Diastereomeric mono- and di-substituted diamino cyclohexane comp

Details Diastereomeric mono- and di-substituted diamino cyclohexane comp Diastereomeric mono- and di-substituted diamino cyclohexane comp

1986-07-07

1993-04-27

Shaver, Paul F.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heavy metal containing

556136, C07F 1500

Patent

active

052064000

ABSTRACT:
One aspect of the present invention relates to a process of making cyclohexane-1,2-di(O)-4,5-di(N) diastereomers which are useful as a synthons for various diastereoisomeric pharmaceutical systems. The present invention also relates to the stereoisomer compounds which are derived from retro-synthetic analysis. In another aspect, the present invention relates to novel antineoplastic Pt(II) complexes derived from the stereoisomers and the processes for making such Pt(II) complexes. Mono- and di-hydroxyl substitution on the cyclohexane ring renders the organoplatinum complex relatively more water soluble, thereby facilitating intravenous administration. The Pt(II) complexes of the present invention are less nephrotoxic than cisplatin and are readily excreted via the kidney due to their enhanced water solubility. In a composition aspect, the present invention encompasses novel pharmaceutical compositions comprising the novel Pt(II) complexes in an amount sufficient to have an antineoplastic effect in an animal or patient.

REFERENCES:
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patent: 4551524 (1985-11-01), Kidani et al.
patent: 4670458 (1987-06-01), Hlavka et al.
patent: 4786725 (1988-11-01), Amundsen et al.
Kuglov et al., Vestsi Akad. Navuk USSR, Ser Khim Vavuk, 1981, 5, 66-71.
Kresze, G. and Melzer, H., Justus Liebige, Ann. Chemie, 1874 (1981).

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