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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。
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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。
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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：US07655649B2
公开(公告)日：2010-02-02
申请号：US11547367
申请日：2005-04-05
申请人： Mark T. Bilodeau , Peter C. Chua , Nicholas D. P. Cosford , Jacob M. Hoffman , Johnny Yasuo Nagasawa
发明人： Mark T. Bilodeau , Peter C. Chua , Nicholas D. P. Cosford , Jacob M. Hoffman , Johnny Yasuo Nagasawa
IPC分类号： C07D401/14 , C07D403/10 , C07D403/14 , C07D405/14 , C07D409/14 , C07D498/04 , C07D413/14 , C07D417/14 , C07D279/12 , C07D295/00 , C07D237/08 , C07D237/10 , C07D401/10 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D239/24 , C07D239/28 , C07D265/16 , C07D487/04 , C07D317/12 , C07F5/04 , A61P35/00
CPC分类号： C07D417/14 , A61K31/501 , A61K31/506 , C07D401/14
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US08003643B2
公开(公告)日：2011-08-23
申请号：US12621124
申请日：2009-11-18
申请人： Mark T. Bilodeau , Peter C. Chua , Nicholas D. P. Cosford , Jacob M. Hoffman , Johnny Yasuo Nagasawa
发明人： Mark T. Bilodeau , Peter C. Chua , Nicholas D. P. Cosford , Jacob M. Hoffman , Johnny Yasuo Nagasawa
IPC分类号： A61P35/00 , A61P9/00 , A61P25/28 , C07D413/04 , A61K31/5377 , C07D401/10 , C07D239/26 , A61K31/501 , A61K31/506
CPC分类号： C07D417/14 , A61K31/501 , A61K31/506 , C07D401/14
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US07589068B2
公开(公告)日：2009-09-15
申请号：US11795156
申请日：2006-02-10
申请人： Nicholas D. P. Cosford , Mark E. Layton , Jun Liang , Craig W. Lindsley , Philip E. Sanderson , Zhijian Zhao
发明人： Nicholas D. P. Cosford , Mark E. Layton , Jun Liang , Craig W. Lindsley , Philip E. Sanderson , Zhijian Zhao
IPC分类号： A01N43/04 , A01N43/58 , 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： C07D471/04
摘要： The instant invention provides for 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：US09120787B2
公开(公告)日：2015-09-01
申请号：US14238374
申请日：2012-08-27
IPC分类号： C07D239/22 , C07D417/04 , C07D417/14 , A61K31/513 , A61K31/675 , A61K45/06
CPC分类号： C07D417/14 , A61K31/513 , A61K31/675 , A61K45/06 , C07D239/22 , C07D417/04
摘要： Compounds of Formula (I) wherein B is selected from the group consisting of substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl; Y is a linker moiety selected from the group consisting of a direct bond. R, R1, R2, and R3 are each individually selected from the group consisting substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or heterocycle.
摘要翻译： 式（I）的化合物，其中B选自取代或未取代的芳基，取代或未取代的杂芳基; Y是选自直接键的连接基团。 R，R 1，R 2和R 3各自独立地选自取代或未取代的芳基，取代或未取代的杂芳基或杂环。
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公开(公告)号：US08748632B2
公开(公告)日：2014-06-10
申请号：US13051798
申请日：2011-03-18
申请人： Nicholas D. P. Cosford , Dhanya Raveendra Panickar , Shyama Sidique , Svetlana Semenova , Athinia Markou
发明人： Nicholas D. P. Cosford , Dhanya Raveendra Panickar , Shyama Sidique , Svetlana Semenova , Athinia Markou
IPC分类号： C07D209/46 , A61K31/4035
CPC分类号： C07D209/46 , A61K31/4035 , C07D209/48 , C07D215/20 , C07D217/24 , C07D261/20 , C07D275/04
摘要： The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive allosteric modulators of the metabotropic glutamate subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like.
摘要翻译： 本公开提供化合物和组合物以及使用这些化合物和组合物作为代谢型谷氨酸亚型2（mGlu2）受体的阳性变构调节剂的方法，以及用于治疗与mGlu2受体相关的CNS紊乱，包括精神分裂症，焦虑，成瘾等。 可卡因成瘾，尼古丁成瘾等。
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9.发明授权公开(公告)号：US07888355B2
公开(公告)日：2011-02-15
申请号：US12854730
申请日：2010-08-11
IPC分类号： A61K31/40 , A61K31/4406 , A61K31/215 , A61K31/165 , A61K31/16 , A61K31/5375 , A61K31/495 , C07D265/30 , C07D241/04 , C07D211/00 , C07D207/04
CPC分类号： C07C235/82 , C07C2603/52 , C07J63/008
摘要： There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
摘要翻译： 提供了抑制黑素瘤生长和转移的方法，使黑素瘤细胞对凋亡敏感的方法，以及使用乙酰基异烟酸，celastrol或其衍生物治疗患有黑素瘤的受试者的方法。 还提供了celastrol的衍生物和包含乙酰基异烟酸，celastrol或其衍生物的组合物。
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10.发明授权Heteroaryl substituted triazole modulators of metabotropic glutamate receptor-5 失效代谢型谷氨酸受体-5的杂芳基取代三唑调节剂公开(公告)号：US07105548B2
公开(公告)日：2006-09-12
申请号：US10499391
申请日：2002-12-13
申请人： Nicholas D. P. Cosford , Petpiboon Prasit , Jeffrey R. Roppe , Nicholas D. Smith , Lida R. Tehrani
发明人： Nicholas D. P. Cosford , Petpiboon Prasit , Jeffrey R. Roppe , Nicholas D. Smith , Lida R. Tehrani
IPC分类号： A61K31/44 , A61K31/41 , C07D401/00 , C07D249/04
CPC分类号： C07D401/04 , C07D401/14
摘要： Triazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl which are metabotropic glutamate receptor—subtype 5 (“mGluR5”) modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other diseases.
摘要翻译： 直接或桥接的三唑化合物与杂芳基部分相邻的杂芳基部分，杂芳基部分与杂交点相邻，杂芳基是代谢型谷氨酸受体 - 亚型5（“mGluR5”）调节剂，可用于治疗精神病和情绪障碍，例如 例如精神分裂症，焦虑症，抑郁症，双相情感障碍和恐慌，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律紊乱，药物成瘾，药物滥用，戒毒等疾病。
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