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1. 发明授权

US08815931B2 Oral formulations for tetrapyrrole derivatives 有权
标题翻译：四吡咯衍生物的口服制剂
公开(公告)号：US08815931B2
公开(公告)日：2014-08-26
申请号：US12768244
申请日：2010-04-27
申请人： Susanna Gräfe , Nikolay Nifantiev , Albrecht Volker , Wolfgang Neuberger , Gerhard Wieland , Dietrich Scheglmann , Alfred Fahr , Arno Wiehe
发明人： Susanna Gräfe , Nikolay Nifantiev , Albrecht Volker , Wolfgang Neuberger , Gerhard Wieland , Dietrich Scheglmann , Alfred Fahr , Arno Wiehe
IPC分类号： A61K31/40 , A61K9/127 , A61K31/498 , A61K9/00 , A61K31/409
CPC分类号： A61K31/409 , A61K9/0065 , A61K9/127 , A61K9/1271 , A61K31/498
摘要： Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles. The oral formulation, in case of a hydrophobic photosensitizer in the present invention, is stabilized using suitable surfactants/solubilizers thus preventing aggregation of the drug in the stomach and until it is absorbed in the duodenum and the small intestine. Oral formulations can be administered in the form of liquid, capsule, tablet, powder, paste or gel. Formulated drugs can be administered orally as one single dose or in multiple doses before administering PDT. In one embodiment Temoporfin (m-THPC) is used as a photosensitizer in the oral formulations. Temoporfin like many hydrophobic photosensitizers are especially suitable to be administered orally because there is no known enzyme system in the mammalian body which can metabolize Temoporfin or similar photosensitizers. Temoporfin can reach the blood system unchanged and fully active after absorption of the formulation in the gastrointestinal tract.
摘要翻译：提出了在光动力治疗（PDT）和抗微生物光动力疗法（APDT）治疗中配制口服光敏剂的口服制剂和方法。口服配制的光敏剂显示增加的溶解度和渗透性，从而提高光敏剂在治疗部位的生物利用度。口服给药的光敏剂适于配制用于通过胃肠粘膜进行粘膜粘附和吸收。本文提供的口服制剂通过口服途径使用脂质和已知蛋白质作为光敏剂的载体。用于封装预选光敏剂的载体包括常规脂质体，聚乙二醇化脂质体，纳米乳剂，纳米胶体，纳米颗粒，脂肪乳剂，脂质制剂，水溶胶，SMEDDS，α-铁蛋白（AFP）和牛血清白蛋白（BSA），脂肪乳剂，热熔融挤出物和纳米颗粒。在本发明的疏水性光敏剂的情况下，使用合适的表面活性剂/增溶剂稳定口服制剂，从而防止药物在胃中的聚集，直到其被吸收到十二指肠和小肠中。口服制剂可以以液体，胶囊，片剂，粉末，糊剂或凝胶的形式施用。配制药物可以在给予PDT之前以一次剂量或多次剂量口服给药。在一个实施方案中，Temoporfin（m-THPC）用作口服制剂中的光敏剂。类似于许多疏水性光敏剂的Temoporfin特别适合于口服给药，因为哺乳动物体内没有已知的可以代谢Temoporfin或类似光敏剂的酶系统。 Temoporfin可以在胃肠道吸收制剂后达到血液系统不变和充分活性。

