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11. 发明授权

US09999673B2 PEGylated lipids and their use for drug delivery 有权
公开(公告)号：US09999673B2
公开(公告)日：2018-06-19
申请号：US13979336
申请日：2012-01-11
申请人： Kallanthottathil G. Rajeev , Muthiah Manoharan , Muthusamy Jayaraman , Martin Maier , Jayaprakash K. Nair , David Butler
发明人： Kallanthottathil G. Rajeev , Muthiah Manoharan , Muthusamy Jayaraman , Martin Maier , Jayaprakash K. Nair , David Butler
IPC分类号： A61K47/18 , C07C235/06 , C07C271/16 , C07D207/12 , C07D307/20 , C07D207/14 , C07D307/12 , C08G65/329 , A61K47/48
CPC分类号： A61K47/18 , A61K47/6911 , C07C235/06 , C07C271/16 , C07D207/12 , C07D207/14 , C07D307/12 , C07D307/20 , C08G65/329 , C08L2203/02
摘要： The invention provides poly(ethylene glycol)-lipid conjugates for use in drug delivery.

12. 发明授权

US08999351B2 Lipids and compositions for the delivery of therapeutics 有权
标题翻译：用于递送治疗剂的脂质和组合物
公开(公告)号：US08999351B2
公开(公告)日：2015-04-07
申请号：US13128287
申请日：2009-11-10
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Narayanannair , Martin Maier , Laxman Eltepu
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Narayanannair , Martin Maier , Laxman Eltepu
IPC分类号： A61K39/12 , A61K9/127 , A61K39/00 , C12N15/11
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 (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.
摘要翻译：本发明提供有利地用于脂质颗粒以用于体内递送治疗剂至细胞的脂质。特别地，本发明提供具有以下结构（I）的脂质，其中R1和R2各自独立地为任何取代的C 10 -C 30烷基，任选取代的C 10 -C 30烯基，任选取代的C 10 -C 30炔基，任选取代的C 10 -C 30 酰基或 - 连接子 - 配体; R 3为H，任选取代的C 1 -C 10烷基，任选取代的C 2 -C 10烯基，任选取代的C 2 -C 10炔基，烷基硫代烷基磷酸酯，烷基硫代磷酸酯，烷基二硫代磷酸酯，烷基膦酸酯，烷基胺，羟基烷基，ω-氨基烷基，ω-（取代的）氨基烷基， ω-磷酸烷基酯，ω-硫代磷酰基烷基酯，任选取代的聚乙二醇（PEG，mw 100-40K），任选取代的mPEG（mw 120-40K），杂芳基，杂环或连接基 - 配体; E是O，S，N（Q），C（O），N（Q）C（O），C（O）N（Q），（Q）），S（O），NS（O）2N（Q），S（O）2，N（Q）S（O）2，SS，O = N，芳基，杂芳基，环状或杂环; Q为H，烷基，ω-氨基烷基，ω-（取代）氨基烷基，ω-磷酸烷基或ω-硫代磷酰基烷基。

13. 发明申请

US20120095075A1 NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS 审中-公开
标题翻译：用于输送治疗药物的新型脂肪和组合物
公开(公告)号：US20120095075A1
公开(公告)日：2012-04-19
申请号：US13211150
申请日：2011-08-16
申请人： Muthiah MANOHARAN , Kallanthottathil G. Rajeev , David Butler , Narayanannair K. Jayaprakash , Muthusamy Jayaraman , Laxman Eltepu
发明人： Muthiah MANOHARAN , Kallanthottathil G. Rajeev , David Butler , Narayanannair K. Jayaprakash , Muthusamy Jayaraman , Laxman Eltepu
IPC分类号： A61K31/7088 , C07D491/113 , A61K31/713 , C07D491/18 , C07H15/26 , A61K47/44 , C07D491/056 , C07D491/153
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:
摘要翻译：本发明提供有利地用于脂质颗粒以用于体内递送治疗剂至细胞的脂质。特别地，本发明提供具有以下结构的脂质：

