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1. 发明申请

WO2006102533A2 PHARMACEUTICALLY ACTIVE LIPID-BASED FORMULATION OF NUCLEOSIDE-LIPID CONJUGATES 审中-公开
标题翻译：基于脂质体的药物基于脂质体的配方
公开(公告)号：WO2006102533A2
公开(公告)日：2006-09-28
申请号：PCT/US2006010638
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： A61K31/7072
CPC分类号： C07H19/06 , C07H19/16
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.
摘要翻译：提供了核苷 - 脂质缀合物的新型制剂，其制备方法及其施用方法。更具体地，提供了制备核苷 - 心磷脂及其类似物的脂质体制剂的方法。通过封装核苷前药，药物被保护免于降解，从而延长药物的血浆半衰期和细胞内释放。此外，产生显示更大功效和更高细胞毒性的组合物。因此，产生显示出更大的体外和体内活性的核苷 - 脂质缀合物。

2. 发明申请

WO2005067632A3 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：WO2005067632A3
公开(公告)日：2009-04-02
申请号：PCT/US2005000418
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 , C07H21/04 , C12N15/11 , C12N15/113 , C12N15/88
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。

3. 发明申请

WO2006029081A3 NUCLEOSIDE-LIPID CONJUGATES, THEIR METHOD OF PREPARATION AND USES THEREOF 审中-公开
标题翻译：核苷脂酸结合体，其制备方法及其用途
公开(公告)号：WO2006029081A3
公开(公告)日：2009-04-23
申请号：PCT/US2005031543
申请日：2005-09-02
申请人： NEOPHARM INC , AHMAD MOGHIS U , ALI SHOUKATH M , KHAN ABDUL R , AHMAD IMRAN
发明人： AHMAD MOGHIS U , ALI SHOUKATH M , KHAN ABDUL R , AHMAD IMRAN
IPC分类号： A61K31/70 , A61K31/7052 , A61K31/7068 , A61K31/7072 , A61K31/7076
CPC分类号： A61K31/7072 , A61K9/127
摘要： The invention provides methods for synthesizing nucleoside-lipid conjugates having varying fatty acid and alkyl chain lengths with or without unsaturation and their use in the treatment of cancer and viral diseases. More particularly, the invention provides methods for preparing gemcitabine-cardiolipin conjugates, and analogues thereof, cytarabine-cardiolipin conjugates, and analogues thereof. Additionally, the methods of the invention comprise administering a compound of invention as prodrug or a pharmaceutical preparation to combat mammalian diseases, preferably cancer, viral infections and bone disorders.
摘要翻译：本发明提供了具有不同脂肪酸和具有或不具有不饱和键的烷基链长度的核苷 - 脂质缀合物的方法及其在治疗癌症和病毒性疾病中的用途。更具体地，本发明提供了制备吉西他滨 - 心磷脂偶联物及其类似物的方法，阿糖胞苷 - 心磷脂缀合物及其类似物。此外，本发明的方法包括施用本发明化合物作为前药或药物制剂，以对抗哺乳动物疾病，优选癌症，病毒感染和骨骼疾病。

4. 发明申请

WO2004062569A3 CARDIOLIPIN COMPOSITIONS THEIR METHODS OF PREPARATION AND USE 审中-公开
标题翻译：卡泊醇组合物他们的制备和使用方法
公开(公告)号：WO2004062569A3
公开(公告)日：2004-09-02
申请号：PCT/US0313917
申请日：2003-05-04
申请人： NEOPHARM INC , AHMAD MOGHIS U , LIN ZHEN , ALI SHOUKATH M , AHMAD IMRAN
发明人： AHMAD MOGHIS U , LIN ZHEN , ALI SHOUKATH M , AHMAD IMRAN
IPC分类号： A61K9/127 , A61K31/522 , A61K31/7068 , A61K31/7072 , A61K47/18 , A61K47/24 , C07F9/10 , A61K48/00 , C07F9/11 , C07H11/04 , C07K5/04 , C12N15/88
CPC分类号： C07F9/10 , A61K9/0014 , A61K9/0019 , A61K9/1271 , A61K9/1272 , A61K31/522 , A61K31/7068 , A61K31/7072 , A61K47/18 , A61K47/24
摘要： The invention provides new synthetic routes for cardiolipin with different fatty acids and/or alkyl chains with varying chain length and also with or without unsaturation. The reaction schemes can be used to generate new forms of cardiolipin, including cardiolipin variants. The cardiolipin prepared by the present methods can conveniently be incorporated into liposomes and other lipid formulations that can also include active agents such as hydrophobic or hydrophilic drugs. Such formulations can be used to treat diseases or in diagnostic and/or analytical assays. Liposomes also can include ligands, e.g., for targeting them to a cell type or specific tissue.
摘要翻译：本发明为心磷脂与不同脂肪酸和/或具有不同链长以及有或没有不饱和度的烷基链提供新的合成途径。反应方案可用于产生新形式的心磷脂，包括心磷脂变体。通过本发明方法制备的心磷脂可方便地并入脂质体和其它也可包括活性剂如疏水或亲水药物的脂质制剂。这样的制剂可用于治疗疾病或诊断和/或分析测定。脂质体还可以包括配体，例如用于将它们靶向细胞类型或特定组织。

