IP Library Granted Patent US 7,381,735
Granted Patent B2
US 7,381,735 · App. 11/257,323 · Granted Jun 3, 2008

Ultrashort-acting opioids for transdermal application

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 7,381,735
App. No.
11/257,323
Granted
Jun 3, 2008
Kind
B2
Abstract

The subject invention concerns analogs of fentanyl opioids. The subject invention also concerns methods for synthesizing the compounds of the invention. The invention also concerns methods for treating pain in a patient by administering a compound of the invention to a person in need of such treatment.

Claims (40)

1. An compound having a structure selected from the group consisting of:

wherein,

X is

Y is H,

Z is H,

R is alkyl or aryl;

R′ is alkyl, aryl, alkyloxy, or aryloxy;

R 1 and R 2 are, independently, H or CH 3 ;

and R 3 is alkyl.

2. The compound according to claim 1 , wherein R is methyl, ethyl, ter-butyl, or phenyl, R 3 is methyl, ethyl, isopropyl, or ter-butyl, and R′ is methyl, ethyl, ter-butyl, phenyl, or methoxy.

3. The compound according to claim 1 , wherein R 2 is H, Y is H, and Z is —C(O)—CH 2 CH 3 .

4. The compound according to claim 1 , wherein R 2 is H, Y is —C(O)—OCH 3, and Z is —C(O)—CH 2 CH 3 .

5. The compound according to claim 1 , wherein R 2 is H, Y is —C(O)—OH, and Z is —C(O)—CH 2 CH 3 .

6. The compound according to claim 1 , wherein R 2 is H, Y is —CH 2 —OCH 3, and Z is —C(O)—CH 2 CH 3 .

7. The compound according to claim 1 , wherein R 2 is H, Y is H, and Z is —C(O)—OCH 3 .

8. The compound according to claim 1 , wherein R 2 is H, Y is —C(O)—OCH 3, and Z is —C(O)—OCH 3 .

9. The compound according to claim 1 , wherein R 2 is H, Y is —C(O)—OH, and Z is —C(O)—OCH 3 .

10. The compound according to claim 1 , wherein R 2 is H, Y is —CH 2 —OCH 3, and Z is —C(O)—OCH 3 .

11. The compound according to claim 1 that has the structure

12. A composition comprising an opioid compound according to claim 1 and a carrier or diluent.

13. A composition comprising a compound according to claim 3 and a carrier or diluent.

14. A composition comprising a compound according to claim 4 and a carrier or diluent.

15. A composition comprising a compound according to claim 5 and a carrier or diluent.

16. A composition comprising a compound according to claim 6 and a carrier or diluent.

17. A composition comprising a compound according to claim 7 and a carrier or diluent.

18. A composition comprising a compound according to claim 8 and a carrier or diluent.

19. A composition comprising a compound according to claim 9 and a carrier or diluent.

20. A composition comprising a compound according to claim 10 and a carrier or diluent.

21. A composition comprising a compound according to claim 11 and a carrier or diluent.

22. A method for treating pain wherein said method comprises administering to a patient in need of such a treatment an effective amount of a compound according to claim 1 optionally combined with a carrier or diluent.

23. A method for treating pain wherein said method comprises administering to a patient in need of such a treatment an effective amount of a compound according to claim 3 optionally combined with a carrier or diluent.

24. A method for treating pain wherein said method comprises administering to a patient in need of such a treatment an effective amount of a compound according to claim 4 optionally combined with a carrier or diluent.

25. A method for treating pain wherein said method comprises administering to a patient in need of such a treatment an effective amount of a compound according to claim 5 optionally combined with a carrier or diluent.

26. A method for treating pain wherein said method comprises administering to a patient in need of such a treatment an effective amount of a compound according to claim 6 optionally combined with a carrier or diluent.

27. A method for treating pain wherein said method comprises administering to a patient in need of such a treatment an effective amount of a compound according to claim 7 optionally combined with a carrier or diluent.

28. A method for treating pain wherein said method comprises administering to a patient in need of such a treatment an effective amount of a compound according to claim 8 optionally combined with a carrier or diluent.

29. A method for treating pain wherein said method comprises administering to a patient in need of such a treatment an effective amount of a compound according to claim 9 optionally combined with a carrier or diluent.

30. A method for treating pain wherein said method comprises administering to a patient in need of such a treatment an effective amount of a compound according to claim 10 optionally combined with a carrier or diluent.

31. A method for treating pain wherein said method comprises administering to a patient in need of such a treatment an effective amount of a compound according to claim 11 optionally combined with a carrier or diluent.

32. The method according to claim 22 wherein the patient is a human.

Assignments (4)
SECURITY AGREEMENT Recorded Oct 18, 2010
From: ARYX THERAPEUTICS, INC.
To: AYER CAPITAL PARTNERS MASTER FUND, L.P.; MPM BIOVENTURES III, L.P.; MPM BIOVENTURES III-QP, L.P.; MPM BIOVENTURES III GMBH & CO. BETEILIGUNGS KG; MPM BIOVENTURES III PARALLEL FUND, L.P.; AYER CAPITAL PARTNERS KESTREL FUND, L.P.; MPM ASSET MANAGEMENT INVESTORS 2002 BVIII LLC
Reel/Frame 025150/0379 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 19, 2008
From: DRUZGALA, PASCAL
To: ARYX THERAPEUTICS
Reel/Frame 020967/0740 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 19, 2008
From: DRUZGALA, PASCAL
To: ARYX THERAPEUTICS, INC.
Reel/Frame 020967/0798 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 19, 2008
From: ARYX THERAPEUTICS
To: ARYX THERAPEUTICS, INC.
Reel/Frame 020968/0028 →