IP Library Granted Patent US 9,206,139
Granted Patent B2
US 9,206,139 · App. 14/422,018 · Granted Dec 8, 2015

Aggrecanase inhibitors

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Quick Facts
Patent No.
US 9,206,139
App. No.
14/422,018
Granted
Dec 8, 2015
Kind
B2
Abstract

The present invention provides compounds having the formula: wherein R 1 is selected from methyl, ethyl, propyl, cyclopropyl, and dimethyl, or a pharmaceutically acceptable salt thereof, along with methods and intermediates for their preparation, and uses thereof.

Claims (22)

1. A compound having the formula:

wherein R 1 is selected from methyl, ethyl, propyl, dimethyl, and cyclopropyl, or a pharmaceutically acceptable salt thereof.

2. The compound according to claim 1 having the formula:

or a pharmaceutically acceptable salt thereof.

3. The compound according to claim 1 having the formula:

or a pharmaceutically acceptable salt thereof.

4. The compound according to claim 3 having the formula:

or a pharmaceutically acceptable salt thereof.

5. The compound according to claim 1 having the formula:

or a pharmaceutically acceptable salt thereof.

6. A pharmaceutical composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and at least one of a pharmaceutically acceptable carrier, excipient, or diluent.

7. The pharmaceutical composition of claim 6 , wherein said pharmaceutical composition is adapted for oral administration.

8. A method of treating arthritis in a patient in need thereof, said method comprising administering an effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, to said patient.

9. The method of claim 8 , wherein said patient is administered at least one additional active agent.

10. The method of claim 8 , wherein said patient is a human.

11. The method of claim 8 , wherein said patient is a dog.

12. The method of claim 8 , wherein said administration is oral administration.

13. A method of inhibiting cartilage erosion in a patient in need thereof, said method comprising administering an effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, to said patient.

14. The method of claim 13 , wherein said patient is administered at least one additional active agent.

15. The method of claim 13 , wherein said patient is a human.

16. The method of claim 13 , wherein said patient is a dog.

17. The method of claim 13 , wherein said administration is oral administration.

Assignments (4)
ASSIGNMENT OF SECURITY INTEREST IN PATENT RIGHTS, RECORDED ON AUGUST 3, 2020, AT REEL/FRAME 053388/0967 Recorded Dec 3, 2025
From: GOLDMAN SACHS BANK USA, AS RETIRING COLLATERAL AGENT
To: JPMORGAN CHASE BANK, N.A., AS SUCCESSOR COLLATERAL AGENT
Reel/Frame 073816/0021 →
SECURITY INTEREST Recorded Aug 3, 2020
From: ELANCO US INC.
To: GOLDMAN SACHS BANK USA, AS COLLATERAL AGENT
Reel/Frame 053388/0967 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 23, 2018
From: ELI LILLY AND COMPANY
To: ELANCO US INC.
Reel/Frame 044702/0839 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 17, 2015
From: DURHAM, TIMOTHY BARRETT; MARIMUTHU, JOTHIRAJAH; WILEY, MICHAEL ROBERT
To: ELI LILLY AND COMPANY
Reel/Frame 034969/0875 →