Cyclohexanol derivatives, production and use thereof

Details Cyclohexanol derivatives, production and use thereof Cyclohexanol derivatives, production and use thereof

1990-08-29

1993-01-19

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

549 58, 549 52, 549 55, 549 56, 549 60, 549551, 549553, 549554, 549561, 549562, 544147, 544238, 544339, 544246, 544241, 544374, 544408, 544409, 544336, 544235, 544234, 544242, 544168, 544171, 544174, 546159, 546153, 546207, 546286, 5142315, 514432, 514444, 514475, 514825, 514866, 514863, 514336, 514252, 514422, 514314, 548517, 548518, 548527, A61K 3138, C07D30780

Patent

active

051807351

ABSTRACT:
The present invention relates to a compound of the formula: ##STR1## wherein A is halogen, N(O)mR.sup.1 R.sup.2, N.sup..sym. R.sup.1 R.sup.2 R.sup.3 .multidot.X.sup..crclbar., S(O)nR.sup.1 or S.sup..sym. (O)mR.sup.1 R.sup.2 .multidot.X.sup..crclbar. where R.sup.1, R.sup.2 and R.sup.3 are each optionally substituted hydrocarbon or heterocyclic group, X.sup..crclbar. is a counter anion; m is an integer of 0 or 1; n is an integer of 0 to 2; R.sup.1 and R.sup.2 may form a nitrogen-containing or a sulfur-containing heterocyclic ring, which may further form a condensed ring, with the adjacent nitrogen atom or sulfur atom, and these nitrogen-containing or sulfur-containing heterocyclic rings may have substituents, Z is O or NR.sup.4 where R.sup.4 is hydrogen or an optionally substituted lower alkyl or aryl group, D is 2-methyl-1-propenyl group or isobutyl group, and E is hydrogen, an optionally substituted hydrocarbon or an optionally substituted acyl group; provided that, when A is chlorine, E is an optionally substituted hydrocarbon or acyl excepting dinitrobenzoyl, a salt thereof, production and use thereof.
The novel cyclohexanol derivatives of the present invention have angiogenesis inhibiting activity and anti-tumor activity, and they are used as antirheumatic agents, therapeutic agents of psoriasis, therapeutic agents of diabetic retinopathy and anti-tumor agents.

REFERENCES:
patent: 4954496 (1990-09-01), Oka et al.
Landquist, J. Chem. Soc., "Some Degradation Products of Fumagillin," pp. 4237-4245 (1956).

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