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1. 发明授权

US09346808B2 Hsp90 inhibitors 有权
标题翻译： Hsp90抑制剂
公开(公告)号：US09346808B2
公开(公告)日：2016-05-24
申请号：US14009976
申请日：2012-04-05
申请人： Weilin Sun , Tony Taldone , Pallav Patel , Gabriela Chiosis
发明人： Weilin Sun , Tony Taldone , Pallav Patel , Gabriela Chiosis
IPC分类号： A61K31/52 , C07D473/34 , C07D473/40
CPC分类号： C07D473/34 , A61K31/52 , C07D473/40
摘要： The disclosure relates to Compounds of Formulae (IA) and (IB): and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Xd, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (IA) and/or (IB), and methods to treat or prevent a condition, such cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (IA) or (IB). The disclosure further relates to compounds of Formulae (IA) and IB) in which X2 is a leaving for introducing a radiolabeled atom, such as 124I or 131I and to methods of using such compounds in the preparation of radiolabeled compounds, particularly for use in imaging.
摘要翻译：本公开涉及式（IA）和（IB）的化合物及其药学上可接受的盐，其中Z1，Z2，Z3，Xa，Xb，Xc，Xd，Y，X2和X4如本文所定义，式（IA）和/或（IB）的化合物的量，以及治疗或预防这种过度表达Her-激酶的这种癌症的方法，包括向有需要的患者施用治疗有效量的式（IA）或（IB）。本公开还涉及式（IA）和IB）的化合物，其中X 2是用于引入放射性标记的原子（例如124I或131I）的离去，以及在制备放射性标记化合物中使用这些化合物的方法，特别是用于成像。

2. 发明申请

US20140088121A1 HSP90 Inhibitors 有权
标题翻译： HSP90抑制剂
公开(公告)号：US20140088121A1
公开(公告)日：2014-03-27
申请号：US14009976
申请日：2012-04-05
申请人： Weilin Sun , Tony Taldone , Pallav Patel , Gabriela Chiosis
发明人： Weilin Sun , Tony Taldone , Pallav Patel , Gabriela Chiosis
IPC分类号： C07D473/34
CPC分类号： C07D473/34 , A61K31/52 , C07D473/40
摘要： The disclosure relates to Compounds of Formulae (IA) and (IB): and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Xd, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (IA) and/or (IB), and methods to treat or prevent a condition, such cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (IA) or (IB). The disclosure further relates to compounds of Formulae (IA) and IB) in which X2 is a leaving for introducing a radiolabeled atom, such as 124I or 131I and to methods of using such compounds in the preparation of radiolabeled compounds, particularly for use in imaging.
摘要翻译：本公开涉及式（IA）和（IB）的化合物及其药学上可接受的盐，其中Z1，Z2，Z3，Xa，Xb，Xc，Xd，Y，X2和X4如本文所定义，式（IA）和/或（IB）的化合物的量，以及治疗或预防这种过度表达Her-激酶的这种癌症的方法，包括向有需要的患者施用治疗有效量的式（IA）或（IB）。本公开还涉及式（IA）和IB）的化合物，其中X 2是用于引入放射性标记的原子（例如124I或131I）的离去，以及在制备放射性标记化合物中使用这些化合物的方法，特别是用于成像。

