Farmitalia Carlo Erba S.r.l.

Maristella Colombo

Franco Buzzetti

Antonio Longo

Paolo Lombardi

Enrico Di Salle

Fabrizio Orzi

The present invention provides compounds of the formula ##STR1## wherein Y is a naphthyl, tetrahydronaphthyl, pyridyl, quinolyl, isoquinolyl or indolyl ring system, R is a moiety which is an acrylic acid, a CN-substituted acrylic acid, acrylamide, acrylonitrile or thioacrylamide, or a group of formulae (e) to (j): ##STR2## wherein R.sub.3 is OH or NH.sub.2, R.sub.1 is H, alkyl or alkanoyl, R.sub.2 is H, halogen, CN or alkyl; and n is 0, 1, 2 or 3; and the pharmaceutically acceptable salts thereof are useful as tyrosine kinase inhibitors.

Arylethenylene compounds which are useful as tyrosine kinase inhibitors

The present invention provides novel aryl- and heteroarylethenylene derivatives which are useful as tyrosine kinase activity inhibitors.

2-oxindole compounds which have useful tyrosine kinase activity

Methylen-oxindole derivatives compositions and tyrosine kinase

2-oxindole compounds which are useful as tyrosine kinase inhibitors

A process for the preparation of 4-aminoandrostenediones of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, and the symbol indicates that each of (x) and (y), independently, is a single bond or a double bond, comprising reacting a compound of formula (II) ##STR2## wherein E is a halogen atom and R.sub.1, R.sub.2, (x) and (y) each are as defined as above with ammonia.

Process for the preparation of 4-amino-androstenedione derivatives

The invention relates to 4-substituted 6-alkylidenandrostene-3,17-dione derivatives of the following formula ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3 is, independently, hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.4 is hydrogen of fluorine; (x) represents a single or double bond; and R is, especially, a hydroxy or mercapto or amino group or a functional derivative thereof. The compounds of the invention show aromatase inhibitory activity and may be useful, for instance, in the treatment of hormone-dependent tumors and of prostatic hyperplasia.

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Cesano Boscone, Italy

Maristella Colombo