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1. 发明申请

US20070185124A1 Cancer treatment with topoisomerase-ii inhibitor, a bis-dioxypiperazine and radiation 有权
标题翻译：用拓扑异构酶-II抑制剂，双二氧嘧啶和辐射进行癌症治疗
公开(公告)号：US20070185124A1
公开(公告)日：2007-08-09
申请号：US10591847
申请日：2005-03-02
申请人： Kenneth Hofland , Maxwell Sehested , Paul Kristjansen , Annenette Thougaard , Peter Jensen
发明人： Kenneth Hofland , Maxwell Sehested , Paul Kristjansen , Annenette Thougaard , Peter Jensen
IPC分类号： A61K31/497 , A61K31/357
CPC分类号： A61K31/496 , A61K31/7048 , A61K41/00 , A61K2300/00
摘要： The present invention relates to a method of treatment of a tumour cell which comprises administering to a subject in need of treatment an effective amount of a topoisomerase-II poison, e.g. etoposide, in combination with a bis-dioxypiperazine, e.g. dexrazoxane wherein said subject is further treated with radiation.
摘要翻译：本发明涉及一种治疗肿瘤细胞的方法，其包括向需要治疗的受试者施用有效量的拓扑异构酶II毒物，例如，依托泊苷，与双 - 二氧代哌嗪，其中所述受试者进一步用辐射治疗。

2. 发明授权

US07906515B2 Cancer treatment with topoisomerase-II inhibitor, a bis-dioxypiperazine and radiation 有权
标题翻译：用拓扑异构酶II抑制剂，双二氧嘧啶和辐射进行癌症治疗
公开(公告)号：US07906515B2
公开(公告)日：2011-03-15
申请号：US10591847
申请日：2005-03-02
申请人： Kenneth Hofland , Maxwell Sehested , Paul Kristjansen , Annemette Thougaard , Peter Buhl Jensen
发明人： Kenneth Hofland , Maxwell Sehested , Paul Kristjansen , Annemette Thougaard , Peter Buhl Jensen
IPC分类号： A61K31/497 , A61K31/357
CPC分类号： A61K31/496 , A61K31/7048 , A61K41/00 , A61K2300/00
摘要： The present invention relates to a method of treatment of a tumour cell which comprises administering to a subject in need of treatment an effective amount of a topoisomerase-II poison, e.g. etoposide, in combination with a bis-dioxypiperazine, e.g. dexrazoxane wherein said subject is further treated with radiation.
摘要翻译：本发明涉及一种治疗肿瘤细胞的方法，其包括向需要治疗的受试者施用有效量的拓扑异构酶II毒物，例如，依托泊苷，与双 - 二氧代哌嗪，其中所述受试者进一步用辐射治疗。

3. 发明申请

US20110003777A1 Methods of Treatment Employing Prolonged Continuous Infusion of Belinostat 审中-公开
标题翻译：使用长时间持续输注贝利诺定治疗方法
公开(公告)号：US20110003777A1
公开(公告)日：2011-01-06
申请号：US12920484
申请日：2009-03-06
申请人： Maxwell Sehested , Peter Buhl Jensen , Nis Nissen
发明人： Maxwell Sehested , Peter Buhl Jensen , Nis Nissen
IPC分类号： A61K31/63 , A61P35/00
CPC分类号： A61K31/18 , A61K9/0019 , A61K47/18 , Y02A50/411
摘要： The present invention relates generally to the treatment of diseases and disorders that are mediated by histone deacetylase (HDAC), for example, cancer, with Belinostat™ (also known as (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide; PXD101; and PX 105684), and more particularly, to improvement treatments of such diseases (for example, cancers, for example, leukemias), which employ prolonged continuous infusion (e.g., prolonged continuous intravenous infusion) of Belinostat™.
摘要翻译：本发明一般涉及由Belinostat TM（也称为（E）-N-羟基-3-（3-苯基氨磺酰基 - 苯基） - 苯基）酯，由组蛋白脱乙酰酶（HDAC）介导的疾病和病症的治疗，），更特别地涉及使用Belinostat TM的延长连续输注（例如延长连续静脉内输注）的这些疾病（例如，癌症，例如白血病）的改善治疗。

