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1. 发明申请

WO2008042973A2 LIPID CONTAINING FORMULATIONS 审中-公开
标题翻译：含脂制剂
公开(公告)号：WO2008042973A2
公开(公告)日：2008-04-10
申请号：PCT/US2007/080331
申请日：2007-10-03
申请人： ALNYLAM PHARMACEUTICALS, INC. , MANOHARAN, Muthiah , RAJEEV, Kallanthottahil G. , AKINC, Akin , JAYAPRAKASH, K. Narayanannair , JAYRAMAN, Muthusamy , MAIER, Martin A.
发明人： MANOHARAN, Muthiah , RAJEEV, Kallanthottahil G. , AKINC, Akin , JAYAPRAKASH, K. Narayanannair , JAYRAMAN, Muthusamy , MAIER, Martin A.
IPC分类号： A61K31/325
CPC分类号： C07C219/06 , A61K9/1272 , A61K9/1273 , A61K31/325 , A61K47/34 , C07C209/78 , C07C233/36 , 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.
摘要翻译：描述了用于施用基于核酸的疗法，例如缔合复合物如脂质体和脂质复合物的组合物和方法。

2. 发明申请

US20110311583A1 NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS 有权
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：US20110311583A1
公开(公告)日：2011-12-22
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 , A61K47/08 , C07J41/00 , A61K47/28 , C07C211/22 , A61K47/16 , C07C211/21 , C07D211/72 , A61K47/22 , C07C251/78 , C07C279/12 , C07C271/12 , A61K48/00 , A61K31/713 , C12N5/00 , A61K39/39 , A61K39/00 , A61K39/02 , A61P37/04 , A61P31/12 , A61P31/04 , A61P33/00 , C07C49/203
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： (A1) Translate this text 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, ?-aminoalkyls, ?-(substituted)aminoalkyls, ?-phosphoalkyls, ?-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(0)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, ?-aminoalkyl, ?-(substituted)aminoalky, ?-phosphoalkyl or ?-thiophosphoalkyl.
摘要翻译：（A1）翻译本发明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，烷基硫代磷酸烷基酯，硫代磷酸烷基酯，磷酸二烷基酯，烷基膦酸酯，烷基胺，羟烷基，α-氨基烷基，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，α-氨基烷基，β-（取代）氨基烷基，α-磷酸烷基或α-硫代磷酰烷基。

3. 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。

4. 发明授权

US08106022B2 Carbohydrate conjugates as delivery agents for oligonucleotides 有权
标题翻译：碳水化合物缀合物作为寡核苷酸的递送剂
公开(公告)号：US08106022B2
公开(公告)日：2012-01-31
申请号：US12328528
申请日：2008-12-04
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Martin Maier
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Martin Maier
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： A61K47/28 , A61K31/70 , A61K31/7004 , A61K31/7052 , A61K31/7088 , A61K31/713 , A61K47/16 , A61K47/22 , A61K47/543 , A61K47/549 , A61K47/60 , A61K48/00 , C07H21/02 , Y02A50/385 , Y02A50/411 , Y02A50/467 , Y02P20/55
摘要： The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl 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-Linker-OP(Z′″)(Z″″)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z′)(Z″)-formula (I), —P(Z′)(Z″)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g., monosaccharide, disaccharide, trisaccharide, tetrasaccharide, oligosaccharide, polysaccharide; RN is independently for each occurrence H, methyl, ethyl, propyl, isopropyl, butyl, or benzyl; and Z′, Z″, Z′″ and Z″″ are each independently for each occurrence O or S.
摘要翻译：本发明提供包含至少一个式（I）亚基的iRNA试剂：其中：A和B各自独立地为O，N（RN）或S; X和Y各自独立地为H，OH，羟基保护基，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，亲脂性，聚合物，-P（Z'）（Z“）O-Linker- OP（Z'“）（Z”“） - 寡核苷酸，寡核苷酸，-P（Z'）（Z”） - 式（I），-P（Z'）（Z“） - 链接器R R是LG，-Linker-LG，或具有如下结构：每次出现LG独立为碳水化合物，例如单糖，二糖，三糖，四糖，寡糖，多糖; 乙烯基，丙基，异丙基，丁基或苄基各自独立地为N，和Z'，Z“，Z”“和Z”“各自独立地为O或S.

