Abstract: The invention concerns isotopically coded marker (ICAT) for mass spectrometric analysis of proteins, and the preparation and use of said markers.

Abstract: This invention relates to compounds containing a trioxane moiety, especially certain artemisinin derivatives, which have cytotoxic and antitumour activity and their use in the treatment of cancer. Some of these compounds comprise a ligand which is capable of binding to a nucleic acid and a group containing a trioxane moiety which is capable of acting as source of free radicals which are capable of chemically interacting with a nucleic acid. Processes for the preparation of such compounds and pharmaceutical compositions containing such compounds are also provided.

Abstract: The present invention relates to glycoconjugates of 20(S)-camptothecin, in which a 3-O-methylated &bgr;-L-fucose unit is linked to the 20-hydroxyl group of a camptothecin derivative via a thiourea-modified peptide spacer. The invention furthermore relates to processes for the preparation of the compounds according to the invention and to their use as medicaments, in particular in connection with oncoses.

Abstract: The present invention relates to cytostatics which have a tumour-specific action as a result of linkage to &agr;v&bgr;3 integrin antagonists via preferred linking units which can be selectively cleaved by elastase, i.e. by an enzyme which can especially be found in tumour tissue. The preferred linking units provide sufficient stability of the conjugate of cytostatic and &agr;v&bgr;3 integrin antagonist in biological fluids and, at the same time, the desired intracellular action within tumour cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic.

Abstract: The present invention relates to glycoconjugates of camptothecin derivatives in which at least one carbohydrate component is linked via suitable spacers with the 20-hydroxyl group of a camptothecin derivative. The invention furthermore relates to processes for preparing the compounds according to the invention and to their use as medicaments, in particular in connection with cancer.

Abstract: The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to &agr;v&bgr;3 integrin antagonists via preferred linking units which can be selevtively cleaved by enzymes such as metallo matrixproteases (MMPs), i.e. by enzymes which can especially be found in tumor tissue. The preferred linking units guarantee the serum stability of the conjugate of cytostatic and &agr;v&bgr;3 integrin antagonist and, at the same time, the desired intracellular action within tumor cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic.

Abstract: The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to specific carbohydrate moeities via preferred linking units which can be selevtively cleaved by enzymes such as metallo matrixproteases (MMPs), elastase or cathepsines, i.e. by enzymes which can especially be found in tumor tissue. The preferred linking units guarantee sufficient serum stability of the conjugate of cytostatic and carbohydrate moeity and, at the same time, the desired intracellular action within tumor cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic.

Abstract: The present invention relates to conjugates of cytostatics and N-thiocarbonyl-modified amino acids or peptides, processes for their preparation and their use as medicaments, in particular in connection with carcinomatous disorders.

Abstract: The present invention relates to compounds of the general formula (I) in which R1 and R12 represent the same or different radicals selected from the group of C2-9-alkyl, C1-8-halogen-alkyl, C3-6-cycloalkyl, aralkyl or aryl, R3 to R10 represent the same or different radicals selected from the group of hydrogen, C1-5-alkyl which may optionally be substituted by hydroxyl, alkoxy, carboxyl, carboxamide, imidazolyl, indolyl, guanidino, thio- or thioalkyl, and represent aryl, alkylaryl or heteroarylmethyl which are optionally substituted by halogen, hydroxyl, alkyl, alkoxy, nitro or a —NR13R14 group in which R13 or R14 independently from each other represent hydrogen or alkyl or together with the adjoining nitrogen atom form a 5, 6 or 7-membered ring which is optionally interrupted by O, S or N and which is optionally substituted by C1-4-alkyl, R2 and R11 represent the same of different radicals selected from the group of C1-4-alkyl, and stereoisomers thereof, to processes for their prep

Abstract: The present invention relates to compounds of the general formula (I) in which R1, R2, R11 and R12 represent the same or different radicals selected from the group of C1-8-alkyl, C1-8-halogenoalkyl, C3-6-cycloalkyl, aralkyl or aryl, R3, R5, R7, R9, represent the same or different radicals selected from the group of hydrogen or straight-chain C1-5-alkyl or branched C4-7-alkyl which may optionally be substituted by hydroxyl, C1-4-alkoxy, carboxyl  carboxamide,  imidazolyl, indolyl, guanidino, —SH or C1-4-alkylthio, and furthermore represents aryl, aralkyl or heteroarylmethyl which may be substituted by halogen, hydroxyl, C1-4-alkyl, C1-4-alkoxy, nitro or a —NR13R14 group in which R13 and R14 independently from each other represent hydrogen or alkyl or together with the adjoining nitrogen atom forms a 5, 6 or 7-membered ring which is optionally interrupted by O, S or N and which is optionally C1-4-alkyl substituted, R4, R6, R8, R10

Abstract: The invention relates to cytostatics which, by modification with sugar, are tumor-specific. Suitable spacers ensure serum stability and at the same time an intracellular action.

Abstract: The present invention relates to glycoconjugates of camptothecin derivatives in which at least one carbohydrate component is linked via suitable spacers with the A or B ring of a camptothecin derivative. The invention furthermore relates to processes for preparing the compounds according to the invention and to their use as medicaments, in particular in connection with cancer.

Abstract: The present invention relates to 2,2'-bridged bis-2,4-diaminoquinazolines of the general formula (I): ##STR1## in which the indicated substituents are as defined in the description. The invention also provides processes for the preparation of the compounds of the formula (I), their use for the preparation of drugs, and drugs containing said compounds.

Abstract: The present invention relates to the use of open-chain octadepsipeptides of the general formula: ##STR1## wherein the R variables have been defined in the specification.

Abstract: 4,4'-Bridged bis-2,4-diaminoquinazolines of the general formula (I) ##STR1## processes for their preparation and use as agents acting on the potassium channels of the brain.

Abstract: The present invention relates to compounds of the general formula (I) ##STR1## in which R.sup.1 and R.sup.12 represent the same or different radicals selected from the group of C.sub.2-9 -alkyl, C.sub.1-8 -halogeno-alkyl, C.sub.3-6 -cycloalkyl, aralkyl or aryl,R.sup.3 to R.sup.10 represent the same or different radicals selected from the group of hydrogen, C.sub.1-5 -alkyl which may optionally be substituted by hydroxyl, alkoxy, carboxyl, carboxamide, imidazolyl, indolyl, guanidino, thio- or thioalkyl, and represent aryl, alkylaryl or heteroarylmethyl which are optionally substituted by halogen, hydroxyl, alkyl, alkoxy, nitro or a --NR.sup.13 R.sup.14 group in which R.sup.13 or R.sup.14 independently from each other represent hydrogen or alkyl or together with the adjoining nitrogen atom form a 5, 6 or 7-membered ring which is optionally interrupted by O, S or N and which is optionally substituted by C.sub.1-4 -alkyl,R.sup.2 and R.sup.11 represent the same of different radicals selected from the group of C.