Thanks to the ill-named and conceived "America Invents Act", my guess is this will receive an insurmountable 101 rejection--claims recite non patent-eligible subject matter. Because the independent claims 1 and 15 claim things of nature. And you can't claim Mother Nature!
Claims:
1. An inhalable analgesic composition comprising microparticles of a diketopiperazine and a peptide comprising less than 20 amino acids; wherein said composition is effective at relieving pain.
2. The inhalable analgesic composition of claim 1, wherein the peptide comprises at least three amino acids independently selected from arginine, phenylalanine, leucine, isoleucine, norleucine, tyrosine, serine, proline, and tryptophan.
3. The inhalable analgesic composition of claim 2, wherein the peptide is an opioid receptor agonist.
4. The inhalable analgesic composition of claim 2, wherein the peptide is an amino acid sequence of from three to eight amino acids in length.
5. The inhalable analgesic composition of claim 4, wherein the peptide is a four amino acid sequence and the composition is for pulmonary administration.
6. The inhalable analgesic composition of claim 4, wherein the peptide comprises: Trp-(D)Pro-Ser-Phe-NH.sub.2 (SEQ ID NO: 3), Trp-(D)Ser-Ser-Phe-NH.sub.2 (SEQ ID NO: 4), Dmt-D-Arg-Phe-Lys-NH.sub.2 (SEQ ID NO: 5), Ac-His-(D)Phe-Arg-(D)Trp-Gly-NH.sub.2 (SEQ ID NO: 6), or Ac-Nle-Gln-His-(D)Phe-Arg-(D)Trp-Gly-NH.sub.2 (SEQ ID NO:7).
7. The inhalable analgesic composition of claim 1, wherein the peptide binds to a .mu. opioid receptor, a .delta. opioid receptor, or a .kappa. opioid receptor, or combinations of receptors thereof, of cells in the central or peripheral nervous systems.
8. The inhalable analgesic composition of claim 1, wherein the peptide is a .kappa. opioid receptor agonist.
9. The inhalable analgesic composition of claim 1, wherein the composition comprises a dry powder, and the peptide comprises at least 0.25% of the weight of the composition.
10. The inhalable analgesic composition of claim 1, wherein the composition comprises a dry powder for inhalation and comprises microparticles having a volumetric mean geometric diameter less than 8 .mu.m in diameter.
11. The inhalable analgesic composition of claim 1, wherein the diketopiperazine is an N-substituted-3,6-aminoalkyl-2,5-diketopiperazine.
12. The inhalable analgesic composition of claim 1, wherein the diketopiperazine is 2,5-diketo-3,6-di(4-X-aminobutyl)piperazine.
13. The inhalable analgesic composition of claim 11, wherein the diketopiperazine is bis[3,6-(N-fumaryl-4-aminobutyl)]-2,5,diketopiperazine, or bis[3,6-(N-fumaryl-4-aminobutyl)]-2,5-diketopiperazine disodium salt.
14. A dry powder for pulmonary inhalation comprising the inhalable analgesic composition of claim 13.
15. A method for treating pain, comprising administering to a subject in need of treatment a therapeutically effective amount of an inhalable analgesic composition comprising microparticles of a diketopiperazine and a peptide comprising less than 20 amino acids using a dry powder drug delivery system.
16. The method of claim 15, wherein the dry powder drug delivery system comprises a dry powder inhaler comprising a container configured to hold said inhalable analgesic composition in a containment configuration and in a dosing configuration.
17. The method of claim 15, wherein the inhalable analgesic composition comprises a dry powder comprising a peptide that binds to an opiate receptor.
18. The method of claim 17, wherein the diketopiperazine is bis[3,6-(N-fumaryl-4-aminobutyl)]-2,5, diketopiperazine, or bis[3,6-(N-fumaryl-4-aminobutyl)]-2,5-diketopiperazine disodium salt.
19. The method of claim 17, wherein the peptide comprises: Trp-(D)Pro-Ser-Phe-NH.sub.2 (SEQ ID NO: 3), Trp-(D)Ser-Ser-Phe-NH.sub.2 (SEQ ID NO: 4), Dmt-D-Arg-Phe-Lys-NH.sub.2 (SEQ ID NO: 5), Ac-His-(D)Phe-Arg-(D)Trp-Gly-NH.sub.2 (SEQ ID NO: 6), or Ac-Nle-Gln-His-(D)Phe-Arg-(D)Trp-Gly-NH.sub.2 (SEQ ID NO:7).
20. The method of claim 17, wherein the peptide binds to a .mu. opioid receptor, a .delta. opioid receptor, or a .kappa. opioid receptor, or combinations of receptors thereof, of cells in the central or peripheral nervous systems.
21. The inhalable analgesic composition of claim 12, wherein X is fumaryl, succinyl, glutaryl, maleyl, malonyl, oxalyl, or a pharmaceutically acceptable salt thereof.
22. The inhalable analgesic composition of claim 1, further comprising one or more pharmaceutical carrier or excipients selected from amino acids, sugars, and surfactants.
23. The inhalable analgesic composition of claim 22, wherein the amino acids comprise at least one of leucine, isoleucine, glycine, and methionine.
24. The inhalable analgesic composition of claim 22, wherein the sugars comprise at least one of mannitol, lactose, trehalose, and raffinose.
25. A synthetic peptide having an amino acid sequence Trp-(D)Pro-Ser-Phe-NH.sub.2 (SEQ ID NO: 3).
26. A synthetic peptide having an amino acid sequence Trp-(D)Ser-Ser-Phe-NH.sub.2 (SEQ ID NO: 4).
27. An inhalable analgesic composition comprising a diketopiperazine, a synthetic peptide having an amino acid sequence Trp-(D)Pro-Ser-Phe-NH.sub.2 (SEQ ID NO: 3), and optionally, a pharmaceutically acceptable excipient.
28. An inhalable analgesic composition comprising a diketopiperazine, a synthetic peptide having an amino acid sequence Trp-(D)Ser-Ser-Phe-NH.sub.2 (SEQ ID NO: 4), and optionally, a pharmaceutically acceptable excipient.