A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
167/199
A61K 31/70 (2006.01) A61K 51/04 (2006.01) C07H 15/18 (2006.01) C07H 15/203 (2006.01) C12Q 1/34 (2006.01) G01N 33/50 (2006.01)
Patent
CA 1148086
Abstract of the Disclosure Hyperacidified tumors having high .beta.-glucuronidase activity can be treated with glucuronides with aglycones toxic to the tumor cells with great safety toward the rest of the body by first administering an alkalinizing agent in an amount sufficient to maintain the pH level of non- tumor tissues at approximately 7.4 during the glucuronide treatment. This will cause inactivation of .beta.-glucuronidase activity in the rest of the body. When nitrile-containing aglycones are used sodium thiosulfate is also administered to avoid cyanide poisoning. Novel glucuronides are disclosed the aglycones of which exert a higher toxic effect in an acid environment or are water-soluble only in an alkaline environ- ment. Such compounds have particular utility with the above process. By substituting radioisotopes into the aglycone, diagnosis and in situ radiation therapy may be accomplished. Bacterial cells having .beta.-glucuronidase activity may also be diagnosed and treated in accordance with the present invention. A urine test is disclosed to determine the amount of free glucuronic acid in the urine which is an indication of the presence of a tumor in the body having high .beta.-glucu- ronidase activity. Novel methods of synthesizing the glucu- ronide used in the present invention are also disclosed.
337483
Mcfadden Fincham
Rubin David
Schwartz Irwin S.
Schwimmer Adolf W.
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