Prostaglandins

Details Prostaglandins Prostaglandins

1990-03-28

1991-12-31

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514529, 514530, 514542, 514562, 514564, 514565, 546290, 546304, 546310, 548161, 548170, 548180, 548217, 548221, 548222, 549463, 560 16, 560 34, 560 43, 560 32, 560118, 560120, 560121, 560125, 560126, 562426, 562439, 562452, 562460, 562500, 562502, 562503, 562507, 562508, C07C17700, A61K 31557

Patent

active

050773097

ABSTRACT:
Novel compounds have the formula (I) ##STR1## where ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)-NV'R, respectively; R.sup.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.W' in which D is --NH, --NH,CS--, --NH.CO--, --NH.CO.CH.sub.2 N(R.sup.6)--, --NH.SO.sub.2 --, --NH.CO.NH--, --NH.CS.NH--, --NH.CO.O-- or --NH.CS.O--, G is --CO-- or --CS-- and W and W' together are a group --(CH.sub.2).sub.d -- in which d is 3, 4, or 5, R.sup.3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by one or more aromatic groups directly or through an oxygen or sulphur atom, R.sup.4 is an aliphatic hydrocarbon group which is substituted through an oxygen atom by an aliphatic hydrocarbon group which is itself substituted directly by one or more aromatic groups, R.sup.5 is an aliphatic hydrocarbon group, and aromatic group in which the .pi.-electron system is not fully delocalized over the entire ring system, or aliphatic hydrocarbon group substituted by one or more aromatic groups directly or through an oxygen or sulphur atom, and R.sup.6 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by one or more aromatic groups directly or through an oxygen or sulphur atom. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

REFERENCES:
patent: 4368332 (1983-01-01), Jones
patent: 4430345 (1984-02-01), Jones et al.
patent: 4438136 (1984-03-01), Jones
patent: 4458091 (1984-07-01), Jones et al.
patent: 4513103 (1985-04-01), Das et al.
patent: 4596823 (1986-06-01), Jones et al.
patent: 4628061 (1986-12-01), Jones et al.
patent: 4902717 (1990-02-01), Senior
W. Krause et al., "Biotransformation of the Stable Prostacyclin . . . ", Drug Metabolism & Disposition, vol. 12, No. 5, 1984, pp. 645-651.
W. Skuballa et al., "Synthesis of a New Chemically and Metabolical Stable . . . ", Jour. of Medicinal Chem., vol. 29, No. 3, Mar. 1986, pp. 313-316.
G. Bundy et al., "Novel Prostaglandin Syntheses", New York Academy of Sciences, pp. 77-90.

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