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公开(公告)号：WO2010048559A3
公开(公告)日：2010-07-08
申请号：PCT/US2009061927
申请日：2009-10-23
Applicant: CALCIMEDICA INC , WHITTEN JEFFREY P , PEI YAZHONG , STAUDERMAN KENNETH A , ROOS JACK
Inventor： WHITTEN JEFFREY P , PEI YAZHONG , STAUDERMAN KENNETH A , ROOS JACK
IPC: A61K31/415 , A61P19/02 , A61P29/00
CPC classification number: A61K31/415 , C07D231/12 , C07D231/14 , C07D409/12 , C07D417/12
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.
Abstract translation: 本文描述了含有这种化合物的化合物和药物组合物，其调节商店操作的钙（SOC）通道的活性。 本文还描述了单独使用此类SOC通道调节剂并与其他化合物组合用于治疗将受益于SOC通道活性抑制的疾病，病症或病症的方法。
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公开(公告)号：WO2010027875A3
公开(公告)日：2010-06-10
申请号：PCT/US2009055090
申请日：2009-08-26
Applicant: CALCIMEDICA INC , VELICELEBI GONUL , STAUDERMAN KENNETH A , WHITTEN JEFFREY P , PEI YAZHONG , CAO JIANGUO , WANG ZHIJUN , ROGERS EVAN , DYCK BRIAN , GREY JONATHAN
Inventor： VELICELEBI GONUL , STAUDERMAN KENNETH A , WHITTEN JEFFREY P , PEI YAZHONG , CAO JIANGUO , WANG ZHIJUN , ROGERS EVAN , DYCK BRIAN , GREY JONATHAN
IPC: C07D409/02 , A61K31/415 , A61P19/00 , A61P19/02 , A61P25/28 , C07D231/56 , C07D277/60 , C07D413/12 , C07D495/04
CPC classification number: C07D409/04 , C07D333/38 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
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公开(公告)号：WO2008148108A1
公开(公告)日：2008-12-04
申请号：PCT/US2008/064915
申请日：2008-05-27
Applicant: CALCIMEDICA, INC. , STAUDERMAN, Kenneth, A. , ROOS, Jack , VELICELEBI, Gonul
Inventor： STAUDERMAN, Kenneth, A. , ROOS, Jack , VELICELEBI, Gonul
IPC: A61K38/17 , C07H21/04 , C07K14/435
CPC classification number: G01N33/5008 , G01N33/5076 , G01N33/6872 , G01N2333/705
Abstract: Described herein are compositions and uses thereof related to Ca 2+ release-activated Ca 2+ (CRAC) channel activity. Also described herein CRAC channel modulators for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
Abstract translation: 本文描述了与Ca 2+释放激活的Ca2 +（CRAC）通道活性相关的组合物和用途。 本文还描述了用于治疗将受益于SOC通道活性抑制的疾病或病症的CRAC通道调节剂。
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公开(公告)号：WO2010034003A3
公开(公告)日：2010-07-01
申请号：PCT/US2009057883
申请日：2009-09-22
Applicant: CALCIMEDICA INC , WHITTEN JEFFREY P , PEI YAZHONG , STAUDERMAN KENNETH A , ROOS JACK
Inventor： WHITTEN JEFFREY P , PEI YAZHONG , STAUDERMAN KENNETH A , ROOS JACK
CPC classification number: A61K31/41
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.