14. 发明授权

US09186325B2 Lipids and compositions for the delivery of therapeutics 有权
标题翻译：用于递送治疗剂的脂质和组合物
公开(公告)号：US09186325B2
公开(公告)日：2015-11-17
申请号：US13128283
申请日：2009-11-10
申请人： Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev , Laxman Eltepu , Steven Ansell , Jianxin Chen
发明人： Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev , Laxman Eltepu , Steven Ansell , Jianxin Chen
IPC分类号： A61K39/12 , A61K9/127 , A61K39/00 , C12N15/11
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 formula (I) provides lipids having the following structure XXXIII 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, alky lhetro cycle, 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; and E is C(O)O or OC(O).
摘要翻译：本发明提供有利地用于脂质颗粒以用于体内递送治疗剂至细胞的脂质。具体地，本发明式（I）提供具有以下结构XXXIII的脂质，其中：R1和R2各自独立地为任何取代的C 10 -C 30烷基，任选取代的C 10 -C 30烯基，任选取代的C 10 -C 30炔基，任选取代的 C10-C30酰基或 - 连接子 - 配体; R 3是H，任选取代的C 1 -C 10烷基，任选取代的C 2 -C 10烯基，任选取代的C 2 -C 10炔基，烷基杂芳基，烷基磷酸酯，烷基硫代磷酸酯，烷基磷酸二烷基酯，烷基膦酸酯，烷基胺，羟基烷基，ω-氨基烷基，ω-（取代的）氨基烷基，ω-磷酸烷基酯，ω-硫代磷酰基烷基，任选取代的聚乙二醇（PEG，mw 100-40K），任选取代的mPEG（mw 120-40K），杂芳基，杂环或连接体 - 配体; 并且E是C（O）O或OC（O）。

15. 发明授权

US08575123B2 Site-specific delivery of nucleic acids by combining targeting ligands with endosomolytic components 有权
标题翻译：通过将靶向配体与内体分解组分结合来进行核酸的位点特异性递送
公开(公告)号：US08575123B2
公开(公告)日：2013-11-05
申请号：US12936961
申请日：2009-04-10
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , David Butler , Muthusamy Jayaraman
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , David Butler , Muthusamy Jayaraman
IPC分类号： A61K48/00 , C12N15/11 , C12N15/00 , A01N63/00 , A01N65/00
CPC分类号： A61K47/554 , A61K47/545 , A61K47/549 , A61K47/551 , A61K48/0008 , C12N15/111 , C12N15/1137 , C12N15/87 , C12N2310/11 , C12N2310/14 , C12N2310/315 , C12N2310/322 , C12N2310/346 , C12N2310/351 , C12N2310/3513 , C12N2320/32 , C12Y304/21021
摘要： The invention relates to compositions and methods for site-specific delivery of nucleic acids by combining them with targeting ligands and endosomolytic components.
摘要翻译：本发明涉及通过将它们与靶向配体和内体分解组分组合而用于位点特异性递送核酸的组合物和方法。

