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1. 发明申请

WO2004035032A3 PHARMACEUTICAL FORMULATIONS OF CAMPTOTHECINE DERIVATIVES 审中-公开
公开(公告)号：WO2004035032A3
公开(公告)日：2004-04-29
申请号：PCT/US2003/025825
申请日：2003-08-15
申请人： NEOPHARM, INC. , AHMAD, Imran , ZHANG, Jia-Ai
发明人： AHMAD, Imran , ZHANG, Jia-Ai
IPC分类号： A61K9/127
摘要： SN38, camptothecin derivatives are poorly water soluble, highly lipophilic camptothecin derivatives and are very active against a variety of human cancers. Because of their very poor water solubility, SN38 has not been used to treat human patients with cancer due to the inability to administer sufficient quantities of dissolved in a pharmaceutical formulation. This invention overcomes these limitations by teaching novel pharmaceutically acceptable SN38 liposome complex formulation for the direct administration of the formulation to human patients with cancer. The claimed invention also describes the methods to prepare liposomal SN 38 complexes to allow the administration in sufficient amounts to treat various types of cancer. This invention is also directed to injectable sterile solutions, antitumor compositions, liposomes. The present invention is for novel compositions and methods for treating diseases caused by cellular proliferation, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include SN38 lipid complexes in which the complexes can contain any of a variety of neutral or charged lipids and, desirably, cardiolipin. The compositions are capable of efficiently incorporating SN38 into complexes and are capable of solubilizing relatively high concentrations of SN38.

2. 发明申请

WO2006102533A3 PHARMACEUTICALLY ACTIVE LIPID-BASED FORMULATION OF NUCLEOSIDE-LIPID CONJUGATES 审中-公开
公开(公告)号：WO2006102533A3
公开(公告)日：2006-09-28
申请号：PCT/US2006/010638
申请日：2006-03-23
申请人： NEOPHARM, INC. , ZHANG, Jia-Ai , UGWU, Sydney , MA, Lan , AHMAD, Moghis, U. , ALI, Shoukath, M. , KHAN, Abdul, R. , AHMAD, Imran
发明人： ZHANG, Jia-Ai , UGWU, Sydney , MA, Lan , AHMAD, Moghis, U. , ALI, Shoukath, M. , KHAN, Abdul, R. , AHMAD, Imran
IPC分类号： A01N43/04 , A61K31/70
摘要： Novel formulations of nucleoside-lipid conjugates, the methods of preparing them and the methods for administering them are provided. More particularly, methods for making liposomal formulations of nucleoside-cardiolipin and analogues thereof are provided. By encapsulating nucleoside prodrugs, drugs are protected from degradation, thereby extending the drugs' plasma half-life and intracellular release. In addition, compositions that demonstrate greater efficacy and higher cytotoxicity are produced. Accordingly, nucleoside-lipid conjugates that demonstrate greater in-vitro and in-vivo activity are produced.

3. 发明申请

WO2004069224A2 STABLE STERILE FILTERABLE LIPOSOMAL ENCAPSULATED TAXANE AND OTHER ANTINEOPLASTIC DRUGS 审中-公开
标题翻译：稳定的无菌滤过性脂质体包封的紫杉醇和其他抗肿瘤药物
公开(公告)号：WO2004069224A2
公开(公告)日：2004-08-19
申请号：PCT/US2004/003157
申请日：2004-02-03
申请人： NEOPHARM, INC. , ZHANG, Jia-Ai , UGWU, Sydney , MA, Lan , ANYARAMBHATLA, Gopal , AHMAD, Imran
发明人： ZHANG, Jia-Ai , UGWU, Sydney , MA, Lan , ANYARAMBHATLA, Gopal , AHMAD, Imran
IPC分类号： A61K9/127
CPC分类号： A61K9/127 , A61K9/1272 , A61K9/19 , A61K31/337
摘要： The invention provides a formulation of one or more antineoplastic drugs encapsulated in liposomes including at least a lipid fraction in addition to the antineoplastic drug, wherein the composition is stable in an aqueous solution at room temperature.
摘要翻译：本发明提供了包封在脂质体中的一种或多种抗肿瘤药物的制剂，所述脂质体除抗肿瘤药物外还包含至少一种脂质部分，其中所述组合物在室温下在水溶液中稳定。 p>

