Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-12-20
1997-02-04
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514252, 514249, 514258, 514259, 514183, 514217, 514248, 544368, 544363, 544364, 544354, 544282, 544284, 544 11, 544 52, 544215, 544236, 544235, 544 8, 544 10, 544 47, 544123, 540461, 540592, C07D41714, A61K 3155, A61K 3150, A61K 31495
Patent
active
055998151
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
This application is a 371 of PCT/JP94/00159 filed Feb. 3, 1994.
1. Field of the Invention
The present invention relates to compounds having an anti-psychotic activity and little extrapyramidal side effect, and to an anti-psychotic agent comprising at least one of the compounds and a pharmacologically acceptable salt thereof as an active ingredient.
2. Related Art
There have hitherto been used chlorpromazine, haloperidol and the like as anti-psychotic agents, which involve central side effects such as extrapyramidal effects, for example parkinsonism. The other side effects thus causing clinically serious problems.
In these years, there have been proposed the compounds of the following formula (I), wherein W represents an imide derivative, such as tiospiron or SM-9018 as the compounds with which the aforementioned problems were to be solved (e.g. in EP 464846, Japanese Patent Laid-Open Publication No. 235865/1990, U.S. Pat. No. 4,968,792, U.S. Pat. No. 4,956,368, WO 9002552, EP 329168, EP 314098, Japanese Patent Laid-Open Publication Nos. 10786/1988 and 83067/1988, and DE 3247530).
There are also known the compounds represented by the following general formula (I) in which W represents --O--R and R represents a phenyl derivative (Japanese Patent Application No. 63263/1990), or an imide or amide derivative (Japanese Patent Application No. 4771/1990). Furthermore, there are similarly known the compounds wherein W represents a group having an amide skeleton such as those described in EP 329168, U.S. Pat. No. 4,933,458 or EP 316723, or W represents an aromatic ring or a heteroaromatic ring which is directly bonded to the main structure without intervening a hetero atom such as described in EP 409435, EP 378255, EP 378255, EP 353821, U.S. Pat. No. 4,831,031 and EP 281309.
Although the above compounds have been reported and that the side effects have successfully been reduced, the ratio of a dose for exhibiting anti-psychotic activity to a dose for exhibiting extrapyramidal side effects such as catalepsy causing action remains relatively small. Thus it has been desired to dissociate sufficiently the difference between the effective dose and the side effect causing dose.
SUMMARY OF THE INVENTION
The present inventors have now found that certain compounds have a strong anti-psychotic activity and little extrapyramidal side effect, and thus accomplished the present invention.
Therefore, an object of the present invention is to provide compounds which have an anti-psychotic activity and little extrapyramidal side effect.
Another object of the present invention is to provide an anti-psychotic agent comprising the above derivative.
The compounds according to the present invention are the compounds represented by the general formula (I) ##STR2## wherein n represents an integer of 2-4, and ##STR3## wherein m represents an integer of 0-2, double bond, simultaneously represent N or NH, ##STR4## R.sup.1 represents a hydrogen atom, a halogen atom, a lower alkyl group which may be substituted by halogen atoms, a substituted or unsubstituted phenyl group, a hydroxyl group, a nitro group, a lower alkoxy group, an amino group or a cyano group, hydrogen atom, a halogen atom, a lower alkyl which may be substituted with halogen, lower alkoxy or amino group or a cyano group, provided that R.sup.2 is not present when X represents a bond, or wherein p represents an integer of 3 to 5, to form a substituted or unsubstituted saturated ring or heterocyclic saturated ring, and
The compounds represented by the general formula (I) have a strong anti-psychotic activity and little extrapyramidal side effect. Therefore, an anti-psychotic agent having safety to humans can be proposed according to the present invention.
DETAILED DESCRIPTION OF THE INVENTION
Compounds of the Formula (I)
The term "lower alkyl" or "lower alkoxy" as a group or a part of a group means herein a straight chain or branched chain alkyl or alkoxy group having 1-6 carbon atoms, preferably 1-4 carbon atoms. The term "halogen atom" means a
REFERENCES:
patent: 5001130 (1991-03-01), New et al.
Yaso, M. et al. Chemical Abstract 120:245,158 (1994).
Asahi Chemical Derwent World Patent Index 94-012260 (1994).
Fukuda Yoshimasa
Ichimaru Yasuyuki
Imanishi Taiichiro
Nakatani Yuuko
Sasaki Toshiro
Meiji Seika Kabushiki Kaisha
Shah Mukund J.
Wong King Lit
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