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1. 发明专利

JP2011168619A Method for treating cancer by co-administration of anticancer agents 审中-公开
标题翻译：通过联合治疗癌症药物治疗癌症的方法
公开(公告)号：JP2011168619A
公开(公告)日：2011-09-01
申请号：JP2011121330
申请日：2011-05-31
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： NAKAHARA TAKAHITO , YAMANAKA KENTARO , KITA AYA , KAMITOKU HIROSHI
IPC分类号： A61K31/282 , A61K31/497 , A61K31/7068 , A61K33/24 , A61K39/395 , A61P35/00 , A61P43/00
CPC分类号： A61K45/06 , A61K31/337 , A61K31/4745 , A61K31/475 , A61K31/497 , A61K31/655 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K33/24 , C07D403/06 , Y10S435/975 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a companion drug having a good antineoplastic effect.
SOLUTION: The present invention relates to therapeutic compositions containing medicament as an active component, particularly 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazine-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide, and is applied in combination with one or more anticancer agents selected from the group consisting of carboplatin, cisplatin, paclitaxel, vinorelbine, gemcitabine, irinotecan, doxorubicin, and dacarbazine, or a retuximab-containing combination therapy of R-DHAP. The therapeutic compositions are useful for the treatment of cancers, preferably all solid cancers and lymphomas, particularly skin cancer, bladder cancer, breast cancer, uterine cancer, ovary cancer, prostate cancer, lung cancer, colon cancer, pancreas cancer, renal cancer, gastric cancer, and the like. Particularly, they are expected as therapeutic agents for some kinds of cancers which show resistance against other anticancer agents.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供具有良好抗肿瘤效果的伴侣药物。解决方案：本发明涉及含有作为活性成分的药物，特别是1-（2-甲氧基乙基）-2-甲基-4,9-二氧代-3-（吡嗪-2-基甲基）-4， 9-二氢-1H-萘并[2,3-d]咪唑-3-鎓溴化物，并与一种或多种抗癌剂组合使用，所述抗癌剂选自卡铂，顺铂，紫杉醇，长春瑞滨，吉西他滨，伊立替康，多柔比星和达卡巴嗪或含有瑞替西单抗R-DHAP的联合疗法。治疗组合物可用于治疗癌症，优选全部固体癌症和淋巴瘤，特别是皮肤癌，膀胱癌，乳腺癌，子宫癌，卵巢癌，前列腺癌，肺癌，结肠癌，胰腺癌，肾癌，胃癌癌症等。特别地，作为对抗其它抗癌剂的抗性的某些癌症，预期它们是治疗剂。版权所有（C）2011，JPO＆INPIT

2. 发明专利

JP2014156400A Labeled derivative for image diagnosis of tumor 审中-公开
标题翻译：用于图像诊断肿瘤的标签衍生物
公开(公告)号：JP2014156400A
公开(公告)日：2014-08-28
申请号：JP2011115628
申请日：2011-05-24
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： MURAKAMI YOSHIHIRO , MIYOSHI SOSUKE , NODA AKIHIRO , MITSUOKA KEISUKE , JITSUOKA MAKOTO , MATSUYA TAKAHIRO , KITA AYA , YAMANAKA KENTARO , NAKAHARA TAKAHITO
IPC分类号： C07D403/06 , A61K51/00
CPC分类号： C07D403/06 , A61K51/0453
摘要： PROBLEM TO BE SOLVED: To provide labeled derivatives for image diagnosis with which prompt and noninvasive classification can be performed between sensitive patients and insensitive patients to a survivin expression inhibitor, particularly YM155.SOLUTION: The present inventors conducted intensive studies about a method of performing classification between sensitive patients and insensitive patients to YM155 and has found that 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium or labeled derivatives of a salt thereof has good accumulation to a YM155-sensitive tumor and enables the tumor to be imaged by positron emission tomography (PET) or single photon emission computed tomography (SPECT). Thus, the labeled derivatives of the present invention can be used as a radio-labelled tracer for the prompt and noninvasive classification between the sensitive patients and the insensitive patients to YM155, diagnosis of size and staging of the YM155-sensitive tumor, and diagnosis for a therapeutic effect by YM155 or other antitumor agents.
摘要翻译：要解决的问题：提供用于图像诊断的标记衍生物，其可以在敏感患者和不敏感患者之间进行快速和非侵入性分类至存活蛋白表达抑制剂，特别是YM155。解决方案：本发明人对进行分类的方法进行了深入研究敏感患者和不敏感患者之间的YM155，发现1-（2-甲氧基乙基）-2-甲基-4,9-二氧代-3-（吡嗪-2-基甲基）-4,9-二氢-1H-萘并[ 2,3-d]咪唑-3-酮或其盐的标记衍生物对YM155敏感的肿瘤具有良好的积累，并且能够通过正电子发射断层摄影（PET）或单光子发射计算机断层摄影（SPECT）对肿瘤进行成像，。因此，本发明的标记衍生物可以用作放射性标记的示踪剂，用于敏感患者和不敏感患者之间的YM155的快速和非侵入性分类，YM155敏感性肿瘤的大小和分期的诊断，以及诊断 YM155或其他抗肿瘤剂的治疗作用。

