Abstract: The present invention concerns a process for improving doxorubicin production by means of a recombinant Streptomyces peucetius strain bearing a mutation in the gene dnrU coding for a protein involved in the metabolism of daunorubicin.

Abstract: Novel 2(4-substituted)-benzylamino-2-methyl-propanamides compounds, having CNS activity, of general formula (I) wherein: n is zero, 1, 2 or 3; X is --O--, --S--, --CH.sub.2 -- or --NH--; each of R and R.sub.1 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 alkoxy or trifluoromethyl; each of R.sub.2, R.sub.3 and R.sub.4 independently is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.7 cycloalkyl; and the pharmacetically acceptable salts thereof, are disclosed.

Abstract: Compounds of formula (I), wherein: the symbol represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; R.sub.f and R'.sub.f, each independently, are C.sub.1 -C.sub.4 alkyl groups substituted by one or more fluorine atoms; and R.sub.1 and R.sub.2, each independently, are selected from: a hydrogen atom; a phenyl group; a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms; a halogen atom; a cyano (CN) group; a group OR.sub.4, wherein R.sub.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; a group SR.sub.5, wherein R.sub.5 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and a group COR.sub.6, wherein R.sub.6 is a group OR.sub.4 in which R.sub.4 is as defined above or a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms. They are useful as testosterone 5a-reductase inhibitors.

Abstract: The present invention relates to terpenoidic derivatives, known in the art as Sarcodictyins, for use as therapeutic agents, and to pharmaceutical compositions containing them.In particular, Sarcodictyins can be useful as therapeutic antineoplastic agents in the treatment of cancers in human or animal beings.

Abstract: The present invention relates to a process for the generation of a plurality of different benzofuran derivatives, and to the use of said benzofuran derivatives to search for novel classes of compounds and individual compounds possessing selected properties for pharmaceutical applications.

Abstract: The present invention relates to compounds of the following formulas: ##STR1## which are endowed with antitumor activity. The invention also relates to methods of treating tumors using these compounds.

Abstract: The invention in the field of cell biology relates to novel peptides able to interact with intracellular signal transducers, thus interfering with signal transduction pathways leading to cell proliferation and motility.The peptides of the invention may be chemically synthesized from single amino acids and/or preformed peptides of two or more amino acid residues.The peptides of the invention find an useful application in the treatment of a neoplastic disease.

Abstract: The present invention relates to novel N-(4-substituted-benzyl)-2-aminolactams as therapeutic agents, pharmaceutical compositions and a process of preparation.

Abstract: Quinolylmethylen-oxindole derivatives having general formula (I), wherein R is H or --(CH.sub.2).sub.n --COR.sub.7 group in which n is an integer of 1 to 4 and R.sub.7 is hydroxy, amino, C.sub.1 -C.sub.6 alkoxy or --NR.sub.5 R.sub.6 in which one of R.sub.5 and R.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.5 and R.sub.6 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle or R.sub.7 is a N-terminally linked peptidyl residue containing from 1 to 3 aminoacids in which the terminal carboxyl group may be present as such, as amide, as alkali metal salt or as a C.sub.1 -C.sub.4 alkyl ester, one or two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are selected from: a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.5 R.sub.6 or --X--(CH.sub.2).sub.m --NHR.sub.8 group; b) --NH--C(.dbd.NH)--NR.sub.5 R.sub.6, --NH--C(.dbd.NH)--NHR.sub.8, --N.dbd.CH--NH.sub.2, --N.dbd.

Abstract: Novel 5-HT.sub.3 receptor antagonist compounds having following formula (I) ##STR1## wherein n is 1, 2 or 3;each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N (R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7) N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group; and the pharmaceutically acceptable salts thereof, are disclosed.

Abstract: A method of treating tumors in a human or animal by administering thereto a pharmaceutically effective amount of a Sarcodictyin compound selected from Sarcodictyin A, B, C, D, E, and F. Sarcodictyin A has the formula (-)-(4R,4aR,7R,10S,11S,12aR,1Z,5E,8Z)-7,10-Epoxy3,4,4a,7,10,11,12,12a-octa hydro-7-hydroxy-6-(methoxy-carbonyl)-1,10- dimethyl-4-(1-methylethyl)benzo cyclodecen-11-yl(E)-3-(1-Methyl-1H-imidazol-4-yl) acrylate (Sarcodictyin A).

Abstract: Derivatives of gamma-amino-alpha,beta-unsaturated sulfonic acids, a process for the preparation of the same and their utilization in the synthesis of pseudopeptides characterized by the presence of at least a sulfonamide type bond conjugated to a double bond are described.

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: The present invention relates to substituted camptothecin derivatives of formula (I) wherein the symbol - - - - represents a single or double bond; R.sub.1, R.sub.2 and R.sub.3 are as defined under (a) or (b) below: (a) R.sub.1 and R.sub.2 are, each independently, hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.3 -C.sub.7 cycloalkyl; phenyl C.sub.1 -C.sub.6 alkyl; an optionally substituted phenyl ring; --NR.sub.5 R.sub.6 wherein one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl and the other is hydrogen, C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted benzoyl, phenyl C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted phenoxycarbonyl or phenyl C.sub.1 -C.sub.6 alkoxycarbonyl, or R.sub.5 and R.sub.6, combined together with the nitrogen atom to which they are linked, form a 4-7 membered saturated, optionally substituted, heteromonocyclic ring residue; COOR.sub.8 wherein R.

Abstract: The present invention relates to indol-3-ylmethylene-2-oxindole derivatives which are useful as tyrosine kinase inhibitors. The compounds are suitable for use as anti-proliferative agents, anti-metastatic agents, anti-cancer agents, and in the control of angiogenesis and in inhibiting the development of atheromatous and an immunomogulating agents.

Abstract: The present invention is related to a process for the preparation of 5-?2H-pyrrol-2-ylidene)methyl!-2,2'-bi-1H-pyrrole compounds and an intermediate compound.

Abstract: Disclosed are isolated DNAs encoding a kynurenine aminotransferase selected from the group consisting of: (a) an isolated DNA sequence which encodes rat KAT; (b) an isolated DNA sequence which hybridizes to the isolated DNA sequence of (a) above and which encodes a KAT enzyme; and (c) an isolated DNA sequence differing from the isolated DNA sequences of (a) and (b) above in codon sequence due to the degeneracy of the genetic code, and which encodes a KAT enzyme. Also disclosed are vectors and host cells containing the same; oligonucleotide probes for identifying kynurenine aminotransferase; and isolated and purified kynurenine aminotransferase.

Abstract: Immunoglobulin conjugates, comprising idarubicin (Ida) conjugated to a monoclonal antibody or fragment thereof comprising at least one of the antigen binding sites of the antigen, are useful for treating a human or other animal suffering from a cancer or for depleting a subset of T lymphocytes from a population of cells.

Abstract: The ability to convert daunorubicin to doxorubicin can be conferred on a host cell by transformation with a recombinant vector comprising DNA encoding daunorubicin 14-hydroxylase. The host cell can then be used to produce doxorubicin.