公开(公告)号：US07223738B2

公开(公告)日：2007-05-29

申请号：US10510069

申请日：2003-04-04

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

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

IPC分类号： 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分类号： C07D401/10 ,  A61K31/498 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

摘要： 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：US07579355B2

公开(公告)日：2009-08-25

申请号：US10554001

申请日：2004-04-20

申请人： Mark T. Bilodeau ,  Mark E. Duggan ,  John C. Hartnett ,  Craig W. Lindsley ,  Zhicai Wu ,  Zhijian Zhao

发明人： Mark T. Bilodeau ,  Mark E. Duggan ,  John C. Hartnett ,  Craig W. Lindsley ,  Zhicai Wu ,  Zhijian Zhao

IPC分类号： A61K31/52 ,  C07D401/14

CPC分类号： C07F9/65583 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

摘要： The present invention is directed to compounds which contain a substituted pyridine moeity 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.

摘要翻译： 本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代吡啶甲氧基化合物。 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：US07304063B2

公开(公告)日：2007-12-04

申请号：US10554186

申请日：2004-04-20

申请人： Mark T. Bilodeau ,  Craig W. Lindsley ,  Zhijian Zhao

发明人： Mark T. Bilodeau ,  Craig W. Lindsley ,  Zhijian Zhao

IPC分类号： C07D401/10 ,  C07D403/10 ,  A61K31/53 ,  A61P35/00 ,  C07D253/06

CPC分类号： C07D417/14 ,  C07D253/065 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

摘要： The present invention is directed to compounds which contain a heterocyclic triazine 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.

摘要翻译： 本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的杂环三嗪部分的化合物。 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：US20080280899A1

公开(公告)日：2008-11-13

申请号：US11547113

申请日：2005-04-05

申请人： 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

发明人： 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分类号： A61K31/519 ,  C07D471/04 ,  A61K31/4375 ,  A61P35/00 ,  A61K31/5377 ,  C07D413/12

CPC分类号： C07D471/04 ,  C07D519/00

摘要： 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.

摘要翻译： 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：US07750151B2

公开(公告)日：2010-07-06

申请号：US11547113

申请日：2005-04-05

申请人： 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

发明人： 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分类号： C07D471/04 ,  C07D413/12 ,  C07D521/00 ,  C07D401/14 ,  C07D487/08 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： 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.

摘要翻译： 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：US20090325936A1

公开(公告)日：2009-12-31

申请号：US12519789

申请日：2007-12-14

申请人： Mark T. Bilodeau ,  Christopher S. Burgey ,  Zhengwu James Deng ,  Nathan R. Kett ,  Jeffrey Melamed ,  Peter M. Munson ,  Kausik K. Nanda ,  Wayne Thompson ,  B. Wesley Trotter ,  Zhicai Wu ,  John C. Hartnett

发明人： Mark T. Bilodeau ,  Christopher S. Burgey ,  Zhengwu James Deng ,  Nathan R. Kett ,  Jeffrey Melamed ,  Peter M. Munson ,  Kausik K. Nanda ,  Wayne Thompson ,  B. Wesley Trotter ,  Zhicai Wu ,  John C. Hartnett

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61K31/506 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/541 ,  A61P19/00 ,  A61P25/00

CPC分类号： C07D471/04

摘要： The present invention relates to compounds represented by Formula (I) and Formula (II): (I) (II) or 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.

摘要翻译： 本发明涉及由式（I）和式（II）表示的化合物：（I）（II）或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：US07544677B2

公开(公告)日：2009-06-09

申请号：US11659606

申请日：2005-08-19

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

发明人： 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分类号： A61K31/541 ,  A61K31/5355 ,  A61K31/519 ,  C07D471/04 ,  C07D519/00 ,  A61P35/00

CPC分类号： C07D471/04

摘要： 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.

摘要翻译： 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：US20120196894A1

公开(公告)日：2012-08-02

申请号：US13499844

申请日：2010-09-28

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

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

IPC分类号： A61K31/136 ,  C07D215/38 ,  A61K31/47 ,  C07C255/59 ,  A61K31/4706 ,  C07D311/74 ,  A61K31/352 ,  A61P29/00 ,  C07D215/44 ,  C07C211/48 ,  A61K31/277

CPC分类号： 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

摘要： 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.

摘要翻译： 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：US08389720B2

公开(公告)日：2013-03-05

申请号：US13127898

申请日：2009-11-03

申请人： 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

发明人： 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分类号： A61K31/551 ,  A61K31/5355 ,  A61K31/497 ,  A61K31/519 ,  A61K31/4412 ,  A61K31/4704 ,  C07D243/08 ,  C07D413/14 ,  C07D471/04 ,  C07D401/14 ,  C07D401/12 ,  C07D405/14

CPC分类号： A61K31/47 ,  C07D401/12 ,  C07D405/12

摘要： 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.

摘要翻译： 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：US20110212946A1

公开(公告)日：2011-09-01

申请号：US13127898

申请日：2009-11-03

申请人： 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

发明人： 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分类号： A61K31/4704 ,  C07D405/14 ,  A61K31/496 ,  A61K31/55 ,  C07D401/12 ,  A61K31/4709 ,  C07D413/12 ,  A61K31/5377 ,  C07D215/227 ,  A61P25/00

CPC分类号： A61K31/47 ,  C07D401/12 ,  C07D405/12

摘要： 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.

摘要翻译： 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。