Alkoxyphenylalkylamine derivatives

Details Alkoxyphenylalkylamine derivatives Alkoxyphenylalkylamine derivatives

1994-03-31

1996-02-27

Prescott, Arthur C.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acids and salts thereof

564 5, C07C21756, C07C21786, C07C21762

Patent

active

054950465

DESCRIPTION:

BRIEF SUMMARY
CROSS-REFERENCE TO RELATED APPLICATION

The present application was filed under the provisions of 35 usc 371(c) as the U.S. National Phase of PCT application PCT/JP92/10259 filed Sep. 30, 1992.


TECHNICAL FIELD

This invention relates to alkoxyphenylalkylamine derivatives having an antipsychotic action.


BACKGROUND ART

Antipsychotic drugs are used for treating not only schizophrenia but also troublesome behaviors (for example, aggression, mental excitation, fugue, delirium) accompanying cerebrovascular disorders and senile dementia. However, there is a serious problem that these classical antipsychotic drugs cause extrapyramidal disorders as a side effect. In order to solve this problem, approaches have been made in recent years to develop antipsychotic drugs from a viewpoint which is completely different from the action mechanism of the classical drugs. As an example of these approaches, a sigma receptor antagonist may be cited. It is considered that sigma receptor is a receptor participating in mental abnormality such as hallucination. A compound having a specific affinity for this receptor would exhibit an antipsychotic action without causing any extrapyramidal disorders.
Although Rimcazole is known as an example of such a compound, its affinity and specificity for sigma receptor are restricted.
There have been known some compounds, for example, N,N-dimethyl-2-(3-benzyloxy-4-methoxy-phenyl)ethylamine described in J. C. S. Perkin I, (1975), page 1140, which are similar to the compound of the present invention in structure. However, these compounds are described merely as a synthesis intermediate. Thus the action of the compound of the present invention has never been reported hitherto.
It is an object of the present invention to provide a novel compound which has an antipsychotic action without causing any extrapyramidal disorders.


DISCLOSURE OF THE INVENTION

The present inventors have conducted extensive studies on alkoxyphenylalkylamine derivatives. As a result, they have found out a novel alkoxyphenylalkylamine derivative which shows a specific and high affinity for sigma receptor, thus completing the present invention.
Now the present invention will be described in greater detail.
The present invention relates to an alkoxyphenylalkylamine derivative represented by the following formula (I): ##STR2## (wherein X.sup.1 and X.sup.2 may be either the same or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group or an alkoxy group having 1 to 5 carbon atoms, which may be substituted with a phenyl group; R.sup.1 and R.sup.2 may be either the same or different from each other and each represents a hydrogen atom or an alkyl group having 1 to 7 carbon atoms, which may be substituted with "a hydroxyl group, a carboxyl group or an alkoxycarbonyl group" at the end, or, R.sup.1 and R.sup.2 together with the adjacent nitrogen atom represent a pyrrolidino group, a piperidino group, a homopiperidino group, a morpholino group, a piperazino group, a homopiperazino group or a piperazino group substituted with "a phenyl group, a phenyl group substituted with a lower alkyl group or a lower alkoxy group, a pyridyl group, a pyridyl group substituted with a lower alkyl group or a lower alkoxy group, a pyrimidyl group or a pyrimidyl group substituted with a lower alkyl group or a lower alkoxy group"; A represents a phenyl group, a phenyl group substituted with 1 to 3 substituents arbitrarily selected from "a halogen atom, a hydroxyl group and an alkoxy group having 1 to 5 carbon atoms", or a thienyl group; m is an integer of from 2 to 5; and n is an integer of from 2 to 7), and a salt thereof.
In further aspects, the present invention relates to the followings:
an alkoxyphenylalkylamine derivative represented by the following formula: ##STR3## wherein X.sup.1 and X.sup.2 may be either the same or different from each other and each represents a hydrogen atom, a halogen atom or an alkoxy group having 1 to 5 carbon atoms; R.sup.1 and R.sup.2 may be either the same or different from

REFERENCES:
patent: 4329367 (1982-11-01), Francis
patent: 5086054 (1992-02-01), Parish

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