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AssigneeProtein Delivery, Inc.
InventorNnochiri N. Ekwuribe
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A stabilized conjugated peptide complex comprising a peptide conjugatively coupled to a polymer including lipophilic and hydrophilic moieties, wherein the peptide may for example be selected from the group consisting of insulin, calcitonin, ACTH, glucagon, somatostatin, somatotropin, somatomedin, parathyroid hormone, erythropoietin, hypothalamic releasing factors, prolactin, thyroid stimulating hormones, endorphins, enkephalins, vasopressin, non-naturally occurring opioids, superoxide dismutase, interferon, asparaginase, arginase, arginine deaminease, adenosine deaminase, ribonuclease, trypsin, chymotrypsin, and papain. In a particular aspect, the invention comprises an insulin composition suitable for parenteral as well as non-parenteral administration, preferably oral or parenteral administration, comprising insulin covalently coupled with a polymer including (i) a linear polyalkylene glycol moiety and (ii) a lipophilic moiety, wherein the insulin, the linear polyalkylene glycol moiety and the lipophilic moiety are conformationally arranged in relation to one another such that the insulin in the composition has an enhanced in vivo resistance to enzymatic degradation, relative to insulin alone. One, two, or three polymer constituents may be covalently attached to the insulin molecule, with one polymer constituent being preferred. The conjugates of the invention are usefully employed in therapeutic as well as non-therapeutic, e.g., diagnostic, applications, and the peptide and polymer may be covalently coupled to one another, or alternatively may be associatively coupled to one another, e.g., by hydrogen bonding or other associative bonding relationship.
A peptide composition comprising a peptide stabilizingly and covalently conjugatively coupled with one or more molecules of a non-naturally-occurring polymer, said polymer comprising a lipophilic moiety and a hydrophilic polymer moiety, thereby imparting balanced lipophilic and hydrophilic characteristics to the composition such that the composition is soluble in pharmaceutically acceptable solvents and able to interact with biological membranes.
A peptide composition comprising a peptide stabilizingly and conjugatively coupled with one or more molecules of a non-naturally-occurring polymer comprising a lipophilic moiety and a hydrophilic polymer moiety wherein the peptide is soluble in aqueous solvents and active in prophylaxis or treatment of conditions or disease states in a plant or component thereof.
A physiologically active peptide composition comprising a physiologically active peptide covalently coupled with one or more molecules of a polymer comprising (i) a linear polyalkylene glycol moiety and (ii) a lipophilic moiety, wherein the physiologically active peptide, the linear polyalkylene glycol moiety and the lipophilic moiety are conformationally arranged in relation to one another such that the physiologically active peptide in the physiologically active peptide composition has an enhanced in vivo resistance to enzymatic degradation, relative to the physiologically active peptide alone.
A physiologically active peptide composition of three-dimensional conformation comprising a physiologically active peptide covalently coupled with a polysorbate complex comprising (i) a linear polyalkylene glycol moiety and (ii) a lipophilic moiety, wherein the physiologically active peptide, the linear polyalkylene glycol moiety and the lipophilic moiety are conformationally arranged in relation to one another such that (a) the lipophilic moiety is exteriorly available in the three-dimensional conformation, and (b) the physiologically active peptide in the physiologically active peptide composition has an enhanced in vivo resistance to enzymatic degradation, relative to the physiologically active peptide alone.
A multiligand conjugated peptide complex comprising a triglyceride backbone moiety, having:
A polysorbate complex comprising a polysorbate moiety including a triglyceride backbone having a fatty acid group covalently coupled to one of the .alpha.,.alpha.' and .beta. carbon atoms thereof, and having a polyethylene glycol group covalently coupled to one of the .alpha.,.alpha.' and .beta. carbon atoms thereof.
A stable, aqueously soluble, conjugated peptide complex comprising a peptide stabilizingly and conjugatively coupled to a polyethylene glycol modified glycolipid moiety.
A polysorbate complex comprising a polysorbate moiety including a triglyceride backbone having covalently coupled to carbon atoms independently selected from .alpha.,.alpha.' and .beta. carbon atoms thereof, functionalizing groups including:
A polymer-peptide conjugate comprising a conjugating polymer selected from the group consisting of polymers of the formulae:
Dependencies are inferred from the claim text.