Claims
- 1. A method of stimulating the β3 receptor which comprises administering to a patient in need thereof a compound of Formula I:
- 2. The method of claim 1 wherein R1 is
- 3. The method of claim 2 wherein R7 is hydrogen and R3 is hydrogen.
- 4. The method of claim 3 wherein X3 is O or a bond.
- 5. The method of claim 4 wherein R5 and R6 are methyl, X2 is methylene or ethylene, and X3 is a bond.
- 6. The method of claim 5 wherein.R4 is
- 7. The method of claim 6 wherein R4 is
- 8. The method of claim 7 wherein R10 is phenyl or pyridyl said phenyl or pyridyl being substituted with CN, hydroxy, CON11R12, CO2R2, SO2R2, or SO2NR11R12.
- 9. The method of claim 8 wherein the compound is:
- 10. The method of claim 9 wherein the compound is
- 11. A method of treating obesity which comprises administering to a patient in need thereof a compound of Formula I:
- 12. The method of claim 11 wherein R1 is
- 13. The method of claim 12 wherein R7 is hydrogen and R3 is hydrogen.
- 14. The method of claim 13 wherein X3 is O or a bond.
- 15. The method of claim 14 wherein R5 and R6 are methyl, X2 is methylene or ethylene, and X3 is a bond.
- 16. The method of claim 15 wherein R4 is
- 17. The method of claim 16 wherein R4 is
- 18. The method of claim 17 wherein R10 is phenyl or pyridyl said phenyl or pyridyl being substituted with CN, hydroxy, CONR11R2, CO2R2, SO2R2, or SO2NR11R12.
- 19. The method of claim 18 wherein the compound is:
- 20. The method of claim 19 wherein the compound is
- 21. A method of treating Type II diabetes which comprises administering to a patient in need thereof a compound of Formula I:
- 21. The method of claim 20 wherein R1 is
- 23. The method of claim 22 wherein R7 is hydrogen and R3 is hydrogen.
- 24. The method of claim 23 wherein X3 is O or a bond.
- 25. The method of claim 24 wherein R5 and R6 are methyl, X2 is methylene or ethylene, and X3 is a bond.
- 26. The method of claim 25 wherein R4 is
- 27. The method of claim 26 wherein R4 is
- 28. The method of claim 27 wherein R10 is phenyl or pyridyl said phenyl or pyridyl being substituted with CN, hydroxy, CONR11R12, CO2R2, SO2R2, or SO2NR11R12.
- 29. The method of claim 28 wherein the compound is:
- 30. The method of claim 29 wherein the compound is
- 31. A compound of the Formula II
- 32. A compound of claim 31 wherein R5 and R6 are methyl or ethyl.
- 33. A compound of claim 32 wherein R1 is
- 34. A compound of claim 33 wherein X2 is methylene or ethylene.
- 35. A compound of claim 34 wherein R4 is
- 36. A compound of claim 35 wherein R4 is
- 37. A compound of claim 36 wherein R10 is phenyl or pyridyl said phenyl or pyridyl being substituted with CN, CONR11R12, CO2R2, SO2R2, or SO2NR11R12.
- 38. A compound of claim 37 which is:
- 39. The compound of claim 38 of the formula
- 39. A pharmaceutical formulation comprising as an active ingredient a compound of claim 31, associated with one or more pharmaceutically acceptable carriers, excipients or diluents.
- 40. A pharmaceutical formulation comprising as an active ingredient a compound of claim 32, associated with one or more pharmaceutically acceptable carriers, excipients or diluents.
- 41. A pharmaceutical formulation comprising as an active ingredient a compound of claim 33, associated with one or more pharmaceutically acceptable carriers, excipients or diluents.
- 42. A pharmaceutical formulation comprising as an active ingredient a compound of claim 34, associated with one or more pharmaceutically acceptable carriers, excipients or diluents.
- 43. A pharmaceutical formulation comprising as an active ingredient a compound of claim 35, associated with one or more pharmaceutically acceptable carriers, excipients or diluents.
- 44. A pharmaceutical formulation comprising as an active ingredient a compound of claim 36, associated with one or more pharmaceutically acceptable carriers, excipients or diluents.
- 45. A pharmaceutical formulation comprising as an active ingredient a compound of claim 38, associated with one or more pharmaceutically acceptable carriers, excipients or diluents.
- 46. A pharmaceutical formulation comprising as an active ingredient a compound of claim 39, associated with one or more pharmaceutically acceptable carriers, excipients or diluents.
- 47. A process of preparing a compound of claim 31 of the formula III:
- 48. The process of claim 47 wherein in step 1 the hydrolysis is of a compound of the formula
- 49. A process of preparing a compound of claim 31, which comprises:
in step 1, reacting an epoxide of the formula XI: 281with an amine of formula B: 282and optionally in step 2, reacting the product of step 1 with an acid to form an acid addition salt.
- 50. A process of claim 48, wherein the amine is of the formula:
- 51. The process of claim 50 wherein;
A3 is N; and R14 is COOR2, CONR11R12, CONH(C1-C4 alkoxy), or cyano.
Parent Case Info
[0001] This application claims the benefit of U.S. Provisional Application 60/025,818 filed Sep. 5, 1996 and U.S. Provisional Application 60/029,228 filed Oct. 30, 1996.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60025818 |
Sep 1996 |
US |
|
60029228 |
Oct 1996 |
US |
Divisions (1)
|
Number |
Date |
Country |
Parent |
09068192 |
May 1998 |
US |
Child |
09610096 |
Jun 2000 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
09610096 |
Jun 2000 |
US |
Child |
10120302 |
Apr 2002 |
US |