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长春瑞滨衍生物、其药物组合物及其制备方法和用途
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Vinorelbine derivative, medicine composition thereof, and preparation method and application of derivative and medicine composition

申请号:201310167103.2 申请日:2013-05-08
摘要:本发明公开了具有下式(I)所示结构的长春瑞滨衍生物或其可药用的盐,以及含治疗有效量的所述长春瑞滨衍生物或其可药用的盐的药物组合物;还公开了所述长春瑞滨衍生物或其可药用的盐的制备方法及其在制备治疗肿瘤的药物中的应用。所述长春瑞滨衍生物对多种人源肿瘤细胞株具有抑制活性,可作为治疗恶性肿瘤的药物。
Abstract: The invention discloses a vinorelbine derivative with a formula I as shown in the description, and a medicinal salt thereof, as well as a medicine composition containing the derivative or the medicinal salt composition of the derivative. The invention also discloses a preparation method for the vinorelbine derivative or the medicinal salt thereof, as well as application thereof in preparing medicines used for curing cancers. The vinorelbine derivative has an activity suppression function for various anthropogenic tumor cell lines and can serve as a medicine for treating malignancy.
申请人: 石家庄以岭药业股份有限公司
Applicant: SHIJIAZHUANG YILING PHARMACEUTICAL CO LTD
地址: 050035 河北省石家庄市高新********(隐藏)
发明(设计)人: 胡立宏 赵韶华 王宏涛 李向军 安军永 王超 王永 李云鹏 秦拢 王猛
Inventor: HU LIHONG; ZHAO SHAOHUA; WANG HONGTAO; LI XIANGJUN; AN JUNYONG; WANG CHAO; WANG YONG; LI YUNPENG; QIN LONG; WANG MENG
主分类号: C07D519/04(2006.01)I
分类号: C07D519/04(2006.01)I A61K31/475(2006.01)I A61P35/00(2006.01)I A61P35/02(2006.01)I
  • 法律状态
2016-03-02  授权
2013-12-25  实质审查的生效IPC(主分类):C07D 519/04申请日:20130508
2013-12-04  公开
注:本法律状态信息仅供参考,即时准确的法律状态信息须到国家知识产权局办理专利登记簿副本。
  • 其他信息
主权项  具有式Ⅰ所示结构的长春瑞滨衍生物或其可药用的盐:其中R1为C1?C6烷酰基;和R2选自以下任一结构基团:OR3、NR4R5;其中R3为H、C1?C6烷酰基或芳香酰基,R4、R5各自独立地位为H、C1?C6烷酰基、C3?C6环烷酰基、芳香酰基或C3?C6杂芳香酰基;R3、R4、R5中所述芳香酰基中的芳香基为苯基或者被1?4个选自卤素、甲基、三氟甲基和甲氧基中的基团所取代的苯基,且所述杂芳香酰基中的杂原子是1?3个选自O、S和N的原子。FDA00003159209200011.jpg
公开号  103421028A
公开日  2013-12-04
专利代理机构  北京邦信阳专利商标代理有限公司 11012
代理人  黄泽雄 陈万青
颁证日  
优先权  2012.05.16 CN 201210154298.2
 
国别 优先权号 优先权日 类型
CN  201210154298  20120516 
CN  201310167103  20130508 
国际申请  
国际公布  
进入国家日期  
  • 专利对比文献
类型 阶段 文献号 公开日期 涉及权利要求项 相关页数
SEA  CN101628916A  20100120  1-15  全文 
SEA  WO2007098091A2  20070830  1-15  说明书全文 
SEA  CN101235046A  20080806  1-15  权利要求1-2、9,说明书第2页 
注:不保证该信息的有效性、完整性、准确性,以上信息也不具有任何效力,仅供参考。使用前请另行委托专业机构进一步查核,使用该信息的一切后果由用户自行负责。
X:单独影响权利要求的新颖性或创造性的文件;
Y:与检索报告中其他 Y类文件组合后影响权利要求的创造性的文件;
A:背景技术文件,即反映权利要求的部分技术特征或者有关的现有技术的文件;
R:任何单位或个人在申请日向专利局提交的、属于同样的发明创造的专利或专利申请文件;
P:中间文件,其公开日在申请的申请日与所要求的优先权日之间的文件,或会导致需核实该申请优先权的文件;
E:单独影响权利要求新颖性的抵触申请文件。
  • 期刊对比文献
类型 阶段 期刊文摘名称 作者 标题 涉及权利要求项 相关页数
SEA  《Journal of Natural Products》200809047110  Han-Kun Zhang 等  Synthesis and Structure-Activity Relationship Studies of Cytotoxic Ester and Ether Anhydrovinblastine Derivatives  1-15  第1669-1676页,尤其流程图1,表1 
HAN-KUN ZHANG 等: "Synthesis and Structure-Activity Relationship Studies of Cytotoxic Ester and Ether Anhydrovinblastine Derivatives", 《JOURNAL OF NATURAL PRODUCTS》, vol. 71, no. 10, 4 September 2008 (2008-09-04) 
SEA  《Bioorganic & Medicinal Chemistry Letters》20111106221doi:10.1016/j.bmcl.2011.10.114  Weibin Song 等  Ceric ammonium nitrate-promoted oxidative coupling reaction for the synthesis and evaluation of a series of anti-tumor amide anhydrovinblastine analogs  1-15  第387-390页,尤其图1,流程图1,表1-2 
