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1.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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2.发明申请公开(公告)号：US20110166216A1
公开(公告)日：2011-07-07
申请号：US13021548
申请日：2011-02-04
IPC分类号： A61K31/352 , C12N5/02 , A61P35/04
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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3.发明授权公开(公告)号：US07776894B2
公开(公告)日：2010-08-17
申请号：US12192753
申请日：2008-08-15
IPC分类号： A61K31/40 , A61K31/4406 , A61K31/215 , A61K31/165 , A61K31/16
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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公开(公告)号：US20110257233A1
公开(公告)日：2011-10-20
申请号：US13051910
申请日：2011-03-18
申请人： Nicholas D. P. Cosford , Hudson H. Freeze , Russell Dahl , Yalda Bravo , Vandana Sharma , Mie Ichikawa
发明人： Nicholas D. P. Cosford , Hudson H. Freeze , Russell Dahl , Yalda Bravo , Vandana Sharma , Mie Ichikawa
IPC分类号： A61K31/428 , A61P31/04 , A61P31/00 , A61P3/10 , A61P25/00 , A61P1/16 , A61P13/12 , C07D275/04 , A61P27/10
CPC分类号： C07D275/04
摘要： The disclosure provides new compounds and compositions thereof, and methods for treating or ameliorating a disorder relating to CDG-Ia. In particular, the disclosure provides benzoisothiazolone inhibitors of PMI, which have been synthesized and their ability to drive glycosylation has been demonstrated. The disclosure provides two synthetic routes for these compounds, including a new copper-catalyzed N-arylation reaction amenable to parallel derivitization. The disclosed compounds represent potent inhibitors of PMI, and their dose-dependent efficacy in cell-based models of glycosylation have been demonstrated. In addition, the disclosed compounds are selective over PMM and therefore, are useful in treating or ameliorating a disorder relating to CDG-Ia.
摘要翻译： 本公开提供了新的化合物及其组合物，以及用于治疗或改善与CDG-1a有关的病症的方法。 特别地，本发明提供了已经合成的PMI的苯并异噻唑酮抑制剂及其驱动糖基化的能力。 本公开为这些化合物提供了两条合成途径，包括适于平行衍生的新的铜催化的N-芳基化反应。 所公开的化合物代表有效的PMI抑制剂，并且已经证明了它们在基于细胞的糖基化模型中的剂量依赖性功效。 此外，所公开的化合物对PMM是选择性的，因此可用于治疗或改善与CDG-1a相关的病症。
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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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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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8.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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9.发明授权Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5 有权代谢型谷氨酸受体-5的杂芳基取代的吡唑调节剂公开(公告)号：US07569592B2
公开(公告)日：2009-08-04
申请号：US10497122
申请日：2002-12-13
申请人： Nicholas D. P. Cosford , Chixu Chen , Brian W. Eastman , Dehua Huang , Benito Munoz , Petpiboon Prasit , Nicholas D. Smith
发明人： Nicholas D. P. Cosford , Chixu Chen , Brian W. Eastman , Dehua Huang , Benito Munoz , Petpiboon Prasit , Nicholas D. Smith
IPC分类号： A61K31/4439 , A61K31/4155 , C07D401/04
CPC分类号： C07D231/38 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/04
摘要： Pyrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are 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, circadian rhythm disorders, and other diseases.
摘要翻译： 直接或通过桥连与杂芳基相连接的杂芳基部分的吡唑化合物是可用于治疗精神病和情绪障碍（例如精神分裂症，焦虑症，抑郁症）的mGluR5调节剂， 双相情感障碍和恐慌，以及治疗疼痛，昼夜节律紊乱和其他疾病。
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10.发明授权Di-aryl substituted pyrrole modulators of metabotropic glutamate receptor-5 失效代谢型谷氨酸受体-5的二芳基取代吡咯调节剂公开(公告)号：US07393959B2
公开(公告)日：2008-07-01
申请号：US10551574
申请日：2004-03-31
IPC分类号： C07D401/14 , A61K31/4418 , A61K31/4439
CPC分类号： A61K31/4439 , A61K31/444 , A61K31/485 , A61K31/551 , A61K33/00 , A61K45/06 , C07D401/04 , C07D401/14 , C07D417/04 , C07D417/14 , A61K2300/00
摘要： Pyrrole compounds of Formula (I): and pharmaceutically acceptable salts thereof (where A, B, R11, R12, R13, W, X, Y and Z are as defined herein), which are substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases
摘要翻译： 式（I）的吡咯化合物及其药学上可接受的盐（其中A，B，R 11，R 12，R 13，W ，X，Y和Z如本文所定义），其直接取代或通过桥连，其中i）杂芳基部分，其含有与杂芳基的连接点相邻的N，和ii）另一个杂芳基或芳基环， 至少一个被另一个环进一步取代的环是用于治疗精神病和情绪障碍例如精神分裂症，焦虑，抑郁，恐慌和双相情感障碍以及治疗疼痛的mGluR5调节剂 ，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，肥胖等疾病
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