Preventive agent for platelet aggregation

Details Preventive agent for platelet aggregation Preventive agent for platelet aggregation

1995-04-26

1997-09-02

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544234, A61K 3150

Patent

active

056631723

DESCRIPTION:

BRIEF SUMMARY
This application is a Section 371 or PCT/JP93/01527 filed Oct. 29, 1993 published as WO94/09784, May 11, 1994.


FIELD OF THE INVENTION

The present invention relates to a preventive agent for platelet aggregation.


BACKGROUND ART

In Japanese Patent Laid-opened No. Hei 2-56468, compounds represented by the following general formula [II]: ##STR2## wherein Z is alkylene containing 1 to 4 carbons and optionally substituted by alkyl, lower alkoxy, lower alkylthio lower alkyl, lower alkoxycarbonyl or benzyl, or a group represented by a general formula --C(r.sub.6) .dbd.C(r.sub.7)-- wherein r.sub.6 and r.sub.7 are each independently hydrogen, alkyl, lower alkoxy, lower alkylthio lower alkyl, lower alkoxycarbonyl or benzyl; r.sub.1 is lower alkyl optionally substituted by hydrogen or lower alkoxy, acetyl or lower alkenyl; r.sub.2 is hydrogen or methyl; r.sub.3 and r.sub.4 are each independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; r.sub.5 is lower alkyl optionally substituted by hydrogen or hydroxy; or r.sub.4 may form in together with r.sub.5 a bond, such as --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- and --OCH.sub.2 --; and ---------- represents a single bond or a double bond, and pharmaceutically-compatible complexes thereof are disclosed, and wherein it is described that these compounds and complexes have (1) an excellent cardiotonic effect and therefore can be a therapeutic drug for congestive heart failure and (2) a preventive effect on platelet aggregation.


DISCLOSURE OF THE INVENTION

The inventors of the present invention had investigated on compounds represented by the general formula [I] or the pharmaceutically-compatible complexes thereof for aiming at developing their novel medical use. As the result, the inventors found that compounds represented by the general formula [I], which is a compound group of the compounds represented by a general formula [II] wherein r.sub.1 is C.sub.3 H.sub.7, or the pharmaceutically-compatible complexes thereof have an excellent preventive effect on platelet aggregation and less cardiotonic effect, and they can be used as an preventive agent for platelet aggregation. It is an unexpected fact that the compounds represented by the general formula [I] or the pharmaceutically-compatible complexes thereof have less cardiotonic effect, basing upon the prior knowledge in the art on the compounds represented by the general formula [II] or the pharmaceutically-compatible complexes thereof.
It is an object of the present invention to provide an excellent preventive agent for platelet aggregation, which comprises a compound represented by the following general formula [I]: ##STR3## wherein Y is --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --, R is hydrogen or methyl and ---------- represents a single bond or a double bond, or a pharmaceutically-compatible complex thereof as the active ingredient and gives less side effect.
The compounds represented by the general formula [I] and the pharmaceutically-compatible complexes thereof can be manufactured according to a method disclosed in the Japanese Patent Laid-opened No. Hei 2-56468, which corresponds to U.S. Pat. No. 5,110,925.
Representative compounds for the compounds and the complexes are shown in Table 1.


TABLE 1 __________________________________________________________________________ Physical Structural Formula Data Compound ##STR4## [ ] No. Y R ##STR5## m.p. .degree.C. __________________________________________________________________________ 1 CH.sub.2 CH.sub.2 CH.sub.2 H Single bond 222-225 2, 2' CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3 Single bond 95-100 (173-176) 3 CH.sub.2 CH.sub.2 H Single bond 165-167 __________________________________________________________________________
In addition to the representatives above, in the compounds represented by the general formula [I], pyridazinol exists in the place of pyridazine, and the tautomers, such as enol form and keto form as represented by the following formulas, ##STR6## exist at the place of cycloalkenylamin

REFERENCES:
patent: 5110925 (1992-05-01), Kusase et al.

Affiliated with

Also associated with

Rating

Preventive agent for platelet aggregation does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Preventive agent for platelet aggregation, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Preventive agent for platelet aggregation will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-308423