WEIBIN SONG 等: "Ceric ammonium nitrate-promoted oxidative coupling reaction for the synthesis and evaluation of a series of anti-tumor amide anhydrovinblastine analogs", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》, vol. 22, no. 1, 6 November 2011 (2011-11-06), XP029121540, DOI: doi:10.1016/j.bmcl.2011.10.114 
SEA  《Journal of Natural Products》20090605726  Yong Shao 等  Synthesis and Structure-Activity Relationship Studies of Cytotoxic Anhydrovinblastine Amide Derivatives  1-15  第1170-1177页,尤其流程图1,表1-2 
YONG SHAO 等: "Synthesis and Structure-Activity Relationship Studies of Cytotoxic Anhydrovinblastine Amide Derivatives", 《JOURNAL OF NATURAL PRODUCTS》, vol. 72, no. 6, 5 June 2009 (2009-06-05) 
SEA  《Bioorganic & Medicinal Chemistry Letters》201203292210doi:10.1016/j.bmcl.2012.03.082  Weibin Song 等  The effect of vindoline C-16 substituents on the biomimetic coupling reaction: Synthesis and cytotoxicity evaluation of the corresponding vinorelbine analogues  1-15  第3485-3487页,尤其Figure 1-2,Scheme 1,Table 1-2,第3487页,Supplementary data部分 
WEIBIN SONG 等: "The effect of vindoline C-16 substituents on the biomimetic coupling reaction: Synthesis and cytotoxicity evaluation of the corresponding vinorelbine analogues", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》, vol. 22, no. 10, 29 March 2012 (2012-03-29), XP028479284, DOI: doi:10.1016/j.bmcl.2012.03.082 
SEA  《Bioorganic & Medicinal Chemistry Letters》201203292210doi:10.1016/j.bmcl.2012.03.082  Weibin Song 等  The effect of vindoline C-16 substituents on the biomimetic coupling reaction: Synthesis and cytotoxicity evaluation of the corresponding vinorelbine analogues  1-15   
WEIBIN SONG 等: "The effect of vindoline C-16 substituents on the biomimetic coupling reaction: Synthesis and cytotoxicity evaluation of the corresponding vinorelbine analogues", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》, vol. 22, no. 10, 29 March 2012 (2012-03-29), XP028479284, DOI: doi:10.1016/j.bmcl.2012.03.082 
SEA  《Bioorganic & Medicinal Chemistry》200705231515  Yong Shao 等  Synthesis and structure–activity relationships study of novel anti-tumor carbamate anhydrovinblastine analogues  1-15  第5061-5075页,尤其图1,流程图1-2,表1-2 
YONG SHAO 等: "Synthesis and structure–activity relationships study of novel anti-tumor carbamate anhydrovinblastine analogues", 《BIOORGANIC & MEDICINAL CHEMISTRY》, vol. 15, no. 15, 23 May 2007 (2007-05-23) 
SEA  《Experientia》197811153411  F. Zavala 等  Interaction of vinblastine analogues with tubulin  1-15  第1497-1499页 
F. ZAVALA 等: "Interaction of vinblastine analogues with tubulin", 《EXPERIENTIA》, vol. 34, no. 11, 15 November 1978 (1978-11-15), pages 1497 - 1499 
SEA  《Cancer Biology & Therapy》2007053165  Weihong Li 等  BM6, a New Semi-Synthetic Vinca Alkaloid, Exhibits Its Potent In Vivo Anti-Tumor Activities Via its High Binding Affinity for Tubulin and Improved Pharmacokinetic Profiles  1-15  第787-794页,尤其图1,第788页 
WEIHONG LI 等: "BM6, a New Semi-Synthetic Vinca Alkaloid, Exhibits Its Potent In Vivo Anti-Tumor Activities Via its High Binding Affinity for Tubulin and Improved Pharmacokinetic Profiles", 《CANCER BIOLOGY & THERAPY》, vol. 6, no. 5, 31 May 2007 (2007-05-31) 
  • 书籍对比文献
类型 阶段 书名 作者 标题 涉及权利要求项 相关页数