公开(公告)号：US11319283B2

公开(公告)日：2022-05-03

申请号：US16753035

申请日：2018-10-04

Applicant: 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

Inventor： 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: 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

Abstract: 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

Applicant: 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

Inventor： 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: C07D271/08 ,  C07D413/12

Abstract: 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：US20190175602A1

公开(公告)日：2019-06-13

申请号：US16326039

申请日：2017-08-14

Applicant: Wensheng Yu ,  LING Tong ,  Joseph A. Koziowski ,  Craig: A Coburn ,  De-yi J. Yang ,  Deyou Sha ,  Jae-Hun. Kim ,  Michael Dwyer ,  Kartik M. Keertikar ,  Bin Hu ,  Bin Zhong ,  Jinglai Hao ,  Dahai Wang

Inventor： Wensheng Yu ,  LING Tong ,  Joseph A. Koziowski ,  Craig: A Coburn ,  De-yi J. Yang ,  Deyou Sha ,  Jae-Hun. Kim ,  Michael Dwyer ,  Kartik M. Keertikar ,  Bin Hu ,  Bin Zhong ,  Jinglai Hao ,  Dahai Wang

IPC: A61K31/5365 ,  C07D498/04 ,  A61P31/14 ,  A61K31/4995 ,  C07D519/00

Abstract: The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A′, R2 R3 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Heterocycle-Substituted Tetra-cyclic Compound, and methods of using the Heterocycle-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient.

公开(公告)号：US20190002480A1

公开(公告)日：2019-01-03

申请号：US16064268

申请日：2016-12-16

Applicant: Joseph A. KOZLOWSKI ,  Wensheng YU ,  Merck Sharp & Dohme Corp.

Inventor： Joseph A. Kozlowski ,  Wensheng Yu

IPC: C07F7/08 ,  C07D498/04 ,  A61P31/14

Abstract: The present invention relates to novel Silane-Containing Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A′, B, B′, R1 R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Silane-Containing Heterocyclic Compound, and methods of using the Silane-Containing Heterocyclic Compounds for treating or preventing HCV infection in a patient.

公开(公告)号：US20140378416A1

公开(公告)日：2014-12-25

申请号：US14345114

申请日：2012-09-11

Applicant: Michael P. Dwyer ,  Kartik M. Keertikar ,  Qingbei Zeng ,  Robert D. Mazzola, JR. ,  Wensheng Yu ,  Haiqun Tang ,  Seong Heon Kim ,  Ling Tong ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Anilkumar Gopinadhan Nair

Inventor： Michael P. Dwyer ,  Kartik M. Keertikar ,  Qingbei Zeng ,  Robert D. Mazzola, JR. ,  Wensheng Yu ,  Haiqun Tang ,  Seong Heon Kim ,  Ling Tong ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Anilkumar Gopinadhan Nair

IPC: C07F7/10 ,  A61K45/06 ,  A61K31/695

CPC classification number: C07F7/10 ,  A61K31/695 ,  A61K45/06 ,  A61K2201/094 ,  A61K2300/00 ,  C07F7/0816

Abstract: The present invention relates to novel Silyl-Containing Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, D, E, F and L are as defined herein. The present invention also relates to compositions comprising at least one Silyl-Containing Heterocyclic Compound, and methods of using the Silyl-Containing Heterocyclic Compounds for treating or preventing HCV infection in a patient.

Abstract translation: 本发明涉及式（I）的新的含甲硅烷基的杂环化合物及其药学上可接受的盐，其中A，B，C，D，E，F和L如本文所定义。 本发明还涉及包含至少一种含甲硅烷基的杂环化合物的组合物，以及使用含有甲硅烷基的杂环化合物治疗或预防患者HCV感染的方法。

公开(公告)号：US08609635B2

公开(公告)日：2013-12-17

申请号：US13041082

申请日：2011-03-04

Applicant: Anilkumar Gopinadhan Nair ,  Kartik M. Keertikar ,  Seong Heon Kim ,  Joseph A. Kozlowski ,  Stuart Rosenblum ,  Oleg B. Selyutin ,  Michael Wong ,  Wensheng Yu ,  Qingbei Zeng

Inventor： Anilkumar Gopinadhan Nair ,  Kartik M. Keertikar ,  Seong Heon Kim ,  Joseph A. Kozlowski ,  Stuart Rosenblum ,  Oleg B. Selyutin ,  Michael Wong ,  Wensheng Yu ,  Qingbei Zeng

IPC: A61K31/695 ,  C07F7/10

CPC classification number: C07F7/0816

Abstract: The present invention relates to novel Fused Tricyclic Silyl Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, D, M1, X1 and X2 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Silyl Compound, and methods of using the Fused Tricyclic Silyl Compounds for treating or preventing HCV infection in a patient.

