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1. 发明授权

EP1387844B1 RETINOL DERIVATIVES POTENTIATION OF ACTIVE SUBSTANCES BY MICELLAR PREPARATION 有权
标题翻译： STEIGERUNG DER WIRKSAMKEIT VON WIRKSTOFFEN DURCH MICELLARE ZUBEREITUNG MIT RETINOLDERIVATEN
公开(公告)号：EP1387844B1
公开(公告)日：2007-06-13
申请号：EP02701856.3
申请日：2002-03-05
申请人： Ardenia Investments Ltd.
发明人： STRELCHENOK, Oleg , ALEKSOV, Julian
IPC分类号： C07C11/21 , C07C13/20 , A61K31/185 , A61P35/00
CPC分类号： A61K9/1075 , A61K31/203 , A61K31/40 , C07B2200/09 , C07C403/20 , C07C403/22 , C07C2601/16
摘要： This invention relates to novel compounds, capable of potentiating the efficacy of therapeutically active compounds, for example cytotoxic compounds used in the treatment of cancer. The novel compounds have been shown to increase the pharmacological activity of a conventional paclitaxel formulation and to make it possible to manufacture a new formulation of paclitaxel, exhibiting improved solubility, improved storage properties, and increased therapeutic efficacy as shown in the enclosed examples. (Formula I, II, III, IV, V, VI)
摘要翻译：本发明涉及能够增强治疗活性化合物（例如用于治疗癌症的细胞毒性化合物）的功效的视黄酰衍生物钠盐的合成。已经显示这些化合物增加了常规紫杉醇制剂的药理活性，并且使得可以制备新的紫杉醇制剂，显示出改进的溶解性，改进的储存性能和提高的治疗功效，如所附的实施例所示。

2. 发明授权

EP2231189B1 DRUG DELIVERY SYSTEM FOR ADMINISTRATION OF POORLY WATER SOLUBLE PHARMACEUTICALLY ACTIVE SUBSTANCES 有权转让
标题翻译：用于处理水溶性药物活性物质的药物递送系统
公开(公告)号：EP2231189B1
公开(公告)日：2017-09-06
申请号：EP08861526.5
申请日：2008-12-18
申请人： Ardenia Investments Ltd.
发明人： ALEKSOV, Julian , LOKOT, Igor
IPC分类号： A61K38/13 , A61K47/20 , A61K9/14 , A61P35/00 , A61P37/06 , A61K9/51 , A61K31/337
CPC分类号： A61K9/5123 , A61K9/145 , A61K31/337 , A61K38/13

3. 发明授权

EP2231192B1 DRUG DELIVERY SYSTEM FOR ADMINISTRATION OF A WATER SOLUBLE, CATIONIC AND AMPHIPHILIC PHARMACEUTICALLY ACTIVE SUBSTANCE 失效转让
标题翻译：用于治疗水溶性，阳离子和两性医药活性物质的药物递送系统
公开(公告)号：EP2231192B1
公开(公告)日：2017-08-02
申请号：EP08861217.1
申请日：2008-12-18
申请人： Ardenia Investments Ltd.
发明人： ALEKSOV, Julian , LOKOT, Igor
IPC分类号： A61K47/54 , A61K9/14 , A61P35/00 , A61K9/10 , A61K9/51 , A61K31/704 , A61K31/136 , A61K31/4745
CPC分类号： A61K31/704 , A61K9/0019 , A61K9/10 , A61K9/145 , A61K9/5123 , A61K31/136 , A61K31/4745 , A61K47/541

4. 发明公开

EP2231193A1 DRUG DELIVERY SYSTEM FOR ADMINISTRATION OF A WATER SOLUBLE, CATIONIC AND AMPHIPHILIC PHARMACEUTICALLY ACTIVE SUBSTANCE 有权转让
标题翻译：给药系统管理水溶性，阳离子和营销两亲活性物质
公开(公告)号：EP2231193A1
公开(公告)日：2010-09-29
申请号：EP08863195.7
申请日：2008-12-18
申请人： Ardenia Investments Ltd.
发明人： ALEKSOV, Julian , LOKOT, Igor
IPC分类号： A61K47/48 , A61K9/14 , A61P35/00
CPC分类号： A61K9/5123 , A61K9/0019 , A61K9/10 , A61K9/145 , A61K31/136 , A61K31/232 , A61K31/337 , A61K31/4745 , A61K31/704 , A61K45/06 , A61K47/541 , A61K2300/00
摘要： A drug delivery system (DDS) for administration of a water soluble, cationic, and amphiphilic pharmaceutically active substance (API) which DDS comprises amorphous particles of

