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1. 发明授权

US6160167A Mercaptans and disulfides 有权
标题翻译：硫醇和二硫化物
公开(公告)号：US6160167A
公开(公告)日：2000-12-12
申请号：US145384
申请日：1998-09-01
申请人： Frederick H. Hausheer , Kochat Haridas , Qiuli Huang
发明人： Frederick H. Hausheer , Kochat Haridas , Qiuli Huang
IPC分类号： C07C323/66 , C07F9/38 , C07C309/03
CPC分类号： C07C323/66 , C07F9/3808
摘要： This invention relates to novel compositions of matter which either terminate in a sulfhydryl moiety or are disulfides. The compounds also include a terminal sulfonate or phosphonate moiety, and have many uses, such as toxicity reducing agents when administered with many antineoplastic agents.
摘要翻译：本发明涉及终止于巯基部分或二硫化物的物质的新组合物。化合物还包括末端磺酸盐或膦酸盐部分，并且当与许多抗肿瘤剂一起施用时具有许多用途，例如毒性降低剂。

2. 发明授权

US5880133A Pharmaceutical formulations of highly lipophilic camptothecin derivatives 失效
标题翻译：高亲脂性喜树碱衍生物的药物制剂
公开(公告)号：US5880133A
公开(公告)日：1999-03-09
申请号：US667424
申请日：1996-06-21
申请人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy
发明人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy
IPC分类号： A61K9/08 , A61K9/00 , A61K9/107 , A61K9/48 , A61K31/4745 , A61K31/475 , A61K47/00 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/28
CPC分类号： A61K9/0019 , A61K31/4745 , A61K47/18 , A61K47/22 , A61K9/1075 , A61K9/4858 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/28
摘要： Pharmaceutical formulations of Highly Lipophilic Camptothecin Derivatives (HLCD) include HLCD dissolved in N-methyl Pyrrolidinene (NMP). The formulations also include quantities of pharmaceutically acceptable excipients and diluents incorporated thereinto.
摘要翻译：高亲脂性喜树碱衍生物（HLCD）的药物制剂包括溶解在N-甲基吡咯烷（NMP）中的HLCD。制剂还包括并入其中的药学上可接受的赋形剂和稀释剂的量。

3. 发明授权

US5789000A Sterile aqueous parenteral formulations of cis-diammine dichloro platinum 失效
标题翻译：顺式二氨基二氯铂无菌水性肠胃外制剂
公开(公告)号：US5789000A
公开(公告)日：1998-08-04
申请号：US338379
申请日：1994-11-14
申请人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy , Peddaiahgari Seetharamulu
发明人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy , Peddaiahgari Seetharamulu
IPC分类号： A61K9/08 , A61K9/107 , A61K31/185 , A61K31/255 , A61K31/28 , A61K31/40 , A61K31/505 , A61K33/24 , A61K45/06 , A61P35/00 , A61P43/00 , A61K31/44
CPC分类号： A61K31/505 , A61K31/185 , A61K31/255 , A61K31/28 , A61K31/40 , A61K33/24 , A61K45/06
摘要： This invention describes a novel formulation containing both cis-diammine dichloro platinum and a water soluble disulfide, 2,2'-dithio-bis-ethane sulfonate in the same solution, wherein the presence of the disulfide and the parenteral administration of the formulation reduces the risk of cisplatin induced nephrotoxicity when treating human patients with cancer.
摘要翻译：本发明描述了同一溶液中含有顺式二氨基二氯铂和水溶性二硫化物2,2'-二硫代双乙磺酸盐的新型制剂，其中二硫化物的存在和制剂的肠胃外给药减少了治疗癌症患者时顺铂诱导肾毒性的风险。

