US 2006/0258656 A1 · Compositions and methods for treating cancer

Abstract

Hypoxia-activated prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Claims30

Dependent claims

A protected anti-neoplastic agent of the formula Hyp-L-N or Hyp-N, wherein

Hyp is a hypoxic activator;
N is an anti-neoplastic agent;
and
L is a linking group of the formula
where X is selected from
where
R6 is unsubstituted alkyl or alkyl substituted with one or more heteroatom containing groups;
R7 is hydrogen, unsubstituted alkyl or alkyl substituted with one or more heteroatom containing groups;
and
Y is a spacer group selected from a substituted or unsubstituted —(CH2)n— chain with n=1-4;
a substituted or unsubstituted —(CH2)n— chain with n=1-4 in which one of the carbon backbone chain atoms is substituted by a heteroatom containing group;
and a delayed release group comprising an aromatic group.

9 more elements

A protected anti-neoplastic agent, in which the anti-neoplastic agent includes one or more protectable hydroxyl groups or amine groups, and wherein one or more of the protectable hydroxyl groups or amine groups is substituted with a group selected from Hyp-L- or Hyp-, wherein Hyp is a hypoxic activator;

and L is a linking group of the formula
where X is selected from
where R6 is unsubstituted alkyl or alkyl substituted with one or more heteroatom containing groups;
R7 is hydrogen, unsubstituted alkyl or alkyl substituted with one or more heteroatom containing groups;
and
Y is a spacer group selected from a substituted or unsubstituted —(CH2)n— chain with n=1-4;
a substituted or unsubstituted —(CH2)n— chain with n=1-4 in which one of the carbon backbone chain atoms is substituted by a heteroatom containing group;
and a delayed release group comprising an aromatic group.

5 more elements

Dependencies are inferred from the claim text.

Facts

Application

10/549,545Filed 29 Mar 2004

Priority

28 Mar 2003

Published

16 Nov 2006

Term ends

Not estimatedThe source records don’t support an estimate.

Classification27 codes

A61K 31/415
Having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole: 1,2-Diazoles
A61K 31/4166
1,3-Diazoles: having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
A61K 31/44
Having six-membered rings with one nitrogen as the only ring hetero atom: non condensed pyridines; Hydrogenated derivatives thereof
A61K 31/5377
1,4-Oxazines, e.g. morpholine: not condensed and containing further heterocyclic rings, e.g. timolol

Abstract

Hypoxia-activated prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Claims30

Dependent claims

A protected anti-neoplastic agent of the formula Hyp-L-N or Hyp-N, wherein

Hyp is a hypoxic activator;
N is an anti-neoplastic agent;
and
L is a linking group of the formula
where X is selected from
where
R6 is unsubstituted alkyl or alkyl substituted with one or more heteroatom containing groups;
R7 is hydrogen, unsubstituted alkyl or alkyl substituted with one or more heteroatom containing groups;
and
Y is a spacer group selected from a substituted or unsubstituted —(CH2)n— chain with n=1-4;
a substituted or unsubstituted —(CH2)n— chain with n=1-4 in which one of the carbon backbone chain atoms is substituted by a heteroatom containing group;
and a delayed release group comprising an aromatic group.

9 more elements

and L is a linking group of the formula
where X is selected from
where R6 is unsubstituted alkyl or alkyl substituted with one or more heteroatom containing groups;
R7 is hydrogen, unsubstituted alkyl or alkyl substituted with one or more heteroatom containing groups;
and
Y is a spacer group selected from a substituted or unsubstituted —(CH2)n— chain with n=1-4;
a substituted or unsubstituted —(CH2)n— chain with n=1-4 in which one of the carbon backbone chain atoms is substituted by a heteroatom containing group;
and a delayed release group comprising an aromatic group.

5 more elements

Dependencies are inferred from the claim text.

Compositions and methods for treating cancer

Life of this patent

Abstract

Claims30

Compositions and methods for treating cancer

Life of this patent

Abstract

Claims30