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11.发明申请Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 有权抑制BCL蛋白与结合配偶体相互作用的化合物和方法公开(公告)号：US20070161690A1
公开(公告)日：2007-07-12
申请号：US11600332
申请日：2006-11-15
申请人： Alfredo Castro , Edward Holson , Brian Hopkins , Nii Koney , Daniel Snyder , Thomas Tibbitts
发明人： Alfredo Castro , Edward Holson , Brian Hopkins , Nii Koney , Daniel Snyder , Thomas Tibbitts
IPC分类号： A61K31/42 , C07D413/02 , C07D261/02
CPC分类号： C07D261/02 , C07D261/18 , C07D413/10 , C07D413/12 , C07D417/12 , C07D498/04
摘要： One aspect of the present invention relates to heterocyclic compounds that bind to bcl proteins and inhibit Bcl function. Another aspect of the present invention relates to compositions comprising a heterocyclic compound of the invention. The present invention provides methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译： 本发明的一个方面涉及结合bcl蛋白并抑制Bcl功能的杂环化合物。 本发明的另一方面涉及包含本发明的杂环化合物的组合物。 本发明提供了治疗和调节与过度增生相关的疾病如癌症的方法。
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公开(公告)号：US06166037A
公开(公告)日：2000-12-26
申请号：US141227
申请日：1998-08-27
申请人： Richard J. Budhu , Edward Holson , Jeffrey J. Hale , Christopher Lynch , Malcolm Maccoss , Scott C. Berk , Sander G. Mills , Christopher A. Willoughby
发明人： Richard J. Budhu , Edward Holson , Jeffrey J. Hale , Christopher Lynch , Malcolm Maccoss , Scott C. Berk , Sander G. Mills , Christopher A. Willoughby
IPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D495/10 , A61K31/445
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D495/10
摘要： The present invention is directed to pyrrolidine and piperidine compounds of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.4d, R.sup.4e, R.sup.4f, R.sup.4g, R.sup.4h, m, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
摘要翻译： 本发明涉及式I的吡咯烷和哌啶化合物：其中R1，R2，R3，R4a，R4b，R4c，R4d，R4e，R4f，R4g，R4h，m，n，x和y定义如下） 其可用作趋化因子受体活性的调节剂。 特别地，这些化合物可用作趋化因子受体CCR-1，CCR-2，CCR-2A，CCR-2B，CCR-3，CCR-4，CCR-5，CXCR-3和/或CXCR- 4。
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13.发明授权Use of CI-994 and dinaline for the treatment of memory/cognition and anxiety disorders 有权使用CI-994和迪拉尼碱治疗记忆/认知和焦虑症公开(公告)号：US08841346B2
公开(公告)日：2014-09-23
申请号：US13595048
申请日：2012-08-27
申请人： Li-Huei Tsai , Ji-Song Guan , Stephen J. Haggarty , Edward Holson , Florence Wagner , Johannes Graeff
发明人： Li-Huei Tsai , Ji-Song Guan , Stephen J. Haggarty , Edward Holson , Florence Wagner , Johannes Graeff
IPC分类号： A01N37/18 , A61K31/16 , A61K31/165 , A61K31/195 , C07C237/42 , A61K45/06 , A61K31/167
CPC分类号： A61K31/195 , A61K31/167 , A61K45/06 , C07C237/42 , A61K2300/00
摘要： The invention relates to methods and compositions for promoting cognitive function and/or treating cognitive function disorders and impairments. In particular the methods are accomplished by administering to a subject CI-994 or dinaline or a pharmaceutically acceptable salt, ester, prodrug or metabolite thereof.
摘要翻译： 本发明涉及用于促进认知功能和/或治疗认知功能障碍和损伤的方法和组合物。 特别地，所述方法通过给予受试者CI-994或迪拉丁胺或其药学上可接受的盐，酯，前药或代谢物来完成。
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公开(公告)号：US08729130B2
公开(公告)日：2014-05-20
申请号：US13620761
申请日：2012-09-15
IPC分类号： A61K31/167 , C07C237/40 , A61P25/28 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/30
CPC分类号： C07C233/80 , A61K31/167 , C07B2200/13 , C07C231/12 , C07C237/42
摘要： Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Forms A, B, and D, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline tacedinaline Forms A, B, and D, the novel crystalline tacedinaline TFA salt, and/or amorphous tacedinaline, and methods of treating various conditions by administering those novel solid forms, are also disclosed.