4. 发明授权

US06169080A Highly lipophilic camptothecin derivatives 失效
标题翻译：高亲脂性喜树碱衍生物
公开(公告)号：US06169080A
公开(公告)日：2001-01-02
申请号：US09022310
申请日：1998-02-11
申请人： Frederick H. Hausheer , Kochat Haridas , P. Seetharamulu , Dasharatha G. Reddy , Shijie Yao , Pavankumar N.V. Petluru , Dhanabalan Murali
发明人： Frederick H. Hausheer , Kochat Haridas , P. Seetharamulu , Dasharatha G. Reddy , Shijie Yao , Pavankumar N.V. Petluru , Dhanabalan Murali
IPC分类号： A61K31475
CPC分类号： C07D491/22 , C07F7/0812
摘要： This invention relates to novel derivatives of camptothecin, and will, particularly to derivatives having a substitution at the C-7 position, or at one of the C-9, C-10, C-11 or C-12 positions, or to disubstituted derivatives having a first substitution at C-7 and a second at one of C-9, C-10, C-11 or C-12. The invention also includes methods of using the compounds as Topoisomerase I inhibitors to treat patients with cancer. The invention also includes pharmaceutical formulations which consist of the novel compounds in solution or suspension with one or more pharmaceutical excipients or dilutes.
摘要翻译：本发明涉及喜树碱的新衍生物，特别涉及在C-7位置或C-9，C-10，C-11或C-12位置取代的衍生物，或二取代在C-7具有第一取代基，C-9，C-10，C-11或C-12之一的衍生物。本发明还包括使用化合物作为拓扑异构酶I抑制剂来治疗癌症患者的方法。本发明还包括由溶液或悬浮液中的新化合物与一种或多种药物赋形剂或稀释剂组成的药物制剂。

5. 发明授权

US6057303A Highly lipophilic Camptothecin derivatives 有权
标题翻译：高亲脂性喜树碱衍生物
公开(公告)号：US6057303A
公开(公告)日：2000-05-02
申请号：US175508
申请日：1998-10-20
申请人： Kochat Haridas , Frederick H. Hausheer
发明人： Kochat Haridas , Frederick H. Hausheer
IPC分类号： C07D491/22 , A61K31/4745 , A61P35/00
CPC分类号： C07D491/22
摘要： Derivatives of Camptothecin are disclosed, particularly derivatives having multiple substitutions at the `A`, `B` and `E` rings thereof. The novel compounds are useful in treating a wide variety of susceptible tumors and are potent inhibitors of Topoisomerase I.
摘要翻译：公开了喜树碱的衍生物，特别是在其“A”，“B”和“E”环上具有多个取代基的衍生物。新型化合物可用于治疗多种易感肿瘤，并且是拓扑异构酶I的有效抑制剂。

6. 发明授权

US5859022A Formulations and compositions of poorly water soluble camptothecin derivatives 失效
公开(公告)号：US5859022A
公开(公告)日：1999-01-12
申请号：US956084
申请日：1997-10-22
申请人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy
发明人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy
IPC分类号： A61K9/08 , A61K9/00 , A61K9/107 , A61K9/48 , A61K31/4745 , A61K31/475 , A61K47/00 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/28 , A01N43/42 , A61K31/44
CPC分类号： A61K9/0019 , A61K31/4745 , A61K47/18 , A61K47/22 , A61K9/1075 , A61K9/4858 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/28
摘要： A- and/or B-ring substituted camptothecin derivatives, which are poorly water soluble (less than 5 micrograms per milliliter of water), are highly lipophilic camptothecin derivatives (HLCD) and are very active against a variety of human cancers. Because of their very poor water solubility, HLCD have not been used to treat human patients with cancer due to the inability to administer sufficient quantities of the HLCD dissolved in a pharmaceutical formulation. This invention overcomes these limitations by teaching novel pharmaceutically acceptable HLCD formulations for the direct administration of HLCD to human patients with cancer. The claimed invention also describes the methods to create solutions of HLCD and antitumor compositions of HLCD to allow the administration of HLCD in sufficient amounts to treat human patients with various types of cancer. This invention is also directed to injectable sterile solutions, antitumor compositions, solutions and suspensions comprising N-methyl-2-pyrrolidinone and a highly lipophilic camptothecin derivative.

