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1. 发明申请

WO2009047006A3 AMPHOTERIC LIPOSOMES COMPRISING NEUTRAL LIPIDS 审中-公开
标题翻译：包含中性脂肪的大肠杆菌
公开(公告)号：WO2009047006A3
公开(公告)日：2009-09-24
申请号：PCT/EP2008008621
申请日：2008-10-12
申请人： NOVOSOM AG , PANZNER STEFFEN , LUTZ SILKE , SIEPI EVGENIOS , MULLER CLAUDIA , VINZENS UTE
发明人： PANZNER STEFFEN , LUTZ SILKE , SIEPI EVGENIOS , MULLER CLAUDIA , VINZENS UTE
IPC分类号： A61K9/127 , A61K8/14
CPC分类号： C07J41/00 , A61K8/14 , A61K8/553 , A61K8/63 , A61K9/127 , A61K9/1272 , A61K31/575 , A61K31/58 , A61Q19/00 , C07J43/00 , Y02P20/582
摘要： An amphoteric liposome comprising neutral lipids wherein said neutral lipids are selected from the group comprising cholesterol or mixtures of cholesterol and at least one neutral or zwitterionic lipid and wherein K (neutral) of said mixtures is 0.3 or less. Said amphoteric liposome may encapsulate an active agent, such as nucleic acid therapeutics. Also disclosed are pharmaceutical compositions comprising said amphoteric liposomes as a carrier for the delivery or targeted delivery of active agents or ingredients.
摘要翻译：一种包含中性脂质的两性脂质体，其中所述中性脂质选自胆固醇或胆固醇和至少一种中性或两性离子脂质的混合物，其中所述混合物的K（中性）为0.3以下。所述两性脂质体可以包封活性剂，例如核酸治疗剂。还公开了包含所述两性脂质体作为用于递送或靶向递送活性剂或成分的载体的药物组合物。

2. 发明申请

WO2008074487A3 LIPIDS AND LIPID ASSEMBLIES COMPRISING TRANSFECTION ENHANCER ELEMENTS 审中-公开
标题翻译：包含转运增强元件的脂肪和脂肪组合物
公开(公告)号：WO2008074487A3
公开(公告)日：2009-04-23
申请号：PCT/EP2007011187
申请日：2007-12-19
申请人： NOVOSOM AG , PANZNER STEFFEN , LUTZ SILKE , SIEPI EVGENIOS , REINSCH CHRISTIAN , MULLER CLAUDIA
发明人： PANZNER STEFFEN , LUTZ SILKE , SIEPI EVGENIOS , REINSCH CHRISTIAN , MULLER CLAUDIA
IPC分类号： A61K48/00 , A61K47/48
CPC分类号： A61K9/1272 , A61K9/127 , A61K31/7052 , A61K47/542 , A61K47/544 , A61K47/545 , A61K47/554 , A61K47/6911 , A61K48/0008 , A61K48/0025 , A61K48/0033 , A61K48/0041 , C07C229/24 , C12N15/88 , Y02P20/582
摘要： Lipid assemblies, such as liposomes, comprising transfection enhancer elements (TEE's), which are complexed with the lipid assemblies by means of ionic interactions, or lipids incorporating such TEE's are disclosed for enhancing the fusogenicity of the lipid assemblies. The TEE's have the formula: hydrophobic moiety - pH sensitive hydrophilic moiety (II). The pH sensitive hydrophilic moiety of each TEE is a weak acid having a pka of between (2) and (6) or a zwitterionic structure comprising a combination of acidic groups with weak bases having a pKa of between (3) and (8). Lipids incorporating one or more such TEEs have the formula (I): Lipid moiety- [Hydrophobic moiety - pH sensitive hydrophilic moiety] (I).
摘要翻译：公开了脂质体组合物，例如脂质体，其包含通过离子相互作用与脂质组合物复合的转染增强子元件（TEE）或掺入这种TEE的脂质，用于增强脂质组件的融合性。 TEE具有以下配方：疏水部分 - pH敏感的亲水部分（II）。每个TEE的pH敏感亲水部分是具有（2）和（6）之间pka的弱酸或包含具有pKa（3）和（8）之间的弱碱基的酸性基团的组合的两性离子结构。掺入一种或多种这样的TEE的脂质具有式（I）：脂质部分 - [疏水部分 - pH敏感的亲水部分]（I）。