5. 发明申请

WO2007100808A3 METHOD AND PROCESS FOR PREPARING CARDIOLIPIN 审中-公开
标题翻译：制备心脏纤维蛋白酶的方法和方法
公开(公告)号：WO2007100808A3
公开(公告)日：2008-11-13
申请号：PCT/US2007005038
申请日：2007-02-22
申请人： NEOPHARM INC , ALI SHOUKATH M , AHMAD MOGHIS U , AHMAD IMRAN
发明人： ALI SHOUKATH M , AHMAD MOGHIS U , AHMAD IMRAN
IPC分类号： A61K48/00 , C07F5/06
CPC分类号： C07F9/106
摘要： The invention provides novel methods for preparing cardiolipin and cardiolipin analogs having varying fatty acid chain lengths, particularly l,r,2,2'-tetramyristoyl cardiolipin. The methods comprise reacting a starting compound, such as a 1,2-O-sn- diacylglycerol and a 2-protected glycerol, with a phosphoramidite reagent to produce a protected cardiolipin, which is deprotected to prepare cardiolipin. The cardiolipin and cardiolipin analogs may be prepared in the presence of an activator, such as pyridiniuin trifluororacetate. The methods of the present invention are used to prepare cardiolipin and cardiolipin analogs in large quantities. The cardiolipin prepared by the present methods can be incorporated into liposomes which can also include active agents such as hydrophobic or hydrophilic drugs. Such liposomes can be used to treat diseases or in diagnostic and/or analytical assays.
摘要翻译：本发明提供了制备具有不同脂肪酸链长度的心磷脂和心磷脂类似物的新方法，特别是1，r，2,2'-四磺酰基心磷脂。所述方法包括将起始化合物，例如1,2--O-二酰基甘油和2-保护的甘油与亚磷酰胺试剂反应以产生受保护的心磷脂，将其去保护以制备心磷脂。心磷脂和心磷脂类似物可以在活化剂存在下制备，例如三氟醋酸吡啶二酮。本发明的方法用于大量制备心磷脂和心磷脂类似物。通过本发明方法制备的心磷脂可以并入脂质体中，脂质体还可以包括活性剂如疏水或亲水药物。这样的脂质体可用于治疗疾病或在诊断和/或分析测定中。

6. 发明申请

WO2006004935A3 PEGYLATED CARDIOLIPIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF 审中-公开
标题翻译：聚乙二醇化合物类似物，合成方法及其用途
公开(公告)号：WO2006004935A3
公开(公告)日：2006-06-01
申请号：PCT/US2005023286
申请日：2005-06-29
申请人： NEOPHARM INC , AHMAD MOGHIS U , UKKALAM MURALI K , ALI SHOUKATH M , AHMAD IMRAN
发明人： AHMAD MOGHIS U , UKKALAM MURALI K , ALI SHOUKATH M , AHMAD IMRAN
IPC分类号： C07F9/02
CPC分类号： C07F9/093 , C07F9/10
摘要： The invention provides synthetic methods for PEGylated cardiolipins with varying linkers. The methods can be employed to prepare PEGylated cardiolipin with different fatty acid and/or alkyl chain length with or without unsaturation. The PEGylated cardiolipin, prepared by the present methods, can be incorporated into liposomes that can also include active agents such as hydrophilic or hydrophobic drugs for the treatment of human and animal diseases. In addition, the PEGylated cardiolipin can be incorporated into liposomes that include compounds for therapeutic and diagnostic imaging. The use of such liposomes with PEGylated cardiolipin prolongs the period of liposomal circulation without disrupting the lipid bilayer.
摘要翻译：本发明提供了具有不同接头的聚乙二醇化心磷脂的合成方法。该方法可用于制备具有或不具有不饱和度的不同脂肪酸和/或烷基链长度的聚乙二醇化心磷脂。通过本发明方法制备的聚乙二醇化的心磷脂可以并入脂质体中，脂质体还可以包括活性剂，例如用于治疗人和动物疾病的亲水或疏水性药物。此外，聚乙二醇化的心磷脂可以并入脂质体，其包括用于治疗和诊断成像的化合物。聚乙二醇化心磷脂的这种脂质体的使用延长了脂质体循环的时间，而不会破坏脂质双层。