5. 发明公开

EP2231192A1 DRUG DELIVERY SYSTEM FOR ADMINISTRATION OF A WATER SOLUBLE, CATIONIC AND AMPHIPHILIC PHARMACEUTICALLY ACTIVE SUBSTANCE 失效转让
标题翻译：给药系统管理水溶性，阳离子和营销两亲活性物质
公开(公告)号：EP2231192A1
公开(公告)日：2010-09-29
申请号：EP08861217.1
申请日：2008-12-18
申请人： Ardenia Investments Ltd.
发明人： ALEKSOV, Julian , LOKOT, Igor
IPC分类号： A61K47/48 , A61K9/14 , A61P35/00
CPC分类号： A61K31/704 , A61K9/0019 , A61K9/10 , A61K9/145 , A61K9/5123 , A61K31/136 , A61K31/4745 , A61K47/541
摘要： A drug delivery system (DDS) for administration of a water soluble, cationic, and amphiphilic pharmaceutically active substance (API) which DDS comprises poorly water soluble nanoparticles formed by the API together with a Na-salt of N-all- trans-retinoyl cysteic acid methyl ester and/or a Na-salt of N-13-cis-retinoyl cys- teic acid methyl ester. A pharmaceutical composition comprising such a DDS. Methods for preparation of such a DDS and such a pharmaceutical composition. Use of such a DDS and pharmaceutical composition for treatment of cancer.

6. 发明公开

EP2231189A1 DRUG DELIVERY SYSTEM FOR ADMINISTRATION OF POORLY WATER SOLUBLE PHARMACEUTICALLY ACTIVE SUBSTANCES 有权转让
标题翻译：给药系统行政POOR水溶性活性物质的药物
公开(公告)号：EP2231189A1
公开(公告)日：2010-09-29
申请号：EP08861526.5
申请日：2008-12-18
申请人： Ardenia Investments Ltd.
发明人： ALEKSOV, Julian , LOKOT, Igor
IPC分类号： A61K47/20 , A61K9/14 , A61P35/00 , A61P37/06
CPC分类号： A61K9/5123 , A61K9/145 , A61K31/337 , A61K38/13
摘要： This invention relates to a drug delivery system for administration of poorly water soluble pharmaceutically active substance, a pharmaceutical composition comprising such a drug delivery system, and a method for the preparation of such a drug delivery system. The invention also relates to a method for controlling the particle size and/or particle shape and/or particle size distribution in such a drug delivery system, and to a method for increasing the drug loading capacity of the particles. Furthermore the invention also relates to the use of such a drug delivery system for the preparation of a medicament for the treatment of cancer.
摘要翻译：本发明涉及药物递送系统，用于水溶性差的药用活性物质的给药，药物组合物，其包括寻求的药物递送系统，以及用于寻求药物递送系统的制备方法。本发明因此涉及一种用于控制方法粒径和/或颗粒形状和/或在寻求药物输送系统的颗粒尺寸分布，和用于增加所述颗粒的药物负载能力的方法。因此进一步，本发明涉及使用寻求的药物递送系统在制备用于治疗癌症的治疗。

7. 发明公开

EP1534672A1 RETINOL DERIVATIVES, THEIR USE IN THE TREATMENT OF CANCER AND FOR POTENTIATING THE EFFICACY OF OTHER CYTOTOXIC AGENTS 有权
标题翻译：视黄醇和它们在癌症的治疗和细胞毒性药物的其它增强的有效性
公开(公告)号：EP1534672A1
公开(公告)日：2005-06-01
申请号：EP02783947.1
申请日：2002-11-15
申请人： Ardenia Investments Ltd.
发明人： STRELCHENOK, Oleg , ALEKSOV, Julian
IPC分类号： C07C403/22 , A61K31/198 , A61K31/223 , A61P35/00
CPC分类号： C07C403/20 , C07B2200/09 , C07C2601/16
摘要： A group of new compounds, N-(all-trans-Retinoyl)-L-cysteic acid, N-(13-cis-Retinoyl)-L-cysteic acid, N-(all-trans-Retinoyl)-L-cysteinesulfinic acid, N-(13-cis-Retinoyl)-L-cysteinesulfinic acid, N-(all-trans-Retinoyl)-L-homocysteic acid, N-(13-cis-Retinoyl)-L-homocysteic acid, and sodium salts of these compounds, including sodium salts of their esters and amides, is shown to exhibit therapeutic effects per se, and which compounds in combination with cytotoxic compounds, such as docetaxel, paclitaxel, doxorubicin and mitoxantrone, exhibit a synergistic effect. These compounds make it possible to manufacture new formulations of poorly soluble pharmaceutical compounds, and the present invention discloses a process of manufacturing water-soluble formulations of such compounds, exemplified by docetaxel, and paclitaxel, exhibiting enhanced pharmacological activity, and formulations of water-soluble pharmaceuticals exemplified by doxorubicin and mitoxantrone, exhibiting improved therapeutic efficacy.
摘要翻译： A组的新化合物，N-（全反式 - 视黄酰基）-L-半胱磺酸，N-（13-顺式 - 视黄酰基）-L-半胱磺酸，N-（全反式 - 视黄酰基）-L- cysteinesulfinic酸的，N-（13-顺式 - 视黄酰基）-L- cysteinesulfinic酸，N-（全反式 - 视黄酰基）-L-高半胱磺酸，N-（13-顺式 - 视黄酰基）-L-同型半胱氨酸，及钠盐合成的化合物，包括它们的酯和酰胺的钠盐，被示出为表现出治疗效果本身，并与细胞毒性化合物，颜色组合这些化合物：如多西他赛，紫杉醇，多柔比星和米托蒽醌，表现出了协同作用。这些化合物使人们有可能制造难溶药物化合物的新配方和灰，并且本发明的圆盘更小的制造寻求化合物中，由多西他赛例举，和紫杉醇的水溶性配方和灰，参展增强药理学活性，和式和灰的处理水溶性多柔比星和米托蒽醌例举，药物表现出改善的疗效。

