Asta Medica, Aktiengesellschaft

Asta-werke Aktiengesellschaft, Chemische Fabrik

Asta Pharma Aktiengesellschaft

Asta-werke Aktiengesellschaft

Asta Pharma Aktiengesellshaft

Ulf Niemeyer

Jurgen Engel

Gerhard Scheffler

Norbert Brock

Jorg Pohl

Alfred Olbrich

Wolfgang Schumacher

Bernd Kutscher

Axel Kleemann

Bernhard Kutscher

Peter Hilgard

Michael Bernd

Gerhard Nossner

Hans-Jurgen Hohorst

Georg Voelcker

Ion Neda

Bernard Kutscher

Gerhard Nssner

Joerg Pohl

Harald Niegel

Ludmilla Bielicki

A process for the preparation of oxazaphosphorine-2-amines of the formula (I) described by the reaction scheme

Process for the preparation of oxazaphosphorine-2-amines

A process for the preparation of C.sub.14 -C.sub.18 -alkylphosphocholines by reacting an n-alkanol with a chain length of C.sub.14 -C.sub.18 with phosphorus oxychloride in an inert solvent or also without solvent in the presence or absence of a basic substance in a single vessel process and subsequent reaction of the reaction product in an inert solvent with a choline salt in the presence of a basic substance to form phosphoric acid diester chloride, subsequent hydrolysis and isolation of alkylphosphocholine as well as optionally purification using a mixed-bed ion exchanger or in successive steps with an acid ion exchanger and a basic ion exchanger.

Process for the preparation of alkylphosphocholines and the production

Nova- and decapeptides in the preparation of a drug for the treatment of

There are disclosed compounds of the formula ##STR1## The compounds have antitumour and AIDS treatment activity.

Heterocyclic compounds having a

This invention relates to new oxzaphosphorin-4-thio-alkanesulphonic acids and to the neutral salts thereof corresponding to the general formula I ##STR1## and to methods to use such compounds to treat cancer diseases and to produce immunosuppression in humans and animals.

oxazaphosphorin-4-thio alkanesulphonic acids, neutral salts thereof and

There are provided new antitumor salts of oxazaphosphorine derivatives of the formula ##STR1## where R.sub.1, R.sub.2, and R.sub.3 are the same or different and represent hydrogen, methyl, ethyl, 2-chloroethyl, or 2-methanesulfonyloxyethyl and wherein at least two of these residues are 2-chloroethyl and/or 2-methanesulfonyl-oxyethyl and A is the group --S--alk--SO.sub.3 H or --N(OH)--CONH--alk--CO.sub.2 H and alk represents a C.sub.2 -C.sub.6 -alkylene residue optionally containing a mercapto group, whereby alk also can be --CH.sub.2 -- in case there is a carboxy group attached to the alk group, with homocysteinethiolactone or .alpha.-amino-.epsilon.-caprolactam or a basic compound of the formula: ##STR2## wherein R.sub.4 is a hydroxy group, an amino group or a C.sub.1 -C.sub.6 -alkoxy group, R.sub.5 is hydrogen or a difluoromethyl group, R.sub.6 is hydrogen, an indolyl-(3)-methyl residue, imidazolyl-(4)-methyl residue, a C.sub.1 -C.sub.10 -alkyl group or a C.sub.1 -C.sub.10 -alkyl group which is substituted by a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a mercapto group, a C.sub.1 -C.sub.6 -alkylmercapto group, a phenyl group, a hydroxy phenyl group, an amino-C.sub.1 -C.sub.6 -alkylmercapto group, an amino-C.sub.1 -C.sub.6 -alkoxy group, an amino group, an aminocarbonyl group, a ureido group (H.sub.2 NCONH--), a guanidino group or a C.sub.1 -C.sub.6 -alkoxycarbonyl group, or wherein R.sub.6 together with the structured portion &gt;CR.sub.5 (NR.sub.7 R.sub.8) forms the proline residue, the 4-hydroxy-proline residue or the 2-oxo-3-amino-3-difluoromethyl-piperidine and the residues R.sub.7 and R.sub.8 represent hydrogen or C.sub.1 -C.sub.6 -alkyl residues.

Salts of oxazaphosphorine derivatives

This invention relates to new oxazaphosphorin-4-thio-alkanesulphonic acids and to the neutral salts thereof corresponding to the general formula I ##STR1## and to methods to use such compounds to control cancer diseases and to produce immunosuppression in humans and animals.

Oxazaphosphorin-4-thio-alkanesulphonic acids, and neutral salts thereof

The present invention relates to new 4-carbamoyloxy-oxazaphosphorins of the general Formula I ##STR1## as well as to a method for the treatment of malign tumor diseases in humans using such compounds as active agent.

4-carbamoyloxy-oxazaphosphorins

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Bielefeld, Germany

Ulf Niemeyer