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1. 发明申请

WO2012085171A2 PHARMACEUTICAL COMPOSITIONS OF PYRIDINIUM AND QUINOLINIUM DERIVATIVES 审中-公开
标题翻译：吡啶和喹啉衍生物的药物组合物
公开(公告)号：WO2012085171A2
公开(公告)日：2012-06-28
申请号：PCT/EP2011/073722
申请日：2011-12-22
申请人： TRASLATIONAL CANCER DRUGS PHARMA, S.L. , PALACIOS IZQUIERDO, Beatriz , VAN HOOGEVEST, Peter , L.S. LEIGH, Mathew
发明人： PALACIOS IZQUIERDO, Beatriz , VAN HOOGEVEST, Peter , L.S. LEIGH, Mathew
IPC分类号： A61K9/127 , A61K47/48 , A61K9/00 , A61K31/4425 , A61K31/4706 , A61P31/10 , A61P31/12 , A61P33/00 , A61P35/00
CPC分类号： A61K47/40 , A61K9/0019 , A61K9/08 , A61K9/127 , A61K31/4425 , A61K31/4706 , A61K47/6951 , B82Y5/00 , C07D213/74 , C07D215/44
摘要： The present invention relates to pharmaceutical compositions comprising a compound of formula (I) and a cyclodextrin or a liposome, to the process of preparing said compositions and their use for antitumor, antiviral, antiparasitic and antifungal treatment.
摘要翻译：本发明涉及包含式（I）化合物和环糊精或脂质体的药物组合物，涉及制备所述组合物的方法及其用于抗肿瘤，抗病毒，抗寄生虫和抗真菌治疗的用途。

2. 发明申请

WO2004075872A1 AMBIPHILIC POROUS MATRIX 审中-公开
标题翻译：辅助多孔矩阵
公开(公告)号：WO2004075872A1
公开(公告)日：2004-09-10
申请号：PCT/EP2004/001985
申请日：2004-02-27
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Mathew, Louis, Steven , LEIGH, Steve , KUNG, Elsa , VAN HOOGEVEST, Peter
发明人： LEIGH, Mathew, Louis, Steven , LEIGH, Steve , KUNG, Elsa , VAN HOOGEVEST, Peter
IPC分类号： A61K7/48
CPC分类号： A61K8/0279 , A61K8/24 , A61K8/26 , A61K8/553 , A61K8/731 , A61K8/922 , A61K2800/56 , A61Q1/02 , A61Q1/06 , A61Q1/08 , A61Q1/10 , A61Q19/00
摘要： Compositions are described which are capable of forming external reservoirs comprising a polymeric matrix for adsorbing sebum in exchange for beneficial oils and transfer of hydrating components to the skin. The compositions may be lotions, creams, gels, pastes, lip sticks and water in oil systems. There is also described a method of preparing said lotions, creams, etc containing an ambiphilic powder mixture or complex comprising synthetic porous agglomerates, a lipophilic component, hydrophilic attractant/polymer, optionally biologically active compound and excipients.
摘要翻译：描述了能够形成外部储存器的组合物，其包含用于吸收皮脂的聚合物基质，以换取有益的油并将保湿组分转移至皮肤。组合物可以是乳液，乳膏，凝胶，糊剂，唇膏和油中的水。还描述了一种制备含有含有合成多孔团聚物，亲脂性成分，亲水性引诱剂/聚合物，任选的生物活性化合物和赋形剂的两性粉末混合物或复合物的所述洗剂，霜剂等的方法。

