Pyrazolyl guanidine F

1. A method of treating ulcerative colitis in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula I to treat the ulcerative colitis:

including all stereoisomers, geometric isomers, and tautomers; or a pharmaceutically acceptable salt or solvate of any of the foregoing; wherein:

A 1 is phenylene;

A 2 is

R 1 represents independently for each occurrence halogen, haloalkyl, alkyl, cycloalkyl, heterocycloalkyl, hydroxyl, C 1 -C 6 alkoxy, cyano, —CO 2 R 8 , —C(O)R 9 , —S(O)R 9 , —SO 2 R 9 , —SO 2 N(R 10 )(R 11 ), —C(O)N(R 10 )(R 11 ), —N(R 10 )(R 11 ), or —N(R 8 )C(O)(R 9 );

R 2 is hydrogen or alkyl;

R 3 is aryl, aralkyl, cycloalkyl, —(C(R 8 ) 2 ) m -cycloalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, —(C(R 8 ) 2 ) m -heterocycloalkyl, alkyl, haloalkyl, hydroxyalkyl, —(C(R 8 ) 2 ) m -alkoxyl, —(C(R 8 ) 2 ) m —O—(C(R 8 ) 2 ) m -alkoxyl, or —(C(R 8 ) 2 ) m —CN, wherein said aryl, aralkyl, cycloalkyl, heteroaryl, heteroaralkyl, and heterocycloalkyl are each optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, cycloalkyl, hydroxyalkyl, C 1 -C 6 alkoxy, cyano, and —C 1 -C 6 alkylene-CO 2 R 8 ;

R 4 is hydrogen or alkyl;

R 5 is hydrogen or alkyl;

R 6 is alkyl, cycloalkyl, haloalkyl, cyano, aryl, aralkyl, heteroaryl, heteroaralkyl, —CO 2 R 8 , or —C(O)N(R 10 )(R 11 ), wherein said cycloalkyl, aryl, aralkyl, heteroaryl, and heteroaralkyl are each optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, hydroxyalkyl, C 1 -C 6 alkoxy, —O-aralkyl, and cyano;

R 7 is hydrogen, halogen, alkyl, or haloalkyl;

R 8 represents independently for each occurrence hydrogen, alkyl, or cycloalkyl; or two occurrences of R 8 attached to the same carbon atom are taken together with said carbon atom to form a saturated carbocylic ring;

R 9 represents independently for each occurrence alkyl or cycloalkyl;

R 10 and R 11 each represent independently for each occurrence hydrogen, alkyl, or cycloalkyl; or R 10 and R 11 are taken together with the nitrogen atom to which they are attached to form a 3 to 7 membered heterocyclic ring optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, cycloalkyl, and C 1 -C 6 alkoxy;

n is 1, 2, or 3; and

m is 1, 2, 3, 4, or 5.

2. The method of claim 1 , wherein the compound is a compound of Formula I or a stereoisomer, geometric isomer, or tautomer; or a pharmaceutically acceptable salt of any of the foregoing.

3. The method of claim 1 , wherein A 2 is

4. The method of claim 2 , wherein A 2 is

5. The method of claim 3 , wherein R 1 represents independently for each occurrence halogen or haloalkyl.

6. The method of claim 4 , wherein R 1 represents independently for each occurrence halogen or haloalkyl.

7. The method of claim 3 , wherein R 1 is chloro, fluoro, or trifluoromethyl.

8. The method of claim 4 , wherein R 1 is chloro, fluoro, or trifluoromethyl.

9. The method of claim 7 , wherein R 3 is aryl or aralkyl, each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, alkyl, and cycloalkyl.

10. The method of claim 8 , wherein R 3 is aryl or aralkyl, each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, alkyl, and cycloalkyl.

11. The method of claim 8 , wherein R 3 is phenyl substituted with 1 or 2 substituents independently selected from the group consisting of chloro, fluoro, and trifluoromethyl.

12. The method of claim 11 , wherein R 5 is hydrogen.

13. The method of claim 9 , wherein R 6 is haloalkyl.

14. The method of claim 12 , wherein R 6 is haloalkyl.

15. The method of claim 12 , wherein R 6 is trifluoromethyl.

16. The method of claim 13 , wherein R 7 is hydrogen.

17. The method of claim 15 , wherein R 7 is hydrogen.

18. The method of claim 17 , wherein n is 1 or 2.

19. The method of claim 16 , wherein the compound is administered orally to the patient.

20. The method of claim 18 , wherein the compound is administered orally to the patient.

21. A method of treating ulcerative colitis in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula I-A1 to treat the ulcerative colitis:

including all stereoisomers, geometric isomers, and tautomers; or a pharmaceutically acceptable salt or solvate of any of the foregoing; wherein:

R 1 and R 2 each represent independently for each occurrence hydrogen, chloro, fluoro, or —CF 3 ;

R 3 is alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, or C 1 -C 6 alkylene-C 1 -C 6 alkoxy, wherein said cycloalkyl, aryl, aralkyl, heteroaryl, and heteroaralkyl are each optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, C 1 -C 6 alkoxy, and cyano; and

R 4 is alkyl, cycloalkyl, haloalkyl, cyano, aryl, aralkyl, heteroaryl, or heteroaralkyl, wherein said cycloalkyl, aryl, aralkyl, heteroaryl, and heteroaralkyl are each optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, C 1 -C 6 alkoxy, and cyano.

22. The method of claim 21 , wherein the compound is a compound of Formula I-A1 or a stereoisomer, geometric isomer, or tautomer; or a pharmaceutically acceptable salt of any of the foregoing.

23. The method of claim 22 , wherein R 3 is phenyl substituted with 1 or 2 substituents independently selected from the group consisting of chloro, fluoro, and trifluoromethyl.

24. The method of claim 22 , wherein R 4 is trifluoromethyl.

25. The method of claim 24 , wherein the compound is administered orally to the patient.