Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-08-09
2001-10-16
Goldberg, Jerome D. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
06303646
ABSTRACT:
This invention relates to cancer treatments and especially to cancer treatments directed to protein kinase C &agr; enzyme.
BACKGROUND OF THE INVENTION
Researchers have recognized that a family of enzymes known as protein kinase C enzymes is associated with a large number of cancers. This family includes at least eleven isoenzymes. A particular member of this family is identified as the protein kinase C alpha enzyme, abbreviated: PKC &agr;.
Researches have reported increases in PKC &agr; activity in human breast tumors (NG et al.,
Science.
283:2085-2089) and significant increases in PKC &agr; expression in prostate cancers (Cornford et al.,
Am. J. Pathol.
154: 137-144). Researchers have reported that PKC &agr; is required for the metastasis of human melanoma (Dennis et al.,
Cancer Lett.
128:65-70) and that PKC &agr; is related to the progression of brain tumors (Shen et al.,
Mol. Pharmacol.
55:396-402). There is general agreement among many cancer researchers that some of the most dangerous cancers can be treated with chemotheraputic agents or specially designed oligonuclotides targeted to PKC &agr;.
Recently, Muller et al were granted a patent, U.S. Pat. No. 5,744,460, which discloses a cancer treatment utilizing an antisense oligonuclotide targeted to PKC &agr; combined with a chemotherapeutic agent. U.S. Pat. Nos. 5,882,927 and 5,885,970 issued to Bennett et al also disclose antisense oligonuclotides targeted to PKC. Several patents that disclose PKC &agr; inhibitors for treating cancers have been issued to Heath, Jr., et al. These include U.S. Pat. No. 5,843,935. U.S. Pat. No. 5,723,456 is another example of a cancer treatment in which a PKC directed emzyme is proposed as a method to treat cancer. U.S. Pat. No. 5,821,072 granted to Schwartz, et al proposes the use of certain chemotherapeutic agents to attempt to reduce PKC activity. The disclosures of the above listed patents are incorporated herein by reference.
A chemical known as Gö6976, available from Calbiochem Corp. and Alexis Corp. (both with offices in San Diego, Calif.), is known to be an inhibitor of PKC &agr;. Gö6976 is designated as C24H18N40 and a diagram of the molecule is presented in FIG.
1
. Applicant et al reported in Molecular Cellular Biology, 17:3418-3428 based on a variety of experiments that Gö6976 prevented TPA-induced downregulation of the of PKC &agr; and is a more specific inhibitor for PKC &agr;.
What is needed is a better treatment for cancer.
SUMMARY OF THE INVENTION
The present invention provides a chemotheraputic cancer treatment in which Gö6976 or one of its derivatives is administered to a mammal for the treatment of the cancer. The Gö6976 or its derivative is directed to PKC &agr; activity. Experiments have shown Gö6976 to be effective for the treatment of breast cancer, leukemia, lung cancer, bone cancer and skin cancer. These treatments may be accomplished utilizing Gö6976 or its derivatives alone or in combination with prior art chemotherapy agents or with radiation therapy. In a preferred embodiment Gö6976 is used for the treatment of cancer as a preventative drug by preventing cancer cell formation.
REFERENCES:
patent: 5489608 (1996-02-01), Kleinschroth et al.
patent: 5723456 (1998-03-01), Jirousek
patent: 5744460 (1998-04-01), Muller
patent: 5821072 (1998-10-01), Schwartz
patent: 5843935 (1998-12-01), Heath, Jr.
patent: 5882927 (1999-03-01), Bennett
patent: 5885970 (1999-03-01), Bennett
Lu Zhimin
Wang Keming
Goldberg Jerome D.
Ross John R.
Ross, III John R.
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