Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-02-24
1997-10-07
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5482648, 5482654, C07D24908, A61K 3141
Patent
active
056748868
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JPA 92/01089 filed Aug. 27, 1992.
TECHNICAL FIELD
The present invention relates to novel triazolyl-substituted tertiary amine compounds having an aromatase inhibiting activity useful as medicines.
BACKGROUND ART
Regarding biosynthesis of estrogen in a living body, it is known that an enzyme, aromatase, participates in the final step of the route of the biosynthesis. Aromatase aromatizes A ring of asteroid with a substrate of androgen to form estrogen. Therefore, by inhibiting this enzyme activity, prevention and curing of various diseases caused by estrogen as an exacerbating factor is possible.
On the basis of this knowledge, some aromatase inhibiting compounds have heretofore been proposed. As typical examples of them, mentioned are imidazolyl- or triazolyl- or pyridyl-substituted methyl compounds described in European Patent Laid-Open Nos. 236,940 and 293,978.
However, compounds of the present invention are structurally different from the known compounds in that the former have a triazolyl-substituted tertiary amino group. Such compounds having a triazolyl-substituted tertiary amino group are not known to have been produced up to the present. In particular, any effective method of direct alkylation, especially arylation, of the terminal amino group of the triazolyl group has not been known.
The present invention provides novel triazolyl-substituted tertiary amino compounds which are structurally different from any known compounds and also provides an optimum method of producing them. In addition, the novel compounds were found to have an excellent aromatase inhibiting activity. On the basis of these findings, the present invention has been completed.
DISCLOSURE OF THE INVENTION
The triazolyl-substituted tertiary amino compounds according to the present invention are represented by the following general formula (I): ##STR2## wherein A represents a single bond, a lower alkylene group or a carbonyl group; optionally substituted 5- or 6-membered heterocyclic group having from 1 to 3 hetero atoms of oxygen, sulfur and/or nitrogen atoms, or an optionally substituted bicyclic fused heterocyclic group composed of the preceding hetero ring and a benzene ring; D ring represents an optionally substituted aryl group, an optionally substituted 5- or 6-membered heterocyclic group having from 1 to 3 hetero atoms of oxygen, sulfur and/or nitrogen atoms, or an optionally substituted bicyclic fused heterocyclic group composed of the preceding hetero ring and a benzene ring; and E ring represents a 4H-1,2,4-triazole ring, a 1H-1,2,4-triazole ring or a 1H-1,2,3-triazole ring. These definitions apply hereinafter.
Compounds of the present invention will be explained in more detail hereinafter. The term "lower" as used herein indicates a linear or branched carbon chain having from 1 to 6 carbon atoms, unless otherwise specifically defined.
Therefore, a "lower alkyl group" concretely includes, for example, a methyl group, an ethyl group, a propyl group, an isopropyl group, a butyl group, an isobutyl group, a sec-butyl group, a tert-butyl group, a pentyl (amyl) group, an isopentyl group, a neopentyl group, a tert-pentyl group, a 1-methylbutyl group, a 2-methylbutyl group, a 1,2-dimethylpropyl group, a hexyl group, an isohexyl group, a 1-methylpentyl group, a 2-methylpentyl group, a 3-methylpentyl group, a 1,1-dimethylbutyl group, a 1,2-dimethylbutyl group, a 2,2-dimethylbutyl group, a 1,3-dimethylbutyl group, a 2,3-dimethylbutyl group, a 3,3-dimethylbutyl group, a 1-ethylbutyl group, a 2-ethylbutyl group, a 1,1,2-trimethylpropyl group, a 1,2,2-trimethylpropyl group, a 1-ethyl-1-methylpropyl group, and a 1-ethyl-2-methylpropyl group. Of them, preferred are a methyl group, an ethyl group, a propyl group, an isopropyl group and a butyl group.
A "lower alkylene group" is a linear or branched carbon chain having from 1 to 6 carbon atoms, concretely including, for example, a methylene group, an ethylene group, a propylene group, a tetramethylene group, a 2-methyltrimethylene group, a 1-ethyle
REFERENCES:
patent: 5041458 (1991-08-01), Basarab
World Intellectual Property Organization, WO-A-90 14338 (Fisons PLC) 1990.
Isomura Yasuo
Kawaminami Eiji
Kudou Masafumi
Okada Minoru
Yoden Toru
Gerstl Robert
Yamanouchi Pharmaceutical Co. Ltd.
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