Claims
- 1. A compound having the structure:
- 2. A compound in accordance with claim 1 in which p is 0.
- 3. A compound in accordance with claim 1 in which R1 is oxygen.
- 4. A compound in accordance with claim 1 in which R2 and R3 are —CR= and M is =CR4—.
- 5. A compound in accordance with claim 4 in which p is 0 and R4 and R8 are hydrogen.
- 6. A compound in accordance with claim 5 in which R5 and R7 are —(CR2)n— and R6 is —(CR2)m—.
- 7. A compound in accordance with claim 6 in which R1 is oxygen, R is hydrogen, and m =n=1, said compound being 1-(benzofurazan-5-ylcarbonyl)piperidine.
- 8. A compound in accordance with claim 6 in which R1 is sulfur, R is hydrogen, and m =n=1, said compound being 1-(benzo-2,1,3-thiadiazole-5-ylcarbonyl)piperidine.
- 9. A compound in accordance with claim 1 in which p is 0, R2 and R3 are —CR=, M is =CR4—, R4 and R8 are hydrogen, R5 is —CR=CX—, R6 is —(CR2)m—, R7 is —(CR2)n—, and m is 0.
- 10. A compound in accordance with claim 9 in which R is hydrogen.
- 11. A compound in accordance with claim 10 in which R1 is oxygen, X is F, and n is 1, said compound being 1-(benzofurazan-5-ylcarbonyl)-4-fluoro-1,2,3,6-tetrahydropyridine.
- 12. A compound in accordance with claim 1 in which p is 0, R2 and R3 are —CR=, M is =CR4—, R4 and R8 are hydrogen, R5 is —CR=CR—, R6 is —(CR2)m—, R7 is —(CR2)n—, and m is 0.
- 13. A compound in accordance with claim 12 in which R is hydrogen.
- 14. A compound in accordance with claim 13 in which R1 is oxygen and n is 1, said compound being 1-(benzofurazan-5-ylcarbonyl)-1,2,3,6-tetrahydropyridine.
- 15. A compound in accordance with claim 1 in which p is 0, M is =CR4—, R2 and R3 are —CR=, R4 and R8 are hydrogen, R5 and R7 are —(CR2)n—, and R6 is —C(O)—, —C(RX)—, CX2—, —O—, or —S—.
- 16. A compound in accordance with claim 15 in which R6 is —CRX— or —CX2—.
- 17. A compound in accordance with claim 16 in which R1 is oxygen, X is fluorine, n is 1, and R is hydrogen, said compound being:
a) 1-(benzofurazan-5-ylcarbonyl)-4′-fluoropiperidine; or b) 1-(benzofurazan-5-ylcarbonyl)-4′,4′-difluoropiperidine.
- 18. A compound in accordance with claim 15 in which R1 is oxygen, R6 is —O— or —S—, n is 1, and R is hydrogen.
- 19. A compound in accordance with claim 1 in which M is =CR4—, wherein R4 and R8 together form a single linking moiety linking M to the ring vertex 2′, the linking moiety being a single bond, —CR2—, —CR=CR—, —C(O)—, —O—, —S—, —NR—, or —N=.
- 20. A compound in accordance with claim 19 in which p is 0.
- 21. A compound in accordance with claim 19 in which R1 is oxygen.
- 22. A compound in accordance with claim 19 in which R2 and R3 are —CR=.
- 23. A compound in accordance with claim 22 in which R5 and R7 are —(CR2)n— and R6 is —(CR2)m—.
- 24. A compound in accordance with claim 23 in which n=m=1.
- 25. A compound in accordance with claim 23 in which n is 1 and m is 0.
- 26. A compound in accordance with claim 23 in which the linking moiety is —CR2—, —O—, —S—, or —N=.
- 27. A compound in accordance with claim 23 in which the linking moiety is —O—.
- 28. A method for the treatment of a mammalian subject, wherein the subject suffers from a hypoglutamatergic condition or deficiencies in the number or strength of excitatory synapses or in the number of AMPA receptors, such that memory or other cognitive functions are impaired, said method comprising administering to said subject, in a pharmaceutically acceptable carrier, an effective amount of a compound having the formula:
- 29. A method in accordance with claim 28 in which p is 0.
- 30. A method in accordance with claim 28 in which R1 is oxygen.
- 31. A method in accordance with claim 28 in which R2 and R3 are —CR=and M is =CR4—.
- 32. A method in accordance with claim 28 in which p is 0, R2 and R3 are —CR=, and M is =CR4—.
- 33. A method in accordance with claim 32 in which R4 and R8 are hydrogen.
- 34. A method in accordance with claim 33 wherein R1 is oxygen, R5 and R7 are —(CR2)n—, R6 is —(CR2)m—, and n=m=1, said compound being 1-(benzofurazan-5-ylcarbonyl) piperidine.
- 35. A method in accordance with claim 33, wherein R1 is sulfur, R5 and R7 are —(CR2)n—, R6 is —(CR2)m—, and n=m=1, said compound being 1-(benzo-2,1,3-thiadiazole-5-ylcarbonyl) piperidine.
- 36. A method in accordance with claim 32, wherein R4 and R8 together form a single linking moiety linking M to the ring vertex 2′, the linking moiety being a single bond, —CR2—, —CR=CR—, —C(O)—, —O—, —S—, —NR—, or —N=.
- 37. A method in accordance with claim 36, wherein the linking moiety is —O—.
- 38. A method for the treatment of a mammal wherein the subject suffers from a hypoglutamatergic condition or deficiencies in the number or strength of excitatory synapses or in the number of AMPA receptors such that a cortical/striatal imbalance occurs leading to schizophrenia or schizophreniform behavior, said method comprising administering to said subject, in a pharmaceutically acceptable carrier, an effective amount of a compound having the formula:
- 39. A method in accordance with claim 38 in which p is 0.
- 40. A method in accordance with claim 38 in which R1 is oxygen.
- 41. A method in accordance with claim 38 in which R2 and R3 are —CR=, and M is =CR4—.
- 42. A method in accordance with claim 38 in which p is 0, R2 and R3 are —CR=, and M is =CR4—.
- 43. A method in accordance with claim 42 in which R4 and R8 are hydrogen.
- 44. A method in accordance with claim 43 wherein R1 is oxygen, R5 and R7 are —(CR2)n—, R6 is —(CR2)m—, and n=m=1, said compound being 1-(benzofurazan-5-ylcarbonyl) piperidine.
- 45. A method in accordance with claim 43, wherein R1 is sulfur, R5 and R7 are —(CR2)n—, R6 is —(CR2)m—, and n=m=1, said compound being 1-(benzo-2,1,3-thiadiazole-5-ylcarbonyl) piperidine.
- 46. A method in accordance with claim 42, wherein R4 and R8 together form a single linking moiety linking M to the ring vertex 2′, the linking moiety being a single bond, —CR2—, —CR=CR—, —C(O)—, —O—, —S—, —NR—, or —N=.
- 47. A method in accordance with claim 46, wherein the linking moiety is —O—.
RELATED APPLICATIONS
[0001] This application is a continuation-in-part of Ser. No. 08/800,108, filed Feb. 13, 1997.
Continuations (1)
|
Number |
Date |
Country |
Parent |
09365798 |
Aug 1999 |
US |
Child |
09834349 |
Apr 2001 |
US |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
08800108 |
Feb 1997 |
US |
Child |
09365798 |
Aug 1999 |
US |