Abstract: This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates.

Abstract: This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates.

Abstract: New aminooxylipids of general formula I, wherein n1=5-30 and X is polymethylene linker of the general formula II where n2=2-10, or X is polyethylene glycol linker of the general formula III, wherein n3=1-14 are provided. A method of preparation of the aminooxylipids of general formula I characterized in that the acylation of N-tert-butoxycarbonyl-polymethylenediamine {(CH3)3C—O—(C?O)—HN—(CH2)n—NH2, n=2-13}, or N-tert-butoxycarbonyl-polyethyleglycoldiamine {(CH3)3C—O—(C?O)—HN—(CH2)2—[O—(CH2)]n—O—(CH2)2NH2, n=1-14} with in position C(2) symmetrically branched fatty acids of general formula IV, wherein n1=5-30, in the presence of condensation reagent, or from acid of general formula IV derived acylchloride of general formula V wherein n1=5-30, produces N-Boc-aminolipids of general formula VI, wherein n1=5-30 a X is polymethylene linker of the general formula II or X is polyethylene glycol linker of the general formula III.

Abstract: The present invention relates to novel insulin derivatives and their use in the treatment or prevention of medical conditions relating to diabetes. The insulin derivatives are glucose sensitive and display glucose-sensitive albumin binding. The invention also relates to novel intermediates. Finally, the invention provides a pharmaceutical composition comprising the insulin derivatives of the invention and the use of such a composition in the treatment or prevention of medical conditions relating to diabetes.

Abstract: This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates.

Abstract: This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates. The diboron compounds are characterized by formula (I), which is: R1-X—R2, and wherein “X” is a mono- to multiatomic linker and where R1 and R2, which may be identical or different, each represents a group of Formula (11a) or (IIb) Also described are diboron conjugates represented by the general Formula (I?), which is: R1?-X?—R2?, in which either the moeities R1? or R2? or X? carry a drug that is covalently attached to the diboron compound.

Abstract: New aminooxylipids of general formula I, wherein n1=5-30 and X is polymethylene linker of the general formula II where n2=2-10, or X is polyethylene glycol linker of the general formula III, wherein n3=1-14 are provided. A method of preparation of the aminooxylipids of general formula I characterized in that the acylation of N-tert-butoxycarbonyl-polymethylenediamine {(CH3)3C—O—(C?O)—HN—(CH2)n—NH2, n=2-13}, or N-tert-butoxycarbonyl-polyethyleglycoldiamine {(CH3)3C—O—(C?O)—HN—(CH2)2—[O—(CH2)]n—O—(CH2)2NH2, n=1-14} with in position C(2) symmetrically branched fatty acids of general formula IV, wherein n1=5-30, in the presence of condensation reagent, or from acid of general formula IV derived acylchloride of general formula V wherein n1=5-30, produces N-Boc-aminolipids of general formula VI, wherein n1=5-30 a X is polymethylene linker of the general formula II or X is polyethylene glycol linker of the general formula III.

Abstract: This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates. The diboron compounds are characterized by formula (I), which is: R1-X—R2, and wherein “X” is a mono- to multiatomic linker and where R1 and R2, which may be identical or different, each represents a group of Formula (11a) or (IIb) Also described are diboron conjugates represented by the general Formula (I?), which is: R1?-X?—R2?, in which either the moeities R1? or R2? or X? carry a drug that is covalently attached to the diboron compound.

Abstract: The present invention provides a method for synthesis and binding methods of pentapendant enantiomer-pure chelators of formula (VII) wherein R1, R2, R3, R4 are groups forming an adequate enantiomer of the chelator; and X1-X5, Y1-Y5, Z1-Z5 each individually forming pendant chelating groups.

Abstract: The present invention relates to novel processes for the synthesis of polyazamacrocycle derivatives. Furthermore, the present invention relates to novel polyazamacrocycle derivatives as well as novel intermediates for the synthesis of said polyazamacrocycle derivatives.