3. 发明申请

WO2004047554A1 MARINE LIPID COMPOSITIONS 审中-公开
标题翻译：海洋脂肪组合物
公开(公告)号：WO2004047554A1
公开(公告)日：2004-06-10
申请号：PCT/EP2003/013299
申请日：2003-11-26
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steve , KUNG, Elsa , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
发明人： LEIGH, Steve , KUNG, Elsa , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
IPC分类号： A23K1/18
CPC分类号： A23D9/013 , A23J7/00 , A23K20/147 , A23K40/10 , A23K40/30 , A23K50/80 , A23L33/115 , A23L33/12 , A23L33/17 , A23V2002/00 , C11B1/10 , C11B1/104 , Y02A40/818 , A23V2200/224 , A23V2250/192 , A23V2250/182 , A23V2250/05 , A23V2250/1842
摘要： There is described marine phospholipids (MPL) compositions suitable for human, aquaculture applications comprising a dry composition comprising nutritional components selected from the group consisting of marine phospholipids, marine proteins and amino acid blends obtainable by fluid extraction of a dried marine raw material. The compositions have low amounts of neutral lipids and particularly low amounts of cholesterol and cholesterol esters. They may be used either as such in powder form and for preparing purified MPL compositions by ethanol extraction. Both forms may be used as nutritional supplements, ingredients for functional foods and to optimise the delivery and containment of nutritional components in multicomponent fish feed compositions. There is further described a blend of the purified, ethanol extracted MPL compositions mixed with marine, vegetable, microbial or MCT oils to form liquid preparations for hard or soft gel encapsulation. There is further described MPL concentrates comprising purified and clearly defined phospholipid types dispersed in hydrophilic medium which are nutritionally essential in larvae feed. Still further there is described MPL compositions in unit dosage forms as supplements to supply highly bioavailable omega-3 fatty acids for human use, optionally with biologically active compounds.
摘要翻译：描述了适用于人，水产养殖应用的海洋磷脂（MPL）组合物，其包含干组合物，其包含选自海洋磷脂，海洋蛋白质和通过干燥的海洋原料的流体萃取获得的氨基酸混合物的营养成分。组合物具有低量的中性脂质，特别是低量的胆固醇和胆固醇酯。它们可以以粉末形式使用，也可以通过乙醇提取制备纯化的MPL组合物。两种形式可以用作营养补充剂，功能食品的成分，并优化多组分鱼饲料组合物中营养成分的输送和遏制。进一步描述了与海洋，植物，微生物或MCT油混合的纯化的乙醇提取的MPL组合物的混合物，以形成用于硬或软凝胶包封的液体制剂。进一步描述了MPL浓缩物，其包含分散在亲水介质中的纯化和明确定义的磷脂类型，其在幼虫饲料中是营养必需的。此外，还描述了单位剂型中的MPL组合物作为补充剂，为人类提供高度生物可利用的ω-3脂肪酸，任选地具有生物活性化合物。

4. 发明申请

WO2003010330A3 TEST SYSTEM AND METHOD SUITABLE FOR SELECTING TEST MATERIALS AND FORMULATIONS 审中-公开
公开(公告)号：WO2003010330A3
公开(公告)日：2003-02-06
申请号：PCT/EP2002/008215
申请日：2002-07-23
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
发明人： LEIGH, Steve , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
IPC分类号： G01N33/50
摘要： The present invention provides a test system and a method for screening lipophilic and amphipathic materials with low water solubility. It generally relates to membrane lipid suspensions or dispersions employed as a test system for obtaining desired physico-chemical and biological information relating to the interaction of materials with membrane lipids in early screens in discovery. It serves as a selection method for derivatives of a test material for optimal membrane affinity and membrane permeation and thereby predict the potential for absorption in vivo. Furthermore, it may be used in later screening in formulation development, to select a carrier for a test material or derivative to enable the highest drug load. The data obtained by using the invention in primary screening provide key information on physico-chemical properties early on which may affect drug absorption and may be more predictive than log-octanol determinations. Compared to other screening methods which utilise cell models such as liposomes and cell lines, Transmembrane Screen (TS) is a versatile miniature tool that requires minimal amounts of test substances. It is adaptable, practical, cost effective and may be used routinely in high throughput screening.

