Abstract: Objects of the present invention are novel ureido derivatives of naphthalensulfonic acids, pharmaceutical compositions comprising such derivatives, a process for the preparation thereof and the use of said derivatives as medications, in particular in the treatment of HIV infections.

Abstract: High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498-505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.

Abstract: High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498–505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.

Abstract: A compound which is a benzocyclodecane of the formula I: wherein: at positions 8-9 and 11-12 independently represents a single or double bond, —R1 is ?O, or —OR7, R7 is H, C1-C7 alkanoyl, benzoyl, C1-C10 alkyl, C2-C10 alkenyl or COCH?CHR8, R8 is aryl or heterocyclyl; —R2 and —R3 are H, ?O or —OR9, R9 is H, C1-C7 alkanoyl or benzoyl; when at position 11-12 there is a single bond, then —R4 represents ?O, ?CH2, ?CHCOOR10, R10 is C1-C10 alkyl or aryl; ?CH(OCH3), —OR9; —CH2OR11, R11 is H or a sugar residue, —COR12, R12 is H, —OH or —OR10; or when at position 11-12 there is a double bond, then —R4 is —CH2OR11 or —COR12; —R5 and —R6 are H or, when at position 8-9 there is a single bond, taken together form a cyclopropane ring; R13 is H or 1-3 substituents selected from C1-C6 alkyl, C2-C6 alkenyl, phenyl, phenyl C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy, aryloxy, cyano, nitro, amino, C1-C10 alkylamino, arylamino, C1-C7 alkanoylamino, aroylamino, hydroxycarbonyl, aminocarbonyl, C1-C6 alkylcarbonyl, C1-C6

Abstract: A process for preparing distamycin derivatives possessing antitumor activity, by starting from distamycin A itself, is described.

Abstract: High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498-505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.

Abstract: There are provided sarcodictyin derivatives or pharmaceutically acceptable salts thereof, which are characterized by a simplified chemical structure and have anti-tumor activity. A process for their preparation, the pharmaceutical compositions containing them, and their use in the prevention, control and treatment of cancer are also provided.

Abstract: Compounds which are &agr;-halogenoacryloyl distamycin derivatives of formula (I) wherein R1 is a bromine or chlorine atom; R2 is 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.

Abstract: Herewith provided is a process for preparing useful intermediates in the preparation of distamycin derivatives possessing antitumor activity, said derivatives having the formula reported in the specification, by using distamycin A as the starting material.

Abstract: Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, R.sub.a, R.sub.b, R.sub.c, R.sub.1, R.sub.2, R.sub.3 are appropriate organic residues can be antitumor agents.

Abstract: Use, in the preparation of a medicament for use in the treatment of multiple sclerosis, of a compound which is a ureido derivative of formula (I) ##STR1## wherein each of m and n, which are the same, is an integer of 1 to 3; and each of the R groups, which are the same, is a naphthyl group substituted by 1 to 3 sulfonic acid groups, or a pharmaceutically acceptable salt thereof.

Abstract: A process for preparing libraries of indole compounds by solid phase synthesis in the presence of organometallic catalysts. The resulting compounds have a very high purity degree, which allows biological testing on the crude products with a high confidence degree, without any cross contaminations.

Abstract: A process of making taxane derivatives by reacting Baccatin III derivatives with an oxazolidine which contains a thioester substituent at the 4-position.

Abstract: The present invention relates to compounds of formula (I) ##STR1## The compounds of the invention are useful as antitumor or antiviral agents.

Abstract: A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.

Abstract: Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, R.sub.a, R.sub.b, R.sub.c, R.sub.1, R.sub.2, R.sub.3 are appropriate organic residues can be antitumor agents.

Abstract: Subject of the present invention are new ureido derivatives of naphthalenephosphonic acids having the following formula (I) ##STR1## wherein each of m and n, which are the same, is an integer of 1 to 4; each of p and q, which are the same, is an integer of 1 to 3; and each of the R groups, which are the same, is a free or esterified phosphonic acid group; and the pharmaceutically acceptable salts thereof.