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1.发明授权
公开(公告)号：US5880133A
公开(公告)日：1999-03-09
申请号：US667424
申请日：1996-06-21
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。
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2.发明授权
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。
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公开(公告)号：US5859022A
公开(公告)日：1999-01-12
申请号：US956084
申请日：1997-10-22
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.
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公开(公告)号：US5726181A
公开(公告)日：1998-03-10
申请号：US461385
申请日：1995-06-05
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.
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5.发明授权Pharmaceutical formulations of poorly water soluble camptothecin analogues and NMP 失效药用配方水溶性差的喜树碱类似物和NMP
公开(公告)号：US5955467A
公开(公告)日：1999-09-21
申请号：US955956
申请日：1997-10-22
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 , 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.
摘要翻译： A-和/或B-环取代的喜树碱衍生物，其水溶性差（小于5微克/毫升水）是高度亲脂性的喜树碱衍生物（HLCD），并且对多种人类癌症非常有活性。 由于水溶性非常差，由于不能施用足够量的溶解在药物制剂中的HLCD，HLCD不能用于治疗癌症患者。 本发明克服了这些限制，通过教导用于将HLCD直接给予癌症患者的HLCD的药学上可接受的HLCD制剂。 所要求保护的发明还描述了创建HLCD和HLCD抗肿瘤组合物的溶液的方法，以允许以足够的量施用HLCD来治疗患有各种类型的癌症的患者。 本发明还涉及可注射的无菌溶液，抗肿瘤组合物，包含N-甲基-2-吡咯烷酮和高亲脂性喜树碱衍生物的溶液和悬浮液。
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公开(公告)号：US5900419A
公开(公告)日：1999-05-04
申请号：US955955
申请日：1997-10-22
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 , A61K31/44 , A01N43/42
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.
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公开(公告)号：US5958937A
公开(公告)日：1999-09-28
申请号：US955947
申请日：1997-10-22
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 , 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.
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8.发明授权
公开(公告)号：US5935967A
公开(公告)日：1999-08-10
申请号：US9067
申请日：1998-01-20
IPC分类号： A61K9/107 , A61K31/4745 , A61K47/00 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/28 , A61K31/475
CPC分类号： A61K47/22 , A61K31/4745 , A61K47/18 , A61K9/1075 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/28
摘要： Pharmaceutical formulations of highly lipophilic, poorly water soluble derivatives of Camptothecin are disclosed. The formulations include an effective amount of the HLCD dissolved or suspended in an appropriate amount of N-methyl-2-pyrrolidinone (NMP), and one or more pharmaceutically acceptable excipients.
摘要翻译： 公开了高亲脂性，水溶性差的喜树碱衍生物的药物制剂。 制剂包括溶解或悬浮在适量N-甲基-2-吡咯烷酮（NMP）中的有效量的HLCD和一种或多种药用赋形剂。
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9.发明授权
公开(公告)号：US5859023A
公开(公告)日：1999-01-12
申请号：US958210
申请日：1997-10-22
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.
摘要翻译： A-和/或B-环取代的喜树碱衍生物，其水溶性差（小于5微克/毫升水）是高度亲脂性的喜树碱衍生物（HLCD），并且对多种人类癌症非常有活性。 由于水溶性非常差，由于不能施用足够量的溶解在药物制剂中的HLCD，HLCD不能用于治疗癌症患者。 本发明克服了这些限制，通过教导用于将HLCD直接给予癌症患者的HLCD的药学上可接受的HLCD制剂。 所要求保护的发明还描述了创建HLCD和HLCD抗肿瘤组合物的溶液的方法，以允许以足够的量施用HLCD来治疗患有各种类型的癌症的患者。 本发明还涉及可注射的无菌溶液，抗肿瘤组合物，包含N-甲基-2-吡咯烷酮和高亲脂性喜树碱衍生物的溶液和悬浮液。
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公开(公告)号：US5866615A
公开(公告)日：1999-02-02
申请号：US848361
申请日：1997-04-30
申请人： Frederick Herman Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy , Seetharamulu Peddaiahgari
发明人： Frederick Herman Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy , Seetharamulu Peddaiahgari
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 , A61K47/20
CPC分类号： A61K31/505 , A61K31/185 , A61K31/255 , A61K31/28 , A61K31/40 , A61K33/24 , A61K45/06
摘要： This invention describes novel formulations containing a water soluble disulfide, 2,2'-dithio-bis-ethane sulfonate, with or without cis-diammine dichloro platinum present in the same formulation, wherein the parenteral or oral administration of 2,2'-dithio-bis-ethane sulfonate is used to reduce the risk or prevent or retard the development of cisplatin induced nephrotoxicity, myelosuppression, and neurotoxicity, and wherein the parenteral or oral administration of 2,2'-dithio-bis-ethane sulfonate potentiates the antitumor activity of cisplatin when treating human patients with cancer. This invention also teaches novel formulations containing 2,2'-dithio-bis-ethane sulfonate alone or in combination with cisplatin in lyophilized or dissolved in an aqueous formulations which can be administered to patients with cancer who are being treated with cisplatin. The invention also teaches methods of preparing said formulations and their use in preventing cisplatin related toxicities and potentiation of cisplatin antitumor activity.
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