Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors

• US 9,802,944 B2
• Filed: 09/21/2016
• Issued: 10/31/2017
• Est. Priority Date: 03/26/2014
• Status: Active Grant

• Current Assignee: Hoffmann-La Roche Incorporated (Roche Holding AG)
• Original Assignee: Hoffmann-La Roche Incorporated (Roche Holding AG)
• Inventors: Di Giorgio, Patrick, Hert, Jerome, Hunziker, Daniel, Kuehne, Holger, Mattei, Patrizio, Rudolph, Markus
• Primary Examiner(s): Katakam, Sudhakar
• Application Number:
  US15/272,114
• Publication Number:
  US 20170008900A1
• Time in Patent Office: 405 Days
• CPC Class Codes: A61P 1/16 for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: C07D 487/04 Ortho-condensed systems
• CPC Class Codes: C07D 519/00 Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

Compounds of formula (I)

wherein R¹, R², A, W, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.

Claims

1. A compound of formula (I)

2. The compound of claim 1, wherein m, n, p and q are 1;

or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1, wherein m and n are 1 and p and q are 2;

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 1, wherein m and n are 2 and p and q are 1;

or a pharmaceutically acceptable salt thereof.

5. The compound of claim 1, wherein R² is:

6. The compound of claim 1, wherein R² is:

7. The compound of claim 1, wherein R² is:

8. The compound of claim 1, wherein R² is:

9. The compound of claim 1, wherein R² is:

10. The compound of claim 1, wherein R² is:

11. The compound of claim 1, wherein R² is:

12. The compound of claim 1, wherein R⁴ is cyclopropyl;

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 1, wherein the compound is selected from:

14. The compound of claim 13, wherein the compound is selected from:

15. The compound of claim 14, wherein the compound is selected from:

16. The compound of claim 15, wherein the compound is selected from:

23. A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

17. The compound

18. The compound

19. The compound

20. The compound

21. The compound

22. The compound