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1. 发明申请

WO2013009655A2 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：WO2013009655A2
公开(公告)日：2013-01-17
申请号：PCT/US2012045861
申请日：2012-07-06
申请人： SLOAN KETTERING INST CANCER , CHIOSIS GABRIELA , PILLARSETTY NAGAVARAKISHORE , LEWIS JASON S , LARSON STEVEN M , TALDONE TONY , ALPAUGH MARY L , GOMES-DAGAMA ERICA M
发明人： CHIOSIS GABRIELA , PILLARSETTY NAGAVARAKISHORE , LEWIS JASON S , LARSON STEVEN M , TALDONE TONY , ALPAUGH MARY L , GOMES-DAGAMA ERICA M
IPC分类号： A61K51/04
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： This 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.
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。

2. 发明公开

EP2729806A4 USES OF LABELED HSP90 INHIBITORS 失效
标题翻译： VERWENDUNG VON MARKIERTEN HSP90-INHIBITOREN
公开(公告)号：EP2729806A4
公开(公告)日：2015-04-01
申请号：EP12811358
申请日：2012-07-06
申请人： SLOAN KETTERING INST CANCER , UNIV CORNELL
发明人： CHIOSIS GABRIELA , TALDONE TONY , ALPAUGH MARY L , GOMES-DAGAMA ERICA M , GUZMAN MONICA L , ZONG HONGLIANG
IPC分类号： G01N33/53
CPC分类号： A61K51/0459 , A61K31/52 , G01N33/5011 , G01N33/5017 , G01N33/5044 , G01N33/574 , G01N33/57407 , G01N33/57426 , G01N2500/04 , G01N2800/52

3. 发明专利

CA2841069C USES OF LABELED HSP90 INHIBITORS 未知
公开(公告)号：CA2841069C
公开(公告)日：2021-11-23
申请号：CA2841069
申请日：2012-07-06
申请人： SLOAN KETTERING INST CANCER RES , UNIV CORNELL
发明人： CHIOSIS GABRIELA , TALDONE TONY , ALPAUGH MARY L , GOMES-DAGAMA ERICA M , GUZMAN MONICA L , ZONG HONGLIANG
IPC分类号： G01N33/483 , G01N33/574
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 defmed 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. rnB-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).

4. 发明专利

ES2766623T3 Usos de inhibidores etiquetados HSP90 未知
公开(公告)号：ES2766623T3
公开(公告)日：2020-06-12
申请号：ES17156149
申请日：2012-07-06
申请人： SLOAN KETTERING INST CANCER RES , UNIV CORNELL
发明人： CHIOSIS GABRIELA , PILLARSETTY NAGAVARAKISHORE , LEWIS JASON S , LARSON STEVEN M , TALDONE TONY , ALPAUGH MARY L
IPC分类号： G01N33/574 , A61K31/52 , A61K51/04 , G01N33/50
摘要： Un inhibidor de HSP90 detectablemente etiquetado para su uso en un método para determinar si un tumor probablemente responderá a la terapia con un inhibidor de HSP90 que comprende o bien las etapas siguientes: (a) poner en contacto el tumor con un inhibidor de HSP90 detectablemente etiquetado que se enlaza preferencialmente a una forma específica del tumor de HSP90 presente en un tumor o células tumorales; (b) medir la cantidad de inhibidor de HSP90 etiquetado enlazado al tumor; y (c) comparar la cantidad de inhibidor de HSP90 etiquetado enlazado al tumor medida en la etapa (b) con la cantidad de referencia del inhibidor de HSP90 etiquetado enlazado a células normales; en donde una cantidad mayor de inhibidor de HSP90 etiquetado enlazado al tumor medida en la etapa (b) como se compara con la cantidad de referencia indica que el tumor probablemente responderá a la terapia con un inhibidor de HSP90; o bien que comprende las etapas siguientes: (a) administrar un inhibidor de HSP90 detectablemente etiquetado, en donde el inhibidor de HSP90 detectablemente etiquetado es una forma radioetiquetada del inhibidor de HSP90 que se enlaza preferencialmente a una forma específica del tumor de HSP90 presente en un tumor o células tumorales, al paciente en múltiples puntos de tiempo dentro del periodo durante el cual el paciente está recibiendo terapia con un inhibidor de HSP90; y (b) medir la concentración del inhibidor de HSP90 radioetiquetado en el tumor del paciente en dichos múltiples puntos de tiempo después de la administración en la etapa (a); y (c) comparar las concentraciones del inhibidor de HSP90 radioetiquetado medidas en la etapa (b) con las concentraciones mínimas del inhibidor de HSP90 necesarias para tratar efectivamente el tumor, en donde concentraciones medidas mayores que la mínima necesaria para tratar el tumor indican que el paciente es probable que responda a la terapia con el inhibidor de HSP90, en donde en ambas secuencias de etapas mencionadas anteriormente el inhibidor detectablemente etiquetado es: o una sal farmacéuticamente aceptable del mismo, en donde: X3 es CH2, CF2, S, SO, SO2, O, NH o NR2, en donde R2 es alquilo; X2 es 123I, 124I, 125I o 131I; X4 es hidrógeno o halógeno; X5 es O o CH2; R es 3-isopropilaminopropilo, 3-(isopropil(metil)amino)propilo, 3-(isopropil(etil)amino)propilo, 3-((2- hidroxietil)(isopropil)amino)propilo, 3-(metil(prop-2-inil)amino)propilo, 3-(alil(metil)amino)propilo, 3- (etil(metil)amino)propilo, 3-(ciclopropil(propil)amino)propilo, 3-(ciclohexil(2-hidroxietil)amino)propilo, 3-(2-metilaziridin- 1-il)propilo, 3-(piperidin-1-il)propilo, 3-(4-(2-hidroxietil)piperazin-1-il)propilo, 3-morfolinopropilo, 3- (trimetilamonio)propilo, 2-(isopropilamino)etilo, 2-(isobutilamino)etilo, 2-(neopentilamino)etilo, 2- (ciclopropilmetilamino)etilo, 2-(etil(metil)amino)etilo, 2-(isobutil(metil)amino)etilo o 2-(metil(prop-2-inil)amino)etilo; y n es 1 o 2.

