Patent ID: 7273848

Claim:
An ApoA-I agonist-lipid complex comprising an ApoA-I agonist and a lipid, wherein the ApoA-I agonist is a (i) 22 to 23-residue peptide or peptide analogue which forms an amphipathic α-helix in the presence of lipids and which comprises the structural formula (I): Z 1 -X 1 -X 2 -X 3 -X 4 -X 5 -X 6 -X 7 -X 8 -X 9 -X 10 -X 11 -X 12 -X 13 -X 14 -X 15 -X 16 -X 17 -X 18 -X 19 -X 20 -X 21 -X 22 -X 23 -Z 2 or a pharmaceutically acceptable salt thereof wherein: X 1 is Pro (P), Ala (A), Gly (G), Gln (Q), Asn (N), Asp(D), or D-Pro (p); X 2 is an aliphatic residue; X 3 is Leu (L) or Phe (F); X 4 is Glu (B); X 5 is an aliphatic residue; X 6 is Len (L) or Phe (F); X 7 is Glu (B) or Len (L); X 8 is Asn (N) or Gin (Q); X 9 is Leu (L); X 10 is Len (L), Trp (W) or Gly (G) X 11 is an acidic residue; X 12 is Arg (R) X 13 is Len (L) or Gly (G); X 14 is Len (L), Phe (F) or Gly (G); X 15 is Asp (D); X 16 is Ala (A); X 17 is Leu (L); X 18 is Asn (N) or Gln (Q); X 19 is a basic residue; X 20 is a basic residue; X 21 is Leu (L); X 22 is a basic residue; X 23 is absent or a basic residue; Z 1 is H 2 N— or RC(O)NH—; Z 2 is —C(O)NRR, —C(O)OR or —C(O)OH or a salt thereof; Each R is independently —H, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkenyl, (C 1 -C 6 ) alkynyl, (C 5 -C 20 ) aryl, (C 6 -C 26 ) alkaryl, 5-20 membered heteroaryl or 6-26 membered alkheteroaryl or a 1 to 7-residue peptide or peptide analogue; each “−” between residues X n independently designates an amide linkage, a substituted amide linkage, and isostere of an amide or an amide mimetic; or (ii) an altered form of structural formula (I) in which at least one of the residues X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , X 9 , X 10 , X 11 , X 12 , X 13 , X X 14 , X 15, X 16 , X 17 , X 18 , X 19 , X 20 , X 21 , X 22 or X 23 is conservatively substituted with another residue.