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1. 发明专利

CA2587103A1 SYNTHESIS OF CARDIOLIPIN ANALOGUES AND USES THEREOF 未知
公开(公告)号：CA2587103A1
公开(公告)日：2006-05-18
申请号：CA2587103
申请日：2005-11-08
申请人： AHMAD IMRAN , UKKALAM MURALI K , NEOPHARM INC , ALI SHOUKATH M
发明人： AHMAD MOGHIS U , UKKALAM MURALI K , AHMAD IMRAN , ALI SHOUKATH M
IPC分类号： C07F9/02

2. 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。

3. 发明申请

WO2008127358A2 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，方法和用途
公开(公告)号：WO2008127358A2
公开(公告)日：2008-10-23
申请号：PCT/US2007/080984
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 , Y02A50/409
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络合的活性化合物的方法，以及使用该络合物的方法，例如用于治疗受试者中的疾病的方法。在一些实施方案中，本发明包含组合物，其包含含有至少一种活性化合物（例如多烯抗生素），免疫抑制剂（例如他克莫司或紫杉烷或紫杉烷衍生物）和一种或多种脂质的复合物。在一些实施方案中，本发明提供一种方法，其包括制备包含脂质复合物的组合物，所述脂质复合物包含至少一种活性化合物和至少一种脂质，并将所述组合物施用于受试者在某些实施方案中，受试者是哺乳动物。在某些优选的实施方案中，受试者是人。

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

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。

6. 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。

7. 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。

8. 发明申请

WO2010036947A3 LIPID BASED PHARMACEUTICAL PREPARATIONS FOR ORAL AND TOPICAL APPLICATION; THEIR COMPOSITIONS, METHODS, AND USES THEREOF 审中-公开
公开(公告)号：WO2010036947A3
公开(公告)日：2010-04-01
申请号：PCT/US2009/058463
申请日：2009-09-25
申请人： ALI, Shoukath M. , AHAMD, Ateeq , AHMAD, Moghis U. , SHEIKH, Saifuddin , AHMAD, Imran , JINA PHARMACEUTICALS, INC.
发明人： ALI, Shoukath M. , AHAMD, Ateeq , AHMAD, Moghis U. , SHEIKH, Saifuddin , AHMAD, Imran
IPC分类号： A61K47/44 , A61P17/14 , A61K31/58 , A61K31/506
摘要： The present invention relates to the topical and oral delivery of a composition comprising one or more active agents for treating a disease or symptoms in a subject. In some embodiments, the present invention comprises a composition comprising at least one active compound, e.g., finasteride or minoxidil, and one or more lipids. In some embodiments, the present invention relates to composition and method of preparation for treating androgenic alopecia (AGA), prevention of hair loss and female hirsutism. In some embodiment, the present invention comprises finasteride and at least one lipid component for the treatment of benign prostatic hyperplasia. In some embodiment, the present invention comprises tacrolimus or amphotericin B and at least one lipid component for the treatment of skin or eye related diseases. The present invention provides a method of preparation of a composition comprising at least one active compound and at least one lipid and administering the composition to a subject by oral or topical delivery. In certain embodiments the subject is a mammal. In certain preferred embodiment, the subject is human.

9. 发明申请

WO2008070463A3 ENDOXIFEN METHODS AND COMPOSITIONS 审中-公开
公开(公告)号：WO2008070463A3
公开(公告)日：2008-11-06
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： A61K9/127 , A61K9/12
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.

10. 发明申请

WO2008058156A2 GUGGULPHOSPHOLIPID METHODS AND COMPOSITIONS 审中-公开
标题翻译： GUGGPHPHPHPHIPIPI方法和组合物
公开(公告)号：WO2008058156A2
公开(公告)日：2008-05-15
申请号：PCT/US2007083832
申请日：2007-11-06
申请人： JINA PHARMACEUTICALS INC , AHMAD MOGHIS U , ALI SHOUKATH M , AHMAD ATEEQ , SHEIKH SAIFUDDIN , AHMAD IMRAN
发明人： AHMAD MOGHIS U , ALI SHOUKATH M , AHMAD ATEEQ , SHEIKH SAIFUDDIN , AHMAD IMRAN
IPC分类号： A01N65/00
CPC分类号： C07J13/007 , A61K31/337 , A61K47/554 , A61K47/6907 , A61K47/6911 , C07J7/0005 , C07J31/006 , C07J41/0005 , C07J41/0088 , C07J51/00 , C12N15/85
摘要： The present invention relates to the methods for preparing synthetic guggulphospholipids, their fatty acid analogues and other bioactive molecules. The present invention relates to E-guggulsterone and Z-guggulsterone or mixture of E- and Z-guggulsterones; and E-guggulsterol and Z-guggulsterol or mixture of E- and Z-guggulsterols synthetically modified to guggulphospholipids and analogues and salts thereof, fatty acid analogues of guggulsterols, guggulsulfate and salts thereof, guggulphosphate and salts thereof; and guggulsterols conjugated with drugs for use as prodrugs. Also the present invention provides a novel method for the preparation of E-guggulsterol and Z-guggulsterol or mixture of E-and Z-guggulsterols from a mixture of E- and Z-guggulsterones. The present invention further relates to guggulphospholipids and other bioactive molecules incorporated into complexes such as liposomes, complexes, emulsions, vesicles, micelles, and mixed micelles, which can include other active agents, such as hydrophobic or hydrophilic drugs for use, e.g., in treatment of human and animal diseases.
摘要翻译：本发明涉及制备合成瓜瓜磷脂，其脂肪酸类似物和其它生物活性分子的方法。本发明涉及戊二酮和Z-鬼臼酮或E-和Z-格鲁酮的混合物; 合成修饰成瓜瓜尔斯醇和Z-guggulsterol或者合成修饰成瓜瓜尔斯醇及其类似物及其盐的瓜尔豆甾醇和Z-瓜格尔斯醇的混合物，瓜焦糖醇，巨硫酸盐及其盐的脂肪酸类似物，磷酸瓜瓜酯及其盐; 和与药物缀合的糖苷醇用作前药。本发明还提供了一种从E-和Z-格鲁酮的混合物制备E-guggulsterol和Z-guggulsterol或E-和Z-苦瓜甾醇的混合物的新方法。本发明还涉及结合到诸如脂质体，复合物，乳液，囊泡，胶束和混合胶束的复合物中的瓜瓜磷脂和其它生物活性分子，其可以包括其它活性剂，例如用于治疗的疏水或亲水药物的人类和动物疾病。

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