5. 发明申请

WO2002080883A2 METHOD AND COMPOSITION FOR SOLUBILISING A BIOLOGICALLY ACTIVE COMPOUND WITH LOW WATER SOLUBILITY 审中-公开
标题翻译：用于溶解具有低水溶性的生物活性化合物的方法和组合物
公开(公告)号：WO2002080883A2
公开(公告)日：2002-10-17
申请号：PCT/EP2002/003371
申请日：2002-03-26
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steven , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
发明人： LEIGH, Steven , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , TIEMESSEN, Henricus
IPC分类号： A61K9/127
CPC分类号： A61K9/1075 , A61K9/1278
摘要： Compositions for forming molecular associates with lipophilic compounds and an improved method of loading lipophilic biologically active compounds into previously formed, aqueous suspensions of lipid particles. A preferred embodiment for injection purposes comprise lipid particles having sizes below 1000 nm in diameter, in a vial or other suitable container are described. The method involves mixing a lipophilic compound either in solution or as an amorphous, preferably lyophilised powder in a first container with an aqueous suspension of lipid particles contained in a second container to form molecular associates. Only minimum agitation is required. The entire procedure may be carried out instantly in situ, in sealed sterile units just prior to use in the hospital ward or by the bedside.
摘要翻译：用于与亲脂性化合物形成分子缔合物的组合物和将亲脂性生物活性化合物加载到先前形成的脂质颗粒水悬浮液中的改进方法。用于注射目的的优选实施方案包括直径小于1000nm，在小瓶或其它合适的容器中的脂质颗粒。该方法包括在第一容器中的溶液或无定形，优选冻干的粉末中混合亲脂性化合物与第二容器中含有的脂质颗粒的水性悬浮液以形成分子缔合物。只需要最小的搅动。整个程序可以在即将在医院病房或床边使用前的密封无菌单元中立即进行。

6. 发明申请

WO2010034837A1 METHOD OF SOLUBILISING BIOLOGICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：溶解生物活性化合物的方法
公开(公告)号：WO2010034837A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/062543
申请日：2009-09-28
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Steve , LEIGH, Mathew , Louis ,Steven , VAN HOOGEVEST, Peter
发明人： LEIGH, Steve , LEIGH, Mathew , Louis ,Steven , VAN HOOGEVEST, Peter
IPC分类号： A61K9/127 , A61K47/24
CPC分类号： A61K47/24 , A61K9/1277
摘要： The invention describes a method of preparing lipid compositions by associating pH sensitive compounds which maybe weak acids, bases or amphoteric compounds with at least one ionisable or pH sensitive group and low water solubility into preformed and standardised lipid particles by pH manipulation. Drug association is carried out in situ by changing the pH of the aqueous medium to pH 6-8 wherein the compound spontaneously partitions into the lipid particles. Drug association may also be carried out by exploiting pH changes in the GI tract. The lipophilic compound is solubilised by the lipid particles and may be used as such for in-vitro and pharmacokinetic assessments or processed for oral, parenteral or topical therapy.
摘要翻译：本发明描述了一种制备脂质组合物的方法，其通过pH操作将pH敏感化合物（其弱酸，碱或两性化合物与至少一个可电离或pH敏感基团和低水溶性）结合到预先形成和标准化的脂质颗粒中。通过将水性介质的pH改变为pH6-8，原位进行药物缔合，其中化合物自发分配成脂质颗粒。也可以通过利用GI道中的pH变化来进行药物关联。亲脂性化合物被脂质颗粒溶解，并且可以原样用于体外和药代动力学评估或用于口服，肠胃外或局部治疗。

