Claims
- 1. A compound of formula I:
- 2. The compound of claim 1, wherein 3-10 P groups are present.
- 3. The compound of claim 1, wherein 3-8 P groups are present.
- 4. The compound of claim 1, wherein 3-4 P groups are present.
- 5. The compound of claim 1, wherein 4-8 P groups are present.
- 6. The compound of claim 1, wherein 4-6 P groups are present.
- 7. A compound of formula II:
- 8. A compound of formula III:
- 9. A compound of claim 1 or a pharmaceutically acceptable salt thereof wherein the compound is selected from the group consisting of:
K1-P1-P2-P3-P4-P5-P6-P7-P8-P9-K2; K1-P1-P2-P3-P4-P5-P6-P7-P8-K2; K1-P1-P2-P3-P4-P5-P6-P7-K2; K1-P1-P2-P3-P4-P5-P6-K2; K1-P1-P2-P3-P4-P5-K2; K1-P1-P2-P3-P4-K2; K1-P1-P2-P3- K2; K1-P2-P3-P4-P5-P6-P7-P8-P9-P10-K2; K1-P3-P4-P5-P6-P7-P8-P9-P10-K2; K1-P4-P5-P6-P7-P8-P9-P10-K2; K1-P5-P6-P7-P8-P9-P10-K2; K1-P6-P7-P8-P9-P10-K2; K1-P7-P8-P9-P10-K2; and K1-P8-P9-P10-K2.
- 10. A compound of claim 1, or a pharmaceutically acceptable salt thereof wherein the compound is:
AcIHFFKNI; AcVRFFKNI; AcVHPFKNI; AcVHFFPNI; AcVHFFKTI; AcVRFANI; AcVRPFS; AcVRLFANI; AcVVHFFKNI; AcVTFFKNI; AcVH(N-Me Ala)FKNI; AcVHA(N-Me Ala)-F-(N-Me Ala)N; AcVHFVKNI; AcVRF(2-Nal)KNI; AcVRF(1-Nal)KNI; AcVHFFA(N-Me Ala)NI; AcVRLFKN; AcVRF(4′-Pyridyl Ala)KNI; AcVRAFAN; AcVRA(O-Benzyl Ser)KNI; Ac(Tic)FKNI; AcVR(Tic)FKNI; Ac(Cpg)RFFKNI; AcVHSFSN; AcVRF(3′ Cyano Phe)KNI; AcVR(Tiq)FKNI; Ac(Tiq)FKNI; AcVVRFFK; AcVRFF(homo Pro)NI; Ac(Tic)FKNI; Ac(Cpg)R(Tic)FKNI; AcVR(homo Pro)FKNI; AcVRFFK; AcVKFFKNI; AcV(Om)FFKNI; AcV(N′ Alloc Dab)FFKNI; Ac(Cha)RFFKNI; Ac(2′ Furanyl Ala)RFFKNI; Ac(2′ Thienyl Ala)RFFKNI; AcVR(2′ Furanyl Ala)FKNI; AcVR(2′ Thienyl Ala)FKNI; AcVRAFKNI; Benzoyl-VRFFK; Isobutanoyl-VRFFK; Butanoyl-VRFFK; IsoValeroyl-VRFFK; Ac(Cpg)R(Tic)F(homo Pro); AcVVRFF; 3-(Imadazoyl-4-yl)propionyl-VRFFK; Ac(Chg)RFFKNI; AcVRFF(Dap)NI; AcV(Dab)FFKNI; AcVVAGFKNI; AcVAGFKNI; AcV(Dap)FFKNI; AcVRFF; AcVRF(3′ phenoxy Phe)KNI; AcVVKF(3′ Methylamino Phe) K; AcFRFFKNI; AcVRFFK(beta Ala)I; AcV(3′-amino-1′-carboxymethyl-pyridin-2′-one)FKNI; Ac(Idg)RFFKNI; AcAVRFFK; AcAVHFFKNI; AcV(2′ Furanyl Ala)FFKNI; AcV(2′ Thienyl Ala)FFKNI; AcVVKF(3′ Cyano Phe)K; Ac(Phg)RFFKNI; AcIR(Tic)F(homo Pro); AcLRFFKNI; AcVR(Phg)FKNI; AcVVRF(3′ phenoxy Phe)K; AcVRF(Phg)KNI; AcVRFFK(beta Ala); AcVVRFFK(beta Ala); Ac(Chg)VRFFK; Ac(Chg)RF(4′-Indolyl Ala)KNI; AcVRF(3′-Carbazolyl Ala)KNI; Ac(Cpg)-NHNH(COCH2CH(Ph)CO)KNI; AcVRF(3′-amino Phe)KNI; AcWRFFKNI; AcV(ω,ω dimethyl Lys)FFKNI; AcV(Chg)RFFK; AcV(nor Arg)FFKNI; AcVRF(3-Acetylamino Phe)KNI; Ac(Chg)R(Tic)F(4′-hydroxy Pro); Ac(Chg)R(Tic); AcVKFFENI; AcVRIFKNI; Ac(Cpg)-NHNH(COCH2CH(Ph)CO)FKNI; Ac(Chg)R(Tic)-(3′-Carbazolyl Ala); Ac(Chg)R(Tic)F(homo Pro); Ac(Idg)R(Tic)FK; AcV(Idg)R(Tic)FK; AcV(Chg)R(Tic)F; AcV(Chg)RFFK; Ac(Chg)R(Tic)-(3′-Carbazolyl Ala)G; AcV(Chg)R(Tic)-(3′-Carbazolyl Ala)G; AcVVRF(3′-Acetylaminomethyl Phe); AcVVRF(3′-Methylsulphonyl aminomethyl Phe); (2,6-Dimethyl Benzoyl)-VRFFK; AcV(homo Arg)FFKNI; or Ac(Cpg)-NHNH(COCH2CH(Ph)CO)-(4′-Indolyl Ala)K.
