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公开(公告)号：US20180065918A1
公开(公告)日：2018-03-08
申请号：US15492898
申请日：2017-04-20
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Akin Akinc , Jayaprakash K. Nair , Muthusamy Jayaraman , Martin Maier
IPC分类号： C07C219/06 , C07C323/25 , C07C271/10 , C07C233/36 , A61K9/127 , C07C209/78 , A61K31/325 , A61K47/34
摘要： Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.
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公开(公告)号：US20230174459A1
公开(公告)日：2023-06-08
申请号：US17863885
申请日：2022-07-13
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Akin Akinc , Jayaprakash K. Nair , Muthusamy Jayaraman , Martin Maier
IPC分类号： C07C219/06 , A61K9/127 , A61K31/325 , C07C209/78 , C07C233/36 , C07C271/10 , C07C323/25
CPC分类号： C07C219/06 , A61K9/1272 , A61K9/1273 , A61K31/325 , C07C209/78 , C07C233/36 , C07C271/10 , C07C323/25 , A61K47/34
摘要： Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.
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公开(公告)号：US11420931B2
公开(公告)日：2022-08-23
申请号：US16713712
申请日：2019-12-13
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Akin Akinc , Jayaprakash K. Nair , Muthusamy Jayaraman , Martin Maier
IPC分类号： C07C219/06 , A61K9/127 , A61K31/325 , C07C209/78 , C07C233/36 , C07C271/10 , C07C323/25 , A61K47/34
摘要： Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.
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公开(公告)号：US20190167800A1
公开(公告)日：2019-06-06
申请号：US16123209
申请日：2018-09-06
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Nair , Martin Maier , Laxman Eltepu
IPC分类号： A61K47/44 , C07D317/28 , A61K47/10 , C12N15/113 , C07C229/30 , C07D319/06 , C07D203/10 , A61K31/713 , A61K39/39 , A61K47/28 , C07C229/08 , C07C271/12 , C07C251/38 , C07D317/72 , A61K9/127 , C07C323/25 , C12N15/11 , A61K47/18 , C07D491/113 , C07C271/20 , C07C237/16 , A61K31/7088 , C07D405/12 , C07D317/46 , A61K47/20 , A61K39/00 , C07C251/78 , C07D317/44 , C07D491/056
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalky, ω-phosphoalkyl or ω-thiophosphoalkyl.
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公开(公告)号：US10117941B2
公开(公告)日：2018-11-06
申请号：US15603069
申请日：2017-05-23
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Nair , Martin Maier , Laxman Eltepu
IPC分类号： A61K39/39 , C07D203/10 , A61K47/18 , A61K47/28 , A61K31/713 , A61K39/00 , A61K47/44 , C07C229/08 , C07C229/30 , C07D317/28 , C07D319/06 , C12N15/113 , A61K9/127 , C12N15/11 , A61K47/10 , A61K47/20 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , A61K31/7088 , C07D317/44 , C07D317/46 , C07D317/72 , C07D405/12 , C07D491/056 , C07D491/113
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalky, ω-phosphoalkyl or ω-thiophosphoalkyl.
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公开(公告)号：US09663449B2
公开(公告)日：2017-05-30
申请号：US14149496
申请日：2014-01-07
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Akin Akinc , Jayaprakash K. Nair , Muthusamy Jayaraman , Martin Maier
IPC分类号： A61K9/48 , C07C229/00 , A61K9/127 , A61K47/34 , C07C233/36 , C07C209/78 , C07C219/06 , A61K31/325 , C07C271/10 , C07C323/25
摘要： Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.
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公开(公告)号：US20230381319A1
公开(公告)日：2023-11-30
申请号：US18110791
申请日：2023-02-16
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Nair , Martin Maier , Laxman Eltepu
IPC分类号： A61K47/44 , A61K39/39 , C07C229/08 , A61K31/713 , C07D319/06 , C07D317/28 , C07D203/10 , C07C229/30 , C12N15/113 , A61K39/00 , C12N15/11 , A61K9/127 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , A61K31/7088 , C07D317/44 , C07D317/46 , C07D317/72 , C07D405/12 , C07D491/056 , C07D491/113
CPC分类号： A61K47/44 , A61K39/39 , C07C229/08 , A61K31/713 , C07D319/06 , C07D317/28 , C07D203/10 , C07C229/30 , C12N15/113 , A61K39/00 , C12N15/111 , A61K9/1272 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , A61K31/7088 , C07D317/44 , C07D317/46 , C07D317/72 , C07D405/12 , C07D491/056 , C07D491/113 , A61K2039/55555 , A61K2039/55561 , C12N2310/14 , C12N2310/3515 , C12N2320/32 , Y02A50/30
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure (I) wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalky, ω-phosphoalkyl or ω-thiophosphoalkyl.
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公开(公告)号：US20210162053A1
公开(公告)日：2021-06-03
申请号：US17065208
申请日：2020-10-07
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Nair , Martin Maier , Laxman Eltepu
IPC分类号： A61K47/44 , A61K39/39 , C07C229/08 , A61K31/713 , C07D319/06 , C07D317/28 , C07D203/10 , C07C229/30 , C12N15/113 , A61K39/00 , C12N15/11 , A61K9/127 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , A61K31/7088 , C07D317/44 , C07D317/46 , C07D317/72 , C07D405/12 , C07D491/056 , C07D491/113
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure (I) wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylheterocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalkyl, ω-phosphoalkyl or ω-thiophosphoalkyl.
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公开(公告)号：US10821186B2
公开(公告)日：2020-11-03
申请号：US16123209
申请日：2018-09-06
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Nair , Martin Maier , Laxman Eltepu
IPC分类号： A61K47/44 , A61K39/39 , C07C229/08 , A61K31/713 , C07D319/06 , C07D317/28 , C07D203/10 , C07C229/30 , C12N15/113 , A61K39/00 , C12N15/11 , A61K9/127 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , A61K31/7088 , C07D317/44 , C07D317/46 , C07D317/72 , C07D405/12 , C07D491/056 , C07D491/113
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalky, ω-phosphoalkyl or ω-thiophosphoalkyl.
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公开(公告)号：US20180043009A1
公开(公告)日：2018-02-15
申请号：US15603069
申请日：2017-05-23
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Nair , Martin Maier , Laxman Eltepu
IPC分类号： A61K39/39 , A61K31/713 , A61K39/00 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , C07C229/08 , C07C229/30 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , C07D203/10 , C07D317/28 , C07D319/06 , C12N15/11 , C12N15/113 , A61K9/127
CPC分类号： A61K47/44 , A61K9/1272 , A61K31/7088 , A61K31/713 , A61K39/00 , A61K39/39 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , A61K2039/55555 , A61K2039/55561 , C07C229/08 , C07C229/30 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , C07D203/10 , C07D317/28 , C07D317/44 , C07D317/46 , C07D317/72 , C07D319/06 , C07D405/12 , C07D491/056 , C07D491/113 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/3515 , C12N2320/32 , Y02A50/464
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30alkyl, optionally substituted C10-C30alkenyl, optionally substituted C10-C30alkynyl, optionally substituted C10-C30acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10alkyl, optionally substituted C2-C10alkenyl, optionally substituted C2-C10alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalky, ω-phosphoalkyl or ω-thiophosphoalkyl.
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