Abstract translation: 本发明涉及式（I）的新型稠合三环甲硅烷基化合物及其药学上可接受的盐，其中A，B，C，D，M1，X1和X2如本文所定义。 本发明还涉及包含至少一种熔融三环甲硅烷基化合物的组合物，以及使用融合的三环甲硅烷基化合物治疗或预防患者HCV感染的方法。

公开(公告)号：US08569336B2

公开(公告)日：2013-10-29

申请号：US13127953

申请日：2009-11-09

Applicant: Ling Tong ,  Brian J. Lavey ,  Bandarpalle B. Shankar ,  Seong Heon Kim ,  Wensheng Yu ,  Joseph A. Kozlowski ,  Michael K. C. Wong ,  Lei Chen ,  Guowei Zhou ,  Razia K. Rizvi ,  Robert Feltz ,  Aneta Maria Kosinski ,  De-Yi Yang ,  Chaoyang Dai ,  Luke Fire ,  Vinay Girijavallabhan ,  Dansu Li ,  Janeta Popovici-Muller ,  Judson E. Richard ,  Kristin E. Rosner ,  M. Arshad Siddiqui ,  Liping Yang

Inventor： Ling Tong ,  Brian J. Lavey ,  Bandarpalle B. Shankar ,  Seong Heon Kim ,  Wensheng Yu ,  Joseph A. Kozlowski ,  Michael K. C. Wong ,  Lei Chen ,  Guowei Zhou ,  Razia K. Rizvi ,  Robert Feltz ,  Aneta Maria Kosinski ,  De-Yi Yang ,  Chaoyang Dai ,  Luke Fire ,  Vinay Girijavallabhan ,  Dansu Li ,  Janeta Popovici-Muller ,  Judson E. Richard ,  Kristin E. Rosner ,  M. Arshad Siddiqui ,  Liping Yang

IPC: A61K31/4166 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/506 ,  C07D233/76 ,  C07D213/24

CPC classification number: C07D498/04 ,  C07D513/00 ,  C07D519/00

Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.

Abstract translation: 本发明涉及式（I）的化合物：（化学式应该插在这里，它以纸的形式出现）（I）或其药学上可接受的盐，其可用于治疗疾病或病症介导 通过MMP，ADAM，TACE，聚蛋白聚糖蛋白聚糖酶，TNF-或其组合。

公开(公告)号：US07652020B2

公开(公告)日：2010-01-26

申请号：US11142601

申请日：2005-06-01

Applicant: Zhuyan Guo ,  Peter Orth ,  Zhaoning Zhu ,  Robert D. Mazzola ,  Tin-Yau Chan ,  Henry A. Vaccaro ,  Brian McKittrick ,  Joseph A. Kozlowski ,  Brian J. Lavey ,  Guowei Zhou ,  Sunil Paliwal ,  Shing-Chun Wong ,  Neng-Yang Shih ,  Pauline C. Ting ,  Kristin E. Rosner ,  Gerald W. Shipps, Jr. ,  M. Arshad Siddiqui ,  David B. Belanger ,  Chaoyang Dai ,  Dansu Li ,  Vinay M. Girijavallabhan ,  Janeta Popovici-Muller ,  Wensheng Yu ,  Lianyun Zhao

