  Russell Andrew Lewthwaite ,  Ian Roger Marsh ,  David Simon Millan ,  Manuel Perez Pacheco ,  David James Rawson ,  Nunzio Sciammetta ,  Robert Ian Storer ,  Nigel Alan Swain ,  Steven Matthieu Gaulier

发明人： Andrew Simon Bell ,  Alan Daniel Brown ,  Marcel John De Groot ,  Russell Andrew Lewthwaite ,  Ian Roger Marsh ,  David Simon Millan ,  Manuel Perez Pacheco ,  David James Rawson ,  Nunzio Sciammetta ,  Robert Ian Storer ,  Nigel Alan Swain ,  Steven Matthieu Gaulier

IPC分类号： C07C303/00 ,  A61K31/18

CPC分类号： C07D213/69 ,  C07D213/63 ,  C07D213/64 ,  C07D213/65 ,  C07D213/70 ,  C07D213/74 ,  C07D213/85 ,  C07D215/20 ,  C07D231/56 ,  C07D239/47 ,  C07D401/04 ,  C07D405/12 ,  C07D487/04

摘要： This invention relates to sulfonamide derivative of formula (I), to their use in medicine, to compositions containing them, to processes for their preparation, and to intermediates used in such processes. These compounds are inhibitors of Nav1.7.

摘要翻译： 本发明涉及式（I）的磺酰胺衍生物，其在药物中的用途，含有它们的组合物，其制备方法以及在这些方法中使用的中间体。 这些化合物是Nav1.7的抑制剂。

公开(公告)号：US11319295B2

公开(公告)日：2022-05-03

申请号：US16753043

申请日：2018-10-04

申请人： MERCK SHARP & DOHME CORP. ,  Catherine M. White ,  Meredeth Ann McGowan ,  Yongxin Han ,  Nunzio Sciammetta

发明人： Catherine M. White ,  Meredeth Ann McGowan ,  Yongxin Han ,  Nunzio Sciammetta

IPC分类号： C07D305/08 ,  A61P37/00 ,  A61P25/28 ,  A61P31/12 ,  A61P25/24 ,  A61P27/12 ,  A61P35/00 ,  C07D307/22 ,  C07D307/24 ,  C07D405/04 ,  A61K45/06

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：US20200239423A1

公开(公告)日：2020-07-30

申请号：US16753043

申请日：2018-10-04

申请人： Catherine M. WHITE ,  Meredeth Ann MCGOWAN ,  Yongxin HAN ,  Nunzio SCIAMMETTA ,  MERCK SHARP & DOHME CORP.

发明人： Catherine M. White ,  Meredeth Ann McGowan ,  Yongxin Han ,  Nunzio Sciammetta

IPC分类号： C07D305/08 ,  C07D307/24 ,  C07D307/22 ,  C07D405/04 ,  A61P35/00 ,  A61P31/12 ,  A61P25/24 ,  A61P25/28 ,  A61P27/12 ,  A61P37/00

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：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.