Abstract: The present invention relates to a peptide which consists of more than 50% of sequence sections of the formula -(An-Bm-Co)-, and to a conjugate containing the peptide and at least one covalently bonded active compound, and to a process for the preparation of the conjugate. The present invention furthermore relates to the use of the peptide and the conjugate for targeting of the kidney, and to a medicament comprising the peptide or conjugate.

Abstract: The present invention relates to a conjugate containing at least one kidney-selective carrier molecule and at least one active compound which has a protective action for the kidney against nephrotoxic active compounds, to a process for the preparation of the conjugate, to the use thereof for the protection of the kidney against nephrotoxic active compounds, and to a medicament comprising the conjugate.

Abstract: The present invention relates to conjugates comprising a protein and multivalent cell-penetrating peptide(s), each multivalent cell-penetrating peptide comprising at least two cell-penetrating peptides, wherein the multivalent cell-penetrating peptide(s) is/are covalently attached to the protein. The present invention furthermore relates to a method of generating the conjugates and to their medical uses, in particular their use in the diagnosis, prevention and/or treatment of diseases. The present invention relates to methods of diagnosis, prevention and/or treatment of diseases, comprising administering the conjugates of the invention to a patient.

Abstract: The present invention relates to ?-polylysine conjugates, in particular conjugates of ?-polylysine with compounds carrying carboxyl groups, and to the preparation and use thereof for targeting of the kidney.

Abstract: The present invention relates to hydrophobic modified peptides for the specific delivery of labels to the liver, preferably to hepatocytes, in vitro as well as in vivo. The present invention relates to pharmaceutical compositions comprising said hydrophobic modified peptide(s) and the label(s) to be specifically delivered to the liver. The present invention furthermore relates to the diagnostic use of the inventive hydrophobic modified peptides as well as to a method for the diagnosis of liver diseases or disorders.

Abstract: The present invention relates to hydrophobic modified peptides for the specific delivery of compounds to the liver, preferably to hepatocytes, in vitro as well as in vivo. The present invention relates to pharmaceutical compositions comprising said hydrophobic modified peptide(s) and the compound(s) to be specifically delivered to the liver. The present invention furthermore relates to the use of the inventive hydrophobic modified peptides as well as to a method for the prevention and/or treatment of liver diseases or disorders.

Abstract: The present invention relates to ?-polylysine conjugates, in particular conjugates of ?-polylysine with compounds carrying carboxyl groups, and to the preparation and use thereof for targeting of the kidney.

Abstract: The present invention relates to hydrophobic modified preS-derived peptides of hepatitis B virus (HBV) which are versatile vehicles for the specific delivery of compounds to the liver, preferably to hepatocytes, in vitro as well as in vivo. Any kind of compound, but in particular drugs, such as interferons, viral reverse transcriptase inhibitors or core assembly inhibitors, and/or labels can be specifically targeted to the liver and so be enriched in the liver. This liver targeting can further be used for the targeted diagnosis, prevention and/or treatment of liver diseases or disorders, such as hepatitis, malaria, hepatocellular carcinoma (HCC), as well as for the prevention of HAV, HBV, HCV and/or HDV infection. The present invention relates to pharmaceutical compositions comprising said hydrophobic modified preS-derived peptide(s) and the compound(s) to be specifically delivered to the liver.

Abstract: The present invention relates to hydrophobic modified preS-derived peptides of hepatitis B virus (HBV) which are derived from a HBV preS consensus sequence and are N-terminal preferably acylated and optional C-terminal modified. These hydrophobic modified preS-derived peptides of HBV are very effective HBV entry inhibitors as well as HDV entry inhibitors and are, thus, suitable for the inhibition of HBV and/or HDV infection, prevention of primary HBV and/or HDV infection as well as treatment of (chronic) hepatitis B and/or D. The present invention further relates to pharmaceutical and vaccine compositions comprising these hydrophobic modified preS-derived peptides of HBV.

Abstract: The present invention relates to a polyamine-substituted ligand for the preparation of a contrast agent derived from a chelating molecule selected from the group consisting of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and diethylentriamine-pentaacetic acid (DTPA), wherein at least one of the carboxylic groups of the chelating molecule is reacted with an amine of formula HNR1R2 to form an amide bond, wherein R1, R2 are independently selected from the group consisting of H; (CH2)n—NR3R4; and R5; R3, R4 are independently selected from the group consisting of H; (CH2)m—NR6R7; and (CH2)m-1—CH3; R6, R7 are independently selected from the group consisting of H; and (CH2)o-1—CH3; n, m, o are independently 2, 3, or 4; R5 is of formula and optionally at least one of the carboxylic groups of the chelating molecule is further reacted with a monoalkylamine having 1 to 18 carbon atoms to form an amide bond; provided that at least one of R1, R2 is other than H.

Abstract: The application relates to compounds that are suitable as labelable precursors for synthesis of 3?-[18F]fluoro-3?-deoxythymidine and that have formula (1), in which R denotes triphenylmethyl, triphenylmethyl substituted in the phenyl group, trialkylmethyl, triphenylsilyl, triphenylsilyl substituted in the phenyl group, or trialkylsilyl, R? denotes R1—SO2, where R1 is an unsubstituted or substituted C1 to C5 alkyl or an unsubstituted or substituted phenyl, and R? denotes C2 to C10 alkyloxycarbonyl, with the exception of 3-N-Boc-1-(3-O-nosyl-5-O-trityl-2-deoxy-?-D-lyxofuranosy The application also relates to a method for preparation of these compounds and to the use of the same for synthesis of 3?-[18F]fluoro-3?-deoxythymidine.

Abstract: The application relates to compounds that are suitable as labelable precursors for synthesis of 3′-[18F]fluoro-3′-deoxythymidine and that have formula (1), 1

Abstract: The present invention relates to a saccharide library with different saccharide-containing molecules, in which each of the molecules comprises a nuclear molecule with at least two functional groups and at least two saccharides. The invention also relates to the production of such a library and its use.

Abstract: The invention relates to dendrimers comprising an initiator core with at least two functional groups and at least two saccharides, a process for preparing sch dendrimers as well as uses thereof.

Abstract: The present invention is, generally, directed to the use of betulinic acid and derivatives thereof for the treatment of neuroectodermal tumors. The present invention is based on the discovery that betulinic acid and its derivatives are potent anti-neuroectodermal agents. As disclosed herein, betulinic acid and its derivatives are useful for the treatment of neuroectodermal tumors, including, due to its distinct mechanism of action, neuroectodermal tumors that are resistant to conventional chemotherapeutical agents. In addition to the new use of known compounds, the invention discloses novel compounds and pharmaceutical compositions for the treatment of neuroectodermal tumors.

Abstract: The present invention relates to an oligonucleotide conjugate, comprising: (a) an oligonucleotide at least part of whose sequence is complementary to an intracellular nucleic acid sequence; and (b) a somatostatin analog. The present invention also relates to a medicament containing this oligonucleotide conjugate, preferably for treating tumors in which the somatostatin receptor (SSTR) is overexpressed.

Abstract: Vibration damping means for a mounting post of a roll-over protection canopy of a heavy vehicle such as a tractor, earth mover, or the like. A hollow square post has slightly concave walls and slides over an upright square mounting stub on the vehicle, to which it is secured by a bolt which impales the post and the stub. A reduced upper end portion of the stub receives a vibration damping member which is in the form of a hollow square. The member has rounded corners which fit snugly in the corners of the post, and the span across opposite faces of the member is less than the internal width of the post so as not to bind in the post.