摘要:
The present application relates to a compound having a formula 1: B—R1-R2-M wherein B is a binding element for recognizing and binding a target; R1 is a first group of atoms for reacting with a functionality of the target so as to form a covalent bond with the target; R2 is a second group of atoms; R1 and R2 being such that the formation of the covalent bond between R1 and the target generates cleavage of the bond between R1 and R2 so as to free R2-M; and M is selected from the group consisting of a hydrogen atom and a pharmaceutically acceptable moiety. Alternatively, R1 and R2 can be inverted to form the formula II: B—R2-R1-M and being such that the formation of the covalent bond between R1 and the target generates cleavage of the bond between R1 and R2 so as to free R2-B.
摘要:
The present invention provides processes for the production of preformed albumin conjugates. In particular, the invention provides processes for the in-vitro conjugation of a therapeutic compound to recombinant albumin, wherein a therapeutic compound comprising a reactive group is contacted to recombinant albumin in solution to form a conjugate. The processes provide for conjugation to albumin species of increasing homogeneity. The resulting conjugate is purified by chromatography, in particular hydrophobic interaction chromatography comprising phenyl sepharose and butyl sepharose chromatography.
摘要:
The present invention relates to compounds comprising modified thrombopoietin peptides and conjugates of such modified peptides to serum components, typically serum proteins or peptides. The compounds and conjugates of the invention comprise a reactive group or a residue of a reactive group, which is covalently attached to a modified peptide, optionally through a linking group. The present invention also provides methods for the covalent attachment of a modified peptide to a serum protein or peptide to form a conjugate of the invention. The conjugates of the invention typically exhibit a longer in vivo circulating half-life compared to the corresponding unconjugated peptides. The conjugates of the invention also retain at least some of the biological activity of the unconjugated peptides, and typically exhibit increased biological activity compared to the unconjugated peptides. The present invention also provides methods for the treatment and prevention of a disease or disorder comprising the administration of one or more of the compounds or conjugates of the invention to a subject in need of such treatment or prevention.
摘要:
The present invention relates to a method for separating albumin conjugate from unconjugated albumin in a solution comprising albumin conjugate and unconjugated albumin by loading the solution onto a hydrophobic support equilibrated in aqueous buffer having a high salt content; applying to the support a gradient of decreasing salt concentration; and collecting the eluted albumin conjugate.
摘要:
The present invention provides processes for the production of preformed albumin conjugates. In particular, the invention provides processes for the in-vitro conjugation of a therapeutic compound to recombinant albumin, wherein a therapeutic compound comprising a reactive group is contacted to recombinant albumin in solution to form a conjugate. The processes provide for conjugation to albumin species of increasing homogeneity. The resulting conjugate is purified by chromatography, in particular hydrophobic interaction chromatography comprising phenyl sepharose and butyl sepharose chromatography.
摘要:
This invention relates to C34 peptide derivatives that are inhibitors of viral infection and/or exhibit antifusogenic properties. In particular, this invention relates to C34 derivatives having inhibiting activity against human immunodeficiency virus (HIV), respiratory synctial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) with long duration of action for the treatment of the respective viral infections.
摘要:
This invention relates to C34 peptide derivatives having improved aqueous solubility that are inhibitors of viral infection and/or exhibit antifusogenic properties. In particular, this invention relates to C34 derivatives having inhibiting activity against human immunodeficiency virus (HIV), respiratory synctial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) with long duration of action for the treatment of the respective viral infections.
摘要:
This invention relates to enfuvirtide peptide derivatives that are inhibitors of viral infection and/or exhibit antifusogenic properties. In particular, this invention relates to enfuvirtide derivatives having inhibiting activity against human immunodeficiency virus (HIV), respiratory syncytial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) with long duration of action for the treatment of the respective viral infections.
摘要:
The present invention relates to a method for separating albumin conjugate from unconjugated albumin in a solution comprising albumin conjugate and unconjugated albumin by loading the solution onto a hydrophobic support equilibrated in aqueous buffer having a high salt content; applying to the support a gradient of decreasing salt concentration; and collecting the eluted albumin conjugate.
摘要:
The present invention provides pharmaceutical formulations comprising insulinotropic peptide conjugates, particularly a conjugate of albumin to exendin-4, or a derivative thereof, and methods of administration thereof. The present invention also provides methods for treating diabetes and insulinotropic peptides related diseases or conditions by administering the pharmaceutical formulations described herein.