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1. 发明申请

US20060167103A1 Methods of treating cancer with HDAC inhibitors 有权
公开(公告)号：US20060167103A1
公开(公告)日：2006-07-27
申请号：US11391971
申请日：2006-03-28
申请人： Nicholas Bacopoulos , Judy Chiao , Thomas Miller , Carolyn Paradise , Victoria Richon
发明人： Nicholas Bacopoulos , Judy Chiao , Thomas Miller , Carolyn Paradise , Victoria Richon
IPC分类号： A61K9/64 , A61K31/19
CPC分类号： A61K9/4866 , A61K9/0019 , A61K9/1652 , A61K31/13 , A61K31/165 , A61K31/19 , A61K31/44 , A61K47/12 , A61K47/38
摘要： The present invention provides methods of treating cancers, chemoprevention, selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

2. 发明申请

US20060276547A1 Methods of treating cancer with HDAC inhibitors 审中-公开
标题翻译：用HDAC抑制剂治疗癌症的方法
公开(公告)号：US20060276547A1
公开(公告)日：2006-12-07
申请号：US11492478
申请日：2006-07-24
申请人： Nicholas Bacopoulos , Judy Chiao , Thomas Miller , Carolyn Paradise , Victoria Richon
发明人： Nicholas Bacopoulos , Judy Chiao , Thomas Miller , Carolyn Paradise , Victoria Richon
IPC分类号： A61K31/19 , A61K38/12
CPC分类号： A61K31/19
摘要： The present invention relates to methods of treating cancers, e.g., lymphoma. More specifically, the present invention relates to methods of treating diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.
摘要翻译：本发明涉及治疗癌症例如淋巴瘤的方法。更具体地，本发明涉及通过给药包含HDAC抑制剂例如辛二酰苯胺异羟肟酸（SAHA）的药物组合物来治疗弥漫性大B细胞淋巴瘤（DLBCL）的方法。药物组合物的口服制剂具有有利的药代动力学特征，例如高生物利用度，并且令人惊讶地在长时间内引起活性化合物的高血药浓度。本发明进一步提供这些药物组合物的安全的每日给药方案，其易于遵循，并且其在体内导致治疗有效量的HDAC抑制剂。

3. 发明申请

US20070190022A1 Combination methods of treating cancer 审中-公开
标题翻译：治疗癌症的组合方法
公开(公告)号：US20070190022A1
公开(公告)日：2007-08-16
申请号：US10567953
申请日：2004-08-12
申请人： Nicholas Bacopoulos , Judy Chiao , Paul Marks , Thomas Miller , Carolyn Paradise , Victoria Richon , Richard Rifkind
发明人： Nicholas Bacopoulos , Judy Chiao , Paul Marks , Thomas Miller , Carolyn Paradise , Victoria Richon , Richard Rifkind
IPC分类号： A61K38/20 , A61K38/19 , A61K38/09 , A61K31/7072 , A61K31/57 , A61K31/522 , A61K31/19
CPC分类号： A61K45/06 , A61K9/0019 , A61K31/167 , A61K31/19 , A61K31/522 , A61K31/57 , A61K31/7068 , A61K31/7072 , A61K38/00 , A61K2300/00
摘要： The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor or a pharmaceutically acceptable salt or hydrate thereof, in a first treatment procedure, and a second amount of an anti-cancer agent in a second treatment procedure. The first and second amounts together comprise a therapeutically effective amount. The effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.
摘要翻译：本发明涉及在有需要的受试者中治疗癌症的方法，通过在有需要的受试者的第一处理方法中施用第一量的组蛋白脱乙酰酶（HDAC）抑制剂或其药学上可接受的盐或水合物，以及第二处理程序中的第二量的抗癌剂。第一和第二量一起包括治疗有效量。 HDAC抑制剂和抗癌剂的作用可以是相加的或协同的。

4. 发明申请

US20070060614A1 Methods of treating cancer with hdac inhibitors 审中-公开
标题翻译：用hdac抑制剂治疗癌症的方法
公开(公告)号：US20070060614A1
公开(公告)日：2007-03-15
申请号：US10567952
申请日：2004-08-26
申请人： Nicholas Bacopoulos , Judy Chiao , Thomas Miller , Carolyn Paradise , Victoria Richon
发明人： Nicholas Bacopoulos , Judy Chiao , Thomas Miller , Carolyn Paradise , Victoria Richon
IPC分类号： A61K31/445 , A61K31/44 , A61K31/426 , A61K31/19
CPC分类号： A61K31/19 , A61K31/426 , A61K31/44 , A61K31/445
摘要： The present invention relates to methods of treating cancers, e.g., mesothelioma or lymphoma. More specifically, the present invention relates to methods of treating mesothelioma or diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.
摘要翻译：本发明涉及治疗癌症的方法，例如间皮瘤或淋巴瘤。更具体地，本发明涉及通过给药包含HDAC抑制剂例如辛二酰苯胺异羟肟酸（SAHA）的药物组合物治疗间皮瘤或弥漫性大B细胞淋巴瘤（DLBCL）的方法。药物组合物的口服制剂具有有利的药代动力学特征，例如高生物利用度，并且令人惊讶地在长时间内引起活性化合物的高血药浓度。本发明进一步提供这些药物组合物的安全的每日给药方案，其易于遵循，并且其在体内导致治疗有效量的HDAC抑制剂。