Abstract translation: 本文描述了含有这种化合物的化合物和药物组合物，其调节商店操作的钙（SOC）通道的活性。 本文还描述了单独使用此类SOC通道调节剂并与其他化合物组合用于治疗将受益于SOC通道活性抑制的疾病，病症或病症的方法。
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公开(公告)号：WO2010025295A3
公开(公告)日：2010-06-17
申请号：PCT/US2009055247
申请日：2009-08-27
Applicant: CALCIMEDICA INC , VELICELEBI GONUL , STAUDERMAN KENNETH A , WHITTEN JEFFREY P , PEI YAZHONG , CAO JIANGUO , WANG ZHIJUN , ROGERS EVAN , DYCK BRIAN , GREY JONATHAN
Inventor： VELICELEBI GONUL , STAUDERMAN KENNETH A , WHITTEN JEFFREY P , PEI YAZHONG , CAO JIANGUO , WANG ZHIJUN , ROGERS EVAN , DYCK BRIAN , GREY JONATHAN
IPC: C07D413/04 , A61K31/381 , A61P19/00 , A61P19/02 , C07D409/02 , C07D409/04 , C07D413/02
CPC classification number: C07D409/04 , C07D333/38 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
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Patent Agency Ranking
公开(公告)号：WO2010027875A2
公开(公告)日：2010-03-11
申请号：PCT/US2009/055090
申请日：2009-08-26
Applicant: CALCIMEDICA INC. , VELICELEBI, Gonul , STAUDERMAN, Kenneth A. , WHITTEN, Jeffrey P. , PEI, Yazhong , CAO, Jianguo , WANG, Zhijun , ROGERS, Evan , DYCK, Brian , GREY, Jonathan
Inventor： VELICELEBI, Gonul , STAUDERMAN, Kenneth A. , WHITTEN, Jeffrey P. , PEI, Yazhong , CAO, Jianguo , WANG, Zhijun , ROGERS, Evan , DYCK, Brian , GREY, Jonathan
IPC: C07D409/02 , C07D413/12 , C07D231/56 , C07D277/60 , C07D495/04 , A61K31/415 , A61P19/02 , A61P25/28 , A61P19/00
CPC classification number: C07D409/04 , C07D333/38 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
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7.发明申请METHOD OF MODULATING AND OF IDENTIFYING AGENTS THAT MODULATE INTRACELLULAR CALCIUM 审中-公开调节和调节细胞内钙的试剂的鉴定方法
公开(公告)号：WO2004018700A2
公开(公告)日：2004-03-04
申请号：PCT/US2003/026409
申请日：2003-08-20
Applicant: NEUROGENETICS, INC. , ROOS, Jack , VELICELEBI, Gonul , STAUDERMAN, Kenneth
Inventor： ROOS, Jack , VELICELEBI, Gonul , STAUDERMAN, Kenneth
IPC: C12Q
CPC classification number: G01N33/6872 , G01N2500/04
Abstract: Methods are provided for identifying agents that modulate intracellular calcium. Also provided are methods of modulating calcium within cells and treating disease by modulating intracellular calcium. Also provided are methods of screening for nucleic acids encoding candidate ion transport proteins and methods of identifying nucleic acids encoding ion transport proteins.
Abstract translation: 提供了用于鉴定调节细胞内钙的试剂的方法。 还提供了调节细胞内钙并通过调节细胞内钙来治疗疾病的方法。 还提供了筛选编码候选离子转运蛋白的核酸的方法和鉴定编码离子转运蛋白的核酸的方法。
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公开(公告)号：WO2011109551A3
公开(公告)日：2012-01-19
申请号：PCT/US2011026916
申请日：2011-03-02
Applicant: CALCIMEDICA INC , VELICELEBI GONUL , STAUDERMAN KENNETH A , WHITTEN JEFFREY P , CAO JIANGUO , WANG ZHIJUN , ROGERS EVAN , DYCK BRIAN , GREY JONATHAN
Inventor： VELICELEBI GONUL , STAUDERMAN KENNETH A , WHITTEN JEFFREY P , CAO JIANGUO , WANG ZHIJUN , ROGERS EVAN , DYCK BRIAN , GREY JONATHAN
IPC: C07D471/04 , A61K31/428 , A61K31/437 , A61P19/02 , A61P37/00 , C07D333/38 , C07D417/12
CPC classification number: C07D409/12 , C07D333/38 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
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9.发明申请GAMMA-SECRETASE MODULATORY COMPOUNDS, METHODS FOR IDENTIFYING SAME, AND USES THEREFOR 审中-公开GAMMA-分泌酶调控化合物，识别方法及其用途
公开(公告)号：WO2011057214A3
公开(公告)日：2011-06-30
申请号：PCT/US2010055869
申请日：2010-11-08
