专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US07030243B1 Process for making camptothecin derivatives 失效
标题翻译：制造喜树碱衍生物的方法
公开(公告)号：US07030243B1
公开(公告)日：2006-04-18
申请号：US10976109
申请日：2004-10-28
申请人： Ye Wu , Kesavaram Narkunan , Jianyan Wang , Harry Kochat
发明人： Ye Wu , Kesavaram Narkunan , Jianyan Wang , Harry Kochat
IPC分类号： C07D491/22
CPC分类号： C07D491/22
摘要： A process for synthesizing highly lipophilic derivatives of camptothecin. The process includes reacting dissolved, underivatized camptothecin with a silylated heterocyclic compound in a modified Minisci-type alkylation reaction to produce 7-substituted derivatives of camptothecin.
摘要翻译：合成喜树碱高亲脂性衍生物的方法。该方法包括在经修饰的Minisci型烷基化反应中使溶解的，未衍生的喜树碱与甲硅烷基化杂环化合物反应，以产生喜树碱的7-取代衍生物。

2. 发明授权

US06977311B2 Process for synthesizing L-γ-methylene glutamic acid and analogs 失效
标题翻译：合成L-γ-亚甲基谷氨酸和类似物的方法
公开(公告)号：US06977311B2
公开(公告)日：2005-12-20
申请号：US10627484
申请日：2003-07-25
申请人： Harry Kochat , Xinghai Chen , Ye Wu , Qiuli Huang , Jianyan Wang , Vincent Gerusz
发明人： Harry Kochat , Xinghai Chen , Ye Wu , Qiuli Huang , Jianyan Wang , Vincent Gerusz
IPC分类号： A61K20060101 , C07C53/00 , C07C207/00 , C07C227/22 , C07C229/00 , C07C229/24 , C07C229/30 , C07D209/46
CPC分类号： C07C227/22 , C07C229/30
摘要： A process for synthesizing substantially enantiomerically pure L-amino acids, particularly L-γ-methylene glutamic acid, and esters and salts thereof. The process includes the derivatization of (2S)-pyroglutamic acid, and the decyclization of the resulting derivative to form the desired end product.
摘要翻译：基本上对映体纯的L-氨基酸，特别是L-γ-亚甲基谷氨酸及其酯和盐的合成方法。该方法包括（2S） - 吡咯烷酸的衍生化，以及所得衍生物的脱环形成所需的最终产物。

3. 发明申请

US20050020833A1 Process for synthesizing antifolates 失效
标题翻译：合成抗叶酸剂的方法
公开(公告)号：US20050020833A1
公开(公告)日：2005-01-27
申请号：US10627483
申请日：2003-07-25
申请人： Ye Wu , Harry Kochat
发明人： Ye Wu , Harry Kochat
IPC分类号： C07D239/95 , C07D487/02
CPC分类号： C07D239/95 , Y02P20/55
摘要： A process for synthesizing antifolate compounds is disclosed. The process includes cyclization of a readily available starting reagent, followed by one or more coupling steps to produce compounds that mimic folic acid. The compounds synthesized have commercial use as drugs in oncology, inflammatory disease, and other medical fields.
摘要翻译：公开了合成抗叶酸化合物的方法。该方法包括容易获得的起始试剂的环化，随后进行一个或多个偶联步骤以产生模拟叶酸的化合物。合成的化合物在肿瘤学，炎性疾病和其他医学领域具有商业用途。

