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公开(公告)号：US20240285767A1
公开(公告)日：2024-08-29
申请号：US18589636
申请日：2024-02-28
发明人： Martin MAIER , Muthusamy JAYARAMAN , Akin AKINC , Shigeo MATSUDA , Pachamuthu KANDASAMY , Kallanthottathil G. RAJEEV , Muthiah MANOHARAN , Jayaprakash K. NAIR , Thomas A. BAILLIE
IPC分类号： A61K47/18 , A61K9/127 , A61K9/51 , A61K31/7088 , A61K31/7105 , A61K31/713 , C07C31/125 , C07C211/09 , C07C211/10 , C07C211/11 , C07C217/08 , C07C229/12 , C07C235/06 , C07C251/38 , C07C323/12 , C07C323/58 , C07C327/22 , C07C327/28 , C07C327/32 , C07D207/32 , C07D233/54 , C07D295/08 , C07D295/12 , C07D295/14 , C07D317/30 , C07F5/02
CPC分类号： A61K47/18 , A61K9/1272 , A61K9/5123 , A61K31/7088 , A61K31/7105 , A61K31/713 , C07C31/125 , C07C211/09 , C07C211/10 , C07C211/11 , C07C217/08 , C07C229/12 , C07C235/06 , C07C251/38 , C07C323/12 , C07C323/58 , C07C327/22 , C07C327/28 , C07C327/32 , C07D207/32 , C07D233/54 , C07D295/08 , C07D295/12 , C07D295/14 , C07D317/30 , C07F5/022
摘要： The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.
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2.发明申请公开(公告)号：US20150203847A1
公开(公告)日：2015-07-23
申请号：US14587957
申请日：2014-12-31
发明人： Muthiah MANOHARAN , Kallanthottathil G. RAJEEV , Takeshi YAMADA , David BUTLER , Narayanannair K. JAYAPRAKASH , Muthusamy JAYARAMAN , Shigeo MATSUDA , Rajendra K. PANDEY , Chang Geng PENG
IPC分类号： C12N15/113 , A61K31/713
CPC分类号： C12N15/113 , A61K31/713 , A61K47/544 , A61K47/64 , C07H21/00 , C12N2310/14 , C12N2310/141 , C12N2310/3513 , C12N2310/3515 , H04L65/602 , H04L67/36 , Y02A50/465
摘要： The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.
摘要翻译： 本发明的特征在于式I或II化合物：在一个实施方案中，本发明涉及将配体与寡核苷酸缀合的化合物和方法。 本发明还涉及治疗各种病症和疾病如病毒感染，细菌感染，寄生虫感染，癌症，过敏症，自身免疫疾病，免疫缺陷和免疫抑制的方法。
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公开(公告)号：US20230256098A1
公开(公告)日：2023-08-17
申请号：US18304097
申请日：2023-04-20
发明人： Martin MAIER , Muthusamy JAYARAMAN , Akin AKINC , Shigeo MATSUDA , Pachamuthu KANDASAMY , Kallanthottathil G. RAJEEV , Muthiah MANOHARAN
IPC分类号： A61K47/18 , A61K9/127 , A61K9/51 , A61K31/713 , C07D317/30 , C07C211/09 , C07C211/10 , C07C211/11 , C07C217/08 , C07C229/12 , C07C327/22 , C07C327/28 , C07C327/32 , C07C235/06 , C07C251/38 , C07F5/02 , C07D233/54 , C07D207/32 , C07D295/08 , C07D295/12 , C07D295/14 , C07C323/12 , C07C323/58 , C07C31/125 , A61K31/7088 , A61K31/7105
CPC分类号： A61K47/18 , A61K9/1272 , A61K9/5123 , A61K31/713 , C07D317/30 , C07C211/09 , C07C211/10 , C07C211/11 , C07C217/08 , C07C229/12 , C07C327/22 , C07C327/28 , C07C327/32 , C07C235/06 , C07C251/38 , C07F5/022 , C07D233/54 , C07D207/32 , C07D295/08 , C07D295/12 , C07D295/14 , C07C323/12 , C07C323/58 , C07C31/125 , A61K31/7088 , A61K31/7105
摘要： The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.
