Biocon Limited

Monica Puskas

Nnochiri Ekwuribe

Balasingam Radhakrishnan

Navdeep Balkrishna Malkar

Kenneth D James

Diti Aggarwal

Michelle Ferro

Leo Pavliv

Karen Polowy

Richard Soltero

Diti Sangal

Nnochiri N Ekwuribe

An insulin compound coupled to a modifying moiety having a formula:&#x2014;X&#x2014;R&#x2014;Y-PAG-Z&#x2014;R&#x2003;&#x2003;(Formula VI)

Cation complexes of insulin compound conjugates, formulations and uses thereof

An insulin conjugate is disclosed in which insulin is coupled to a modifying moiety of the formula X&#x2014;R&#x2014;Y-PAG-Z&#x2014;Rwherein X, Y, and Z are linking groups, Ris a capping group, and PAG is a carbon chain that incorporates one or more alkylene glycol moieties.

Insulin-oligomer conjugates, formulations and uses thereof

Fatty acid compositions for administration of of pharmaceutical agents, such as proteins and peptides, protein and peptide conjugates, and/or cation-polypeptide conjugate complexes. In particular, the invention provides a solid pharmaceutical composition formulated for oral administration by ingestion, having from about 0.1 to about 75% w/w fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent. Further, the invention provides a liquid pharmaceutical composition formulated for oral administration by ingestion, comprising: from about 0.1 to about 10% w/v fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent.

Fatty acid formulations and oral delivery of proteins and peptides, and uses thereof

The invention provides a complex including a cation and an insulin compound conjugate. The insulin compound conjugate includes insulin compound, such as human insulin or an analog thereof, conjugated to a modifying moiety, such as a polyethylene glycol moiety. The invention also includes solids and pharmaceutical compositions including such complexes, methods of making such complexes, and methods of using such complexes in the treatment of insulin compound deficiencies and other ailments. Further, the invention includes novel insulin compound conjugates and modifying moieties for use in making novel insulin compound conjugates. The invention also includes fatty acid compositions for administration of pharmaceutical agents, such as the novel insulin compound conjugates, and/or the cation-insulin compound conjugate complexes of the invention.

Cation complexes of insulin compound conjugates, formulation and uses thereof

Fatty acid formulations for oral delivery of proteins and peptides, and uses thereof

Methods for synthesizing proinsulin polypeptides are described that include contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also provided as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates and other pro-polypeptide-oligomer conjugates are also provided.

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Spring Hope, NC, United States of America

Monica Puskas