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1.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。
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2.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。
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3.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。
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4.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。
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5.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。
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公开(公告)号:US20140371456A1
公开(公告)日:2014-12-18
申请号:US14257658
申请日:2014-04-21
申请人: Brian C. Austad , Adilah Bahadoor , Jitendra D. Belani , Somarajannair Janardanannair , Sheldon L. Wallerstein , Gregg F. Keaney , Priscilla L. White , Charles W. Johannes
发明人: Brian C. Austad , Adilah Bahadoor , Jitendra D. Belani , Somarajannair Janardanannair , Sheldon L. Wallerstein , Gregg F. Keaney , Priscilla L. White , Charles W. Johannes
IPC分类号: C07D491/107 , C12P17/18
CPC分类号: C12P17/18 , C07D491/10 , C07D491/107
摘要: Provided are processes for the synthesis of amino analogues from ketone starting materials.
摘要翻译: 提供了从酮起始原料合成氨基类似物的方法。
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公开(公告)号:US08703448B2
公开(公告)日:2014-04-22
申请号:US13175053
申请日:2011-07-01
申请人: Brian C. Austad , Adilah Bahadoor , Jitendra D. Belani , Somarajannair Janardanannair , Charles W. Johannes , Gregg F. Keaney , Priscilla L. White , Sheldon L. Wallerstein
发明人: Brian C. Austad , Adilah Bahadoor , Jitendra D. Belani , Somarajannair Janardanannair , Charles W. Johannes , Gregg F. Keaney , Priscilla L. White , Sheldon L. Wallerstein
IPC分类号: C12P17/18
CPC分类号: C12P17/18 , C07D491/10 , C07D491/107
摘要: The invention relates to the preparation of amino-cyclopamines by the enzymatic transamination of a corresponding keto-cyclopamines in the presence of a cofactor and an amino donor.
摘要翻译: 本发明涉及在辅因子和氨基供体的存在下通过相应的酮 - 环胺的酶转氨酸制备氨基 - 环胺。
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公开(公告)号:US20120083607A1
公开(公告)日:2012-04-05
申请号:US13175053
申请日:2011-07-01
申请人: Brian c. Austad , Adilah Bahadoor , Jitendra D. Belani , Somarajannair Janardanannair , Charles W. Johannes , Gregg F. Keaney , Priscilla L. White , Sheldon L. Wallerstein
发明人: Brian c. Austad , Adilah Bahadoor , Jitendra D. Belani , Somarajannair Janardanannair , Charles W. Johannes , Gregg F. Keaney , Priscilla L. White , Sheldon L. Wallerstein
IPC分类号: C07D491/048 , C12P17/18
CPC分类号: C12P17/18 , C07D491/10 , C07D491/107
摘要: Provided are processes for the synthesis of amino analogues from ketone starting materials.
摘要翻译: 提供了从酮起始原料合成氨基类似物的方法。
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公开(公告)号:US20230083431A1
公开(公告)日:2023-03-16
申请号:US17783224
申请日:2020-12-15
申请人: Nicolas C. BOYER , Michael B. GARRIGOU , Sookhee Nicole HA , Chunhui HUANG , Anthony W. PARTRIDGE , Tomi K. SAWYER , Pietro ARONICA , Charles W. JOHANNES , Srinivasaraghavan KANNAN , Chandra S. VERMA , Tsz Ying YUEN , Merck Sharp & Dohme LLC , MSD International GMBH (Singapore Branch) , Agency for Science, Technology and Research
发明人: Nicolas C. Boyer , Michael B. Garrigou , Sookhee Nicole Ha , Chunhui Huang , Anthony W. Partridge , Tomi K. Sawyer , Pietro Aronica , Charles W. Johannes , Srinivasaraghavan Kannan , Chandra S. Verma , Tsz Ying Yuen
摘要: The invention provides compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein the variables are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12D mutant of Kirsten rat sarcoma (K-Ras) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
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公开(公告)号:US20220267376A1
公开(公告)日:2022-08-25
申请号:US17618751
申请日:2020-06-16
申请人: Tomi K. SAWYER , Pietro ARONICA , Christopher J. BROWN , Fernando J. FERRER , Charles W. JOHANNES , Srinivasaraghavan KANNAN , David P. LANE , Anthony W. PARTRIDGE , Yaw Sing TAN , Chandra S. VERMA , Tsz Ying YUEN , Merck Sharp & Dohme Corp. , Agency for Science, Technology and Research , MSD International GMBH (Singapore Branch)
发明人: Pietro Aronica , Christopher J. Brown , Fernando J. Ferrer , Charles W. Johannes , Srinivasaraghavan Kannan , David P. Lane , Anthony W. Partridge , Tomi K. Sawyer , Yaw Sing Tan , Chandra S. Verma , Tsz Ying Yuen
摘要: Peptidomimetic macrocycles that comprise all-D configuration ?-amino acids and bind mouse double minute 2 (MDM2 aka E3 ubiquitin-protein ligase) and MDMX (aka MDM4) are described. These all-D configuration α-amino acid peptidomimetic macrocycles are protease resistant, cell permeable without inducing membrane disruption, and intracellularly activate p53 by binding MDM2 and MDMX thereby antagonizing MDM2 and MDMX binding to p53. These peptidomimetic macrocycles may be useful in anticancer therapies, particularly in combination with chemotherapy or radiation therapy.
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