Claims
- 1. A compound having the formula:
- 2. The compound according to claim 1, wherein
R1 is selected from substituted or unsubstituted alkyl, 19
- 3. The compound according to claim 2, wherein Y is O; and X is O.
- 4. The compound according to claim 3, wherein R7 and R8 are members independently selected from H, substituted or unsubstituted aminoalkyl, and substituted or unsubstituted alkyl.
- 5. The compound according to claim 4, wherein R2is a member selected from substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; and R3 is a member selected from substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl.
- 6. The compound according to claim 2, wherein
R3 is substituted or unsubstituted aryl.
- 7. The compound according to claim 6, wherein Y is O.
- 8. The compound according to 6 wherein R7 and R8 are members independently selected from H, and substituted or unsubstituted alkyl.
- 9. A compound having the formula:
- 10. The compound according to claim 9, wherein n is 1.
- 11. The compound according to claim 10, wherein X is O.
- 12. The compound according to claim 11, wherein Y is O.
- 13. The compound according to 12, wherein
Z is a member selected from: 23
- 14. A method of decreasing ion flow through voltage-dependent sodium channels in a cell, said method comprising contacting said cell with a sodium channel-inhibiting amount of a compound comprising a piperidinyl moiety.
- 15. The method according to claim 14, wherein said cell is in a human.
- 16. A method of decreasing ion flow through voltage-dependent sodium channels in a cell, said method comprising contacting said cell with a sodium channel-inhibiting amount of a compound of the formula:
- 17. A method of treating a central or peripheral nervous system disorder or condition through inhibition of a voltage-dependent sodium channel, said method comprising administering to a subject in need of such treatment, an effective amount of a compound comprising a piperidinyl moiety.
- 18. The method according to claim 16, said compound having the formula:
- 19. The method according to claim 16, wherein said disorder is pain selected from inflammatory pain, neuropathic pain and combinations thereof.
- 20. A composition comprising a pharmaceutically acceptable excipient and a compound having the formula:
in which
R1 is a member selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted aryl, substituted or unsubsituted arylalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heteroaryl, 30R2 is a member selected from substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, alkoxy, —NR15R16 wherein
R15 and R16 are each members independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl and R15 and R16 taken together with the nitrogen atom to which they are attached form a 4- to 8-membered heterocyclic ring R3 is a member selected from substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl and NR15R16; R4 is a member selected from substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heteroaryl, and NR15R16; R5 is a member selected from H, nitro, substituted or unsubstituted alkyl, cyano, acyl, and SO2R11 wherein
R11 is a member selected from substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; Y is a member selected from O, C—NO2 and S; Z is a member selected from: 31in which A, D, E and M are independently selected from CR12, N, and N-oxide, wherein
R12 is a member selected from hydrogen, halo, amino, hydroxy, cyano, nitro, acyl, alkoxy, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, and at least two of A, D, E and M is a selected from CR12, and at most one of A, D, E, and M is N-oxide; X is a member selected from O, C—NO2, S and NR10; R6, R7 and R8 are members independently selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted aminoalkyl, and R7 and R8 together with the atom to which they are joined are optionally joined to form a 4- to 8-membered heterocycloalkyl ring. R9 is a member selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted and unsubstituted heterocycloalkyl, OR20, and SR20; wherein
R20 is a member selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, and substituted and unsubstituted heterocycloalkyl; R10 is a member selected from hydrogen cyano, nitro, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heterocycloalkyl, substituted and unsubstituted heteroaryl and SO2R11; the dashed bond marked a is either a single or a double bond; and n is and integer selected from 0, 1, and 2.
CROSS-REFERENCES TO RELATED APPLICATIONS
[0001] This is a non-provisional filing of U.S. Provisional Patent Application No. 60/335,930, filed on Nov. 1, 2001, the disclosure of which is incorporated herein by reference in its entirety for all purposes.
Provisional Applications (1)
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Number |
Date |
Country |
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60335930 |
Nov 2001 |
US |