Inventor： Zhuyan Guo ,  Peter Orth ,  Zhaoning Zhu ,  Robert D. Mazzola ,  Tin-Yau Chan ,  Henry A. Vaccaro ,  Brian McKittrick ,  Joseph A. Kozlowski ,  Brian J. Lavey ,  Guowei Zhou ,  Sunil Paliwal ,  Shing-Chun Wong ,  Neng-Yang Shih ,  Pauline C. Ting ,  Kristin E. Rosner ,  Gerald W. Shipps, Jr. ,  M. Arshad Siddiqui ,  David B. Belanger ,  Chaoyang Dai ,  Dansu Li ,  Vinay M. Girijavallabhan ,  Janeta Popovici-Muller ,  Wensheng Yu ,  Lianyun Zhao

IPC: A61K31/519 ,  A61K31/506 ,  A61K31/4709 ,  A61K31/43 ,  A61K31/4245 ,  C07D413/00 ,  C07D241/36 ,  C07D471/00 ,  C07D295/00 ,  C07D471/02 ,  C07D401/00 ,  C07D513/00 ,  C07D277/22 ,  C07D277/62 ,  C07D263/30 ,  C07D261/06 ,  C07D235/00 ,  C07D209/04 ,  C07D207/00 ,  C07D205/00 ,  C07D409/00 ,  C07D307/00

CPC classification number: C07D409/14 ,  C07C235/06 ,  C07C235/08 ,  C07C235/10 ,  C07C2601/08 ,  C07D207/20 ,  C07D207/26 ,  C07D209/44 ,  C07D215/14 ,  C07D217/06 ,  C07D263/32 ,  C07D295/185 ,  C07D307/52 ,  C07D333/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D513/04

Abstract: 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-α or combinations thereof.

Abstract translation: 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-α或其组合介导的疾病或病症。

公开(公告)号：US20060276448A1

公开(公告)日：2006-12-07

申请号：US11353474

申请日：2006-02-14

Applicant: Qingbei Zeng ,  De-Yi Yang ,  Stuart Rosenblum ,  Michael Wong ,  Gopinadhan Anilkumar ,  Seong Kim ,  Wensheng Yu ,  Joseph Kozlowski ,  Neng-Yang Shih ,  Brian McGuinness ,  Lisa Guise-Zawacki ,  Doublas Hobbs

Inventor： Qingbei Zeng ,  De-Yi Yang ,  Stuart Rosenblum ,  Michael Wong ,  Gopinadhan Anilkumar ,  Seong Kim ,  Wensheng Yu ,  Joseph Kozlowski ,  Neng-Yang Shih ,  Brian McGuinness ,  Lisa Guise-Zawacki ,  Doublas Hobbs

IPC: A61K31/5377 ,  A61K31/506 ,  A61K31/497 ,  C07D413/14 ,  C07D403/14

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts or solvates of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates or esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

Abstract translation: 本申请公开了所述化合物或所述前药的所述化合物或其对映异构体，立体异构体，旋转异构体，互变异构体，外消旋体或前药，或所述前药的所述化合物，所述化合物具有式1所示的一般结构：和 其药学上可接受的盐，溶剂合物或酯。 还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的 例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括同种异体移植排斥反应，异种移植排斥），感染性疾病（例如结核性麻风病），固定药物喷发，皮肤迟发型超敏反应 应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

公开(公告)号：US06953780B2

公开(公告)日：2005-10-11

申请号：US10312012

申请日：2001-06-21

Applicant: Keliang Liu ,  Wensheng Yu ,  Yuanjun Liang ,  Hai Wang ,  Yufen Zhao ,  Zhenkai Ding

Inventor： Keliang Liu ,  Wensheng Yu ,  Yuanjun Liang ,  Hai Wang ,  Yufen Zhao ,  Zhenkai Ding

IPC: A61K38/00 ,  A61P9/00 ,  C07K7/06 ,  A61K38/06 ,  C07K5/083 ,  C07K5/097

CPC classification number: C07K7/06 ,  A61K38/00

Abstract: The instant invention relates to some tripeptide derivatives having activity against endothelin a process for preparing them, pharmaceutical composition containing the same and their use in prevention or treatment of some diseases associated with endothelin.

Abstract translation: 本发明涉及具有抗内皮素活性的一些三肽衍生物，其制备方法，含有该三肽衍生物的方法，含有该三肽衍生物的药物组合物及其在预防或治疗与内皮素相关的一些疾病中的用途。