US 9,808,533 B2
Multi-arm polymer prodrugs
Xuan Zhao, Beijing (CN); Michael David Bentley, Huntsville, AL (US); Zhongxu Ren, Foster City, CA (US); and Tacey X. Viegas, Madison, AL (US)
Assigned to Nektar Therapeutics, San Francisco, CA (US)
Filed by Nektar Therapeutics, San Francisco, CA (US)
Filed on May 2, 2016, as Appl. No. 15/144,440.
Application 15/144,440 is a continuation of application No. 14/323,993, filed on Jul. 3, 2014, granted, now 9,333,200, issued on May 10, 2016.
Application 14/323,993 is a continuation of application No. 13/765,433, filed on Feb. 12, 2013, granted, now 8,771,662, issued on Jul. 8, 2014.
Application 13/765,433 is a continuation of application No. 11/948,767, filed on Nov. 30, 2007, granted, now 8,394,365, issued on Mar. 12, 2013.
Application 11/948,767 is a continuation in part of application No. 10/943,799, filed on Sep. 17, 2004, granted, now 7,744,861, issued on Jun. 29, 2010.
Claims priority of provisional application 60/503,673, filed on Sep. 17, 2003.
Claims priority of provisional application 60/584,308, filed on Jun. 30, 2004.
Claims priority of provisional application 60/861,995, filed on Nov. 30, 2006.
Claims priority of provisional application 61/003,163, filed on Nov. 14, 2007.
Prior Publication US 2017/0056514 A1, Mar. 2, 2017
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/00 (2006.01); A61K 47/48 (2006.01); A61K 31/4709 (2006.01)
CPC A61K 47/48215 (2013.01) [A61K 31/4709 (2013.01)] 21 Claims
OG exemplary drawing
 
1. A multi-arm polymer prodrug having the structure:
R(-Q-POLY1-X-D)q   I
wherein
R is an organic radical possessing from 3 to 25 carbon atoms,
Q is a linker, wherein R, when taken together with Q to form R(-Q-)q, is a residue of a polyol after removal of a proton,
POLY1 is a water-soluble poly(alkylene glycol) polymer,
X is a spacer having an atom length of from 5 atoms to 25 atoms possessing the structure Y—Z, where Y has the structure —(CH2)a—C(O)NH—(CH2)b—(CH2CH2O)c— and, Z is C(O)—O—, or O—C(O)—O—,
a ranges from 0 to 12,
b ranges from 0 to 12,
c ranges from 0 to 25,
D is a water-soluble camptothecin, and
q is selected from 3, 4, 5, 6, 7, 8, 9, and 10,
or a pharmaceutically acceptable salt form thereof.