公开(公告)号：US20210309671A1

公开(公告)日：2021-10-07

申请号：US17057875

申请日：2019-05-31

Applicant: Tao Yu ,  Alan Whitehead ,  Yili Chen ,  Chunrui Sun ,  Zhiy-ong Hu ,  Kake Zhao ,  Ronald M. Kim ,  John A. McCauley ,  MERCK SHARP & DOHME CORP.

Inventor： Tao YU ,  Alan WHITEHEAD ,  Yili CHEN ,  Chunrui SUN ,  Zhiyong HU ,  Kake ZHAO ,  Ronald M. KIM ,  John A. McCAULEY

IPC: C07D498/22 ,  C07D471/16 ,  C07D491/22 ,  A61K45/06 ,  A61P31/18

Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, where-in R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

公开(公告)号：US10442819B2

公开(公告)日：2019-10-15

申请号：US15532549

申请日：2015-12-01

Applicant: 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

Inventor： 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: A61K31/351 ,  A61K31/4353 ,  A61K31/5355 ,  A61K31/551 ,  C07D471/04 ,  C07D471/14 ,  C07D498/08 ,  C07D471/08 ,  C07D498/04 ,  C07D498/10 ,  A01N43/00

Abstract: 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.

公开(公告)号：US09126976B2

公开(公告)日：2015-09-08

申请号：US14239452

申请日：2012-08-13

Applicant: Rajan Anand ,  Vincent J. Colandrea ,  Maud Reiter ,  Petr Vachal ,  Aaron Zwicker ,  Jonathan E. Wilson ,  Fengqi Zhang ,  Kake Zhao

Inventor： Rajan Anand ,  Vincent J. Colandrea ,  Maud Reiter ,  Petr Vachal ,  Aaron Zwicker ,  Jonathan E. Wilson ,  Fengqi Zhang ,  Kake Zhao

IPC: A61K31/498 ,  C07D241/42 ,  C07D409/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D409/06 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D241/42 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06

Abstract: Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.

Abstract translation: 具有式Ia结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。

公开(公告)号：US20210395255A1

公开(公告)日：2021-12-23

申请号：US17292511

申请日：2019-11-15

Applicant: Zachary G. BRILL ,  Amjad ALI ,  Jared CUMMING ,  Duane DEMONG ,  Qiaolin DENG ,  Thomas H. GRAHAM ,  Rongze KUANG ,  Yeon-Hee LIM ,  Christopher W. PLUMMER ,  Jenny Lorena RICO DUQUE ,  Huijun WANG ,  Yonglian ZHANG ,  Kake ZHAO ,  Merck Sharp & Dohme Corp.

Inventor： Zachary G. Brill ,  Amjad Ali ,  Jared Cumming ,  Duane DeMong ,  Qiaolin Deng ,  Thomas H. Graham ,  Rongze Kuang ,  Yeon-Hee Lim ,  Christopher W. Plummer ,  Jenny Lorena Rico Duque ,  Huijun Wang ,  Yonglian Zhang ,  Kake Zhao

IPC: C07D487/04 ,  C07K16/28

Abstract: In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): or and pharmaceutically acceptable salts thereof, wherein, R1, R2, and R3 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US20140057893A1

公开(公告)日：2014-02-27

申请号：US14110332

申请日：2012-04-05

Applicant: Scott Edmondson ,  Zhiqiang Guo ,  Harold B. Wood ,  Andrew W. Stamford ,  Michael W. Miller ,  Duane E. DeMong ,  Gregori J. Morriello ,  Rajan Anand ,  Vincent J. Colandrea ,  Megan Macala ,  Milana Maletic ,  Cheng Zhu ,  Yuping Zhu ,  Wanying Sun ,  Kake Zhao ,  Yong Huang ,  Joel M. Harris ,  Lehua Chang ,  Nam Fung Kar ,  Zhiyong Hu ,  Liping Wang ,  Bowei Wang ,  Ping Liu ,  Jason W. Szewczyk ,  William B. Geiss

Inventor： Scott Edmondson ,  Zhiqiang Guo ,  Harold B. Wood ,  Andrew W. Stamford ,  Michael W. Miller ,  Duane E. DeMong ,  Gregori J. Morriello ,  Rajan Anand ,  Vincent J. Colandrea ,  Megan Macala ,  Milana Maletic ,  Cheng Zhu ,  Yuping Zhu ,  Wanying Sun ,  Kake Zhao ,  Yong Huang ,  Joel M. Harris ,  Lehua Chang ,  Nam Fung Kar ,  Zhiyong Hu ,  Liping Wang ,  Bowei Wang ,  Ping Liu ,  Jason W. Szewczyk ,  William B. Geiss

IPC: C07D513/04 ,  C07D413/14 ,  C07D413/04 ,  C07D498/04 ,  C07D405/04 ,  C07D471/04 ,  C07D487/04 ,  C07D401/12 ,  C07D211/22

CPC classification number: C07D513/04 ,  A61K9/4858 ,  C07D211/22 ,  C07D401/12 ,  C07D405/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included

Abstract translation: 公开了取代的式I的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法

公开(公告)号：US11884683B2

公开(公告)日：2024-01-30

申请号：US17057875

申请日：2019-05-31

Applicant: Merck Sharp & Dohme LLC ,  Tao Yu ,  Alan Whitehead ,  Yili Chen ,  Chunrui Sun ,  Zhiyong Hu ,  Kake Zhao ,  Ronald M. Kim ,  John A. McCauley

