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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. 发明申请

WO2009045535A3 FLUORINE-18 DERIVATIVE OF DASATINIB AND USES THEREOF 审中-公开
标题翻译： DASATINIB的荧光素-18衍生物及其用途
公开(公告)号：WO2009045535A3
公开(公告)日：2009-08-13
申请号：PCT/US2008011509
申请日：2008-10-06
申请人： SLOAN KETTERING INST CANCER , VEACH DARREN , PILLARSETTY NAGAVARA KISHORE , DUNPHY MARK , LARSON STEVEN M , SANTOS ELMER B , NAMAVARI MOHAMMAD
发明人： VEACH DARREN , PILLARSETTY NAGAVARA KISHORE , DUNPHY MARK , LARSON STEVEN M , SANTOS ELMER B , NAMAVARI MOHAMMAD
IPC分类号： A61K49/00 , A61K31/496 , A61K31/506 , C07D403/02
CPC分类号： A61K31/50 , A61K31/49 , A61K51/0459
摘要： Provided herein are [l8F]-labeled Dasatinib derivatives or analogs effective for imaging cells or tissue having an increased tyrosine kinase activity associated with a pathophysiological condition. Also provided are methods for in vivo imaging using the [18F]- labeled Dasatinib derivatives or analogs, particularly methods of imaging utilizing positron emission tomography. These methods are effective for diagnosing a pathophysiological condition susceptible to treatment with Dasatinib or other kinase inhibitor in a subject, or determining whether a cancer in a subject susceptible to being treated with Dasatinib or other kinase inhibitor has developed resistance to the same and for maximizing tumor response to kinase inhibitor with minimal toxicity to the subject.
摘要翻译：本文提供[18 F]标记的达沙替尼衍生物或类似物，其有效成像具有与病理生理条件相关的酪氨酸激酶活性增加的细胞或组织。还提供了使用[18 F]标记的达沙替尼衍生物或类似物的体内成像的方法，特别是使用正电子发射断层扫描的成像方法。这些方法对于诊断受试者中达沙替尼或其他激酶抑制剂治疗敏感的病理生理条件，或者确定易感受杜沙替丁或其他激酶抑制剂治疗的受试者的癌症是否已经产生对其的抗性并使肿瘤最大化对激素抑制剂的反应，对受试者的毒性最小。

3. 发明公开

EP2948132A4 METHOD FOR DIAGNOSING OR TREATING TUMORS USING SPHINGOMYELIN CONTAINING LIPOSOMES 有权
标题翻译：诊断和治疗肿瘤的方法，使用SPHINGOMYELINHALTIGER LIPOSOME
公开(公告)号：EP2948132A4
公开(公告)日：2016-09-28
申请号：EP14743490
申请日：2014-01-23
申请人： SLOAN KETTERING INST CANCER
发明人： PENATE-MEDINA TUULA , PENATE-MEDINA OULA , LARSON STEVEN M , GRIMM JAN , THOREK DANIEL L J , KOLESNICK RICHARD N
IPC分类号： A61K9/127 , A61K49/00 , A61K49/18 , A61K51/08 , A61K51/12
CPC分类号： A61K49/1812 , A61K49/0032 , A61K49/0084 , A61K51/081 , A61K51/1234
摘要： The invention provides compositions and methods for diagnosing tumors and augmentic therapeutic intervention and measuring response to cell stress using sphingomyelin containing liposomes. The liposomes can include radiotracers, contrast agents, chromophores, dyes, enzyme substrates, therapeutic agents, chemotherapeutic agents or DNA segments. The indicators enable measurement of the extent of cellular release of Acid SMase at a localized site of cell stress. The nanoparticles have the capacity to locally release their contents, be it imaging (for diagnosis) or therapeutic agents (to augment therapy).

4. 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.

5. 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.

6. 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.

7. 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.

8. 发明专利

MX2014000292A USOS DE INHIBIDORES ETIQUETADOS HSP90. 未知
公开(公告)号：MX2014000292A
公开(公告)日：2015-03-06
申请号：MX2014000292
申请日：2012-07-06
申请人： SLOAN KETTERING INST CANCER
发明人： CHIOSIS GABRIELA , ALPAUGH MARY L , NAGAVARAKISHORE PILLARSETTY , LEWIS JASON S , LARSON STEVEN M , TONY TALDONE , ERICA M GOMES-DAGAMA
IPC分类号： G01N33/50
摘要： Esta invención se refiere a diversos métodos de uso de inhibidores etiquetados HSP90 para mejorar el tratamiento de pacientes con cáncer con inhibidores HSP90, incluyendo métodos ex vivo e in vivo para determinar si un tumor responderá probablemente a la terapia con un inhibidor HSP90.

9. 发明专利

AU2012282903A1 Uses of labeled HSP90 inhibitors 未知
公开(公告)号：AU2012282903A1
公开(公告)日：2014-02-13
申请号：AU2012282903
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： A61K51/04 , G01N33/50
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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