公开(公告)号：WO2012170952A4

公开(公告)日：2013-05-30

申请号：PCT/US2012041753

申请日：2012-06-08

Applicant: NITTO DENKO CORP ,  NIITSU YOSHIRO ,  PAYNE JOSEPH E ,  HOU ZHENG ,  GAUDETTE JOHN A ,  NAGARAJAN SRIDHAR C ,  KNOPOV VICTOR ,  WITTE RICHARD P ,  AHMADIAN MOHAMMAD ,  PERELMAN LOREN A ,  TANAKA YASUNOBU ,  AKOPIAN VIOLETTA ,  KARMALI PRIYA

Inventor： NIITSU YOSHIRO ,  PAYNE JOSEPH E ,  HOU ZHENG ,  GAUDETTE JOHN A ,  NAGARAJAN SRIDHAR C ,  KNOPOV VICTOR ,  WITTE RICHARD P ,  AHMADIAN MOHAMMAD ,  PERELMAN LOREN A ,  TANAKA YASUNOBU ,  AKOPIAN VIOLETTA ,  KARMALI PRIYA

IPC: C07C237/08 ,  A61K31/16 ,  A61P1/16 ,  C07C237/22 ,  C07C323/60 ,  C07C333/04

CPC classification number: C07C237/08 ,  A61K9/1271 ,  C07C237/22 ,  C07C323/60 ,  C07C333/04

Abstract: 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=l -4; wherein c=l-4; and wherein Z is a counterion; and compounds consisting of the structure (targeting molecule)m-linker-(targeting molecule)n, wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including one or both of these compounds which are useful for the delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.

Abstract translation: 这里描述的是式I的化合物：其中R 1和R 2独立地选自由C 10至C 18烷基，C 12至C 18烯基和油烯基组成的组; 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 - （CH2）n，-S（CH2）n，-O（CH2）n-，噻吩，-SO2（CH2）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; 和由结构（靶向分子）m-连接体 - （靶向分子）n组成的化合物，其中靶向分子是在靶细胞上具有特定受体的类视黄醇或脂溶性维生素; 其中m和n独立地为0,1,2或3; 并且其中接头包含聚乙二醇（PEG）或PEG-样分子，以及包含用于递送治疗剂的这些化合物中的一种或两种的组合物和药物制剂; 以及使用这些组合物和药物制剂的方法。

公开(公告)号：WO2012170952A3

公开(公告)日：2013-04-11

申请号：PCT/US2012041753

申请日：2012-06-08

Applicant: NITTO DENKO CORP ,  NIITSU YOSHIRO ,  PAYNE JOSEPH E ,  HOU ZHENG ,  GAUDETTE JOHN A ,  NAGARAJAN SRIDHAR C ,  KNOPOV VICTOR ,  WITTE RICHARD P ,  AHMADIAN MOHAMMAD ,  PERELMAN LOREN A ,  TANAKA YASUNOBU ,  AKOPIAN VIOLETTA ,  KARMALI PRIYA

Inventor： NIITSU YOSHIRO ,  PAYNE JOSEPH E ,  HOU ZHENG ,  GAUDETTE JOHN A ,  NAGARAJAN SRIDHAR C ,  KNOPOV VICTOR ,  WITTE RICHARD P ,  AHMADIAN MOHAMMAD ,  PERELMAN LOREN A ,  TANAKA YASUNOBU ,  AKOPIAN VIOLETTA ,  KARMALI PRIYA

IPC: C07C237/08 ,  A61K31/16 ,  A61P1/16 ,  C07C237/22 ,  C07C323/60 ,  C07C333/04

CPC classification number: C07C237/08 ,  A61K9/1271 ,  C07C237/22 ,  C07C323/60 ,  C07C333/04

Abstract: 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=l -4; wherein c=l-4; and wherein Z is a counterion; and compounds consisting of the structure (targeting molecule)m-linker-(targeting molecule)n, wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including one or both of these compounds which are useful for the delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.

Abstract translation: 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; 以及由结构（靶向分子）m-接头（靶向分子）n组成的化合物，其中靶向分子是靶细胞上具有特异性受体的类视黄醇或脂溶性维生素; 其中m和n独立地为0,1,2或3; 并且其中所述接头包含聚乙二醇（PEG）或PEG样分子，以及包含这些化合物中的一种或两种可用于递送治疗剂的组合物和药物制剂; 以及使用这些组合物和药物制剂的方法。

公开(公告)号：WO2013185116A1

公开(公告)日：2013-12-12

申请号：PCT/US2013/044849

申请日：2013-06-07

Applicant: PAYNE, Joseph, E. ,  GAUDETTE, John, A. ,  HOU, Zheng ,  AHMADIAN, Mohammad ,  YU, Lei ,  KNOPOV, Victor ,  AKOPIAN, Violetta ,  KARMALI, Priya ,  WITTE, Richard, P. ,  SAFARZADEH, Neda ,  YING, Wenbin ,  ZHANG, Jun

Inventor： PAYNE, Joseph, E. ,  GAUDETTE, John, A. ,  HOU, Zheng ,  AHMADIAN, Mohammad ,  YU, Lei ,  KNOPOV, Victor ,  AKOPIAN, Violetta ,  KARMALI, Priya ,  WITTE, Richard, P. ,  SAFARZADEH, Neda ,  YING, Wenbin ,  ZHANG, Jun

