公开(公告)号：US11884683B2

公开(公告)日：2024-01-30

申请号：US17057875

申请日：2019-05-31

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

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

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

CPC分类号： C07D498/22 ,  A61K45/06 ,  A61P31/18 ,  C07D471/16 ,  C07D491/22

摘要： 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：US11225471B2

公开(公告)日：2022-01-18

申请号：US15733056

申请日：2018-11-12

申请人： Steven L. Colletti ,  Duane DeMong ,  Kevin D. Dykstra ,  Zhiyong Hu ,  Michael Miller ,  Merck Sharp & Dohme Corp.

发明人： Steven L. Colletti ,  Duane DeMong ,  Kevin D. Dykstra ,  Zhiyong Hu ,  Michael Miller

IPC分类号： C07D405/14 ,  A61P3/10

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia Formula (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

申请人： 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

发明人： 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分类号： 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分类号： C07D513/04 ,  A61K9/4858 ,  C07D211/22 ,  C07D401/12 ,  C07D405/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

摘要： 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.

摘要翻译： 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：US20140128368A1

公开(公告)日：2014-05-08

申请号：US14126685

申请日：2012-06-11

申请人： Michael Miller ,  Andrew Stamford ,  Kallol Basu ,  Harold B. Wood ,  Duane DeMong ,  Wanying Sun ,  Joie Garfunkle ,  Christopher Moyes ,  Zhiyong Hu ,  Ping Liu ,  Scott D. Edmondson ,  Xing Dai ,  Byron Gabriel DuBois

发明人： Michael Miller ,  Andrew Stamford ,  Kallol Basu ,  Harold B. Wood ,  Duane DeMong ,  Wanying Sun ,  Joie Garfunkle ,  Christopher Moyes ,  Zhiyong Hu ,  Ping Liu ,  Scott D. Edmondson ,  Xing Dai ,  Byron Gabriel DuBois

IPC分类号： C07D417/14 ,  C07D211/24 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D401/14 ,  C07D401/04

CPC分类号： C07D211/24 ,  C07D211/22 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： 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.

摘要翻译： 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：US09006228B2

公开(公告)日：2015-04-14

申请号：US14126685

申请日：2012-06-11

申请人： Michael Miller ,  Andrew Stamford ,  Kallol Basu ,  Harold B. Wood ,  Duane DeMong ,  Wanying Sun ,  Joie Garfunkle ,  Christopher Moyes ,  Zhiyong Hu ,  Ping Liu ,  Scott D. Edmondson ,  Xing Dai ,  Byron Gabriel DuBois

发明人： Michael Miller ,  Andrew Stamford ,  Kallol Basu ,  Harold B. Wood ,  Duane DeMong ,  Wanying Sun ,  Joie Garfunkle ,  Christopher Moyes ,  Zhiyong Hu ,  Ping Liu ,  Scott D. Edmondson ,  Xing Dai ,  Byron Gabriel DuBois

IPC分类号： C07D417/14 ,  C07D211/24 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D211/22

CPC分类号： C07D211/24 ,  C07D211/22 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： 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.

摘要翻译： 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：US20210094938A1

公开(公告)日：2021-04-01

申请号：US15733056

申请日：2018-11-12

申请人： Steven L. COLLETTI ,  Duane DEMONG ,  Kevin D. DYKSTRA ,  Zhiyong HU ,  Michael MILLER ,  Merck Sharp & Dohme Corp.

发明人： Steven L. Colletti ,  Duane DeMong ,  Kevin D. Dykstra ,  Zhiyong Hu ,  Michael Miller

IPC分类号： C07D405/14 ,  A61P3/10

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia Formula (I).

