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：US11161854B2

公开(公告)日：2021-11-02

申请号：US16755172

申请日：2018-10-08

申请人： Merck Sharp & Dohme Corp. ,  David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

发明人： David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

IPC分类号： C07D491/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/08 ,  C07D498/04 ,  C07D498/10 ,  C07D519/00

摘要： The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z 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 such diseases in which LRRK-2 kinase is involved.

公开(公告)号：US20210188863A1

公开(公告)日：2021-06-24

申请号：US16755172

申请日：2018-10-08

申请人： David Annunziato CANDITO ,  Thomas, H. GRAHAM ,  John ACTON ,  Ryan Wing-Kun CHAU ,  Joanna L. CHEN ,  J. Michael ELLIS ,  Peter H. FULLER ,  Anmol GULATI ,  Hakan GUNAYDIN ,  Solomon KATTAR ,  Mitchell Henry KEYLOR ,  Blair T. LAPOINTE ,  Ping LIU ,  Weiguo LIU ,  Joey L. METHOT ,  Santhosh F. NEELAMKAVIL ,  Vladimir SIMOV ,  Ling TONG ,  Harold B. WOOD ,  Merck Sharp & Dohme Corp.

发明人： David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

IPC分类号： C07D491/10 ,  C07D403/14 ,  C07D487/08 ,  C07D405/14 ,  C07D401/14 ,  C07D413/14 ,  C07D498/10 ,  C07D519/00 ,  C07D498/04 ,  C07D403/04

摘要： The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z 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 such diseases in which LRRK-2 kinase is involved.

公开(公告)号：US07687527B2

公开(公告)日：2010-03-30

申请号：US12338425

申请日：2008-12-18

申请人： Wensheng Yu ,  Ling Tong ,  Lei Chen ,  Joseph A. Kozlowski ,  Brian J. Lavey ,  Neng-Yang Shih ,  Vincent S. Madison ,  Guowei Zhou ,  Peter Orth ,  Zhuyan Guo ,  Michael K. C. Wong ,  De-Yi Yang ,  Seong Heon Kim ,  Bandarpalle B. Shankar ,  M. Arshad Siddiqui ,  Kristin E. Rosner ,  Chaoyang Dai ,  Umar Faruk Mansoor ,  Janeta Popovici-Muller ,  Vinay M. Girijavallabhan ,  Dansu Li

发明人： Wensheng Yu ,  Ling Tong ,  Lei Chen ,  Joseph A. Kozlowski ,  Brian J. Lavey ,  Neng-Yang Shih ,  Vincent S. Madison ,  Guowei Zhou ,  Peter Orth ,  Zhuyan Guo ,  Michael K. C. Wong ,  De-Yi Yang ,  Seong Heon Kim ,  Bandarpalle B. Shankar ,  M. Arshad Siddiqui ,  Kristin E. Rosner ,  Chaoyang Dai ,  Umar Faruk Mansoor ,  Janeta Popovici-Muller ,  Vinay M. Girijavallabhan ,  Dansu Li

IPC分类号： A61K31/415 ,  A61K31/425

CPC分类号： C07D403/06 ,  C07D401/14 ,  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：US20090170875A1

公开(公告)日：2009-07-02

申请号：US12338425

申请日：2008-12-18

申请人： Wensheng Yu ,  Ling Tong ,  Lei Chen ,  Joseph A. Kozlowski ,  Brian J. Lavey ,  Neng-Yang Shih ,  Vincent S. Madison ,  Guowei Zhou ,  Peter Orth ,  Zhuyan Guo ,  Michael K.C. Wong ,  De-Yi Yang ,  Seong Heon Kim ,  Bandarpalle B. Shankar ,  M. Arshad Siddiqui ,  Kristin E. Rosner ,  Chaoyang Dai ,  Umar Faruk Mansoor ,  Janeta Popovici-Muller ,  Vinay M. Girijavallabhan ,  Dansu Li

发明人： Wensheng Yu ,  Ling Tong ,  Lei Chen ,  Joseph A. Kozlowski ,  Brian J. Lavey ,  Neng-Yang Shih ,  Vincent S. Madison ,  Guowei Zhou ,  Peter Orth ,  Zhuyan Guo ,  Michael K.C. Wong ,  De-Yi Yang ,  Seong Heon Kim ,  Bandarpalle B. Shankar ,  M. Arshad Siddiqui ,  Kristin E. Rosner ,  Chaoyang Dai ,  Umar Faruk Mansoor ,  Janeta Popovici-Muller ,  Vinay M. Girijavallabhan ,  Dansu Li

IPC分类号： A61K31/497 ,  C07D403/06 ,  A61K31/4166 ,  A61K31/4709 ,  C07D403/14 ,  C07D401/14 ,  C07D417/14 ,  A61K31/427

CPC分类号： C07D403/06 ,  C07D401/14 ,  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.

