公开(公告)号：US20130040929A1

公开(公告)日：2013-02-14

申请号：US13642646

申请日：2011-05-06

Applicant: Jeffrey J. Hale ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Zhicai Wu ,  Cangming Yang

Inventor： Jeffrey J. Hale ,  Jinlong Jiang ,  Dong-Ming Shen ,  Zhi-Cai Shi ,  Min Shu ,  Zhicai Wu ,  Cangming Yang

IPC: A61K31/506 ,  C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61P3/00 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/4985 ,  A61P3/04 ,  A61P3/10 ,  C07D401/14 ,  A61K31/497

CPC classification number: C07D401/04 ,  C07D401/14

Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.

公开(公告)号：US07125888B2

公开(公告)日：2006-10-24

申请号：US10512927

申请日：2003-04-28

Applicant: Mark T. Bilodeau ,  Mark E. Fraley ,  Zhicai Wu

Inventor： Mark T. Bilodeau ,  Mark E. Fraley ,  Zhicai Wu

IPC: A61K31/535 ,  A61K31/5513 ,  A61K31/4375 ,  C07D407/04

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：US20060030595A1

公开(公告)日：2006-02-09

申请号：US11188466

申请日：2005-07-25

Applicant: Mark Bilodeau ,  Christopher Dinsmore ,  Jeffrey Bergman ,  B. Trotter ,  Lou Neilson ,  Zhicai Wu ,  Peter Manley ,  John Hartnett

Inventor： Mark Bilodeau ,  Christopher Dinsmore ,  Jeffrey Bergman ,  B. Trotter ,  Lou Neilson ,  Zhicai Wu ,  Peter Manley ,  John Hartnett

IPC: A61K31/506 ,  A61K31/444 ,  C07D401/14 ,  C07D403/14

CPC classification number: C07D213/57 ,  C07D213/06 ,  C07D213/30 ,  C07D213/42 ,  C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D213/81 ,  C07D213/84 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

公开(公告)号：US08933113B2

公开(公告)日：2015-01-13

申请号：US13979875

申请日：2012-01-19

Applicant: Alejandro Crespo ,  Ping Lan ,  Rudrajit Mal ,  Anthony Ogawa ,  Hong Shen ,  Peter J. Sinclair ,  Zhongxiang Sun ,  Ellen K. Vande Bunte ,  Zhicai Wu ,  Kun Liu ,  Robert J. DeVita ,  Dong-Ming Shen ,  Min Shu ,  John Qiang Tan ,  Changhe Qi ,  Yuguang Wang ,  Richard Beresis

Inventor： Alejandro Crespo ,  Ping Lan ,  Rudrajit Mal ,  Anthony Ogawa ,  Hong Shen ,  Peter J. Sinclair ,  Zhongxiang Sun ,  Ellen K. Vande Bunte ,  Zhicai Wu ,  Kun Liu ,  Robert J. DeVita ,  Dong-Ming Shen ,  Min Shu ,  John Qiang Tan ,  Changhe Qi ,  Yuguang Wang ,  Richard Beresis

IPC: A61K31/416 ,  C07D231/56 ,  A61K31/405 ,  A61K31/404 ,  C07D403/06 ,  C07D209/08 ,  C07D209/10 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K45/06 ,  C07D413/06

CPC classification number: C07D413/06 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/405 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K45/06 ,  C07D209/08 ,  C07D209/10 ,  C07D231/56 ,  C07D403/04 ,  C07D403/06 ,  C07D405/06

Abstract: Disclosed are the compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, which are useful for treating aldosterone-mediated diseases. The processes for preparing compounds of the Formula (I), the use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and the pharmaceutical compositions which comprise compounds of the formula (I) are disclosed too.

Abstract translation: 公开了式（I）化合物及其药学上可接受的盐，其可用于治疗醛固酮介导的疾病。 还公开了制备式（I）化合物，用于治疗和预防上述疾病和用于制备用于此目的的药物的方法和包含式（I）化合物的药物组合物。

公开(公告)号：US20130123237A1

公开(公告)日：2013-05-16

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: A61K31/5377 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/351 ,  A61K31/397 ,  A61K31/4412 ,  C07D471/04 ,  A61K31/496

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：US08030332B2

公开(公告)日：2011-10-04

申请号：US12223353

申请日：2007-01-29

Applicant: B. Wesley Trotter ,  Richard C. A. Isaacs ,  Zhicai Wu ,  Jacob M. Hoffman ,  Mark T. Bilodeau ,  Ahren Iver Green

Inventor： B. Wesley Trotter ,  Richard C. A. Isaacs ,  Zhicai Wu ,  Jacob M. Hoffman ,  Mark T. Bilodeau ,  Ahren Iver Green

IPC: C07D401/14 ,  A61K31/506

CPC classification number: C07D413/14

Abstract: The present invention relates to dipyridin-3-ylmethoxy compounds and derivatives thereof having the structure I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

Abstract translation: 本发明涉及具有用作治疗心律失常的钾通道抑制剂的结构I的二吡啶-3-基甲氧基化合物及其衍生物等。

公开(公告)号：US20100099673A1

公开(公告)日：2010-04-22

申请号：US12523192

申请日：2008-01-11

Applicant: Mark T. Bilodeau ,  Nathan R. Kett ,  Craig Lindsley ,  Peter J. Manley ,  Jeffrey Y. Melamed ,  Daniel Vincent Paone ,  B. Wesley Trotter ,  Zhicai Wu

Inventor： Mark T. Bilodeau ,  Nathan R. Kett ,  Craig Lindsley ,  Peter J. Manley ,  Jeffrey Y. Melamed ,  Daniel Vincent Paone ,  B. Wesley Trotter ,  Zhicai Wu

IPC: C07D215/02 ,  A61K31/47 ,  C07D401/02 ,  A61K31/497 ,  A61K31/498 ,  A61K31/5377 ,  C07D413/02 ,  A61P29/00 ,  A61P19/10 ,  A61P9/00 ,  A61P37/00 ,  A61P19/02

CPC classification number: C07D413/06 ,  C07D215/08 ,  C07D215/233 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D413/12 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention relates to compounds represented by Formula (I): and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.

Abstract translation: 本发明涉及由式（I）表示的化合物及其药学上可接受的盐。 本发明还提供包含本发明化合物的药物组合物。 本发明还提供了治疗和预防疼痛，呼吸和非呼吸道疾病的方法。

公开(公告)号：US07569589B2

公开(公告)日：2009-08-04

申请号：US11188466

申请日：2005-07-25

Applicant: Mark T. Bilodeau ,  Christopher J. Dinsmore ,  Jeffrey M. Bergman ,  B. Wesley Trotter ,  Lou Anne Neilson ,  Zhicai Wu ,  Peter Manley ,  John Hartnett

Inventor： Mark T. Bilodeau ,  Christopher J. Dinsmore ,  Jeffrey M. Bergman ,  B. Wesley Trotter ,  Lou Anne Neilson ,  Zhicai Wu ,  Peter Manley ,  John Hartnett

IPC: C07D403/14 ,  A61K31/44

CPC classification number: C07D213/57 ,  C07D213/06 ,  C07D213/30 ,  C07D213/42 ,  C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D213/81 ,  C07D213/84 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

Abstract translation: 本发明涉及具有用作治疗心律失常的钾通道抑制剂的结构的化合物等。

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。