Applicant: NEUROGENETIC PHARMACEUTICALS INC , KOUNNAS MARIA Z , ACKERMAN ELIZABETH J , STAUDERMAN KENNETH A , VELICELEBI GONUL , WAGNER STEVE
Inventor： KOUNNAS MARIA Z , ACKERMAN ELIZABETH J , STAUDERMAN KENNETH A , VELICELEBI GONUL , WAGNER STEVE
CPC classification number: G01N33/6896 , G01N2500/02
Abstract: In accordance with the present invention, it has been discovered that compounds which modulate the ?-secretase enzyme to make more of the shorter, less toxic and less aggregation-prone Aß peptides (such as Aß37 and Aß38), while making less of the longer and more toxic and aggregation-prone AB peptides (such as AB40 and AB42) are useful as gamma-secretase modulators. In addition, these GSM compounds have further been discovered to have the selective property of modulating the formation of various AB peptides, while not inhibiting the overall activity of the ?-secretase enzyme. Thus, such compounds do not impede other critical functions of the ?-secretase enzyme, such as generating fragments from Notch that appear to control gene expression and cell differentiation. Therefore, in accordance with the present invention, there are provided screening assays useful for determining whether test compounds have GSM activity; accordingly, invention assays facilitate the identification of new gamma-secretase modulators. Such screening assays can be performed in a variety of ways, e.g., by assessing whether test compounds: lower the level of Aß42 peptide,increase the level of Aß37 and/or Aß38 peptides, have substantially no effect on the processing of other ?-secretase substrates, and/or interact with at least one component of the ?-secretase complex. Also provided in accordance with the present invention are compounds having gamma-secretase modulatory activity as identified by any of the methods described herein; methods for producing formulations useful for modulating gamma-secretase activity, as well as the resulting formulations; methods for modulating gamma-secretase activity employing compounds identified according to invention methods and/or invention formulations, and the like.
Abstract translation: 根据本发明，已经发现调节β-分泌酶以制造更多更短，更低毒性和更少聚集倾向的Aβ肽（如Aβ37和Aβ38），同时减少更长时间 和更多毒性和易聚集的AB肽（如AB40和AB42）可用作γ-分泌酶调节剂。 此外，还发现这些GSM化合物具有调节各种AB肽形成的选择性，同时不抑制β-分泌酶的整体活性。 因此，这样的化合物不阻碍β-分泌酶的其他关键功能，例如产生Notch片段，似乎控制基因表达和细胞分化。 因此，根据本发明，提供了用于确定测试化合物是否具有GSM活性的筛选测定法; 因此，本发明分析有利于鉴定新的γ-分泌酶调节剂。 这样的筛选测定可以以多种方式进行，例如通过评估测试化合物：降低Aβ42肽水平，增加Aβ37和/或Aβ38肽水平，是否对其他γ-分泌酶加工基本没有影响 底物，和/或与γ-分泌酶复合物的至少一种组分相互作用。 根据本发明还提供具有通过本文所述的任何方法鉴定的γ-分泌酶调节活性的化合物; 生产用于调节γ-分泌酶活性的制剂的方法，以及所得制剂; 使用根据本发明方法和/或发明制剂鉴定的化合物来调节γ-分泌酶活性的方法等。
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10.发明申请PHENYLTHIOPHENYLDIHYDROBENZOTHIAZEPINE INHIBITORS OF STORE OPERATED CALCIUM RELEASE 审中-公开苯基硫代苯基二氢苯并噻唑并芘抑制剂的动态释放
公开(公告)号：WO2010034011A2
公开(公告)日：2010-03-25
申请号：PCT/US2009057905
申请日：2009-09-22
Applicant: CALCIMEDICA INC , WHITTEN JEFFREY P , PEI YAZHONG , STAUDERMAN KENNETH A , ROOS JACK
Inventor： WHITTEN JEFFREY P , PEI YAZHONG , STAUDERMAN KENNETH A , ROOS JACK
IPC: A61K31/554 , A61P17/06 , A61P19/02 , A61P29/00
CPC classification number: A61K31/554
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.
Abstract translation: 本文描述了含有这种化合物的化合物和药物组合物，其调节商店操作的钙（SOC）通道的活性。 本文还描述了单独使用此类SOC通道调节剂并与其他化合物组合用于治疗将受益于SOC通道活性抑制的疾病，病症或病症的方法。
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