公开(公告)号：US20080280899A1

公开(公告)日：2008-11-13

申请号：US11547113

申请日：2005-04-05

Applicant: Mark T. Bilodeau ,  Chixu Chen ,  Nicholas D.P. Cosford ,  Brian W. Eastman ,  John C. Hartnett ,  Essa H. Hu ,  Peter J. Manley ,  Lou Anne Neilson ,  Lida R. Tehrani ,  Zhicai Wu

Inventor： Mark T. Bilodeau ,  Chixu Chen ,  Nicholas D.P. Cosford ,  Brian W. Eastman ,  John C. Hartnett ,  Essa H. Hu ,  Peter J. Manley ,  Lou Anne Neilson ,  Lida R. Tehrani ,  Zhicai Wu

IPC: A61K31/519 ,  C07D471/04 ,  A61K31/4375 ,  A61P35/00 ,  A61K31/5377 ,  C07D413/12

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract translation: 本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代萘啶的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。

公开(公告)号：US07223738B2

公开(公告)日：2007-05-29

申请号：US10510069

申请日：2003-04-04

Applicant: Mark T. Bilodeau ,  Mark E. Duggan ,  John C. Hartnett ,  Craig W. Lindsley ,  Peter J. Manley ,  Zhicai Wu ,  Zhijian Zhao

Inventor： Mark T. Bilodeau ,  Mark E. Duggan ,  John C. Hartnett ,  Craig W. Lindsley ,  Peter J. Manley ,  Zhicai Wu ,  Zhijian Zhao

IPC: A01N43/04 ,  A01N43/58 ,  A01N43/60 ,  A01N43/42 ,  A61K31/70 ,  A61K31/50 ,  A61K31/495 ,  A61K31/52 ,  A61K31/47 ,  C07D487/00 ,  C07D491/00 ,  C07H15/00 ,  C07H17/00 ,  C07H17/02 ,  C09B25/00

CPC classification number: C07D401/10 ,  A61K31/498 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

公开(公告)号：US20060205765A1

公开(公告)日：2006-09-14

申请号：US10554185

申请日：2004-04-20

Applicant: Mark Bilodeau ,  Zhicai Wu

Inventor： Mark Bilodeau ,  Zhicai Wu

IPC: A61K31/4745 ,  C07D498/02 ,  C07D491/02 ,  C07D471/02

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract translation: 本发明涉及含有与取代的吡啶部分稠合的五元杂环的化合物，所述取代吡啶部分抑制丝氨酸/苏氨酸蛋白激酶Akt的活性。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。

公开(公告)号：US20050176753A1

公开(公告)日：2005-08-11

申请号：US10512927

申请日：2003-04-28

Applicant: Mark Bilodeau ,  Mark Fraley ,  Zhicai Wu

Inventor： Mark Bilodeau ,  Mark Fraley ,  Zhicai Wu

IPC: A61K31/09 ,  A61K31/4196 ,  A61K31/437 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/551 ,  A61K31/575 ,  A61K31/737 ,  A61K38/00 ,  A61K38/21 ,  A61P17/00 ,  A61P19/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention relates to imidazopyridine compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

Abstract translation: 本发明涉及抑制，调节和/或调节酪氨酸激酶信号转导的咪唑并吡啶化合物，含有这些化合物的组合物，及其用于治疗酪氨酸激酶依赖性疾病和病症如血管生成，癌症，肿瘤生长， 动脉粥样硬化，年龄相关性黄斑变性，糖尿病性视网膜病变，炎症性疾病等。

公开(公告)号：US20140088124A1

公开(公告)日：2014-03-27

申请号：US14123246

申请日：2012-06-01

Applicant: Robert J. DeVita ,  QingMei Hong ,  Zhong Lai ,  Kevin D. Dykstra ,  Yang Yu ,  Jian Liu ,  Donald M. Sperbeck ,  Tianying Jian ,  Deodial Guiadeen ,  Ginger Xu-qiang Yang ,  Zhicai Wu ,  Shuwen He ,  Pauline C. Ting ,  Robert Aslanian ,  Jeffrey T. Kuethe ,  James Balkovec ,  Rongze Kuang ,  Gang Zhou ,  Heping Wu

Inventor： Robert J. DeVita ,  QingMei Hong ,  Zhong Lai ,  Kevin D. Dykstra ,  Yang Yu ,  Jian Liu ,  Donald M. Sperbeck ,  Tianying Jian ,  Deodial Guiadeen ,  Ginger Xu-qiang Yang ,  Zhicai Wu ,  Shuwen He ,  Pauline C. Ting ,  Robert Aslanian ,  Jeffrey T. Kuethe ,  James Balkovec ,  Rongze Kuang ,  Gang Zhou ,  Heping Wu

IPC: C07D401/14 ,  C07D417/14 ,  C07D493/04 ,  C07D471/04

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04

Abstract: Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

Abstract translation: 本文描述的是式（I）的化合物。式I化合物作为DGAT1抑制剂，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的补救剂。

