会员体验
专利管家（专利管理）
工作空间（专利管理）
风险监控（情报监控）
数据分析（专利分析）
侵权分析（诉讼无效）
联系我们
交流群
官方交流：
QQ群： 891211   
微信请扫码    >>>
现在联系顾问~
下载
著录项
PDF全文
热词
    • 2. 发明申请
      US20050288240A1 Novel-prodrugs for phosphorus-containing compounds 有权
    • Novel-prodrugs for phosphorus-containing compounds
    • US20050288240A1
    • 2005-12-29
    • US11145194
    • 2005-06-03
    • Mark Erion , K. Reddy , Edward Robinson , Bheemarao Ugarkar
    • Mark Erion , K. Reddy , Edward Robinson , Bheemarao Ugarkar
    • A61K31/7056 , A61K31/7072 , A61K31/7076 , C07F9/6571 , C07F9/6574 , C07H19/10 , C07H19/20 , C07H19/207
    • C07H19/10 , A61K31/7056 , A61K31/7072 , A61K31/7076 , C07F9/657154 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07H19/20 , C07H19/207 , Y02A50/411
    • Prodrugs of formula I, their uses, their intermediates, and their method of manufacture are described: wherein: V, W, and W′ are independently selected from the group consisting of —H, alkyl, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, and 1-alkynyl; or together V and Z are connected via an additional 3-5 atoms to form a cyclic group containing 5-7 atoms, optionally 1 heteroatom, substituted with hydroxy, acyloxy, alkoxycarbonyloxy, or aryloxycarbonyloxy attached to a carbon atom that is three atoms from both O groups attached to the phosphorus; or together V and Z are connected via an additional 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, that is fused to an aryl group at the beta and gamma position to the O attached to the phosphorus; together V and W are connected via an additional 3 carbon atoms to form an optionally substituted cyclic group containing 6 carbon atoms and substituted with one substituent selected from the group consisting of hydroxy, acyloxy, alkoxycarbonyloxy, alkylthiocarbonyloxy, and aryloxycarbonyloxy, attached to one of said carbon atoms that is three atoms from an O attached to the phosphorus; together Z and W are connected via an additional 3-5 atoms to form a cyclic group, optionally containing one heteroatom, and V must be aryl, substituted aryl, heteroaryl, or substituted heteroaryl; together W and W′ are connected via an additional 2-5 atoms to form a cyclic group, optionally containing 0-2 heteroatoms, and V must be aryl, substituted aryl, heteroaryl, or substituted heteroaryl; Z is selected from the group consisting of —CHR2OH, —CHR2OC(O)R3, —CHR2OC(S)R3, —CHR2OC(S)OR3, —CHR2OC(O)SR3, —CHR2OCO2R3, —OR2, —SR2, —CHR2N3, —CH2aryl, —CH(aryl)OH, —CH(CH═CR22)OH, —CH(C≡CR2)OH, —R2, —NR22, —OCOR3, —OCO2R3, —SCOR3, —SCO2R3, —NHCOR2, —NHCO2R3, —CH2NHaryl, —(CH2)p—OR12, and —(CH2)p—SR12; p is an integer 2 or 3; with the provisos that: a) V, Z, W, W′ are not all —H; and b) when Z is —R2, then at least one of V, W, and W′ is not —H, alkyl, aralkyl, or alicyclic; R2 is selected from the group consisting of R3 and —H; R3 is selected from the group consisting of alkyl, aryl, alicyclic, and aralkyl; R12 is selected from the group consisting of —H, and lower acyl; M is selected from the group that attached to PO32−, P2O63−, or P3O94− is a biologically active agent, and is attached to the phosphorus in formula I via a carbon, oxygen, sulfur or nitrogen atom; and pharmaceutically acceptable prodrugs and salts thereof.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      US20050101775A1 Prodrugs for liver specific drug delivery 有权
    • Prodrugs for liver specific drug delivery
    • 用于肝脏特异性药物递送的前药
    • US20050101775A1
    • 2005-05-12
    • US10844747
    • 2004-05-12
    • Mark Erion , K. Reddy
    • Mark Erion , K. Reddy
    • A61K31/661 , A61K31/664 , A61K49/00 , A61P3/06 , A61P3/10 , A61P29/00 , A61P31/00 , A61P31/12 , A61P33/10 , A61P35/00 , C07F9/28 , C07F9/547 , C07F9/6571 , C07F9/6584 , C07H15/252 , C07H15/26
    • C07F9/657118 , C07F9/657127 , C07F9/657154 , C07F9/65846 , C07H15/252 , C07H15/26
    • The present invention is directed towards novel cyclic phosph(oramid)ate prodrugs of alcohol-, amine-, and thiol-containing drugs, their preparation, their synthetic intermediates, and their uses. Another aspect of the invention is the use of the prodrugs to treat diseases that benefit from enhanced drug distribution to the liver and like tissues and cells that express cytochrome P450, including hepatitis, cancer, liver fibrosis, malaria, other viral and parasitic infections, and metabolic diseases where the liver is responsible for the overproduction of the biochemical end product, e.g. glucose (diabetes); cholesterol, fatty acids and triglycerides (hyperlipidemia) (atherosclerosis) (obesity). In one aspect, the invention is directed towards the use of the prodrugs to enhance oral drug delivery. In another aspect, the prodrugs are used to prolong pharmacodynamic half-life of the drug. In addition, the prodrug methodology of the current invention is used to achieve sustained delivery of the parent drug. In another aspect, the prodrugs are used to increase the therapeutic index of the drug. In another aspect of the invention, a method of making these prodrugs is described. In another aspect, the prodrugs are also useful in the delivery of diagnostic imaging agents to the liver.
    • 本发明涉及新型环状磷酸酯（oramid），其包含醇，胺和硫醇的药物，其制备方法，其合成中间体及其用途。 本发明的另一方面是使用前药治疗受益于增强的药物分布到肝脏和表达细胞色素P450的组织和细胞（包括肝炎，癌症，肝纤维化，疟疾，其他病毒和寄生虫感染）的细胞的疾病，以及 肝脏负责生化终产物过度生成的代谢性疾病，例如， 葡萄糖（糖尿病）; 胆固醇，脂肪酸和甘油三酯（高脂血症）（动脉粥样硬化）（肥胖）。 一方面，本发明涉及前药用于增强口服药物递送的用途。 另一方面，前药用于延长药物的药效半衰期。 此外，本发明的前药方法用于实现母体药物的持续递送。 在另一方面，前药用于增加药物的治疗指数。 在本发明的另一方面，描述了制备这些前药的方法。 在另一方面，前药还可用于将诊断成像剂递送至肝脏。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
每页展示10个专利
每页展示10个专利
每页展示20个专利
每页展示50个专利
每页展示100个专利

IPRDB

最新中国发明专利 最新美国发明专利 技术领域 专利库 专利分类库 国际专利分类库

热门服务

会员版试用 API 数据接口 找代理 知嘟嘟专利交易 排行榜 大学排行榜 专利百科

关于我们

平台介绍 战略合作 网站地图

友情链接

知嘟嘟专利交易 国家知识产权局 中国商标网

联系方式


©2019-2023 上海吉码数字技术有限公司 版权所有，并保留所有权利 沪ICP备20016256号-6 沪公网安备31011702005475号