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Last Updated: December 31, 2025

Claims for Patent: 9,802,954


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Summary for Patent: 9,802,954
Title:Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma
Abstract:Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein:
Inventor(s):Pascale A. J. Pouzet, Peter Nickolaus, Ulrike Werthmann, Rogelio P. Frutos, Bing-Shiou Yang, Soojin Kim, Jason Alan Mulder, Nitinchandra D. Patel, Chris Hugh Senanayake, Thomas Gabriel Tampone, Xudong Wei
Assignee: Boehringer Ingelheim International GmbH
Application Number:US13/963,513
Patent Claims: 1. A method of treating COPD, asthma or idiopathic pulmonary fibrosis comprising the step of administering to a patient in need thereof an effective amount of a compound of formula I wherein: Ring A is a 6-membered aromatic ring optionally comprising one or two nitrogen atoms, R is Cl and is located in the para-, meta-, or ortho-position of Ring A, and S* is a sulphur atom that represents a chiral center, or of a pharmaceutically acceptable salt thereof.

2. The method of claim 1, wherein R is Cl and is located in the para-position of Ring A.

3. The method of claim 1, wherein Ring A is phenyl, pyridinyl, or pyrimidinyl.

4. The method of claim 1, wherein the compound of formula I is

5. The method of claim 1, wherein the compound of formula I is

6. The method of claim 1, wherein S* is in the R-configuration.

7. The method of claim 2, wherein S* is in the R-configuration.

8. The method of claim 4, wherein S* is in the R-configuration.

9. The method of claim 5, wherein S* is in the R-configuration.

10. The method of claim 1, wherein S* is in the S-configuration.

11. The method of claim 2, wherein S* is in the S-configuration.

12. The method of claim 4, wherein S* is in the S-configuration.

13. The method of claim 5, wherein S* is in the S-configuration.

14. The method of claim 5, wherein the compound of formula I shows a reflex peak in the X-ray powder diffraction diagram with a d-value of 4.62 Å.

15. The method of claim 5, wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å, 6.82 Å, and 10.09 Å.

16. The method of claim 5, wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å, 4.17 Å, and 3.66 Å.

17. The method of claim 5, wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å, 6.82 Å, 10.09 Å, 3.93 Å, and 4.94 Å.

18. The method of claim 5, wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å, 4.17 Å, 3.66 Å, 3.73 Å, and 18.47 Å.

19. The method of claim 5, wherein the compound of formula I shows a reflex peak in the X-ray powder diffraction diagram with a d-value of 4.12 Å.

20. The method of claim 5, wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.12 Å, 4.29 Å, and 5.15 Å.

21. The method of claim 5, wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.12 Å, 4.29 Å, 5.15 Å, 3.95 Å, and 3.36 Å.

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