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1. 发明授权

US09750812B2 Lipid based pharmaceutical preparations for oral and topical application; their compositions, methods, and uses thereof 有权
公开(公告)号：US09750812B2
公开(公告)日：2017-09-05
申请号：US13120127
申请日：2009-09-25
申请人： Shoukath M. Ali , Ateeq Ahmad , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
发明人： Shoukath M. Ali , Ateeq Ahmad , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
IPC分类号： A61K47/24 , A61K9/127 , A61K8/04 , A61K9/00 , A61K9/08 , A61K9/10 , A61K31/506 , A61K31/58 , A61K45/06 , A61K47/44
CPC分类号： A61K47/24 , A61K9/0014 , A61K9/08 , A61K9/10 , A61K31/506 , A61K31/58 , A61K45/06 , A61K47/44 , Y02A50/409 , A61K2300/00
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.

2. 发明申请

US20100151002A1 Guggulphospholipid Methods and Compositions 有权
标题翻译： Guculphospholipid方法和组成
公开(公告)号：US20100151002A1
公开(公告)日：2010-06-17
申请号：US12513654
申请日：2007-11-06
申请人： Moghis U. Ahmad , Shoukath M. Ali , Ateeq Ahmad , Saifuddin Sheikh , Imran Ahmad
发明人： Moghis U. Ahmad , Shoukath M. Ali , Ateeq Ahmad , Saifuddin Sheikh , Imran Ahmad
IPC分类号： A61K9/127 , C07J13/00 , C07J31/00 , A61K31/56 , A61K31/66 , C12N15/00 , C12N5/00 , A61P3/10 , A61P9/00
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. The present invention also 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。本发明还提供了一种从E-和Z-庚烷酮的混合物制备E-guggulsterol和Z-guggulsterol或E-和Z-瓜焦糖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。

3. 发明申请

US20110212167A1 LIPID BASED PHARMACEUTICAL PREPARATIONS FOR ORAL AND TOPICAL APPLICATION; THEIR COMPOSITIONS, METHODS, AND USES THEREOF 有权
标题翻译：用于口腔和局部应用的基于脂质的药物制剂; 它们的组成，方法及其用途
公开(公告)号：US20110212167A1
公开(公告)日：2011-09-01
申请号：US13120127
申请日：2009-09-25
申请人： Shoukath M. Ali , Ateeq Ahmad , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
发明人： Shoukath M. Ali , Ateeq Ahmad , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
IPC分类号： A61K9/127 , A61K31/58 , A61K31/513 , A61K31/7048 , A61K31/436 , A61P17/14 , A61P31/10 , A61P31/00 , A61P27/04 , A61P29/00
CPC分类号： A61K47/24 , A61K9/0014 , A61K9/08 , A61K9/10 , A61K31/506 , A61K31/58 , A61K45/06 , A61K47/44 , Y02A50/409 , A61K2300/00
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.
摘要翻译：本发明涉及包含用于治疗受试者的疾病或症状的一种或多种活性剂的组合物的局部和口服递送。在一些实施方案中，本发明包含包含至少一种活性化合物，例如非那雄胺或米诺地尔和一种或多种脂质的组合物。在一些实施方案中，本发明涉及治疗雄激素性脱发（AGA），预防脱发和雌性多毛症的制剂的组合物和方法。在一些实施方案中，本发明包含非那雄胺和用于治疗良性前列腺增生的至少一种脂质组分。在一些实施方案中，本发明包含他克莫司或两性霉素B和至少一种用于治疗皮肤或眼睛相关疾病的脂质组分。本发明提供了制备包含至少一种活性化合物和至少一种脂质并通过口服或局部递送将组合物给予受试者的组合物的方法。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。