4. 发明授权

US07060825B2 Process for synthesizing 6-quinazolinyl-ethyl-benzoyl and related antifolates 失效
标题翻译：合成6-喹唑啉基 - 苯甲酰基和相关抗叶酸剂的方法
公开(公告)号：US07060825B2
公开(公告)日：2006-06-13
申请号：US10627483
申请日：2003-07-25
申请人： Ye Wu , Harry Kochat
发明人： Ye Wu , Harry Kochat
IPC分类号： C07D239/80 , C07D239/84
CPC分类号： C07D239/95 , Y02P20/55
摘要： The invention claimed herein relates to an improvement in a process for synthesizing a compound of formula Ib: wherein R1 and R2 are each individually amino or N-alkyl substituted amino; hydroxy; alkoxy; keto; lower alkyl; or a nitrogen or oxygen protecting group; R3 is hydrogen; hydroxy; alkoxy; trifluoromethyl alkoxy; halo; sulfhydryl or alkylthio; R4 is —C(O)—X; X is hydroxy; alkoxy; or an amino acid residue; in which process a 2-amino-5-nitro-benzonitrile starting reagent is cyclized to form 2,4-diamino-6-nitro-quinazoline, which is converted to 2,4,6-triamino-quinazoline, which is converted to 2,4-diamino-6-cyano-quinazoline, which is converted to 2,4-diamino-6-formyl-quinazoline; in which the improvement includes: reacting an R4-p-benzoic acid alkylene moiety with triethyl phosphite to form a 4-R4-carbonyloxyalkyl-phenyl-alkyldiethylphosphite; and reacting the 2,4-diamino-6-formyl-quinazoline with the 4-R4-carbonyloxyalkyl-phenyl-alkyldiethylphosphite to form the compound of formula Ib.
摘要翻译：本发明要求涉及用于合成式Ib化合物的方法的改进：其中R 1和R 2各自为氨基或N-烷基取代的氨基; 羟基; 烷氧基酮低级烷基或氮或氧保护基团; R 3是氢; 羟基; 烷氧基三氟甲基烷氧基; 光环; 巯基或烷硫基; R 4是-C（O）-X; X是羟基; 烷氧基或氨基酸残基; 在该方法中，2-氨基-5-硝基 - 苄腈起始试剂环化形成2,4-二氨基-6-硝基 - 喹唑啉，将其转化为2,4,6-三氨基 - 喹唑啉，将其转化为2 ，4-二氨基-6-氰基 - 喹唑啉，其转化为2,4-二氨基-6-甲酰基 - 喹唑啉; 其中的改进包括：使R 4对 - 苯甲酸亚烷基部分与亚磷酸三乙酯反应以形成4-R 4 - 碳酰氧基烷基 - 苯基 - 烷基二乙基亚磷酸酯; 并使2,4-二氨基-6-甲酰基 - 喹唑啉与4-R 4 - 羰基氧基烷基 - 苯基 - 烷基亚乙基亚乙基酯反应，形成式Ib化合物。

5. 发明申请

US20060094876A1 PROCESS FOR MAKING CAMPTOTHECIN DERIVATIVES 失效
标题翻译：制备CAMPTOTHECIN衍生物的方法
公开(公告)号：US20060094876A1
公开(公告)日：2006-05-04
申请号：US10976109
申请日：2004-10-28
申请人： Ye Wu , Kesavaram Narkunan , Jianyan Wang , Harry Kochat
发明人： Ye Wu , Kesavaram Narkunan , Jianyan Wang , Harry Kochat
IPC分类号： C07F7/02
CPC分类号： C07D491/22
摘要： A process for synthesizing highly lipophilic derivatives of camptothecin. The process includes reacting dissolved, underivatized camptothecin with a silylated heterocyclic compound in a modified Minisci-type alkylation reaction to produce 7-substituted derivatives of camptothecin.
摘要翻译：合成喜树碱高亲脂性衍生物的方法。该方法包括在经修饰的Minisci型烷基化反应中使溶解的，未衍生的喜树碱与甲硅烷基化杂环化合物反应，以产生喜树碱的7-取代衍生物。

6. 发明授权

US07687497B2 C10-substituted camptothecin analogs 有权
标题翻译： C10取代的喜树碱类似物
公开(公告)号：US07687497B2
公开(公告)日：2010-03-30
申请号：US11974756
申请日：2007-10-16
申请人： Kesavaram Narkunan , Xinghai Chen , Harry Kochat , Frederick Hausheer
发明人： Kesavaram Narkunan , Xinghai Chen , Harry Kochat , Frederick Hausheer
IPC分类号： A61K31/4375 , A61K31/5377 , A61P35/00 , C07F7/10
CPC分类号： C07F7/0812 , A61K31/4375 , A61K31/5377
摘要： The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW
摘要翻译：本发明的新颖的C10修饰的喜树碱类似物及其药学上可接受的盐：（i）具有有效的抗肿瘤活性（即纳米摩尔或亚纳摩尔浓度），用于在体外抑制人和动物肿瘤细胞的生长; （ii）是拓扑异构酶I的有效抑制; （iii）对MDR / MRP耐药性不敏感; （iv）不需要代谢药物活化：（v）缺乏A环或B环的葡糖醛酸化; （vi）降低与血浆蛋白质的药物结合亲和力; （vii）维持内酯稳定性; （viii）维持药物效力; 和（ix）具有低分子量（例如MW <600）。