4. 发明申请

US20090209535A1 6-ETHER/THIOETHER-PURINES AS TOPOISOMERASE II CATALYTIC INHIBITORS AND THEIR USE IN THERAPY 审中-公开
标题翻译： 6-ETHER / THIOETHER-PURINES作为TOPOISOMERASE II催化抑制剂及其在治疗中的应用
公开(公告)号：US20090209535A1
公开(公告)日：2009-08-20
申请号：US11815782
申请日：2006-02-08
申请人： Lars Hollund Jensen , Maxwell Sehested
发明人： Lars Hollund Jensen , Maxwell Sehested
IPC分类号： A61K31/5377 , A61K31/52 , C12N5/02
CPC分类号： C07H19/16 , A61K31/52 , A61K31/5377 , A61K31/7076 , A61K45/06 , A61K2300/00 , C07D473/00 , C07D473/18 , C07D473/24 , C07D473/38
摘要： The present invention relates to certain purines of the following formulae, which act as topoisomerase II catalytic inhibitors: wherein: J is independently: —H or —NRN1RN2; X is independently: —O—, or —S—; Q is independently: a covalent bond, C1-7alkylene, C2-7alkenylene, C2-7alkynylene, C3-7cycloalkylene, C3-7cycloalkenylene, or C3-7cycloalkynylene; T is independently: a group A1 or a group A2; A1 is independently: C6-14carboaryl, C5-14heteroaryl, C3-12carbocyclic, or C3-12heterocyclic; and is independently unsubstituted or substituted; A2 is independently: —H, —CN, —OH, or —O(C═O)—C1-7alkyl; RN is independently —H or a nitrogen ring substituent; R8 is independently —H or a ring substituent; either: each of RN1 and RN2 is independently —H or a nitrogen substituent; or: RN1 and RN2 taken together with the nitrogen atom to which they are attached form a ring having from 3 to 7 ring atoms; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. These compounds are useful in combination with topoisomerase II poisons, such as anthracyclines and epipodophyllotoxins, in the treatment of proliferative conditions (e.g., cancer). These compounds are also useful in the treatment of tissue damage associated with extravasation of a topoisomerase II poison, such as an anthracycline or an epipodophyllotoxin.
摘要翻译：本发明涉及作为拓扑异构酶II催化抑制剂的下式的某些嘌呤：其中：J独立地是：-H或-NRN1RN2; X独立地为：-O-或-S-; Q独立地为：共价键，C 1-7亚烷基，C 2-7亚烯基，C 2-7亚炔基，C 3-7亚环烷基，C 3-7环亚烯基或C 3-7环亚炔基; T独立地为：A1组或A2组; A1独立地为：C 6-14碳氢化芳基，C 5-4杂芳基，C 3-12碳环或C 3-12杂环; 并且独立地是未取代的或取代的; A 2独立地为：-H，-CN，-OH或-O（C 1 -C 6）烷基; RN独立地为-H或氮环取代基; R8独立地是-H或环取代基; 或者：RN1和RN2各自独立地为-H或氮取代基; 或：RN1和RN2与它们所连接的氮原子一起形成具有3至7个环原子的环; 酰胺，酯，醚，N-氧化物，化学保护形式及其前体药物。这些化合物可用于拓扑异构酶II毒物（例如蒽环类和表鬼臼毒素）在治疗增殖性疾病（例如癌症）中的应用。这些化合物也可用于治疗与拓扑异构酶II毒素例如蒽环类或表鬼臼毒素外渗相关的组织损伤。

