Farmitalia Carlo Erba S.r.l.

Farmitalia Carlo Erba

Pharmacia Italia S.p.a.

Pharmacia & Upjohn

Nerviano Medical Sciences S.r.l.

Paolo Cozzi

Italo Beria

Antonio Pillan

Patricia Salvati

Marina Caldarelli

Pier P Lovisolo

Germano Carganico

Laura Capolongo

Maria Cristina Geroni

Corrado Ferti

Pier Giovanni Baraldi

Romeo Romagnoli

Leone Bertone

Nicola Mongelli

Arsenia Rossi

Augusto Chiari

Maria Menichincheri

Enrico Pesenti

Dino Severino

Umberto Branzoli

Giancarlo Ghiselli

Angelo D Volpi

Maurizio Pulici

Tiziano Bandiera

Daniele Fancelli

Antonio Giordani

Paola Vianello

Fabrizio Orzi

Giovanni Biasoli

Arturo Galvani

Maria Cristina Rosa Geroni

Giampiero Spalluto

Severino Dino

Marla Menichincheri

Mariia Menichincheri

Ivo De Carneri

Piero Menchetti

Franca Trane

Giulia Pennella

Osvaldo Magni

Romano Angelucci

Cristina Franzetti

Maria Bergamaschi

Pierpaolo Lovisolo

Danielle Fancelli

M Cristina Geroni

Compounds which are &#x3b1;-halogenoacryloyl distamycin derivatives of formula (I) wherein Ris a bromine or chlorine atom; Ris a distamycin or distamycin-like framework as set forth in the specification; or a pharmaceutically acceptable salt thereof; are cytotoxic agents particularly effective in the treatment of tumors over expressing GSH/GSTs system and which are poorly responsive or even resistant to conventional antitumor therapies.

Combined therapy against tumors comprising substituted acryloyl distamycin derivatives and platinum derivatives

A pharmaceutical composition and a product which includes an acryloyl distamycin derivative, an antimicrotubule agent and/or an antimetabolite useful in the treatment of tumors.

Pharmaceutical composition and a product which includes a substituted acryloyl distamycin derivative, an antimicrotubule agent and/or an antimetabolite

Use of substituted acryloyl distamycin derivatives in the treatment of tumors associated with high levels of glutathione

Novel propanoic acid derivatives are integrin receptor antagonists or inhibitors, in particular of the avb3 integrin receptor. The compounds of the invention are for instance useful for the treatment of solid tumors by inhibition of angiogenic growth of tumor vessel network, thus promoting tumor regression, inhibition of metastatic spread, thus avoiding cancer metastases, inhibition of bone resorption, thus controlling osteoporosis, inhibition of smooth muscle cells migration into neointima, thus blocking restenosis after percutaneous coronary angioplasty and the treatment of other pathological conditions mediated by cell adhesion, cell migration or angiogenesis such e.g. diabetic retinopaty, rheumatoid arthritis and inflammation.

Propanoic acid derivatives as intergrin receptor antagonists

A process for preparing distamycin derivatives possessing antitumor activity, by starting from distamycin A itself, is described. The process involves the preparation of the novel intermediates of formula (III)

Process for preparing distamycin derivatives

The present invention refers to distamycin and derivatives thereof, such as bromo- or chloro-acryloyl derivatives of distamycin, which are conjugated with glutathione, to a process for their preparation and to pharmaceutical compositions thereof. The compounds of the invention are endowed with a remarkable antitumor activity and are thus useful in therapy in the treatment of cancer.

Glutathiaone conjugates with distamycin derivatives having antitumoral activity

Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring of the polyetherocyclic chain, from N and CH; R and R , which are the same or different, are selected from hydrogen, halogen, and C -C alkyl; R is hydrogen or halogen; B is selected from (a), (b), (c), (d), (e), (f), (g) and &mdash;C&equiv;N; wherein R , R , R , R , R , R , R , and R are, independently from each other, hydrogen or C -C alkyl; and R is hydrogen or hydroxy, or pharmaceutically acceptable salt thereof; provided that a) at least one of R , R and R is alkyl b) at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrole; and c) X and Y are not both N for the same heterocyclic ring; are useful as antitumor agents.

Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents

Compounds which are cinnamoyl distamycin derivatives of formula (I), wherein n is 2, 3, or 4; R is C -C alkyl or C -C haloalkyl; R and R , which are the same or different, are selected from hydrogen, C -C alkyl optionally substituted by one or more fluorine atoms; and C -C alkoxy; X is a halogen atom; Y and Z are the same or different and are selected, independently for each heterocyclic ring of the polyheterocyclic chain, from N and CH; B is selected from (a), (b), (c), (d), (e), (f), (g)and (h) wherein R , R , R , R and R are, independently from each other, hydrogen or C -C alkyl; or pharmaceutically acceptable salts thereof; provided that at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrrole; are useful as antitumor agents.

Cinnamoyl distamycin analogous derivatives, process for their preparation, and their use as antitumor agents

The present invention relates to acrylol substituted distamycin derivatives, to pharmaceutical compositions comprising such derivatives as well as their use in methods of treating humans and animals, particularly as anti-tumor agents.

Acryloyl substituted distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents

Compounds which are benzoheterocyclic distamycin derivatives of formula (I), wherein n is 2, 3 or 4; A is a heteroatom selected from O and S or is a group NR, wherein R is hydrogen or C -C alkyl; B is CH or N; R is hydrogen or C -C alkyl; G is selected from the group consisting of (a, b, c, d, e, f, g, h, i, j), and &mdash;C&equiv;N; wherein R , R , R , R , R , R , R and R are, independently from each other, hydrogen or C -C alkyl; T is a group of formula (II) or (III) as defined above, wherein p is 0 or 1; R and R are, independently from each other, hydrogen, C -C alkyl optionally substituted by one or more fluorine atoms, or C -C alkoxy; R is C -C alkyl or C -C haloalkyl; X and X are halogen atoms or pharmaceutically acceptable salts thereof; provided that at least one of R , R and R is alkyl; are useful as antitumor agents.

Benzoheterocyclic distamycin derivatives, process for preparing them, and their use as antitumor agents

A compound which is a distamycin derivative of formula (I), wherein n is 2, 3 or 4; R,is C,-C,alkyl or C,-C,haloalkyl; R,and R,, which may be the same or different, are each hydrogen, C,-C,alkyl optionally substituted by one or more fluorine atoms, or C,-C,alkoxy; X is a halogen atom; B is selected from (A, B, C, D, E, F, G, H, I, J and K); wherein R,, R,, R,, R,, R,, R,, and R,, which may be the same or different, are each hydrogen or C,-C,alkyl, and m is 0, 1, or 2; or a pharmaceutically acceptable salt thereof. Such compounds are useful as antineoplastic and antiviral agents.

Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents

Distamycin derivatives, process for preparing them, and their use as

Benzoheterocyclic distamycin derivatives, process for preparing them,

Imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines of formula (I) ##STR1## wherein Het is ##STR2## A represents a direct linkage, --CH.sub.2 --, CH.sub.2 --CH.sub.2 -- or, when Het is ##STR3## A may also represent --CH.dbd.CH--; R is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy; each of R.sub.3 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group; one of R.sub.1 and R.sub.2 is a group --OR' wherein R' is a C.sub.1 -C.sub.6 alkyl either unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy or cyano, and the other is, independently,

Imidazolyl and pyridyl derivatives of phenyl substituted

Compounds which are useful in anti-tumors therapy having the formula (I) ##STR1## wherein Het imidazole, A represents a direct linkage at the phenyl 4-position: R is hydrogen; one of R.sub.3 and R.sub.4 is C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy, and the other, independently, is:

Dihydropyridine derivatives useful in antitumor therapy

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Milan, Italy

Paolo Cozzi