2. 发明申请

US20100273803A1 Oral Formulations for Tetrapyrrole Derivatives 有权
标题翻译：四吡咯衍生物的口服制剂
公开(公告)号：US20100273803A1
公开(公告)日：2010-10-28
申请号：US12768244
申请日：2010-04-27
申请人： Susanna Gräfe , Nikolay Nifantiev , Albrecht Volker , Wolfgang Neuberger , Gerhard Wieland , Dietrich Scheglmann , Alfred Fahr , Arno Wiehe
发明人： Susanna Gräfe , Nikolay Nifantiev , Albrecht Volker , Wolfgang Neuberger , Gerhard Wieland , Dietrich Scheglmann , Alfred Fahr , Arno Wiehe
IPC分类号： A61K31/498 , C07D241/46 , A61K31/409 , C07D487/22 , A61P35/00 , A61P31/00 , A61K8/49 , A61Q19/00 , A61Q9/00
CPC分类号： A61K31/409 , A61K9/0065 , A61K9/127 , A61K9/1271 , A61K31/498
摘要： Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles. The oral formulation, in case of a hydrophobic photosensitizer in the present invention, is stabilized using suitable surfactants/solubilizers thus preventing aggregation of the drug in the stomach and until it is absorbed in the duodenum and the small intestine. Oral formulations can be administered in the form of liquid, capsule, tablet, powder, paste or gel. Formulated drugs can be administered orally as one single dose or in multiple doses before administering PDT. In one embodiment Temoporfin (m-THPC) is used as a photosensitizer in the oral formulations. Temoporfin like many hydrophobic photosensitizers are especially suitable to be administered orally because there is no known enzyme system in the mammalian body which can metabolize Temoporfin or similar photosensitizers. Temoporfin can reach the blood system unchanged and fully active after absorption of the formulation in the gastrointestinal tract.
摘要翻译：提出了在光动力治疗（PDT）和抗微生物光动力疗法（APDT）治疗中配制口服光敏剂的口服制剂和方法。口服配制的光敏剂显示增加的溶解度和渗透性，从而提高光敏剂在治疗部位的生物利用度。口服给药的光敏剂适于配制用于通过胃肠粘膜进行粘膜粘附和吸收。本文提供的口服制剂通过口服途径使用脂质和已知蛋白质作为光敏剂的载体。用于封装预选光敏剂的载体包括常规脂质体，聚乙二醇化脂质体，纳米乳剂，纳米胶体，纳米颗粒，脂肪乳剂，脂质制剂，水溶胶，SMEDDS，α-铁蛋白（AFP）和牛血清白蛋白（BSA），脂肪乳剂，热熔融挤出物和纳米颗粒。在本发明的疏水性光敏剂的情况下，使用合适的表面活性剂/增溶剂稳定口服制剂，从而防止药物在胃中的聚集，直到其被吸收到十二指肠和小肠中。口服制剂可以以液体，胶囊，片剂，粉末，糊剂或凝胶的形式施用。配制药物可以在给予PDT之前以一次剂量或多次剂量口服给药。在一个实施方案中，Temoporfin（m-THPC）用作口服制剂中的光敏剂。类似于许多疏水性光敏剂的Temoporfin特别适合于口服给药，因为哺乳动物体内没有已知的可以代谢Temoporfin或类似光敏剂的酶系统。 Temoporfin可以在胃肠道吸收制剂后达到血液系统不变和充分活性。

