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公开(公告)号：US10961181B2
公开(公告)日：2021-03-30
申请号：US16700304
申请日：2019-12-02
发明人： Yoshiro Niitsu , Victor Knopov , Joseph E. Payne , Zheng Hou , John A. Gaudette , Violetta Akopian , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Yasunobu Tanaka , Priya Karmali , Sridhar C. Nagarajan
IPC分类号： A61K31/713 , C07C237/08 , A61K47/54 , A61K9/00 , A61K9/10 , A61K9/127 , A61K47/18 , C12N15/113 , C07C323/60 , C07C333/04
摘要： Here described is a composition comprising a compound of formula I: wherein R1 and R2 is independently selected from a group consisting of C10 to C18 alkyl, C12 to C18 alkenyl, and oleoyl group; R3 and R4 are independently selected from a group consisting of C1 to C6 alkyl, and C2 to C6 alkanol; X is selected from a group consisting of —CH2—, —S—, and —O— or absent; Y is selected from —(CH2)n, —S(CH2)n, —O(CH2)n—, thiophene, —SO2(CH2)n—, and ester; n=1-4; a=1-4; b=1-4; c=1-4; and Z− is a counterion.
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公开(公告)号：US20180297938A1
公开(公告)日：2018-10-18
申请号：US15985614
申请日：2018-05-21
发明人： Yoshiro Niitsu , Joseph E. Payne , John A. Gaudette , Zheng Hou , Victor Knopov , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Yasunobu Tanaka , Violetta Akopian
IPC分类号： C07C237/22 , C07C235/48 , A61K47/55 , A61K9/127 , A61K31/713 , C07C233/21 , C07C235/08 , C12N15/113 , C07F9/10 , A61K31/07
摘要： Here described are compounds consisting of the structure (targeting molecule)m-linker-(targeting molecule)n, wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including these compounds which are useful for the targeting and delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.
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公开(公告)号：US20160137593A1
公开(公告)日：2016-05-19
申请号：US15005569
申请日：2016-01-25
发明人： Yoshiro Niitsu , Victor Knopov , Joseph E. Payne , Zheng Hou , John A. Gaudette , Violetta Akopian , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Yasunobu Tanaka , Priya Karmali , Sridhar C. Nagarajan
IPC分类号： C07C237/08 , C07C333/04 , A61K47/48 , C07C323/60
CPC分类号： C07C237/08 , A61K9/0019 , A61K9/10 , A61K9/1271 , A61K31/713 , A61K47/186 , A61K47/543 , C07C323/60 , C07C333/04 , C12N15/113
摘要： Here described are compounds of formula I: wherein R1 and R2 are independently selected from C10 to C18 alkyl, C12 to C18 alkenyl, and oleoyl; R3 and R4 are independently selected from C1 to C6 alkyl and C2 to C6 alkanol; X is selected from —CH2—, —S—, and —O—, or X is absent; Y is selected from —(CH2)n, —S(CH2)n—, —O(CH2)n—, -thiophene-, —SO2(CH2)n—, and ester; n=1-4; a=1-4; b=1-4; c=1-4; and Z− is a counterion. Also described herein are compositions and pharmaceutical formulations including compounds of formula I which are useful for the delivery of therapeutic agents, and methods of using these compositions and formulations.
摘要翻译： 这里描述的是式I化合物：其中R 1和R 2独立地选自C 10至C 18烷基，C 12至C 18烯基和油酰基; R 3和R 4独立地选自C 1至C 6烷基和C 2至C 6烷醇; X选自-CH 2 - ， - S - 和-O-，或X不存在; Y选自 - （CH 2）n，-S（CH 2）n - ， - O（CH 2）n - ， - 噻吩 - ， - SO 2（CH 2）n - n = 1-4; a = 1-4; b = 1-4; c = 1-4; 而Z-是反抗。 本文还描述了可用于递送治疗剂的组合物和药物制剂，包括式I化合物，以及使用这些组合物和制剂的方法。
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4.发明申请公开(公告)号：US20130164400A1
公开(公告)日：2013-06-27
申请号：US13669217
申请日：2012-11-05
发明人： Victor Knopov , Richard P. Witte , Priya Karmali , Robin Lee , David Webb
IPC分类号： A61K9/48
CPC分类号： A61K9/4833 , A61K9/1271 , A61K9/1272 , A61K9/1277 , A61K47/6911 , B01J13/00 , B01J13/04 , B01J13/12 , C12N15/111 , C12N15/88 , C12N2310/11 , C12N2310/14 , C12N2320/32
摘要： What is described is a process of forming lipid-nucleic acid nanoparticles simply and reproducibly under aseptic conditions comprising single use components.
摘要翻译： 描述的是在包含单次使用组分的无菌条件下简单且可重复地形成脂质 - 核酸纳米颗粒的方法。
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公开(公告)号：US20130115274A1
公开(公告)日：2013-05-09
申请号：US13669078
申请日：2012-11-05
发明人： Victor Knopov , Richard P. Witte , Priya Karmali , Robin Lee , David Webb , Violetta Akopian
IPC分类号： A61K9/127 , A61K31/7105 , B82Y5/00 , B82Y40/00
CPC分类号： C12N15/113 , A61K9/0019 , A61K9/10 , A61K9/1271 , A61K9/1272 , A61K9/1277 , A61K9/19 , A61K31/7105 , A61K31/713 , A61K47/12 , A61K47/26 , C12N2310/14 , C12N2320/32
摘要： What is described is a method for preparing a liposome that efficiently encapsulates a negatively charged therapeutic polymer, e.g., siRNA. The process involves preparing a lipid mixture comprising a cationic lipid in a water miscible organic solvent, such as ethanol, at a concentration of 2.3 mg/ml, and adding this solution to the polymer dissolved in water to a final concentration of 35% ethanol in water. The final charge ratio of drug:lipid is 1:2.5. The resulting nanoparticles have a mean size of 50 to 150 nm.
