Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1995-03-31
2001-03-20
Travers, Russell (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S811000, C514S812000
Reexamination Certificate
active
06204284
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention is concerned with treating a chemically dependent mammal with a 1-(substitutedphenyl)-3-azabicyclo[3.1.0]hexane in order to reduce or alleviate the dependency.
2. Description of the Prior Art
A series of 1-(substitutedphenyl)-3-azabicyclo[3.1.0]hexanes are described in U.S. Pat. Nos. 4,088,652; 4,118,393; 4,118,417; 4,131,611; 4,196,120 and 4,231,935. In U.S. Pat. No. 4,435,419 a method of treating depression and stress in warm-blooded blooded animals is described.
Chemical dependency in a mammal is the abnormal craving or desire for, or an addiction to a drug. The drug can encompass alcohol or any of the legal prescription medications as well as those compounds such as cocaine and heroin which are sold illegally.
While abstinence is ineffective in drug dependency, other agents are needed in order to compromise the dependency. Products such as tetraethylthiuram disulfide; TETD (Antabuse) are used in sobriety programs, McNichol, R. W., Ewing, J. A., Faiman, M. D. Disulfiram (Antabuse): a unique medical aid to sobriety, Springfield, Ill., Thomas, 1987 and Mendelson, J. H., Mello, N. K., Eds, The Diagnosis and treatment of alcoholism, New York, McGraw-Hill, 1979, 204.
In U.S. Pat. No. 4,942,175 is described the use of a composition containing local anesthetics such as tetracaine, procaine and mixtures with suitable carriers. These agents can be used to treat cocaine addiction with a method called aversion therapy. In U.S. Pat. No. 4,948,803 is described the treatment of withdrawal symptoms resulting from addiction to a drug by treatment with azabicyclo indazole-3-carboxamides. In European Patent Application 90309062.9 published 06.03.91 is described a method of treating a chemical dependency in a mammal administering a compound (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-m-ethyl-1-naphthalenamine, which is also known by the generic name of sertraline.
The most popular agent for the treatment of substance abuse is 4,4-diphenyl-6-dimethylamino-heptanone-3 hydrochloride also know as methadone. The principal actions of therapeutic value are analgesia and sedation and detoxification or maintenance in narcotic addiction.
SUMMARY OF THE INVENTION
It has been found that 1-(substituted-phenyl)-3-azabicyclo[3.1.0]hexanes of the formula:
wherein R is hydrogen, alkyl (C
1
-C
6
); R
1
is hydrogen, mono or disubstituted halogen, alkoxy (C
1
-C
3
), CF
3
, alkyl (C
1
-C
6
); and R
2
is hydrogen, methyl or ethyl, are useful for the prevention or relief of a withdrawal syndrome resulting from addiction to drugs or substances of abuse and for the treatment of chemical dependencies. Examples of chemical dependencies treatable by the method of the present invention are dependencies of alcohol, nicotine, cocaine, heroin, phenobarbitol and benzodiazepines.
It has also been found that 1-(substituted-phenyl)-3-azabicyclo[3.1.0]hexanes can inhibit the re-uptake of 5-hydroxytryptamine(5-HT), norepinephrine(NE) and dopamine(DA) in crude rat brain synaptosomal preparations, and may be useful, therefore, as agents for the treatment and relief of addictive behavior disorders such as, chemical substance abuse, eating disorders resulting in anorexia or obesity and other compulsive disorders.
REFERENCES:
patent: 4435419 (1984-03-01), Epstein et al.
Amit et al., J. Clin. Psychiatry, 52:12(suppl), Dec. 1991.
Beer Bernard
Epstein Joseph William
American Cyanamid Company
Barrett Rebecca R.
Travers Russell
Wang Shengjun
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