Phototherapeutic monovinyl and divinyl ether-linked dimers

• US 4,961,920 A
• Filed: 05/16/1989
• Issued: 10/09/1990
• Est. Priority Date: 12/08/1988
• Status: Expired due to Fees

• Current Assignee: Luminis Pty Limited
• Original Assignee: Luminis Pty Limited
• Inventors: Ward, A. David
• Primary Examiner(s): Shah, Mukund J.
• Assistant Examiner(s): WARD, EDWARD C
• Application Number:
  US07/352,793
• Time in Patent Office: 511 Days
• Field of Search: 540/145, 514/12, 514/183, 530/387, 530/388, 530/389, 530/391, 424/9
• US Class Current: 424/9.61
• CPC Class Codes: C07D 519/00 Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

Pure dimer compounds prepared and shown to be effective photosensitizing agents are of the formula ##STR1## wherein one R is vinyl and the other R is hydroxyethyl or vinyl and the pharmaceutically acceptable esters and salts thereof in isolated form.

Claims

1. A compound of the formula ##STR3## wherein one R is vinyl and the other R is 1-hydroxyethyl or vinyl and the pharmaceutically acceptable esters and salts thereof, in isolated form.

2. The compound of claim 1 wherein the ester is a methyl or ethyl ester.

3. The compound of claim 1 wherein one R is vinyl and the other R is 1-hydroxyethyl.

4. The compound of claim 1 wherein both R are vivyl.

6. A method to detect or photosensitize a target biological substrate which comprises contacting said target with an effective amount of the compound of claim 1 or a pharmaceutical composition thereof and irradiating said target with light absorbed by said compound.

7. A conjugate which consists essentially of the compound of claim 1 covalently bound to an immunoglobulin or immunologically reactive fragment thereof or a receptor ligand.

8. A pharmaceutical composition useful for labeling malignant tissue which comprises the compound of claim 1 associated with label.

9. A pharmaceutical composition which consists essentially of the conjugate of claim 7 as active ingredient, along with a pharmaceutically acceptable excipient.

5. A pharmaceutical composition which consists essentially of the compound of formula 1 as active ingredient along with a pharmaceutically acceptable excipient.