Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1988-02-17
1990-05-01
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514318, 540575, 540596, 540597, 540600, 540609, 544283, 544335, 544363, 544391, 544403, 546146, 546168, 546174, 546176, 546194, 546196, 546197, 546205, 546206, 546213, 546225, 546236, 546237, 546278, 546281, 548524, 548539, A61K 31445, C07D21100
Patent
active
049218638
DESCRIPTION:
BRIEF SUMMARY
FIELD OF INDUSTRIAL UTILIZATION
The present invention relates to cyclic amine derivatives having excellent medicinal activities.
Prior Art:
Various medicines for cerebral vascular disorders have been proposed. For example, cerebral vasodilator drugs and cerebral metabolism activators have been used. However, no drug which is drastically effective has been proposed as yet. At present, there is no drug effective particularly for cerebral vascular dementia and intellectual function disorders among the symptoms due to cerebral vascular disorders.
OBJECT OF THE INVENTION
After intensive investigations made for the purpose of finding a new compound effective for the treatment of various symptoms due to cerebral vascular disorders, particularly mental symptoms, over a long time under the above-mentioned circumstances, the inventors have found quite effective compounds. The present invention has been completed on the basis of this finding.
Therefore, an object of the present invention is to provide cyclic amine derivatives and pharmacologically acceptable salts thereof which are effective for the treatment of cerebral vascular disorders such as cerebral stroke, apoplexy, infarction and arteriosclerosis and mental symptoms due to multiple infarct dementia. Another object of the invention is to provide a process for producing said compounds or pharmacologically acceptable salts thereof. Still another object of the invention is to provide medicines containing said compound or a pharmacologically acceptable salt thereof as the active ingredient.
Construction and Effect of the Invention:
The intended compounds of the present invention are cyclic amine derivatives of the general formula (I) or pharmacologically acceptable salts thereof: ##STR2##
wherein A represents a substituted or unsubstituted phenyl, pyridyl or thienyl group, substituted or unsubstituted naphthyl, tetralyl, quinolyl, benzofuranyl, quinazolyl or benzothienyl group or a group of the formula: ##STR3## X represents a group of the formula: ##STR4##
n represents an integer of 0 to 4,
m represents an integer of 1 to 3,
Y represents a carbon or nitrogen atom,
Z represents a group of the formula: --CH.sub.2 --, ##STR5## in which R.sup.1 is a hydrogen atom or a lower alkyl, acyl, arylalkyl or heteroarylalkyl group, ##STR6## in which Hal is a halogen atom, ##STR7## in which Hal is a halogen atom, ##STR8## in which Hal is a halogen atom or ##STR9## the symbol " " between Y and Z represents a single or double bond,
the group of the formula: " Z-B" is bonded with the ring in the above formula at the 3- or 4-position, and
B represents a phenyl or naphthyl group which may be substituted with one or two substituents which may be the same or different and which are selected from the group consisting of halogens, lower alkyl groups and lower alkoxy groups.
The lower alkyl groups in the above-mentioned definitions of R.sup.1 and B include, for example, straight-chain or branched alkyl groups having 1 to 6 carbon atoms such as methyl, ethyl, n-propyl, n-butyl, isopropyl, isobutyl, 1-methylpropyl, tertbutyl, n-pentyl, 1-ethylpropyl, isoamyl and n-hexyl groups. Among them, methyl and ethyl groups are the most preferred.
The lower alkoxy groups in the above-mentioned definition of B are those derived from the abovementioned lower alkyl groups. Preferred examples of them include methoxy, ethoxy, propoxy, isopropoxy, butoxy and isobutoxy groups.
The substituents of the "substituted or unsubstituted phenyl group "0 and "substituted or unsubstituted naphthyl group" in the definition of A include, for example, the above-defined lower alkyl and alkoxy groups, hydroxyl group, halogen atoms such as fluorine, bromine, iodine and chlorine, phenyl group and heterocyclic groups having nitrogen atom(s) as the hetero atom such as imidazolyl, pyridyl and pyrazolyl groups. Said compounds may have one to three of these substituents. When the compounds have two or more of these substituents, they may be the same or different.
The phenyl group may have a methylenedioxy or ethylened
REFERENCES:
patent: 3576810 (1968-06-01), Duncan et al.
patent: 4246268 (1981-01-01), Carr
patent: 4665076 (1987-05-01), Mestre et al.
Higurashi Kunizou
Kaneko Takeru
Karibe Norio
Nakamura Takaharu
Nakazawa Takahiro
Eisai Co. Ltd.
Raymond Richard L.
Turnipseed James H.
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