IP Library Granted Patent US 7,288,568
Granted Patent B2
US 7,288,568 · App. 10/395,372 · Granted Oct 30, 2007

Therapeutic compositions and methods of use

Assignee: Trustees of Dartmouth College
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Quick Facts
Patent No.
US 7,288,568
App. No.
10/395,372
Granted
Oct 30, 2007
Kind
B2
Abstract

Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.

Claims (28)

1. A pharmaceutically acceptable composition comprising a compound having the formula:

wherein either A or B is a double bond such that when A is a double bond, C 11 has substituted thereon ═X, and when B is a double bond, C 12 has substituted thereon ═X; R 1 may be substituted anywhere on the six-membered ring denoted by positions 1 through 10; wherein an R 2 group may be substituted anywhere on the structure represented in formula (I); and n is a number from 0 to 100; wherein ═X, R 1 , R 2 , and R 3 are selected from the group consisting of —OR′, alkyl, alkylamino, alkoxy, aryl, aralkyl, aryloxy, alkylthio, alkylcarboxyl, hydrogen, halo, amino, cyano, nitro, thiol and hydroxyl, wherein R′ is H or alkyl, alkylamino, alkoxy, aryl, aralkyl, aryloxy, alkylthio, alkylcarboxyl, said compound being dispersed in a liposome.

2. The composition of claim 1 , wherein R 1 is a cyano group.

3. The composition of claim 1 , wherein B is double bond, X is O, R 3 is —OH, and R 1 is a cyano group.

4. The composition of claim 1 , wherein said composition is selected from the group consisting of 3,11-dioxoolean-1,12-dien-28oic acid, 2-cyano-3,11-dioxoolean-1,12-dien-28oic acid and 2-cyano-3,12-dioxoolean-1,9-dien-28oic acid.

5. The compound of claim 1 , wherein R 1 is selected from the group consisting of cyano, halo, or OR′.

6. The compound of claim 1 , wherein R 1 is at position 2.

7. The compound of claim 1 , wherein the compound has the formula:

8. The compound of claim 7 , wherein R x is methyl.

9. A composition comprising a triterpenoid compound effective for inhibiting IFN-γ-induced NO production in macrophages, said compound having an IC 50 value of at least less than 0.6 μM, said compound being dispersed in a liposome.

10. A pharmaceutically acceptable composition comprising a compound having the formula:

wherein either A or B is a double bond such that when A is a double bond, C 11 has substituted thereon ═X, and when B is a double bond, C 12 has substituted thereon ═X; R 1 may be substituted anywhere on the six-membered ring denoted by positions 1 through 10; wherein an R 2 group may be substituted anywhere on the structure represented in formula (I), and n is a number from 0 to 100, wherein ═X, R 1 , R 2 , and, R 3 are selected from the group consisting of —OR′, alkyl, alkylamino, alkoxy, aryl, aralkyl, aryloxy, alkylthio, alkylcarboxyl, hydrogen, halo, amino, cyano, nitro, thiol and hydroxyl, wherein R′ is H or alkyl, alkylamino, alkoxy, aryl, aralkyl, aryloxy, alkylthio, alkylcarboxyl,

said compound being dispersed in an oil and water emulsion.

11. A composition comprising a triterpenoid compound effective for inhibiting IFN-γ-induced NO production in macrophages, said compound having an IC 50 value of at least less than 0.6 μM, said compound being dispersed in an oil and water emulsion.

12. A pharmaceutically acceptable composition comprising a compound having the formula:

wherein either A or B is a double bond such that when A is a double bond, C 11 has substituted thereon ═X, when B is a double bond, C 12 has substituted thereon ═X; R 1 may be substituted anywhere on the six-membered ring denoted by positions 1 through 10; wherein an R 2 group may be substituted anywhere on the structure represented in formula (I), and n is a number from 0 to 100; wherein ═X, R 1 , R 2 , and R 3 are selected from the group consisting of —OR′, alkyl, alkylamino, alkoxy, aryl, aralkyl, aryloxy, alkylthio, alkylcarboxyl, hydrogen, halo, amino, cyano, nitro, thiol and hydroxyl, wherein R is H or alkyl, alkylamino, alkoxy, aryl, aralkyl, aryloxy, alkylthio, alkylcarboxyl,

said composition being formulated for oral delivery in a pharmaceutically acceptable carrier.

13. The composition of claim 12 , wherein R 1 is a cyano group.

14. The composition of claim 12 , wherein B is double bond, X is O, R 3 is —OH, and R 1 is a cyano group.

15. The composition of claim 12 , wherein said composition is selected from the group consisting of 3,11-dioxoolean-1,12-dien-28oic acid, 2-cyano-3,11-dioxoolean-1,12-dien-28oic acid and 2-cyano-3,12-dioxoolean-1,9-dien-28oic acid.

16. The compound of claim 12 , wherein R 1 is selected from the group consisting of cyano, halo, or OR′.

17. The compound of claim 12 , wherein R 1 is at position 2.

18. The compound of claim 17 , wherein the compound has the formula:

19. The compound of claim 18 , wherein R x is methyl.

20. The compound of claim 17 , wherein the composition is formulated as a hard or soft capsule, a tablet, a syrup, a suspension, a wafer, or an elixir.

21. The compound of claim 17 , wherein said composition comprises a protective coating.

22. The compound of claim 17 , wherein said composition comprises an agent that delays absorption.

23. A composition comprising a triterpenoid compound effective for inhibiting IFN-γ-induced NO production in macrophages, said compound having an IC 50 value of at least less than 0.6 μM, said composition being formulated for oral delivery.

Assignments (2)
CONFIRMATORY LICENSE Recorded Nov 29, 2011
From: DARTMOUTH COLLEGE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 027290/0560 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 3, 2009
From: GRIBBLE, GORDON W.; HONDA, TADASHI; SPORN, MICHAEL B.; SUH, NANJOO
To: TRUSTEES OF DARTMOUTH COLLEGE
Reel/Frame 023462/0245 →
Continuity (4)
Continuation 0992708100 · Aug 9, 2001
Division 0933500300 · Jun 17, 1999
Provisional Application 6009005300 · Jun 19, 1998
Related Publication 20030236303A1 · Dec 25, 2003