Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-10-26
1996-07-23
Gupta, Yogendra N.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514242, 514245, 514252, 544180, 544182, 544194, 544224, 544238, 544322, A61K 31505, C07D23942, C07D23720
Patent
active
055389767
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
This invention relates to a novel substituted tertiary amino compound or a pharmaceutically acceptable salt thereof having an aromatase inhibiting activity and useful as a drug, a process for preparing the same, and a pharmaceutical composition containing the same.
BACKGROUND ART
It is known that an enzyme, aromatase, takes part in the final stage of biosynthesis of estrogen. Aromatase aromatizes the ring A of the steroid and uses androgen as a substrate to produce an estrogen. Inhibition of the aromatase activity leads to prevention and treatment of various diseases in which an estrogen participates as an exacerbating factor.
Several aromatase inhibiting compounds have hitherto been proposed based on the above concept. Typical examples of known aromatase inhibiting compounds include imidazolyl-, triazolyl-, pyridyl- or pyrimidyl-substituted methyl compounds disclosed in EP-B-236940, EP-B-293978, U.S. Pat. No. 4,762,836, and J. Med. Chem., Vol. 33, p. 416 (1990).
Further, U.S. Pat. No. 4,774,251 describes that a compound having a pyridyl- or pyrazyl-substituted tertiary amino group and one or two phenyl groups, as represented by the following general formula, exhibits an aromatase inhibiting activity. ##STR2## (cf. U.S. Pat. No. 4,774,251 as to definitions of the symbols)
The compound according to the present invention is distinctly different in structure from any of the compounds found in the above-described literature in that it contains a pyrimidine ring, a pyridazine ring or a triazine ring as a basic structure.
Additionally, the compound of the present invention has been proved highly useful as it has 100 times or more the aromatase inhibiting activity of the compound disclosed in the literature.
DISCLOSURE OF THE INVENTION
The substituted tertiary amino compound of the present invention is represented by the general formula (I): ##STR3## wherein A represents a single bond, a lower alkylene group or a group represented by formula: ##STR4## wherein n represents an integer of from 1 to 6, and X represents an oxygen atom, a sulfur atom or a group represented by formula: CH.sub.2 ;
and rings D and E, which may be the same or different, each represent a substituted or unsubstituted aryl group, a substituted or unsubstituted 5- or 6-membered heterocyclic group containing 1 to 3 hetero atoms each selected from a nitrogen atom, an oxygen atom, and a sulfur atom, or a substituted or unsubstituted bicyclic condensed heterocyclic group consisting of the above heterocyclic group condensed with a benzene ring; provided that where rings D and E both represent a benzene ring, at least one of them has a substituent.
The compound of the present invention will further be explained. The term "lower" as used in definitions of general formulae in this specification means a straight or branched carbon chain having from 1 to 6 carbon atoms unless otherwise noted.
Accordingly, a "lower alkyl group" as one of the substituents on ring D or E may include 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 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.
The "lower alkylene group" is a straight or branched carbon chain having from 1 to 6 carbon atoms and includes a methylene group, an ethylene group, a propylene group, a tetramethylene group, a 2-methyltrimethylene group, a 1-ethylethylene group, a pentamethylene group, and a 1,2-diethylethylene group, with a methylene group and
REFERENCES:
patent: 4762836 (1988-08-01), Hirsch
patent: 4774251 (1988-09-01), Hirsch et al.
Jones et al. J. Med. Chem., 33, 416-429, 1990.
Isomura Yasuo
Kawaminami Eiji
Kudou Masafumi
Okada Minoru
Shimada Yoshiaki
Gupta Yogendra N.
Yamanouchi Pharmaceutical Co. Ltd.
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