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51. 发明授权

US6028078A 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：US6028078A
公开(公告)日：2000-02-22
申请号：US178780
申请日：1998-10-26
申请人： Frederick H. Hausheer , Pavankumar N. V. Petluru , Dasharatha Reddy , Dhanabalan Murali , Kochat Haridas , Peddaiahgari Seetharamulu , Shijie Yao
发明人： Frederick H. Hausheer , Pavankumar N. V. Petluru , Dasharatha Reddy , Dhanabalan Murali , Kochat Haridas , Peddaiahgari Seetharamulu , Shijie Yao
IPC分类号： A61K31/4745 , A61P35/00 , C07D491/22 , C07D515/00 , C07F7/10 , A61K31/475
CPC分类号： C07D491/22 , Y02P20/55
摘要： Novel compounds, formulations and methods of treating patients with cancer are provided for in this invention. The compounds are derivatives of camptothecin, and specifically relate to compounds having novel substitutions at the C-7 position of the camptothecin scaffold B-ring. The formula I compounds are highly lipophilic, lactone stable, do not require metabolic activation, and are potent antineoplastic compounds.
摘要翻译：在本发明中提供了治疗癌症患者的新型化合物，制剂和方法。化合物是喜树碱的衍生物，具体涉及在喜树碱骨架B-环C-7位上具有新取代基的化合物。式I化合物是高亲脂性的，内酯稳定的，不需要代谢活化，并且是有效的抗肿瘤化合物。

52. 发明授权

US5955467A Pharmaceutical formulations of poorly water soluble camptothecin analogues and NMP 失效
标题翻译：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
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 , 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。

53. 发明授权

US5900419A Formulations and compositions of poorly water soluble camptothecin derivatives 失效
公开(公告)号：US5900419A
公开(公告)日：1999-05-04
申请号：US955955
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 , 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.

54. 发明授权

US5214134A Process of linking nucleosides with a siloxane bridge 失效
标题翻译：用硅氧烷桥连接核苷酸的方法
公开(公告)号：US5214134A
公开(公告)日：1993-05-25
申请号：US581502
申请日：1990-09-12
申请人： Alexander L. Weis , Ashis K. Saha , Frederick H. Hausheer
发明人： Alexander L. Weis , Ashis K. Saha , Frederick H. Hausheer
IPC分类号： C07H20060101 , C07H23/00
CPC分类号： C07H23/00
摘要： A method of linking nucleosides with a siloxane bridge comprising reacting a 3'-silylated-5'-protected nucleoside with an unprotected nucleoside is disclosed. The silylated and unprotected nucleosides may be either monomeric nucleosides or the terminal nucleosides of an oligonucleotide or oligonucleotide analog. A method of synthesizing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed. The method of synthesis comprises silylating a 5'-protected nucleoside with a bifunctional silylating reagent to form a 3'-silylated nucleoside, reacting the silylated nucleoside with an unprotected nucleoside in the presence of a base catalyst and repeating these steps to form an oligonucleotide analog. A modified solid phase synthesis method for preparing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed.
摘要翻译：公开了将核苷与硅氧烷桥连接的方法，包括使3'-甲硅烷基化-5'-保护的核苷与未保护的核苷反应。甲硅烷基化和未保护的核苷可以是单体核苷或寡核苷酸或寡核苷酸类似物的末端核苷。还公开了合成具有硅氧烷核苷间键的寡核苷酸类似物的方法。合成方法包括用双官能甲硅烷基化试剂甲硅烷基化5'-保护的核苷以形成3'-甲硅烷基化核苷，在碱催化剂存在下使甲硅烷基化的核苷与未保护的核苷反应，并重复这些步骤以形成寡核苷酸类似物。还公开了用于制备具有硅氧烷核苷间键的寡核苷酸类似物的改进的固相合成方法。