摘要翻译： 披露了一种新型固体形式的tacedinaline（4-（乙酰氨基）-N-（2-氨基苯基）苯甲酰胺），包括结晶的tacedinaline形式A，B和D，一种新型结晶的tacedineine TFA盐和无定形tacedinaline。 还公开了包含结晶哌啶酮A，B和D的药物组合物，新型结晶哌啶盐酸盐TFA盐和/或无定形泼尼汀，以及通过施用这些新型固体形式治疗各种病症的方法。
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15.发明申请USE OF CI-994 AND DINALINE FOR THE TREATMENT OF MEMORY/COGNITION AND ANXIETY DISORDERS 有权CI-994和DINALINE用于治疗记忆/认知和恶心疾病的使用公开(公告)号：US20110224303A1
公开(公告)日：2011-09-15
申请号：US12917402
申请日：2010-11-01
申请人： Li-Huei Tsai , Ji-Song Guan , Stephen J. Haggarty , Edward Holson , Florence Wagner , Johannes Graeff
发明人： Li-Huei Tsai , Ji-Song Guan , Stephen J. Haggarty , Edward Holson , Florence Wagner , Johannes Graeff
IPC分类号： A61K31/167 , C07C237/40 , A61P25/28 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/30
CPC分类号： A61K31/195 , A61K31/167 , A61K45/06 , C07C237/42 , A61K2300/00
摘要： The invention relates to methods and compositions for promoting cognitive function and/or treating cognitive function disorders and impairments. In particular the methods are accomplished by administering to a subject CI-994 or dinaline or a pharmaceutically acceptable salt, ester, prodrug or metabolite thereof.
摘要翻译： 本发明涉及用于促进认知功能和/或治疗认知功能障碍和损伤的方法和组合物。 特别地，所述方法通过给予受试者CI-994或迪拉丁胺或其药学上可接受的盐，酯，前药或代谢物来完成。
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16.发明申请Uses of chemicals to modulate GSK-3 signaling for treatment of bipolar disorder and other brain disorders 有权使用化学物质调节GSK-3信号治疗双相障碍和其他脑部疾病公开(公告)号：US20110008468A1
公开(公告)日：2011-01-13
申请号：US12660591
申请日：2010-02-27
申请人： Stephen J. Haggarty , Daniel Fass , Jennifer Pan , Josh Ketterman , Edward Holson , Tracey Lynn Petryshen , Michael C. Lewis
发明人： Stephen J. Haggarty , Daniel Fass , Jennifer Pan , Josh Ketterman , Edward Holson , Tracey Lynn Petryshen , Michael C. Lewis
IPC分类号： A61K33/00 , A61K31/407 , A61K31/4545 , A61K31/404 , A61K31/553 , A61K31/506 , A61P25/00
CPC分类号： A61K31/515 , A61K31/675 , A61K33/00 , A61K45/06 , A61K2300/00
摘要： Aspects of this invention are related, at least in part, to the use of chemical compounds able to inhibit GSK-3 and/or to stabilize β-catenin and formulations thereof. Some aspects of this invention relate to compositions comprising such compounds. Some aspects of the invention provide methods of using such compounds and/or compositions in the treatment of subjects having a neurological disease and/or psychiatric disorder. Some aspects of this invention provide methods of using ruboxistaurin, enzastaurin, sunitinib, midostaurin, lestaurtinib, 7-hydroxystaurosporine, and/or Chir99021 in the treatment of subjects having a neurological disease and/or psychiatric disorder. In some embodiments, compounds are administered in combination with Lithium.
