Cyclohexanol derivatives, production and use thereof

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

C - Chemistry, Metallurgy

07

D

167/207, 260/260

C07D 303/46 (2006.01) A61K 31/335 (2006.01) A61K 31/395 (2006.01) C07D 303/22 (2006.01) C07D 303/34 (2006.01) C07D 303/36 (2006.01) C07D 405/08 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 409/08 (2006.01) C07D 409/12 (2006.01) C07D 413/08 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2024306

Abstract of the Disclosure The present invention relates to a compound of the formula: wherein A is halogen, N(O)mR1R2, N?R1R2R3?X?, S(O)nR1 or S?(O)mR1R2?X? where R1,R2 and R3 are each optionally substituted hydrocarbon or heterocyclic group, X? is a counter anion; m is an integer of 0 or 1; n is an integer of 0 to 2; R1 and R2 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, B is O or NR4 where R4 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 anti- rheumatic agents, therapeutic agents of psoriasis, therapeutic agents of diabetic retinopathy and anti- tumor agents.

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