US 11,707,483 B2
Micellic assemblies
Patrick S. Stayton, Seattle, WA (US); Allan S. Hoffman, Seattle, WA (US); Anthony Convertine, Seattle, WA (US); Craig L. Duvall, Nashville, TN (US); Danielle Benoit, Rochester, NY (US); Robert Overell, Shoreline, WA (US); Paul H. Johnson, Snohomish, WA (US); Anna S. Gall, Woodinville, WA (US); Mary G. Prieve, Lake Forest Park, WA (US); Amber E. E. Paschal, Redmond, WA (US); Charbel Diab, Seattle, WA (US); and Priyadarsi De, Mohanpur (IN)
Assigned to UNIVERSITY OF WASHINGTON, Seattle, WA (US); and GENEVANT SCIENCES GMBH, Basel (CH)
Filed by University of Washington, Seattle, WA (US); and GENEVANT SCIENCES GMBH, Basel (CH)
Filed on Sep. 23, 2019, as Appl. No. 16/579,662.
Application 16/579,662 is a continuation of application No. 15/499,683, filed on Apr. 27, 2017, granted, now 10,420,790.
Application 15/499,683 is a continuation of application No. 15/059,026, filed on Mar. 2, 2016, granted, now 9,662,403, issued on May 30, 2017.
Application 15/059,026 is a continuation of application No. 12/992,525, granted, now 9,339,558, issued on May 17, 2016, previously published as PCT/US2009/043849, filed on May 13, 2009.
Claims priority of provisional application 61/171,369, filed on Apr. 21, 2009.
Claims priority of provisional application 61/140,774, filed on Dec. 24, 2008.
Claims priority of provisional application 61/112,048, filed on Nov. 6, 2008.
Claims priority of provisional application 61/091,294, filed on Aug. 22, 2008.
Claims priority of provisional application 61/052,908, filed on May 13, 2008.
Claims priority of provisional application 61/052,914, filed on May 13, 2008.
Prior Publication US 2020/0147121 A1, May 14, 2020
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/713 (2006.01); A61K 9/107 (2006.01); C08F 290/06 (2006.01); C08F 293/00 (2006.01); C12N 15/11 (2006.01); C12N 15/87 (2006.01); A61K 47/69 (2017.01); A61K 47/58 (2017.01); A61K 47/54 (2017.01); A61K 47/60 (2017.01); A61K 48/00 (2006.01)
CPC A61K 31/713 (2013.01) [A61K 9/1075 (2013.01); A61K 47/549 (2017.08); A61K 47/58 (2017.08); A61K 47/60 (2017.08); A61K 47/6907 (2017.08); A61K 48/0041 (2013.01); C08F 290/062 (2013.01); C08F 293/005 (2013.01); C12N 15/111 (2013.01); C12N 15/87 (2013.01); C12N 2320/32 (2013.01); Y02A 50/30 (2018.01)] 16 Claims
 
1. A micelle-like assembly, wherein the micelle-like assembly comprises a plurality of block copolymers of Formula I:

OG Complex Work Unit Chemistry
wherein
A0, A1, A2, A3 and A4 are independently selected from the group consisting of —C—, —C—C—, —C(O)(C)aC(O)O—, —O(C)aC(O)—, and —O(C)bO—; wherein,
a is 1-4;
b is 2-4;
Y4 is selected from the group consisting of hydrogen, -(1C-10C)alkyl,-(3C-6C)cycloalkyl, —O—(1C-10C)alkyl, —C(O)O(1C-10C)alkyl, -(4C-10C)heteroaryl, and -(6C-10C)aryl, any of which is optionally substituted with one or more fluorine groups;
Y0, Y1, and Y2 are independently selected from the group consisting of a covalent bond, -(1C-10C)alkyl-, —C(O)O(2C-10C) alkyl-, —OC(O)(1C-10C) alkyl-, —O(2C-10C)alkyl-, —S(2C-10C)alkyl-, —C(O)NR6(2C-10C) alkyl-, -(4C-10C)heteroaryl-, and -(6C-10C)aryl-;
Y3 is selected from the group consisting of a covalent bond, -(1C-10C)alkyl-, -(4C-10C)heteroaryl-, and -(6C-10C)aryl-;
wherein tetravalent carbon atoms of A0-A4 that are not fully substituted with R1-R5 and Y0-Y4 are completed with an appropriate number of hydrogen atoms;
R1, R2, R3, R4, R5, and R6 are independently selected from the group consisting of hydrogen, —CN, alkyl, alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, any of which may be optionally substituted with one or more fluorine atoms;
Q0 is a residue selected from the group consisting of residues which are hydrophilic at physiologic pH; conjugatable or functionalizable residues; and hydrogen;
Q1 is a residue which is hydrophilic at physiological pH;
Q2 is a residue which is positively charged at physiological pH;
Q3 is a residue which is negatively charged at physiological pH, but undergoes protonation at lower pH;
m is a mole fraction of about 0 to less than 1.0;
n is a mole fraction of greater than 0 to about 1.0; wherein m+n=1;
p is a mole fraction of 0.1 to 0.9;
q is a mole fraction of 0.1 to 0.9;
r is present up to a mole fraction of 0.8; wherein p+q+r=1;
v is from about 1 to about 25 kDa; and
w is from about 1 to about 50 kDa.