Patent application number | Description | Published |
20090111769 | Antithrombotic Compound - The present invention relates compounds of the formula I: oligosaccharide-spacer-GpIIb/IIIa antagonist I, wherein the oligosaccharide is a negatively charged pentasaccharide residue of the structure (I), the charge being compensated by positively charged counterions; the spacer is an essentially pharmacologically inactive linking residue of a length of 15-50 atoms; the GpIIb/IIIa antagonist is a residue derived from tirofiban or an analogue thereof; or a pharmaceutically acceptable salt thereof or a prodrug or a solvate thereof. The compounds of the invention have antithrombotic activity and can be used in treating or preventing thrombotic diseases. | 04-30-2009 |
20100004186 | Antithrombotic Dual Inhibitors Comprising A Biotin Residue - The present invention relates compounds of the formula (I) oligosaccharide-spacer-A (1), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising two to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is an essentially pharmacologically inactive flexible linking residue having a chain length of 10 to 70 atoms; A is the residue —CH[NH—SO | 01-07-2010 |
20100029582 | Anticoagulant Antithrombotic Dual Inhibitors Comprising a Biotin Label - The present invention relates compounds of the formula: oligosaccharide-spacer-(GpIIb/IIIa antagonist), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising four to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-II mediated) anti-Xa activity per se; the spacer is a bond or an essentially pharmacologically inactive linking residue; the GpIIb/IIIa antagonist is a residue mimicking the RGD and/or K(QA)GD fragment of fibrinogen, comprising a carboxylate moiety and a basic moiety located within the residue at a distance of 10-20 Å from each other; or a pharmaceutically acceptable salt thereof or a prodrug or a solvate thereof; wherein the compound of formula I further comprises at least one covalent bond with a biotin label or an analogue thereof. The compounds of the invention have antithrombotic activity and can be used in treating or preventing thrombotic diseases. The antithrombotic activity of the compound of this invention can be neutralized in case of emergency upon administration of avidin, streptavidin and analogues thereof having high biotin affinity. | 02-04-2010 |
20120039843 | CONJUGATES OF A POLYPEPTIDE AND AN OLIGOSACCHARIDE - The present invention relates to conjugates of a polypeptide and an oligosaccharide, wherein the polypeptide is conjugated to at least one oligosaccharide-spacer residue, the oligosaccharide being a synthetic sulfated oligosaccharide comprising 4-18 monosaccharide units and per se having affinity to antithrombin III and the spacer being a bond or an essentially pharmacologically inactive flexible linking residue, or a pharmaceutically acceptable salt thereof. | 02-16-2012 |
20120238512 | ANTITHROMBOTIC DUAL INHIBITORS COMPRISING A BIOTIN RESIDUE - The present invention relates compounds of the formula (I) oligosaccharide-spacer-A (I), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising two to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is an essentially pharmacologically inactive flexible linking residue having a chain length of 10 to 70 atoms; A is the residue —CH[NH—SO | 09-20-2012 |
20140206627 | KISSPEPTIDE-PENTASACCHARIDE CONJUGATES - The invention relates to kisspeptide-pentasaccharide conjugates having the general formula (I) wherein Z | 07-24-2014 |
20140256725 | FSH RECEPTOR ANTAGONISTS - The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders. | 09-11-2014 |
20140350043 | FSH RECEPTOR ANTAGONISTS - The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders. | 11-27-2014 |