Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-06-24
2001-09-04
Jarvis, William R. A. (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
06284760
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to a new use of aminopiperazine derivatives and pharmaceutically acceptable salts thereof for the treatment and/or prevention of schizophrenia, depression, stroke; head injury, nicotine withdrawal, spinal cord injury, anxiety, pollakiuria, incontinence of urine, myotonic dystrophy, attention deficit hyperactivity disorder, excessive daytime sleepiness (narcolepsy), Parkinson's disease or autism in mammals
2. Description of the Background
The aminopiperazine derivatives used in this invention are known as described in PCT International Publication No. WO 91/01979 that said aminopiperazine derivatives possess the potentiation of the cholinergic activity and are useful in the treatment of disorders in the central nervous system for human beings, and more particularly in the treatment of amnesia, dementia, senile dementia and the like.
SUMMARY OF THE INVENTION
The present invention relates to a new use of aminpiperazine derivatives and pharmaceutically acceptable salts thereof for the treatment and/or prevention of schizophrenia, depression, stroke, head injury, nicotine withdrawal, spinal cord injury, anxiety, pollakiuria, incontinence of urine, myotonic dystrophy, attention deficit hyperactivity disorder, excessive daytime sleepiness (narcolepsy), Parkinson's disease or autism for mammals.
Accordingly, this invention is to provide a new use of aminopiperazine derivatives and pharmaceutically acceptable salts thereof for treating and/or preventing schizophrenia, depression, stroke, head injury, nicotine withdrawal, spinal cord injury, anxiety, pollakiuria, incontinence of urine, myotonic dystrophy, attention deficit hyperactivity disorder, excessive daytime sleepiness (narcolepsy), Parkinson's disease or autism.
Further, this invention is to provide an agent and a pharmaceutical composition for treating and/or preventing schizophrenia, depression, stroke, head injury, nicotine withdrawal, spinal cord injury, anxiety, pollakiuria, incontinence of urine, myotonic dystrophy, attention deficit hyperactivity disorder, excessive daytime sleepiness (narcolepsy), Parkinson's disease or autism, which comprises said aminopiperazine derivatives and pharmaceutically acceptable salt thereof.
Still further, this invention is to provide a therapeutic method for the treatment and/or prevention of schizophrenia, depression, stroke, head injury, nicotine withdrawal, spinal cord injury, anxiety, pollakiuria, incontinence of urine, myotonic dystrophy, attention deficit hyperactivity disorder, excessive daytime sleepiness (narcolepsy), Parkinson's disease or autism, which comprises administering said said aminopiperazine derivatives and pharmaceutically acceptable salts thereof to mammals.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
The aminopiperazine derivatives used in this invention can be represented by the following general formula la [I]:
wherein R
1
is lower alkyl, aryl, ar(lower)alkoxy or a heterocyclic group, each of which may be substituted with halogen,
R
2
is hydrogen or lower alkyl,
R
3
is cyclo(lower)alkyl, aryl or ar(lower)alkyl, each of which may be substituted with halogen,
A is
—SO
2
— or lower alkylene, and
Y is
—SO
2
— or
and pharmaceutically acceptable salts thereof.
Said compound (I) and pharmaceutically acceptable salts thereof are useful in the treatment and/or prevention of schizophrenia, depression, stroke, head injury, nicotine withdrawal, spinal cord injury, anxiety, pallkiuria, incontinence of urine, myotonic dystrophy, attention deficit hyperactivity disorder, excessive daytime sleepiness (narcolepsy), Parkinson's disease or autism in mammals.
Particulars of the various definitions mentioned in this specification and preferred examples thereof are explained in the following.
The term “lower” is intended to mean a group having 1 to 6 carbon atom(s), unless otherwise provided.
Suitable “lower alkyl” may be a straight or branched one such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl, or the like, in which preferable one is methyl.
Suitable “aryl” may be phenyl, naphthyl, tolyl, xylyl, mesityl, cumenyl, and the like, Ln which preferable one is phenyl or naphthyl.
Suitable “ar(lower)alkoxy” may be benzyloxy, phenethyloxy, phenylpropoxy, benzhydryloxy, trityloxy and the like.