公开(公告)号：US07750151B2

公开(公告)日：2010-07-06

申请号：US11547113

申请日：2005-04-05

Applicant: Mark T. Bilodeau ,  Chixu Chen ,  Nicholas D. P. Cosford ,  Brian W. Eastman ,  John C. Hartnett ,  Essa H. Hu ,  Peter J. Manley ,  Lou Anne Neilson ,  Lida R. Tehrani ,  Zhicai Wu

Inventor： Mark T. Bilodeau ,  Chixu Chen ,  Nicholas D. P. Cosford ,  Brian W. Eastman ,  John C. Hartnett ,  Essa H. Hu ,  Peter J. Manley ,  Lou Anne Neilson ,  Lida R. Tehrani ,  Zhicai Wu

IPC: C07D471/04 ,  C07D413/12 ,  C07D521/00 ,  C07D401/14 ,  C07D487/08 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract translation: 本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代萘啶的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。

公开(公告)号：US20070254901A1

公开(公告)日：2007-11-01

申请号：US11659606

申请日：2005-08-19

Applicant: Mark Bilodeau ,  Nicolas Cosford ,  John Hartnett ,  Yiwei Li ,  Jun Liang ,  Peter Manley ,  Lou Neilson ,  Tony Siu ,  Zhicai Wu

Inventor： Mark Bilodeau ,  Nicolas Cosford ,  John Hartnett ,  Yiwei Li ,  Jun Liang ,  Peter Manley ,  Lou Neilson ,  Tony Siu ,  Zhicai Wu

IPC: A61K31/519 ,  A61P35/00 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract translation: 本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代的5-取代哌啶部分的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。

公开(公告)号：US20230416227A1

公开(公告)日：2023-12-28

申请号：US18043357

申请日：2021-09-09

Applicant: Merck Sharp & Dohme LLC ,  Anthony Ken OGAWA ,  Christopher J. SINZ ,  Jacqueline D. HICKS ,  Alan C. CHENG ,  Song YANG ,  Jianming BAO ,  Donna A. A. W. HAYES ,  Simon B. LANG ,  Maoqun TIAN ,  Salman JABRI ,  Galen Paul SHEARN-NANCE ,  Rongze KUANG ,  Zhiqiang ZHAO ,  Zhicai WU

Inventor： Anthony Ken Ogawa ,  Christopher J. Sinz ,  Jacqueline D. Hicks ,  Alan C. Cheng ,  Song Yang ,  Jianming Bao ,  Donna A. A. W. Hayes ,  Simon B. Lang ,  Maoqun Tian ,  Salman Jabri ,  Galen Paul Shearn-Nance ,  Rongze Kuang ,  Zhiqiang Zhao ,  Zhicai Wu

IPC: C07D401/14 ,  A61K45/06 ,  A61P9/10

CPC classification number: C07D401/14 ,  A61P9/10 ,  A61K45/06

Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

公开(公告)号：US08796258B2

公开(公告)日：2014-08-05

申请号：US13812536

申请日：2012-02-23

Applicant: Rajan Anand ,  James M. Apgar ,  Tesfaye Biftu ,  Ping Chen ,  Lin Chu ,  Vincent J. Colandrea ,  Guizhen Dong ,  James F. Dropinski ,  Danqing Feng ,  Jacqueline D. Hicks ,  Jinlong Jiang ,  Alexander J. Kim ,  Kenneth J. Leavitt ,  Bing Li ,  Xiaoxia Qian ,  Iyassu Sebhat ,  Lan Wei ,  Robert R. Wilkening ,  Zhicai Wu

Inventor： Rajan Anand ,  James M. Apgar ,  Tesfaye Biftu ,  Ping Chen ,  Lin Chu ,  Vincent J. Colandrea ,  Guizhen Dong ,  James F. Dropinski ,  Danqing Feng ,  Jacqueline D. Hicks ,  Jinlong Jiang ,  Alexander J. Kim ,  Kenneth J. Leavitt ,  Bing Li ,  Xiaoxia Qian ,  Iyassu Sebhat ,  Lan Wei ,  Robert R. Wilkening ,  Zhicai Wu

IPC: A61K31/00 ,  C07D513/02

CPC classification number: A61K31/5377 ,  A61K31/351 ,  A61K31/366 ,  A61K31/397 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/519 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

Abstract: Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

Abstract translation: 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

公开(公告)号：US07638530B2

公开(公告)日：2009-12-29

申请号：US10554185

申请日：2004-04-20

Applicant: Mark T. Bilodeau ,  Zhicai Wu

Inventor： Mark T. Bilodeau ,  Zhicai Wu

IPC: A61K31/4745 ,  C07D498/02 ,  C07D491/02 ,  C07D471/02

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract translation: 本发明涉及含有与取代的吡啶部分稠合的五元杂环的化合物，所述取代吡啶部分抑制丝氨酸/苏氨酸蛋白激酶Akt的活性。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。