8. 发明公开

EP1387844A1 RETINOL DERIVATIVES POTENTIATION OF ACTIVE SUBSTANCES BY MICELLAR PREPARATION 有权
标题翻译：增物质的有效性与视黄醇胶束的制备
公开(公告)号：EP1387844A1
公开(公告)日：2004-02-11
申请号：EP02701856.3
申请日：2002-03-05
申请人： Ardenia Investments Ltd.
发明人： STRELCHENOK, Oleg , ALEKSOV, Julian
IPC分类号： C07D487/14 , A61K31/40 , A61P31/00
CPC分类号： A61K9/1075 , A61K31/203 , A61K31/40 , C07B2200/09 , C07C403/20 , C07C403/22 , C07C2601/16
摘要： This invention relates to novel compounds, capable of potentiating the efficacy of therapeutically active compounds, for example cytotoxic compounds used in the treatment of cancer. The novel compounds have been shown to increase the pharmacological activity of a conventional paclitaxel formulation and to make it possible to manufacture a new formulation of paclitaxel, exhibiting improved solubility, improved storage properties, and increased therapeutic efficacy as shown in the enclosed examples. (Formula I, II, III, IV, V, VI)

9. 发明公开

EP3386947A1 METHOD FOR PRODUCING N-RETINOYLCYSTEIC ACID ALKYL ESTER 有权转让
公开(公告)号：EP3386947A1
公开(公告)日：2018-10-17
申请号：EP16873468.9
申请日：2016-12-09
申请人： Ardenia Investments, Ltd.
发明人： BABROU, Dzianis , BUDNIKAVA, Maryna , BJÖRKLUND, Mikael , ALEKSOV, Julian
IPC分类号： C07C403/22 , C07C309/18 , C07C309/23 , C07C313/04
CPC分类号： C07C403/22 , C07C403/20 , C07C2601/16 , C07D301/00 , C07D301/32 , C07D303/46
摘要： A method for producing derivatives of N-retinoylaminoalkane sulfonic acid, the method comprising providing retinoic acid, chloroformate, aminoalkanesulfonic acid selected from the group consisting of cysteic acid and alkyl ester thereof, cysteinesulfinic acid and alkyl ester thereof, homocysteic acid and alkyl ester thereof, homocysteinesulfinic acid and alkyl esters thereof, taurine and derivatives thereof, and an organic solvent, and a base, mixing said components under substantial absence of oxidizing compounds thereby forming a reaction mixture comprising a liquid phase, wherein the liquid phase is one phase and the derivatives of N-retinoylaminoalkane sulfonic acid are formed in said liquid phase.

10. 发明授权

EP2231193B1 DRUG DELIVERY SYSTEM FOR ADMINISTRATION OF A WATER SOLUBLE, CATIONIC AND AMPHIPHILIC PHARMACEUTICALLY ACTIVE SUBSTANCE 有权转让
公开(公告)号：EP2231193B1
公开(公告)日：2018-07-18
申请号：EP08863195.7
申请日：2008-12-18
申请人： Ardenia Investments, Ltd.
发明人： ALEKSOV, Julian , LOKOT, Igor
IPC分类号： A61K9/14 , A61P35/00 , A61K9/10 , A61K9/51 , A61K31/704 , A61K31/232 , A61K31/337 , A61K31/136 , A61K31/4745 , A61K45/06 , A61K47/54
CPC分类号： A61K9/5123 , A61K9/0019 , A61K9/10 , A61K9/145 , A61K31/136 , A61K31/232 , A61K31/337 , A61K31/4745 , A61K31/704 , A61K45/06 , A61K47/541 , A61K2300/00
摘要： A drug delivery system (DDS) for administration of a water soluble, cationic, and amphiphilic pharmaceutically active substance (API) which DDS comprises amorphous particles of

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