16. 发明授权

US08507455B2 Folate conjugates 有权
标题翻译：叶酸共轭物
公开(公告)号：US08507455B2
公开(公告)日：2013-08-13
申请号：US12328537
申请日：2008-12-04
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , Jayaprakash K. Narayanannair
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , Jayaprakash K. Narayanannair
IPC分类号： C12N15/11 , A61K48/00 , C07H21/02 , C07H21/04
CPC分类号： C12N15/113 , A61K47/55
摘要： The present invention provides iRNA agent including at least one monomer having the structure shown in formula (I′) wherein: A and B are each independently for each occurrence O, N(RN) or S; X is H, a protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z′)(Z″)O-nucleoside, —P(Z′)(Z″)O-oligonucleotide, a lipid, a PEG, a steroid, a polymer, —P(Z′)(Z″)O-L6-Q′-L7-OP(Z′″)(Z′″″)O-oligonucleotide, a nucleotide, or an oligonucleotide; Y is H, a protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z′)(Z″)O-nucleoside, —P(Z′)(Z″)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z′)(Z″)O-L6-Q′-L7-OP(Z′″)(Z′″″)O-oligonucleotide, a nucleotide, or an oligonucleotide; R is folate, a folate analog a folate mimic or a folate receptor binding ligand; L6 and L7 are each independently for each occurrence —(CH2)n—, —C(R′)(R″)(CH2)n—, —(CH2)nC(R′)(R″)—, —(CH2CH2O)mCH2CH2—, or —(CH2CH2O)mCH2CH2NH—; Q′ is NH, O, S, CH2, C(O)O, C(O)NH, —NH—CH(Ra)—C(O)—, —C(O)—CH(Ra)—NH—, CO, where Ra is H or amino acid side chain; R′ and R″ are each independently H, CH3, OH, SH, NH2, NH(Alkyl=Me, Et, Pr, isoPr, Bu, Bn) or N(diAlkyl=Me2, Et2, Bn2); Z′, Z″, Z′″ and Z″″ are independently O or S; n represent independently for each occurrence 1-20; and m represent independently for each occurrence 0-50.
摘要翻译：本发明提供包含至少一种具有式（I'）所示结构的单体的iRNA试剂，其中：A和B各自独立地为O，N（RN）或S; X是H，保护基，磷酸基，磷酸二酯基，活化磷酸酯基，活化亚磷酸酯基，亚磷酰胺，固体载体，-P（Z'）（Z“）O-核苷，-P （Z'）（Z“）O-寡核苷酸，脂质，PEG，类固醇，聚合物，-P（Z'）（Z”）O-L6-Q'-L7-OP（Z“ '）（Z“”）O-寡核苷酸，核苷酸或寡核苷酸; Y是H，保护基，磷酸基，磷酸二酯基，活化磷酸酯基，活化亚磷酸酯基，亚磷酰胺，固体载体，-P（Z'）（Z“）O-核苷，-P （Z'）（Z“）（Z”）O-寡核苷酸，脂质，PEG，类固醇，亲脂性，聚合物，-P（Z'）（Z“）O-L6-Q'-L7-OP Z“'）（Z”“）O-寡核苷酸，核苷酸或寡核苷酸; R是叶酸，叶酸类似物叶酸类似物或叶酸受体结合配体; L 6和L 7各自独立地为 - （CH 2）n - ， - C（R'）（R“）（CH 2）n - ， - （CH 2）n C（R'）（R” （CH 2 CH 2 O）mCH 2 CH 2 - 或 - （CH 2 CH 2 O）m CH 2 CH 2 NH-; Q'是NH，O，S，CH2，C（O）O，C（O）NH，-NH-CH（Ra）-C（O） - ， - （O）-CH（Ra），CO，其中Ra为H或氨基酸侧链; R'和R“各自独立地为H，CH 3，OH，SH，NH 2，NH（烷基= Me，Et，Pr，isoPr，Bu，Bn）或N（二烷基= Me 2，Et 2，Bn 2）; Z'，Z“，Z”“和”Z“独立地为O或S; n每次出现1-20，独立地表示1-20; 而m代表每次出现的0-50。

17. 发明申请

US20120128760A1 LIPID COMPOSITIONS 有权
标题翻译：脂肪组合物
公开(公告)号：US20120128760A1
公开(公告)日：2012-05-24
申请号：US13318600
申请日：2010-05-05
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Michael E. Jung
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Michael E. Jung
IPC分类号： A61K31/7088 , A61K31/713 , A61P35/00 , A61K47/42 , C07D295/13 , C07D295/14 , A61K9/127 , A61K47/34
CPC分类号： A61K47/22 , A61K9/1272 , C07D295/13 , C12N15/113 , C12N15/1137 , C12N2310/14 , Y02A50/463
摘要： Disclosed herein are lipid compositions comprising a cationic lipid of formula (I), a neutral lipid, a sterol and a PEG or PEG-modified lipid, wherein formula (I) is (F). Also disclosed are methods of producing the cationic lipid of formula (I).
摘要翻译：本文公开了包含式（I）的阳离子脂质，中性脂质，固醇和PEG或PEG修饰的脂质的脂质组合物，其中式（I）是（F）。还公开了制备式（I）的阳离子脂质的方法。

