IP Library Granted Patent US 8,063,057
Granted Patent B2
US 8,063,057 · App. 12/750,278 · Granted Nov 22, 2011

Multicyclic amino acid derivatives and methods of their use

Assignee: Lexicon Pharmaceuticals, Inc.
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 8,063,057
App. No.
12/750,278
Granted
Nov 22, 2011
Kind
B2
Abstract

Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders:

Claims (29)

1. A compound of the formula:

or a pharmaceutically acceptable salt thereof, wherein:

A is optionally substituted biphenyl;

R 1 is hydrogen or optionally substituted alkyl; and

R 2 is hydrogen or optionally substituted alkyl.

2. The compound of claim 1 , which is of the formula:

3. The compound of claim 1 , wherein A is substituted with one or more alkyl, halogenated alkyl, heteroalkyl, or halo moieties.

4. The compound of claim 1 , wherein R 1 is hydrogen.

5. The compound of claim 1 , wherein R 2 is hydrogen.

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

7. A pharmaceutical formulation comprising the compound of claim 1 and an excipient.

8. A solid dosage form suitable for oral administration to a patient comprising the compound of claim 1 .

9. A liquid dosage form suitable for oral administration to a patient comprising the compound of claim 1 .

10. A compound of the formula:

or a pharmaceutically acceptable salt thereof.

11. A pharmaceutical formulation comprising the compound of claim 10 and an excipient.

12. A solid dosage form suitable for oral administration to a patient comprising the compound of claim 10 .

13. A liquid dosage form suitable for oral administration to a patient comprising the compound of claim 10 .

14. A method of treating irritable bowel syndrome, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of the formula:

or a pharmaceutically acceptable salt thereof, wherein:

A is optionally substituted biphenyl;

R 1 is hydrogen or optionally substituted alkyl; and

R 2 is hydrogen or optionally substituted alkyl.

15. The method of claim 14 , wherein the compound is of the formula:

16. The method of claim 14 , wherein A is substituted with one or more alkyl, halogenated alkyl, heteroalkyl, or halo moieties.

17. The method of claim 14 , wherein R 1 is hydrogen.

18. The method of claim 14 , wherein R 2 is hydrogen.

19. The method of claim 14 , wherein R 2 is ethyl.

20. The method of claim 14 , wherein the compound is of the formula:

Assignments (11)
RELEASE OF INTELLECTUAL PROPERTY SECURITY AGREEMENTS AT R/F 41939/0487, 46591/0544 AND 53940/0001 Recorded Apr 15, 2026
From: MIDCAP FINANCIAL TRUST
To: TERSERA THERAPEUTICS LLC,
Reel/Frame 075420/0453 →
RELEASE OF INTELLECTUAL PROPERTY SECURITY AGREEMENT RECORDED AT R/F 63227/0852 Recorded Jan 7, 2025
From: NEWSTONE CAPITAL PARTNERS, LLC
To: TERSERA THERAPEUTICS LLC
Reel/Frame 069835/0704 →
SECURITY INTEREST Recorded Apr 5, 2023
From: TERSERA THERAPEUTICS LLC
To: NEWSTONE CAPITAL PARTNERS, LLC
Reel/Frame 063227/0852 →
RELEASE OF SECURITY INTEREST Recorded Apr 4, 2023
From: MIDCAP FINANCIAL TRUST, AS AGENT
To: TERSERA THERAPEUTICS LLC
Reel/Frame 063253/0942 →
RELEASE OF SECURITY INTEREST Recorded Apr 4, 2023
From: NEWSTONE CAPITAL PARTNERS, LLC
To: TERSERA THERAPEUTICS LLC; JDP THERAPEUTICS LLC
Reel/Frame 063221/0546 →
SECURITY INTEREST Recorded Apr 4, 2023
From: TERSERA THERAPEUTICS LLC
To: ANTARES CAPITAL LP, AS AGENT
Reel/Frame 063215/0724 →
SECURITY INTEREST Recorded Sep 30, 2020
From: TERSERA THERAPEUTICS LLC
To: MIDCAP FINANCIAL TRUST, AS AGENT
Reel/Frame 053940/0001 →
RELEASE OF SECURITY INTEREST Recorded Sep 14, 2020
From: BIOPHARMA CREDIT PLC
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 053767/0445 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 14, 2020
From: LEXICON PHARMACEUTICALS, INC.
To: TERSERA THERAPEUTICS LLC
Reel/Frame 053763/0754 →
SECURITY INTEREST Recorded Sep 9, 2020
From: TERSERA THERAPEUTICS LLC
To: NEWSTONE CAPITAL PARTNERS, LLC
Reel/Frame 053721/0037 →
SECURITY INTEREST Recorded Dec 20, 2017
From: LEXICON PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 044958/0377 →
Continuity (3)
Continuation 11638677 · Dec 12, 2006
Provisional Application 60754955 · Dec 29, 2005
Related Publication 20100280054A1 · Nov 4, 2010