C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
530/15.12, 167/1
C07D 261/04 (2006.01) A61K 47/48 (2006.01) C07C 271/28 (2006.01) C07K 5/083 (2006.01) C07K 5/103 (2006.01) C07K 14/575 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1158557
ABSTRACT OF THE DISCLOSURE Antineoplastic agents are rendered tumor- specific by derivatization with a peptide specifier so as to convert the antineoplastic agent into a pharmacologically inactive pro-drug which is selectively activatible at the tumor site. The peptide specifier has an amino acid residue sequence such that it will be selectively enzymatically cleaved from the antineoplastic agent by tumor-associated fibrinolytic and/or blood- coagulating proteases, such as plasmin and plasminogen activator, so as to effect release of the antineoplastic agent in pharmacologically active form in the vicinity of the tumor. These and other similar hydrolytic enzyme- activatible pro-drugs may be formed with their specifier moiety and their drug moiety covalently linked together through an intermediate self-immolative connector moiety having a molecular structure such that enzymatic cleavage of the bond covalently linking it to the specifier moiety will initiate spontaneous cleavage of the bond covalently linking it to the drug moiety to thereby effect re- lease or the drug in pharmacologically active form.
362379
Carl Philip L.
Katzenellenbogen John A.
Weber Michael J.
Gowling Lafleur Henderson Llp
University Of Illinois Foundation
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