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AssigneeProtein Delivery, Inc.
InventorNnochiri Nkem Ekwuribe
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A stabilized conjugated therapeutic agent complex comprising a therapeutic agent conjugatively coupled to a polymer including lipophilic and hydrophilic moieties, wherein the therapeutic agent 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, papain, Ara-A (Arabinofuranosyladenine), Acylguanosine, Nordeoxyguanosine, Azidothymidine, Dideoxyadenosine, Dideoxycytidine, Dideoxyinosine Floxuridine, 6-Mercaptopurine, Doxorubicin, Daunorubicin, or I-darubicin, Erythormycin, Vancomycin, oleandomycin, Ampicillin; Quinidine and Heparin. 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 therapeutic agent 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 therapeutic agent 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 composition comprising a therapeutic agent 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 composition comprising a therapeutic agent 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 therapeutic agent is soluble in aqueous solvents and active in prophylaxis or treatment of conditions or disease states in a mammalian subject.
A physiologically active therapeutic agent composition comprising a physiologically active therapeutic agent 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 therapeutic agent, the linear polyalkylene glycol moiety and the lipophilic moiety are conformationally arranged in relation to one another such that the physiologically active therapeutic agent in the physiologically active therapeutic agent composition has an enhanced in vivo resistance to enzymatic degradation, relative to the physiologically active therapeutic agent alone.
A physiologically active therapeutic agent composition of three-dimensional conformation comprising a physiologically active therapeutic agent covalently coupled with a polysorbate complex comprising (i) a linear polyalkylene glycol moiety and (ii) a lipophilic moiety, wherein the physiologically active therapeutic agent, 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 therapeutic agent in the physiologically active therapeutic agent composition has an enhanced in vivo resistance to enzymatic degradation, relative to the physiologically active therapeutic agent alone.
A multiligand conjugated therapeutic agent 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, wherein the polysorbate moiety has a physiological active nucleoside covalently bonded thereto.
A stable, aqueously soluble, conjugated therapeutic agent complex comprising a therapeutic agent 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-therapeutic agent conjugate comprising a conjugating polymer selected from the group consisting of polymers of the formulae:
A method of prophylactically or interventionally treating a potential or developed condition or disease state in a human or non-human mammalian subject with a therapeutic agent effective therefor, comprising administering to the subject an effective amount of a conjugated therapeutic agent composition comprising a stable, aqueously soluble, conjugated therapeutic agent complex comprising said therapeutic agent coupled to a physiologically compatible polyethylene glycol modified glycolipid moiety.
A method of prolonging the activity of a therapeutically active agent in an in vivo or in vitro system, comprising conjugatively coupling said therapeutic agent with one or more molecules of a non-naturally-occurring polymer comprising a lipophilic moiety and a hydrophilic polymer moiety to yield a conjugatively coupled polymer-therapeutic agent composition, and introducing the conjugatively coupled polymer-therapeutic agent composition to the in vivo or in vitro system.
Dependencies are inferred from the claim text.