Hoechst Aktiengesellschaft

Samba Laxminarayan Kattige

Noel J De Souza

Jurgen Blumbach

Richard H Rupp

Alihussein N Dohadwalla

Adolf D'Sa

Ramchandra G Naik

Aftab D Lakdawalla

Gulab Bajirao Padwal

Process for the preparation of 6-(substitutedaminopropionyl)-derivatives of forskolin Process for the manufacture of 6.beta.-(3-substitutedamino) propionyloxy forskolin derivatives of the general formula ##STR1##

Process for the preparation of 6-(substitutedaminopropionyl)-derivatives

The present invention relates to novel 4H-1-benzopyran-4-one derivatives, to processes for the preparation thereof and to their use as anti-inflammatory, analgesic, immuno-suppressive and anti-allergic agents. In particular, the present invention relates to novel compounds of the formula I, ##STR1## in which R.sub.1 is hydrogen, alkyl having 1 to 6 carbon atoms, arly-C.sub.1 -C.sub.4 -alkyl, substituted C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, aryl or carboxyl or an aldehyde or COO--C.sub.1 -C.sub.4 -alkyl group, R.sub.2 is hydrogen, alkyl having 1 to 6 carbon atoms, nitro, amino, di-C.sub.1 -C.sub.4 -alkylamino or a halogen, R.sub.3 is C.sub.1 -C.sub.4 -alkyl, substituted C.sub.1 -C.sub.4 -alkyl, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, aryl-C.sub.1 -C.sub.4 -alkyl, nitro, amino, a C.sub.1 -C.sub.4 -alkylamino or di-C.sub.1 -C.sub.4 -alkylamino group or halogen, R.sub.4 is hydrogen, hydroxyl, C.sub.1 -C.sub.4 -alkyoxy, C.sub.1 -C.sub.4 -alkyoxycarbonyl, aryloxy, amino or a C.sub.1 -C.sub.4 -alkylamino or di-C.sub.1 -C.sub.4 -alkylamino group, R.sub.5 is hydrogen, C.sub.1 -C.sub.6 -alkyl, substituted C.sub.1 -C.sub.6 -alkyl, aryl-C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkanoyl or aroyl, the aryl group being phenyl which is unsubstituted, monosubstituted or polysubstituted, m is an integer between 0 and 3 and n is an integer between 0 and 2, and to pharmacologically acceptable acid addition salts thereof.

4H-1-benzopyran-4-one compounds which have anti-inflamatory or

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Bombay, India

Samba Laxminarayan Kattige