Derivatives of benzocycloalkenyldihydroxyalkanoic acids and medi

Details Derivatives of benzocycloalkenyldihydroxyalkanoic acids and medi Derivatives of benzocycloalkenyldihydroxyalkanoic acids and medi

1990-01-24

1992-01-21

Fan, Jane T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514461, 514462, 514467, 549 64, 549313, 549370, 549448, A61K 31335, C07D33334

Patent

active

050828592

ABSTRACT:
Derivatives of benzocycloalkenyldihydroxyalkanoic acids, inhibitors of HMG CoA reductase, antagonists of thromoboxane A.sub.2 receptors and antifungals, denoted by the formula I ##STR1## in which X=CH.sub.2, O or S; R.sub.1 and R.sub.2, identical or different, =H, C.sub.1-3 alkyl or together from a --(CH.sub.2).sub.n -- chain (n=4,5) optionally substituted symmetrically by one or two C.sub.1-3 alkyl radicals.
R.sub.3 and R.sub.4, identical or different, =H, CF.sub.3, halogen (Cl, F, Br), C.sub.1-5 N,N-dialkylamino, C.sub.1-4 alkyl, C.sub.1-5 -alkoxy, C.sub.1-3 alkylthio, or phenyl optionally substituted by at most two substitutents which may be identical or different and may denote C.sub.1-3 alkyl or C.sub.1-3 alkoxy radicals or halogens (F, Cl), it being understood that when one of R.sub.3 and R.sub.4 denotes the radicals: CF.sub.3, N,N-dialkylamino, C.sub.6 H.sub.5 or substituted phenyl, it is present at the vertices 3', 4'or 5' according to formula 1 and the other denotes a hydrogen atom.
R.sub.5 and R.sub.6, (which may be identical or different)=H, halogen (F, Cl, Br), CF.sub.3, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.6 H.sub.5, optionally substituted by at most two substitutents which may be identical or different and may denote radicals: C.sub.1-3 alkyl or C.sub.1-3 alkoxy or halogen atoms (F, Cl), on condition that when one of R.sub.5 and R.sub.6 =CF.sub.3, C.sub.6 H.sub.5 or substituted phenyl, it is present at the vertex 6 or 7 and the other denotes a hydrogen atom.
The substitutents R.sub.3 and R.sub.4 or R.sub.5 and R.sub.6 may also together form, on condition of being at two contiguous vertices, diradicals of formulae: --CH.dbd.CH--CH.dbd.CH--, --(CH.sub.2).sub.m -- and --O(CH.sub.2).sub.p O--, in which m=3 or 4, p=1 or 2, it being understood that when R.sub.3 and R.sub.4 or R.sub.5 and R.sub.6 form the chain sequence --O(CH.sub.2).sub.p O--, the latter is linked to the vertices 3' and 4' or 4' and 5' or 6 and 7 according to the formula 1.
R.sub.7 and R.sub.8 =H or, together with the existing C--C bond, form a double bond of trans geometry; R.sub.9 and R.sub.10 =H or together form a C.sub.1-3 dialkylmethylene residue.
In the form of free acids, salts, esters, amides or .delta.-lactones.
Hypocholesterolaemiant, antithrombotic and antifungal medications containing them.

REFERENCES:
Patent Abstacts of Japan vol. 12, No. 33 (C-472)(2880), 30 Janvier 1988; & JP-A-62 181276 (Sagami Chem. Res. Center) 08.08.1987.
Chemical Abstacts vol. 83, No. 8, 25 aout 1975, p. 677, colonne 2, abstract No. 68643f, Columbus, Ohio, U.S.A.; L. Penn et al.: "Chemical Shift Measurements of Substitutent Effects on Out-of-Plane Magnetic Shielding in Benzene Derivatives" & J. Mang. Reson. 1975, vol. 18, No. 1, pp. 6-11.
Chemical Abstracts vol. 76, No. 23, 5 Juin 1972, p. 446, colonne 1, abstract No. 140440n, Columbus, Ohio, U.S.A., J. Degani et al.: "Hetero-Aromatic Cations. XV. Synthesis of some 2-, 3- and 4-aryl derivatives of 1-thianaphthalenium Perchlorate" & Ann. Chim. (Rome) 1971, vol. 61, No. 12, pp. 793-813.

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