Abstract: This invention is directed to compounds useful as intermediates in the synthesis of lipoxin A4 analogs of the following formulas (I) and (II): wherein R1, R2, R3, R4 and R5 are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.
Abstract: The invention relates to substituted pyridines and to processes for preparation thereof, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of haematological disorders, preferably of leukopenia and neutropenia.
Abstract: The present invention is directed to novel pyrazolo-estrien and triazolo-estrien-derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by an estrogen receptor such as hot flashes, vaginal dryness, osteopenia, osteoporosis, hyperlipidemia, loss of cognitive function, degenerative brain diseases, cardiovascular diseases, cerebrovascular diseases, hormone sensitive cancers and hyperplasia (in tissues including breast, endometrium, and cervix in women and prostate in men), endometriosis, uterine fibroids, osteoarthritis; and as contraceptive agents either alone or in combination with a progestogen or progestogen antagonist. The compounds of the invention are selective estrogen receptor modulators.
Abstract: This invention relates to novel sulfone 2I3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis mediated disorders, as a sole agent or in combination with other active ingredients.
Abstract: The present application relates to novel 4-chromenonyl-1,4-dihydropyridines, process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
Abstract: The invention relates to novel forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate of the formula (I), in particular to the modification I, to processes for their preparation, to medicaments comprising them and to their use for fighting diseases.
Abstract: The present application relates to novel 3-cyanoalkyl- and 3-hydroxyalkyl-substituted indole derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of cardiovascular diseases.
Inventors:
Kai Thede, Elisabeth Woltering, Peter Kolkhof, Carsten Schmeck, Elisabeth Pook, Alexander Hillisch, Lars Bärfacker, Klemens Lustig, Dieter Lang, Martin Radtke, Rolf Grosser, Astrid Brüns, Michael Gerisch
Abstract: The invention relates to novel substituted dibenzoic acid derivatives of formula (I), wherein A represents a group of formula (II) or (III), to methods for producing the same, and to their use in the treatment and/or prophylaxis of diseases. The invention also relates to the use of said substances in the production of drugs for the treatment and/or prophylaxis of diseases, especially in the treatment and/or prevention of cardiovascular diseases.
Abstract: Use of 9?-estra-1,3,5(10)-triene derivatives of formula (I) for the prevention and treatment of intestinal cancer, in particular adenoma and adenocarcinoma of the duodenum, ileum, colon, and rectum.
Abstract: The present invention relates to pharmaceutical compositions and combinations for treating, preventing or managing heart failure and/or connected diseases therewith comprising 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide optionally combined with at least one additional therapeutic agent.
Abstract: The invention pertains to a compound for detecting cell death. According to the invention, the compound comprises a cyclic polyamine unit for the complexation of a bi- or trivalent metal ion. The compound of the invention may contain a reporting tag like fluorescein or a radioisotope including substituent.
Abstract: This invention relates to novel annellated 4-(indazolyl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
Abstract: The present invention relates to the use of selective inhibitors of coagulation factor Xa, in particular of oxazolidinones of the formula (I), for the treatment and/or prophylaxis of inflammatory conditions of the gastrointestinal tract such as inflammatory bowel disease (IBD) and celiac disease and/or disorders related to inflammatory bowel disease (IBD) and/or celiac disease such as thromboembolic events (including e.g. pulmonary embolism (PE), arterial and venous thrombosis, myocardial infarction, stroke) as well their use for the preparation of pharmaceutical drugs for the treatment and/or prophylaxis of inflammatory bowel disease (IBD) and/or celiac disease and/or disorders related to inflammatory bowel disease (IBD) and/or celiac disease such as thromboembolic events.
Abstract: The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-3-[2-fluoro-4-(3-oxomorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.
Inventors:
Hans-Georg Lerchen, Ursula Krenz, Michael Härter, Mark Jean Gnoth, Georges Von Degenfeld, Elke Dittrich-Wengenroth, Anja Buchmüller, Susanne Röhrig, Swen Allerheiligen, Elisabeth Perzborn, Christoph Gerdes, Karl-Heinz Schlemmer, Metin Akbaba
Abstract: The present application relates to novel substituted furopyrimidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases.
Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.
Abstract: The present invention relates to sulphone-substituted quinazoline derivatives of the formula (I), processes for their preparation and their use as a medicament for the treatment of various diseases.
Abstract: The present invention relates to solutions which are suitable for the perfusion and preservation of organs, organ parts, tissues or tissue parts of human or animal origin. The solutions suitable for this contain at least one active agent, which is selected from the group of NO-independent stimulators and activators of soluble guanylate cyclase. The invention furthermore relates to methods for producing the solutions according to the invention, and to the use of the solutions in various types of medical procedures, particularly in the field of transplantation medicine.
Abstract: The invention relates to methods for the determination of pharmacological properties of substances, such as, e.g., chemical substances. The invention also relates to methods and kits for use in the determination of the free fraction, fu, of pharmacologically active compounds in aqueous solutions and serum. The invention also relates to the above methods in which solid particles, coated with a lipophilic medium, are used.
Abstract: This invention relates to novel antibodies that bind with greater affinity to the factor VIIa/tissue factor (FVIIa/TF) complex than to tissue factor (TF) alone, do not compete for binding to TF with FVII and FX, an inhibit FX activation. The antibodies bind at the site of injury and prevent the initiation of thrombosis. The antibodies can be used to treat a variety of thrombotic conditions including but not limited to deep vein thrombosis, disseminated intravascular coagulation, and acute coronary syndrome.