Ergolines exhibiting protactin secretion inhibition activity

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514218, 514253, 514254, 540545, 544361, 546 67, 546 68, 546 69, A61K 3148, C07D45704

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active

046909290

ABSTRACT:
Compounds of formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen or halogen atom or a methyl, cyano, C.sub.1 -C.sub.4 alkylthio or phenylthio group; R.sub.7 and R.sub.8 represent hydrogen atoms and R.sub.3 represents a hydrogen atom or a methoxy group, or R.sub.7 represents a hydrogen atom and R.sub.3 and R.sub.8 taken together represent a bond, or R.sub.3 represents a hydrogen atom or a methoxy group and R.sub.7 and R.sub.8 taken together represent a bond; R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; R.sub.5 represents a hydrogen atom or a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group; X represents an oxygen or sulphur atom or an imino group, R.sub.9 represents a hydrogen atom and B represents a cyano, a C.sub.2 -C.sub.5 alkoxycarbonyl or carbamoyl group, or R.sub.9 and B taken together represent a ##STR2## group wherein W represents an oxygen atom or an imino group; A represents a group of the formula CHR.sub.6, CH.sub.2 --CHR.sub.6 or CH.dbd.CR.sub.6 group wherein R.sub.6 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and n is 0, 1 or 2; and their pharmaceutically acceptable salts are disclosed, along with the use of these compounds as antiprolactinic and antihypertensive agents. The preparation of these compounds and pharmaceutical compositions containing them are also described.

REFERENCES:
patent: 3821226 (1974-06-01), Fehr et al.
patent: 4500712 (1985-02-01), Bernardi et al.
Salvati, et al., "Ergoline Derivatives and their Use", Chem. Abst. 96, 199974 (1982).
Temperilli, et al., "Ergoline Derivatives", Chem. Abst. 98:161005w (1983).
Fehr, et al., "Antihypertensiv wirksame Harnstoff Derivative . . . ,", Eur. J. Med. Chem. 1974 pp. 597-601.

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