Sigma-tau Industrie Farmaceutiche Riunite S.p.a.

Biogem S.c. a R.l.

Istituto Nazionale Per Lo Studio E La Cura Dei Tumori

Other

Farmitalia Carlo Erba S.p.a.

Instituto Nazionale Per Lo Studio E La Cura Dei Tumori

Istituto Nazional Per Lo Studio E La Cura Dei Tumori

Lucio Merlini

Sergio Penco

Claudio Pisano

Franco Zunino

Sabrina Dallavalle

Giuseppe Giannini

Loredana Vesci

Maria Ornella Tinti

Raffaella Cincinelli

Paolo Carminati

Domenico Alloatti

Alma Dal Pozzo

Alessandro Rossi

Metilde Buonamici

Ni Minghong

Ni Ming Hong

The present invention relates to compounds of formula (I) and to pharmaceutical compositions containing them: wherein meanings of the substituents are indicated in the description. Such compounds for use in the treatment of cancer and other diseases related to altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, are also within the scope of the present invention.

Retinoid derivatives with antitumor activity

Are described compounds of Formula (I) in which R, R', R&#x2033;, A, and D have the meanings described in the text, as useful agents in the cure of pathologies characterized by altered angiogenesis and as antitumorals.

Retinoid derivatives with antiangiogenic, antitumoral and proapoptotic activities

Biphenyl and phenyl-naphthyl compounds bearing a hydroxamic group, which are endowed with antitumor, and anti-angiogenic activity These compounds are therefore particularly useful for the treatment of drug-resistant tumors.

Biphenyl and Naphthyl-Phenyl Hydroxamic Acid Derivatives

Compounds of Formula (I) are described in which the Rgroup is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors &#x3b1;&#x3b2;and &#x3b1;&#x3b2;and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.

Camptothecins conjugated in position 7 to cyclic peptides as cytostatic agents

Compounds are disclosed with the general formula in which the groups are as defined in the description here below and characterized by the presence of polyamine substituents on the imine/oxime residue, such amine groups being in turn protected by suitable protective groups. Said compounds are endowed with potent topoisomerase I inhibiting activity and therefore are useful as medicaments for the treatment of tumors and viral and parasite infections.

7-Polyaminoalkyl(oxy)iminomethylcamptothecins bearing protective groups

Compounds of Formula (I) are described: in which the Rgroup is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors &#x3b1;&#x3b2;and &#x3b1;&#x3b2;and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.

7-t-butoxyiminomethylcamptothecin conjugated in position 20 with integrin antagonists

Described and claimed are compounds of Formula (I) in which R, R', R&#x2033;, A, and D have the meanings described in the text, as useful agents in the cure of pathologies characterized by altered angiogenesis and as antitumorals.

Camptothecin derivatives having antitumor activity

Compounds of formula (I), wherein: R,is &mdash;CN, &mdash;CH(CN)&mdash;R,, &mdash;CH&boxH;C(CN)&mdash;R,, &mdash;CH,&mdash;CH(CN)&mdash;R,, &mdash;C(&boxH;NOH)&mdash;NH,, &mdash;C(&boxH;NH)&mdash;NH,, &mdash;CH&boxH;C(NO,)&mdash;R,, &mdash;CH(CN)&mdash;R,, &mdash;CH(CH,NO,)&mdash;R,; 5-tetrazolyl, 2-(4,5-dihydrooxazolyl), 1,2,4-oxadiazolin-3-yl-5-one; R,is hydrogen; R,is hydrogen, OR,; R,is hydrogen, C,-C,linear or branched alkyl, CN, COOR,; R,is hydrogen, OR,; R,is hydrogen, C,-C,linear or branched alkyl, (C,-C,) aryl (C,-C,) alkyl, (C,-C,) alkoxy (C,-C,) alkyl, (C,-C,) alkyl (C,-C,) aryl, (C,-C,) aryl (C,-C,) acyl, (C,-C,) acyl, amino (C,-C,) alkyl, amino (C,-C,) acyl, glycosyl; R,is hydrogen, C,-C,linear or branched alkyl, (C,-C,) aryl (C,-C,) alkyl, (C,-C,) alkoxy (C,-C,) alkyl, (C,-C,) alkyl (C,-C,) aryl; R,has the same meanings of R,, independently of the latter. These compounds are active as topoisomerase I inhibitors and can be used as antitumor drugs.

Methods for inhibiting the growth of tumors with 7-substituted camptothecin derivatives

Camptothecin derivatives of camptothecin of formula (I)

7-Substituted camptothecin derivatives and methods for inhibiting the

Substituted imino derivatives of 4 H-2, 3-dihydrobenzopyran and 4 H-2, 3-dihydrobenzothiopyran, and pharmaceutical compositions containing them. The compounds are active on the central nervous system, in particular as central nervous system depressants, i.e., sedatives, anticonvulsive agents, tranquilizers and sleep-inducing agents.

Growing community of inventors

Milan, Italy

Lucio Merlini