Substituted oxime derivatives and processes for their preparatio

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546333, A61K 3144

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active

056936591

ABSTRACT:
Compounds of general formula (1) are described: ##STR1## wherein .dbd.W-- is (1) .dbd.C(Y)-- where Y is a halogen atom, or an alkyl hydrogen atom or an optionally substituted alkyl group! and R.sup.a is a hydrogen atom or an optionally substituted alkyl group or, (2) .dbd.N--; L cycloalkyl or cyloalkenyl group!, --C(R.sup.5).dbd.C(R.sup.1)(R.sup.2) or hydrogen or a fluorine atom or a methyl group, and R.sup.1 and R.sup.2, which may be the same or different, is each a hydrogen or fluorine atom or an optionally substituted alkyl, alkenyl, alkynyl, alkoxy, alkylthio, R.sup.7 and R.sup.8, which may be the same or different are as defined for R.sup.6 !, --CSNR.sup.7 R.sup.8, --CN or --NO.sub.2 group, or R.sup.1 and R.sup.2 together with the C atom to which they are attached are linked to form an optionally substituted cycloalkyl or cycloalkenyl group and n is zero or the integer 1; Ar is a group --(CH.sub.2).sub.n --Z--Ar' where Ar' is an optionally substituted monocyclic or bicyclic heteroaryl group and Z is a bond, an atom --O--, or --S-- or a group --N(R.sup.b)-- and n is zero or the integer 1, 2, 3 or 4; R.sup.3 is a hydrogen atom, or an optionally substituted alkyl, alkenyl, alkynyl, --C(O)R.sup.4 (where R.sup.4 is an amino, alkylamino, arylamino, alkoxy, aryloxy or an optionally substituted alkyl group) or --C(S)R.sup.4 group; and the salts, solvates, hydrates, prodrugs and N-oxides thereof.
Compounds according to the invention are phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of disease such as asthma where an unwanted inflammatory response or muscular spasm is present.

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