5. 发明申请

US20090239814A1 Carbohydrate Conjugates as Delivery Agents for Oligonucleotides 有权
标题翻译：碳水化合物缀合物作为寡核苷酸的递送剂
公开(公告)号：US20090239814A1
公开(公告)日：2009-09-24
申请号：US12328528
申请日：2008-12-04
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Martin Maier
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Martin Maier
IPC分类号： A61K31/715 , C07H17/02 , C12N5/06
CPC分类号： A61K47/28 , A61K31/70 , A61K31/7004 , A61K31/7052 , A61K31/7088 , A61K31/713 , A61K47/16 , A61K47/22 , A61K47/543 , A61K47/549 , A61K47/60 , A61K48/00 , C07H21/02 , Y02A50/385 , Y02A50/411 , Y02A50/467 , Y02P20/55
摘要： The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl 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-Linker-OP(Z′″)(Z″″)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z′)(Z″)-formula (I), —P(Z′)(Z″)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g., monosaccharide, disaccharide, trisaccharide, tetrasaccharide, oligosaccharide, polysaccharide; RN is independently for each occurrence H, methyl, ethyl, propyl, isopropyl, butyl, or benzyl; and Z′, Z″, Z′″ and Z″″ are each independently for each occurrence O or S.
摘要翻译：本发明提供包含至少一个式（I）亚基的iRNA试剂：其中：A和B各自独立地为O，N（RN）或S; X和Y各自独立地为H，OH，羟基保护基，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'）（Z“）O - 寡核苷酸，脂质，PEG，类固醇，亲脂体，聚合物，-P（Z'）（Z”）O （Z'）（Z“） - （Z”）（Z“）（Z”）（Z“）（Z”）（Z“） - 或-Linker-R; R是LG，-Linker-LG，或具有如下结构：每次出现LG独立为碳水化合物，例如单糖，二糖，三糖，四糖，寡糖，多糖; 乙烯基，丙基，异丙基，丁基或苄基各自独立地为N， Z'，Z“，Z”“和Z”“各自独立地为O或S.

6. 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））。

7. 发明申请

US20120058144A1 LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS 有权
标题翻译：用于输送治疗药物的脂肪和组合物
公开(公告)号：US20120058144A1
公开(公告)日：2012-03-08
申请号：US13128363
申请日：2009-11-10
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Narayanannair , Marco A. Ciufolini
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Narayanannair , Marco A. Ciufolini
IPC分类号： A61K39/00 , C07D211/46 , C07D207/12 , C07D317/28 , C07C217/52 , C07C291/04 , A61K47/18 , A61K47/28 , A61K47/22 , A61K48/00 , A61K31/713 , C12N5/00 , A61K39/12 , A61K39/02 , A61P31/12 , A61P31/04 , A61P33/00 , A61P35/00 , A61P37/04 , C07C229/46
CPC分类号： A61K31/7088 , A61K9/1272 , A61K31/7105 , A61K39/00 , A61K2039/55561 , A61K2039/6018 , C12N15/111 , C12N15/1137 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2320/32 , C12N2310/3521 , C12N2310/3533
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 XIV or XVII.
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XIV或XVII的脂质。

8. 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。

9. 发明授权

US08158601B2 Lipid formulation 有权
标题翻译：脂质配方
公开(公告)号：US08158601B2
公开(公告)日：2012-04-17
申请号：US12813448
申请日：2010-06-10
申请人： Jianxin Chen , Steven Ansell , Akin Akinc , Joseph Robert Dorkin , Xiaojun Qin , William Cantley , Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Muthusamy Jayaraman
发明人： Jianxin Chen , Steven Ansell , Akin Akinc , Joseph Robert Dorkin , Xiaojun Qin , William Cantley , Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Muthusamy Jayaraman
IPC分类号： A61K31/70 , A61K47/00 , C07C229/00
CPC分类号： A61K9/1272 , A61K9/1278 , A61K31/22 , A61K31/7088 , A61K31/712 , A61K31/713 , A61K38/1709 , A61K38/4846 , A61K47/14 , A61K47/549 , A61K47/551 , A61K47/6911 , A61K48/0033 , C07C29/58 , C07C227/18 , C07C227/40 , C07C229/12 , C07D475/04 , C12N15/113 , C12N15/1137 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/341 , C12N2310/346 , C12N2310/351 , C12N2310/3515 , C12N2320/32 , Y02A50/463 , A61K2300/00 , C12N2310/3521 , C12N2310/3533
摘要： The invention features a cationic lipid of formula I, an improved lipid formulation comprising a cationic lipid of formula I and corresponding methods of use. Also disclosed are targeting lipids, and specific lipid formulations comprising such targeting lipids.
摘要翻译：本发明的特征在于式I的阳离子脂质，包含式I的阳离子脂质和相应的使用方法的改进的脂质制剂。还公开了靶向脂质和包含这种靶向脂质的特定脂质制剂。

10. 发明申请

US20120027796A1 NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS 有权
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：US20120027796A1
公开(公告)日：2012-02-02
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 , C07D317/44 , C07D317/46 , C07D493/04 , C07D317/70 , C07D491/113 , C07D317/28 , C07D317/72 , C07F9/655 , A61K47/44 , A61K31/7088 , A61K31/713 , C12N5/071 , A61K39/39 , A61K39/00 , A61K39/02 , A61P37/04 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , C07D491/056
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））。

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