7. 发明申请

WO2007100808A2 METHOD AND PROCESS FOR PREPARING CARDIOLIPIN 审中-公开
标题翻译：制备心脏纤维蛋白酶的方法和方法
公开(公告)号：WO2007100808A2
公开(公告)日：2007-09-07
申请号：PCT/US2007005038
申请日：2007-02-22
申请人： NEOPHARM INC , ALI SHOUKATH M , AHMAD MOGHIS U , AHMAD IMRAN
发明人： ALI SHOUKATH M , AHMAD MOGHIS U , AHMAD IMRAN
CPC分类号： C07F9/106
摘要： The invention provides novel methods for preparing cardiolipin and cardiolipin analogs having varying fatty acid chain lengths, particularly l,r,2,2'-tetramyristoyl cardiolipin. The methods comprise reacting a starting compound, such as a 1,2-O-sn- diacylglycerol and a 2-protected glycerol, with a phosphoramidite reagent to produce a protected cardiolipin, which is deprotected to prepare cardiolipin. The cardiolipin and cardiolipin analogs may be prepared in the presence of an activator, such as pyridiniuin trifluororacetate. The methods of the present invention are used to prepare cardiolipin and cardiolipin analogs in large quantities. The cardiolipin prepared by the present methods can be incorporated into liposomes which can also include active agents such as hydrophobic or hydrophilic drugs. Such liposomes can be used to treat diseases or in diagnostic and/or analytical assays.
摘要翻译：本发明提供了制备具有不同脂肪酸链长度的心磷脂和心磷脂类似物的新方法，特别是1，r，2,2'-四磺酰基心磷脂。所述方法包括将起始化合物，例如1,2--O-二酰基甘油和2-保护的甘油与亚磷酰胺试剂反应以产生受保护的心磷脂，将其去保护以制备心磷脂。心磷脂和心磷脂类似物可以在活化剂存在下制备，例如三氟醋酸吡啶二酮。本发明的方法用于大量制备心磷脂和心磷脂类似物。通过本发明方法制备的心磷脂可以并入脂质体中，脂质体还可以包括活性剂如疏水或亲水药物。这样的脂质体可用于治疗疾病或在诊断和/或分析测定中。

8. 发明申请

WO2006052906A3 SYNTHESIS OF CARDIOLIPIN ANALOGUES AND USES THEREOF 审中-公开
标题翻译：心磷脂类似物的合成及其用途
公开(公告)号：WO2006052906A3
公开(公告)日：2006-08-24
申请号：PCT/US2005040325
申请日：2005-11-08
申请人： NEOPHARM INC , AHMAD MOGHIS U , UKKALAM MURALI K , ALI SHOUKATH M , AHMAD IMRAN
发明人： AHMAD MOGHIS U , UKKALAM MURALI K , ALI SHOUKATH M , AHMAD IMRAN
IPC分类号： C07F9/02
CPC分类号： C07F9/106
摘要： The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.
摘要翻译：本发明提供了用于制备心磷脂，迁移的心磷脂（心磷脂的1,2-位置异构体）及其具有不同长度和饱和度/不饱和度的各种脂肪酸和/或烷基链的类似物的新合成方法。该方法包括：（a）使光学纯的1,2-O-二烷基-sn-甘油或1,2-O-二烷基-sn-甘油与一种或多种亚磷酰胺试剂反应，其中产生亚磷酸三酯; （b）将（a）的产物与甘油偶联，其中产生受保护的心磷脂; 和（c）将受保护的心磷脂去保护，从而制备出心磷脂。可以将通过本发明方法制备的心磷脂及其类似物掺入到脂质体中，所述脂质体还可以包含活性剂，例如疏水或亲水药物，反义核苷酸或诊断剂。这种脂质体可用于治疗疾病或可用于诊断和/或分析测定。

