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

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：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：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：US20150274664A1

公开(公告)日：2015-10-01

申请号：US14431366

申请日：2013-09-25

申请人： John J. ACTON ,  Scott D. EDMONDSON ,  Ping LIU ,  Michael W. MILLER ,  Harold B. WOOD ,  Byron G. DUBOIS ,  William B. GEISS ,  MERCK SHARP & DOHME CORP.

发明人： John J. Acton ,  Scott D. Edmondson ,  Ping Liu ,  Michael W. Miller ,  Harold B. Wood ,  Byron G. DuBois ,  William B. Geiss

IPC分类号： C07D211/60 ,  C07D401/12 ,  C07D413/04 ,  C07D401/14 ,  C07D401/04

CPC分类号： C07D211/60 ,  A61K31/506 ,  C07D211/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14

摘要： Substituted cyclopropyl piperidinyl compounds 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： 公开了用于治疗或预防2型糖尿病和类似病症的取代的环丙基哌啶基化合物及其药学上可接受的盐。 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：US20160060256A1

公开(公告)日：2016-03-03

申请号：US14786466

申请日：2014-04-22

申请人： Kenneth L. ARRINGTON ,  Byron DUBOIS ,  John S. DEBENHAM ,  Ping LIU ,  Alan B. NORTHRUP ,  Jason W. SZEWCZYK ,  Liping WANG ,  Ming WANG ,  MERCK SHARP & DOHME CORP.

发明人： Kenneth L. Arrington ,  Byron DuBois ,  John S. Debenham ,  Ping Liu ,  Alan B. Northrup ,  Jason W. Szewczyk ,  Liping Wang ,  Ming Wang

IPC分类号： C07D417/14 ,  C07D417/12 ,  A61K31/5377 ,  A61K31/506

CPC分类号： C07D417/14 ,  A61K31/427 ,  A61K31/506 ,  A61K31/5377 ,  C07D417/12

摘要： The invention provides certain thiazole-substituted aminopyrimidine compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, and the subscripts r, s, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

摘要翻译： 本发明提供了式（I）（I）的某些噻唑取代的氨基嘧啶化合物或其药学上可接受的盐，其中R1，R2，R3，R5，R6和下标r，s和t如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。

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：US20170114056A1

公开(公告)日：2017-04-27

申请号：US15129206

申请日：2015-03-23

申请人： Helen MITCHELL ,  Mark E. FRALEY ,  Andrew J. COOKE ,  Craig A. STUMP ,  Yi Heng CHEN ,  Douglas C. BESHORE ,  Xu-Fank ZHANG ,  Casey C. MCCOMAS ,  Kathy SCHIRRIPA ,  Melody MCWHERTER ,  Swati P. MERCER ,  Keith P. MOORE ,  Ping LIU ,  Harold B. WOOD ,  Chun Sing LI ,  Qinghua MAO ,  Merck Sharp & Dohme Corp.

发明人： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Yi- Heng Chen ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Swati P. Mercer ,  Keith P. Moore ,  Ping Liu ,  Harold B. Wood ,  Chun Sing Li ,  Qinghua Mao ,  Douglas C. Beshore

IPC分类号： C07D471/04 ,  C07D513/04

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

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：US10208060B2

公开(公告)日：2019-02-19

申请号：US15513854

申请日：2015-09-23

申请人： Jiaqiang Cai ,  Alejandro Crespo ,  John Debenham ,  Xiaoxing Du ,  Ping Liu ,  Rongqiang Liu ,  Christina B. Madsen-Duggan ,  Weiguo Quan ,  Christopher Sinz ,  Liping Wang

发明人： Jiaqiang Cai ,  Alejandro Crespo ,  John Debenham ,  Xiaoxing Du ,  Ping Liu ,  Rongqiang Liu ,  Christina B. Madsen-Duggan ,  Weiguo Quan ,  Christopher Sinz ,  Liping Wang

IPC分类号： C07D491/048 ,  C07D495/04 ,  A61P7/06

摘要： The present invention concerns compounds of formula I or a pharmaceutically acceptable salt thereof which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.