7. 发明申请

WO2006125591A8 DIRECT DISSOLUTION 审中-公开
标题翻译：直接溶解
公开(公告)号：WO2006125591A8
公开(公告)日：2007-04-19
申请号：PCT/EP2006004842
申请日：2006-05-22
申请人： PHARES PHARM RES NV , LEIGH STEVE , LEIGH MATHEW LOUIS STEVEN , VAN HOOGEVEST PETER
发明人： LEIGH STEVE , LEIGH MATHEW LOUIS STEVEN , VAN HOOGEVEST PETER
IPC分类号： A23K1/16 , A23L1/275 , A23L1/30 , A23L1/302 , C09B61/00
CPC分类号： C09B61/00 , A23K20/158 , A23K20/179 , A23K40/20 , A23K40/25 , A23K50/80 , A23L5/44 , A23L33/105 , A23L33/115 , A23L33/15 , A23L33/155 , A23P10/35 , A23V2002/00 , Y02A40/818 , Y02P20/13 , A23V2250/211 , A23V2200/224 , A23V2250/186 , A23V2250/156
摘要： The present invention describes a method for the continuous dissolution of e.g. crystalline astaxanthin or canthaxanthin suspension in oil, by applying heat for a predetermined period using an in-line or optionally batch wise-process, followed by cooling the heated solution with an oil phase or heat exchanger. The resulting oil solution may be used as such or added directly to feed components which are turned into feed compositions by extrusion, compaction or granulation. Alternatively the oil solution is spray coated or directly loaded to extruded or compacted pellets and granulates. The invention avoids using formulated carotenoids prepared by known multi-step production methods requiring solvents, solvent removal, cooling and emulsification with an aqueous phase or precipitation and recovery steps. Thus the present invention is a more economical, efficient and environmentally friendly method to add nutrients and colorants to feed compositions instead of using colloid dispersed particulate Hydrocolloid compositions.
摘要翻译：本发明描述了用于连续溶解的方法。结晶的虾青素或角黄素悬浮液在油中，通过使用在线或任选的分批方法施加热量预定的时间，然后用油相或热交换器冷却加热的溶液。所得油溶液可以直接使用或直接加入通过挤出，压实或造粒转化成进料组合物的进料组分。或者，油溶液被喷涂或直接装载到挤出或压实的颗粒和颗粒中。本发明避免使用通过已知的多步骤生产方法制备的配制的类胡萝卜素，其需要溶剂，溶剂去除，冷却和乳化用水相或沉淀和回收步骤。因此，本发明是一种更经济，有效和环保的方法，用于向饲料组合物中加入营养物和着色剂，而不是使用胶体分散的颗粒状水胶体组合物。

8. 发明申请

WO2005110360A3 COMPOSITIONS FOR INJECTION 审中-公开
标题翻译：注射用组合物
公开(公告)号：WO2005110360A3
公开(公告)日：2006-04-06
申请号：PCT/EP2005005365
申请日：2005-05-17
申请人： PHARES PHARM RES NV , LEIGH STEVE , LEIGH MATHEW LOUIS STEVEN , VAN HOOGEVEST PETER
发明人： LEIGH STEVE , LEIGH MATHEW LOUIS STEVEN , VAN HOOGEVEST PETER
IPC分类号： A61K9/00 , A61K9/127 , A61K47/06 , A61K47/24 , A61K47/00
CPC分类号： A61K9/0024 , A61K9/0019 , A61K9/1274 , A61K47/06 , A61K47/24
摘要： The present invention relates to a homogeneous pharmaceutical composition for the gradual release of biologically active compounds after intramuscular or subcutaneous administration comprising at least one membrane lipid which is in the liquid crystalline state and a process for the preparation of said composition.
摘要翻译：本发明涉及用于在肌内或皮下给药后逐渐释放生物活性化合物的均匀药物组合物，其包含至少一种处于液晶状态的膜脂质和制备所述组合物的方法。