5. 发明专利

CA2841173A1 USES OF LABELED HSP90 INHIBITORS 未知
公开(公告)号：CA2841173A1
公开(公告)日：2013-06-17
申请号：CA2841173
申请日：2012-07-06
申请人： SLOAN KETTERING INST CANCER
发明人： CHIOSIS GABRIELA , PILLARSETTY NAGAVARAKISHORE , LEWIS JASON S , LARSON STEVEN M , TALDONE TONY , ALPAUGH MARY L , GOMES-DAGAMA ERICA M
IPC分类号： A61K51/04 , A61K31/52 , A61P35/00 , G01N33/574
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.

6. 发明专利

AU2012282905B8 Uses of labeled HSP90 inhibitors 未知
公开(公告)号：AU2012282905B8
公开(公告)日：2017-08-31
申请号：AU2012282905
申请日：2012-07-06
申请人： UNIV CORNELL , SLOAN KETTERING INST CANCER RES
发明人： CHIOSIS GABRIELA , TALDONE TONY , ALPAUGH MARY L , GOMES-DAGAMA ERICA M , GUZMAN MONICA L , ZONG HONGLIANG
IPC分类号： G01N33/53
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 defmed 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. rnB-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).

7. 发明专利

AU2012282905A1 Uses of labeled HPS90 inhibitors 未知
公开(公告)号：AU2012282905A1
公开(公告)日：2014-02-13
申请号：AU2012282905
申请日：2012-07-06
申请人： UNIV CORNELL , SLOAN KETTERING INST CANCER
发明人： CHIOSIS GABRIELA , TALDONE TONY , ALPAUGH MARY L , GOMES-DAGAMA ERICA M , GUZMAN MONICA L , ZONG HONGLIANG
IPC分类号： G01N33/53
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 defmed 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. rnB-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).

8. 发明专利

AU2017204369B2 Uses of labeled HSP90 inhibitors 未知
公开(公告)号：AU2017204369B2
公开(公告)日：2019-08-01
申请号：AU2017204369
申请日：2017-06-27
申请人： SLOAN KETTERING INST CANCER RES
发明人： CHIOSIS GABRIELA , PILLARSETTY NAGAVARAKISHORE , LEWIS JASON S , LARSON STEVEN M , TALDONE TONY , ALPAUGH MARY L , GOMES-DAGAMA ERICA M
IPC分类号： A61K51/04 , G01N33/50
摘要： USES OF LABELED HSP90 INIHIBITORS Abstract of the Disclosure This 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.

9. 发明专利

MX2014000286A USO DE INHIBIDORES HSP90 ETIQUETADOS. 未知
公开(公告)号：MX2014000286A
公开(公告)日：2015-03-06
申请号：MX2014000286
申请日：2012-07-06
申请人： SLOAN KETTERING INST CANCER
发明人： TALDONE TONY , CHIOSIS GABRIELA , ALPAUGH MARY L , GOMES-DAGAMA ERIC M , GUZMAN MONICA L , ZONG HONGLIANG
IPC分类号： G01N33/53
摘要： La descripción proporciona evidencia de que la abundancia de esta especie "HSP90 oncogénica" particular, que no se dictamina por la expresión HSP90 sola, predice la sensibilidad a terapia de inhibición HSP90, y de esta manera es un biomarcador para terapia de HSP90. La descripción también proporciona evidencia que identifica y mide la abundancia de esta especie HSP90 oncogénica en predicciones de tumores de respuesta a terapia HSP90. "HSP90 oncogénico" se define en la presente como la fracción HSP90 que representa una forma específica de tensión celular del complejo acompañante, que se expande y mantiene constitutivamente en el contexto de célula de tumor, y que puede ejecutar funciones necesarias para mantener el fenotipo maligno. Tales papeles no sólo son para regular el plegado de proteínas sobreexpresadas (es decir, HER2), mutadas (es decir, rnB-Raf) o quiméricas (es decir, Ver-Abl), sino también para facilitar el andamiaje y formación de complejo de moléculas involucradas en los complejos de señalización aberrantemente activados (es decir STATS, BCL6).

10. 发明专利

CA2841173C USES OF LABELED HSP90 INHIBITORS 未知
公开(公告)号：CA2841173C
公开(公告)日：2022-06-21
申请号：CA2841173
申请日：2012-07-06
申请人： SLOAN KETTERING INST CANCER RES
发明人： CHIOSIS GABRIELA , PILLARSETTY NAGAVARAKISHORE , LEWIS JASON S , LARSON STEVEN M , TALDONE TONY , ALPAUGH MARY L , GOMES-DAGAMA ERICA M
IPC分类号： G01N33/574
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.

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