5. 发明申请

US20080213399A1 Combination Therapies Using Hdac Inhibitors 审中-公开
标题翻译：使用Hdac抑制剂的组合疗法
公开(公告)号：US20080213399A1
公开(公告)日：2008-09-04
申请号：US11815372
申请日：2006-02-03
申请人： Henri Lichenstein , Mike Jeffers , Xiaozhang Qian , Maxwell Sehested , Kamille Dumong Petersen , James Ritchie
发明人： Henri Lichenstein , Mike Jeffers , Xiaozhang Qian , Maxwell Sehested , Kamille Dumong Petersen , James Ritchie
IPC分类号： A61K33/24 , A61K31/18 , A61K31/505 , A61K31/282 , A61K31/4353 , A61K31/337 , A61K31/704 , A61K31/56 , A61K31/53 , A61K31/66 , A61K31/517 , A61P35/00
CPC分类号： A61K31/18 , A61K31/138 , A61K31/196 , A61K31/198 , A61K31/24 , A61K31/282 , A61K31/337 , A61K31/4745 , A61K31/475 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/555 , A61K31/573 , A61K31/704 , A61K31/706 , A61K31/7068 , A61K31/7076 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The present invention pertains to a method for treating cancer, such as lung cancer, multiple myeloma, lymphoma, and epithelial ovarian cancer, comprising the administration to a patient in need thereof a first amount or dose of a histone deacetylase (HDAC) inhibitor, such as PXD-101, and a second amount or dose of another chemotherapeutic agent, such as dexamethasone or 5-fluorouracil, or an epidermal growth factor receptor (EGFR) inhibitor, such as TarcevaÚ, wherein the first and second amounts or doses together comprise a therapeutically effective amount.
摘要翻译：本发明涉及用于治疗癌症的方法，例如肺癌，多发性骨髓瘤，淋巴瘤和上皮性卵巢癌，其包括向有需要的患者施用第一量或剂量的组蛋白脱乙酰酶（HDAC）抑制剂，例如作为PXD-101，以及第二量或剂量的另一种化学治疗剂，例如地塞米松或5-氟尿嘧啶，或表皮生长因子受体（EGFR）抑制剂如TarcevaÚ，其中第一和第二量或剂量一起包括治疗有效量。

6. 发明授权

US06265385B1 Topoisomerase II poison and bis-dioxopiperazine derivative combination therapy 有权
标题翻译：拓扑异构酶II毒物和双二氧代哌嗪衍生物联合治疗
公开(公告)号：US06265385B1
公开(公告)日：2001-07-24
申请号：US09101499
申请日：1999-03-08
申请人： Peter Buhl Jensen , Maxwell Sehested
发明人： Peter Buhl Jensen , Maxwell Sehested
IPC分类号： A61K3170
CPC分类号： A61K31/704 , A61K31/70 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a method for selectively killing tumor or metastatic cells within a defined compartment of the organism of a large mammal, in particular a human, said method comprising administering to a mammal an effective tumor—or metastasis-killing amount of a topoisomerase II poison except doxorubicin, and protecting non-tumorous tissue of the mammal against the toxic action of the topoisomerase II poison by administration of a bis-dioxypiperazine compound. In particular, the invention relates to a pharmaceutical kit for selectively killing tumor or metastatic cells within the central nervous system in a large mammal, in particular a human, said kit comprising: a) a dosage unit of a bis-dioxypiperazine and a pharmaceutically acceptable carrier, and b) a dosage unit of topoisomerase II poisons except doxorubicin and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及一种选择性地杀死大型哺乳动物特别是人的生物体的限定区域内的肿瘤或转移细胞的方法，所述方法包括向哺乳动物施用有效的肿瘤或转移的量的拓扑异构酶 II毒物，并且通过施用双二氧代哌嗪化合物保护哺乳动物的非肿瘤组织免受拓扑异构酶II毒物的毒性作用。特别地，本发明涉及用于选择性地杀死大型哺乳动物特别是人的中枢神经系统内的肿瘤或转移性细胞的药物试剂盒，所述试剂盒包含：a）双二氧嘧啶的剂量单位和药学上可接受的载体，和b）拓扑异构酶II毒物的剂量单位，除了多柔比星和药学上可接受的载体。

