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：US20240246937A1

公开(公告)日：2024-07-25

申请号：US18556196

申请日：2022-04-28

申请人： George Madalin GIAMBASU ,  Andrew M. HAIDLE ,  Brett A. HOPKINS ,  James P. JEWELL ,  Matthew A. LARSEN ,  Charles A. LESBURG ,  Ping LIU ,  Qinglin PU ,  Sulagna SANYAL ,  Phieng SILIPHAIVANH ,  Matthew TUDOR ,  Catherine M. WHITE ,  Xin YAN ,  Lianyun ZHAO ,  Xiao Mei ZHENG ,  William P. KAPLAN ,  Michaelyn Claire LUX ,  Derun LI ,  Rebecca JOHNSON ,  MERCK SHARP & DOHME LLC ,  MSD R&D (CHINA) CO., LTD.

发明人： George Madalin GIAMBASU ,  Andrew M. HAIDLE ,  Brett A. HOPKINS ,  James P. JEWELL ,  Matthew A. LARSEN ,  Charles A. LESBURG ,  Ping LIU ,  Qinglin PU ,  Sulagna SANYAL ,  Phieng SILIPHAIVANH ,  Matthew TUDOR ,  Catherine M. WHITE ,  Xin YAN ,  Lianyun ZHAO ,  Xiao Mei ZHENG ,  William P. KAPLAN ,  Michaelyn Claire LUX ,  Derun LI ,  Rebecca JOHNSON

IPC分类号： C07D403/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D487/04

CPC分类号： C07D403/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D487/04

摘要： The invention discloses a synthesizing method of benzimidazole derivant and intermediate, which is characterized by the following: proceeding arylation among aryl halide and primary amine; adopting L-pro as additive, cuprous iodide as catalyst; proceeding molecular arylation coupling reaction for aryl iodide or aryl bromide and primary amine; adopting iodo phenylamine compound and bromophenylamine compound as starting material; synthesizing the material through several-step transformation.

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：US08334405B2

公开(公告)日：2012-12-18

申请号：US12080634

申请日：2008-04-03

申请人： Derun Li ,  John R. Falck

发明人： Derun Li ,  John R. Falck

IPC分类号： C07C335/00

CPC分类号： C07C335/16 ,  C07B2200/07 ,  C07B2200/09 ,  C07C29/143 ,  C07C335/08 ,  C07C335/14 ,  C07C335/18 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/10 ,  C07C2602/42 ,  C07D295/185 ,  C07C31/1355 ,  C07C33/14 ,  C07C33/18 ,  C07C33/20 ,  C07C33/22 ,  C07C33/30 ,  C07C33/46 ,  C07C35/36

摘要： Chiral thioureas are effective catalysts for the borane reduction of prochiral ketones to optically active alcohols. A prochiral ketone may be reduced to an optically active alcohol in the presence of a substantially sub-stoichiometric amount of chiral thiourea. The asymmetric thiourea compound of the present invention may be produced according to a production method described herein.

摘要翻译： 手性硫脲是将前手性酮还原成旋光醇的有效催化剂。 在大致亚化学计量的手性硫脲的存在下，前手性酮可以还原成光学活性的醇。 本发明的不对称硫脲化合物可以根据本文所述的制备方法制备。

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：US09695198B2

公开(公告)日：2017-07-04

申请号：US14652150

申请日：2013-12-16

申请人： Cameron James Smith ,  Edward Sherer ,  Louis-Charles Campeau ,  James Balkovec ,  William John Greenlee ,  Derun Li ,  Liangqin Guo ,  Tin-Yau Chan ,  Yi-Heng Chen ,  Yili Chen ,  Samuel Chackalamannil ,  John Qiang Tan ,  Tomokazu Hirabayashi ,  Mika Sekioka ,  MERCK SHARP & DOHME CORP. ,  MOCHIDA PHARMACEUTICAL CO., LTD.

发明人： Cameron James Smith ,  Edward Sherer ,  Louis-Charles Campeau ,  James Balkovec ,  William John Greenlee ,  Derun Li ,  Liangqin Guo ,  Tin-Yau Chan ,  Yi-Heng Chen ,  Yili Chen ,  Samuel Chackalamannil ,  John Qiang Tan ,  Tomokazu Hirabayashi ,  Mika Sekioka

IPC分类号： C07D413/14 ,  C07D417/06 ,  C07D498/04 ,  C07D513/04 ,  C07D413/12 ,  C07D471/04 ,  C07D413/06

CPC分类号： C07D513/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D498/04

摘要： The present invention provides a compound of Formula (I) where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.

公开(公告)号：US20150368269A1

公开(公告)日：2015-12-24

申请号：US14652150

申请日：2013-12-16

申请人： Tomokazu HIRABAYASHI ,  Mika KATSUNO ,  Cameron James SMITH ,  Edward SHERER ,  Louis-Charles CAMPEAU ,  James BALKOVEC ,  William John GREENLEE ,  Derun LI ,  Liangqin GUO ,  Tin Yan CHAN ,  Yi-Heng CHEN ,  Yili CHEN ,  Samuel CHACKALAMANNIL ,  John Qiang TAN ,  MERCH SHARP & DOHME CORP. ,  MOCHIDA PHARMACEUTICAL CO., LTD.

发明人： Cameron James Smith ,  Edward Sherer ,  Louis-Charles Campeau ,  James Balkovec ,  William John Greenlee ,  Derun Li ,  Liangqin Guo ,  Tin-Yau Chan ,  Yi-Heng Chen ,  Yili Chen ,  Samuel Chackalamannil ,  John Qiang Tan ,  Tomokazu Hirabayashi ,  Mika Sekioka

IPC分类号： C07D513/04 ,  C07D417/06 ,  C07D413/06 ,  C07D498/04 ,  C07D471/04

CPC分类号： C07D513/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D498/04

摘要： The present invention provides a compound of Formula (I) where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.

摘要翻译： 本发明提供式（I）化合物，其中A为杂环环系，B为杂环环系或芳环系，以及包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防的方法 血栓形成，栓塞，高凝状态或纤维化变化。

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：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：US10414774B2

公开(公告)日：2019-09-17

申请号：US16324596

申请日：2017-08-10

申请人： Merck Sharp & Dohme Corp. ,  Jared N. Cumming ,  Kevin D. Dykstra ,  Alan Hruza ,  Derun Li ,  Hong Liu ,  Haiqun Tang ,  Brandon M. Taoka ,  Andreas Verras ,  Shawn P. Walsh ,  Wen-Lian Wu

发明人： Jared N. Cumming ,  Kevin D. Dykstra ,  Alan Hruza ,  Derun Li ,  Hong Liu ,  Haiqun Tang ,  Brandon M. Taoka ,  Andreas Verras ,  Shawn P. Walsh ,  Wen-Lian Wu

IPC分类号： C07D487/04 ,  C07D519/00 ,  A61P3/10 ,  C07D498/04 ,  C07D513/04 ,  C07D471/04

摘要： Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.