4. 发明授权

US09333190B2 Endoxifen compositions and methods 有权
标题翻译：内给药组合物和方法
公开(公告)号：US09333190B2
公开(公告)日：2016-05-10
申请号：US12515261
申请日：2007-11-21
申请人： Ateeq Ahmad , Shoukath M. Ali , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
发明人： Ateeq Ahmad , Shoukath M. Ali , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
IPC分类号： A61K9/20 , A61K9/28 , A61K9/48 , A61K31/138 , A61K31/35 , A61K9/00 , A61K9/127 , A61K9/19 , C07D309/10
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：本发明提供了含有内皮素的内含物，制剂和脂质体的组合物，这些药剂和制剂的制备方法，以及用于治疗乳腺癌和其它乳腺疾病和对内给药易感染的疾病的制剂和制剂的用途。特别地，本发明的组合物包括脂质体，复合物，囊泡，乳剂，胶束和内皮素的混合胶束，其中所述组合物还含有任何多种中性或带电荷的脂质，并且期望地，胆固醇和胆固醇衍生物，甾醇，Z - 和戊二酮，磷脂，脂肪酸，维生素D和维生素E.本发明还提供了内皮素的制备方法。本发明提供了通过施用包含治疗有效量的内皮素的新制剂或组合物来治疗和预防乳腺癌和其它乳腺相关疾病的方法。

5. 发明申请

US20100112041A1 Endoxifen Compositions And Methods 有权
标题翻译：内给药组合物和方法
公开(公告)号：US20100112041A1
公开(公告)日：2010-05-06
申请号：US12515261
申请日：2007-11-21
申请人： Ateeq Ahmad , Shoukath M. Ali , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
发明人： Ateeq Ahmad , Shoukath M. Ali , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
IPC分类号： A61K31/138 , A61K9/127 , A61K9/10 , C07C213/10 , A61P35/00 , C07C215/08 , A61K9/48 , A61K9/28
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：本发明提供了含有内皮素的内含物，制剂和脂质体的组合物，这些药剂和制剂的制备方法，以及用于治疗乳腺癌和其它乳腺疾病和对内给药易感染的疾病的制剂和制剂的用途。特别地，本发明的组合物包括脂质体，复合物，囊泡，乳剂，胶束和内皮素的混合胶束，其中所述组合物还含有任何多种中性或带电荷的脂质，并且期望地，胆固醇和胆固醇衍生物，甾醇，Z - 和戊二酮，磷脂，脂肪酸，维生素D和维生素E.本发明还提供了内皮素的制备方法。本发明提供了通过施用包含治疗有效量的内皮素的新制剂或组合物来治疗和预防乳腺癌和其它乳腺相关疾病的方法。

6. 发明申请

US20100068251A1 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系统; 组合，方法和用途
公开(公告)号：US20100068251A1
公开(公告)日：2010-03-18
申请号：US11915345
申请日：2007-10-10
申请人： Shoukath M. Ali , Moghis U. Ahmad , Ateeq Ahmad , Saifuddin Sheikh , Imran Ahmad
发明人： Shoukath M. Ali , Moghis U. Ahmad , Ateeq Ahmad , Saifuddin Sheikh , Imran Ahmad
IPC分类号： A61K9/127 , A61K9/14 , A61K31/7048 , A61K31/337 , A61K31/436 , A61K31/704 , C12N5/071 , A61P31/10 , A61P35/00
CPC分类号： A61K9/19 , A61K9/127 , A61K9/1277 , A61K9/145 , A61K9/5123
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的组合物，并将所述组合物给予受试者。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。

7. 发明授权

US09637515B2 Guggulphospholipid methods and compositions 有权
公开(公告)号：US09637515B2
公开(公告)日：2017-05-02
申请号：US12513654
申请日：2007-11-06
申请人： Moghis U. Ahmad , Shoukath M. Ali , Ateeq Ahmad , Saifuddin Sheikh , Imran Ahmad
发明人： Moghis U. Ahmad , Shoukath M. Ali , Ateeq Ahmad , Saifuddin Sheikh , Imran Ahmad
IPC分类号： A61K9/127 , C07J13/00 , C07J7/00 , C07J31/00 , C07J41/00 , C07J51/00 , A61K48/00
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. The present invention also 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.

