Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1996-07-16
2001-03-13
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...
C514S383000, C424S649000
Reexamination Certificate
active
06200992
ABSTRACT:
TECHNICAL FIELD
This invention is a pharmaceutical composition that inhibits the growth of cancers, leukemia and tumors in mammals, particularly in human and warm blooded animals. The composition contains a 1H-1,2,4-triazole derivative and a chemotherapeutic agent.
BACKGROUND OF THE INVENTION
Cancers are the leading cause of death in animals and humans. The exact cause of cancer is not known, but links between certain activities such as smoking or exposure to carcinogens and the incidence of certain types of cancers and tumors has been shown by a number of researchers.
Many types of chemotherapeutic agents have been shown to be effective against cancers and tumor cells, but not all types of cancers and tumors respond to these agents. Unfortunately, many of these agents also destroy normal cells. The exact mechanism for the action of these chemotherapeutic agents are not always known.
Despite advances in the field of cancer treatment the leading therapies to date are surgery, radiation and chemotherapy. Chemotherapeutic approaches are said to fight cancers that are metastasized or ones that are particularly aggressive. Such cytocidal or cytostatic agents work best on cancers with large growth factors, i.e., ones whose cells are rapidly dividing. To date, hormones, in particular estrogen, progesterone and testosterone, and some antibiotics produced by a variety of microbes, alkylating agents, and anti-metabolites form the bulk of therapies available to oncologists. Ideally cytotoxic agents that have specificity for cancer and tumor cells while not affecting normal cells would be extremely desirable. Unfortunately, none have been found and instead agents which target especially rapidly dividing cells (both tumor and normal) have been used.
Clearly, the development of materials that would target tumor cells due to some unique specificity for them would be a breakthrough. Alternatively, materials that were cytotoxic to tumor cells while exerting mild effects on normal cells would be desirable. It is believed that the 1H-1,2,4-triazole when used in conjunction with chemotherapeutic agents can both reduce and suppress the growth of cancers, tumors and leukemia. Therefore, it is an object of this invention to provide a pharmaceutical composition that is effective in suppressing and inhibiting the growth of tumors and cancers in mammals with mild or no effects on normal cells.
It has been found that the 1H-1,2,4-triazole derivatives are especially effective in suppressing the growth of the cancer, tumor, virus, or bacteria. The use of these 1H-1,2,4-triazole derivative in combination with other chemotherapeutic agents which are effective in destroying the tumor is a novel method of treatment of cancers and tumors
More specifically, it is an object of this invention to provide an anti-cancer composition comprising a pharmaceutical carrier and a 1H-1,2,4-triazole derivative and a chemotherapeutic agent along with a method for treating such cancers. Potentiators may also enhance the effectiveness of this composition.
These and other objects will become evident from the following detailed description of this inventions.
SUMMARY OF THE INVENTION
A pharmaceutical composition for treatment of mammals, and in particular, warm blooded animals and humans, comprising a pharmaceutical carrier and an effective amount of a chemotherapeutic agent and a safe and effective amount of an anti-cancer compound selected from the group consisting of:
wherein Z is an alkylene selected from the group consisting of CH
2
—CH
2
—,—CH
2
—CH
2
—CH
2
—, —CH(CH
3
)—CH(CH
3
)— and —CH
2
—CH(alkyl) wherein said alkyl has from 1 to about 10 carbon atoms; and Ar is a member selected from the group consisting of phenyl, substituted phenyl, thienyl, halothienyl, naphthyl and fluorenyl, wherein “substituted phenyl” has the meaning of a phenyl radical having thereon from 1 to 3 substituents selected independently from the group consisting of halo, lower alkyl, lower alkyloxy, cyano and nitro. The therapeutically active acid addition salts of the foregoing compound (I) are also embraced within the scope of this invention.
As used in the foregoing definition of Z, the term “alkyl” is meant to include straight and branch chained hydrocarbon radicals having from 1 to about 10 carbon atoms, such as, for example, methyl, ethyl, 1-methylethyl, propyl, 1,1-dimethylethyl, butyl, pentyl, hexyl, heptyl, octyl, decyl and the like; as used herein “lower alkyl” may be straight or branch chained saturated hydrocarbons having from 1 to 6 carbon atoms, such as, for example, methyl, ethyl, propyl, 1-methylethyl, butyl, 1,1-dimethylethyl, pentyl, hexyl and the like alkyls; and the term “halo” is generic to halogen atoms of atomic weight less than 127; i.e., fluoro, chloro, bromo and iodo.
These compositions can be used to inhibit the growth of cancers and other tumors in humans or animals by administration of an effective amount either orally, rectally, topically or parenterally, intravenously or by injection into the tumor. These compositions do not significantly affect healthy cells as compared to adriamvcin which has a detrimental effect on healthy cells. Potentiators may be included in the compositions.
The 1H-1,2,4-triazole derivatives along with the potentiators compositions can also be used to treat viruses. Combinations with other fungicides are also effective.
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Physicians Desk Reference, 15:35:33, Diflucan, Medical Economics Data Production Co, Montvale, NJ (1995).
Benzaquen et al, Nature Medicine, 1, (6), Jun. 1995.
Schwartz, “Inhibition of all-trans-retinoic acid metabolism by fluconazole in vitro and in patents with acute promyelocytic leukemia,” Biochemical Pharmacology, vol. 50, No. 7, 923-928, (1995).
Dabek Rose Ann
Goldberg Jerome D.
Miller Steven W.
The Procter & Gamble & Company
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