摘要翻译： 本发明的方面至少部分地涉及能够抑制GSK-3和/或稳定β-联蛋白及其制剂的化学化合物的用途。 本发明的一些方面涉及包含这些化合物的组合物。 本发明的一些方面提供了使用这些化合物和/或组合物来治疗患有神经疾病和/或精神障碍的受试者的方法。 本发明的一些方面提供了在治疗患有神经系统疾病和/或精神障碍的受试者时使用ruboxistaurin，enzastaurin，舒尼替尼，midostaurin，lestaurtinib，7-羟基头孢菌素和/或Chir99021的方法。 在一些实施方案中，化合物与锂组合施用。
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17.发明申请Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 有权抑制BCL蛋白与结合配偶体相互作用的化合物和方法公开(公告)号：US20070155705A1
公开(公告)日：2007-07-05
申请号：US11640480
申请日：2006-12-15
申请人： Alfredo Castro , Michael Grogan , Edward Holson , Brian Hopkins , Nii Koney , Stephane Peluso , Daniel Snyder
发明人： Alfredo Castro , Michael Grogan , Edward Holson , Brian Hopkins , Nii Koney , Stephane Peluso , Daniel Snyder
IPC分类号： A61K31/66 , A61K31/421 , A61K31/426 , C07F9/02
CPC分类号： C07D207/16 , C07D207/08 , C07D207/12 , C07D207/14 , C07D211/60 , C07D233/32 , C07D265/30 , C07D277/04 , C07D277/06 , C07D295/04
摘要： The present invention relates to heterocyclic compounds that bind to Bcl proteins and inhibit Bcl function, compositions comprising such compounds, and methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译： 本发明涉及结合Bcl蛋白并抑制Bcl功能的杂环化合物，包含这些化合物的组合物，以及用于治疗和调节与过度增殖相关的疾病如癌症的方法。
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18.发明申请公开(公告)号：US20060025460A1
公开(公告)日：2006-02-02
申请号：US11156364
申请日：2005-06-17
申请人： Alfredo Castro , Wei Deng , Kristopher Depew , Michael Foley , Christian Fritz , Asimina Georges Evangelinos , Michael Grogan , Nafeeza Hafeez , Edward Holson , Brian Hopkins , Nii Koney , Tao Liu , David Mann , Lisa Marcaurelle , Daniel Snyder , Dennis Underwood , Andrew Wylie , Lin-Chen Yu , Linping Zhang
发明人： Alfredo Castro , Wei Deng , Kristopher Depew , Michael Foley , Christian Fritz , Asimina Georges Evangelinos , Michael Grogan , Nafeeza Hafeez , Edward Holson , Brian Hopkins , Nii Koney , Tao Liu , David Mann , Lisa Marcaurelle , Daniel Snyder , Dennis Underwood , Andrew Wylie , Lin-Chen Yu , Linping Zhang
IPC分类号： C07D261/02 , A61K31/42
CPC分类号： C07D261/02 , C07D261/18 , C07D413/10 , C07D413/12 , C07D417/12 , C07D498/04
摘要： One aspect of the present invention relates to heterocyclic compounds that bind to bcl proteins and inhibit Bcl function. Another aspect of the present invention relates to compositions comprising a heterocyclic compound of the invention. The present invention provides methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
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公开(公告)号：US20140107141A1
公开(公告)日：2014-04-17
申请号：US14052661
申请日：2013-10-11
申请人： Florence Fevrier Wagner , Jennifer Q. Pan , Sivaraman Dandapani , Andrew Germain , Edward Holson , Benito Munoz , Partha P. Nag , Michel Weiwer , Michael C. Lewis , Stephen J. Haggarty , Joshua A. Bishop
发明人： Florence Fevrier Wagner , Jennifer Q. Pan , Sivaraman Dandapani , Andrew Germain , Edward Holson , Benito Munoz , Partha P. Nag , Michel Weiwer , Michael C. Lewis , Stephen J. Haggarty , Joshua A. Bishop
IPC分类号： C07D471/04 , C07D471/10
CPC分类号： A61K31/4745 , A61K31/4747 , C07D471/04 , C07D471/10
摘要： The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3α or GSK3β) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychriatic disorders, metabolic disorders, and cancer.
摘要翻译： 本发明提供式I化合物，其药学上可接受的盐及其药物组合物。 本发明的化合物可用于抑制激酶（例如GSK3（例如GSK3α或GSK3和bgr））或CK1）活性。 本发明还提供使用本文所述化合物治疗激酶介导的疾病如神经疾病，精神障碍，代谢紊乱和癌症的方法。
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20.发明申请Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 有权抑制BCL蛋白与结合配偶体相互作用的化合物和方法公开(公告)号：US20080306127A9
公开(公告)日：2008-12-11
申请号：US11600332
申请日：2006-11-15
申请人： Alfredo Castro , Edward Holson , Brian Hopkins , Nii Koney , Daniel Snyder , Thomas Tibbitts
发明人： Alfredo Castro , Edward Holson , Brian Hopkins , Nii Koney , Daniel Snyder , Thomas Tibbitts
IPC分类号： A61K31/42 , C07D413/02 , C07D261/02
CPC分类号： C07D261/02 , C07D261/18 , C07D413/10 , C07D413/12 , C07D417/12 , C07D498/04
摘要： One aspect of the present invention relates to heterocyclic compounds that bind to bcl proteins and inhibit Bcl function. Another aspect of the present invention relates to compositions comprising a heterocyclic compound of the invention. The present invention provides methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译： 本发明的一个方面涉及结合bcl蛋白并抑制Bcl功能的杂环化合物。 本发明的另一方面涉及包含本发明的杂环化合物的组合物。 本发明提供了治疗和调节与过度增生相关的疾病如癌症的方法。
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