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The urotoxicity of oxazaphosphorine cytostatics is not based on their alkylating activity but on the presence of acrolein, which is spontaneously formed in the urine from the primary metabolites eliminated via the kidneys. Thus, acrolein proved to be the causative factor in the urotoxicity of oxazaphosphorines. The mechanism of action of the uroprotector… (More)
— An IC 1 for consumer electronics TV sets performing 100 Hz interlaced / 60 Hz progressive scan rate conversion has been designed. Picture-in-picture, split screen and picture improvement capabilities are also integrated. It applies a motion-compensating algorithm for high-quality scan rate conversion. PIP processing is performed using a full frame based… (More)
The primary metabolite of cyclophosphamide (CP, 1), i.e. 4-hydroxy-CP 2, has high pharmacological activity, but it is a very unstable compound. Chemical approaches to the stabilization involved in the substitution of the hydroxy group at the C 4-position, especially by a sulfoalkylthio-moiety. Within this new class of compounds ASTA Z 7557… (More)
Synthesis of new basic enol ethers with valuable pharmacological properties is described. The structure of these compounds is elucidated by 1H- and 13C-NMR-spectroscopy; the stereochemistry of the double bond is determined by use of the intramolecular nuclear Overhauser effect. An X-ray analysis of an isolated diastereomer confirms the proposed constitution.
Two ifosfamide (CAS 3778-73-2) analogs with a five-membered ring, i.e. the oxazaphospholidine derivatives 6 and 7, were synthesized and their cytotoxic activity in vitro, acute toxicity and antitumor activity in vivo determined in comparison with the oxazaphorinane ifosfamide 1. The observed low biological activity gives evidence that both, the six-membered… (More)
The synthesis of 4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone hydrochloride (14C-azelastine hydrochloride, Asta A 5610) is described Starting material was 14C-phthalic anhydride.
The synthesis of 4-ureidooxycyclophosphamide, a potential cytostatic, whose cis/trans-isomers can be stereoselectively obtained from 4-hydroxycyclophosphamide and hydroxyurea in DMF in DMF or water, is described. These compounds are remarkably stable at room temperature. For the first time, the two epimers from a derivative of 4-hydroxycyclophosphamide can… (More)