INDENOISOQUINOLINE-RELEASABLE POLYMER CONJUGATES
First Claim
Patent Images
1. A compound of Formula (I) wherein A is a capping group R is a substantially non-antigenic water-soluble polymer;
- and L and L′
are independently selected releasable linkers.
2 Assignments
0 Petitions
Accused Products
Abstract
The present invention provides releasably-linked indenoisoquinoline polymer conjugates. Methods of making the conjugates and methods of treating mammals using the same are also disclosed.
-
Citations
25 Claims
-
1. A compound of Formula (I)
wherein A is a capping group R is a substantially non-antigenic water-soluble polymer; - and
L and L′
are independently selected releasable linkers. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24)
- and
-
25. A method of preparing a compound of Formula (III), comprising;
-
(a) providing an activated polymer having the structure; (b) reacting the activated polymer with a protected indenoisoquinoline having the structure; (c) removing the protecting group from the resulting intermediate of step (b) to form the compound of Formula (III); wherein A is a capping group or R is a substantially non-antigenic water-soluble polymer; L1 is a bifunctional linking moiety; Y1-4 are independently O, S, or NR12; R1, R4, R9, R10, and R12, are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, and substituted C1-6 heteroalkyls; R2, R3, R5 and R6 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C1-6 alkoxy, phenoxy, C1-8 heteroalkyls, C1-8 heteroalkoxy, substituted C1-6 alkyls, C3-8 cycloalkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, halo-, nitro-, cyano-, carboxy-, C1-6 carboxyalkyls and C1-6 alkyl carbonyls; Ar is an aromatic moiety which when included in Formula (II) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heteroaromatic group; (r), (s), (t), and (u) are independently zero or one; (m) and (p) are independently zero or a positive integer; B1 is a leaving group; and B2 is a protecting group.
-
Specification