Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1997-05-16
2003-01-14
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
06506783
ABSTRACT:
TECHNICAL FIELD
This invention is a pharmaceutical composition that is effective in the treatment of HIV and other viral infections and inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition contains a benzimidazole derivative, the pharmaceutically acceptable salts thereof or mixtures thereof with other viral cancer treatments.
BACKGROUND OF THE INVENTION
HIV and other viral infections are one leading cause of death. HIV is a disease in which a virus is replicated in the body which attacks the body's immune system. The HIV virus is not easily destroyed nor is there a good mechanism for keeping the host cells from replicating the virus. Herpes Simplex is another viral infection which is difficult, if not impossible, to cure. A method of treating these diseases and other viral infections in highly desirable. Clearly a material which would target the HIV virus and inhibit viral replication is highly desirable.
Cancers are a 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-metabolics 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. Therefore, it is an object of this invention to provide a pharmaceutical composition that is effective in inhibiting the growth of tumors and cancers in mammals with mild or no effects on normal cells.
More specifically, it is an object of this invention to provide an anti-cancer composition comprising a pharmaceutical carrier and a benzimidazole derivative as defined herein along with a method for treating such cancers.
These compositions are also effective against viruses and can be used to treat viral infections. Therefore it is another object of this invention to provide a method of treating viral infections such as HIV, influenza and rhinoviruses.
These and other objects will become evident from the following detailed description of this inventions.
A pharmaceutical composition for treatment of viral infections and cancer in mammals, and in particular, warm blooded animals and humans, comprising a pharmaceutical carrier and an effective amount of compound having the formula.
wherein R is selected from the group consisting of H, carboxyl (—CO
2
H), hydroxyl, amino or esters (O
2
) wherein R is selected from the group consisting of alkoxy, haloalkyl, alkenyl, and cycloalkyl wherein the alkyl groups have from 1-8 carbons or CH
3
CH
2
(OCH
2
CH
2
)
n
—or CH
3
CH
2
CH
2
(OCH
2
CH
2
CH
2
)
n
—or (CH
3
)
2
CH—and
and (OCH(CH
3
)CH
2
)
N
—wherein n is from 1-3 or the pharmaceutically acceptable inorganic or organic acid salts thereof, or mixtures thereof. The preferred alkyl groups are straight chain. Preferably the halogen is substituted on the terminal carbon, and the halogen is chlorine. The preferred cycloalkyl groups are those having 3-6 carbon atoms. The cycloalkyl groups also include those which are substituted on an alkyl chain, 2-cyclopropylethyl, cyclopropylmethyl, 2-cyclopropyl propyl or 2-cyclopropylpropyl or cyclohexylmethyl. Preferred compounds are those having the formulas:
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.
DETAILED DESCRIPTION OF THE INVENTION
A. DEFINITIONS:
As used herein, the term “comprising” means various components can be conjointly employed in the pharmaceutical composition of this invention. Accordingly, the term “consisting essentially of ” and “consisting of” are embodied in the term comprising.
As used herein, a “pharmaceutically acceptable” component is one that is suitable for use with humans and/or animals without undue adverse side effects (such as toxicity, irritation, and allergic response) commensurate with a reasonable benefit/risk ratio.
As used herein, the term “safe and effective amount” refers to the quantity of a component which is sufficient to yield a desired therapeutic response without undue adverse side effects (such as toxicity, irritation, or allergic response) commensurate with a reasonable benefit/risk ratio when used in the manner of this invention. The specific “safe and effective amount” will, obviously, vary with such factors as the particular condition being treated, the physical condition of the patient, the type of mammal being treated, the duration of the treatment, the nature of concurrent therapy (if any), and the specific formulations employed and the structure of the compounds or its derivatives.
As used herein, a “pharmaceutical addition salts”a is salt of the anti-cancer compound with an organic or inorganic acid. These preferred acid addition salts are chlorides, bromides, sulfated, nitrates, phosphates, sulfonates, formates, tartrates, maleates, malates, citrates, benzoates, salicylates, ascorbates, and the like.
As used herein, a “pharmaceutical carrier” is a pharmaceutically acceptable solvent, suspending agent or vehicle for delivering the anti-cancer agent to the animal or human. The carrier may be liquid or solid and is selected with the planned manner of administration in mind.
As used herein, “cancer” refers to all types of cancers or neoplasm or malignant tumors found in mammals, including leukemia.
As used herein, the “anti-cancer compounds” are benzimidazole derivatives, and their salts. The exact benzimidazoles derivatives are described in detail below.
As used herein “chemotherapeutic agents” includes DNA-interactive Agents, Antimetabolites, Tubulin-Interactive Agents, Hormonal agents and others, such as Asparaginase or hydroxyurea.
As used herein, “viruses” includes viruses which cause diseases (viral infection) in man and other warm blooded animals such as HIV virus, herpes, influenza and rhinoviruses.
As used herein “potentiators” are materials such as triprolidine and its cis-isomer and procodazole which are used in combination with the chemotherapeutic agents and benzimidazole derivatives.
As used herein “significantly reduce” means to reduce the mass of the tumor by significant amount. This will usually be to less than 50% of its original mass, and preferably to reduce the mass to non-detectable amounts.
B. THE ANTI-CANCER AND ANTI-VIRAL COMPOUNDS
The anti-cancer and anti-viral compounds are benzimidazole derivatives. These derivatives have the formula:
wherein R is selected from the group consisting of H, carboxyl (—CO
2
H), hydroxyl, amino or esters (—CO
2
R′) wherein R′ is selected from the group of alkoxy, haloalky
Goldberg Jerome D.
Hersko Bart S.
The Procter & Gamble & Company
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