Patent classifications
C07H15/207
COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF AS INHIBITORS OF RAN GTPase
Compounds of general formula IA, IB and IC outlined below, including pharmaceutically acceptable salts, solvates and hydrates thereof. Such compounds and pharmaceutical compositions comprising them may be used in medical conditions involving Ran GTPase.
##STR00001##
Use of cyanoglucosides and pharmaceutical formulations thereof in the treatment of diabetes
The present invention relates to the use of cyanoglucoside according to formula (I) and formulations thereof in the prevention and/or treatment of diabetes and/or metabolic syndrome; wherein R.sub.1, R.sub.2 and R.sub.3 are independently selected from an optionally substituted mono- or di-saccharide, —O—R.sub.4, —O—C(O)—R.sub.4 and halogen, such as Cl, F or Br, wherein R.sub.4 is selected from H, alkyl, such as methyl, as well as tautomers, geometrical isomers, optically active forms, pharmaceutically acceptable salts and pharmaceutically active derivative thereof.
Use of cyanoglucosides and pharmaceutical formulations thereof in the treatment of diabetes
The present invention relates to the use of cyanoglucoside according to formula (I) and formulations thereof in the prevention and/or treatment of diabetes and/or metabolic syndrome; wherein R.sub.1, R.sub.2 and R.sub.3 are independently selected from an optionally substituted mono- or di-saccharide, —O—R.sub.4, —O—C(O)—R.sub.4 and halogen, such as Cl, F or Br, wherein R.sub.4 is selected from H, alkyl, such as methyl, as well as tautomers, geometrical isomers, optically active forms, pharmaceutically acceptable salts and pharmaceutically active derivative thereof.
Carbohydrate ligands that bind to IgM antibodies against myelin-associated glycoprotein
The invention relates to carbohydrate ligands presenting the minimal Human Natural Killer-1 (HNK-1) epitope that bind to anti-MAG (myelin-associated glycoprotein) IgM antibodies, and their use in diagnosis as well as for the treatment of anti-MAG neuropathy. In particular, the invention relates to disaccharides of formula (I) and (II) wherein Z is optionally substituted phenyl, heteroaryl, arylcarbonyl, or heteroarylmethyl, and to therapeutically acceptable polymers comprising a multitude of substituents of formula (I) and/or formula (II), wherein Z is a bifunctional linker connecting the disaccharides to the polymer backbone. ##STR00001##
Carbohydrate ligands that bind to IgM antibodies against myelin-associated glycoprotein
The invention relates to carbohydrate ligands presenting the minimal Human Natural Killer-1 (HNK-1) epitope that bind to anti-MAG (myelin-associated glycoprotein) IgM antibodies, and their use in diagnosis as well as for the treatment of anti-MAG neuropathy. In particular, the invention relates to disaccharides of formula (I) and (II) wherein Z is optionally substituted phenyl, heteroaryl, arylcarbonyl, or heteroarylmethyl, and to therapeutically acceptable polymers comprising a multitude of substituents of formula (I) and/or formula (II), wherein Z is a bifunctional linker connecting the disaccharides to the polymer backbone. ##STR00001##
AMINO ACID DERIVATIVE OF GLUCOSAMINE STIMULATING EXTRACELLULAR MATRIX SYNTHESIS AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
The present patent application relates to the use of an innovative amino acid derivative of glucosamine having the Formula 1 of the general structure which follows, or of a pharmaceutical composition which contains it as a single active ingredient or in association with one or more further active ingredients for the preparation of a medicament for the treatment or prophylaxis of diseases involved mainly with the regulation of the turnover of macromolecules that make up the ECM of connective tissue in general and more specifically of the cartilage.
##STR00001##
AMINO ACID DERIVATIVE OF GLUCOSAMINE STIMULATING EXTRACELLULAR MATRIX SYNTHESIS AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
The present patent application relates to the use of an innovative amino acid derivative of glucosamine having the Formula 1 of the general structure which follows, or of a pharmaceutical composition which contains it as a single active ingredient or in association with one or more further active ingredients for the preparation of a medicament for the treatment or prophylaxis of diseases involved mainly with the regulation of the turnover of macromolecules that make up the ECM of connective tissue in general and more specifically of the cartilage.
##STR00001##
Quinone methide analog signal amplification
Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step.
Quinone methide analog signal amplification
Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step.
Highly potent multimeric e-selectin antagonists
Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, highly potent multimeric E-selectin antagonist are desorbed and pharmaceutical compositions comprising at least one of the same.