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1. 发明授权

US08609706B2 Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 失效
标题翻译：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：US08609706B2
公开(公告)日：2013-12-17
申请号：US13472136
申请日：2012-05-15
申请人： Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence Blas Perez , Daniel A. Snyder , Thomas T. Tibbitts
发明人： Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence Blas Perez , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号： A61K31/42 , C07D261/02
CPC分类号： C07D261/02 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D413/10 , C07D413/12 , C07D417/12
摘要： The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译：本发明涉及与bcl蛋白结合并抑制Bcl功能的含异唑烷的化合物。该化合物可用于治疗和调节与过度增生相关的疾病，例如癌症。

2. 发明申请

US20130131063A1 Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners 失效
标题翻译：抑制BCL蛋白与结合伙伴相互作用的化合物和方法
公开(公告)号：US20130131063A1
公开(公告)日：2013-05-23
申请号：US13472136
申请日：2012-05-15
申请人： Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence Blas Perez , Daniel A. Snyder , Thomas T. Tibbitts
发明人： Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence Blas Perez , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号： C07D261/02 , C07D417/12 , A61K31/5377 , A61K31/454 , A61K31/496 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , C07D413/10 , C07D413/12 , A61K45/06
CPC分类号： C07D261/02 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D413/10 , C07D413/12 , C07D417/12
摘要： The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译：本发明涉及与bcl蛋白结合并抑制Bcl功能的含异唑烷的化合物。该化合物可用于治疗和调节与过度增生相关的疾病，例如癌症。

3. 发明授权

US08178690B2 Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 有权
标题翻译：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：US08178690B2
公开(公告)日：2012-05-15
申请号：US13089530
申请日：2011-04-19
申请人： Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence Blas Perez , Daniel A. Snyder , Thomas T. Tibbitts
发明人： Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence Blas Perez , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号： C07D261/02 , A61K31/42
CPC分类号： C07D261/02 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D413/10 , C07D413/12 , C07D417/12
摘要： The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译：本发明涉及与bcl蛋白结合并抑制Bcl功能的含异唑烷的化合物。该化合物可用于治疗和调节与过度增生相关的疾病，例如癌症。

4. 发明授权

US07928244B2 Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 有权
标题翻译：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：US07928244B2
公开(公告)日：2011-04-19
申请号：US11842581
申请日：2007-08-21
申请人： Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence B. Perez , Daniel A. Snyder , Thomas T. Tibbitts
发明人： Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence B. Perez , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号： C07D261/02 , A61K31/42
CPC分类号： C07D261/02 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D413/10 , C07D413/12 , C07D417/12
摘要： The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译：本发明涉及与bcl蛋白结合并抑制Bcl功能的含异唑烷的化合物。该化合物可用于治疗和调节与过度增生相关的疾病，例如癌症。

5. 发明申请

US20110213145A1 Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners 有权
标题翻译：抑制BCL蛋白与结合伙伴相互作用的化合物和方法
公开(公告)号：US20110213145A1
公开(公告)日：2011-09-01
申请号：US13089530
申请日：2011-04-19
申请人： Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence B. Perez , Daniel A. Snyder , Thomas T. Tibbitts
发明人： Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence B. Perez , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号： C07D413/12 , C07D413/10 , C07D261/02 , C07D498/04
CPC分类号： C07D261/02 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D413/10 , C07D413/12 , C07D417/12
摘要： The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译：本发明涉及与bcl蛋白结合并抑制Bcl功能的含异唑烷的化合物。该化合物可用于治疗和调节与过度增生相关的疾病，例如癌症。

6. 发明授权

US07851637B2 Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 有权
标题翻译：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：US07851637B2
公开(公告)日：2010-12-14
申请号：US11156364
申请日：2005-06-17
申请人： Alfredo C. Castro , Wei Deng , Kristopher M. Depew , Michael A. Foley , Christian C. Fritz , Asimina T. Georges Evangelinos , Michael J. Grogan , Nafeeza Hafeez , Edward B. Holson , Brian T. Hopkins , Nii O. Koney , Tao Liu , David A. Mann , Lisa A. Marcaurelle , Daniel A. Snyder , Dennis J. Underwood , Andrew A. Wylie , Lin-Chen Yu , Linping Zhang
发明人： Alfredo C. Castro , Wei Deng , Kristopher M. Depew , Michael A. Foley , Christian C. Fritz , Asimina T. Georges Evangelinos , Michael J. Grogan , Nafeeza Hafeez , Edward B. Holson , Brian T. Hopkins , Nii O. Koney , Tao Liu , David A. Mann , Lisa A. Marcaurelle , Daniel A. Snyder , Dennis J. Underwood , Andrew A. 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.
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。

7. 发明授权

US06824987B1 Small molecule printing 失效
标题翻译：小分子印刷
公开(公告)号：US06824987B1
公开(公告)日：2004-11-30
申请号：US09567910
申请日：2000-05-10
申请人： Stuart L. Schreiber , Gavin MacBeath , Angela N. Koehler , Paul Hergenrother , Kristopher M. Depew
发明人： Stuart L. Schreiber , Gavin MacBeath , Angela N. Koehler , Paul Hergenrother , Kristopher M. Depew
IPC分类号： G01N3353
CPC分类号： G01N31/00 , B01J19/0046 , B01J2219/00387 , B01J2219/00454 , B01J2219/00459 , B01J2219/005 , B01J2219/00533 , B01J2219/00605 , B01J2219/0061 , B01J2219/00612 , B01J2219/00626 , B01J2219/00637 , B01J2219/0072 , C07B2200/11 , C07C311/49 , C40B30/04 , C40B40/04 , C40B50/14 , C40B60/14 , G01N33/54353 , Y10S436/809
摘要： The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction. In general, these inventive arrays are generated by: (1) providing a solid support, wherein said solid support is functionalized with a selected chemical moiety capable of interacting with a desired chemical compound to form an attachment; (2) providing one or more solutions of one or more types of compounds to be attached to the solid support; and (3) delivering said one or more types of compounds to the solid support, whereby an array is formed and the array of compounds has a density of at least 1000 spots per cm2. In another aspect, the present invention provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest comprising: (1) providing an array of compounds, wherein the array has a density of at least 1000 spots per cm2; (2) contacting the array with one of more types of biological macromolecules of interest; and (3) determining the interaction of specific small molecule-biological macromolecule partners.
摘要翻译：本发明提供了有助于鉴定能够与感兴趣的生物大分子相互作用的化合物的组合物和方法。在一个方面，提供了包含连接到固体支持物上的一种或多种类型化学化合物的阵列的组合物，其中化合物阵列的密度为至少1000个斑点/ cm 2。在特别优选的实施方案中，这些化合物通过共价相互作用连接到固体支持物上。通常，这些本发明的阵列通过以下方式产生：（1）提供固体支持物，其中所述固体支持物用能够与所需化学化合物相互作用以形成附着物的选定化学部分官能化; （2）提供待连接到固体支持物上的一种或多种类型化合物的一种或多种溶液; 和（3）将所述一种或多种类型的化合物递送到固体支持物，由此形成阵列，并且所述化合物阵列的密度至少为1000个点/ cm 2。另一方面，本发明提供了利用这些阵列来识别感兴趣的生物大分子的小分子配偶体的方法，包括：（1）提供化合物阵列，其中阵列的密度至少为1000个点/ cm 2 ; （2）使阵列与感兴趣的多种生物大分子之一接触; 和（3）确定特定小分子 - 生物大分子伴侣的相互作用。

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