W-amino alkylsulfonate derivatives for improving microcirculatio

Details W-amino alkylsulfonate derivatives for improving microcirculatio W-amino alkylsulfonate derivatives for improving microcirculatio

1988-04-04

1989-09-26

Shen, Cecilia

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544394, A61K 31495, C07D29508, C07D29520

Patent

active

048700789

DESCRIPTION:

BRIEF SUMMARY
DESCRIPTION

1. Technical Field
This invention relates to a novel taurine-type compound.
2. Prior Art
Since the lumen diameter of blood vessels is regarded as one of the factors which have great influence on blood flow, vasodilators are used. However, the lumen diameter of blood vessels with arteriosclerosis, etc. is less responsive to drugs, and smooth muscle does not exist in microvessels. Further, from the standpoint of rheology, unless a pressure gradient is varied, blood flow is not sufficiently improved even if lumen diameter of vessels is changed. Therefore, for the improvement of microcirculation under ischemic condition, treatment with vasodilators alone is not expected to produce sufficient effect. Rather, it is very important to positively improve hematological properties from the standpoint of promoting the deformability of erythrocytes and of controlling platelet functions. Thus, therapies for thrombosis or microcirculation disorder from this standpoint have been attaching attention in recent years, and the investigation of the conventional agents for cardiovascular system from hemorheological standpoint has revealed that pentoxifylline, trapidil and dilazep are useful as drugs for improving hematological properties as well.
However, few agent have been developed so far which put stress on the promotion of deformability of erythrocytes and the control of platelet function that have significant hemorheological influence on the flow within microvessels. Therefore, agents that display excellent effects thereon have been demanded.


DISCLOSURE OF THE INVENTION

The main object of the present invention is to satisfy the above demand.
That is, the invention provides agents which can accelerate deformability of erythrocytes and control platelet function to thereby improve microcirculation.
We conducted extensive research on compounds having said effects, and found that certain taurine-type compounds can fulfil the above object, and accomplished the present invention.
The present invention provides a taurine-type compound represented by the formula ##STR2## wherein R is a phenyl group optionally having substituent(s) selected from lower alkyl, halogen-substituted lower alkyl, lower alkoxy, lower alkanoyl and halogen atom, and n is 2 or 3.
The taurine-type compounds of the present invention are novel compounds undisclosed in any literatures. They not only have extremely strong effect of improving erythrocyte deformability when compared with conventional agents, but also possess inhibitory effect on platelet aggregation, and thus exert remarkable effect of improving hematological properties and are useful as medicaments for mammals including humans. That is to say, the compounds (I) of the present invention have an excellent effect of promoting erythrocyte deformability and effect of inhibiting platelet aggregation, and improve blood fluidity in microcirculatory regions, i.e., microcirculation. Therefore, the compounds (I) of the present invention are useful as agents for preventing and treating arterioclerosis, cerebral infarction, myocardial infarction, peripheral thrombosis and obstruction, etc.
Thus the present invention also provides an agent for the improvement of microcirculation which contains an effective amount of the compound of the above formula (I) and a pharmaceutically acceptable carrier or excipient.
Further the present invention provides a method of improving microcirculation in a patient in need of amelioration of microcirculation comprising administering an effective amount of the compound of the formula (I) to said patient.
Throughout the specification and particularly in the definition of the formula (I), lower alkyl and alkyl moiety of halogen-substituted lower alkyl, lower alkoxy and lower alkanoyl are intended to mean straight or branched saturated hydrocarbon chains having 1 to 6 carbon atoms or alicyclic saturated hydrocarbon groups having 3 to 6 carbon atoms. Examples thereof are methyl, ethyl, propyl, cyclopropyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, cyclobutyl,

REFERENCES:
patent: 4616086 (1986-10-01), Witte et al.

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