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Claims for Patent: 4,628,098

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Claims for Patent: 4,628,098

Title: 2-[2-pyridylmethylthio-(sulfinyl)]benzimidazoles
Abstract:The compound of the formula ##STR1## wherein R.sup.1 is hydrogen, methoxy or trifluoromethyl, R.sup.2 and R.sup.3 are independently hydrogen or methyl, R.sup.4 is a C.sub.2-5 fluorinated alkyl and n denotes 0 or 1, or a pharmacologically acceptable salt thereof is novel, and useful for prophylaxis and therapy of digestive ulcers (e.g. gastric ulcer, duodenal ulcer) and gastritis.
Inventor(s): Nohara; Akira (Kyoto, JP), Maki; Yoshitaka (Kyoto, JP)
Assignee: Takeda Chemical Industries, Ltd. (Osaka, JP)
Application Number:06/760,568
Patent Claims: 1. A compound of the formula ##STR8## wherein R.sup.1 is hydrogen, methoxy or trifluoromethyl, R.sup.2 and R.sup.3 are independently hydrogen or methyl, R.sup.4 is a C.sub.2-5 fluorinated alkyl and n denotes 0 or 1, and a pharmacologically acceptable salt thereof.

2. A compound according to claim 1, wherein R.sup.1 is hydrogen.

3. A compound according to claim 1, wherein R.sup.1 is methoxy.

4. A compound according to claim 1, wherein R.sup.2 is hydrogen.

5. A compound according to claim 1, wherein R.sup.2 is methyl.

6. A compound according to claim 1, wherein R.sup.3 is hydrogen.

7. A compound according to claim 1, wherein R.sup.3 is methyl.

8. A compound according to claim 1, wherein R.sup.4 is a C.sub.2-3 fluorinated alkyl.

9. A compound according to claim 1, wherein the compound is 2-[4-(2,2,2-trifluoroethoxy)-pyrid-2-yl]methylsulfinylbenzimidazole.

10. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,2-trifluoroethoxy)-pyrid-2-yl]methylsulfinylbenzimidazo le.

11. A compound according to claim 1, wherein the compound is 2-[4-(2,2,2-trifluoroethoxy)-5-methyl-pyrid-2-yl]methylsulfinylbenzimidazo le.

12. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,2-trifluoroethoxy)-5-methyl-pyrid-2-yl]methylsulfinylbe nzimidazole.

13. A compound according to claim 1, wherein the compound is 2-[4-(2,2,3,3,3-pentafluoropropoxy)-pyrid-2-yl]methylsulfinylbenzimidazole

14. A compound according to claim 1, wherein the compound is 2-[4-(2,2,3,3,3-pentafluoropropoxy)-5-methyl-pyrid-2-yl]methylsulfinylbenz imidazole.

15. A compound according to claim 1, wherein the compound is 2-[4-(2,2,3,3-tetrafluoropropoxy)-pyrid-2-yl]methylsulfinylbenzimidazole.

16. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,3,3,3-pentafluoropropoxy)-pyrid-2-yl]methylsulfinylbenz imidazole.

17. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,3,3-tetrafluoropropoxy)-pyrid-2-yl]methylsulfinylbenzim idazole.

18. A compound according to claim 1, wherein the compound is 2-[5-methyl-4-(2,2,3,3-tetrafluoropropoxy)-pyrid-2-yl]methylsulfinylbenzim idazole.

19. A compound according to claim 1, wherein the compound is 2-[3,5-dimethyl-4-(2,2,3,3,3-pentafluoropropoxy)-pyrid-2-yl]methylsulfinyl benzimidazole.

20. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,2-trifluoroethoxy)-pyrid-2-yl]methylsulfinyl-5-trifluor omethylbenzimidazole.

21. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,2-trifluoroethoxy)-pyrid-2-yl]methylsulfinyl-5-methoxyb enzimidazole.

22. A compound according to claim 1, wherein the compound is 2-[4-(2,2,2-trifluoroethoxy)-pyrid-2-yl]-methylsulfinyl-5-methoxybenzimida zole.

23. A compound according to claim 1, wherein the compound is 2-[4-(2,2,2-trifluoroethoxy)-pyrid-2-yl]-methylthiobenzimidazole.

24. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,2-trifluoroethoxy)-pyrid-2-yl]methylthiobenzimidazole.

25. A compound according to claim 1, wherein the compound is 2-[5-methyl-4-(2,2,2-trifluoroethoxy)-pyrid-2-yl]methylthiobenzimidazole.

26. A compound according to claim 1, wherein the compound is 2-[3,5-dimethyl-4-(2,2,2-trifluoroethoxy)-pyrid-2-yl]methylthiobenzimidazo le.

27. A compound according to claim 1, wherein the compound is 2-[4-(2,2,3,3,3-pentafluoropropoxy)-pyrid-2-yl]methylthiobenzimidazole.

28. A compound according to claim 1, wherein the compound is 2-[5-methyl-4-(2,2,3,3,3-pentafluoropropoxy)-pyrid-2-yl]methylthiobenzimid azole.

29. A compound according to claim 1, wherein the compound is 2-[4-(2,2,3,3-tetrafluoropropoxy)-pyrid-2-yl]methylthiobenzimidazole.

30. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,3,3-tetrafluoropropoxy)-pyrid-2-yl]methylthiobenzimidaz ole.

31. A compound according to claim 1, wherein the compound is 2-[5-methyl-4-(2,2,3,3-tetrafluoropropoxy)-pyrid-2-yl]methylthiobenzimidaz ole.

32. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,3,3,3-pentafluoropropoxy)-pyrid-2-yl]methylthiobenzimid azole.

33. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,3,3,3-pentafluoropropoxy)-5-methyl-pyrid-2-yl]methylthi obenzimidazole.

34. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,2-trifluoroethoxy)-pyrid-2-yl-methylthio-5-trifluoromet hylbenzimidazole.

35. A compound according to claim 1, wherein the compound is 2-[3-methyl-4-(2,2,2-trifluoroethoxy)-pyrid-2-yl-methylthio-5-methoxybenzi midazole.

36. A compound according to claim 1, wherein the compound is 2-[4-(2,2,2-trifluoroethoxy)-pyrid-2-yl]methylthio-5-methoxybenzimidazole.
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