Farmitalia Carlo Erba

Pharmacia & Upjohn

Nerviano Medical Sciences S.r.l.

Farmitalia Carlo Erba S.r.l.

Sergio Vioglio

Carlo Battistini

Giovanni Franceschi

Dario Ballinari

Antonella Ermoli

Mario Varasi

Daniele Fancelli

Franco Buzzetti

Paola Vianello

Simona Bindi

Dania Tesei

Roberto Bianchini

Sergio Penco

Leonardo Marsili

Domenico Ungheri

Aurora Sanfilippo

Maria A Verini

Pierluigi Griggi

Stefano Del Nero

Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

1H-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors

Substituted tetralymethylen-Oxindoles analogues as tyrosine kinase

Substituted quinolymethylen-oxindole analogues as tyrosine kinase

Substituted indolylmethylene-oxindole analogues as tyrosine kinase

The present invention relates to the use as antivirals of compounds of formula: ##STR1## wherein B is a purinic or pyrimidinic heterocycle; X is oxygen or sulphur; R.sup.1 is a hydroxyl group or a hydrogen atom; R.sup.2 is a linear, branched or cyclic, alkyl group of up to twenty carbon atoms; R.sup.3 is as specified for R.sup.2 above or a hydrogen atom, a cation or a polyhydroxy group.

5'-alkylphosphonylnucleosides as antivirals

A crystalline form of (5R,6S)-2-carbamoyloxymethyl-6-[(1R)-hydroxyethyl]-2-penem-3-carboxylic acid incorporates two molecules of water per molecule of the acid and is useful as an antibacterial agent.

Crystalline

Orally administrable pharmaceutical compositions comprising 3-(N-piperidinomethyl-azino)methylrifamycin S as the active substance are disclosed. The active substance is easily soluble in water even at low pH values and is provided with good bioavailability. Such compositions are useful in the treatment of bacterial infections.

Pharmaceutical composition comprising 3-(N-piperidinomethyl-azino)

Azinomethyl-rifamycins I ##STR1## (wherein Y=H or COCH.sub.3 and either R.sub.1 =C.sub.1 -C.sub.7 alkyl or C.sub.3 -C.sub.4 alkenyl and R.sub.2 =C.sub.1 -C.sub.7 alkyl, C.sub.2 -C.sub.4 cloro-, hydroxy-, or alkoxy-alkyl C.sub.3 -C.sub.4 alkenyl, cycloalkyl having a C.sub.3 -C.sub.7 ring, cycloalkylalkyl having a C.sub.3 -C.sub.6 ring, phenyl or C.sub.7 -C.sub.8 aralkyl optionally monohalogen substituted in the aryl group or NR.sub.1 R.sub.2 = a cyclic moiety, said moiety being pyrrolidinyl, piperidinyl, hexahydroazepinyl or heptahydroazocinyl, each of which are unsubstituted or substituted with 1 or 2 methyl radicals, 4-alkyl-1-piperazinyl, morpholinyl or 1,2,3,4-tetrahydroisoquinolinyl) are prepared from rifamycin S by

Preparation of azinomethyl-rifamycins

There are provided azino rifamycin compounds of the formula (I): ##STR1## Y.dbd.H or CH.sub.3 CO; R.sub.1 linear or branched C.sub.1 -C.sub.7 alkyl or C.sub.3 -C.sub.4 alkenyl- R.sub.2 =linear or branched C.sub.1 -C.sub.7 alkyl, C.sub.2 -C.sub.4 chloroalkyl, C.sub.3 -C.sub.4 alkenyl, Cycloalkyl having 3 to 7 C atoms in the ring, cycloalkyl alkyl having 3 to 6 C atoms in the ring, phenyl, or C.sub.7 -C.sub.8 aralkyl, unsubstituted or mono-substituted by a halogen atom in the aryl group; or NR.sub.1 R.sub.2 =a cyclic moiety having 5 to 8 C atoms, unsubstituted or substituted by 1 or 2 CH.sub.3 groups, morpholino. The compounds inhibit the growth of gram positive bacteria and Mycobacterium tuberculosis. Oxidized compounds, preparative methods and pharmaceutical compositions are also described and claimed.

Azino rifamycins

Growing community of inventors

Cusano Milanino, Italy

Sergio Vioglio