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11. 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。

12. 发明申请

US20170007561A1 CONTEMPORANEOUS, HETEROGENEOUSLY-ORIENTED, MULTI-TARGETED THERAPEUTIC MODIFICATION AND/OR MODULATION OF DISEASE BY ADMINISTRATION OF SULFUR-CONTAINING, AMINO ACID-SPECIFIC SMALL MOLECULES 审中-公开
公开(公告)号：US20170007561A1
公开(公告)日：2017-01-12
申请号：US14455855
申请日：2014-08-08
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： A61K31/185 , A61K31/517 , A61K31/198 , C07K5/062 , C07K5/083 , C12Q1/34 , A61K38/06 , A61K45/06 , C12Q1/48 , C12Q1/26 , G01N33/50 , C12Q1/28 , A61K31/4545 , A61K38/05
CPC分类号： A61K31/185 , A61K31/198 , A61K31/4545 , A61K31/517 , A61K38/05 , A61K38/06 , A61K45/06 , C07K5/06026 , C07K5/0606 , C07K5/06069 , C07K5/06104 , C07K5/0806 , C07K5/081 , C07K5/0819 , C07K5/1019 , G01N33/57484 , G01N33/6893 , G01N2333/71 , G01N2333/72 , G01N2333/908 , G01N2333/91171 , G01N2333/912 , G01N2333/922 , G01N2800/52 , A61K2300/00
摘要： The present invention discloses and claims novel pharmaceutical compositions, methods, and kits used for the contemporaneous, heterogeneously-oriented, multi-targeted therapeutic modification and/or modulation of cellular metabolic anomalies or other undesirable physiological conditions, including cancer, where the normal cellular biochemical function and/or the expression levels of various proteins/enzymes (i.e., the target molecules) are abnormal and must be modified and/or modulated in order to treat these metabolic anomalies or other undesirable physiological conditions, including cancer. The aforementioned target molecules, by way of non-limiting example, include: anaplastic lymphoma kinase (ALK), mesenchymal epithelial transition (MET) kinase, the receptor tyrosine kinase (ROS1), epidermal growth factor receptor (EGFR), peroxiredoxin (Prx), excision repair cross-complementing protein 1 (ERCC1), insulin growth factor 1 receptor (IGF1R), ribonucleotide reductase (RNR), tubulin, farnesyltransferase, and various other classes of proteins/enzymes. Additionally, the present invention discloses and claims methods and kits for (a) the selection of subjects for treatment; (b) the determination of the most effective medicinal agent(s) to be administered in combination with the administration of the sulfur-containing, amino acid-specific small molecules of the present invention; (c) the dosage of the medicinal agent(s) to be administered; (d) the determination of the length and/or number of treatment cycles; (e) the adjustment of the specific medicinal agent(s) used and the dosage administered during treatment; and/or (f) ascertaining the potential treatment responsiveness of the specific disease to the medicinal agents (s) selected for administration to a subject suffering from one or more types of: (i) cancer or (ii) metabolic anomalies or other undesirable physiological conditions by quantitatively determining the level of the abnormal biochemical activity and/or abnormal expression of any combination of the aforementioned target molecules; by use of quantitative measurement methodologies including, but not limited to: fluorescence in situ hybridization (FISH), nucleic acid microarray analysis, immunohistochemistry (IHC), radioimmunoassay (RIA), quantitative immunofluorescence and/or automated quantitative analysis; ELISA and flow cytometry-based analyses; PCR coupled with MS approaches; mass spectroscopy-based methods; and X-ray crystallography, and other related analytic methodologies.