Suitable “heterocyclic group” may include saturated or unsaturated, monocyclic or polycyclic one containing at least one hetero atom such as nitrogen atom, oxygen atom or sulfur atom.
The preferred examples of thus defined “heterocyclic group” may be an unsaturated, 3 to 8-membered, more preferably 5 or 6-membered heteromonocyclic group containing 1 to 4-nitrogen atom(s), for example, pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyridyl N-oxide, dihydropyridyl, tetrahydropyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazinyl, triazolyl, tetrazinyl, tetrazolyl, etc.;
unsaturated, condensed heterocyclic group containing 1 to 5 nitrogen atom(s), for example, indolyl, isoindolyl, indolizinyl, benzimidazolyl, quinolyl, isoquinolyl, indazolyl, benzotriazolyl, etc.;
unsaturated, 3 to 8-membered heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3 nitrogen atom(s), for example, oxazolyl, isoxazolyl, oxadiazolyl, etc.;
saturated, 3 to 8-membered heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3 nitrogen atom(s), for example, morpholino, sydnonyl, etc.;
unsaturated, condensed heterocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3 nitrogen atom(s), for example, benzoxazolyl, benzoxadiazolyl, etc.;
unsaturated, 3 to 8-membered heteromonoyclcic group containing 1 to 2 sulfur atom(s) and 1 to 3 nitrogen atom(s), for example, thiazolyl, isothiazolyl, thiadiazolyl, etc.;
unsaturated, 3 to 8-membered heteromonocyclic group containing 1 to 2 sulfur atom(s), for example, thienyl, etc.;
unsaturated, condensed heterocyclic group containing 1 to 2 sulfur atom(s) and 1 to 3 nitrogen atom(s), for example, benzothiazolyl, benzothiadiazolyl, etc.;
unsaturated, 3 to 8-membered heteromonocyclic group containing an oxygen atom, for example, furyl, etc.;
unsaturated, condensed heterocyclic group containing 1 to 2 sulfur atom(s), for example, benzothienyl, etc.;
unsaturated, condensed heterocyclic group containing 1 to 2 oxygen atom(s), for example, benzofuranyl, etc.; or the like.
Suitable “cyclo(lower)alkyl” may be cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and the like.
Suitable “ar(lower)alkyl” may be benzyl, phenethyl, phenylpropyl, benzhydryl, trityl, and the like.
Suitable “lower alkylene” may be methylene, ethylene, propylene, pentamethylene, hexamethylene, and the like.
The above-mentioned “lower alkyl”, “aryl”, “ar(lower)alkoxy”, “heterocyclic group”, “cyclo(lower)alkyl” and “ar(lower)alkyl” may be substituted with halogen [e.g. fluorine, chlorine, bromine and iodine].
Preferred compound [I] is one which has a lower alkyl, phenyl, naphthyl or thienyl for R
1
, hydrogen or lower alkyl for R
2
, phenyl which may be substituted with a halogen for R
3
,
for A, and
or —SO
2
— for Y.
More preferred compound [I] is one which has a lower alkyl for R hydrogen for R
2
, phenyl which is substituted with a halogen for R
3
,
for A, and
for Y.
Most preferred compound [I] is N-(4-acetyl-1-piperazinyl)-4-fluorobenzamide.
Suitable pharmaceutically acceptable salts of the compound [I] are conventional non-toxic salts and include acid addition salt such as an inorganic acid addition salt [e.g. hydrochloride, hydrobromide, sulfate, phosphate, etc.], an organic acid addition salt [e.g. formate, acetate, trifluoroacetate, maleate, tartrate, methanesulfonate, benzenesulfonate, toluenesulfonate, etc.], a salt with an amino acid [e.g. aspartic acid salt, glutamic acid, salt, etc.] and the like.
It is to be noted that the compound [I] may include one or more stereoisomer(s) due to asymmetric carbon atoms, and all of such isomers and mixture thereof are i
Kelly John S.
Marston Hugh M.
Fujisawa Pharmaceutical Co. Ltd.
Jarvis William R. A.
Oblon & Spivak, McClelland, Maier & Neustadt P.C.
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