The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 28, 1993

Filed:

Dec. 13, 1991
Applicant:
Inventor:

Arnold Glazier, Newton, MA (US);

Assignee:

Other;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A01N / ; A01N / ; A01N / ; A61K / ; C07F / ;
U.S. Cl.
CPC ...
558166 ; 514118 ; 514553 ; 514603 ; 514114 ; 558169 ; 558170 ; 558171 ; 558172 ; 562 67 ; 564 85 ; 564 94 ;
Abstract

The composition, methods of synthesis, and applications of a new class of tumor selective antineoplastic drugs is described. These novel antineoplastic agents are of the general structure: A-C-B. The agents are designed with two key functionalities: a trigger which toxifies the drug; (A) and a deactivator which detoxifies the drug (B) The trigger is selected such that it is activated by an enzyme which is present in elevated levels in the tumor. The deactivator is selected such that it is actuated by an enzyme ubiquitous to all tissues. The fate of the drug in a given cell is then determined by the ratio of the enzymatic activity that triggers toxication to the enzymatic activity which detoxifies the drug. The partitioning of the drug between toxic metabolite and nontoxic metabolite defines the resulting specificity of cytotoxic effect. The application of this invention is exemplified by a new class of antineoplastic drugs which are designed to be selectively toxic for tumor cells bearing the enzyme guanidinobenzoatase.


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