公开(公告)号：US07544677B2

公开(公告)日：2009-06-09

申请号：US11659606

申请日：2005-08-19

Applicant: Mark T. Bilodeau ,  Nicholas D. P. Cosford ,  John C. Hartnett ,  Yiwei Li ,  Jun Liang ,  Peter J. Manley ,  Lou Anne Neilson ,  Tony Siu ,  Zhicai Wu

Inventor： Mark T. Bilodeau ,  Nicholas D. P. Cosford ,  John C. Hartnett ,  Yiwei Li ,  Jun Liang ,  Peter J. Manley ,  Lou Anne Neilson ,  Tony Siu ,  Zhicai Wu

IPC: A61K31/541 ,  A61K31/5355 ,  A61K31/519 ,  C07D471/04 ,  C07D519/00 ,  A61P35/00

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：US20090069312A1

公开(公告)日：2009-03-12

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: A61K31/538 ,  C07D413/14 ,  A61P9/06

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：US20090030043A1

公开(公告)日：2009-01-29

申请号：US12223356

申请日：2007-01-29

Applicant: Jacob M. Hoffman ,  Anthony M. Smith ,  John Hartnett ,  Zhicai Wu ,  Mark T. Bilodeau

Inventor： Jacob M. Hoffman ,  Anthony M. Smith ,  John Hartnett ,  Zhicai Wu ,  Mark T. Bilodeau

IPC: A61K31/444 ,  C07D401/14

CPC classification number: C07D213/74

Abstract: The present invention relates to tetraaryl methyl amine 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）的四芳基甲胺化合物及其衍生物等。

公开(公告)号：US07879839B2

公开(公告)日：2011-02-01

申请号：US11658114

申请日：2005-07-27

Applicant: Christopher J. Dinsmore ,  Jeffrey M. Bergman ,  Douglas C. Beshore ,  B. Wesley Trotter ,  Kausik K. Nanda ,  Richard Isaacs ,  Linda S. Payne ,  Lou Anne Neilson ,  Zhicai Wu ,  Mark T. Bilodeau ,  Peter J. Manley ,  Adrienne E. Balitza

Inventor： Christopher J. Dinsmore ,  Jeffrey M. Bergman ,  Douglas C. Beshore ,  B. Wesley Trotter ,  Kausik K. Nanda ,  Richard Isaacs ,  Linda S. Payne ,  Lou Anne Neilson ,  Zhicai Wu ,  Mark T. Bilodeau ,  Peter J. Manley ,  Adrienne E. Balitza

IPC: C07D401/14 ,  A61K31/438

CPC classification number: C07D213/36 ,  C07D213/30 ,  C07D213/32 ,  C07D213/38 ,  C07D213/40 ,  C07D213/42 ,  C07D213/55 ,  C07D213/56 ,  C07D213/64 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D491/08

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：US08410111B2

公开(公告)日：2013-04-02

申请号：US13590210

申请日：2012-08-21

Applicant: Mark T. Bilodeau ,  Kausik K. Nanda ,  B. Wesley Trotter

Inventor： Mark T. Bilodeau ,  Kausik K. Nanda ,  B. Wesley Trotter

IPC: A61K31/496 ,  C07D417/12

CPC classification number: A61K31/496 ,  C07D417/12

Abstract: The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction.

Abstract translation: 本发明涉及非典型抗精神病药治疗剂，其可用于治疗与多巴胺D2和5-羟色胺5-HT2A神经传递功能障碍相关的神经和精神疾病。

公开(公告)号：US07973059B2

公开(公告)日：2011-07-05

申请号：US11992919

申请日：2006-10-17

Applicant: Scott Wolkenberg ,  Mark T. Bilodeau ,  M. Brad Nolt

Inventor： Scott Wolkenberg ,  Mark T. Bilodeau ,  M. Brad Nolt

IPC: A61K31/44 ,  C07D213/30

CPC classification number: C07D213/30

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：US07115597B2

公开(公告)日：2006-10-03

申请号：US10677687

申请日：2003-10-02

Applicant: Mark T. Bilodeau ,  George D. Hartman ,  Jacob M. Hoffman, Jr. ,  John T. Sisko ,  Peter J. Manley ,  Anthony M. Smith ,  Thomas J. Tucker ,  William C. Lumma, Jr. ,  Leonard Rodman

Inventor： Mark T. Bilodeau ,  George D. Hartman ,  Jacob M. Hoffman, Jr. ,  John T. Sisko ,  Peter J. Manley ,  Anthony M. Smith ,  Thomas J. Tucker ,  William C. Lumma, Jr. ,  Leonard Rodman

IPC: C07D417/12 ,  A61K31/427 ,  C07D241/04

CPC classification number: C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08

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：US08829196B2

公开(公告)日：2014-09-09

申请号：US13499844

申请日：2010-09-28

Applicant: Mark T. Bilodeau ,  Melissa Egbertson ,  Ahren Green ,  John C. Hartnett ,  Yiwei Li

Inventor： Mark T. Bilodeau ,  Melissa Egbertson ,  Ahren Green ,  John C. Hartnett ,  Yiwei Li

IPC: C07D215/38 ,  C07C215/20 ,  C07C211/34 ,  C07C25/02 ,  A61K31/133

CPC classification number: C07C215/20 ,  A61K31/133 ,  C07C25/02 ,  C07C211/34 ,  C07C215/44 ,  C07C255/58 ,  C07C2602/10 ,  C07D215/38 ,  C07D215/44 ,  C07D311/74 ,  C07D311/76 ,  C07D405/04 ,  C07D405/06

Abstract: The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.

Abstract translation: 本发明涉及调节至少一种TRP家族成员的组合物和方法。 具体地说，本发明涉及新型TRPA1拮抗剂及其用于治疗慢性炎性和神经性疼痛等疼痛的用途。 可以调节一种或多种TRPA1功能的化合物在许多方面是有用的，包括但不限于维持钙稳态; 维持钠稳态; 调节细胞内钙含量; 调节膜极化（膜电位）; 调节阳离子水平; 和/或治疗或预防与钙稳态相关的疾病，病症或病症，钠稳态，钙或钠血管平衡，或膜极化/超极化（包括低钠和过度兴奋性）和/或治疗或预防与疾病，病症或病症相关 与TRPA1表达或功能调节或失调。 本发明还涉及拮抗TRPA1的功能和一种或多种另外的TRP通道的功能的方法和组合物。

公开(公告)号：US08592425B2

公开(公告)日：2013-11-26

申请号：US13144123

申请日：2010-01-12

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

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

IPC: A01N43/58 ,  A61K31/50 ,  C07D487/00

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：US08003643B2

公开(公告)日：2011-08-23

申请号：US12621124

申请日：2009-11-18

Applicant: Mark T. Bilodeau ,  Peter C. Chua ,  Nicholas D. P. Cosford ,  Jacob M. Hoffman ,  Johnny Yasuo Nagasawa

Inventor： Mark T. Bilodeau ,  Peter C. Chua ,  Nicholas D. P. Cosford ,  Jacob M. Hoffman ,  Johnny Yasuo Nagasawa

IPC: A61P35/00 ,  A61P9/00 ,  A61P25/28 ,  C07D413/04 ,  A61K31/5377 ,  C07D401/10 ,  C07D239/26 ,  A61K31/501 ,  A61K31/506

CPC classification number: C07D417/14 ,  A61K31/501 ,  A61K31/506 ,  C07D401/14

Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines 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: 本发明涉及含有取代的哒嗪和嘧啶部分的化合物，其抑制Akt（丝氨酸/苏氨酸蛋白激酶）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。