13. 发明申请

US20160038519A1 ADMINISTRATION OF KARENITECIN FOR THE TREATMENT OF ADVANCED OVARIAN CANCER, INCLUDING CHEMOTHERAPY-RESISTANT AND/OR THE MUCINOUS ADENOCARCINOMA SUB-TYPES 审中-公开
标题翻译：用于治疗先天性OVARIAN癌症的卡荣霉素的治疗，包括抗化学药物和/或MUCNOUS ADENOCARCINOMA亚型
公开(公告)号：US20160038519A1
公开(公告)日：2016-02-11
申请号：US14455847
申请日：2014-08-08
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： A61K31/695 , A61K31/185 , A61K47/48
CPC分类号： A61K31/695 , A61K31/185 , A61K31/4738 , A61K47/6803 , A61K2300/00
摘要： The present invention discloses and claims methods and compositions for the treatment of platinum and/or taxane cancer treating agent-resistant/-refractory sub-populations and/or the mucinous adenocarcinoma sub-type of ovarian cancer subjects with the silicon-containing highly lipophilic camptothecin derivative (HLCD), Karenitecin (also known as BNP1350; cositecan; 7-[(2′-trimethylsilyl)ethyl]-20(S) camptothecin). The administration of Karenitecin by intravenous (i.v.) and/or oral methodologies are also disclosed and claimed. Karenitecin analogues, including but not limited to, Germanium-substituted Karenitecin, Deuterated Karenitecin, and “flipped” E-ring Karenitecin, are disclosed and claimed. In addition, Karenitecin and one or more cancer treating agents administered either concomitantly or in series via oral and/or i.v. means, are also disclosed and claimed. Methods for the administration of Karenitecin to: (i) increase Progression Free Survival (PFS); (ii) increase the platinum-free time interval; (iii) decrease CA-125 marker levels; and (iv) mitigate or prevent chemotherapeutic drug-resistance from developing are disclosed and claimed herein. Methods for the use of Karenitecin to treat advanced solid tumors; refractory or recurrent solid tumors; recurrent malignant glioma; primary malignant glioma; persistent or recurrent epithelial ovarian or primary peritoneal carcinoma; and other identified cancer types are also disclosed and claimed.
摘要翻译：本发明公开并说明用于治疗铂和/或紫杉烷类癌症治疗剂抗性/不利子群和/或具有含硅高亲脂性喜树碱的卵巢癌患者的粘液腺癌亚型的方法和组合物衍生物（HLCD），Karenitecin（也称为BNP1350;丝明甘露; 7 - [（2'-三甲基甲硅烷基）乙基] -20（S）喜树碱）。通过静脉内（i.v.）和/或口服方法管理Karenitecin也被披露和要求保护。包括但不限于锗取代的卡伦替宁，氘代卡伦定和“翻转的”E环Karenitecin的Karenitecin类似物被公开和要求保护。此外，卡尼替替和一种或多种癌症治疗剂通过口服和/或i.v同时或串联施用。手段，也被披露和要求保护。 Karenitecin的治疗方法：（i）增加无进展生存期（PFS）; （ii）增加无铂时间间隔; （iii）降低CA-125标记水平; 本文公开和要求保护（iv）缓解或预防化学治疗耐药性的发展。使用Karenitecin治疗晚期实体瘤的方法; 难治或复发性实体瘤; 复发性恶性胶质瘤; 原发恶性胶质瘤; 持续性或复发性上皮性卵巢癌或原发性腹膜癌; 并且还公开并要求保护其他鉴定的癌症类型。

14. 发明申请

US20120282261A1 Deuterated analogs of (4S)-4-Ethyl-4-hydroxy-11-[2- (trimethylsilyl)ethyl]-1H-pyrano[3', 4':6,7] indolizino [1,2-b]quinoline-3,14(4H, 12H)-dione and methods of use thereof 有权
标题翻译：（4S）-4-乙基-4-羟基-11- [2-（三甲基甲硅烷基）乙基] -1H-吡喃并[3'，4'：6,7]中氮茚并[1,2-b] 3,4（4H，12H） - 二酮及其使用方法
公开(公告)号：US20120282261A1
公开(公告)日：2012-11-08
申请号：US13068244
申请日：2011-05-06
申请人： Xinghai Chen , Qiuli Huang , Harry Kochat , Andrey Malakhov , Frederick H. Hausheer
发明人： Xinghai Chen , Qiuli Huang , Harry Kochat , Andrey Malakhov , Frederick H. Hausheer
IPC分类号： A61K31/695 , A61K31/7064 , A61K31/7076 , A61K33/24 , A61P35/02 , A61K38/43 , A61K39/395 , A61K38/02 , A61P35/00 , A61P35/04 , C07F7/10 , A61K38/22
CPC分类号： C07B59/004 , A61K38/00 , C07F7/0812
摘要： The present invention discloses: (i) two novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (ii) methods of synthesis of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (iii) pharmaceutically-acceptable formulations comprising said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents; and (iv) methods of administration of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof.
摘要翻译：本发明公开了：（i）两种新型氘代Karenitecin？类似物，其药学上可接受的盐和/或衍生物; （ii）合成所述新型氘化Karenitecin®类似物，其药学上可接受的盐和/或衍生物的方法; （iii）药学上可接受的制剂，其包含所述新型氘代Karenitecin？类似物，其药学上可接受的盐，衍生物; 和/或任选的一种或多种另外的化学治疗剂; 和（iv）所述新型氘化Karenitecin®类似物，其药学上可接受的盐，衍生物的给药方法; 和/或任选的一种或多种另外的化学治疗剂给予有需要的受试者。

15. 发明授权

US07829540B2 Compounds and methods for reducing undesired toxicity of chemotherapeutic agents 有权
公开(公告)号：US07829540B2
公开(公告)日：2010-11-09
申请号：US11985244
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.

16. 发明授权

US07829538B2 Compounds and methods for reducing undesired toxicity of chemotherapeutic agents 有权
公开(公告)号：US07829538B2
公开(公告)日：2010-11-09
申请号：US11985242
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.

17. 发明申请

US20080261919A1 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：US20080261919A1
公开(公告)日：2008-10-23
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： A61K31/555 , A61K31/695 , A61K31/7052 , A61K39/395 , A61K9/00 , A61P35/00 , C07F7/10 , C07F7/30
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。

18. 发明授权

US06468993B1 Method for reducing development of osteoporosis 失效
标题翻译：减少骨质疏松症发展的方法
公开(公告)号：US06468993B1
公开(公告)日：2002-10-22
申请号：US09411767
申请日：1999-10-04
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： A61K3166
CPC分类号： A61K31/66 , A61K31/105 , A61K31/255
摘要： This invention relates to a method of treating patients afflicted with osteoporosis. 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骨质疏松症的患者的方法。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。

19. 发明授权

US06194579B1 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：US06194579B1
公开(公告)日：2001-02-27
申请号：US09470773
申请日：1999-12-23
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： C07D51500
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。

20. 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。

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