55. 发明授权

US07687487B2 Camptothecin-analog with a novel, “flipped” lactone-stable, E-ring and methods for making and using same 有权
标题翻译：喜树碱类似物具有新颖的“翻转”内酯稳定性，E型环及其制备和使用方法
公开(公告)号：US07687487B2
公开(公告)日：2010-03-30
申请号：US11788223
申请日：2007-04-19
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： A61K31/33 , C07D491/22
CPC分类号： A61K9/4858 , A61K9/0019 , A61K9/0024 , A61K9/08 , A61K9/1075 , A61K9/127 , A61K9/1275 , A61K31/555 , A61K31/695 , A61K31/7052 , A61K47/12 , A61K47/28
摘要： The present invention discloses: (i) a novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (ii) methods of synthesis of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (iii) pharmaceutically-acceptable formulations comprising said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents; (iv) methods of administration of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof; and (v) devices for the administration of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more chemotherapeutic agents, to subjects in need thereof.
摘要翻译：本发明公开：（i）一种新颖的内酯稳定的“翻转的”E环喜树碱，其药学上可接受的盐和/或类似物; （ii）合成所述新型内酯稳定的“翻转”E-环喜树碱，其药学上可接受的盐和/或类似物的方法; （iii）包含所述新型内酯稳定的“翻转”E环喜树碱，其药学上可接受的盐和/或类似物，以及任选的一种或多种另外的化学治疗剂的药学上可接受的制剂; （iv）向有需要的受试者施用所述新型内酯稳定的“翻转的”E环喜树碱，其药学上可接受的盐和/或类似物，以及任选的一种或多种另外的化学治疗剂的方法; 和（v）用于将所述新型内酯稳定的“翻转的”E环喜树碱，其药学上可接受的盐和/或类似物以及任选的一种或多种化学治疗剂施用给有需要的受试者的装置。

56. 发明申请

US20090232906A1 Treatment methods and compositions for lung cancer, adenocarcinoma, and other medical conditions 审中-公开
标题翻译：肺癌，腺癌和其他医疗条件的治疗方法和组合物
公开(公告)号：US20090232906A1
公开(公告)日：2009-09-17
申请号：US12075980
申请日：2008-03-14
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： A61K33/24 , A61K31/185 , A61P35/00
CPC分类号： A61K45/06 , A61K31/185 , A61K31/555 , A61K33/24 , A61K2300/00
摘要： The present invention discloses and claims: (i) compositions, methods, and kits which lead to an increase in patient survival time in cancer patients receiving chemotherapy; (ii) compositions and methods which cause cytotoxic or apoptotic potentiation of the anti-cancer activity of chemotherapeutic agents; (iii) compositions and methods for maintaining or stimulating hematological function in patients in need thereof, including those patients suffering from cancer; (iv) compositions and methods for maintaining or stimulating erythropoietin function or synthesis in patients in need thereof, including those patients suffering from cancer; (v) compositions and methods for mitigating or preventing anemia in patients in need thereof, including those patients suffering from cancer; (vi) compositions and methods for maintaining or stimulating pluripotent, multipotent, and unipotent normal stem cell function or synthesis in patients in need thereof, including those patients suffering from cancer; (vii) compositions and methods which promote the arrest or retardation of tumor progression in those cancer patients receiving chemotherapy; (viii) compositions and methods for increasing patient survival and/or delaying tumor progression while maintaining or improving the quality of life in a cancer patient receiving chemotherapy; (ix) novel methods of the administration of taxane and/or platinum medicaments and a Formula (I) compound of the present invention to a cancer patient; and (x) kits to achieve one or more of the aforementioned physiological effects in a patient in need thereof, including those patients suffering from cancer.
摘要翻译：本发明公开并要求：（i）导致接受化疗的癌症患者的患者存活时间增加的组合物，方法和试剂盒; （ii）引起化学治疗剂的抗癌活性的细胞毒性或凋亡增强作用的组合物和方法; （iii）用于维持或刺激有需要的患者血液功能的组合物和方法，包括患有癌症的患者; （iv）维持或刺激有需要的患者的促红细胞生成素功能或合成的组合物和方法，包括患有癌症的患者; （v）减轻或预防有需要的患者的贫血的组合物和方法，包括患有癌症的患者; （vi）用于在有需要的患者（包括患有癌症的患者）中维持或刺激多能，多能和单能正常干细胞功能或合成的组合物和方法; （vii）促进在接受化疗的那些癌症患者中阻滞或延缓肿瘤进展的组合物和方法; （viii）用于在维持或改善接受化疗的癌症患者的生活质量的同时增加患者存活和/或延缓肿瘤进展的组合物和方法; （ix）向癌症患者施用紫杉烷和/或铂药物和本发明式（I）化合物的新方法; 和（x）用于在有需要的患者中实现一种或多种上述生理作用的试剂盒，包括患有癌症的患者。