4. 发明申请

WO2004017940A2 PHARMACEUTICALLY ACTIVE LIPID BASED FORMULATION OF SN38 审中-公开
标题翻译：药物活性脂质基制剂SN38
公开(公告)号：WO2004017940A2
公开(公告)日：2004-03-04
申请号：PCT/US2003/025880
申请日：2003-08-19
申请人： NEOPHARM, INC. , AHMAD, Imran , ZHANG, Jia-Ai
发明人： AHMAD, Imran , ZHANG, Jia-Ai
IPC分类号： A61K9/00
CPC分类号： A61K9/127 , A61K31/4745
摘要： SN38, camptothecin derivatives are poorly water soluble, highly lipophilic camptothecin derivatives and are very active against a variety of human cancers. Because of their very poor water solubility, SN38 has not been used to treat human patients with cancer due to the inability to administer sufficient quantities of dissolved in a pharmaceutical formulation. This invention overcomes these limitations by teaching novel pharmaceutical acceptable SN38 liposome complex formulation for the direct administration of the formulation to human patients with cancer. The claimed invention also describes the methods to prepare liposomal SN38 complexes and antitumor compositions of liposomal SN38 complexes to allow the administration in sufficient amounts to treat various types of cancer and as antiviral agents. This invention is also directed to injectable sterile solutions, antitumor compositions, liposomes. The present invention is for novel compositions and methods for treating diseases caused by cellular proliferation, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include SN38 lipid complexes in which the complexes can contain any of a variety of neutral or charged lipids and, desirably, cardiolipin. The compositions are capable of efficiently incorporating SN38 into complexes and are capable of solubilizing relatively high concentrations of SN38.
摘要翻译： SN38，喜树碱衍生物水溶性差，高度亲脂性喜树碱衍生物，并且对多种人类癌症非常有活性。由于它们的水溶性非常差，SN38尚未用于治疗患有癌症的人类患者，因为无法施用足量的药物制剂溶解。本发明通过教导新的药学上可接受的SN38脂质体复合物制剂以将制剂直接施用于患有癌症的人类患者来克服这些限制。要求保护的发明还描述了制备脂质体SN38复合物和脂质体SN38复合物的抗肿瘤组合物以允许以足够量施用以治疗各种类型的癌症和作为抗病毒剂的方法。本发明还涉及可注射的无菌溶液，抗肿瘤组合物，脂质体。本发明是用于治疗由细胞增殖引起的疾病的新组合物和方法，特别是用于治疗哺乳动物，更特别是人类的癌症。本发明的治疗组合物包括SN38脂质复合物，其中复合物可以含有各种中性或带电脂质中的任何一种，并且理想地为心磷脂。该组合物能够有效地将SN38掺入复合物并能够溶解较高浓度的SN38。

5. 发明申请

WO2005067632A2 LIPID COMPOSITIONS AND USE THEREOF 审中-公开
标题翻译：脂肪组合物及其用途
公开(公告)号：WO2005067632A2
公开(公告)日：2005-07-28
申请号：PCT/US2005/000418
申请日：2005-01-07
申请人： NEOPHARM, INC. , AHMAD, Moghis U. , SHEIKH, Saifuddin , ALI, Shoukath , CHIEN, Pei-Yu , JAMIL, Haris , ZHANG, Jia-Ai , UGWU, Sydney , ZHANG, Zhi-Yi , WANG, Jinkang , BHAMIDIPATI, Shastri , AHMAD, Zafeer , AHMAD, Imran
发明人： AHMAD, Moghis U. , SHEIKH, Saifuddin , ALI, Shoukath , CHIEN, Pei-Yu , JAMIL, Haris , ZHANG, Jia-Ai , UGWU, Sydney , ZHANG, Zhi-Yi , WANG, Jinkang , BHAMIDIPATI, Shastri , AHMAD, Zafeer , AHMAD, Imran
IPC分类号： A61K9/127 , A61K31/14 , A61K31/355 , A61K31/575 , A61K31/685 , A61K31/7088 , A61K31/7105 , A61K31/711 , A61K45/06 , A61K48/00 , C12N15/11 , C12N15/113
CPC分类号： A61K31/14 , A61K9/1272 , A61K31/355 , A61K31/575 , A61K31/685 , A61K31/7088 , A61K31/7105 , A61K31/711 , A61K45/06 , A61K48/0025 , A61K48/0041 , C12N15/111 , C12N15/1135 , C12N2310/11 , C12N2310/14 , C12N2320/32 , A61K2300/00
摘要： The invention provides a composition suitable for use as a transfection agent, comprising a cationic cardiolipin analogue and, another lipid species. The composition of the present invention can facilitate transfection of a wide variety of polynucleotide species (e.g., oligodeoxyribonucleotides, plasmids, RNAi species, etc.). Moreover, the transfection agent of the present invention is effective in promoting transfection of primary cell cultures as well as transformed cells. Also, the inventive transfection agent is suitable for use both in vitro and in vivo . The inventive composition has additional uses as well, such as delivery of a variety of active agents, dermatological and cosmetic uses, and uses in agriculture. The invention further provides a method of introducing an active agent into a cell by contacting the cell with the inventive composition. The invention further provides a method of inhibiting the growth of neoplastic cells and a method of treating a patient suffering from a neoplastic disease by employing the inventive composition, wherein an active agent is an antineoplastic agent. The invention further provides a method for validating a genetic target, comprising (a) administering to a cell a composition comprising a cationic liposome and a siRNA, whereby the siRNA enters the cell inhibits the expression of a gene within the cell and (b) assaying for the inhibition of the gene. The method also provides a fluorescent/ luminescent cationic cardiolipin analogue and compositions including such analogues. Using a cationic cardiolipin analogue, the invention provides a method of tracking the migration of a lipid substance within an animal.
摘要翻译：本发明提供适合用作转染剂的组合物，其包含阳离子心磷脂类似物和另一种脂质物质。本发明的组合物可以促进多种多样性物质（例如，寡脱氧核糖核苷酸，质粒，RNAi物种等）的转染。此外，本发明的转染剂有效促进原代细胞培养物以及转化细胞的转染。此外，本发明的转染剂适用于体外和体内。本发明的组合物也具有额外的用途，例如递送各种活性剂，皮肤病学和美容用途以及农业中的用途。本发明还提供了通过使细胞与本发明组合物接触将活性剂引入细胞的方法。本发明进一步提供抑制肿瘤细胞生长的方法和通过使用本发明组合物治疗患有肿瘤疾病的患者的方法，其中活性剂是抗肿瘤剂。本发明还提供了一种用于验证遗传靶标的方法，包括（a）向细胞施用包含阳离子脂质体和siRNA的组合物，由此siRNA进入细胞抑制细胞内基因的表达，（b）测定用于抑制基因。该方法还提供荧光/发光阳离子心磷脂类似物和包含这些类似物的组合物。使用阳离子心磷脂类似物，本发明提供了跟踪动物体内脂质的迁移的方法。

