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公开(公告)号：US20170081663A1
公开(公告)日：2017-03-23
申请号：US15284494
申请日：2016-10-03
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 , Zheng Hou , John A. Gaudette , Priya Karmali , Sridhar C. Nagarajan
IPC分类号： C12N15/113 , A61K47/18 , A61K47/24 , A61K31/713
CPC分类号： C12N15/113 , A61K9/0048 , A61K9/127 , A61K9/1271 , A61K31/713 , A61K45/06 , A61K47/18 , A61K47/186 , A61K47/24 , C07H21/02 , C12N15/111 , C12N2310/11 , C12N2310/14 , C12N2320/32
摘要： What is described is a pharmaceutical composition for treating a fibrotic disease 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：US11084779B2
公开(公告)日：2021-08-10
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：US20140294934A1
公开(公告)日：2014-10-02
申请号：US14256306
申请日：2014-04-18
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： A61K47/18 , C12N15/113 , A61K31/713
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 is independently selected from a group consisting of C10 to C18 alkyl, C12 to C18 alkenyl, and oleyl group; wherein R3 and R4 are independently selected from a group consisting of C1 to C6 alkyl, and C2 to C6 alkanol; wherein X is selected from a group consisting of —CH2—, —S—, and —O— or absent; wherein Y is selected from —(CH2)n, —S(CH2)n, —O(CH2)n—, thiophene, —SO2(CH2)n—, and ester, wherein n=1-4; wherein a=1-4; wherein b=1-4; wherein c=1-4; and wherein Z is a counterion; as well as 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烯基和油基; 其中R3和R4独立地选自C1-C6烷基和C2-C6链烷醇; 其中X选自-CH 2 - ， - S-和-O-或不存在; 其中Y选自 - （CH 2）n，-S（CH 2）n，-O（CH 2）n - ，噻吩，-SO 2（CH 2）n - 和酯，其中n = 1-4; 其中a = 1-4; 其中b = 1-4; 其中c = 1-4; 并且其中Z是抗衡离子; 以及包含可用于递送治疗剂的式I化合物的组合物和药物制剂; 以及使用这些组合物和制剂的方法。
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公开(公告)号：US20180208547A1
公开(公告)日：2018-07-26
申请号：US15919098
申请日：2018-03-12
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 , C12N15/113 , C07C333/04 , C07C323/60 , A61K47/18 , A61K47/54 , A61K9/127 , A61K9/10 , A61K9/00 , A61K31/713
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 is a method of delivery of a drug to a stellate cell using a composition comprising a compound 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.
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公开(公告)号：US09963424B2
公开(公告)日：2018-05-08
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： A61K9/10 , A61K31/713 , C07C237/08 , A61K9/00 , A61K9/127 , A61K47/18 , C12N15/113 , C07C323/60 , C07C333/04 , A61K47/54
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.
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公开(公告)号：US09242001B2
公开(公告)日：2016-01-26
申请号：US14256306
申请日：2014-04-18
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： A61K47/18 , A61K31/713 , C12N15/113 , A61K9/00 , A61K9/10 , A61K9/127
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 is independently selected from a group consisting of C10 to C18 alkyl, C12 to C18 alkenyl, and oleyl group; wherein R3 and R4 are independently selected from a group consisting of C1 to C6 alkyl, and C2 to C6 alkanol; wherein X is selected from a group consisting of —CH2—, —S—, and —O— or absent; wherein Y is selected from —(CH2)n, —S(CH2)n, —O(CH2)n—, thiophene, —SO2(CH2)n—, and ester, wherein n=1-4; wherein a=1-4; wherein b=1-4; wherein c=1-4; and wherein Z is a counterion; as well as 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.
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公开(公告)号：US10532975B2
公开(公告)日：2020-01-14
申请号：US15919098
申请日：2018-03-12
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 , A61K9/00 , A61K9/10 , A61K9/12 , A61K47/54 , A61K47/18 , C07C237/08 , A61K9/127 , C12N15/113 , C07C323/60 , C07C333/04
摘要： Here described is a method of delivery of a drug to a stellate cell using a composition comprising a compound 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.
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公开(公告)号：US10196637B2
公开(公告)日：2019-02-05
申请号：US15284494
申请日：2016-10-03
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 , Zheng Hou , John A. Gaudette , Priya Karmali , Sridhar C. Nagarajan
IPC分类号： C12N15/113 , A61K31/713 , A61K47/18 , A61K47/24 , A61K9/127 , C07H21/02 , C12N15/11 , A61K45/06
摘要： What is described is a pharmaceutical composition for treating a fibrotic disease 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：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：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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