7. 发明授权

US08722886B1 Methods for the total chemical synthesis of enantiomerically-pure 7-(2′-trimethylsilyl)ethyl camptothecin 有权
标题翻译：完全化学合成对映体纯7-（2'-三甲基甲硅烷基）乙基喜树碱的方法
公开(公告)号：US08722886B1
公开(公告)日：2014-05-13
申请号：US13694255
申请日：2012-11-13
申请人： Xinghai Chen , Frederick H. Hausheer , Andrey Malakhov , Harry Kochat
发明人： Xinghai Chen , Frederick H. Hausheer , Andrey Malakhov , Harry Kochat
IPC分类号： C07F7/02 , C07D491/147
CPC分类号： C07F7/10 , C07F7/0812
摘要： The present invention discloses and claims five (5) novel, highly efficient synthetic routes for the total synthesis of enantiomerically-pure (i.e., 99%) 7-(2′-trimethylsilyl)ethyl camptothecin (BNP1350; Karenitecin; Cositecan). These aforementioned synthetic schemes are the first to disclose the total syntheses of 7-(2′-trimethylsilyl)ethyl camptothecin using a highly novel direct, non-linear and convergent synthetic strategy which involves annealing the key C7-(trimethylsilyl)ethyl side chain-bearing A ring key synthons to an enantiomerically-pure tricyclic pyridone; rather than through the conventional methodology which incorporates the C7-(trimethylsilyl)ethyl side chain as the final synthetic step on a totally synthesized camptothecin parent compound. The current novel synthetic approaches reported herein since utilize desirably functionalized A-ring with preinstalled trimethyl silyl ethyl side chain, the aforementioned synthetic methodologies have a wider scope of making wide range of pharmaceutically relevant A-ring substituted BNP1350 analogs by substituting desirably functionalized nitro or protected amino phenyl carboxy A-ring as the starting material.
摘要翻译：本发明公开并要求五（5）种用于全合成对映体纯（即99％）7-（2'-三甲基甲硅烷基）乙基喜树碱（BNP1350; Karenitecin; CositECAN））的新型高效合成途径。这些上述合成方案是首先使用高度新颖的直接，非线性和收敛的合成策略来公开7-（2'-三甲基甲硅烷基）乙基喜树碱的总合成，其涉及关键的C7-（三甲基甲硅烷基）乙基侧链 - 带有A对键合物到对映体纯的三环吡啶酮; 而不是通过在全合成的喜树碱母体化合物上结合C7-（三甲基甲硅烷基）乙基侧链作为最终合成步骤的常规方法。由于利用预先安装的三甲基甲硅烷基乙基侧链所需的官能化的A环，本文报道的目前新的合成方法，通过将期望的官能化硝基或被保护的取代基取代了较宽范围的药学上相关的A环取代的BNP1350类似物氨基苯基羧基A环作为起始原料。

8. 发明申请

US20140073793A1 Germanium-containing camptothecin analogues 审中-公开
标题翻译：含锗喜树碱类似物
公开(公告)号：US20140073793A1
公开(公告)日：2014-03-13
申请号：US13573294
申请日：2012-09-07
申请人： Xinghai Chen , Harry Kochat , Pavankumar N.V. Petluru , Aulma Parker , Frederick H. Hausheer
发明人： Xinghai Chen , Harry Kochat , Pavankumar N.V. Petluru , Aulma Parker , Frederick H. Hausheer
IPC分类号： C07F7/30
CPC分类号： C07F7/30
摘要： The present invention discloses: (i) the novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts thereof; (ii) methods of synthesis of said novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts; (iii) pharmaceutically-acceptable formulations comprising said novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts thereof; and (iv) methods of administration of said novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts thereof to subjects in need thereof, including subjects with cancer.
摘要翻译：本发明公开：（i）新颖的含锗喜树碱化合物，7 [2'-三甲基甲酰基]乙基-20（S）喜树碱及其药学上可接受的盐; （ii）合成所述新颖的含锗喜树碱化合物的方法，7 [2'-三甲基麦角糖基]乙基-20（S）喜树碱及其药学上可接受的盐; （iii）包含所述新颖的含锗喜树碱化合物，7 [2'-三甲基麦角糖基]乙基-20（S）喜树碱的药学上可接受的制剂及其药学上可接受的盐; 和（iv）将所述新颖的含锗喜树碱化合物，7 [2'-三甲基甲酰基]乙基-20（S）喜树碱及其药学上可接受的盐给予需要的受试者，包括患有癌症的受试者的方法。

9. 发明授权

US07829541B2 Compounds and methods for reducing undesired toxicity of chemotherapeutic agents 有权
公开(公告)号：US07829541B2
公开(公告)日：2010-11-09
申请号：US11985272
申请日：2007-11-14
申请人： Frederick H. Hausheer , Harry Kochat , Qiuli Huang
发明人： Frederick H. Hausheer , Harry Kochat , Qiuli Huang
IPC分类号： A61K38/05
CPC分类号： A61K45/06 , A61K38/00
摘要： Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.

10. 发明授权

US07829539B2 Compounds and methods for reducing undesired toxicity of chemotherapeutic agents 有权
公开(公告)号：US07829539B2
公开(公告)日：2010-11-09
申请号：US11985243
申请日：2007-11-14
申请人： Frederick H. Hausheer , Harry Kochat , Qiuli Huang
发明人： Frederick H. Hausheer , Harry Kochat , Qiuli Huang
IPC分类号： A61K38/05
CPC分类号： A61K45/06 , A61K38/00
摘要： Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式