公开(公告)号：US20120010209A1

公开(公告)日：2012-01-12

申请号：US13144123

申请日：2010-01-12

Applicant: Michael D. Altman ,  Mark T. Bilodeau ,  Jongwon Lim ,  Alan Nortrup ,  Matthew G. Stanton ,  Brandon M. Taoka

Inventor： Michael D. Altman ,  Mark T. Bilodeau ,  Jongwon Lim ,  Alan Nortrup ,  Matthew G. Stanton ,  Brandon M. Taoka

IPC: A61K31/5025 ,  A61P25/28 ,  A61K31/437 ,  C07D487/04 ,  C07D471/04

CPC classification number: A61K31/5025 ,  C07D471/04 ,  C07D487/04

Abstract: The invention encompasses imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.

Abstract translation: 本发明包括选择性抑制微管亲和调节激酶（MARK）的咪唑并[1,2-a]吡啶和咪唑并[1,2-b]哒嗪衍生物，因此可用于治疗或预防阿尔茨海默氏病。 还包括药物组合物和使用方法。

公开(公告)号：US20110212946A1

公开(公告)日：2011-09-01

申请号：US13127898

申请日：2009-11-03

Applicant: James C. Barrow ,  Mark T. Bilodeau ,  Christopher D. Cox ,  John C. Hartnett ,  Nathan R. Kett ,  Yiwei Li ,  Peter J. Manley ,  Jeffrey Melamed ,  William D. Shipe ,  B. Wesley Trotter ,  Amy Zartman

Inventor： James C. Barrow ,  Mark T. Bilodeau ,  Christopher D. Cox ,  John C. Hartnett ,  Nathan R. Kett ,  Yiwei Li ,  Peter J. Manley ,  Jeffrey Melamed ,  William D. Shipe ,  B. Wesley Trotter ,  Amy Zartman

IPC: A61K31/4704 ,  C07D405/14 ,  A61K31/496 ,  A61K31/55 ,  C07D401/12 ,  A61K31/4709 ,  C07D413/12 ,  A61K31/5377 ,  C07D215/227 ,  A61P25/00

CPC classification number: A61K31/47 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. 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 the neuropeptide S receptor is involved.

Abstract translation: 本发明涉及作为神经肽S受体的拮抗剂的喹诺酮化合物，其可用于治疗或预防神经和精神疾病以及涉及神经肽S受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及神经肽S受体的疾病中的用途。

公开(公告)号：US20100004229A1

公开(公告)日：2010-01-07

申请号：US12223357

申请日：2007-01-29

Applicant: Mark T. Bilodeau ,  Jacob M. Hoffman ,  M. Brad Nolt

Inventor： Mark T. Bilodeau ,  Jacob M. Hoffman ,  M. Brad Nolt

IPC: A61K31/5415 ,  C07D279/16 ,  C07D213/02 ,  A61K31/444 ,  A61P9/00

CPC classification number: C07D213/74 ,  C07D401/14 ,  C07D417/14

Abstract: The present invention relates to pyridin-3-yl pyridin-3-amine compounds and derivatives thereof having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

Abstract translation: 本发明涉及可用作治疗心律失常的钾通道抑制剂的结构式（I）的吡啶-3-基吡啶-3-胺化合物及其衍生物等。

公开(公告)号：US20080287457A1

公开(公告)日：2008-11-20

申请号：US11792121

申请日：2005-12-09

Applicant: Jeannie M. Arruda ,  Brian T. Campbell ,  Nicholas D.P. Cosford ,  Jacob M. Hoffman ,  Essa H. Hu ,  Mark E. Layton ,  Yiwei Li ,  Jun Liang ,  Kevin J. Rodzinak ,  Tony Siu ,  Brian A. Stearns ,  Lida R. Tehrani ,  Mark T. Bilodeau ,  Peter J. Manley

Inventor： Jeannie M. Arruda ,  Brian T. Campbell ,  Nicholas D.P. Cosford ,  Jacob M. Hoffman ,  Essa H. Hu ,  Mark E. Layton ,  Yiwei Li ,  Jun Liang ,  Kevin J. Rodzinak ,  Tony Siu ,  Brian A. Stearns ,  Lida R. Tehrani ,  Mark T. Bilodeau ,  Peter J. Manley

IPC: A61K31/496 ,  C07D487/04 ,  A61P35/04 ,  A61K31/4375

CPC classification number: C07D471/04

Abstract: The present invention is directed to compounds which contain substituted naphthyridines 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. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.

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。 与PCT公开WO2003 / 086394中报道的其它萘啶类相比，这些取代的萘啶具有意想不到的有利性质，这种意想不到的有利性质可包括增加的细胞效力/溶解度，更大的选择性，增强的药物动力学性质，缺乏目标活性等。

公开(公告)号：US20080274107A1

公开(公告)日：2008-11-06

申请号：US12148649

申请日：2008-04-21

Applicant: Mark E. Fraley ,  Kenneth L. Arrington ,  Mark T. Bilodeau ,  George D. Hartman ,  William F. Hoffman ,  Yuntae Kim ,  Randall W. Hungate

Inventor： Mark E. Fraley ,  Kenneth L. Arrington ,  Mark T. Bilodeau ,  George D. Hartman ,  William F. Hoffman ,  Yuntae Kim ,  Randall W. Hungate

IPC: A61K39/395 ,  C07D215/20 ,  A61K31/337 ,  A61K31/445 ,  A61K31/47 ,  A61P43/00

CPC classification number: C07D401/14 ,  A61K31/495 ,  A61K45/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K2300/00

Abstract: The present invention relates to 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，动脉粥样硬化的方法 ，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：US06586424B2

公开(公告)日：2003-07-01

申请号：US10062351

申请日：2002-02-01

Applicant: Mark T. Bilodeau ,  George D. Hartman ,  Peter J. Manley

Inventor： Mark T. Bilodeau ,  George D. Hartman ,  Peter J. Manley

IPC: C07D41312

CPC classification number: C07D417/12 ,  C07D417/14

Abstract: The present invention relates to 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.

公开(公告)号：US06465484B1

公开(公告)日：2002-10-15

申请号：US09786004

申请日：2001-02-28

Applicant: Mark T. Bilodeau ,  Randall W. Hungate ,  April M. Cunningham ,  Timothy J. Koester

Inventor： Mark T. Bilodeau ,  Randall W. Hungate ,  April M. Cunningham ,  Timothy J. Koester

IPC: A61K31437

CPC classification number: C07D235/06 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04 ,  C07D471/04

Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tryrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.

Abstract translation: 本发明涉及抑制酪氨酸激酶的化合物，含有酪氨酸激酶抑制化合物的组合物和使用酪氨酸激酶抑制剂治疗酪氨酸激酶依赖性疾病/病症如血管生成，癌症，动脉粥样硬化，糖尿病性视网膜病变或自身免疫性疾病的方法 哺乳动物。