3. 发明授权

US09567318B2 Substituted pyrimidine compounds and uses thereof 有权
标题翻译：取代的嘧啶化合物及其用途
公开(公告)号：US09567318B2
公开(公告)日：2017-02-14
申请号：US13391148
申请日：2010-08-17
申请人： Gabriela Chiosis , Tony Taldone , Anna Rodina , Pallav Patel , Yanlong Kang
发明人： Gabriela Chiosis , Tony Taldone , Anna Rodina , Pallav Patel , Yanlong Kang
IPC分类号： A61K31/496 , C07D403/14 , C07D495/04 , C07D403/12 , C07D239/38 , C07D239/47 , C07D239/56 , C07D239/60
CPC分类号： A61K31/513 , A61K31/496 , A61K31/506 , A61K2121/00 , C07D239/38 , C07D239/47 , C07D239/56 , C07D239/60 , C07D403/12 , C07D495/04
摘要： The present subject matter relates to a compound represented by the general formula (I) or (I′) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
摘要翻译：本发明涉及由通式（I）或（I'）表示的化合物或其药理学上可接受的盐; 含有这些化合物中的至少一种的药物组合物; 制备这些化合物中的至少一种的方法; 使用这些化合物中的至少一种治疗和/或预防各种癌症和/或增殖病症的方法; 使用这些化合物中的至少一种来监测针对各种癌症的抗癌疗法的有效性的方法。在一个实施方案中，主题涉及与热休克蛋白70（Hsp70）的特异性水平结合的化合物。在另一个实施方案中，主题涉及以特异性水平结合以抑制热休克蛋白70（Hsp70）和热休克同源蛋白70（Hsc70）的化合物。

4. 发明申请

US20120252818A1 HEAT SHOCK PROTEIN BINDING COMPOUNDS, COMPOSITIONS, AND METHODS FOR MAKING AND USING SAME 有权
标题翻译：热休克蛋白结合化合物，组合物及其制备和使用方法
公开(公告)号：US20120252818A1
公开(公告)日：2012-10-04
申请号：US13391148
申请日：2010-08-17
申请人： Gabriela Chiosis , Tony Taldone , Anna Rodina , Pallav Patel , Yanlong Kang
发明人： Gabriela Chiosis , Tony Taldone , Anna Rodina , Pallav Patel , Yanlong Kang
IPC分类号： A61K31/496 , G01N27/62 , G06G7/58 , G01N21/76 , A61P35/00 , C07D495/04 , C12N9/99 , C07D403/14
CPC分类号： A61K31/513 , A61K31/496 , A61K31/506 , A61K2121/00 , C07D239/38 , C07D239/47 , C07D239/56 , C07D239/60 , C07D403/12 , C07D495/04
摘要： The present subject matter relates to a compound represented by the general formula (I) or (I′) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
摘要翻译：本发明涉及由通式（I）或（I'）表示的化合物或其药理学上可接受的盐; 含有这些化合物中的至少一种的药物组合物; 制备这些化合物中的至少一种的方法; 使用这些化合物中的至少一种治疗和/或预防各种癌症和/或增殖病症的方法; 使用这些化合物中的至少一种来监测针对各种癌症的抗癌疗法的有效性的方法。在一个实施方案中，主题涉及结合热休克蛋白70（Hsp70）的特异性水平的化合物。在另一个实施方案中，主题涉及以特异性水平结合以抑制热休克蛋白70（Hsp70）和热休克同源蛋白70（Hsc70）的化合物。

5. 发明授权

US09328114B2 Hsp90 inhibitors 有权
标题翻译： Hsp90抑制剂
公开(公告)号：US09328114B2
公开(公告)日：2016-05-03
申请号：US13500809
申请日：2010-10-07
申请人： Gabriela Chiosis , Tony Taldone , Weilin Sun
发明人： Gabriela Chiosis , Tony Taldone , Weilin Sun
IPC分类号： C07D473/34 , A61K31/52 , A61P35/00 , A61P25/28 , A61P25/16
CPC分类号： A61K31/52 , A61K31/538 , C07D473/34
摘要： The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease.
摘要翻译：本申请提供了可用于抑制Hsp90，因此用于治疗疾病的化合物。