5. 发明申请

US20080114069A1 Methods of inducing terminal differentiation 审中-公开
标题翻译：诱导终末分化的方法
公开(公告)号：US20080114069A1
公开(公告)日：2008-05-15
申请号：US11983469
申请日：2007-11-09
申请人： Victoria Richon , Judy Chiao , William Kelly , Thomas Miller
发明人： Victoria Richon , Judy Chiao , William Kelly , Thomas Miller
IPC分类号： A61K31/19
CPC分类号： A61K9/4866 , A61K9/0019 , A61K9/1652 , A61K31/13 , A61K31/164 , A61K31/165 , A61K31/19 , A61K31/44 , A61K38/12 , A61K47/12 , A61K47/38
摘要： The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.
摘要翻译：本发明提供了通过施用包含有效的HDAC抑制剂的药物组合物选择性诱导肿瘤细胞的终末分化，细胞生长停滞和/或细胞凋亡和/或抑制组蛋白脱乙酰酶（HDAC）的方法。本发明的药物组合物中活性化合物的口服生物利用度令人惊奇的高。此外，药物组合物在长时间内意外地引起活性化合物的高，治疗有效的血液水平。本发明进一步提供这些药物组合物的安全的每日给药方案，其易于遵循，并且其在体内导致治疗有效量的HDAC抑制剂。

6. 发明申请

US20070117815A1 Method of treating cancers with SAHA and pemetrexed 审中-公开
标题翻译：用SAHA和培美曲塞治疗癌症的方法
公开(公告)号：US20070117815A1
公开(公告)日：2007-05-24
申请号：US11592512
申请日：2006-11-03
申请人： James Pluda , Stanley Frankel , Victoria Richon , Steven Averbuch , Judy Chiao
发明人： James Pluda , Stanley Frankel , Victoria Richon , Steven Averbuch , Judy Chiao
IPC分类号： A61K31/519 , A61K31/19
CPC分类号： A61K31/167 , A61K31/19 , A61K31/4985 , A61K31/519 , A61K31/69 , A61K2300/00
摘要： The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of an anti-cancer agent. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.
摘要翻译：本发明涉及通过向有需要的受试者施用第一量的组蛋白脱乙酰酶（HDAC）抑制剂或其药学上可接受的盐或水合物，并且将第二量的一种抗癌剂。 HDAC抑制剂和抗癌剂可以施用以包含治疗有效量。在各个方面，HDAC抑制剂和抗癌剂的作用可以是相加的或协同的。

7. 发明申请

US20090105329A1 Methods of Treating Cancers with SAHA, Carboplatin, and Paclitaxel and Other Combination Therapies 审中-公开
标题翻译：用SAHA，卡铂和紫杉醇等组合治疗癌症的方法
公开(公告)号：US20090105329A1
公开(公告)日：2009-04-23
申请号：US12084026
申请日：2006-11-03
申请人： Judy Chiao , Carolyn Paradise , Stanley R. Frankel , Suresh Sakkarai Ramalingam , Chandra Belani
发明人： Judy Chiao , Carolyn Paradise , Stanley R. Frankel , Suresh Sakkarai Ramalingam , Chandra Belani
IPC分类号： A61K31/337 , A61P35/00
CPC分类号： A61K31/167 , A61K31/337 , A61K31/555 , A61K2300/00
摘要： The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof an amount of a histone deacetylase (HDAC) inhibitor, e.g., suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and an amount of one or more anticancer agents such as Carboplatin or Paclitaxel. The HDAC inhibitor and the anticancer agents may be administered to comprise therapeutically effective amounts.
摘要翻译：本发明涉及通过向有需要的受试者施用一定量的组蛋白脱乙酰酶（HDAC）抑制剂，例如辛二酰苯胺异羟肟酸（SAHA）或其药学上可接受的盐或其水合物，以及一种或多种抗癌剂如卡铂或紫杉醇的量。 HDAC抑制剂和抗癌剂可以施用以包含治疗有效量。