3. 发明授权

US08580839B2 Photosensitizer formulations and their use 有权
标题翻译：光敏剂配方及其用途
公开(公告)号：US08580839B2
公开(公告)日：2013-11-12
申请号：US12080767
申请日：2008-04-04
申请人： Nikolay Nifantiev , Volker Albrecht
发明人： Nikolay Nifantiev , Volker Albrecht
IPC分类号： A61K31/409
CPC分类号： A61K31/195 , A61K31/366 , A61K31/409 , A61K41/0057 , A61K41/0061 , A61K41/0071
摘要： A new treatment regime is presenter using a low concentration formulation at a low dosage of hydrophobic photosensitizers (PS) that shows improved pharmacokinetics and an effective method for photodynamic therapy (“PDT”). The new formulation has better pharmacological effect compared to standard photosensitizer formulation with standard dosage. It was found that PDT treatments using the disclosed low concentration formulations provide for more accurate, more efficient and more convenient dosing. It was found that the inventive formulation; (1) reduces the time for a therapeutically effective level of photosensitizer to accumulate in diseased tissue; and, (2) reduces the time for achieving a sufficient ratio of photosensitizer in diseased tissue vs. healthy tissue. As a result, the formulation of the invention reduces the time interval between PS application/administration and irradiation (the drug-light interval or “DLI”) and can provide for a “same day” PDT treatment option. The inventive formulation can be used for PDT treatment regimes where photosensitizers are administered in at least one preselected dose, including a low concentration therapy for PDT. In particular, when meta-(Tetrahydroxyphenyl)Chlorin (m-THPC) is the photosensitizer, then a concentration of 0.8 mg/ml to 0.04 mg/ml in a mixture of pure propylene glycol and ethanol in a 3:2 volume ratio accumulates in diseased tissue and differentiates between diseased tissue and normal tissue sufficiently quickly for ‘one day’ or overnight administration and activation treatment procedures to be possible.
摘要翻译：在低剂量的疏水性光敏剂（PS）中使用低浓度制剂来呈现新的治疗方案，其显示改善的药物动力学和光动力学治疗（“PDT”）的有效方法。与标准剂量的标准光敏剂配方相比，新配方具有更好的药理作用。发现使用所公开的低浓度制剂的PDT治疗提供更准确，更有效和更方便的给药。发现本发明的制剂; （1）减少治疗有效水平的光敏剂累积在患病组织中的时间; 和（2）减少在病变组织中对光固化剂与健康组织的足够比例的时间。结果，本发明的制剂减少了PS施用/给药和照射之间的时间间隔（药物光间隔或“DLI”），并且可以提供“同一天”PDT治疗选择。本发明的制剂可用于PDT治疗方案，其中光敏剂以至少一种预选剂量施用，包括用于PDT的低浓度治疗。特别是当Meta-（四羟基苯基）二氢卟酚（m-THPC）是光敏剂时，在纯丙二醇和3:2体积比的乙醇混合物中的浓度为0.8mg / ml至0.04mg / ml，病变组织并且在病变组织和正常组织之间充分快速地分离“一天”或过夜施用和活化处理程序以使其成为可能。

4. 发明申请

US20110245198A1 ENHANCED TREATMENTS TO KILL OR DEBILITATE PATHOGENIC MICROORGANISMS OF A MAMMALIAN BODY 审中-公开
标题翻译：增强杀死或治疗哺乳动物体内致病微生物的治疗方法
公开(公告)号：US20110245198A1
公开(公告)日：2011-10-06
申请号：US12727383
申请日：2010-03-19
申请人： Nikolay Nifantiev , Gerhard D. Wieland
发明人： Nikolay Nifantiev , Gerhard D. Wieland
IPC分类号： A61K31/737 , A61P31/04 , A61M37/00
CPC分类号： A61K31/715 , A61K41/0019 , A61K41/0038
摘要： Present invention relates to a composition of matter and a method that improves treatments to inactivate, kill and debilitate pathogenic microorganisms that infect on or within a mammal body, such as Helicobacter pylori. The composition of matter comprises anti-adhesive polysaccharide molecules to abolish or reduce the adhesion of H. pylori to themselves and to gastric mucin without affecting the viability of either bacteria or gastric epithelial cells. Polysaccharides isolated from seaweed are preferred anti-adhesive materials and fucoidans is a most preferred embodiment. To facilitate bacteria eradication, methods include the administration of fucoidans before, during and/or after other killing and destroying physical or chemical therapy. The inhibition or impairment of the mechanism of bacterial adhesion due to the treatment with fucoidans is aimed to diminish colonization and pathogenesis of pathogenic bacteria by making them more fragile or susceptible to killing or destroying therapies. The combined use of fucoidans with PDT is a preferred method to eradicate H. Pylori in the gastrointestinal tract.
摘要翻译：本发明涉及一种物质组合物和一种改善对哺乳动物体内如感染幽门螺杆菌或感染的致病微生物灭活，杀死和衰弱的治疗方法。物质的组成包括抗粘多糖分子以消除或减少幽门螺杆菌对其自身和胃粘蛋白的粘附，而不影响细菌或胃上皮细胞的活力。从海藻中分离的多糖是优选的抗粘剂材料，岩藻聚糖是最优选的实施方案。为了促进细菌根除，方法包括在其他杀伤和破坏物理或化学疗法之前，期间和/或之后施用岩藻多糖。由于用岩藻多糖处理引起的细菌粘附机制的抑制或损伤旨在通过使其变得更脆弱或易于杀死或破坏治疗来减少致病细菌的定植和发病。岩藻多糖与PDT的组合使用是消除胃肠道幽门螺杆菌的优选方法。