6. 发明申请

US20120208806A1 Hsp90 Inhibitors 有权
标题翻译： Hsp90抑制剂
公开(公告)号：US20120208806A1
公开(公告)日：2012-08-16
申请号：US13500809
申请日：2010-10-07
申请人： Gabriela Chiosis , Tony Taldone , Weilin Sun
发明人： Gabriela Chiosis , Tony Taldone , Weilin Sun
IPC分类号： A61K31/538 , A61P25/28 , A61P35/00 , A61K31/52 , C07D473/34
CPC分类号： A61K31/52 , A61K31/538 , C07D473/34
摘要： The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease.
摘要翻译：本申请提供了可用于抑制Hsp90，因此用于治疗疾病的化合物。

7. 发明授权

US09546170B2 Hsp90 inhibitors 有权
标题翻译： Hsp90抑制剂
公开(公告)号：US09546170B2
公开(公告)日：2017-01-17
申请号：US14110095
申请日：2012-04-05
申请人： Tony Taldone , Gabriela Chiosis
发明人： Tony Taldone , Gabriela Chiosis
IPC分类号： C07D473/34 , C07D473/40
CPC分类号： A61K31/52 , C07D473/34 , C07D473/40
摘要： The disclosure relates to Compounds of Formula (1) : and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof, and methods to treat or prevent a condition, such as cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof.
摘要翻译：本公开涉及式（1）的化合物及其药学上可接受的盐，其中Z1，Z2，Z3，Xa，Xb，Xc，Y，X2和X4如本文所定义，组合物包含有效量的式（1）或其药学上可接受的盐，以及治疗或预防诸如过表达Her-激酶的癌症的病症的方法，包括向有需要的患者施用治疗有效量的式（1）的化合物或其药学上可接受的盐。

8. 发明申请

US20140045867A1 HSP90 Inhibitors 有权
标题翻译： HSP90抑制剂
公开(公告)号：US20140045867A1
公开(公告)日：2014-02-13
申请号：US14110095
申请日：2012-04-05
申请人： Tony Taldone , Gabriela Chiosis
发明人： Tony Taldone , Gabriela Chiosis
IPC分类号： C07D473/34
CPC分类号： A61K31/52 , C07D473/34 , C07D473/40
摘要： The disclosure relates to Compounds of Formula (1) : and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof, and methods to treat or prevent a condition, such as cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof.
摘要翻译：本公开涉及式（1）的化合物及其药学上可接受的盐，其中Z1，Z2，Z3，Xa，Xb，Xc，Y，X2和X4如本文所定义，组合物包含有效量的式（1）或其药学上可接受的盐，以及治疗或预防诸如过表达Her-激酶的癌症的病症的方法，包括向有需要的患者施用治疗有效量的式（1）的化合物或其药学上可接受的盐。

9. 发明申请

US20140294725A1 USES OF LABELED HSP90 INHIBITORS 审中-公开
标题翻译：标签HSP90抑制剂的使用
公开(公告)号：US20140294725A1
公开(公告)日：2014-10-02
申请号：US14131420
申请日：2012-07-06
申请人： Gabriela Chiosis , Nagavarakishore Pillarsetty , Jason S. Lewis , Steven M. Larson , Tony Taldone , Mary L. Alpaugh , Erica M. Gomes
发明人： Gabriela Chiosis , Nagavarakishore Pillarsetty , Jason S. Lewis , Steven M. Larson , Tony Taldone , Mary L. Alpaugh , Erica M. Gomes
IPC分类号： A61K51/04 , G01N33/574
CPC分类号： A61K51/0459 , A61K31/52 , G01N33/5011 , G01N33/5017 , G01N33/5044 , G01N33/574 , G01N33/57407 , G01N33/57426 , G01N2500/04 , G01N2800/52
摘要： The invention concerns various methods of using labeled HSP90 inhibitors to improve treatment of cancer patients with HSP90 inhibitors, including ex vivo and in vivo methods for determining whether a tumor will likely respond to therapy with an HSP90 inhibitor. The disclosure provides a method for determining whether a tumor will likely respond to therapy with an HSP90 inhibitor which comprises the following steps: (a) contacting the tumor or a sample containing cells from the tumor with a detectably labeled HSP90 inhibitor which binds preferentially to a tumor-specific form of HSP90; (b) measuring the amount of labeled HSP90 inhibitor bound to the tumor or the tumor cells in the sample; and (c) comparing the amount of labeled HSP90 inhibitor bound to the tumor or the tumor cells in the sample measured in step (b) to the amount of labeled-HSP90 inhibitor bound to a reference.
摘要翻译：本发明涉及使用标记的HSP90抑制剂改善用HSP90抑制剂治疗癌症患者的各种方法，包括用于确定肿瘤是否可能对HSP90抑制剂治疗有反应的离体和体内方法。本公开提供了一种用于确定肿瘤是否可能响应于HSP90抑制剂治疗的方法，该方法包括以下步骤：（a）使来自肿瘤的肿瘤或含有细胞的样品与优先结合于肿瘤的可检测标记的HSP90抑制剂接触肿瘤特异性形式的HSP90; （b）测量与样品中的肿瘤或肿瘤细胞结合的标记的HSP90抑制剂的量; 和（c）将在步骤（b）中测量的样品中与肿瘤或肿瘤细胞结合的标记HSP90抑制剂的量与结合参考物的标记的HSP90抑制剂的量进行比较。