18. 发明授权

US09687550B2 Compositions for nucleic acid delivery 有权
公开(公告)号：US09687550B2
公开(公告)日：2017-06-27
申请号：US13514352
申请日：2010-12-07
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Mamta Kapoor , Rajesh Kumar Kainthan
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Mamta Kapoor , Rajesh Kumar Kainthan
IPC分类号： C07C229/12 , A61K47/18 , C07C217/08 , C07C219/08 , C07C251/40 , C07C271/12 , C07C271/20 , C07C323/25 , C07D317/28 , C07D317/44 , C07D317/72 , C07D491/10 , C12N15/88 , A61K31/7105 , A61K31/713 , A61K47/22
CPC分类号： A61K47/18 , A61K31/7105 , A61K31/713 , A61K47/186 , A61K47/22 , C07C217/08 , C07C219/08 , C07C229/12 , C07C251/40 , C07C271/12 , C07C271/20 , C07C323/25 , C07C2601/02 , C07D317/28 , C07D317/44 , C07D317/72 , C07D491/10 , C12N15/88
摘要： The present invention is based, in part, upon the discovery of charged lipids that provide advantages when used in lipid particles for the in vivo delivery of a therapeutic agent. As such, described herein are compounds useful for delivering a nucleic acid to a cell.

19. 发明授权

US09220683B2 Lipids and compositions for the delivery of therapeutics 有权
标题翻译：用于递送治疗剂的脂质和组合物
公开(公告)号：US09220683B2
公开(公告)日：2015-12-29
申请号：US13128253
申请日：2009-11-10
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , David Butler , Jayaprakash K. Narayanannair , Muthusamy Jayaraman , Laxmab Eltepu
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , David Butler , Jayaprakash K. Narayanannair , Muthusamy Jayaraman , Laxmab Eltepu
IPC分类号： A61K39/12 , A61K9/127 , A61K39/00 , C12N15/11
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 structures: (Formula (I) or (XXXV)).
摘要翻译：本发明提供有利地用于脂质颗粒以用于体内递送治疗剂至细胞的脂质。特别地，本发明提供具有以下结构的脂质：（式（I）或（XXXV））。

20. 发明申请

US20120101148A1 LIPID FORMULATION 审中-公开
标题翻译：脂质配方
公开(公告)号：US20120101148A1
公开(公告)日：2012-04-26
申请号：US13147189
申请日：2010-01-29
申请人： Akin Aking , William Querbes , Frances M.P. Wong , Joseph R. Dorkin , Xiaojun Qin , William Cantley , Anna Borodovsky , Soma De , Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev
发明人： Akin Aking , William Querbes , Frances M.P. Wong , Joseph R. Dorkin , Xiaojun Qin , William Cantley , Anna Borodovsky , Soma De , Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev
IPC分类号： A61K31/713 , A61P43/00 , A61K31/7088 , A61K47/42 , A61K47/28 , A61K31/7105
CPC分类号： A61K48/0008 , A61K9/1272
摘要： The invention features an improved lipid formulation comprising a cationic lipid of formula (A), a neutral lipid, a sterol and a PEG or PEG-modified lipid, where R1 and R2 are independently alkyl, alkenyl or alkynyl, each can be optionally substituted, and R3 and R4 are independently lower alkyl or R3 and R4 can be taken together to form an optionally substituted heterocyclic ring. In one embodiment, R1 and R2 are independently selected from oleoyl, pamitoyl, steroyl, linoleyl and R3 and R4 are methyl. Also disclosed are targeting lipids, and specific lipid formulations comprising such targeting lipids.
摘要翻译：本发明的特征在于改进的脂质制剂，其包含式（A）的阳离子脂质，中性脂质，固醇和PEG或PEG修饰的脂质，其中R 1和R 2独立地为烷基，烯基或炔基，各自可任选被取代，并且R 3和R 4独立地为低级烷基或R 3和R 4可以一起形成任选取代的杂环。在一个实施方案中，R 1和R 2独立地选自油酰基，苯甲酰基，甾烷基，亚油酰基，并且R 3和R 4是甲基。还公开了靶向脂质和包含这种靶向脂质的特定脂质制剂。

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