6. 发明申请

WO2004017944A1 LIPOSOMAL GEMCITABINE COMPOSITIONS FOR BETTER DRUG DELIVERY 审中-公开
标题翻译：用于更好的药物递送的组织化学药物组合物
公开(公告)号：WO2004017944A1
公开(公告)日：2004-03-04
申请号：PCT/US2003/025293
申请日：2003-08-13
申请人： NEOPHARM, INC. , ZHANG, Jia-Ai , AHMAD, Imran
发明人： ZHANG, Jia-Ai , AHMAD, Imran
IPC分类号： A61K9/127
CPC分类号： A61K45/06 , A61K9/127 , A61K9/1272 , A61K31/66 , A61K31/7068 , A61K31/7072 , A61K2300/00
摘要： The present invention is for novel compositions and methods for treating cancer, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include liposome entrapped gemcitabine in which the liposome can contain any of a variety of neutral or charged liposome-forming compounds including cardiolipin.
摘要翻译：本发明是用于治疗癌症的新型组合物和方法，特别是用于治疗哺乳动物，特别是人类的癌症。本发明的治疗组合物包括脂质体包埋的吉西他滨，其中脂质体可以含有多种中性或带电荷的脂质体形成化合物，包括心磷脂。

7. 发明申请

WO2003018018A2 VINORELBINE COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译： VINORELINE组合物和使用方法
公开(公告)号：WO2003018018A2
公开(公告)日：2003-03-06
申请号：PCT/US2002/026907
申请日：2002-08-23
申请人： NEOPHARM, INC. , ZHANG, Jia-Ai , AHMAD, Imran
发明人： ZHANG, Jia-Ai , AHMAD, Imran
IPC分类号： A61K31/475
CPC分类号： A61K45/06 , A61K9/127 , A61K31/4745 , A61K31/475 , A61K2300/00
摘要： The present invention is for novel compositions and methods for treating cancer, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include liposome entrapped vinorelbine in which the liposome can contain any of a variety of neutral or charged liposome-forming compounds and cardiolipin. The liposomes of the present invention can be either multilamellar vesicles or unilamellar vesicles, as desired.
摘要翻译：本发明是用于治疗癌症，特别是用于治疗哺乳动物，更特别是治疗人类癌症的新型组合物和方法。本发明的治疗组合物包括脂质体包埋的长春瑞滨，其中脂质体可以含有多种中性或带电脂质体形成化合物和心磷脂中的任何一种。根据需要，本发明的脂质体可以是多层囊泡或单层囊泡。

