Stable soluble 1,2-diaminocyclohexane platinum complexes

• US 4,680,308 A
• Filed: 12/26/1985
• Issued: 07/14/1987
• Est. Priority Date: 12/26/1985
• Status: Expired due to Fees

• Current Assignee: Andrulis Pharmaceuticals Corporation
• Original Assignee: Andrulis Research Corporation
• Inventors: McGrath, Kenneth J., Gill, Devinder S., Schwartz, Paul
• Primary Examiner(s): SNEED, HELEN
• Application Number:
  US06/813,451
• Time in Patent Office: 565 Days
• Field of Search: 556/137, 514/492
• US Class Current: 514/492
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07F 15/0093 without a metal-carbon linkage

Abstract

Platinum complexes of the formula ##STR1## wherein Z is --CO-- or a single bond and R is --COOH or --SO₃ H, and the pharmaceutically acceptable salts thereof with bases, are stable readily water-soluble pharmaceutically active compounds having antitumor, anti-inflammatory and trypanocidal activities.

Claims

1. A platinum complex of the formula ##STR5## wherein Z is --CO-- or a single bond and R is --COOH or --SO₃ H, or a pharmaceutically acceptable salt thereof.

2. A complex according to claim 1, wherein Pt is Pt(II).

3. A complex according to claim 1, wherein the cyclohexane ring is in the trans configuration.

4. A complex according to claim 1, wherein Z is a single bond.

5. A complex according to claim 1, wherein Z is --CO.

6. A complex according to claim 1, wherein R is --COOH.

7. A complex according to claim 1, wherein R is --SO₃ H.

8. 4-Carboxycatecholato(trans-1,2-diaminocyclohexane) -platinum(II), a complex according to claim 1.

9. 5-Sulfosalicylato(trans-1,2-diaminocyclohexane) -platinum(II), a complex according to claim 1.

10. 5-Carboxysalicylato(trans-1,2-diaminocyclohexane) -platinum(II), a complex according to claim 1.

11. 4-Sulfocatecholato(trans-1,2-diaminocyclohexane) -platinum(II), a complex according to claim 1.

12. A pharmaceutical composition comprising a concentration effective to achieve an antitumor effect against a tumor respsonsive to platinum complex antitumor therapy, of a complex according to claim 1 in sterile admixture with a pharmaceutically acceptable carrier adapted for systemic admistration.

13. An admixture according to claim 12, adapted for intravenous administration.

14. An admixture according to claim 12, wherein the vehicle is aqueous.

15. An admixture according to claim 12, wherein the complex is 5-sulfosalicylato(1,2-diaminocyclohexane)platinum (II).

16. An admixture according to claim 12, wherein the complex is 5-carboxysalicylato(1,2-diaminocyclohexane)platinum (II).