3. 发明专利

DK2127652T3 FREMGANGSMÅDE TIL BEHANDLING AF CANCER UNDER ANVENDELSE AF ANTICANCERMIDDEL I KOMBINATION 未知
公开(公告)号：DK2127652T3
公开(公告)日：2013-06-10
申请号：DK07860480
申请日：2007-12-28
申请人： ASTELLAS PHARMA INC
发明人： NAKAHARA TAKAHITO , YAMANAKA KENTARO , KITA AYA , KOUTOKU HIROSHI
IPC分类号： A61K31/497 , A61K31/337 , A61K31/4164 , A61K31/4745 , A61K31/475 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K33/24 , A61K39/395 , A61K45/06 , A61P35/00 , C07D403/06

4. 发明专利

ES2409755T3 Método para Tratar el Cáncer Utilizando un Agente Anticanceroso Combinado 未知
公开(公告)号：ES2409755T3
公开(公告)日：2013-06-27
申请号：ES07860480
申请日：2007-12-28
申请人： ASTELLAS PHARMA INC
发明人： NAKAHARA TAKAHITO , YAMANAKA KENTARO , KITA AYA , KOUTOKU HIROSHI
IPC分类号： A61K31/497 , A61K31/337 , A61K31/4164 , A61K31/4745 , A61K31/475 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K33/24 , A61K39/395 , A61K45/06 , A61P35/00 , C07D403/06
摘要： Una composición farmacéutica que comprende bromuro de 1-(2-metoxietil)-2-metil-4,9-dioxo-3-(pirazin-2-ilmetil)-4,9-dihidro-1H-nafto[2,3-d]imidazol-3-io como ingrediente activo, para su uso en el tratamiento del cáncer en una terapia combinada que comprende el uso de i) rituximab, o ii) una terapia combinada seleccionada entre R-ICE que consiste en rituximab, ifosfamida, carboplatino y etopósido, y R-DHAP que consiste en rituximab, citarabina y cisplatino como agentes anticancerosos.