摘要翻译： 描述的是制备有效地包封带负电荷的治疗性聚合物例如siRNA的脂质体的方法。 该方法包括在水混合性有机溶剂如乙醇中制备含有阳离子脂质的浓度为2.3mg / ml的脂质混合物，并将该溶液加入到溶于水的聚合物中至终浓度为35％乙醇 水。 药物：脂质的最终充电比为1:2.5。 所得纳米颗粒的平均尺寸为50至150nm。
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公开(公告)号：US11103583B2
公开(公告)日：2021-08-31
申请号：US16460812
申请日：2019-07-02
发明人： Joseph E. Payne , John A. Gaudette , Zheng Hou , Mohammad Ahmadian , Lei Yu , Victor Knopov , Violetta Akopian , Priya Karmali , Richard P. Witte , Neda Safarzadeh , Wenbin Ying , Jun Zhang
IPC分类号： A61K47/20 , C07C323/60 , C07D333/38 , C07C271/16 , C07D333/40 , C07C317/44 , C07C333/04 , C07C235/08 , C07C237/08 , C07D207/16 , A61K47/14 , A61K9/127 , A61K47/18 , A61K47/22 , C07C237/16
摘要： The description is directed to ionizable lipids useful for enhancing the delivery of therapeutic agents in liposomes.
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公开(公告)号：US10441659B2
公开(公告)日：2019-10-15
申请号：US14872951
申请日：2015-10-01
发明人： Joseph E. Payne , John A. Gaudette , Zheng Hou , Mohammad Ahmadian , Lei Yu , Victor Knopov , Violetta Akopian , Priya Karmali , Richard P. Witte , Neda Safarzadeh , Wenbin Ying , Jun Zhang
IPC分类号： A61K47/14 , A61K47/20 , A61K47/18 , A61K47/22 , C07C271/16 , C07D333/40 , C07C317/44 , C07C333/04 , C07C235/08 , C07C237/08 , C07D207/16 , A61K9/127 , C07D333/38 , C07C323/60 , C07C237/16
摘要： The description is directed to ionizable lipids useful for enhancing the delivery of therapeutic agents in liposomes.
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公开(公告)号：US10195145B2
公开(公告)日：2019-02-05
申请号：US15283179
申请日：2016-09-30
发明人： Yoshiro Niitsu , Victor Knopov , Joseph E. Payne , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Violetta Akopian , Yasunobu Tanaka , Elena Feinstein , Sharon Avkin-Nahum , Hagar Kalinski , Igor Mett , Kenjiro Minomi , Wenbin Ying , Yun Liu
IPC分类号： C12N15/113 , A61K9/127 , C12N15/11 , A61K31/713 , C07H21/02
摘要： What is described is a method for treating a fibrotic disease by administering a pharmaceutical composition comprising a drug carrier, which comprises a lipid and a retinoid, and a double-stranded nucleic acid molecule, which comprises an antisense sequence to mRNA encoding human hsp47.
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公开(公告)号：US10155945B2
公开(公告)日：2018-12-18
申请号：US15430387
申请日：2017-02-10
发明人： Victor Knopov , Richard P. Witte , Priya Karmali , Robin Lee , David Webb , Violetta Akopian
IPC分类号： C12N15/113 , A61K31/7105 , A61K9/00 , A61K9/10 , A61K9/127 , A61K9/19 , A61K31/713 , A61K47/12 , A61K47/26
摘要： What is described is a method for preparing a liposome that efficiently encapsulates a negatively charged therapeutic polymer, e.g., siRNA. The process involves preparing a lipid mixture comprising a cationic lipid in a water miscible organic solvent, such as ethanol, at a concentration of 2.3 mg/ml, and adding this solution to the polymer dissolved in water to a final concentration of 35% ethanol in water. The final charge ratio of drug:lipid is 1:2.5. The resulting nanoparticles have a mean size of 50 to 150 nm.
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公开(公告)号：US20170152516A1
公开(公告)日：2017-06-01
申请号：US15430387
申请日：2017-02-10
发明人： Victor Knopov , Richard P. Witte , Priya Karmali , Robin Lee , David Webb , Violetta Akopian
IPC分类号： C12N15/113 , A61K31/713 , A61K47/12 , A61K9/19 , A61K9/127 , A61K47/26
CPC分类号： C12N15/113 , A61K9/0019 , A61K9/10 , A61K9/1271 , A61K9/1272 , A61K9/1277 , A61K9/19 , A61K31/7105 , A61K31/713 , A61K47/12 , A61K47/26 , C12N2310/14 , C12N2320/32
摘要： What is described is a method for preparing a liposome that efficiently encapsulates a negatively charged therapeutic polymer, e.g., siRNA. The process involves preparing a lipid mixture comprising a cationic lipid in a water miscible organic solvent, such as ethanol, at a concentration of 2.3 mg/ml, and adding this solution to the polymer dissolved in water to a final concentration of 35% ethanol in water. The final charge ratio of drug:lipid is 1:2.5. The resulting nanoparticles have a mean size of 50 to 150 nm.
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