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公开(公告)号：US20240269289A1
公开(公告)日：2024-08-15
申请号：US18589688
申请日：2024-02-28
发明人： Martin MAIER , Muthusamy JAYARAMAN , Akin AKINC , Shigeo MATSUDA , Pachamuthu KANDASAMY , Kallanthottathil G. RAJEEV , Muthiah MANOHARAN , Jayaprakash K. NAIR , Thomas A. BAILLIE
IPC分类号： A61K47/18 , A61K9/127 , A61K9/51 , A61K31/7088 , A61K31/7105 , A61K31/713 , C07C31/125 , C07C211/09 , C07C211/10 , C07C211/11 , C07C217/08 , C07C229/12 , C07C235/06 , C07C251/38 , C07C323/12 , C07C323/58 , C07C327/22 , C07C327/28 , C07C327/32 , C07D207/32 , C07D233/54 , C07D295/08 , C07D295/12 , C07D295/14 , C07D317/30 , C07F5/02
CPC分类号： A61K47/18 , A61K9/1272 , A61K9/5123 , A61K31/7088 , A61K31/7105 , A61K31/713 , C07C31/125 , C07C211/09 , C07C211/10 , C07C211/11 , C07C217/08 , C07C229/12 , C07C235/06 , C07C251/38 , C07C323/12 , C07C323/58 , C07C327/22 , C07C327/28 , C07C327/32 , C07D207/32 , C07D233/54 , C07D295/08 , C07D295/12 , C07D295/14 , C07D317/30 , C07F5/022
摘要： The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.
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公开(公告)号：US20240009225A1
公开(公告)日：2024-01-11
申请号：US18311484
申请日：2023-05-03
发明人： Jayaprakash K. NAIR , Martin MAIER , Vasant JADHAV , Stuart MILSTEIN , Kirk BROWN , Rubina G. PARMAR , Kallanthottathil G. RAJEEV , Muthiah MANOHARAN , Alexander V. KEL'IN , Muthusamy JAYARAMAN , Klaus CHARISSE , Adam CASTORENO , Christopher THEILE , Kevin FITZGERALD
IPC分类号： A61K31/713 , A61K47/54 , A61K9/00 , C12N15/113
CPC分类号： A61K31/713 , A61K47/543 , A61K9/0019 , C12N15/1137 , C12N15/1138 , C12N2310/14 , C12N2310/3515
摘要： One aspect of the present invention relates to a double stranded iRNA agent comprising an antisense strand which is complementary to a target gene; a sense strand which is complementary to said antisense strand; and one or more lipophilic moieties conjugated to one or more internal positions on at least one strand, optionally via a linker or carrier. Another aspect of the invention relates to a method of gene silencing, comprising administering to a cell or a subject in need thereof a therapeutically effective amount of the lipophilic moieties-conjugated double-stranded iRNAs.
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6.发明申请公开(公告)号：US20160376585A1
公开(公告)日：2016-12-29
申请号：US14901945
申请日：2014-07-11
发明人： Muthiah MANOHARAN , Jayaprakash K. NAIR , Pachamuthu KANDASAMY , Shigeo MATSUDA , Alexander V. KELIN , Muthusamy JAYARAMAN , Kallanthottathil G. RAJEEV
IPC分类号： C12N15/113 , A61K47/48
摘要： The present invention relates to ligand conjugates of oligonucleotides (e.g., iRNA agents) and methods for their preparation. The ligands are derived primarily from monosaccharides These conjugates are useful for the in vivo delivery of oligonucleotides.
摘要翻译： 本发明涉及寡核苷酸的配体缀合物（例如，iRNA试剂）及其制备方法。 配体主要衍生自单糖这些缀合物可用于体内递送寡核苷酸。
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公开(公告)号：US20240285768A1
公开(公告)日：2024-08-29
申请号：US18594172
申请日：2024-03-04
发明人： Martin MAIER , Muthusamy JAYARAMAN , Akin AKINC , Shigeo MATSUDA , Pachamuthu KANDASAMY , Kallanthottathil G. RAJEEV , Muthiah MANOHARAN , Jayaprakash K. NAIR , Thomas A. BAILLIE
IPC分类号： A61K47/18 , A61K9/127 , A61K9/51 , A61K31/7088 , A61K31/7105 , A61K31/713 , C07C31/125 , C07C211/09 , C07C211/10 , C07C211/11 , C07C217/08 , C07C229/12 , C07C235/06 , C07C251/38 , C07C323/12 , C07C323/58 , C07C327/22 , C07C327/28 , C07C327/32 , C07D207/32 , C07D233/54 , C07D295/08 , C07D295/12 , C07D295/14 , C07D317/30 , C07F5/02
CPC分类号： A61K47/18 , A61K9/1272 , A61K9/5123 , A61K31/7088 , A61K31/7105 , A61K31/713 , C07C31/125 , C07C211/09 , C07C211/10 , C07C211/11 , C07C217/08 , C07C229/12 , C07C235/06 , C07C251/38 , C07C323/12 , C07C323/58 , C07C327/22 , C07C327/28 , C07C327/32 , C07D207/32 , C07D233/54 , C07D295/08 , C07D295/12 , C07D295/14 , C07D317/30 , C07F5/022
摘要： The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.