7. 发明授权

US5604233A Lactone stable formulation of 7-ethyl camptothecin and methods for uses thereof 失效
标题翻译：内酯稳定配方的7-乙基喜树碱及其应用方法
公开(公告)号：US5604233A
公开(公告)日：1997-02-18
申请号：US234131
申请日：1994-04-28
申请人： Frederick H. Hausheer , Kochat Haridas
发明人： Frederick H. Hausheer , Kochat Haridas
IPC分类号： A61K9/107 , A61K9/48 , A61K31/47 , A61K47/18 , A61K47/26 , A61K31/44
CPC分类号： A61K47/26 , A61K31/47 , A61K47/18 , A61K9/0019 , A61K9/4858 , A61K9/1075
摘要： 7-ethyl camptothecin (ECPT), an active metabolite of the camptothecin analog CPT-11, is poorly soluble in water. Because of its poor water solubility, ECPT has not been directly administered by parenteral or oral routes in human patients for the purpose of inhibiting the growth of cancer cells. There is also unpredictable interpatient variability in the metabolic production of ECPT from CPT-11 which limits the utility of CPT-11. This invention overcomes these limitations by teaching novel pharmaceutically acceptable lactone stable ECPT formulations for the direct administration of ECPT. The claimed invention also describes novel dosages, schedules, and routes of administration of the lactone stable ECPT formulations to patients with various forms of cancer.
摘要翻译：喜树碱喜树碱（ECPT）是喜树碱类似物CPT-11的活性代谢物，难溶于水。由于其水溶性差，ECPT尚未通过肠胃外或口服途径直接施用于人类患者，目的是抑制癌细胞的生长。来自CPT-11的ECPT的代谢生成也存在不可预测的患者间变异，这限制了CPT-11的功效。本发明通过教导用于直接施用ECPT的新型药学上可接受的内酯稳定的ECPT制剂来克服这些限制。所要求保护的发明还描述了具有各种形式的癌症的患者的内酯稳定的ECPT制剂的新型剂量，时间表和途径。

8. 发明授权

US5726181A Formulations and compositions of poorly water soluble camptothecin derivatives 失效
公开(公告)号：US5726181A
公开(公告)日：1998-03-10
申请号：US461385
申请日：1995-06-05
申请人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy
发明人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy
IPC分类号： A61K9/08 , A61K9/00 , A61K9/107 , A61K9/48 , A61K31/4745 , A61K31/475 , A61K47/00 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/28 , A01N43/42 , A61K31/44
CPC分类号： A61K9/0019 , A61K31/4745 , A61K47/18 , A61K47/22 , A61K9/1075 , A61K9/4858 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/28
摘要： A- and/or B-ring substituted camptothecin derivatives, which are poorly water soluble (less than 5 micrograms per milliliter of water), are highly lipophilic camptothecin derivatives (HLCD) and are very active against a variety of human cancers. Because of their very poor water solubility, HLCD have not been used to treat human patients with cancer due to the inability to administer sufficient quantities of the HLCD dissolved in a pharmaceutical formulation. This invention overcomes these limitations by teaching novel pharmaceutically acceptable HLCD formulations for the direct administration of HLCD to human patients with cancer. The claimed invention also describes the methods to create solutions of HLCD and antitumor compositions of HLCD to allow the administration of HLCD in sufficient amounts to treat human patients with various types of cancer. This invention is also directed to injectable sterile solutions, antitumor compositions, solutions and suspensions comprising N-methyl-2-pyrrolidinone and a highly lipophilic camptothecin derivative.

