Patent classifications
C07D207/46
Method for obtaining novel derivatives of naphthalene for the in vivo diagnosis of alzheimer's disease
This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R.sub.1:-alkylenyl-C(O)NH-alkylenyl-R.sub.3, -alkylenyl-C(O)O—R.sub.4, R.sub.3:—COOH, —OH, —SH, —NH.sub.2, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R.sub.4: H, succinimidyl group, R.sub.2: —H,-alkyl. In II: R.sub.1: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R.sub.2: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN).sub.2, —HC═CHNO.sub.2, -alkylenyl-NH.sub.2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.
Method for obtaining novel derivatives of naphthalene for the in vivo diagnosis of alzheimer's disease
This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R.sub.1:-alkylenyl-C(O)NH-alkylenyl-R.sub.3, -alkylenyl-C(O)O—R.sub.4, R.sub.3:—COOH, —OH, —SH, —NH.sub.2, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R.sub.4: H, succinimidyl group, R.sub.2: —H,-alkyl. In II: R.sub.1: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R.sub.2: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN).sub.2, —HC═CHNO.sub.2, -alkylenyl-NH.sub.2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.
OLIGOMER EXTENDED INSULIN-FC CONJUGATES AND THEIR MEDICAL USE
This invention is in the field of protein conjugates. More specifically the invention relates to oligomer extended insulins with covalently attached Fc monomer polypeptides, for use in the treatment of a metabolic disorder or condition, and to methods of producing such oligomer extended insulin-Fc conjugates. The invention also relates to a novel Fc fragment, to intermediate products, and to the use of such intermediate products in processes for the synthesis of the oligomer extended insulin-Fc conjugates of the invention. Finally the invention provides pharmaceutical compositions comprising the oligomer extended insulin-Fc conjugates of the invention, and relates to the use of such compositions for the treatment or prevention of medical conditions relating to metabolic disorders or conditions.
OLIGOMER EXTENDED INSULIN-FC CONJUGATES AND THEIR MEDICAL USE
This invention is in the field of protein conjugates. More specifically the invention relates to oligomer extended insulins with covalently attached Fc monomer polypeptides, for use in the treatment of a metabolic disorder or condition, and to methods of producing such oligomer extended insulin-Fc conjugates. The invention also relates to a novel Fc fragment, to intermediate products, and to the use of such intermediate products in processes for the synthesis of the oligomer extended insulin-Fc conjugates of the invention. Finally the invention provides pharmaceutical compositions comprising the oligomer extended insulin-Fc conjugates of the invention, and relates to the use of such compositions for the treatment or prevention of medical conditions relating to metabolic disorders or conditions.
Sulfoxide-based reagent for mass spectrometry
The present disclosure relates to sulfoxide-based reagents suitable in the mass spectrometric determination of analyte molecules such as peptides as well as adducts of such reagents and analyte molecules and applications of the reagents and adducts. Further, the present disclosure relates to methods for the mass spectrometric determination of analyte molecules.
Sulfoxide-based reagent for mass spectrometry
The present disclosure relates to sulfoxide-based reagents suitable in the mass spectrometric determination of analyte molecules such as peptides as well as adducts of such reagents and analyte molecules and applications of the reagents and adducts. Further, the present disclosure relates to methods for the mass spectrometric determination of analyte molecules.
Isobaric mass labels
The present invention relates to a set of two or more mass labels, wherein each mass label comprises the formula:
X-L-M-Re
wherein X is a reporter moiety having an exact mass, L is a bond cleavable by collision in a mass spectrometer, M is a mass modifier, and Re is a) a reactive functionality for attaching the mass label to an analyte or b) the analyte, wherein each mass label in the set has an integer mass, wherein each mass label in the set has the same integer mass, and wherein the set comprises two or more subsets of mass labels, each subset comprising one, two or more mass labels, and wherein, when the subset comprises two or more mass labels, the exact mass of the reporter moiety X of each mass label in the subset is different from the exact mass of the reporter moiety X of the mass labels in the same subset and in all other subsets, and wherein each mass label is distinguishable by mass spectrometry.
Isobaric mass labels
The present invention relates to a set of two or more mass labels, wherein each mass label comprises the formula:
X-L-M-Re
wherein X is a reporter moiety having an exact mass, L is a bond cleavable by collision in a mass spectrometer, M is a mass modifier, and Re is a) a reactive functionality for attaching the mass label to an analyte or b) the analyte, wherein each mass label in the set has an integer mass, wherein each mass label in the set has the same integer mass, and wherein the set comprises two or more subsets of mass labels, each subset comprising one, two or more mass labels, and wherein, when the subset comprises two or more mass labels, the exact mass of the reporter moiety X of each mass label in the subset is different from the exact mass of the reporter moiety X of the mass labels in the same subset and in all other subsets, and wherein each mass label is distinguishable by mass spectrometry.
METHODS AND COMPOSITIONS RELATING TO SYNTHETIC BETA-1,6 GLUCOSAMINE OLIGOSACCHARIDES
The invention relates to the compositions of synthetic oligo-γ-(1.fwdarw.6)-2-amino-2-deoxy-D-glu-copyranosides conjugated to carriers, and methods for making and use same.
METHODS AND COMPOSITIONS RELATING TO SYNTHETIC BETA-1,6 GLUCOSAMINE OLIGOSACCHARIDES
The invention relates to the compositions of synthetic oligo-γ-(1.fwdarw.6)-2-amino-2-deoxy-D-glu-copyranosides conjugated to carriers, and methods for making and use same.