Methods and compositions for reducing side effects in chemotherapeutic treatments
AssigneePro-Pharmaceuticals, Inc.
InventorsAnatole Klyosov, David Platt
Life of this patent
Estimating the term…
Abstract
A pharmaceutical compound and a process for making the compound is provided where the compound includes a therapeutic agent, a spacer and a galactose, the spacer being covalently linked to the therapeutic agent at a first site on the spacer and covalently linked to the galactose by an ether bond at a second site on the spacer to form a conjugate. The conjugate may be used to treat a subject suffering from a medical condition, so as to reduce the side effects associated with the therapeutic agent by administering an effective dose of the conjugate to the subject so that the side effects in the subject are less then they would have been with the unconjugated therapeutic agent.
Claims29
A pharmaceutical compound, comprising:
- a therapeutic agent, a spacer and a galactose, the spacer being covalently linked to the therapeutic agent at a first site on the spacer and the spacer being covalenly linked via an ether linkage with the galactose at a second site on the spacer wherein the spacer linked to galactose has a formula
- where n=≧0 and ≦20, or
- where n=≧0 and ≦20 and m=≧0 and ≦50.
A method for synthesizing a pharmaceutical compound, comprising:
- (a) providing (i) a therapeutic agent;
- and (ii) a spacer linked to galactose;
- (b) protecting reactive groups on the therapeutic agent other than at a reactive site for linking to the spacer;
- (c) reacting the protected therapeutic agent with the spacer linked to galactose;
- and
- (d) deprotecting the therapeutic agent to form the pharmaceutical compound,
- wherein the protecting, reacting and deprotecting steps are performed using protic solvents.
A method of treating a subject suffering from a medical condition, so as to reduce side effects associated with a therapeutic agent selected for treating the condition without substantially reducing efficacy of the agent, comprising:
- (a) providing as a conjugate, the therapeutic agent covalently linked to a spacer at a first site and galactose covalently linked to the spacer at a second site, wherein the spacer linked to galactose has a formula
- where n=≧0 and ≦20, or
- where n=≧0 and ≦20 and m=≧0 and ≦50;
- and
- (b) administering an effective dose of the conjugate to the subject so that the side effects in the subject are less then they would have been with the unconjugated therapeutic agent.
Dependencies are inferred from the claim text.