10. 发明申请

US20140242602A1 USES OF LABELED HSP90 INHIBITORS 有权
标题翻译：标签HSP90抑制剂的使用
公开(公告)号：US20140242602A1
公开(公告)日：2014-08-28
申请号：US14131423
申请日：2012-07-06
申请人： Gabriela Chiosis , Tony Taldone , Mary L. Alpaugh , Erica M. Gomes-Dagama , Monica L. Guzman , Hongliang Zong
发明人： Gabriela Chiosis , Tony Taldone , Mary L. Alpaugh , Erica M. Gomes-Dagama , Monica L. Guzman , Hongliang Zong
IPC分类号： G01N33/574
CPC分类号： A61K51/0459 , A61K31/52 , G01N33/5011 , G01N33/5017 , G01N33/5044 , G01N33/574 , G01N33/57407 , G01N33/57426 , G01N2500/04 , G01N2800/52
摘要： The disclosure provides evidence that the abundance of this particular “oncogenic HSP90” species, which is not dictated by HSP90 expression alone, predicts for sensitivity to HSP90 inhibition therapy, and thus is a biomarker for HSP90 therapy. The disclosure also provides evidence that identifying and measuring the abundance of this oncogenic HSP90 species in tumors predicts of response to HSP90 therapy. “Oncogenic HSP90” is defined herein as the HSP90 fraction that represents a cell stress specific form of chaperone complex, that is expanded and constitutively maintained in the tumor cell context, and that may execute functions necessary to maintain the malignant phenotype. Such roles are not only to regulate the folding of overexpressed (i.e. HER2), mutated (i.e. mB-Raf) or chimeric proteins (i.e. Bcr-Abl), but also to facilitate scaffolding and complex formation of molecules involved in aberrantly activated signaling complexes (i.e. STATS, BCL6).
摘要翻译：该公开提供了证据表明，单独HSP90表达不规定的特定“致癌HSP90”物种的丰度预测对HSP90抑制疗法的敏感性，因此是HSP90治疗的生物标志物。本公开还提供了证据，确定和测量肿瘤中这种致癌HSP90物种的丰度预测了对HSP90治疗的反应。 “致癌HSP90”在本文中被定义为代表分子伴侣复合物的细胞应激特异性形式的HSP90级分，其在肿瘤细胞环境中被扩增和组成型维持，并且可以执行维持恶性表型所需的功能。这样的作用不仅是调节过表达（即HER2），突变（即mB-Raf）或嵌合蛋白（即Bcr-Abl）的折叠，而且还促进涉及异常激活的信号传导复合体的分子的支架和复合物形成即STATS，BCL6）。

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