3. 发明申请

WO2008043575A2 IMPROVEMENTS IN OR RELATING TO AMPHOTERIC LIPOSOMES, A METHOD OF FORMULATING AN AMPHOTERIC LIPOSOME AND A METHOD OF LOADING AN AMPHOTERIC LIPOSOME 审中-公开
标题翻译：对AMPHTERIC LIPOSOMES的改善或相关的方法，制备AMPHTERIC脂质体的方法和装载AMPHTERIC脂质体的方法
公开(公告)号：WO2008043575A2
公开(公告)日：2008-04-17
申请号：PCT/EP2007008917
申请日：2007-10-12
申请人： NOVOSOM AG , PANZNER STEFFEN , LUTZ SILKE , SIEPI EVGENIOS , MULLER CLAUDIA
发明人： PANZNER STEFFEN , LUTZ SILKE , SIEPI EVGENIOS , MULLER CLAUDIA
IPC分类号： A61K9/127 , A61K8/14
CPC分类号： A61K9/127 , A61K9/1272 , A61K31/713 , Y02P20/582
摘要： An amphoteric liposome composed of a mixture of lipids, said mixture comprising a cationic amphiphile, an anionic amphiphile and optionally one or more neutral amphiphiles, at least one of said cationic and anionic amphiphiles being chargeable and the respective amounts of said cationic and anionic amphiphiles being selected such there is a stoichiometric excess of positively charged cationic amphiphile at a first lower pH, a stoichiometric excess of negatively charged anionic amphiphile at a second higher pH and said mixture has an isoelectric point intermediate said first and second pHs; characterised in that said positively charged cationic and negatively charged anionic amphiphiles are adapted to form a lipid salt with one another at said isoelectric point. Also disclosed are methods of predicting the fusogenicity of an amphoteric liposome at a given pH, formulating an amphoteric liposome and loading an amphoteric liposome with a cargo moiety.
摘要翻译：由脂质混合物组成的两性脂质体，所述混合物包含阳离子两亲物，阴离子两亲物和任选的一个或多个中性两亲物，所述阳离子和阴离子两亲物中的至少一个是可带电的，并且相应量的所述阳离子和阴离子两亲物为选择这样，在第二较低pH下，在第一较低pH下具有化学计量过量的带正电荷的阳离子两亲物，在第二较高pH下具有化学计量过量的带负电荷的阴离子两亲物，并且所述混合物具有介于所述第一和第二pH之间的等电点; 其特征在于所述带正电荷的阳离子和带负电荷的阴离子两亲物适于在所述等电点处彼此形成脂质盐。还公开了在给定pH下预测两性脂质体的融合性的方法，配制两性脂质体并加载具有货物部分的两性脂质体。

4. 发明专利

CA2665783C IMPROVEMENTS IN OR RELATING TO AMPHOTERIC LIPOSOMES, A METHOD OF FORMULATING AN AMPHOTERIC LIPOSOME AND A METHOD OF LOADING AN AMPHOTERIC LIPOSOME 未知
公开(公告)号：CA2665783C
公开(公告)日：2015-12-15
申请号：CA2665783
申请日：2007-10-12
申请人： NOVOSOM AG
发明人： PANZNER STEFFEN , LUTZ SILKE , SIEPI EVGENIOS , MULLER CLAUDIA
IPC分类号： A61K9/127 , A61K8/14
摘要： An amphoteric liposome composed of a mixture of lipids, said mixture comprising a cationic amphiphile, an anionic amphiphile and optionally one or more neutral amphiphiles, at least one of said cationic and anionic amphiphiles being chargeable and the respective amounts of said cationic and anionic amphiphiles being selected such there is a stoichiometric excess of positively charged cationic amphiphile at a first lower pH, a stoichiometric excess of negatively charged anionic amphiphile at a second higher pH and said mixture has an isoelectric point intermediate said first and second pHs; characterised in that said positively charged cationic and negatively charged anionic amphiphiles are adapted to form a lipid salt with one another at said isoelectric point. Also disclosed are methods of predicting the fusogenicity of an amphoteric liposome at a given pH, formulating an amphoteric liposome and loading an amphoteric liposome with a cargo moiety.

