Piperdine derivatives and hypotensives containing the same

Details Piperdine derivatives and hypotensives containing the same Piperdine derivatives and hypotensives containing the same

1999-02-10

2003-09-23

Raymond, Richard L. (Department: 1611)

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C546S089000, C546S187000, C546S191000, C546S196000, C546S202000, C546S203000, C546S204000, C546S208000, C546S209000, C546S210000, C546S213000, C546S214000

Reissue Patent

active

RE038257

ABSTRACT:

BACKGROUND OF THE INVENTION
FIELD OF THE INVENTION
The present invention relates to a piperidine derivative and hypotensives containing the same.
DESCRIPTION OF THE BACKGROUND
It is said that there are about 13,000,000 patients with hypertension in Japan and its frequency of occurrence in individuals becomes greater with advancing age. Further, as the age of a given population increases, increased attention is directed to hypertension which becomes more and more of a dangerous factor in severe heart and cerebral diseases represented by cardiac infarction and cerebral apoplexy. In recent years, calcium antagonists or angiotensin convertase inhibitors have been widely used as excellent primary selection drugs for treatment of hypertension. But the pharmaceutical effects or safety of these hypotensives have recently come into question.
A need therefore continues to exist for new hypotensive agents which exhibit excellent pharmaceutical effects and safety which can be industrially prepared at low cost and in a simple manner.
SUMMARY OF THE INVENTION
Accordingly, one object of the present invention is to provide an effective hypotensive agent which is relatively simple to prepare at low cost.
Briefly, this object and other objects of the present invention as hereinafter will become more readily apparent can be attained by a piperidine derivative of formula (I):
wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH
2
)
n
, which may be substituted, in which n is 0 or an integer of 1 to 10, —CH≡CH—, —C≡C—, —O—, —S—, —NH—, —N(COCH
3
)—, —N(COOC
2
H
5
)—, —N(CHO)—, —N(CH
3
)—, —CO—, —SO—, or —SO
2
—; Y is —CH≡CH—, —CH
2
CH
2
—, —CH
2
CO—, —O—, —S—, —NH—, —OCH
2
—, —SCH
2
—, —NHCH
2
—, —CH(OH)CH
2
—or —CH (OH) CH (OH) —; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the —(CH
2
)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by —CH≡CH—, —C≡C—, —O—, —S—, —NH—, —N (COCH
3
), —N(COC
2
H
5
)—, —N(CHO)—, —N(CH
3
)—, —CO—, —SO— or —SO
2
—, and wherein one or more of the —(CH
2
)-groups in X and Q may be substituted by —(CH
2
)
4
— or —(CH
2
)
5
— thereby forming a ring structure.


REFERENCES:
patent: 4031222 (1977-06-01), Remy
patent: 4073912 (1978-02-01), Kaiser et al.
patent: 4356184 (1982-10-01), Deason et al.
patent: 4912222 (1990-03-01), Griffith et al.
patent: 5229400 (1993-07-01), Hirasawa et al.
patent: 5231105 (1993-07-01), Shoji et al.
patent: 005 607 (1979-11-01), None
patent: 1 153 977 (1969-06-01), None
White, Chemical Patent Practice, pp. 240-241, 1998.

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