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公开(公告)号：US20220125823A1
公开(公告)日：2022-04-28
申请号：US17052945
申请日：2019-05-07
发明人： Jayaprakash K. NAIR , Martin MAIER , Vasant JADHAV , Stuart MILSTEIN , Kirk BROWN , Rubina G. PARMAR , Kallanthottathil G. RAJEEV , Muthiah MANOHARAN , Alexander V. KEL'IN , Muthusamy JAYARAMAN , Klaus CHARISSE , Adam CASTORENO , Christopher S. THEILE , Kevin FITZGERALD
IPC分类号： A61K31/713 , C12N15/113 , A61K47/54 , A61K9/00
摘要： The invention relates to a method of gene silencing, comprising administering to a cell or a subject in need thereof a therapeutically effective amount of the lipophilic moieties-conjugated double-stranded iRNAs at one or more internal positions on at least one strand, optionally via a linker or carrier.
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公开(公告)号：US20160009637A1
公开(公告)日：2016-01-14
申请号：US14661945
申请日：2015-03-18
发明人： Muthiah MANOHARAN , Martin MAIER , Muthusamy JAYARAMAN , Shigeo MATSUDA , Jayaprakash K. NAIR , Kallanthottathil G. RAJEEV , Akin AKINC , Thomas A. BAILLIE
IPC分类号： C07C229/12 , C12N15/113 , A61K39/00 , A61K47/44 , A61K31/713
CPC分类号： C07C229/12 , A61K31/713 , A61K39/0005 , A61K47/44 , C12N15/113 , C12N15/88 , C12N2310/14 , C12N2320/30
摘要： The present invention relates to a cationic lipid having one or more biodegradable groups located in the mid- or distal section of a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.
摘要翻译： 本发明涉及一种阳离子脂质，其具有位于阳离子脂质的脂质部分（例如，疏水链）的中间或远端部分中的一个或多个可生物降解基团。 这些阳离子脂质可以掺入用于递送活性剂（例如核酸）的脂质颗粒中。 本发明还涉及包含中性脂质，能够减少聚集的脂质，本发明的阳离子脂质和任选的固醇的脂质颗粒。 脂质颗粒可以进一步包括治疗剂如核酸。
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公开(公告)号：US20150273068A1
公开(公告)日：2015-10-01
申请号：US14677801
申请日：2015-04-02
发明人： Martin MAIER , Muthusamy JAYARAMAN , Akin AKINC , Shigeo MATSUDA , Pachamuthu KANDASAMY , Kallanthottathil G. RAJEEV , Muthiah MANOHARAN
IPC分类号： A61K47/18 , A61K31/7105 , A61K31/7088
CPC分类号： A61K47/18 , A61K9/1272 , A61K9/5123 , A61K31/7088 , A61K31/7105 , A61K31/713 , C07C211/09 , C07C211/10 , C07C211/11 , C07C217/08 , C07C229/12 , C07C235/06 , C07C251/38 , C07C323/12 , C07C323/58 , C07C327/22 , C07C327/28 , C07C327/32 , C07D207/32 , C07D233/54 , C07D295/08 , C07D295/12 , C07D295/14 , C07D317/30 , C07F5/022
摘要： The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.
摘要翻译： 本发明涉及具有位于阳离子脂质的脂质部分（例如，疏水链）中的一个或多个可生物降解基团的阳离子脂质。 这些阳离子脂质可以掺入用于递送活性剂（例如核酸）的脂质颗粒中。 本发明还涉及包含中性脂质，能够减少聚集的脂质，本发明的阳离子脂质和任选的固醇的脂质颗粒。 脂质颗粒可以进一步包括治疗剂如核酸。
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