Farmitalia Carlo Erba

Pharmacia & Upjohn

Nerviano Medical Sciences S.r.l.

Farmitalia Carlo Erba S.r.l.

Pharmacia Italia S.p.a.

Farmitalia Carlo Erba S.r.l. an Italian Body Corporate

Sergio Mantegani

Aldemio Temperilli

Gabriella Traquandi

Mario Varasi

Enzo Brambilla

Tiziano Bandiera

Alessandro Rossi

Luigi Bernardi

Laura Chiodini

Patricia Salvati

Patrizia Ferrari

Mauro Gobbini

Carla Caccia

Daniela Ruggieri

Germano Bosisio

Lorenzo Pegrassi

Nicola Carfagna

Anna M Caravaggi

Giuliana Arcari

Carmela Speciale

Teresa Disingrini

Paolo Cremonesi

Daniel Ruggieri

Maria Gabriella Brasca

Ettore Perrone

Manuela Villa

Ron Ferguson

Fabio Zuccotto

Francesco Casuscelli

Jacqueline Lansen

Helena Posteri

Pierluigi Bissolino

Elena Casale

Daniela Jabes

Metilde Buonamici

Francesca Abrate

Carlo Visco

Guiliana Arcari

Roberto Maj

Maurizio Meroni

Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

Tricyclopyrazole derivatives

Bicyclic pyrazole and isoxazole 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 mediated by HSP90 protein, like cancer and neurodegenerative disorders.

Bicyclic pyrazole and isoxazole derivatives as antitumor and antineurodegenerative agents

Compounds which are 3-arylsulfonyl-2-methyl propanoic acid derivatives of formula (I): wherein X is HO&mdash;NH&mdash; or HO&mdash;, R1 is selected from phenyl, 4-chlorophenyl, 4-florophenyl, 4-cyanophenyl, benzamido (i.e., &mdash;NH&mdash;CO-Ph) and benzamido substituted on the terminal phenyl ring by C -C alkyl, fluoro, chloro, cyano or C alkoxy; R is selected from (a) &mdash;S&mdash;Ar or &mdash;S&mdash;CH &mdash;Ar wherein Ar is an aromatic moiety; (b) &mdash;O&mdash;Ar wherein Ar is as defined above; (c) &mdash;S-Het or &mdash;S&mdash;CH -Het wherein Het is a heterocyclic ring; and (d) 2,5-dioxo-1-imidazolidinyl or 2,4-dioxo-1-imidazolinyl; and the pharmaceutically acceptable salts thereof; have potent and selective inhibitory activity against matrix metalloproteinases (MMPs) and can thus be used in the treatment and prevention of diseases mediated by MMPs.

3-Arylsulfonyl-2 (substituted methyl) propanoic acid derivatives as matrix metalloproteinase inhibitors

Amino-benzothiazole derivatives

A compound of formula (1) wherein R,is hydrogen, hydroxy, a group of formula OR,wherein R,is C,-C,alkyl, C,-C,alkenyl or C,-C,cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C,-C,alkyl, C,-C,alkenyl, aralkyl, acyl or trifluoroacetyl; R,is hydrogen, hydroxy, a group NR,R,wherein R,and R,independently represent hydrogen, an optionally substituted C,-C,alkyl, C,-C,alkenyl, C,-C,cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C,-C,heterocyclic ring; R,is hydrogen, hydroxy, R,is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.

Heterocyclyl anthracyclinone derivatives

There are provided compounds of formula (I), wherein R,is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R,is C,-C,alkyl or an alkyl group; R,and R,are independently a hydrogen atom, a C,-C,alkyl group, a C,-C,alkenyl group, a C,-C,cycloalkyl C,-C,alkyl group, a phenyl-C,-C,alkenyl or phenyl group: which groups are optionally substituted by C,-C,alkyl, C,-C,alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R,is hydrogen atom or a C,-C,alkyl group and R,is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R,is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.

Abeo-ergoline derivatives as 5HT1A ligands

Heterocyclyl-ergoline derivatives as 5-HT.sub.1A receptor ligands

Antineurodegenerative ergoline derivatives

Disubstituted piperidine derivatives as neuroprotective agents

The present invention provides compounds of the formula (I) ##STR1## wherein A, R.sub.1, R.sub.2 and R.sub.3 are defined as in the specification, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmacetical compositions comprising them are also provided.

Serotoninergic ergoline derivatives

Process for preparing ergoline derivatives

##STR1## Compounds I [R.sub.1 =H or C.sub.1 -C.sub.3 alkyl, R.sub.2 =an (alkyl-substituted) aminodeoxy or aminodideoxy or aminotrideoxy sugar residue of the D and L series, the glycosidic linkage being .alpha. or .beta.] and their pharmaceutically acceptable salts are useful as antihypertensive agents. Their preparation and use as well as pharmaceutical compositions containing them are also described.

Aminoglycoside steroids, a process for their preparation, their use and

##STR1## Compounds I (either R.sub.1 =OH, C.sub.1 -C.sub.4 alkoxy and R.sub.2 =H, C.sub.1 -C.sub.4 alkyl, or R.sub.1 +R.sub.2 =a chemical bond; R.sub.3 =an aminodeoxy or aminodideoxy or aminotrideoxy sugar residue of the D and L series, the glycosidic linkage being .alpha. or .beta.: and either R.sub.4 =OH and R.sub.5 =H or R.sub.4 +R.sub.5 =a chemical bond) and their pharmaceutically acceptable salts are useful as antihypertensive agents. Their preparation and use as well as pharmaceutical compositions containing them are also described.

Nor-cholanic acid derivatives, a process for their preparation, their

##STR1## Compounds I (either R.sub.1 =OH, C.sub.1 -C.sub.4 alkoxy and R.sub.2 =H, C.sub.1 -C.sub.4 alkyl, or R.sub.1 +R.sub.2 =a chemical bond; R.sub.3 =an aminodeoxy or aminodideoxy or aminotrideoxy sugar residue of the D and L series, the glycosidic linkage being .alpha. or .beta.) and their pharmaceutically acceptable salts are useful as antihypertensive agents. Their preparation and use as well as pharmaceutical compositions containing them are also described.

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Milan, Italy

Sergio Mantegani