5. 发明专利

AU2007306556A1 Improvements in or relating to amphoteric liposomes 未知
公开(公告)号：AU2007306556A1
公开(公告)日：2008-04-17
申请号：AU2007306556
申请日：2007-10-12
申请人： NOVOSOM AG
发明人： LUTZ SILKE , SIEPI EVGENIOS , MULLER CLAUDIA , PANZNER STEFFEN
IPC分类号： A61K8/14 , A61K9/127

6. 发明专利

CA2665783A1 IMPROVEMENTS IN OR RELATING TO AMPHOTERIC LIPOSOMES, A METHOD OF FORMULATING AN AMPHOTERIC LIPOSOME AND A METHOD OF LOADING AN AMPHOTERIC LIPOSOME 未知
公开(公告)号：CA2665783A1
公开(公告)日：2008-04-17
申请号：CA2665783
申请日：2007-10-12
申请人： NOVOSOM AG
发明人： MULLER CLAUDIA , PANZNER STEFFEN , SIEPI EVGENIOS , LUTZ SILKE
IPC分类号： A61K9/127 , A61K8/14
摘要： An amphoteric liposome composed of a mixture of lipids, said mixture comp rising a cationic amphiphile, an anionic amphiphile and optionally one or mo re neutral amphiphiles, at least one of said cationic and anionic amphiphile s being chargeable and the respective amounts of said cationic and anionic a mphiphiles being selected such there is a stoichiometric excess of positivel y charged cationic amphiphile at a first lower pH, a stoichiometric excess o f negatively charged anionic amphiphile at a second higher pH and said mixtu re has an isoelectric point intermediate said first and second pHs; characte rised in that said positively charged cationic and negatively charged anioni c amphiphiles are adapted to form a lipid salt with one another at said isoe lectric point. Also disclosed are methods of predicting the fusogenicity of an amphoteric liposome at a given pH, formulating an amphoteric liposome and loading an amphoteric liposome with a cargo moiety.

7. 发明专利

CA2702103A1 IMPROVEMENTS IN OR RELATING TO AMPHOTARIC LIPOSOMES COMPRISING NEUTRAL LIPIDS 未知
公开(公告)号：CA2702103A1
公开(公告)日：2009-04-16
申请号：CA2702103
申请日：2008-10-12
申请人： NOVOSOM AG
发明人： PANZNER STEFFEN , LUTZ SILKE , SIEPI EVGENIOS , MULLER CLAUDIA , VINZENS UTE
IPC分类号： C07J41/00 , A61K8/14 , A61K9/127 , A61K31/575 , A61K31/58 , A61P35/00 , A61P37/02 , C07J43/00
摘要： An amphoteric liposome comprising neutral lipids wherein said neutral lipids are selected from the group comprising cholesterol or mixtures of cholesterol and at least one neutral or zwitterionic lipid and wherein K (neutral) of said mixtures is 0.3 or less. Said amphoteric liposome may encapsulate an active agent, such as nucleic acid therapeutics. Also disclosed are pharmaceutical compositions comprising said amphoteric liposomes as a carrier for the delivery or targeted delivery of active agents or ingredients.

8. 发明专利

AU2008309880A1 Amphoteric liposomes comprising neutral lipids 未知
公开(公告)号：AU2008309880A1
公开(公告)日：2009-04-16
申请号：AU2008309880
申请日：2008-10-12
申请人： NOVOSOM AG
发明人： VINZENS UTE , PANZNER STEFFEN , LUTZ SILKE , SIEPI EVGENIOS , MULLER CLAUDIA
IPC分类号： A61K9/127 , A61K8/14 , A61K31/575 , A61K31/58 , A61P35/00 , A61P37/02 , C07J41/00 , C07J43/00

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