Granted Patent B2

US 8,884,000 · App. 12/932,051 · Granted Nov 11, 2014

Inventors: Vern L. Schramm (New Rochelle, NY); Gary Brian Evans (Lower Hutt, NZ); Peter Charles Tyler (Wellington, NZ); Jennifer Mary Mason (Petone, NZ)

Assignees: Albert Einstein College of Medicine of Yeshiva University; Industrial Research Limited

Abstract

Claims (38)

1. A transition state inhibitor of saporin-L1 selected from the group consisting of:

an inhibitor having the structure:

wherein each R is independently OCH 3 or aryl or alkyl, where the aryl or alkyl can be optionally substituted with one or more of OH, ═O, OCH 3 , NH 2 , C1-C6 alkyl or halogen;

or a pharmaceutically acceptable salt thereof;

an inhibitor having the structure:

or a pharmaceutically acceptable salt thereof;

an inhibitor having the structure:

or a pharmaceutically acceptable salt thereof;

an inhibitor having the structure:

or a pharmaceutically acceptable salt thereof;

an inhibitor having the structure:

or a pharmaceutically acceptable salt thereof;

an inhibitor having the structure:

or a pharmaceutically acceptable salt thereof; and

an inhibitor having the structure:

or a pharmaceutically acceptable salt thereof.

2. The inhibitor of claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

3. The inhibitor of claim 1 , wherein R at one or more positions is OCH 3 .

4. The inhibitor of claim 1 , wherein R at one or more positions is aryl.

5. The inhibitor of claim 1 , wherein R at one or more positions is alkyl.

6. The inhibitor of claim 1 , wherein aryl is phenyl or phenyl substituted with one or more of —CH 3 , —OH, —OCH 3 , —F, —Cl, —Br, or —I.

7. The inhibitor of claim 1 , wherein alkyl is C1-C6.

8. The inhibitor of claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

9. The inhibitor of claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

10. The inhibitor of claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

11. The inhibitor of claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

12. The inhibitor of claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

13. The inhibitor of claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

14. A pharmaceutical composition comprising the inhibitor of claim 1 and a pharmaceutically acceptable carrier.

15. A method for inhibiting the activity of saporin-L1 comprising contacting saporin -L1 with the inhibitor of claim 1 .

16. The method of claim 15 carried out at a pH of 7.3-7.5.

Assignments (9)

Continuity (2)