Title:
薬物送達を標的化しｓｉＲＮＡ活性を増強する化合物
Document Type and Number:
Japanese Patent JP6590888
Kind Code:
B2
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=1-4; wherein c=1-4; 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.
Inventors:
Yoshiro Niitsu
Payne, Joseph E.
Ho, Zen
Gaudette, John A.
Perelman, Loren A.
Yasunori Tanaka
Vicotta, accopian
Kalmari, Priya
Sridal, C. Nagarajan
Kinopov, Victor
Witte, Richard P.
Ahmadian, Mohammed
Payne, Joseph E.
Ho, Zen
Gaudette, John A.
Perelman, Loren A.
Yasunori Tanaka
Vicotta, accopian
Kalmari, Priya
Sridal, C. Nagarajan
Kinopov, Victor
Witte, Richard P.
Ahmadian, Mohammed
Application Number:
JP2017203199A
Publication Date:
October 16, 2019
Filing Date:
October 20, 2017
Export Citation:
Assignee:
NITTO DENKO CORPORATION
International Classes:
A61K47/69; A61K9/127; A61K31/713; A61K47/18; A61K47/20; A61K47/24; A61K47/60; A61P35/00; A61P43/00; C07C237/22; C07C403/20; C08G65/329
Domestic Patent References:
| JP2001501639A | ||||
| JP2005507934A |
Foreign References:
| WO2010029760A1 | ||||
| WO2010014117A1 |
Other References:
Journal of Medicinal Chemistry,2010年,Vol.53, No.9,p.3782-3792
Attorney, Agent or Firm:
Misa Odagiri
Kiyoji Kuzuwa
Kiyoji Kuzuwa