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US 5,861,481 AGranted
Peptide lung surfactants and therapeutic combinations
AssigneeMerrell Pharmaceuticals Inc.
InventorsLarry R. McLean, J. Vincent Edwards
Life of this patent
Estimating the term…
Abstract
Synthetic pulmonary surfactant consisting of a complex of a polypeptide of 3-4 amino acid residues having alpha-helical structure and a covalently bound long chain acyl group. The peptides are useful when consisting of one or more associated lipids in combination in conditions associated with respiratory distress.
Claims16
A polypeptide of the formula:
- X--A.sub.1 --A.sub.2 --A.sub.3 --A.sub.4 --Y
- or an optically active isomer or pharmaceutically acceptable salt thereof;
- wherein
- X is an acyl or alkyl group of 8 to 18 carbon atoms;
- Y is --OH or --NH.sub.2 ;
- A.sub.1 is a bond, Glu or Asp;
- A.sub.2 is Trp, Tyr, Phe, His, Val, Leu, or Ile;
- A.sub.3 is Aib, Glu, Gln, Leu, Ala, Orn, or a bond;
- and
- A.sub.4 is Lys, Arg, or His;
- wherein, when A.sub.3 is a bond, A.sub.1 and A.sub.2 may be interchanged;
- which optionally may be associated with a lipid wherein the lipid is comprised of one or more of the type assoicated with natural pulmonary surfactant
- with the proviso that when A.sub.1 is a bond or Glu;
- A.sub.2 is Trp;
- A.sub.3 is Aib, Glu, or Ala;
- and A.sub.4 is Lys, X is not an aromatic acyl.
13 more elements
A polypeptide of the formula:
- X--A.sub.1 --A.sub.2 --A.sub.3 --A.sub.4 --Y
- or an optically active isomer or pharmaceutically acceptable salt thereof;
- wherein
- X is an acyl or alkyl group of 8 to 18 carbon atoms;
- Y is --OH or --NH.sub.2 ;
- A.sub.1 is a bond, Glu or Asp;
- A.sub.2 is Trp, Tyr, Phe, His, Val, Leu, or Ile;
- A.sub.3 is Aib, Glu, Gln, Leu, Ala, Orn, or a bond;
- and
- A.sub.4 is Lys, Arg, or His;
- which optionally may be associated with a lipid wherein the lipid is comprised of one or more of the type assoicated with natural pulmonary surfactant;
- with the proviso that when A.sub.1 is a bond or Glu;
- A.sub.2 is Trp;
- A.sub.3 is Aib, Glu, or Ala;
- and A.sub.4 is Lys, X is not an aromatic acyl.
12 more elements
A polypeptide of the formula:
- X--A.sub.1 --A.sub.2 --A.sub.3 --A.sub.4 --Y
- or an optically active isomer or pharmaceutically acceptable salt thereof;
- wherein
- X is an acyl or alkyl group of 8 to 18 carbon atoms;
- Y is --OH or --NH.sub.2 ;
- A.sub.1 is a bond, Glu or Asp;
- A.sub.2 is Trp, Glu or Asp;
- A.sub.3 is Aib, Glu, Gln, Leu, Ala, Orn-X, or a bond;
- and
- A.sub.4 is Lys or Arg;
- which optionally may be associated with a lipid wherein the lipid is comprised of one or more of the type assoicated with natural pulmonary surfactant;
- with the proviso that when A.sub.1 is a bond or Glu;
- A.sub.2 is Trp;
- A.sub.3 is Aib, Glu, or Ala;
- and A.sub.4 is Lys, X is not an aromatic acyl.
12 more elements
Dependencies are inferred from the claim text.