8. 发明申请

US20120164075A1 ENDOXIFEN METHODS AND COMPOSITIONS IN THE TREATMENT OF MAMMALIAN DISEASES 审中-公开
标题翻译：内分泌方法和组合物治疗马马里兰病
公开(公告)号：US20120164075A1
公开(公告)日：2012-06-28
申请号：US13321767
申请日：2010-05-21
申请人： Ateeq Ahmad , Shoukath M. Ali , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
发明人： Ateeq Ahmad , Shoukath M. Ali , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
IPC分类号： A61K31/138 , A61K9/48 , A61K31/205 , A61K49/00 , A61P25/18 , A61P25/28 , A61P25/00 , A61P25/16 , A61P25/08 , A61P31/00 , A61P31/04 , A61P31/12 , A61P33/02 , A61P9/00 , A61P19/10 , A61P15/08 , A61K9/127 , A61K9/28
CPC分类号： A61K31/138 , A61K9/06 , A61K9/107 , A61K9/19 , Y02A50/409
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 a subject having or at risk for psychiatric and neurodegenerative diseases, infectious diseases, fertility disorders, osteoporosis, osteoarthritis, and/or cardiovascular diseases. Specifically, the present invention relates to compositions comprising endoxifen for use in the treatment of such disorders or predisposition to such disorders, for use in manufacture of medicaments for treating such disorders, and methods comprising use of such compositions in such treatments.
摘要翻译：本发明提供了含有内皮素的内含物，制剂和脂质体的组合物，这些药剂和制剂的制备方法，以及这些药剂和制剂用于治疗患有精神和神经退行性疾病，感染性疾病，生育能力或有风险的受试者的用途疾病，骨质疏松症，骨关节炎和/或心血管疾病。具体地说，本发明涉及包含用于治疗这种疾病或易患这些病症的内给素的组合物，用于制备用于治疗这种病症的药物，以及包括在这种治疗中使用这些组合物的方法。

9. 发明申请

US20090291134A1 ENDOXIFEN METHODS AND COMPOSITIONS IN THE TREATMENT OF PSYCHIATRIC AND NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：治疗精神病学和神经病变疾病的内毒素方法和组合物
公开(公告)号：US20090291134A1
公开(公告)日：2009-11-26
申请号：US12470219
申请日：2009-05-21
申请人： Ateeq Ahmad , Shoukath M. Ali , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
发明人： Ateeq Ahmad , Shoukath M. Ali , Moghis U. Ahmad , Saifuddin Sheikh , Imran Ahmad
IPC分类号： A61K9/48 , A61K31/138 , A61P25/18 , A61P25/28 , A61P25/16 , A61K9/28 , C12N5/06
CPC分类号： A61K9/06 , A61K9/0014 , A61K9/08 , A61K9/19 , A61K31/138 , Y02A50/409
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 a subject having or at risk for psychiatric and neurodegenerative diseases. Specifically, the present invention relates to the composition comprising endoxifen in the treatment of bipolar disorder, schizophrenia, multiple sclerosis (MS), Alzheimer disease, Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis (ALS), and/or epilepsy by administrating formulations or compositions comprising an effective amount of endoxifen.
摘要翻译：本发明提供了含有内皮素的内含物，制剂和脂质体的组合物，这些药剂和制剂的制备方法，以及这些药剂和制剂用于治疗患有精神病和神经退行性疾病或有风险的受试者的用途。具体地说，本发明涉及包含治疗双相情感障碍，精神分裂症，多发性硬化（MS），阿尔茨海默氏病，帕金森病，亨廷顿舞蹈病，肌萎缩性侧索硬化（ALS），和/或癫痫中的内给予的组合物，包含有效量的内皮素的组合物。

10. 发明申请

US20080300418A1 Synthesis of Cardiolipin Analogues and Uses Thereof 审中-公开
标题翻译：心磷脂类似物及其用途的合成
公开(公告)号：US20080300418A1
公开(公告)日：2008-12-04
申请号：US11667232
申请日：2005-11-08
申请人： Moghis U. Ahmad , Murali K. Ukkalam , Shoukath M. Ali , Imran Ahmad
发明人： Moghis U. Ahmad , Murali K. Ukkalam , Shoukath M. Ali , Imran Ahmad
IPC分类号： C07F9/202
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：本发明提供了新的合成方法，用于制备心磷脂，迁移的卡立二磷（心磷脂的1,2位异构体）及其类似物，其具有不同长度和饱和度/不饱和度变化的脂肪酸和/或烷基链。该方法包括（a）使光学纯的1,2-O-二烷基-sn-甘油或1,2-二烷基-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）使保护的心磷脂脱保护，使得制备心磷脂。通过本发明方法制备的心磷脂及其类似物可以掺入脂质体中，脂质体还可以包括活性剂如疏水或亲水药物，反义核苷酸或诊断剂。这样的脂质体可用于治疗疾病或可用于诊断和/或分析测定。

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