公开(公告)号：US09393315B2

公开(公告)日：2016-07-19

申请号：US13492424

申请日：2012-06-08

Applicant: Yoshiro Niitsu ,  Joseph E. Payne ,  John A. Gaudette ,  Zheng Hou ,  Victor Knopov ,  Richard P. Witte ,  Mohammad Ahmadian ,  Loren A. Perelman ,  Yasunobu Tanaka ,  Violetta Akopian

Inventor： Yoshiro Niitsu ,  Joseph E. Payne ,  John A. Gaudette ,  Zheng Hou ,  Victor Knopov ,  Richard P. Witte ,  Mohammad Ahmadian ,  Loren A. Perelman ,  Yasunobu Tanaka ,  Violetta Akopian

IPC: A61K9/127 ,  C07C235/30 ,  A61K31/166 ,  A61K31/23 ,  A61P1/16 ,  A61P1/18 ,  A61P11/04 ,  C07F9/10 ,  A61K31/685 ,  A61K31/713 ,  C07C229/32 ,  C07C235/48 ,  A61K47/48 ,  C07C237/22 ,  C07C235/08

CPC classification number: C07C237/22 ,  A61K9/127 ,  A61K9/1271 ,  A61K31/07 ,  A61K31/713 ,  A61K47/551 ,  C07C233/21 ,  C07C235/08 ,  C07C235/48 ,  C07C2601/16 ,  C07F9/10 ,  C12N15/113 ,  C12N2310/14 ,  C12N2320/32 ,  Y10S977/773 ,  Y10S977/906 ,  Y10S977/907

Abstract: Here described are 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 these compounds which are useful for the targeting and delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.

Abstract translation: 这里描述的是由结构（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的组合物和药物制剂，其可用于治疗剂的靶向和递送; 以及使用这些组合物和药物制剂的方法。

公开(公告)号：US20130017249A1

公开(公告)日：2013-01-17

申请号：US13492424

申请日：2012-06-08

Applicant: Yoshiro Niitsu ,  Joseph E. Payne ,  John A. Gaudette ,  Zheng Hou ,  Victor Knopov ,  Richard P. Witte ,  Mohammad Ahmadian ,  Loren A. Perelman ,  Yasunobu Tanaka ,  Violetta Akopian

Inventor： Yoshiro Niitsu ,  Joseph E. Payne ,  John A. Gaudette ,  Zheng Hou ,  Victor Knopov ,  Richard P. Witte ,  Mohammad Ahmadian ,  Loren A. Perelman ,  Yasunobu Tanaka ,  Violetta Akopian

IPC: A61K9/127 ,  A61K31/16 ,  C07C235/78 ,  A61K31/166 ,  A61K31/23 ,  A61P1/16 ,  A61P1/18 ,  A61P11/04 ,  C07F9/10 ,  A61K31/685 ,  A61K31/713 ,  C07C229/32 ,  C07C235/48 ,  C07C235/08 ,  C07C235/30

CPC classification number: C07C237/22 ,  A61K9/127 ,  A61K9/1271 ,  A61K31/07 ,  A61K31/713 ,  A61K47/551 ,  C07C233/21 ,  C07C235/08 ,  C07C235/48 ,  C07C2601/16 ,  C07F9/10 ,  C12N15/113 ,  C12N2310/14 ,  C12N2320/32 ,  Y10S977/773 ,  Y10S977/906 ,  Y10S977/907

Abstract: Here described are 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 these compounds which are useful for the targeting and delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.

Abstract translation: 这里描述的是由结构（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的组合物和药物制剂，其可用于治疗剂的靶向和递送; 以及使用这些组合物和药物制剂的方法。

公开(公告)号：US09011903B2

公开(公告)日：2015-04-21

申请号：US13492650

申请日：2012-06-08

Applicant: 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

Inventor： 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: A61K31/225 ,  C07C69/34 ,  A61K9/127 ,  A61K31/7052 ,  A61K47/18 ,  A61K9/00 ,  A61K9/10 ,  A61K31/713 ,  C12N15/113

CPC classification number: C07C237/08 ,  A61K9/0019 ,  A61K9/10 ,  A61K9/1271 ,  A61K31/713 ,  A61K47/186 ,  A61K47/543 ,  C07C323/60 ,  C07C333/04 ,  C12N15/113

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=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.

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。

公开(公告)号：US20130022665A1

公开(公告)日：2013-01-24

申请号：US13492650

申请日：2012-06-08

Applicant: 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

Inventor： 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: A61K31/225 ,  A61K9/127 ,  A61K31/7052 ,  C07C69/34

CPC classification number: C07C237/08 ,  A61K9/0019 ,  A61K9/10 ,  A61K9/1271 ,  A61K31/713 ,  A61K47/186 ,  A61K47/543 ,  C07C323/60 ,  C07C333/04 ,  C12N15/113

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=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.

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。