57. 发明授权

US06468963B1 Methods and formulations for reducing toxicity associated with diabetes treatments 有权
标题翻译：减少与糖尿病治疗有关的毒性的方法和制剂
公开(公告)号：US06468963B1
公开(公告)日：2002-10-22
申请号：US09562160
申请日：2000-05-01
申请人： Frederick H. Hausheer , Aulma Parker , Susan E. Hamilton
发明人： Frederick H. Hausheer , Aulma Parker , Susan E. Hamilton
IPC分类号： A61K31155
CPC分类号： A61K31/662 , A61K31/155 , A61K31/185 , A61K38/26 , A61K38/28 , A61K2300/00
摘要： Formulations and methods for reducing the unwanted toxicity and complications associated with treatments for diabetes mellitus. The formulations include co-formulations of an anti-diabetic agent and a toxicity reducing agent of the formula described in the specification. The methods include administration of effective amounts of the anti-diabetic agent and the toxicity reducing agent to safely treat the diabetic patient.
摘要翻译：用于减少与糖尿病治疗相关的不想要的毒性和并发症的制剂和方法。该制剂包括说明书中描述的抗糖尿病药物和毒性降低剂的配制剂。所述方法包括施用有效量的抗糖尿病药和毒性降低剂以安全治疗糖尿病患者。

58. 发明授权

US6143796A Method for reducing development of free radical induced malignancies 有权
标题翻译：减少自由基诱发恶性肿瘤发展的方法
公开(公告)号：US6143796A
公开(公告)日：2000-11-07
申请号：US389520
申请日：1999-09-02
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： A61K31/105 , A61K31/185 , A61K31/66 , A01N41/12
CPC分类号： A61K31/185 , A61K31/105 , A61K31/66
摘要： This invention relates to a method of treating patients at risk of developing a free radical induced malignancy. The method includes administering an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification to a patient at risk.
摘要翻译：本发明涉及治疗患有自由基诱发恶性肿瘤风险的患者的方法。该方法包括将有效量的硫醇或可还原的二硫化物化合物按照说明书中给出的公式给予处于危险中的患者。

59. 发明授权

US06100247A Method of treating diabetic neuropathy 有权
标题翻译：治疗糖尿病性神经病变的方法
公开(公告)号：US06100247A
公开(公告)日：2000-08-08
申请号：US422485
申请日：1999-10-21
申请人： Frederick H. Hausheer , Aulma Parker , Seetharamulu Peddaiaghari
发明人： Frederick H. Hausheer , Aulma Parker , Seetharamulu Peddaiaghari
IPC分类号： A61K31/185 , A61K31/10
CPC分类号： A61K31/185
摘要： This invention relates to a method of treating patients afflicted with diabetic neuropathy. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.
摘要翻译：本发明涉及治疗患有糖尿病性神经病变的患者的方法。该方法包括向需要治疗的患者施用有效量的根据说明书中阐述的式的硫醇或可还原的二硫化物化合物。

60. 发明授权

US6037336A Reducing toxic effects of carboplatin using dithioethers 有权
标题翻译：使用二硫醚减少卡铂的毒性作用
公开(公告)号：US6037336A
公开(公告)日：2000-03-14
申请号：US269360
申请日：1999-05-10
申请人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Seetharamulu Peddaiahgari , Dasharatha G. Reddy
发明人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Seetharamulu Peddaiahgari , Dasharatha G. Reddy
IPC分类号： A01N51/00 , A61K31/66 , A61K31/185 , A61K31/28
CPC分类号： A01N51/00
摘要： To reduce the toxic effect of carboplatin, particularly myelosuppression and emesis, a dithioether having the formula R.sub.1 -(CH.sub.2).sub.n --S--S--(CH.sub.2).sub.m --R.sub.2 (I) wherein:each of R.sub.1 and R.sub.2 individually is SO.sub.3 H or PO.sub.3 H.sub.2 ; andeach of m and n is individually 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof, preferably disodium 2,2'-dithiobis(ethane sulfonate) (dimesna), is administered in combination with carboplatin to a patient, at substantially the same time or sequentially, whereby the dithioether and the carboplatin become co-present in the blood of the patient. Compositions comprising carboplatin and the dithioether are included in the invention.
摘要翻译： PCT No.PCT / GB97 / 02582 Sec。 371日期1999年5月10日 102（e）1999年5月10日PCT PCT 1997年9月23日PCT公布。公开号WO98 / 11898 1998年3月26日为了降低卡铂的毒性作用，特别是骨髓抑制和呕吐，具有式R1-（CH2）nSS-（CH2）m-R2（I）的二硫醚其中：R1和R2各自分别是SO3H或 PO3H2; m和n分别为1,2,3或4; 或其药学上可接受的盐，优选2,2'-二硫代双（乙磺酸）二钠（dimesna）与卡铂组合施用于患者，基本上相同或相继，由此二硫醚和卡铂变成共存在于患者的血液中。包含卡铂和二硫醚的组合物包括在本发明中。

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