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公开(公告)号：US20130040892A1
公开(公告)日：2013-02-14
申请号：US13578574
申请日：2011-02-11
申请人： Alain Laurent , Melanie Proulx , Yannick Rose , Irina Denissova , Kenza Dairi , Scott Jarvis , James B. Jaquith
发明人： Alain Laurent , Melanie Proulx , Yannick Rose , Irina Denissova , Kenza Dairi , Scott Jarvis , James B. Jaquith
IPC分类号： A61K38/05 , C12N5/078 , C12N5/0787 , A61P29/00 , C07D471/04 , A61P35/00 , A61P37/00 , C12N5/071 , C07K5/062
CPC分类号： C07K5/06026 , A61K38/00 , C07K5/06034
摘要： A compound of Formula 1: (I) or salt thereof, as well as methods of making compounds of Formula 1, methods of using compounds of Formula 1 to treat proliferative disorders such as cancer, and related compounds, composition, and methods.
摘要翻译： 式1化合物或其盐，以及制备式1化合物的方法，使用式1化合物治疗增殖性疾病如癌症的方法及其相关化合物，组合物和方法。
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公开(公告)号：US09284350B2
公开(公告)日：2016-03-15
申请号：US13578574
申请日：2011-02-11
申请人： Alain Laurent , Melanie Proulx , Yannick Rose , Irina Denissova , Kenza Dairi , Scott Jarvis , James B. Jaquith
发明人： Alain Laurent , Melanie Proulx , Yannick Rose , Irina Denissova , Kenza Dairi , Scott Jarvis , James B. Jaquith
CPC分类号： C07K5/06026 , A61K38/00 , C07K5/06034
摘要： A compound of Formula 1: (I) or salt thereof, as well as methods of making compounds of Formula 1, methods of using compounds of Formula 1 to treat proliferative disorders such as cancer, and related compounds, composition, and methods.
摘要翻译： 式1化合物或其盐，以及制备式1化合物的方法，使用式1化合物治疗增殖性疾病如癌症的方法及其相关化合物，组合物和方法。
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公开(公告)号：US20120009141A1
公开(公告)日：2012-01-12
申请号：US13057730
申请日：2009-08-07
IPC分类号： A61K31/427 , C07D413/14 , C07D403/12 , C07D403/14 , C07D519/00 , A61K31/422 , A61K31/428 , A61K31/4025 , A61K31/4045 , A61K31/437 , A61K38/19 , A61K39/395 , A61P35/00 , A61P29/00 , A61P19/02 , A61K31/56 , A61K31/4706 , A61K31/675 , A61K38/13 , A61K38/20 , C12N5/071 , C07D417/14
CPC分类号： C07K16/2878 , A61K38/00 , C07K5/06026 , C07K14/4747 , C07K2317/73 , C12N9/6475 , G01N2500/04 , G01N2510/00
摘要： A compound of Formula 1: or a salt thereof, and methods for the use thereof, especially as an IAP inhibitor, as well as related compounds, compositions, and methods.
摘要翻译： 式1化合物或其盐及其用途，特别是作为IAP抑制剂的方法，以及相关的化合物，组合物和方法。
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4.发明申请BRIDGED SECONDARY AMINES AND USE THEREOF AS IAP BIR DOMAIN BINDING COMPOUNDS 审中-公开连接的二级氨基酸和作为IAP双键结合化合物的用途公开(公告)号：US20110171171A1
公开(公告)日：2011-07-14
申请号：US13001028
申请日：2009-06-26
IPC分类号： A61K38/20 , C07D403/12 , C07D405/14 , C07D401/14 , C07D417/14 , C07D401/12 , C07D413/12 , A61K38/05 , A61K39/395 , C12N5/071 , A61P35/00 , A61P19/02 , A61P29/00 , A61P37/02 , A61P7/06 , A61P7/00 , A61P1/08
CPC分类号： G01N33/6872 , A61K38/00 , C07K5/06026 , G01N2333/4704 , G01N2500/00
摘要： A compound of Formula 1.1A: 1.1A or salt thereof, as well as methods of making compounds of Formula 1.1A, methods of using compounds of Formula 1.1A to treat proliferative disorders such as cancer, and related compounds, composition, and methods.
摘要翻译： 式1.1A的化合物或其盐，以及制备式1.1A化合物的方法，使用式1.1A化合物治疗增殖性疾病如癌症的方法，以及相关化合物，组合物和方法。
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公开(公告)号：US08575113B2
公开(公告)日：2013-11-05
申请号：US12825197
申请日：2010-06-28
申请人： Scott Jarvis , Alain Boudreault , Patrick Bureau , James B. Jaquith , Alain Laurent , Delphine Labit
发明人： Scott Jarvis , Alain Boudreault , Patrick Bureau , James B. Jaquith , Alain Laurent , Delphine Labit
CPC分类号： C07D207/09 , C07K5/06026 , C07K5/06034 , C07K5/06069
摘要： The present invention is directed towards an isomer, an enantiomer, a diastereoisomer, or a tautomer of a pyrrolidine compound represented by Formula I: in which the substituents R1, R1a, R2, R2a, R3, A and Q are defined herein; or a prodrug, or a salt thereof, and which bind to IAP BIR domains. In particular, the compounds are useful in treating proliferative disorders such as cancer.
