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Details for Patent: 3,941,790

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Details for Patent: 3,941,790

Title: Bis diketopiperazines
Abstract:A pharmaceutical composition useful for aiding regression and palliation of cancer in mammals comprises a therapeutically effective amount of a compound of formula ##EQU1## wherein R.sub.1 and R.sub.2 are each separately selected from hydrogen and methyl or together represent an ethylene bridging group, with the proviso that when both of the groups R.sub.1 and R.sub.2 are methyl they are disposed in the meso configuration, or a non-toxic salt thereof with a physiologically acceptable inorganic or organic acid, in combination with a physiologically acceptable diluent or carrier.
Inventor(s): Creighton; Andrew Malcolm (London, EN)
Assignee: National Research Development Corporation (EN)
Filing Date:Feb 21, 1974
Application Number:05/444,485
Claims:1. A bis(3,5-dioxopiperazin-1-yl) alkane selected from the group consisting of:

1,2-bis(3,5-dioxopiperazin-1-yl) propane,

meso-2,3-bis(3,5-dioxopiperazin-1-yl) butane,

1,2-bis(3,5-dioxopiperazin-1-yl) cyclobutane,

and acid addition salts thereof with a physiologically acceptable inorganic or organic acid.

2. The bis(3,5-dioxopiperazin-1-yl) alkane of claim 1 which is dl-1,2-bis(3,5-dioxopiperazin-1-yl) propane or an acid addition salt thereof with a physiologically acceptable inorganic or organic acid.

3. The bis(3,5-dioxopiperazin-1-yl) alkane of claim 1 which consists essentially of d-1,2-bis(3,5-dioxopiperazin-1-yl) propane, or an acid addition salt thereof with a physiologically acceptable inorganic or organic acid.

4. The bis(3,5-dioxopiperazin-1-yl) alkane of claim 1 which consists essentially of l-1,2-bis(3,5-dioxopiperazin-1-yl) propane, or an acid addition salt thereof with a physiologically acceptable inorganic or organic acid.

5. The bis(3,5-dioxopiperazin-1-yl) alkane of claim 1 which is meso-2,3-bis(3,5-dioxopiperazin-1-yl) butane, or an acid addition salt thereof with a physiologically acceptable inorganic or organic acid.

6. A bis(3,5-dioxopiperazin-1-yl) alkane acid addition salt of claim 1 which is the hydrochloric, isethionic, tartaric or methane sulphonic acid salt.

7. A process for the preparation of a bis(3,5-dioxopiperazin-1-yl) alkane of claim 1 which comprises heating a compound selected from N,N,N',N' -tetracarboxamidomethyl-1,2-diamino propane, meso-N,N,N',N'-tetracarboxamidomethyl-2,3-diaminobutane and N,N,N',N'-tetracarboxamidomethyl-1,2-diaminocyclobutane with polyphosphoric acid as reagent.
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