9. 发明授权

US5633260A 11,7 Substituted camptothecin derivatives and formulations of 11,7 substituted camptothecin derivatives and methods for uses thereof 失效
标题翻译： 11,7取代的喜树碱衍生物和11,7取代的喜树碱衍生物的制剂及其用途的方法
公开(公告)号：US5633260A
公开(公告)日：1997-05-27
申请号：US518644
申请日：1995-08-24
申请人： Frederick H. Hausheer , Kochat Haridas
发明人： Frederick H. Hausheer , Kochat Haridas
IPC分类号： A61K9/00 , A61K31/4745 , A61K47/12 , A61K47/26 , A61K47/28 , C07D491/22 , A61K31/475
CPC分类号： C07D491/22 , A61K31/4745 , A61K47/12 , A61K47/26 , A61K47/28 , A61K9/0014 , A61K9/0019
摘要： The novel compounds 11-hydroxy-7-ethyl camptothecin and 11-hydroxy-7-methoxy camptothecin (11,7-HECPT and 11,7-HMCPT) are active anticancer compounds which are poorly soluble in water. Because of their novelty, 11,7-HECPT and 11,7-HMCPT derivatives have not been directly administered by parenteral or oral routes to human subjects as an antitumor composition for the purpose of inhibiting the growth of cancer cells. The claimed compositions are useful as compared to the water soluble camptothecin derivatives, such as CPT-11, in clinical trials. The unpredictable interpatient variability in the metabolic production of an active metabolite from CPT-11 limits the utility of CPT-11. This invention overcomes these limitations by claiming novel pharmaceutically acceptable lactone stable formulations of 11,7-HECPT or 11,7-HMCPT, to directly administer to patients. The present invention also claims 11,7-HECPT and 11,7-HMCPT compositions, the synthesis of 11,7-HECPT or 11,7-HMCPT, the methods of formulation of 11,7-HECPT or 11,7 -HMCPT, and the methods of use of 11,7-HECPT or 11,7-HMCPT. Additionally, the claimed invention is directed to novel dosages, schedules, and routes of administration for both the 11,7-HECPT or 11,7-HMCPT formulations to humans with various forms of cancer. Other embodiments of this invention include isolation methods and methods of synthesis of certain camptothecin derivatives.
摘要翻译：新型化合物11-羟基-7-乙基喜树碱和11-羟基-7-甲氧基喜树碱（11,7-HECPT和11,7-HMCPT）是难溶于水的活性抗癌化合物。由于其新颖性，11,7-HECPT和11,7-HMCPT衍生物没有通过肠胃外或口服途径直接施用于人类受试者作为用于抑制癌细胞生长的抗肿瘤组合物。与临床试验中的水溶性喜树碱衍生物（例如CPT-11）相比，要求保护的组合物是有用的。来自CPT-11的活性代谢物的代谢产生中不可预测的患者间变异性限制了CPT-11的效用。本发明通过要求11,7-HECPT或11,7-HMCPT的新的药学上可接受的内酯稳定制剂来克服这些限制，直接给予患者。本发明还要求11,7-HECPT和11,7-HMCPT组合物，11,7-HECPT或11,7-HMCPT的合成，11,7-HECPT或11,7-HMCPT的制备方法，以及使用11,7-HECPT或11,7-HMCPT的方法。另外，要求保护的发明涉及11,7-HECPT或11,7-HMCPT制剂对具有各种形式癌症的人的新型剂量，时间表和给药途径。本发明的其它实施方案包括合成某些喜树碱衍生物的分离方法和方法。

10. 发明授权

US5597829A Lactone stable formulation of camptothecin and methods for uses thereof 失效
标题翻译：内酯稳定的喜树碱配方及其用途
公开(公告)号：US5597829A
公开(公告)日：1997-01-28
申请号：US240035
申请日：1994-05-09
申请人： Frederick H. Hausheer , Kochat Haridas
发明人： Frederick H. Hausheer , Kochat Haridas
IPC分类号： A61K9/107 , A61K9/48 , A61K31/47 , A61K47/18 , A61K47/26 , A61K31/44
CPC分类号： A61K31/47 , A61K47/18 , A61K47/26 , A61K9/0019 , A61K9/4858 , A61K9/1075
摘要： Camptothecin (CPT) an anticancer drug is poorly soluble in water. This invention overcomes this limitation by teaching novel pharmaceutically acceptable lactone stable CPT formulations for the direct administration of CPT to human subjects with cancer. The claimed invention also describes novel dosages, schedules, and routes of administration of the lactone stable CPT formulations to patients with various forms of cancer.
摘要翻译：喜树碱（CPT）抗癌药物难溶于水。本发明通过教导用于直接向患有癌症的受试者的CPT直接给药的新的药学上可接受的内酯稳定的CPT制剂来克服这个限制。所要求保护的发明还描述了具有各种形式的癌症的患者的内酯稳定CPT制剂的新型剂量，时间表和途径。

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