公开(公告)号：US10059667B2

公开(公告)日：2018-08-28

申请号：US15110894

申请日：2015-02-03

申请人： MERCK SHARP & DOHME CORP. ,  Harry Chobanian ,  Duane DeMong ,  Yan Guo ,  Zhiyong Hu ,  Michael Miller ,  Barbara Pio ,  Christopher W. Plummer ,  Dong Xiao ,  Cangming Yang ,  Rui Zhang

发明人： Harry Chobanian ,  Duane DeMong ,  Yan Guo ,  Zhiyong Hu ,  Michael Miller ,  Barbara Pio ,  Christopher W. Plummer ,  Dong Xiao ,  Cangming Yang

IPC分类号： C07D211/42 ,  A61K45/06 ,  A61K31/366 ,  A61K31/397 ,  A61K31/40 ,  A61K31/44 ,  C07D231/20 ,  A61K31/4985 ,  C07D401/04 ,  C07D239/52 ,  C07C217/52 ,  C07D205/04 ,  C07D491/056 ,  C07D265/30 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D209/52 ,  C07D209/54 ,  C07D211/22 ,  C07D213/30 ,  C07D213/64 ,  C07D213/65 ,  C07D213/69 ,  C07D307/86 ,  C07D307/88 ,  C07C59/72 ,  C07D205/12 ,  C07D213/647

CPC分类号： C07D211/42 ,  A61K31/366 ,  A61K31/397 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4985 ,  A61K45/06 ,  C07C59/72 ,  C07C217/52 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07D205/04 ,  C07D205/12 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D209/52 ,  C07D209/54 ,  C07D211/22 ,  C07D213/30 ,  C07D213/64 ,  C07D213/647 ,  C07D213/65 ,  C07D213/69 ,  C07D231/20 ,  C07D239/52 ,  C07D265/30 ,  C07D307/86 ,  C07D307/88 ,  C07D401/04 ,  C07D491/056 ,  A61K2300/00

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US20160332968A1

公开(公告)日：2016-11-17

申请号：US15110894

申请日：2015-02-03

申请人： Harry CHOBANIAN ,  Duane DEMONG ,  Yan Guo ,  Zhiyong Hu ,  Barbara PIO ,  Christopher PLUMMER ,  Dong XIAO ,  Cangming YANG ,  Rui ZHANG ,  Merck Sharp & Dohme Corp. ,  Michael MILLER

发明人： Harry Chobanian ,  Duane DeMong ,  Yan Guo ,  Zhiyong Hu ,  Michael Miller ,  Barbara Pio ,  Christopher W. Plummer ,  Dong Xiao ,  Michael Yang

IPC分类号： C07D211/42 ,  C07D211/22 ,  C07D205/04 ,  C07D209/54 ,  C07D209/52 ,  C07D207/12 ,  C07D205/12 ,  C07C217/52 ,  C07D401/04 ,  C07D265/30 ,  C07C59/72 ,  C07D213/64 ,  C07D213/69 ,  C07D239/52 ,  C07D231/20 ,  C07D307/88 ,  C07D491/056 ,  C07D307/86 ,  C07D213/30 ,  C07D213/647 ,  C07D207/08

CPC分类号： C07D211/42 ,  A61K31/366 ,  A61K31/397 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4985 ,  A61K45/06 ,  C07C59/72 ,  C07C217/52 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07D205/04 ,  C07D205/12 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D209/52 ,  C07D209/54 ,  C07D211/22 ,  C07D213/30 ,  C07D213/64 ,  C07D213/647 ,  C07D213/65 ,  C07D213/69 ,  C07D231/20 ,  C07D239/52 ,  C07D265/30 ,  C07D307/86 ,  C07D307/88 ,  C07D401/04 ,  C07D491/056 ,  A61K2300/00

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

摘要翻译： 结构式（I）的新型化合物及其药学上可接受的盐是G蛋白偶联受体40（GPR40）的激动剂，可用于治疗，预防和抑制G蛋白偶联受体 受体40.本发明的化合物可用于治疗2型糖尿病，以及通常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合或糖尿病性血脂异常，高脂血症，高胆固醇血症和 高甘油三酯血症

公开(公告)号：US20140057893A1

公开(公告)日：2014-02-27

申请号：US14110332

申请日：2012-04-05

申请人： 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

发明人： 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分类号： C07D513/04 ,  C07D413/14 ,  C07D413/04 ,  C07D498/04 ,  C07D405/04 ,  C07D471/04 ,  C07D487/04 ,  C07D401/12 ,  C07D211/22

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

摘要： 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

摘要翻译： 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