Claims
- 1. A compound of formula (I):
- 2. A compound according to claim 1 wherein R2 and R3 are both hydrogen, and R1 is —C(═O)OR19.
- 3. A compound according to claim 2 wherein R19 is C1-6-alkyl.
- 4. A compound according to claim 1 wherein R3 is hydrogen, and R1 and R2, together with the nitrogen atom to which they are attached, form a ring
- 5. A compound according to claim 4 wherein R4 and R5 are independently selected from hydrogen, C1-6-alkyl, phenyl-C1-6-alkyl and oxo.
- 6. A compound according to claim 5 wherein R4 is hydrogen or Cl-alkyl, and R5 is hydrogen or oxo.
- 7. A compound according to claim 4 wherein R3 is hydrogen, and R1 and R2, together with the nitrogen atom to which they are attached, form a ring
- 8. A compound according to claim 1 wherein R2 and R3, together with A and the nitrogen atom and the carbon atom, respectively, to which they are attached, form a ring
- 9. A compound according to claim 8 wherein R2 and R3, together with A and the nitrogen atom and the carbon atom, respectively, to which they are attached, form a ring
- 10. A compound according to claim 8 or 9 wherein R1 is hydrogen, C1-6-alkyl, phenyl-C1-6-alkyl or —C(═O)OR10, wherein R10 is as defined in claim 1, and R13 and R14 are independently hydrogen, C1-6-alkyl, phenyl-C1-6-alkyl or oxo.
- 11. A compound according to claim 10 wherein R1 is hydrogen or —C(═O)O—C1-6-alkyl, and R13 and R14 are hydrogen.
- 12. A compound according to claim 1 wherein R1, R2 and R3 are hydrogen.
- 13. A compound according to claim 1 wherein A is C1-6-alkylene.
- 14. A compound according to claim 13 wherein A is methylene or ethylene.
- 15. A compound according to claim 14 wherein A is ethylene.
- 16. A compound according to claim 1 wherein B is —C(═O)—.
- 17. A compound according to claim 1 wherein D is C3-8-cycloalkyl, heteroaryl or aryl, which may optionally be substituted.
- 18. A compound according to claim 1 wherein D is C3-8-cycloalkyl, heteroaryl or aryl, which may optionally be substituted, but not in the positions adjacent to the point of attachment of D to B.
- 19. A compound according to claim 17 or 18 wherein D is cyclopropyl, thienyl or phenyl, which may optionally be substituted.
- 20. A compound according to claim 17 wherein D is cyclopropyl.
- 21. A compound according to claim 17 or 18 wherein D is thienyl, which is substituted with halogen.
- 22. A compound according to claim 17 or 18 wherein D is phenyl, which is optionally substituted with
hydroxy, halogen, heteroaryl-C1-6-alkoxy, aryl-C1-6-alkoxy, wherein the ring moieties are optionally substituted.
- 23. A compound according to claim 22 wherein D is phenyl which is optionally substituted with halogen or benzyloxy, wherein the ring moiety of benzyloxy is optionally substituted.
- 24. A compound according to claim 23 wherein D is phenyl, which is substituted with benzyloxy.
- 25. A pharmaceutical composition comprising at least one compound according to claim 1 together with one or more pharmaceutically acceptable carriers or excipients.
- 26. A pharmaceutical composition according to claim 25 in unit dosage form, comprising from about 0.05 mg to about 1000 mg of the compound according to claim 1.
- 27. A method for treating diseases, disorders, syndromes and conditions wherein an inhibition of glycogen synthase kinase-3 (GSK-3) is beneficial, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 28. The method according to claim 27, wherein the effective amount of the compound is in the range of from about 0.05 mg to about 2000 mg per day.
- 29. A pharmaceutical composition according to claim 25 in unit dosage form; comprising from about 0.1 mg to about 500 mg of the compound according to claim 1.
- 30. A pharmaceutical composition according to claim 25 in unit dosage form, comprising from about 0.5 mg to about 200 mg of the compound according to claim 1.
- 31. The method according to claim 27, wherein the effective amount of the compound is in the range of from about 0.1 mg to about 1000 mg per day.
- 32. The method according to claim 27, wherein the effective amount of the compound is in the range of from about 0.5 mg to about 500 mg per day.
- 33. A method for treating diseases, disorders, syndromes and conditions related to glycogen synthase kinase-3 (GSK-3), said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 34. A method for treating diseases, disorders, syndromes and conditions wherein growth factor induced inhibition of glycogen synthase kinase-3 (GSK-3) is insufficient, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 35. A method for treating diseases, disorders, syndromes and conditions wherein glycogen metabolism exhibits abnormalities, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 36. A method for treating diseases, disorders, syndromes and conditions wherein glycogen synthase is insufficiently activated, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 37. A method for treating diseases, disorders, syndromes and conditions involving elevated blood glucose, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 38. A method for treating hyperglycemia, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 39. A method for treating impaired glucose tolerance, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 40. A method for treating type 2 diabetes, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 41. A method for treating type 1 diabetes, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 42. A method for treating obesity, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 43. A method for treating Alzheimer's disease, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 44. A method for treating bipolar disorder, said method comprising administering to a subject in need thereof an effective amount of a compound of formula (I′):
- 45. The method according to claims 27 and 33-42, said method comprising further administering to said subject one or more agents selected from the group consisting of antidiabetic agents, antihyperlipidemic compounds, antiobesity compounds and antihypertensive compounds.
- 46. The method according to claim 43, said method further comprising further administering to said subject one or more agents for treating Alzheimer's disease.
- 47. The method according to claim 44, said method further comprising further administering to said subject one or more agents for treating bipolar disorder.
Priority Claims (2)
Number |
Date |
Country |
Kind |
PA 2001 01175 |
Aug 2001 |
DK |
|
PCT/DK02/00508 |
Jul 2002 |
WO |
|
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit priority under 35 U.S.C. 119 of Danish application no. PA 2001 01175 filed Aug. 3, 2001 and U.S. provisional application No. 60/309,953 filed Aug. 3, 2001 and further claims priority under 35 U.S.C. 120 of international application no. PCT/DK02/00508 filed Jul. 22, 2002, the contents of all of which are fully incorporated herein by reference.