IPC: C07C271/16 ,  C07D333/40 ,  C07C317/44 ,  C07C321/14 ,  C07C333/04 ,  C07C235/08 ,  C07C237/08 ,  C07D207/16 ,  A61K47/16 ,  A61K47/18 ,  A61K47/22

CPC classification number: A61K47/20 ,  A61K9/1272 ,  A61K47/14 ,  A61K47/18 ,  A61K47/22 ,  C07C235/08 ,  C07C237/08 ,  C07C237/16 ,  C07C271/16 ,  C07C317/44 ,  C07C323/60 ,  C07C333/04 ,  C07D207/16 ,  C07D333/38 ,  C07D333/40 ,  Y10T428/2998

Abstract: The description is directed to ionizable lipids useful for enhancing the delivery of therapeutic agents in liposomes.

Abstract translation: 该描述针对可用于增强脂质体中治疗剂递送的可离子化脂质。

公开(公告)号：WO2012170952A9

公开(公告)日：2013-02-21

申请号：PCT/US2012041753

申请日：2012-06-08

Applicant: NITTO DENKO CORP ,  NIITSU YOSHIRO ,  PAYNE JOSEPH E ,  HOU ZHENG ,  GAUDETTE JOHN A ,  NAGARAJAN SRIDHAR C ,  KNOPOV VICTOR ,  WITTE RICHARD P ,  AHMADIAN MOHAMMAD ,  PERELMAN LOREN A ,  TANAKA YASUNOBU ,  AKOPIAN VIOLETTA ,  KARMALI PRIYA

Inventor： NIITSU YOSHIRO ,  PAYNE JOSEPH E ,  HOU ZHENG ,  GAUDETTE JOHN A ,  NAGARAJAN SRIDHAR C ,  KNOPOV VICTOR ,  WITTE RICHARD P ,  AHMADIAN MOHAMMAD ,  PERELMAN LOREN A ,  TANAKA YASUNOBU ,  AKOPIAN VIOLETTA ,  KARMALI PRIYA

IPC: C07C237/08 ,  A61K31/16 ,  A61P1/16 ,  C07C237/22 ,  C07C323/60 ,  C07C333/04

CPC classification number: C07C237/08 ,  A61K9/1271 ,  C07C237/22 ,  C07C323/60 ,  C07C333/04

Abstract: 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=l -4; wherein c=l-4; and wherein Z is a counterion; and compounds consisting of the structure (targeting molecule)m-linker-(targeting molecule)n, wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including one or both of these compounds which are useful for the delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.

公开(公告)号：WO2012170952A2

公开(公告)日：2012-12-13

申请号：PCT/US2012/041753

申请日：2012-06-08

Applicant: NITTO DENKO CORPORATION ,  NIITSU, Yoshiro ,  PAYNE, Joseph E. ,  HOU, Zheng ,  GAUDETTE, John A. ,  NAGARAJAN, Sridhar C. ,  KNOPOV, Victor ,  WITTE, Richard P. ,  AHMADIAN, Mohammad ,  PERELMAN, Loren A. ,  TANAKA, Yasunobu ,  AKOPIAN, Violetta ,  KARMALI, Priya

Inventor： NIITSU, Yoshiro ,  PAYNE, Joseph E. ,  HOU, Zheng ,  GAUDETTE, John A. ,  NAGARAJAN, Sridhar C. ,  KNOPOV, Victor ,  WITTE, Richard P. ,  AHMADIAN, Mohammad ,  PERELMAN, Loren A. ,  TANAKA, Yasunobu ,  AKOPIAN, Violetta ,  KARMALI, Priya

IPC: C07C237/08 ,  A61K31/16 ,  A61P1/16 ,  C07C237/22 ,  C07C323/60 ,  C07C333/04

CPC classification number: C07C237/08 ,  A61K9/1271 ,  C07C237/22 ,  C07C323/60 ,  C07C333/04

Abstract: Here described are compounds of formula I: wherein R 1 and R 2 is independently selected from a group consisting of C 10 to C 18 alkyl, C 12 to C 18 alkenyl, and oleyl group; wherein R 3 and R 4 are independently selected from a group consisting of C 1 to C 6 alkyl, and C 2 to C 6 alkanol; wherein X is selected from a group consisting of -CH 2 -, -S-, and -O- or absent; wherein Y is selected from -(CH 2 )n, -S(CH 2 ) n , -O(CH 2 ) n -, thiophene, -SO 2 (CH 2 ) n -, and ester, wherein n = 1 -4; wherein a = 1 -4; wherein b=l -4; wherein c=l-4; and wherein Z is a counterion; and compounds consisting of the structure (targeting molecule) m -linker-(targeting molecule) n , wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including one or both of these compounds which are useful for the delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.

Abstract translation: 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; 以及由结构（靶向分子）m-接头（靶向分子）n组成的化合物，其中靶向分子是靶细胞上具有特异性受体的类视黄醇或脂溶性维生素; 其中m和n独立地为0,1,2或3; 并且其中所述接头包含聚乙二醇（PEG）或PEG样分子，以及包含这些化合物中的一种或两种可用于递送治疗剂的组合物和药物制剂; 以及使用这些组合物和药物制剂的方法。