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公开(公告)号：US20110319443A1
公开(公告)日：2011-12-29
申请号：US13255757
申请日：2010-03-03
IPC分类号： A61K31/4375 , A61P35/00 , C07D471/04
CPC分类号： A61K31/4375 , C07D471/04
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
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公开(公告)号：US08008317B2
公开(公告)日：2011-08-30
申请号：US11921352
申请日：2006-06-07
申请人： Donna J. Armstrong , Essa H. Hu , Michael J. Kelly, III , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Michael J. Rossi , Philip E. Sanderson , Jiabing Wang
发明人： Donna J. Armstrong , Essa H. Hu , Michael J. Kelly, III , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Michael J. Rossi , Philip E. Sanderson , Jiabing Wang
IPC分类号： A61K31/437 , A61K31/4375 , C07D471/14 , C07D471/16
CPC分类号： C07D471/14 , C07D487/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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公开(公告)号：US08168652B2
公开(公告)日：2012-05-01
申请号：US13255757
申请日：2010-03-03
IPC分类号： A61K31/44 , C07D471/02
CPC分类号： A61K31/4375 , C07D471/04
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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公开(公告)号：US20100022573A1
公开(公告)日：2010-01-28
申请号：US12517492
申请日：2007-12-04
IPC分类号： A61K31/4375 , C07D471/14
CPC分类号： C07D471/14 , C07D519/00
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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![Substituted [1,2,4]triazolo[4′,3′:1,6]pyrido[2,3-b]pyrazines of the formula D](/abs-image/US/2012/06/26/US08207169B2/abs.jpg.150x150.jpg)
5.发明授权Substituted [1,2,4]triazolo[4′,3′:1,6]pyrido[2,3-b]pyrazines of the formula D 有权取代的[1,2,4]三唑并[4'，3'：1,6]吡啶并[2,3-b]公开(公告)号：US08207169B2
公开(公告)日：2012-06-26
申请号：US12995832
申请日：2009-05-28
申请人： Hidetomo Furuyama , Yasuhiro Goto , Nobuhiko Kawanishi , Mark E. Layton , Takashi Mita , Akira Naya , Yoshio Ogino , Yu Onozaki , Kevin J. Rodzinak , Toshihiro Sakamoto , Philip E. Sanderson , Jiabing Wang
发明人： Hidetomo Furuyama , Yasuhiro Goto , Nobuhiko Kawanishi , Mark E. Layton , Takashi Mita , Akira Naya , Yoshio Ogino , Yu Onozaki , Kevin J. Rodzinak , Toshihiro Sakamoto , Philip E. Sanderson , Jiabing Wang
IPC分类号： A61K31/495
CPC分类号： C07D471/14
摘要： The compounds of Formula D are of the class of triazolo-pyrido-pyrazines which are inhibitors of AKT useful for the treatment of cancer
摘要翻译： 式D的化合物是三唑并 - 吡啶并吡嗪类，其是可用于治疗癌症的AKT抑制剂
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公开(公告)号：US20110092511A1
公开(公告)日：2011-04-21
申请号：US12995832
申请日：2009-05-28
申请人： Hidetomo Furuyama , Yasuhiro Goto , Nobuhiko Kawanishi , Mark E. Layton , Takashi Mita , Akira Naya , Yoshio Ogino , Yu Onozaki , Kevin J. Rodzinak , Toshihiro Sakamoto , Philip E. Sanderson , Jiabing Wang
发明人： Hidetomo Furuyama , Yasuhiro Goto , Nobuhiko Kawanishi , Mark E. Layton , Takashi Mita , Akira Naya , Yoshio Ogino , Yu Onozaki , Kevin J. Rodzinak , Toshihiro Sakamoto , Philip E. Sanderson , Jiabing Wang
IPC分类号： A61K31/4985 , C07D471/14 , A61K31/4375 , C07D403/14 , A61K31/506 , A61P35/00
CPC分类号： C07D471/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity especially Akt1 by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型，优选Akt1。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性，尤其是Akt1的方法。
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公开(公告)号：US20100222321A1
公开(公告)日：2010-09-02
申请号：US11921352
申请日：2006-06-07
申请人： Donna J. Armstrong , Essa H. Hu , Michael J. Kelly, III , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Michael A. Rossi , Philip E. Sanderson , Jiabing Wang
发明人： Donna J. Armstrong , Essa H. Hu , Michael J. Kelly, III , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Michael A. Rossi , Philip E. Sanderson , Jiabing Wang
IPC分类号： A61K31/4375 , C07D471/14 , A61K31/496 , A61K31/519 , A61K31/506 , C07D513/04 , A61K31/501 , A61K31/5377 , A61K31/517 , A61K31/4709 , A61P35/00
CPC分类号： C07D471/14 , C07D487/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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公开(公告)号：US20130143880A1
公开(公告)日：2013-06-06
申请号：US13814870
申请日：2011-08-05
申请人： Vadim Y. Dudkin , Mark E. Fraley , Kenneth L. Arrington , Mark E. Layton , Alexander J. Reif , Kevin J. Rodzinak , Joseph E. Pero
发明人： Vadim Y. Dudkin , Mark E. Fraley , Kenneth L. Arrington , Mark E. Layton , Alexander J. Reif , Kevin J. Rodzinak , Joseph E. Pero
IPC分类号： A61K31/4745 , C07D235/26 , A61K31/4439 , C07D417/14 , C07D405/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D413/10 , C07D409/10 , C07D405/10 , A61K31/4184 , C07D413/02 , C07D401/02 , C07D403/02 , A61K31/4709 , C07D471/04
CPC分类号： C07D235/26 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/14 , C07D453/02 , C07D471/04 , C07D513/14
摘要： The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 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 metabotropic glutamate receptors are involved, such as schizophrenia.
摘要翻译： 本发明涉及作为mGluR2受体的正变构调节剂的苯并咪唑酮衍生物，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及mGluR2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代谢型谷氨酸受体的疾病如精神分裂症中的用途。
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公开(公告)号：US07910561B2
公开(公告)日：2011-03-22
申请号：US11792121
申请日：2005-12-09
申请人： 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
发明人： 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分类号： A01N43/04 , A01N43/58 , A01N43/42 , A61K31/541 , A61K31/70 , A61K31/50 , A61K31/495 , A61K31/52 , C09B25/00 , C07D487/00 , C07D491/00 , C07H15/00
CPC分类号： C07D471/04
摘要： 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.
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。 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。
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公开(公告)号：US08993779B2
公开(公告)日：2015-03-31
申请号：US13814870
申请日：2011-08-05
申请人： Vadim Y. Dudkin , Mark E. Fraley , Kenneth L. Arrington , Mark E. Layton , Alexander J. Reif , Kevin J. Rodzinak , Joseph E. Pero
发明人： Vadim Y. Dudkin , Mark E. Fraley , Kenneth L. Arrington , Mark E. Layton , Alexander J. Reif , Kevin J. Rodzinak , Joseph E. Pero
IPC分类号： C07D235/26 , C07D417/14 , C07D403/04 , C07D403/14 , C07D401/04 , C07D401/14 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/06 , C07D453/02 , C07D513/14 , C07D405/10 , C07D409/10 , C07D413/10 , C07D471/04
CPC分类号： C07D235/26 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/14 , C07D453/02 , C07D471/04 , C07D513/14
摘要： The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 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 metabotropic glutamate receptors are involved, such as schizophrenia.
摘要翻译： 本发明涉及作为mGluR2受体的正变构调节剂的苯并咪唑酮衍生物，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及mGluR2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代谢型谷氨酸受体的疾病如精神分裂症中的用途。
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