5. 发明申请

US20110150880A1 METHODS AND COMPOSITIONS RELATING TO SYNTHETIC BETA-1,6 GLUCOSAMINE OLIGOSACCHARIDES 有权
标题翻译：与合成β-1,6葡萄糖胺低聚糖相关的方法和组合物
公开(公告)号：US20110150880A1
公开(公告)日：2011-06-23
申请号：US13055178
申请日：2009-07-21
申请人： Gerald B. Pier , Nikolay Nifantiev , Yury Tsvetkov , Marina Gening
发明人： Gerald B. Pier , Nikolay Nifantiev , Yury Tsvetkov , Marina Gening
IPC分类号： A61K39/385 , C07C53/00 , C07D207/46 , C07C381/00 , C07H5/06 , A61K31/70 , A61K39/395 , A61P31/00 , A61P37/00
CPC分类号： A61K39/085 , A61K47/6415 , A61K47/646 , A61K2039/55 , A61K2039/552 , A61K2039/575 , A61K2039/6037 , C07C327/32 , C07D207/46 , C07H3/06 , C07K16/1232 , C07K16/1271 , C07K2317/33 , Y02A50/407
摘要： The invention relates to the compositions of synthetic oligo-β-(1→6)-2-amino-2-deoxy-D-glucopyranosides conjugated to carriers, and methods for making and use same.
摘要翻译：本发明涉及与载体缀合的合成寡聚 - （1→6）-2-氨基-2-脱氧-D-吡喃葡萄糖苷的组合物，以及制备和使用它们的方法。

6. 发明授权

US07825153B2 Photosensitizer formulations and their use 有权
标题翻译：光敏剂配方及其用途
公开(公告)号：US07825153B2
公开(公告)日：2010-11-02
申请号：US11153703
申请日：2005-06-15
申请人： Nikolay Nifantiev , Volker Albrecht
发明人： Nikolay Nifantiev , Volker Albrecht
IPC分类号： A61K31/409
CPC分类号： A61K31/195 , A61K31/366 , A61K31/409 , A61K41/0057 , A61K41/0061 , A61K41/0071
摘要： A low concentration formulation for hydrophobic photosensitizers (PS) and method for photodynamic therapy (“PDT”) using the disclosed low concentration formulations provide for more accurate, more efficient and more convenient dosing. The inventive formulation (1) reduces the time for a therapeutically effective level of photosensitizer to accumulate in diseased tissue and (2) reduces the time for achieving a sufficient ratio of photosensitizer in diseased tissue vs. healthy tissue. The inventive formulation reduces the time interval between PS application/administration and irradiation (the drug-light interval or “DLI”) and can provide for a “same day” PDT treatment option. 0.08 mg/ml to 1.3 mg/ml meta Tetra-Hydroxy-Phenyl Chlorin (m-THPC) as the photosensitizer in a mixture of pure propylene glycol and ethanol (3:2 volume ratio) accumulates in diseased tissue and differentiates between diseased tissue and normal tissue sufficiently quickly for ‘one day’ or overnight administration and activation treatment procedures to be possible.
摘要翻译：使用所公开的低浓度制剂的疏水性光敏剂（PS）和光动力学治疗（“PDT”）的低浓度制剂提供更准确，更有效和更方便的给药。本发明的制剂（1）减少治疗有效水平的光敏剂积累在患病组织中的时间，和（2）减少在患病组织与健康组织中获得足够比例的光敏剂的时间。本发明的配方减少PS施用/施用和照射之间的时间间隔（药物光间隔或“DLI”），并且可以提供“同一天”PDT治疗选择。在纯丙二醇和乙醇（3:2体积比）的混合物中作为光敏剂的间 - 四羟基苯基二氢卟酚（m-THPC）的0.08mg / ml至1.3mg / ml在患病组织中积累并分化为患病组织和正常组织足够快地“一天”或过夜施用和活化处理程序是可能的。