Inventor： Tao Yu ,  Alan Whitehead ,  Yili Chen ,  Chunrui Sun ,  Zhiyong Hu ,  Kake Zhao ,  Ronald M. Kim ,  John A. McCauley

IPC: C07D498/22 ,  C07D471/16 ,  C07D491/22 ,  A61P31/18 ,  A61K45/06

CPC classification number: C07D498/22 ,  A61K45/06 ,  A61P31/18 ,  C07D471/16 ,  C07D491/22

Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

公开(公告)号：US09221834B2

公开(公告)日：2015-12-29

申请号：US13881896

申请日：2011-10-25

Applicant: Zhijian Lu ,  Yi-Heng Chen ,  Cameron Smith ,  Hong Li ,  Christopher F. Thompson ,  Julianne Hunt ,  Florida Kallashi ,  Ramzi Sweis ,  Peter Sinclair ,  Samantha E. Adamson ,  Guizhen Dong ,  Debra L. Ondeyka ,  Xiaoxia Qian ,  Wanying Sun ,  Petr Vachal ,  Kake Zhao

Inventor： Zhijian Lu ,  Yi-Heng Chen ,  Cameron Smith ,  Hong Li ,  Christopher F. Thompson ,  Julianne Hunt ,  Florida Kallashi ,  Ramzi Sweis ,  Peter Sinclair ,  Samantha E. Adamson ,  Guizhen Dong ,  Debra L. Ondeyka ,  Xiaoxia Qian ,  Wanying Sun ,  Petr Vachal ,  Kake Zhao

IPC: A61K31/4439 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/444 ,  C07D491/08 ,  C07D417/14 ,  C07D413/14 ,  A61K31/42 ,  A61K45/06 ,  C07D413/06

CPC classification number: C07D491/08 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  A61K2300/00

Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, A3 is a substituted phenyl group or indanyl group. Formula (I).

Abstract translation: 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。 在式I的化合物中，A3是取代的苯基或茚满基。 式（I）。

公开(公告)号：US08957062B2

公开(公告)日：2015-02-17

申请号：US14110332

申请日：2012-04-05

Applicant: Scott Edmondson ,  Zhiqiang Guo ,  Harold B. Wood ,  Andrew W. Stamford ,  Michael W. Miller ,  Duane E. DeMong ,  Gregori J. Morriello ,  Rajan Anand ,  Vincent J. Colandrea ,  Megan Macala ,  Milana Maletic ,  Cheng Zhu ,  Yuping Zhu ,  Wanying Sun ,  Kake Zhao ,  Yong Huang ,  Joel M. Harris ,  Lehua Chang ,  Nam Fung Kar ,  Zhiyong Hu ,  Liping Wang ,  Bowei Wang ,  Ping Liu ,  Jason W. Szewczyk ,  William B. Geiss

Inventor： Scott Edmondson ,  Zhiqiang Guo ,  Harold B. Wood ,  Andrew W. Stamford ,  Michael W. Miller ,  Duane E. DeMong ,  Gregori J. Morriello ,  Rajan Anand ,  Vincent J. Colandrea ,  Megan Macala ,  Milana Maletic ,  Cheng Zhu ,  Yuping Zhu ,  Wanying Sun ,  Kake Zhao ,  Yong Huang ,  Joel M. Harris ,  Lehua Chang ,  Nam Fung Kar ,  Zhiyong Hu ,  Liping Wang ,  Bowei Wang ,  Ping Liu ,  Jason W. Szewczyk ,  William B. Geiss

IPC: C07D513/04 ,  C07D401/12 ,  C07D413/14 ,  C07D413/04 ,  C07D211/22 ,  C07D405/04 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  A61K9/48 ,  C07D417/14 ,  C07D495/04

CPC classification number: C07D513/04 ,  A61K9/4858 ,  C07D211/22 ,  C07D401/12 ,  C07D405/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.

Abstract translation: 公开了取代的式I的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病症。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法。

公开(公告)号：US20130331372A1

公开(公告)日：2013-12-12

申请号：US13881896

申请日：2011-10-25

Applicant: Zhijian Lu ,  Yi-Heng Chen ,  Cameron Smith ,  Hong Li ,  Christopher F. Thompson ,  Julianne Hunt ,  Florida Kallashi ,  Ramzi Sweis ,  Peter Sinclair ,  Samantha E. Adamson ,  Guizhen Dong ,  Debra L. Ondeyka ,  Xiaoxia Qian ,  Wanying Sun ,  Petr Vachal ,  Kake Zhao

Inventor： Zhijian Lu ,  Yi-Heng Chen ,  Cameron Smith ,  Hong Li ,  Christopher F. Thompson ,  Julianne Hunt ,  Florida Kallashi ,  Ramzi Sweis ,  Peter Sinclair ,  Samantha E. Adamson ,  Guizhen Dong ,  Debra L. Ondeyka ,  Xiaoxia Qian ,  Wanying Sun ,  Petr Vachal ,  Kake Zhao

IPC: C07D491/08 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/497 ,  C07D417/14 ,  C07D413/14 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/506

CPC classification number: C07D491/08 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  A61K2300/00

Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, A3 is a substituted phenyl group or indanyl group. Formula (I).

Abstract translation: 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。 在式I的化合物中，A3是取代的苯基或茚满基。 式（I）。