9. 发明申请

WO2004071494A2 LIPOPHILIC COMPOSITIONS 审中-公开
标题翻译：脂肪组合物
公开(公告)号：WO2004071494A2
公开(公告)日：2004-08-26
申请号：PCT/EP2004/001355
申请日：2004-02-13
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , QUINTON, Jacques , LEIGH, Steve
发明人： LEIGH, Mathew, Louis, Steven , VAN HOOGEVEST, Peter , QUINTON, Jacques , LEIGH, Steve
IPC分类号： A61K9/16
CPC分类号： A61K9/1652 , A61K9/146 , A61K9/4866
摘要： There is described dry compositions comprising lipophilic compounds associated with low viscosity grades of water insoluble polymer and optionally hydrophilic agent/ s associated either as monomolecular or amorphous complexes. There is also described a method of preparing said lipophilic polymer complexes from a solution or homogeneous dispersion employing either water miscible or immiscible organic solvents. The lipophilic polymer complex is precipitated from the solution comprising a water miscible solvent by dilution with water, separating out the precipitated complex, washing, drying and conversion to oral and topical dosage forms. The lipophilic polymer complex may also be prepared by solvent removal involving spray drying or vacuum drying under elevated temperatures using either water miscible or water immiscible solvents. The compositions are characterised by improved dissolution and solubility of the associated compound in aqueous medium.
摘要翻译：描述了包含与低粘度等级的水不溶性聚合物相关的亲脂性化合物和任选的作为单分子或无定形络合物缔合的亲水剂的干组合物。还描述了使用水可混溶或不混溶的有机溶剂的溶液或均匀分散体制备所述亲脂性聚合物复合物的方法。通过用水稀释，从包含水混溶性溶剂的溶液中沉淀亲脂性聚合物络合物，分离出沉淀的复合物，洗涤，干燥和转化为口服和局部剂型。亲脂性聚合物复合物也可以通过溶剂去除制备，包括喷雾干燥或在高温下使用水混溶或水不混溶的溶剂进行真空干燥。组合物的特征在于相关化合物在水性介质中的溶解和溶解度的改善。

10. 发明申请

WO2004037216A1 MICRODISPERSION AND METHOD OF PRODUCING SAME 审中-公开
标题翻译：微生物及其生产方法
公开(公告)号：WO2004037216A1
公开(公告)日：2004-05-06
申请号：PCT/EP2003/011936
申请日：2003-10-28
申请人： PHARES PHARMACEUTICAL RESEARCH N.V. , LEIGH, Mathew, Louis, Steven , LEIGH, Steve , VAN HOOGEVEST, Peter , KUNG, Elsa
发明人： LEIGH, Mathew, Louis, Steven , LEIGH, Steve , VAN HOOGEVEST, Peter , KUNG, Elsa
IPC分类号： A61K7/00
CPC分类号： A61K8/06 , A61K8/345 , A61K8/37 , A61K8/375 , A61K8/553 , A61K2800/21 , A61Q19/00 , A61Q19/08
摘要： The invention describes homogeneous microdispersions comprising at least one hydrogenated or partially hydrogenated membrane lipid with or without enzyme hydrolysis, dispersed in substantially non aqueous, non volatile hydrophilic medium with boiling point above 40°C. More preferably the compositions comprise a mixture of hydrogenated monoacyl and hydrogenated diacyl lipids and at least one oil. The phospholipid mixture is obtained by controlled enzyme hydrolysis of lecithin or a specific phospholipid, followed by hydrogenation. The compositions have improved rheology, physical and chemical properties, functionality and industrial applicability. The microdispersions are used as such in all types of applications and as functional components with active compounds in products, particularly for improving skin function and facilitating skin repair due to UV damage and aging, in cosmetics and other topical products.
摘要翻译：本发明描述了均匀的微分散体，其包含至少一种具有或不具有酶水解的氢化或部分氢化的膜脂质，分散在沸点高于40℃的基本上非水性的非挥发性亲水介质中。更优选地，组合物包含氢化单酰基和氢化二酰基脂质与至少一种油的混合物。磷脂混合物通过卵磷脂或特定磷脂的受控酶水解，然后氢化而获得。组合物具有改善的流变性，物理和化学性质，功能性和工业适用性。微分散体在所有类型的应用中都是这样使用的，并且作为在产品中具有活性化合物的功能组分，特别是用于改善皮肤功能并促进由于紫外线损伤和老化引起的皮肤修复，在化妆品和其它局部产品中。

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