7. 发明申请

US20080195032A1 Photosensitizer formulations and their use 有权
标题翻译：光敏剂配方及其用途
公开(公告)号：US20080195032A1
公开(公告)日：2008-08-14
申请号：US12080767
申请日：2008-04-04
申请人： Nikolay Nifantiev , Volker Albrecht
发明人： Nikolay Nifantiev , Volker Albrecht
IPC分类号： A61N1/30 , A61K31/407 , A61P43/00
CPC分类号： A61K31/195 , A61K31/366 , A61K31/409 , A61K41/0057 , A61K41/0061 , A61K41/0071
摘要： A new treatment regime is presenter using a low concentration formulation at a low dosage of hydrophobic photosensitizers (PS) that shows improved pharmacokinetics and an effective method for photodynamic therapy (“PDT”). The new formulation has better pharmacological effect compared to standard photosensitizer formulation with standard dosage. It was found that PDT treatments using the disclosed low concentration formulations provide for more accurate, more efficient and more convenient dosing. It was found that the inventive formulation; (1) reduces the time for a therapeutically effective level of photosensitizer to accumulate in diseased tissue; and, (2) reduces the time for achieving a sufficient ratio of photosensitizer in diseased tissue vs. healthy tissue. As a result, the formulation of the invention reduces the time interval between PS application/administration and irradiation (the drug-light interval or “DLI”) and can provide for a “same day” PDT treatment option. The inventive formulation can be used for PDT treatment regimes where photosensitizers are administered in at least one preselected dose, including a low concentration therapy for PDT. In particular, when meta-(Tetrahydroxyphenyl) Chlorin (m-THPC) is the photosensitizer, then a concentration of 0.8 mg/ml to 0.04 mg/ml in a mixture of pure propylene glycol and ethanol in a 3:2 volume ratio accumulates in diseased tissue and differentiates between diseased tissue and normal tissue sufficiently quickly for ‘one day’ or overnight administration and activation treatment procedures to be possible.
摘要翻译：在低剂量的疏水性光敏剂（PS）中使用低浓度制剂来呈现新的治疗方案，其显示改善的药物动力学和光动力学治疗（“PDT”）的有效方法。与标准剂量的标准光敏剂配方相比，新配方具有更好的药理作用。发现使用所公开的低浓度制剂的PDT治疗提供更准确，更有效和更方便的给药。发现本发明的制剂; （1）减少治疗有效水平的光敏剂累积在患病组织中的时间; 和（2）减少在病变组织中对光固化剂与健康组织的足够比例的时间。结果，本发明的制剂减少了PS施用/给药和照射之间的时间间隔（药物光间隔或“DLI”），并且可以提供“同一天”PDT治疗选择。本发明的制剂可用于PDT治疗方案，其中光敏剂以至少一种预选剂量施用，包括用于PDT的低浓度治疗。特别是当Meta-（四羟基苯基）二氢卟酚（m-THPC）是光敏剂时，在纯丙二醇和3:2体积比的乙醇混合物中的浓度为0.8mg / ml至0.04mg / ml，病变组织并且在病变组织和正常组织之间充分快速地分离“一天”或过夜施用和活化处理程序以使其成为可能。