公开(公告)号：US07504424B2

公开(公告)日：2009-03-17

申请号：US11333663

申请日：2006-01-17

申请人： Wensheng Yu ,  Ling Tong ,  Lei Chen ,  Joseph A. Kozlowski ,  Brian J. Lavey ,  Neng-Yang Shih ,  Vincent S. Madison ,  Guowei Zhou ,  Peter Orth ,  Zhuyan Guo ,  Michael K. C. Wong ,  De-Yi Yang ,  Seong Heon Kim ,  Bandarpalle B. Shankar ,  M. Arshad Siddiqui ,  Kristin E. Rosner ,  Chaoyang Dai ,  Umar Faruk Mansoor ,  Janeta Popovici-Muller ,  Vinay M. Girijavallabhan ,  Dansu Li

发明人： Wensheng Yu ,  Ling Tong ,  Lei Chen ,  Joseph A. Kozlowski ,  Brian J. Lavey ,  Neng-Yang Shih ,  Vincent S. Madison ,  Guowei Zhou ,  Peter Orth ,  Zhuyan Guo ,  Michael K. C. Wong ,  De-Yi Yang ,  Seong Heon Kim ,  Bandarpalle B. Shankar ,  M. Arshad Siddiqui ,  Kristin E. Rosner ,  Chaoyang Dai ,  Umar Faruk Mansoor ,  Janeta Popovici-Muller ,  Vinay M. Girijavallabhan ,  Dansu Li

IPC分类号： A61K31/416 ,  A61K31/428 ,  C07D209/04 ,  C07D231/08 ,  C07D275/04 ,  C07D417/14 ,  C07D513/12

CPC分类号： C07D403/06 ,  C07D401/14 ,  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：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：US20050282861A1

公开(公告)日：2005-12-22

申请号：US11197979

申请日：2005-08-05

申请人： Richard Friary ,  Joseph Kozlowski ,  Bandarpalle Shankar ,  Michael Wong ,  Guowei Zhou ,  Brian Lavey ,  Neng-Yang Shih ,  Ling Tong ,  Lei Chen ,  Youhen Shu

发明人： Richard Friary ,  Joseph Kozlowski ,  Bandarpalle Shankar ,  Michael Wong ,  Guowei Zhou ,  Brian Lavey ,  Neng-Yang Shih ,  Ling Tong ,  Lei Chen ,  Youhen Shu

IPC分类号： A61K31/445 ,  A61K31/4535 ,  A61K31/454 ,  A61K45/00 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P27/06 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P37/08 ,  C07D211/26 ,  C07D211/96 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

CPC分类号： C07D401/12 ,  C07D211/26 ,  C07D211/96 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： There are disclosed compounds of the formula I: or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.

摘要翻译： 公开了具有抗炎和免疫调节活性的式I化合物或化合物的药学上可接受的盐。 还公开了含有所述化合物的药物组合物。

公开(公告)号：US20070197564A1

公开(公告)日：2007-08-23

申请号：US11653511

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 ,  Razia Rizvi ,  Lei Chen ,  De-Yi Yang ,  Robert Feltz ,  Seong-Heon Kim

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 ,  Razia Rizvi ,  Lei Chen ,  De-Yi Yang ,  Robert Feltz ,  Seong-Heon Kim

IPC分类号： A61K31/52 ,  C07D471/02 ,  A61K31/4745 ,  A61K31/513 ,  A61K31/519 ,  C07D473/02 ,  C07D487/02

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，溶剂合物或异构体，其可用于治疗由MMP，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：US20060276506A1

公开(公告)日：2006-12-07

申请号：US11333663

申请日：2006-01-17

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 ,  Umar Mansoor ,  Janeta Popovici-Muller ,  Vinay Girijavallabhan ,  Dansu Li

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 ,  Umar Mansoor ,  Janeta Popovici-Muller ,  Vinay Girijavallabhan ,  Dansu Li

IPC分类号： A61K31/4709 ,  A61K31/4245 ,  A61K31/4178 ,  C07D413/14 ,  C07D403/02

CPC分类号： C07D403/06 ,  C07D401/14 ,  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.