Abstract: The present invention provides compounds or formula (1) R1—HN—CH2—CF2—(CH2)l—CR3R4—CO—R2, wherein: l is 0, 1 or 2, R1 is a labile amino protecting group, R2 is hydroxy group or the residue or an activated ester or halogen atom; R3 and R4 are independently hydrogen atom or C1-C4 alkyl chain. There are also provided their preparation and the water-soluble conjugates based on these linkers, endowed with selective anticancer activity.

Abstract: There are provided the combined use of 4-demethoxy-3′-deamino-3′-aziridinyl-4′-methansulfonyl daunorubicin or 4-demethoxy-N,N-bis(2-chloroethyl)-4′-methansulfonyl daunorubicin and an anti-neoplastic anti-mitotic compound and/or a platinum derivative in the treatment of tumors, as well as in the prevention or treatment of metastasis or in the treatment of tumors by inhibition of angiogenesis.

Abstract: The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an alkylating agent, an antimetabolite, a topoisomerase II inihbitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.

Abstract: The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an allylating agent, an antimetabolite, a topoisomerase II inihbitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.

Abstract: The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an alkylating agent, an antimetabolite, a topoisomerase II inhibitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.

Abstract: The combination of 4-demethoxy-3′-deamino-3′-aziridinyl-4′-methansulfonyl daunorubicin or 4-demethoxy-N,N-bis(2-chloroethyl)-4′-methansulfonyl daunorubicin together with an antineoplastic topoisomerase I inhibitor yields preparations exhibiting anti-cancer effects. These preparations can be used in the treatment of tumors and especially 4-demethoxy-3′-deamino-3′-aziridinyl-4′-methansulfonyl daunorubicin in the treatment of brain tumors.

Abstract: Water soluble polymeric conjugates of camptothecin consist essentially of N-(2-hydroxypropyl)methacryloylamide units linked via a spacer group to a residue of a camptothecin such as irinotecan or its non-soluble metabolite, 7-ethyl-10-hydroxy-camptothecin. The conjugates possess enhance antitumor activity and decreased toxicity with respect to the free drug. A process for their preparation and the pharmaceutical compositions containing them are also described.

Abstract: Water soluble polymeric conjugates of camptothecin consist essentially of N-(2-hydroxypropyl)methacryloylamide units linked via a spacer group to a residue of a camptothecin such as irinotecan or its non-soluble metabolite, 7-ethyl-10-hydroxy amptothecin. The conjugates possess enhance antitumor activity and decreased toxicity with respect to the free drug. A process for their preparation and the pharmaceutical compositions containing them are also described.

Abstract: The invention relates to polymeric conjugates of 20-O-[glycyl-aminoacyl-glycyl]-camptothecins and a process for producing the same.

Abstract: A compound of formula (1), wherein R1 represents hydrogen, hydroxy, a group of formula OR7, wherein R7 is C1-C6 alkyl, C2-C6 alkenyl; R2 represents hydrogen, hydroxy, diethylamino, piperidino, tetrahydropyridino or morpholino, and either R3, taken alone, represtnts hydrogen or hydroxy, and R4 and R5, taken alone, independently represent hydrogen, hydroxy or, taken together with the carbon atom, represent a carbonyl group; or R3 and R4, taken together, represent a group of formula (A), wherein R8 and R9 represent a C1-C6 alkyl and R5 represents hydrogen; R6 represents hydrogen or a phenyl group, optionally substituted by methyl, methoxy or halogen and the pharnaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.

Abstract: The present invention relates to anthracycline glycosides, to a process for their preparation and to pharmaceutical compositions containing the same.

Abstract: A lyophilized composition comprising (a) a conjugate comprising a N-alkyl methacrylamide-based copolymer and an anthracycline glycoside linked through a peptide spacer to the copolymer and (b) a cosolubilizing agent may optionally also contain (c) a filler. Also optionally, a targeting moiety may be linked to the copolymer of the conjugate via a peptide spacer. An injectable solution of the conjugate is obtained by reconstitution of the lyophilized composition.

Abstract: The present invention provides imino aza-anthracyclinones and a method of treating amyloidoses using the same.

Abstract: Compounds of formula (A), wherein R.sub.1, R.sub.2, R.sub.3, Y and Z are organic substituents, are useful in the diagnosis of amyloidosis; some of the compounds of formula (A) are novel. Processes for their preparation, and pharmaceutical compositions containing them are also described.

Abstract: The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.

Abstract: The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.

Abstract: Compounds of formula I ##STR1## wherein X.sub.1 and X.sub.2 are C.dbd.O, C.dbd.NH or CH.sub.2, X.sub.3 is CH.sub.2, CO, CHOH, ##STR2## wherein n=2 or, 3 or C.dbd.N(R.sub.9) wherein R.sub.9 is hydroxy or amino-aryl, and each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are hydrogen, halogen or an organic residue, are useful in the treatment of amyloidosis. A process for their preparation and pharmaceutical compositions containing them are also described.

Abstract: The present invention provides anthracycline conjugates with carriers such as monoclonal polyclonal antibodies, proteins or peptides, or other synthetic carriers. These anthracycline conjugates provide pharmaceutical compositions which are useful for treating certain mammalian tumors. The compounds of the present invention have higher potency than anthracyclines, and improved therapeutic efficacy and reduced toxic effects.

Abstract: A polymeric conjugate consists essentially of: (i) from 60 to 99 mol % of N-(2-hydroxypropyl) methacryloylamide units represented by formula 1: ##STR1## (ii) from 1 to 40 mol % of 20-0-(N-methacryloylglycyl-aminoacyl) camptothecin units represented by formula 2 ##STR2## wherein ?A! is a spacer group having respective terminal amino and carbonyl groups which are separated by at least three atoms and O-CPT represents a residue of a camptothecin, the C-20 hydroxy group of the camptothecin being linked to the terminal carbonyl group of the spacer group ?A!; and (iii) from 0 to 10 mol % of N-methacryloylglycine or N-(2-hydroxy-propyl)methacryloylglycinamide units represented by formula 3: ##STR3## wherein Z represents hydroxy or a residue of formula --NH--CH.sub.2 --CH(OH)--CH.sub.3.

Abstract: The present invention provides the new use in the manufacture of a medicament for use in the treatment of amyloidosis of an anthracycline of formula A: wherein R1, R2, R3 and X are appropriate substituents. Novel compounds of the formula A, processes for their production and pharmaceutical compositions containing them are also described.