Nobex Corporation

Biocon Limited

Aslam M Ansari

Nnochiri Ekwuribe

Christopher H Price

Amy L Odenbaugh

Balasingam Radhakrishnan

James Gordon Still

Jennifer Ann Filbey

Balasingam Rhadakrishnan

Wes Anderson, Jr

Nnochiri N Ekwuribe

Wes Anderson Jr

A mixture of conjugates in which each conjugate in the mixture comprises an insulin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may also be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may also result in less inter-subject variability than polydispersed mixtures of similar conjugates.

Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same

Methods of treating diabetes mellitus in a patient in need of such treatment include administering an effective amount of an insulin polypeptide-oligomer conjugate of formula V to the patient in order to treat diabetes mellitus in the patient. Methods according to the present invention may 'activate' the liver, potentially restoring normal glucose homeostasis to individuals suffering from diabetes mellitus.

Insulin conjugates for treating diabetes mellitus

Methods of treating diabetes mellitus in a patient in need of such treatment include administering an effective amount of an insulin drug to the patient in order to treat diabetes mellitus in the patient. Methods according to the present invention may 'activate' the liver, potentially restoring normal glucose homeostasis to individuals suffering from diabetes mellitus.

Methods of treating diabetes mellitus

Methods of synthesizing a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties include:

Substantially monodispersed mixtures of polymers having polyethylene glycol moieties

A mixture of conjugates in which each conjugate in the mixture comprises a calcitonin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may lower serum calcium levels in a subject by 10, 15 or even 20 percent or more. Moreover, the mixture may be more effective at surviving an in vitro model of intestinal digestion than non-conjugated calcitonin. Furthermore, the mixture may exhibit a higher bioavailability than non-conjugated calcitonin.

Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same

Mixtures of insulin drug-oligomer comprising polyalkylene glycol

The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier ('BBB') and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugates comprise a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.

Enkephalin conjugates

The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier ('BBB') and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugate comprises a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.

Methods of activating a receptor using amphiphilic drug-oligomer conjugates

A non-polydispersed mixture of conjugates in which each conjugate in the mixture comprises a drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may result in less inter-subject variability than polydispersed mixtures of similar conjugates.

Mixtures of drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same

Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties

Mixtures of conjugates in which each conjugate in the mixture comprises a growth hormone drug coupled to an oligomer that includes a polyalkylene glycol moiety wherein the mixtures have a molecular weight distribution with a standard deviation of less than about 22 Daltons are disclosed. Methods of treating growth hormone deficiency in a subject in need of such treatment and methods of accelerating the growth rate of an animal arc also disclosed. Processes for synthesizing substantially monodispersed mixtures of conjugates wherein each conjugate comprises a growth hormone drug coupled to an oligomer that comprises a polyethylene glycol moiety are further provided.

Mixtures of growth hormone drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same

Substantiallymonodispersed mixtures of polymers having polyethylene glycol moieties

The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier (&ldquo;BBB&rdquo;) and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugates comprise a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.

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Rockville, MD, United States of America

Aslam M Ansari