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US 2020/0270304 A1Published application
Polymer agonists of mu opioid receptors
AssigneeCytogel Pharma, LLC
InventorsTHEODORE E. MAIONE, JAMES HAMSHER, CONSTANTINE BASIL MAGLARIS
Life of this patent
Estimating the term…
Abstract
The subject invention provides compositions and methods for alleviating pain. Specifically, the subject invention provides pharmaceutical formulations of polymers, and/or their salts, having advantageous μ-opioid receptor binding activity.
Claims21
1-54. (canceled)
A polymer having the sequence selected from SEQ ID NO:
- 1:
- Tyr1-Xaa2-Xaa3-Phe4, SEQ ID NO:
- 2:
- Tyr1-Xaa2-Xaa3-Phe4-Glu5, SEQ ID NO:
- 3:
- Tyr1-Xaa2-Xaa3-Phe4-Asp5, SEQ ID NO:
- 4:
- Tyr1-c[Xaa2-Xaa3-Phe4-Glu5], and SEQ ID NO:
- 5:
- Tyr1-c[Xaa2-Xaa3-Phe4-Asp5],
- wherein Xaa2 and Xaa3 are each an amino acid,
- with the proviso that:
- either Xaa2 is a residue other than lysine, glutamate, aspartate, ornithine, or proline;
- or Xaa3 is a residue other than an aromatic amino acid.
11 more elements
A polymer having the sequence selected from SEQ ID NO:
- 1:
- Tyr1-Xaa2-Xaa3-Phe4, SEQ ID NO:
- 2:
- Tyr1-Xaa2-Xaa3-Phe4-Glu5, SEQ ID NO:
- 3:
- Tyr1-Xaa2-Xaa3-Phe4-Asp5, SEQ ID NO:
- 4:
- Tyr1-c[Xaa2-Xaa3-Phe4-Glu5], and SEQ ID NO:
- 5:
- Tyr1-c[Xaa2-Xaa3-Phe4-Asp5],
- wherein Xaa2 and Xaa3 are each an amino acid and one or more of Tyr1, Xaa2, Xaa3, Phe4, Glu5, and Asp5 is/are conjugated to a moiety.
8 more elements
A composition comprising a polymer and a pharmaceutically acceptable carrier and/or excipient, the polymer having a sequence selected from SEQ ID NO:
- 1:
- Tyr1-Xaa2-Xaa3-Phe4, SEQ ID NO:
- 2:
- Tyr1-Xaa2-Xaa3-Phe4-Glu5, SEQ ID NO:
- 3:
- Tyr1-Xaa2-Xaa3-Phe4-Asp5, SEQ ID NO:
- 4:
- Tyr1-c[Xaa2-Xaa3-Phe4-Glu5], and SEQ ID NO:
- 5:
- Tyr1-c[Xaa2-Xaa3-Phe4-Asp5],
- wherein Xaa2 and Xaa3 are each an amino acid,
- and wherein the pharmaceutically acceptable carrier and/or excipient comprises one or more of cyclodextrin, polyethylene glycol, a sugar, and a poly-alcohol;
- and optionally, further comprises lysophosphatidic acid (LPA) and/or amitriptyline.
10 more elements
Dependencies are inferred from the claim text.