9. 发明申请

WO2008070463A9 ENDOXIFEN METHODS AND COMPOSITIONS 审中-公开
标题翻译： ENDOXIFEN方法和组合物
公开(公告)号：WO2008070463A9
公开(公告)日：2008-09-18
申请号：PCT/US2007085443
申请日：2007-11-21
申请人： JINA PHARMACEUTICALS INC , AHMAD ATEEQ , ALI SHOUKATH M , AHMAD MOGHIS U , SHEIKH SAIFUDDIN , AHMAD IMRAN
发明人： AHMAD ATEEQ , ALI SHOUKATH M , AHMAD MOGHIS U , SHEIKH SAIFUDDIN , AHMAD IMRAN
IPC分类号： A61K31/35
CPC分类号： A61K31/138 , A61K9/0014 , A61K9/127 , A61K9/19 , A61K31/35 , C07D309/10
摘要： The present invention provides compositions containing endoxifen, formulations and liposomes of endoxifen, methods of preparation of such agents and formulations, and use of such agents and formulations for the treatment of breast cancer and other breast diseases and diseases susceptible to endoxifen. In particular, the compositions of the present invention include liposomes, complexes, vesicles, emulsions, micelles and mixed micelles of endoxifen in which the compositions further contain any of a variety of neutral or charged lipids and desirably, cholesterol and cholesterol derivatives, sterols, Z- and E- guggulsterones, phospholipids, fatty acids, vitamin D, and vitamin E. The present invention also provides methods of preparing endoxifen. The present invention provides methods for treating and preventing breast cancer and other breast related diseases by administrating novel formulations or compositions comprising a therapeutically effective amount of endoxifen.
摘要翻译：本发明提供了包含endoxifen，endoxifen的制剂和脂质体的组合物，制备这些制剂和制剂的方法，以及这些制剂和制剂用于治疗乳腺癌和其他乳腺疾病和易患endoxifen的疾病的用途。特别地，本发明的组合物包括endoxifen的脂质体，复合物，囊泡，乳剂，胶束和混合胶束，其中所述组合物进一步含有多种中性或带电脂质中的任何一种，并且期望胆固醇和胆固醇衍生物，甾醇，Z - 和E-胍酯，磷脂，脂肪酸，维生素D和维生素E.本发明还提供了制备烯诺昔芬的方法。本发明提供了通过施用包含治疗有效量的多昔多芬的新制剂或组合物来治疗和预防乳腺癌和其他乳房相关疾病的方法。

10. 发明申请

WO2008127358A3 AQUEOUS SYSTEMS FOR THE PREPARATION OF LIPID-BASED PHARMACEUTICAL COMPOUNDS; COMPOSITIONS, METHODS, AND USES THEREOF 审中-公开
标题翻译：用于制备基于脂质的药物化合物的水性体系; 组合物，方法及其用途
公开(公告)号：WO2008127358A3
公开(公告)日：2008-12-24
申请号：PCT/US2007080984
申请日：2007-10-10
申请人： JINA PHARMACEUTICALS INC , ALI SHOUKATH M , AHMAD MOGHIS U , AHMAD ATEEQ , SHEIKH SAIFUDDIN , AHMAD IMRAN
发明人： ALI SHOUKATH M , AHMAD MOGHIS U , AHMAD ATEEQ , SHEIKH SAIFUDDIN , AHMAD IMRAN
IPC分类号： A61K9/127
CPC分类号： A61K47/28 , A61K9/0019 , A61K9/1075 , A61K9/127 , A61K9/1617 , A61K9/1682 , A61K9/19 , A61K9/5123 , A61K31/337 , A61K31/436 , A61K31/704 , A61K31/7048 , A61K47/10 , A61K47/24 , A61K47/541 , A61K47/554
摘要： The present invention relates to a methods of preparing active compounds complexed with lipids using aqueous systems that are free of organic solvents, and methods of using the complexes, e.g., in treating a disease in a subject. In some embodiments, the present invention comprises a composition comprising a complex comprising at least one active compound, e.g., a polyene antibiotic, an immunosuppressant agent such as tacrolimus or a taxane or taxane derivative, and one or more lipids. In some embodiments, the present invention provides a method comprising preparing a composition comprising a lipid complex comprising at least one active compound and at least one lipid and administering the composition to a subject. In certain embodiments the subject is a mammal. In certain preferred embodiments, the subject is human.
摘要翻译：本发明涉及使用不含有机溶剂的水性体系制备与脂质复合的活性化合物的方法，以及使用复合物例如治疗受试者疾病的方法。在一些实施方案中，本发明包含包含至少一种活性化合物，例如多烯抗生素，免疫抑制剂如他克莫司或紫杉烷或紫杉烷衍生物的复合物和一种或多种脂质的组合物。在一些实施方案中，本发明提供了一种方法，其包括制备包含至少一种活性化合物和至少一种脂质的脂质复合物并将组合物给予受试者的组合物。在某些实施方案中，受试者是哺乳动物。在某些优选实施方案中，受试者是人。

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