8. 发明申请

US20060035952A1 Photosensitizer formulations and their use 有权
标题翻译：光敏剂配方及其用途
公开(公告)号：US20060035952A1
公开(公告)日：2006-02-16
申请号：US11153703
申请日：2005-06-15
申请人： Nikolay Nifantiev , Volker Albrecht
发明人： Nikolay Nifantiev , Volker Albrecht
IPC分类号： A61K31/409 , A61K31/366 , A61K31/195
CPC分类号： A61K31/195 , A61K31/366 , A61K31/409 , A61K41/0057 , A61K41/0061 , A61K41/0071
摘要： A low concentration formulation for hydrophobic photosensitizers (PS) and improved method for photodynamic therapy (“PDT”). It was found that PDT treatments using the disclosed low concentration formulations provide for more accurate, more efficient and more convenient dosing. It was found that the inventive formulation (1) reduces the time for a therapeutically effective level of photosensitizer to accumulate in diseased tissue and (2) reduces the time for achieving a sufficient ratio of photosensitizer in diseased tissue vs. healthy tissue. As a result, the formulation of the invention reduces the time interval between PS application/administration and irradiation (the drug-light interval or “DLI”) and can provide for a “same day” PDT treatment option. The inventive formulation can be used for PDT treatment regimes where photosensitizers are administered in at least one preselected dose, including a low concentration therapy for PDT. In particular, when meta Tetra-Hydroxy-Phenyl Chlorin (m-THPC) is the photosensitizer then a concentration of 0.8 mg/ml to 0.04 mg/ml in a mixture of pure propylene glycol and ethanol in a 3:2 volume ratio accumulates in diseased tissue and differentiates between diseased tissue and normal tissue sufficiently quickly for ‘one day’ or overnight administration and activation treatment procedures to be possible.
摘要翻译：疏水性光敏剂（PS）的低浓度配方和光动力疗法（“PDT”）的改进方法。发现使用所公开的低浓度制剂的PDT治疗提供更准确，更有效和更方便的给药。发现本发明的制剂（1）减少了治疗有效水平的光敏剂积累在患病组织中的时间，和（2）减少了在患病组织中与光健康组织相比达到足够的光敏剂比例的时间。结果，本发明的制剂减少了PS施用/给药和照射之间的时间间隔（药物光间隔或“DLI”），并且可以提供“同一天”PDT治疗选择。本发明的制剂可用于PDT治疗方案，其中光敏剂以至少一种预选剂量施用，包括用于PDT的低浓度治疗。特别地，当间苯四酚（m-THPC）是光敏剂时，在纯丙二醇和乙醇3:2体积比的混合物中的浓度为0.8mg / ml至0.04mg / ml，病变组织并且在病变组织和正常组织之间充分快速地分离“一天”或过夜施用和活化处理程序以使其成为可能。

9. 发明授权

US08492364B2 Methods and compositions relating to synthetic β-1,6 glucosamine oligosaccharides 有权
标题翻译：与合成的β-1,6葡糖胺寡糖有关的方法和组合物
公开(公告)号：US08492364B2
公开(公告)日：2013-07-23
申请号：US13055178
申请日：2009-07-21
申请人： Gerald B. Pier , Nikolay Nifantiev , Yury Tsvetkov , Marina Gening
发明人： Gerald B. Pier , Nikolay Nifantiev , Yury Tsvetkov , Marina Gening
IPC分类号： A61K31/70
CPC分类号： A61K39/085 , A61K47/6415 , A61K47/646 , A61K2039/55 , A61K2039/552 , A61K2039/575 , A61K2039/6037 , C07C327/32 , C07D207/46 , C07H3/06 , C07K16/1232 , C07K16/1271 , C07K2317/33 , Y02A50/407
摘要： The invention relates to the compositions of synthetic oligo-β-(1→6)-2-amino-2-deoxy-D-glucopyranosides conjugated to carriers, and methods for making and use same.
摘要翻译：本发明涉及与载体缀合的合成低聚β-（1-> 6）-2-氨基-2-脱氧-D-吡喃葡萄糖苷的组合物，以及制备和使用它们的方法。

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