8. 发明申请

WO2014136079A1 ORAL FORMULATIONS OF DEFERASIROX 审中-公开
标题翻译： DEFERASIROX的口服制剂
公开(公告)号：WO2014136079A1
公开(公告)日：2014-09-12
申请号：PCT/IB2014/059494
申请日：2014-03-06
申请人： NOVARTIS AG , GHOSH, Indrajit , ZHANG, Jia-Ai
发明人： GHOSH, Indrajit , ZHANG, Jia-Ai
IPC分类号： A61K9/20 , A61K9/28 , A61K9/50 , A61K31/4196 , A61P39/04
CPC分类号： A61K31/4196 , A61K9/0053 , A61K9/148 , A61K9/2013 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2077 , A61K9/2095 , A61K9/2846 , A61K9/2886 , A61K9/2893 , A61K9/5026 , A61K9/5089 , A61K31/125
摘要： Orally administerable deferasirox formulations are disclosed having reduced release under gastric conditions and fast release at near neutral pH or at neutral pH.
摘要翻译：本发明公开了口服给药的去铁调脂素配方，其在胃液条件下具有减少的释放，并在接近中性pH或中性pH下快速释放。

9. 发明公开

EP1742661A2 LIPID COMPOSITIONS AND USE THEREOF 审中-公开
标题翻译：脂质成分及其用途
公开(公告)号：EP1742661A2
公开(公告)日：2007-01-17
申请号：EP05705189.8
申请日：2005-01-07
申请人： Neopharm, Inc.
发明人： AHMAD, Moghis U. , SHEIKH, Saifuddin , ALI, Shoukath , CHIEN, Pei-Yu , JAMIL, Haris , ZHANG, Jia-Ai , UGWU, Sydney , ZHANG, Zhi-Yi , WANG, Jinkang , BHAMIDIPATI, Shastri , AHMAD, Zafeer , AHMAD, Imran
IPC分类号： A61K45/06
CPC分类号： A61K31/14 , A61K9/1272 , A61K31/355 , A61K31/575 , A61K31/685 , A61K31/7088 , A61K31/7105 , A61K31/711 , A61K45/06 , A61K48/0025 , A61K48/0041 , C12N15/111 , C12N15/1135 , C12N2310/11 , C12N2310/14 , C12N2320/32 , A61K2300/00
摘要： The invention provides a composition suitable for use as a transfection agent, comprising a cationic cardiolipin analogue and, another lipid species. The composition of the present invention can facilitate transfection of a wide variety of polynucleotide species (e.g., oligodeoxyribonucleotides, plasmids, RNAi species, etc.). Moreover, the transfection agent of the present invention is effective in promoting transfection of primary cell cultures as well as transformed cells. Also, the inventive transfection agent is suitable for use both in vitro and in vivo. The inventive composition has additional uses as well, such as delivery of a variety of active agents, dermatological and cosmetic uses, and uses in agriculture. The invention further provides a method of introducing an active agent into a cell by contacting the cell with the inventive composition. The invention further provides a method of inhibiting the growth of neoplastic cells and a method of treating a patient suffering from a neoplastic disease by employing the inventive composition, wherein an active agent is an antineoplastic agent. The invention further provides a method for validating a genetic target, comprising (a) administering to a cell a composition comprising a cationic liposome and a siRNA, whereby the siRNA enters the cell inhibits the expression of a gene within the cell and (b) assaying for the inhibition of the gene. The method also provides a fluorescent/ luminescent cationic cardiolipin analogue and compositions including such analogues. Using a cationic cardiolipin analogue, the invention provides a method of tracking the migration of a lipid substance within an animal.

10. 发明公开

EP1539102A2 PHARMACEUTICALLY ACTIVE LIPID BASED FORMULATION OF SN38 审中-公开
标题翻译：药理学活性的含脂质SN-38配方
公开(公告)号：EP1539102A2
公开(公告)日：2005-06-15
申请号：EP03774459.6
申请日：2003-08-19
申请人： Neopharm, Inc.
发明人： AHMAD, Imran , ZHANG, Jia-Ai
IPC分类号： A61K9/00
CPC分类号： A61K9/127 , A61K31/4745
摘要： SN38, camptothecin derivatives are poorly water soluble, highly lipophilic camptothecin derivatives and are very active against a variety of human cancers. Because of their very poor water solubility, SN38 has not been used to treat human patients with cancer due to the inability to administer sufficient quantities of dissolved in a pharmaceutical formulation. This invention overcomes these limitations by teaching novel pharmaceutical acceptable SN38 liposome complex formulation for the direct administration of the formulation to human patients with cancer. The claimed invention also describes the methods to prepare liposomal SN38 complexes and antitumor compositions of liposomal SN38 complexes to allow the administration in sufficient amounts to treat various types of cancer and as antiviral agents. This invention is also directed to injectable sterile solutions, antitumor compositions, liposomes. The present invention is for novel compositions and methods for treating diseases caused by cellular proliferation, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include SN38 lipid complexes in which the complexes can contain any of a variety of neutral or charged lipids and, desirably, cardiolipin. The compositions are capable of efficiently incorporating SN38 into complexes and are capable of solubilizing relatively high concentrations of SN38.

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