8. 发明申请

US20090118315A1 Methods of Treatment Using Sapacitabine 有权
标题翻译：使用沙美他滨治疗方法
公开(公告)号：US20090118315A1
公开(公告)日：2009-05-07
申请号：US12265553
申请日：2008-11-05
申请人： Athos Gianella-Borradori , Judy Chiao
发明人： Athos Gianella-Borradori , Judy Chiao
IPC分类号： A61K31/505
CPC分类号： A61K31/505
摘要： A first aspect of the invention relates to a method of treating leukaemia or myelodysplastic syndromes (MDS), said method comprising administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, to a subject in accordance with a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 7 consecutive days every 21 days or 14 consecutive days every 21 days.A second aspect of the invention relates to a method of treating a proliferative disorder, said method comprising administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, to a subject in accordance with a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 7 consecutive days every 21 days or 14 consecutive days every 21 days, wherein the sapacitabine, or metabolite thereof, is administered in the form of a liquid filled capsule.A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, to a subject in accordance with a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 7 consecutive days every 21 days.Further aspects of the invention relate to kits directed to the same.
摘要翻译：本发明的第一方面涉及一种治疗白血病或骨髓增生异常综合征（MDS）的方法，所述方法包括根据包含至少一种治疗的给药方案向受试者施用治疗有效量的沙美沙胺或其代谢物其中所述治疗周期包括每21天或连续第14天每21天施用治疗有效量的西他滨或其代谢物连续7天。本发明的第二方面涉及治疗增殖性疾病的方法，所述方法包括根据包含至少一个治疗周期的给药方案向受试者施用治疗有效量的沙美他滨或其代谢物，其中所述治疗周期包括每21天或连续第21天每21天施用治疗有效量的西他滨或其代谢物连续7天，其中所述的沙美他滨或其代谢物以液体填充的胶囊的形式施用。本发明的第三方面涉及一种治疗增殖性疾病的方法，所述方法包括根据包含至少一个治疗周期的给药方案向受试者施用治疗有效量的沙美沙胺或其代谢物，其中所述治疗周期包括每21天施用治疗有效量的西沙必利或其代谢物连续7天。本发明的其它方面涉及针对其的试剂盒。

9. 发明申请

US20100125084A1 DOSING REGIMENS FOR TREATMENT OF PROLIFERATIVE DISORDERS COMPRISING ADMINISTRATION OF SAPACITABINE 有权
标题翻译：治疗包含SAPACITABINE治疗的增殖性疾病的剂量方案
公开(公告)号：US20100125084A1
公开(公告)日：2010-05-20
申请号：US12597293
申请日：2008-04-24
申请人： Judy Chiao
发明人： Judy Chiao
IPC分类号： A61K31/506 , A61P35/00
CPC分类号： A61K31/7068 , A61K31/513
摘要： One aspect of the present invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating a proliferative disorder, wherein the sapacitabine or metabolite thereof is administered in a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine or metabolite thereof for about 2 to about 6 days per week, for 2 weeks out of 3 weeks. Another aspect of the invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating cutaneous T-cell lymphoma (CTCL).
摘要翻译：本发明的一个方面涉及用于制备用于治疗增殖性病症的药物中的西他滨或其代谢物的用途，其中所述的沙美他滨或其代谢物以包含至少一个治疗周期的给药方案施用，其中所述治疗周期包括在3周内给予治疗有效量的每周约2至约6天的治疗有效量的沙美他滨或其代谢物2周。本发明的另一方面涉及用于制备用于治疗皮肤T细胞淋巴瘤（CTCL）的药物的西他滨或其代谢物的用途。

10. 发明授权

US08124593B2 Methods of treatment using sapacitabine 有权
标题翻译：使用西他滨的治疗方法
公开(公告)号：US08124593B2
公开(公告)日：2012-02-28
申请号：US12265553
申请日：2008-11-05
申请人： Athos Gianella-Borradori , Judy Chiao
发明人： Athos Gianella-Borradori , Judy Chiao
IPC分类号： A61K31/70
CPC分类号： A61K31/505
摘要： A first aspect of the invention relates to a method of treating leukaemia or myelodysplastic syndromes (MDS), said method comprising administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, to a subject in accordance with a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 7 consecutive days every 21 days or 14 consecutive days every 21 days.A second aspect of the invention relates to a method of treating a proliferative disorder, said method comprising administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, to a subject in accordance with a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 7 consecutive days every 21 days or 14 consecutive days every 21 days, wherein the sapacitabine, or metabolite thereof, is administered in the form of a liquid filled capsule.A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, to a subject in accordance with a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 7 consecutive days every 21 days.Further aspects of the invention relate to kits directed to the same.
摘要翻译：本发明的第一方面涉及一种治疗白血病或骨髓增生异常综合征（MDS）的方法，所述方法包括根据包含至少一种治疗的给药方案向受试者施用治疗有效量的沙美沙胺或其代谢物其中所述治疗周期包括每21天或连续第14天每21天施用治疗有效量的西他滨或其代谢物连续7天。本发明的第二方面涉及治疗增殖性疾病的方法，所述方法包括根据包含至少一个治疗周期的给药方案向受试者施用治疗有效量的沙美他滨或其代谢物，其中所述治疗周期包括每21天或连续第21天每21天施用治疗有效量的西他滨或其代谢物连续7天，其中所述的沙美他滨或其代谢物以液体填充的胶囊的形式施用。本发明的第三方面涉及一种治疗增殖性疾病的方法，所述方法包括根据包含至少一个治疗周期的给药方案向受试者施用治疗有效量的沙美沙胺或其代谢物，其中所述治疗周期包括每21天施用治疗有效量的西沙必利或其代谢物连续7天。本发明的其它方面涉及针对其的试剂盒。

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