Carbostyril derivatives

Details Carbostyril derivatives Carbostyril derivatives

1981-04-30

1984-03-06

Rivers, Diana G.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

546157, 546158, 546155, A61K 3147, C07D21522

Patent

active

044354045

DESCRIPTION:

BRIEF SUMMARY
THECHNICAL FIELD

The present invention relates to novel carbostyril derivatives and process for producing the same and to a treating agent for preventing thrombosis and embolism containing said carbostyril derivative as the active ingredient.


BACKGROUND ART

There have been known certain numbers of carbostyril derivatives which exhibit useful pharmacological activities. For example, U.S. Pat. No. 4,070,470 and German Pat. (Laid-open) No. 2,527,937 teach carboxyalkoxy substituted carbostyril derivatives having blood platelet aggregation inhibitory effect; German Pat. (Laid-open) No. 2,825,048 teaches aminocarbonylalkoxycarbostyril derivatives having platelet aggregation inhibitory effect, phosphodiesterase inhibitory, effect, antiinflammatory effect, antiulcer effect and vasodilation effect. Further, U.S. Pat. No. 3,682,920 teaches 1-substituted derivatives of 3,4-dihydrocarbostyril which are useful as analgesic agents.
However, these carbostyril derivatives known in the prior art have some side effects, and which will cause some troubles in medical use.


DISCLOSURE OF INVENTION

In consideration of these facts, the present inventors have made extensive studies on carbostyril derivatives for the purpose of to obtain novel carbostyril derivatives having less side effects, particularly less side effects to heart and succeeded the present invention.
Thus the novel carbostyril derivative of the present invention has excellent blood platelet aggregation inhibitory effect, phosphodiesterase inhibitory effect, myocardium contraction increasing effect (positive inotropic effect), anti-ulcer effect, anti-inflammatory effect, hypotensive effect, cerebral blood flow increasing effect, blood platelet clot dissociation effect and thromboxan A.sub.2 antagonism, and therefore it is useful as prophylaxis and treating agent for thrombosis and embolism, such as cerebral apoplexy, cerebral infarction, myocardinal infarction; cerebral blood flow improver, anti-inflammatory agent, anti-asthmatic agent, cardiac stimulant, hypotensive agent and phosphodiesterase inhibitor. Further, the carbostyril derivative represented by the general formula (1) of the present invention has low toxicity and particularly side effects to heart such as increasing of heart rate, cardiovascular hypertrophy, myocardium disorder or the like are very weak, while it can be absorbed into blood well and quickly and can be kept relatively higher concentration in blood and the useful pharmacological effect as mentioned above can be retained for relatively longer period of time.
According to the present invention, there is provided novel carbostyril derivative and its salt represented by the general formula (1), ##STR8## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a phenyl-lower alkyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a group of the formula ##STR9## [wherein A is a lower alkylene group; R.sup.3 is a lower alkyl group, a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkanoyloxy-lower alkyl group or a benzoyloxy-lower alkyl group; and R.sup.4 is a C.sub.3-10 -cycloalkyl group which may have at least one hydroxyl group as the substituent(s) in the cycloalkyl ring, a C.sub.3-10 -cycloalkyl-lower alkyl group, a phenyl group, a phenyl-lower alkyl group which may have at least one lower alkoxy group as the substituent(s) in the phenyl ring, a lower alkyl group which may have at least one hydroxyl group as the substituent(s), a heterocyclic ring residue or a lower alkyl group having one heterocyclic ring residue as the substituent; further, R.sup.3, R.sup.4 and the adjacent nitrogen atom, as well as with or without another nitrogen atom, may form a group of the formula ##STR10## (wherein R.sup.5 is a phenyl group, a C.sub.3-10 -cycloalkyl group or a phenyl-lower alkyl group; and B is a methyne group or a nitrogen atom)]; the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton is a single or double bond; the substituted position of the group of the formul

REFERENCES:
patent: 4070470 (1978-01-01), Makagawa et al.
patent: 4216220 (1980-08-01), Nakagawa et al.
patent: 4298739 (1981-11-01), Nishi et al.
patent: 4313947 (1982-02-01), Nakagawa et al.
Nishi et al., Chemical Abstracts, vol. 90, 203,891x, (1979).
Nishi et al., Chemical Abstracts, vol. 93, 26,291r, (1980).
Nishi et al., Chemical Abstracts, vol. 93, 46,4397y, (1980).
Otsuka Pharm. Co., Ltd., Chemical Abstracts, vol. 95, 97,609c, (1981).
Otsuka Pharm. Co., Ltd., Chemical Abstracts, vol. 96, 181,163f, (1982).
Balazs, Proc. Europ. Soc. Study Drug Tox., vol. 15, pp. 71-79, (1974).

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