7. 发明申请

US20120270900A1 NOVEL METHOD OF TREATMENT 审中-公开
标题翻译：新的治疗方法
公开(公告)号：US20120270900A1
公开(公告)日：2012-10-25
申请号：US13384559
申请日：2010-07-16
申请人： Uffe Olesen , Annemette Thougaard , Maxwell Sehested
发明人： Uffe Olesen , Annemette Thougaard , Maxwell Sehested
IPC分类号： A61K31/4545 , A61K31/455 , G01N33/573 , A61P35/00
CPC分类号： G01N33/573 , A61K31/00 , A61K31/4406 , A61K31/4409 , A61K31/452 , A61K31/4545 , A61K31/455 , A61K31/5377 , A61K45/06 , G01N33/574 , G01N2333/91091 , G01N2800/52 , A61K2300/00
摘要： The present application discloses a method for the treatment or for alleviating the symptoms of a cancer in a subject comprising the steps of a) determining the level of Nicotinic acid phosphoribosyltransferase (NAPRT) in said subject; and b) 1) in the event of a level of NAPRT which is lower than a predetermined threshold value, treating said subject sequentially/simultaneous with i) an effective amount of a nicotinamide phosphoribosyltransferase inhibitor (NAMPRTi), and ii) an effective amount of a nicotinic acid, a nicotinic acid precursor or a prodrug of nicotinic acid; or 2) in the event of a level of NAPRT which is higher than or equal to a predetermined threshold value, treating said subject with i) an effective amount of a NAMPRTi in the absence of sequential/simultaneous treatment with ii) an effective amount of a nicotinic acid, a nicotinic acid precursor or a prodrug of nicotinic acid.
摘要翻译：本申请公开了用于治疗或减轻受试者的癌症症状的方法，包括以下步骤：a）测定所述受试者中烟酸磷酸核糖基转移酶（NAPRT）的水平; 和b）1）在NAPRT水平低于预定阈值的情况下，依次/同时处理所述受试者，i）有效量的烟酰胺磷酸核糖转移酶抑制剂（NAMPRTi），和ii）有效量的烟酸，烟酸前体或烟酸前药; 或者2）在NAPRT水平高于或等于预定阈值的情况下，用i）在没有顺序/同时治疗的情况下治疗所述受试者，i）有效量的NAMPRTi，ii）有效量的烟酸，烟酸前体或烟酸前药。

8. 发明授权

US06727253B2 Treatment of accidental extravasation of anthracyclines 有权
标题翻译：治疗偶发性外渗蒽环类药物
公开(公告)号：US06727253B2
公开(公告)日：2004-04-27
申请号：US09893521
申请日：2001-06-29
申请人： Seppo W. Langer , Peter B. Jensen , Maxwell Sehested
发明人： Seppo W. Langer , Peter B. Jensen , Maxwell Sehested
IPC分类号： A61K31495
CPC分类号： A61K31/704 , A61K31/495 , A61K31/70 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a method for pharmacological treatment of accidental extravasation of topoisomerase II poisons, such as anthracyclines. In particular, the invention relates to the use of a topo II catalytic inhibitor, such as the bisdioxopiperazine ICRF-187, for the treatment of an accidental extravasation of a topoisomerase II poison. A method for treatment of such extravasation of a topoisomerase poison such as the anthracyclines, daunorubicin, doxorubicin, epirubicin, or idarubicin is disclosed.
摘要翻译：本发明涉及一种用于拓扑异构酶II毒素如蒽环类药物偶然外渗的药理学治疗方法。特别地，本发明涉及用于治疗拓扑异构酶II毒物的意外外渗的二氧代哌嗪ICRF-187的topo II催化抑制剂的用途。公开了一种治疗外源性拓扑异构酶毒素如蒽环类抗生素，柔红霉素，多柔比星，表柔比星或伊达比星的方法。

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