Thioether conjugates

US5606017A · kind A · utility

Assignee

• Bristol-Myers Squibb Company · US

Inventors

• David Willner · Town of DeWitt, US
• Pamela Trail · Farmington, US
• H. Dalton King · Yardley, US
• Sandra J. Hofstead · Middletown, US
• Robert S. Greenfield · Trumbull, US
• Gary R. Braslawsky · San Diego, US

Key dates

• Filing date: Jun 6, 1995
• Grant date: Feb 25, 1997
• Expiry date: Jun 6, 2015

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Provided are drug/ligand compounds of Formula (I): ##STR1## in which D is a drug moiety; PA1 n is an integer from 1 to 10; PA1 p is an integer from 1 to 6; PA1 Y is O or NH.sub.2.sup.+ Cl.sup.- ; PA1 z is 0 or 1; PA1 q is about 1 to about 10; PA1 X is a ligand; and, PA1 A is a Michael Addition Adduct. In a preferred embodiment, the ligand is an immunoglobulin, preferably a chimeric antibody or fragment thereof. Also provided are formulations comprising as an active ingredient a compound of Formula (I), intermediates useful for preparing the compounds of Formula (I), processes for preparing the compounds of Formula (I), and methods for using the compounds of the invention.