Pyrimidinylpyrazole derivatives

Details Pyrimidinylpyrazole derivatives Pyrimidinylpyrazole derivatives

1998-02-04

1998-12-22

Bernhardt, Emily

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

5142358, 514273, 544122, 544123, 544238, 544295, 544296, 544321, 544324, 544331, A61K 31495, C07D40114, C07D40314, C07D41314

Patent

active

058520198

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to novel compounds having antitumor effects, antitumor agents containing these compounds as an active ingredient and a method for treating tumors with the use of these antitumor agents.


BACKGROUND ART

It has been known that pyrimidinylpyrazole derivatives have hypotensive and psychotropic effects (see, for example, JP-B-47-14233 and JP-B-48-42072; the term "JP-B" as used herein means an "examined Japanese patent publication"). However no antitumor effect of these compounds has been reported so far.
An object of the present invention is to provide highly efficacious antitumor agents having novel chemical structures which have never been known hitherto.


DISCLOSURE OF THE INVENTION

As the results of extensive studies, the present inventors have found out that a novel pyrimidinylpyrazole derivative represented by the following formula (I) has a potent antitumor effect, thus completing the present invention.
The present invention relates to a compound represented by formula (I): ##STR3## wherein R.sup.1 and R.sup.2 may be either the same or different and each represents an atom or a substituent selected from a group consisting of: group, an alkylamino group, a dialkylamino group, a hydroxyl group, an alkoxyl group or a thiol group, and group, an alkylamino group, a dialkylamino group, a hydroxyl group, an alkoxyl group or a thiol group; benzyl group; ##STR4## wherein Z represents a phenyl group, a pyridyl group, ##STR5## n represents an integer of from 1 to 3; and R.sup.6 is optionally substituted by one or more atom(s) and/or substituent(s) selected from a group consisting of: alkylamino group, a dialkylamino group, a hydroxyl group, an alkoxyl group or a thiol group, and an alkylamino group, a dialkylamino group, a hydroxyl group, an alkoxyl group or a thiol group; its salt, and an antitumor agent containing the same as an active ingredient.
The compound of the present invention represented by the formula (I) involves compounds having a double bond of cis-form in the alkenyl group as well as those having a double bond of trans-form therein.


MODE FOR CARRYING OUT THE INVENTION

Now, the substituents as used herein will be described.
The term "alkyl" employed for the alkyl moieties of the alkylamino, dialkylamino, alkylthio and alkoxyl groups and the alkyl group herein means an alkyl group having from 1 to 6 carbon atoms.
Preferable examples of R.sup.1 and R.sup.2 include: hydroxyl group, an alkoxyl group or a thiol group,
It is still preferable that R.sup.1 and R.sup.2 are selected from a group consisting of an alkyl group optionally substituted by a halogen atom, an amino group, a hydroxyl group, an alkoxyl group or a thiol group, a halogen atom, a hydrogen atom and an alkoxyl group.
It is preferable that R.sup.3 is a hydrogen atom.
It is preferable that R.sup.4 is a hydrogen atom or an alkyl group, still preferably a methyl group.
It is preferable that R.sup.5 is a hydrogen atom or an alkyl group, still preferably a hydrogen atom or a methyl group.
It is preferable that R.sup.6 represents ##STR6## wherein Z is as defined above; each optionally substituted by one or more substituents selected from a group consisting of: hydroxyl group, an alkoxyl group or a thiol group,
It is preferable that the substituent, which is selected from a group consisting of an alkyl group optionally substituted by a halogen atom, an amino group, a hydroxyl group, an alkoxyl group or a thiol group, a halogen atom, an alkylamino group, a dialkylamino group, an alkoxyl group, a cyano group, a hydroxyl group and a carbamoyl group, is attached to the Z moiety. It is still preferable that R.sup.6 represents ##STR7## each optionally substituted by one or more substituents selected from a group consisting of an alkyl group optionally substituted by a halogen atom, an amino group or a hydroxyl group, a halogen atom, a hydroxyl group and an alkoxyl group.
It is preferable that the substituent, which is selected from a group consisting of an alkyl group optionally substituted by a halogen atom,

REFERENCES:
patent: 5102893 (1992-04-01), Picard et al.
Ubusawa et al., "1-(4-Methoxy-6-methyl-2-pyrimidinyl)-3-methyl-5-methtoxypyrazole and related compunds as neoplasm inhibitors", Chemical Abstr., abstr. No. 183956, 105:21, Nov. 24, 1986.
Ueno et al., "Pyrazole derivatives", Chemical Abstr., abstr. No. 3933q, 81:1:, Jul. 8, 1974.

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