- 11. A compound of claim 8, wherein all natural amino acids and non-natural amino acids are L-amino acids.
- 12. A compound of claim 8, wherein one or more of the natural amino acids or non-natural amino acids is a D-amino acid.
- 13. A compound of claim 8, wherein one or more of the natural amino acids or non-natural amino acids has an R configuration.
- 14. A compound of claim 8, wherein one or more of the natural amino acids or non-natural amino acids has an S configuration.
- 15. A pharmaceutical composition comprising a compound of claim 1, 7, 8 or 10 and a pharmaceutically acceptable carrier.
- 16. A method for treating or preventing a disease responsive to the inhibition of antigen binding to a MHC class II molecule comprising administering to a patient in need thereof a compound of claim 1, 7, 8 or 10, or a pharmaceutically acceptable salt thereof.
- 17. A method for treating or preventing a disease responsive to the inhibition of antigen presentation by a MHC class II molecule comprising administering to a patient in need thereof a compound of claim 1, 7, 8 or 10, or a pharmaceutically acceptable salt thereof.
- 18. A method for treating or preventing a disease responsive to the inhibition of T cell proliferation comprising administering to a patient in need thereof a compound of claim 1, 7, 8 or 10, or a pharmaceutically acceptable salt thereof.
- 19. The method of claim 16, wherein the MHC class II molecule is HLA-DR2.
- 20. The method of claim 17, wherein the MHC class II molecule is HLA-DR2.
- 21. A method for treating or preventing an autoimmune disease comprising administering to a patient in need thereof a compound of claim 1, 7, 8 or 10, or a pharmaceutically acceptable salt thereof.
- 22. The method of claim 21, wherein the autoimmune disease is multiple sclerosis.
- 23. A method of inhibiting binding to a MHC class II HLA-DR2 molecule comprising contacting a cell with an effective amount of a compound of claim 1, 7, 8 or 10.
- 24. A method of inhibiting antigen presentation by a MHC class II HLA-DR2 molecule comprising contacting a cell with an effective amount of a compound of claim 1, 7, 8 or 10.
- 25. A method of inhibiting T cell proliferation comprising contacting a cell with an effective amount of a compound of claim 1, 7, 8 or 10.
Parent Case Info
[0001] This application claims the benefit of U.S. provisional application No. 60/447,949, filed Feb. 14, 2003, the contents of which are incorporated by reference herein in their entirety.
Provisional Applications (1)
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Number |
Date |
Country |
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60447949 |
Feb 2003 |
US |