Applied Research Systems Ars Holding N.v.

Merck Serono S. A.

Laboratoires Serono S.a.

Nabil El-Tayar

Michael David Bentley

Xuan Zhao

Michael James Roberts

Milton Harris

Wayne Sawlivich

PEG-IFN-&#x3b2; conjugates, where a PEG moiety is covalently bound to Cysof human IFN-&#x3b2;, are produced by a process of site specific PEGylation with a thiol reactive PEGylating agent. A pharmaceutical composition and a method for treating infections, tumors and autoimmune and inflammatory diseases are also provided. The invention further relates to a method for the stepwise attachment of PEG moieties in series to a polypeptide, and more particularly to IFN-&#x3b2;.

Method for producing polyol-IFN-&#x3b2; conjugate

Method for treating disorders and diseases treatable with human fibroblast interferon

PEG-LHRH analog conjugates, where a PEG moiety is covalently bound to a serine residue of a LHRH analog, and methods for producing these conjugates are provided in the present invention. Also provided are a pharmaceutical composition and a method for treating pathologies in which LHRH analog administration is beneficial.

PEG-LHRH analog conjugates

PEG-LHRH analog conjugates, where a PEG moiety is covalently bound to a serine residue of a LHRH analog either directly or via a bifunctional linker molecule, such as an amino acid, and methods for producing these conjugates are provided in the present invention. Also provided are a pharmaceutical composition and a method for treating pathologies in which LHRH analog administration is beneficial.

PEG-IFN-&bgr; conjugates, where a PEG moiety is covalently bound to Cys of human IFN-&bgr;, are produced by a process of site specific PEGylation with a thiol reactive PEGylating agent. A pharmaceutical composition and a method for treating infections, tumors and autoimmune and inflammatory diseases are also provided. The invention further relates to a method for the stepwise attachment of PEG moieties in series to a polypeptide, and more particularly to IFN-&bgr;.

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Milton, MA, United States of America

Nabil El-Tayar