Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1995-12-11
1997-04-29
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514539, 514546, 514618, 514630, 560 42, 560138, 564158, 564220, 564354, C07C21718, C07C21758, C07C21302, A61K 31135
Patent
active
056249616
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP95/00187, filed Feb. 10, 1995.
TECHNICAL FIELD
The present invention relates to a novel benzylaminoethoxybenzene derivative which has a superior blocking effect on an .alpha.-adrenoceptor, particularly an .alpha..sub.1 -adrenoceptor and is useful for the prevention and treatment of diseases related to the sympathetic nervous system, such as hypertension, pulmonary hypertension, congestive heart failure, myocardial ischemia, arrhythmia, angina pectoris, peripheral vascular diseases, cardiovascular disorders due to the change in vascular resistance, abnormal serum lipid, benign prostrate hypertrophy, dysuria, diabetes, glaucoma, ocular hypertension, obesity, colic convulsion, gastrointestinal dyskinesia (e.g. irritable intestinal syndromes and constipation) and central nervous diseases (e.g. impotence, depression and senile dementia), a pharmaceutically acceptable salt thereof, a solvate thereof, a method for production thereof and a pharmaceutical composition comprising said compound.
BACKGROUND ART
There have been conventionally investigated and developed blockers of various .alpha..sub.1 -adrenoceptors, and many compounds have been reported. As the compounds having an .alpha..sub.1 -adrenoceptor-blocking effect, for example, Arzneim. Forsh., vol. 17, 305 (1967) discloses moxisylyte hydrochloride, which is not entirely satisfactory in the effect as an .alpha..sub.1 -adrenoceptor blocker. Also, prazosin hydrochloride is used as a therapeutic agent for hypertension and dysuria, whereas it causes side effects such as orthostatic hypotension.
The conventional .alpha..sub.1 -adrenoceptor blockers are not sufficient for the treatment of the diseases mediated by the sympathetic nervous system, such as hypertension, pulmonary hypertension, congestive heart failure, myocardial ischemia, arrhythmia, angina pectoris, peripheral vascular diseases, cardiovascular disorders due to the change in vascular resistance, abnormal serum lipid, benign prostatic hypertrophy, dysuria, diabetes, glaucoma, ocular hypertension, obesity, colic convulsion, gastrointestinal dyskinesia (e.g. irritable intestinal syndromes and constipation) and central nervous diseases (e.g. impotence, depression and senile demantia). In addition, the conventional .alpha..sub.1 -adrenoceptor blockers are known to cause side effects such as orthostatic hypotension. It is therefore an object of the present invention to overcome these defects of the conventional .alpha..sub.1 -adrenoceptor blockers and provide an .alpha..sub.1 -adrenoceptor blocker which exhibits strong .alpha..sub.1 -adrenoceptor-blocking effect and causes less side effects such as orthostatic hypotension.
DISCLOSURE OF THE INVENTION
The present inventors have synthesized various compounds in an attempt to obtain a medicine having superior .alpha..sub.1 -adrenoceptor blocking action on the symptoms mediated by the sympathetic nervous system, such as hypertension, pulmonary hypertension, congestive heart failure, myocardial ischemia, arrhythmia, angina pectoris, peripheral vascular diseases, cardiovascular disorders due to the change in vascular resistance, abnormal serum lipid, benign prostatic hypertrophy, dysuria, diabetes, glaucoma, ocular hypertension, obesity, colic convulsion, gastrointestinal dyskinesia (e.g. irritable intestinal syndromes and constipation) and central nervous diseases (e.g. impotence, depression and senile demantia), and studied their pharmacological actions. As a result, they have found that a specific, novel benzylaminoethoxybenzene derivative is superior in .alpha..sub.1 -adrenoceptor-blocking effect and that it causes less side effects such as orthostatic hypotension, and completed the invention.
Accordingly, the present invention relates to novel benzylaminoethoxybenzene derivatives of the formula (I) ##STR2## wherein R.sup.1 is a hydrogen atom, a lower alkyl, a lower hydroxyalkyl, a lower alkoxyalkyl, an allyl or a benzyl; benzyl; dialkylaminoalkyl or a lower acyl; and lower acylamino, a hydroxy, a lower acyloxy, a
REFERENCES:
patent: 4818772 (1989-04-01), Pontagnier et al.
Muramatsu et al., Eur. J. Pharmacol., vol. 300, pp. 155-157. 1996.
Ban Masakazu
Deguchi Shuhei
Katsushima Takeo
Shinoda Kiyotaka
Taguchi Hiroaki
Japan Tobacco Inc.
Raymond Richard L.
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