Immunosuppressive analogues and derivatives of succinylacetone

US5252603A · kind A · utility

Assignee

• Cetus Corporation · US

Inventors

• Danute E. Nitecki · Berkeley, US
• Lois Aldwin · San Mateo, US
• Corey Levenson · Oakland, US
• Margaret Moreland · Berkeley, US
• Irwin Braude · Seattle, US
• David F. Mark · Plainsboro, US
• Henry Rapoport · Berkeley, US

Key dates

• Filing date: Dec 6, 1990
• Grant date: Oct 12, 1993
• Expiry date: Dec 6, 2010

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K31/41
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## wherein n=1-6 PA1 R=CH.sub.3, CF.sub.3, --CO.sub.2 R.sup.IV, ##STR2## R.sup.I, R.sup.II =H, F, CH.sub.3, or ##STR3## R.sup.III =H, ##STR4## or tetrazolyl R.sup.IV =H, or alkyl and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.