Abstract: The inventors have designed novel FSH mutants with increased glycosylation and longer half-lives for use in inducing folliculogenesis in human patients. The use of a FSH mutant preparation of the invention permits the use of lower cumulative doses of FSH to achieve the same or better clinical result.

Abstract: A method is described for the site-specific preparation of hGRF-PEG conjugates containing one or more PEG units (per mole of hGRF) covalently bound to Lys12 and/or Lys21 and/or N?, characterized in that the conjugation reaction between the hGRF peptide and activated PEG is carried out in solution and the desired hGRF-PEG conjugate can be purified by chromatography. The conjugates prepared by this method, as well as their use in the treatment, prevention of diagnosis of growth hormone deficiency, are also an object of the present invention.

Abstract: A process for the purification of recombinant human Chorionic Gonadotropin (hCG) from a sample of crude recombinant hCG in the supernatant of CHO cells comprises the combined use of ion-exchange chromatography and reverse phase HPLC. The ion-exchange chromatography is performed twice and the final use of a size exclusion chromatography allows the purification from any residual traces of contaminants. The specific bioactivity of the highly purified hCG obtained form the process is particularly high, amounting to about 25,000 IU/mg.

Abstract: Peptides and derivatives or analogs thereof are provided for having ?-amyloid aggregation inhibitory activity, useful in the treatment and prevention of diseases such as Alzheimer's disease, Dementia pugilistica (including head trauma), Hereditary Cerebral Haemorrhage with amyloidosis of the Dutch type (HCHWA-D) and vascular dementia with amyloid angiopathy.

Abstract: The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing various cancers, inflammation, septic shock, preterm labor, infertility, pain, and ischemia, and other diseases and disorders associated with MEK-1 and/or ERK-2 activation.

Abstract: Variants of homodimer-forming chemokines, such as human CCL2, having a single amino acid substitution in the dimerization interface that alters the pattern of hydrogen bonds and acting as an obligate monomer, can antagonize natural chemokines and have anti-inflammatory activity in vivo. These variants can be used as active ingredient in pharmaceutical compositions for the treatment of inflammatory, autoimmune, or infectious diseases.

Abstract: The present invention provides novel therapeutic molecules called Culling Fusion Proteins (CFPs) that allow the continuous removal of therapeutic targets from extracellular space by exploiting the endosome/lysosome intracellular degradation pathway, and the exocytotic pathway in a combined manner. The products of the invention, by appropriately utilizing the cellular endocytosis and exocytosis mechanism, can be recycled multiple times by cells to eliminate undesired molecules, therefore such therapeutic molecules can be administered at low concentration.

Abstract: The present invention relates generally to searching substructures in virtual combinatorial libraries. More precisely, it describes a method of operating a computer for searching substructures in large, non-enumerated virtual combinatorial libraries. Advantageously, the method can return matching products as non-enumerated substructures.

Abstract: The invention relates to an expression vector comprising the promoter of the mCMV-IE2 gene, or a functional expression promoting fragment thereof, and/or an enhancer of the mCMV-IE2 gene, or a functional expression enhancing fragment thereof, wherein expression vector does not contain any complete gene of the mCMV.

Abstract: The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstituted or substituted C1-C6 alkyl; G is an unsubstituted or substituted pyrimidinyl group.

Abstract: A 21-Hydroxy-6,19-oxidoprogesterone derivative of Formula (1): where R is —C(O)—CH2CH3, —C(O)—(CH2)2—COOH, —C(O)—(CH2)7—CH?CH—(CH2)7—COOH, or —C(O)—PO3Na2.

Abstract: The present invention relates to a method for improving homogeneity and/or secretion of a recombinant protein of interest expressed in mammalian cells by replacing the endogenous signal peptide sequence of the DNA encoding the protein of interest with that of human hGH. Specifically, the present invention relates to a method wherein the protein of interest is a subunit of the follicle stimulating hormone (FSH). The invention also relates to DNA expression vectors containing the sequence encoding such proteins of interest fused to the signal peptide sequence of the hGH and to cells harbouring such vectors.

Abstract: A gamma-lactam diene of Formula I: which is particularly useful as a medicament for the treatment of various disorders such as asthma, hypertension, osteoporosis, sexual dysfunction and fertility disorders.

Abstract: The present invention relates to cell-based assays useful for screening for modulators, such as inhibitors, of activated mutant KIT tyrosine kinase receptors, which are associated with mast cell-related disorders, such as mastocytosis and various types of cancer. The invention further provides for the treatment of mast cell-related disorders with an inhibitor identified by the screening method.

Abstract: The invention relates to the use of osteopontin, or of an agonist of osteopontin activity, for treatment or prevention of a neurologic diseases.

Abstract: A novel CC-chemokine binding protein is isolated from the saliva of Rhipicephalus sanguineus. Compounds prepared in accordance with the present invention can be used as anti-inflammatory compounds and in the treatment or prevention of CC-chemokine-related diseases.

Abstract: 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.

Abstract: The present invention is related to benzimidazole acetonitriles as well as to pharmaceutical formulations containing such benzimidazole acetonitriles of formula (I). Said benzimidazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS) (I). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles. G is pyrimidinyl; L is an amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom selected from N, O, S or L is an acylamino moiety; R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, carboxy, aminocarbonyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, cyano or hydroxy; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C2-C6alkenyl, C2-C6-alkynyl, or C1-C6-alkoxy.

Abstract: The present invention is related to a new synthesis for preparing pyrrolidine oximes of general formula (I). The compounds of formula (I) are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea.

Abstract: The present invention relates to methods of increasing protein expression levels whereby at least one amino acid in a protein amino acid sequence is substituted for the amino acid, proline. Preferably, the substitution occurs within 15 amino acids, more preferably within 10 amino acids and most preferably within 5 amino acids of a cysteine amino acid residue. The present invention not only includes methods for polypeptides with proline substitutions, but also polynucleotides with codon substitutions for which a codon for any amino acid, except proline, is substituted for a codon encoding for proline.