DERIVATIVES OF 4-CYANO-4-PHENYLSUBSTITUTED CYCLOHEXANES OR CYCLOHEXENES, PHARMACEUTICAL COMPOSITION (VARIANTS), METHOD OF INHIBITION OF PHOSPHODIESTERASE ACTIVITY AND TUMOR NECROSIS FACTOR Russian patent published in 1999 - IPC

Abstract RU 2136656 C1

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention describes new derivatives of 4-cyano-4-phenylsubstituted cyclohexanes or cyclohexenes of the formula (I) where R1 means (CR4R5)r; R6, where alkyl groups can be optionally substituted with one or more halogen atoms; r = 0-6; R4 and R5 are taken independently from hydrogen atom or C1-2-alkyl; R6 means hydrogen atom or C3-6-cycloalkyl where cycloalkyl-group can be optionally substituted with 1-3 methyl groups or a single ethyl group; X means YR2; Y means O; X2 means O or NR8; X3 means hydrogen atom; X4 means: (a) or (b); X5 means H, OR8 or NR8R8; R2 is taken independently from the group consisting of -CH3 and -CH2CH3 optionally substituted with one or more halogen atoms; S = 0; R3 means CN, Z-, (5-tetrazolyl), (3- or 5-oxadiazolyl[1,2,4] ), (2-oxadiazolyl-[1,3,4]) being all heterocyclic ring systems can be optionally substituted once or more times with C1-C6-alkyl that is optionally substituted with CN; Y′ means O or S; R7 means C1-6-alkyl, optionally substituted - CN; R8 is taken independently from hydrogen atom or C1-4-alkyl; R10 means R11 where R11 means hydrogen atom or C1-4-alkyl optionally substituted with one-three fluorine atoms; R14 means hydrogen atom or R7, or their pharmaceutically acceptable salts. Invention describes also a pharmaceutical composition that inhibits activity of phosphodiesterase-IV and tumor necrosis factor based on the compound of the formula (I) and a method of inhibition of activity of phosphodiesterase-IV and tumor necrosis factor by administration of the above indicated compounds. EFFECT: new compounds indicated above as inhibitors of phosphodiesterase and tumor necrosis factor. 6 cl, 30 ex

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RU 2 136 656 C1

Authors

Zigfrid Benzhamin Kristensen Iv

Dates

1999-09-10Published

1993-03-05Filed