Prodrugs built as multiple self-elimination-release spacers
First Claim
Patent Images
1. A compound having a formula selected from
V—
- (W—
)w(X—
)C((A—
)aZ)c,
V—
(W—
)w(X—
)C(D((A—
)aZ)d)c,
V—
(W—
)w(X—
)C(D(E((A—
)aZ)e)d)c, and
V—
(W—
)w(X—
)C(D(E(F((A—
)aZ)f)e)d)c,wherein;
V is an enzymatically removable specifier comprising an optionally protected peptide, which is optionally removable after binding to a receptor, ortaken together, V—
B is an oxidized form of B, wherein B is part of W or X;
each of W and X independently is a single release 1, (4+2n) electronic cascade spacer and has the formula;
1 Assignment
0 Petitions
Accused Products
Abstract
This invention concerns multiple release spacers and spacer systems, which release multiple leaving groups following a single activation. It concerns compounds comprising a specifier linked to two or more of the same or different leaving groups (L in the figure) via a self-eliminating multiple release spacer or spacer system, which compounds upon a single activation step, in particular removal or transformation of the specifier, release at least two leaving groups.
33 Citations
40 Claims
-
1. A compound having a formula selected from
V—- (W—
)w(X—
)C((A—
)aZ)c,
V—
(W—
)w(X—
)C(D((A—
)aZ)d)c,
V—
(W—
)w(X—
)C(D(E((A—
)aZ)e)d)c, and
V—
(W—
)w(X—
)C(D(E(F((A—
)aZ)f)e)d)c,wherein; V is an enzymatically removable specifier comprising an optionally protected peptide, which is optionally removable after binding to a receptor, or taken together, V—
B is an oxidized form of B, wherein B is part of W or X;each of W and X independently is a single release 1, (4+2n) electronic cascade spacer and has the formula; - 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, 25, 26, 27, 28, 29, 30, 32, 33, 34, 35, 36, 37, 38, 39, 40)
- (W—
-
31. A compound selected from the group consisting of
Specification