5. 发明公开

EP2127652A4 METHOD FOR TREATING CANCER USING ANTICANCER AGENT IN COMBINATION 有权
标题翻译：方法癌的抗癌代理一个KOMBINATONSTHERAPIE的治疗
公开(公告)号：EP2127652A4
公开(公告)日：2010-04-07
申请号：EP07860480
申请日：2007-12-28
申请人： ASTELLAS PHARMA INC
发明人： NAKAHARA TAKAHITO , YAMANAKA KENTARO , KITA AYA , KOUTOKU HIROSHI
IPC分类号： A61K31/497 , A61K31/337 , A61K31/4164 , A61K31/4745 , A61K31/475 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K33/24 , A61K39/395 , A61K45/06 , A61P35/00 , C07D403/06
CPC分类号： A61K45/06 , A61K31/337 , A61K31/4745 , A61K31/475 , A61K31/497 , A61K31/655 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K33/24 , C07D403/06 , Y10S435/975 , A61K2300/00
摘要： The invention relates to a therapeutic composition which contains as an active ingredient, a pharmaceutical, particularly 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide and is applied in combination with one or more anticancer agents selected from the group consisting of carboplatin, cisplatin, paclitaxel, vinorelbine, gemcitabine, irinotecan, docetaxel, doxorubicin, dacarbazine and rituximab, or R-ICE and R-DHAP, which is a rituximab-containing combination regimen. The composition of the invention is useful for treatment of all solid cancers and lymphomas, preferably skin cancer, bladder cancer, breast cancer, uterine cancer, ovarian cancer, prostate cancer, lung cancer, colon cancer, pancreatic cancer, renal cancer, stomach cancer and the like. In particular it is expected as a therapeutic agent for cancer resistant to other anticancer agents.

6. 发明专利

PL2127652T3 Sposób leczenia choroby nowotworowej wykorzystujący czynnik przeciwnowotworowy w kombinacji 未知
公开(公告)号：PL2127652T3
公开(公告)日：2013-10-31
申请号：PL07860480
申请日：2007-12-28
申请人： ASTELLAS PHARMA INC
发明人： NAKAHARA TAKAHITO , YAMANAKA KENTARO , KITA AYA , KOUTOKU HIROSHI
IPC分类号： A61K31/497 , A61K31/337 , A61K31/4164 , A61K31/4745 , A61K31/475 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K33/24 , A61K39/395 , A61K45/06 , A61P35/00 , C07D403/06

7. 发明专利

PT2127652E AGENTE LIBERTADOR DA HORMONA ESTIMULADORA DOS FOLÍCULOS 未知
公开(公告)号：PT2127652E
公开(公告)日：2013-07-08
申请号：PT07860480
申请日：2007-12-28
申请人： ASTELLAS PHARMA INC
发明人： NAKAHARA TAKAHITO , YAMANAKA KENTARO , KITA AYA , KOUTOKU HIROSHI
IPC分类号： A61K31/497 , A61K31/337 , A61K31/4164 , A61K31/4745 , A61K31/475 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K33/24 , A61K39/395 , A61K45/06 , A61P35/00 , C07D403/06

8. 发明专利

CA2672933A1 METHOD FOR TREATING CANCER BY A COMBINED THERAPY OF ANTICANCER AGENTS 未知
公开(公告)号：CA2672933A1
公开(公告)日：2008-07-10
申请号：CA2672933
申请日：2007-12-28
申请人： ASTELLAS PHARMA INC
发明人： NAKAHARA TAKAHITO , YAMANAKA KENTARO , KITA AYA , KOUTOKU HIROSHI
IPC分类号： A61K31/497 , A61K31/337 , A61K31/4164 , A61K31/4745 , A61K31/475 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K33/24 , A61K39/395 , A61P35/00 , C07D403/06
摘要： The invention relates to a therapeutic composition which contains as an a ctive ingredient, a pharmaceutical, particularly 1-(2-methoxyethyl)-2-methyl -4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-iu m bromide and is applied in combination with one or more anticancer agents s elected from the group consisting of carboplatin, cisplatin, paclitaxel, vin orelbine, gemcitabine, irinotecan, docetaxel, doxorubicin, dacarbazine and r ituximab, or R-ICE and R-DHAP, which is a rituximab-containing combination r egimen. The composition of the invention is useful for treatment of all soli d cancers and lymphomas, preferably skin cancer, bladder cancer, breast canc er, uterine cancer, ovarian cancer, prostate cancer, lung cancer, colon canc er, pancreatic cancer, renal cancer, stomach cancer and the like. In particu lar, it is expected as a therapeutic agent for cancer resistant to other ant icancer agents.

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