摘要翻译： 本发明涉及由式I表示的吡咯烷化合物的异构体，对映异构体，非对映异构体或互变异构体：其中取代基R1，R1a，R2，R2a，R3，A和Q如本文所定义; 或其前药或其盐，并且其结合IAP BIR结构域。 特别地，这些化合物可用于治疗增殖性疾病如癌症。
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公开(公告)号：US07645741B2
公开(公告)日：2010-01-12
申请号：US11979280
申请日：2007-11-01
IPC分类号： A61K38/08 , A61K39/395 , A61P35/00 , C07K7/06 , C12Q1/02
CPC分类号： C07K5/0812 , A61K31/40 , A61K31/4025 , A61K38/00 , A61K38/08 , A61K38/1761 , C07D207/14 , C07D207/16 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K7/06
摘要： Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I or II or a salt thereof, in which R1, R2, R3, R100, R200, R300, A, A1, BG, Q and Q1 are substituents described herein. Also disclosed is the use of compounds of Formula I and II to treat proliferative disorders such as cancer.
摘要翻译： 公开了由式I或II表示的化合物或其盐的异构体，对映体，非对映异构体或互变异构体，其中R1，R2，R3，R100，R200，R300，A，A1，BG，Q和Q1是描述的取代基 这里。 还公开了使用式I和II的化合物来治疗增殖性疾病如癌症。
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公开(公告)号：US07129250B2
公开(公告)日：2006-10-31
申请号：US10637599
申请日：2003-08-11
IPC分类号： A61K31/437 , A61K31/404 , C07D471/04 , C07D403/14
CPC分类号： C07D403/14 , A61K31/40 , A61K31/415 , A61K31/435 , A61K31/47 , C07D401/14 , C07D403/04 , C07D403/08 , C07D471/04
摘要： This invention features ring-substituted pyrrolo-β-carboline derivatives and ring-substitution and structural derivatives of 3-(1H-indol-3-yl)-1H-pyrrole-2,5-dione of formulas I–III, which are useful as neuroprotective and anti-proliferative compounds. Also disclosed are methods for the preparation of these compounds, selected biological profiles and uses of these compounds in the treatment of various neurodegenerative and inflammatory diseases of the human nervous system and in the treatment of various other proliferative disorders characterized by loss of growth or cellular differentiation control including, but not limited to, cancer and inflammation.
摘要翻译： 本发明具有式I-III的3-（1H-吲哚-3-基）-1H-吡咯-2,5-二酮的环取代的吡咯并-β-咔啉衍生物和环取代和结构衍生物，它们是有用的 作为神经保护和抗增殖化合物。 还公开了用于制备这些化合物的方法，选择的生物学特征和这些化合物在治疗人类神经系统的各种神经变性和炎性疾病中的用途以及治疗以生长丧失或细胞分化为特征的各种其他增殖性疾病 对照包括但不限于癌症和炎症。
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公开(公告)号：US07579320B2
公开(公告)日：2009-08-25
申请号：US11723044
申请日：2007-03-16
IPC分类号： A61K38/08 , A61K39/395 , A61P35/00 , C07K7/06 , C12Q1/02
CPC分类号： C07K5/0812 , A61K31/40 , A61K31/4025 , A61K38/00 , A61K38/08 , A61K38/1761 , C07D207/14 , C07D207/16 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K7/06
摘要： Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I or II or a salt thereof, in which R1, R2, R3, R100, R200, R300, A, A1, BG, Q and Q1 are substituents described herein. Also disclosed is the use of compounds of Formula I and II to treat proliferative disorders such as cancer.
摘要翻译： 公开了由式I或II表示的化合物或其盐的异构体，对映体，非对映异构体或互变异构体，其中R1，R2，R3，R100，R200，R300，A，A1，BG，Q和Q1是描述的取代基 这里。 还公开了使用式I和II的化合物来治疗增殖性疾病如癌症。
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公开(公告)号：US20090179638A1
公开(公告)日：2009-07-16
申请号：US12278071
申请日：2007-02-01
IPC分类号： G01V3/00 , C07D513/04 , C07F5/02 , G01N33/68 , G01N33/566
CPC分类号： G01N33/6896 , G01N2500/02
摘要： Disclosed is an assay for identifying compounds that modulate a neuronal apoptotic pathway, the assay comprises: a) contacting HSP90 protein with a probe to form a probe: HSP90 complex, the probe being displaceable by a test compound; b) measuring a signal from the probe so as to establish a reference level; c) incubating the probe:HSP90 complex with the test compound; d) measuring the signal from the probe; e) comparing the signal from step d) with the reference level, a modulation of the signal indicating that the test compound binds to HSP90. Also disclosed is a probe which is labeled with a detectable label and/or an affinity tag.
摘要翻译： 公开了用于鉴定调节神经元凋亡途径的化合物的测定法，该测定包括：a）使HSP90蛋白与探针接触以形成探针：HSP90复合物，所述探针可被测试化合物置换; b）测量来自探针的信号，以便建立参考水平; c）将探针：HSP90复合物与测试化合物孵育; d）测量探头的信号; e）将来自步骤d）的信号与参考水平进行比较，指示测试化合物与HSP90结合的信号的调制。 还公开了用可检测标记和/或亲和标签标记的探针。
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公开(公告)号：US20080207525A1
公开(公告)日：2008-08-28
申请号：US11979280
申请日：2007-11-01
CPC分类号： C07K5/0812 , A61K31/40 , A61K31/4025 , A61K38/00 , A61K38/08 , A61K38/1761 , C07D207/14 , C07D207/16 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K7/06
摘要： Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I or II or a salt thereof, in which R1, R2, R3, R100, R200, R300, A, A1, BG, Q and Q1 are substituents described herein. Also disclosed is the use of compounds of Formula I and II to treat proliferative disorders such as cancer.
摘要翻译： 公开了由式I或II表示的化合物或其盐的异构体，对映体，非对映异构体或互变异构体，其中R 1，R 2，R 2， 300，R 100，100，100，100，100，100，100， Q和Q 1是本文所述的取代基。 还公开了使用式I和II的化合物来治疗增殖性疾病如癌症。
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