Abstract: Saturated aliphatic straight chain dicarboxylic acids having a total number of carbon atoms which are divisible by four, are selectively toxic to certain tumor cells while non-toxic to normal cells of the same origin. Octacosanedioic acid is particularly preferred as it is a component of normal blood serum. Compositions containing these compounds may be used in the treatment of certain malignancies.
Type:
Grant
Filed:
March 1, 1984
Date of Patent:
January 23, 1990
Assignees:
David Rubin, Ely J. Rubin, Adolf W. Schwimmer, Irwin S. Schwartz, Century Laboratories, Inc.
Abstract: The effectiveness of interferon for treatment against cancer may be increased by first administering an agent for inhibiting tyrosinase. In this manner the tyrosinase which is known to be produced by malignancies, and which may cause inactivation of the interferon, will be substantially inactivated prior to the interferon administration.
Type:
Grant
Filed:
March 29, 1984
Date of Patent:
August 9, 1988
Assignees:
Adolf W. Schwimmer, Irwin Steven Schwartz, David Rubin
Abstract: 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. Novel glucuronides are disclosed the aglycones of which exert a higher toxic effect in an acid environment or is water-soluble only in an alkaline environment. 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.
Type:
Grant
Filed:
October 13, 1978
Date of Patent:
April 22, 1986
Assignees:
Adolf W. Schwimmer, Irwin S. Schwartz, David Rubin
Abstract: Mandelonitrile-.beta.-D-glucuronic acid is produced by condensing a mandelic amide with a tri-O-acetyl methyl ester of glucuronic acid and then reacting the product with acetic anhydride to produce the tri-O-acetyl methyl ester of mandelonitrile-.beta.-D-glucuronic acid. The protecting acetyl groups may be removed and the barium salt formed by reacting with barium hydroxide, which salt, when treated with sulfuric acid, will yield the mandelonitrile-.beta.-D-glucuronic acid. This compound, as well as methacrylonitrile .beta.-D-glucuronic acid may be used in the treatment of bacterial infections having .beta.-glucuronidase activity.
Type:
Grant
Filed:
October 13, 1978
Date of Patent:
January 3, 1984
Assignees:
Adolf W. Schwimmer, Irwin Steven Schwartz, David Rubin
Abstract: A method of diagnosing the presence of tumors having .beta.-glucuronidase activity comprises administering a glucuronide which differs in color or color intensity from the aglycone thereof to a patient. The preferred glucuronide is phenolphthalein glucuronide. The urine is then collecting for a twenty four hour period and the amount of phenolphthalein glucuronides present in the urine is determined. If substantially all of the phenolphthalein glucuronide is expelled then it is apparent that the body has no tumors or bacterial infections exhibiting .beta.-glucuronidase activity. If however substantial amounts of phenolphthalein is retained, then this is an indication of the presence of tumors having .beta.-glucuronidase activity or a bacterial infection having .beta.-glucuronidase activity.
Type:
Grant
Filed:
July 18, 1980
Date of Patent:
September 28, 1982
Assignees:
Adolf W. Schwimmer, Irwin S. Schwartz, David Rubin
Abstract: 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. Novel glucuronides are disclosed the aglycones of which exert a higher toxic effect in an acid environment or is water-soluble only in an alkaline environment. 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.