Abstract: The compounds and the synthesis of [F-18]-labeled L-glutamic acid, [F-18]-labeled L-glutamate, their derivatives as set forth in formula (I) and their uses are described.
Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.
Inventors:
Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
Abstract: The invention provides pharmacological compositions comprising a stimulator or activator of the soluble guanylate cyclase alone (sGC) or in combination with a PDE5 inhibitor for the treatment of urological disorders comprising of Benign Prostate Syndrome (BPS), Benign Prostate Hyperplasia (BPH), Benign Prostate Enlargement (BPE), Bladder Outlet Obstruction (BOO), Lower Urinary Tract Symptoms (LUTS), genitourinary disorders comprising neurogenic bladder syndrome (OAB) and (IC), urinary incontinence (UI) like mixed-, urge-, stress-, or overflow incontinence (MUI, UUI, SUI, OUI) and pelvic pain (PP).
Abstract: This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating respiratory diseases associated with influenza A viruses, such as for example H5N1 and its mutations. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
Abstract: The invention relates to substituted [(phenylethanoyl)amino]benzamides and methods for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of inflammatory disorders such as, for example, cutaneous, respiratory tract and cardiovascular disorders such as, for example, arteriosclerosis and coronary heart disease.
Inventors:
Ulf Brüggemeier, Petros Gatsios, Mark Meininghaus, Leila Telan, Elisabeth Woltering, Martina Wuttke, Hartmut Beck, Nils Griebenow, Frank Süβmeier, Niels Svenstrup, Axel Kretschmer, Marcus Bauser, Johannes Köbberling, Wahed Moradi, Siegfried Zaiss, Claudia Hirth-Dietrich, Barbara Albrecht
Abstract: The invention relates to combinations of A) oxazolidinones of formula (I) and B) other active ingredients, to a method for producing said combinations and to the use thereof as medicaments, in particular for the treatment and/or prophylaxis of thrombo-embolic diseases.
Abstract: The invention relates to novel heterocyclic derivatives of the general formula (I), processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction, and heart failure development.
Abstract: The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
Inventors:
Swen Allerheiligen, Marcus Bauser, Dirk Heimbach, Stefan Heitmeier, Mark Jean Gnoth, Christoph Gerdes, Georges Von Degenfeld, Susanne Röhrig, Ulrich Rester, Elke Dittrich-Wengenroth, Uwe Saatman, Adrian Tersteegen
Abstract: The invention provides pharmacological compositions comprising PDE-5 inhibitors for the treatment of hearing impairment i.e. hearing loss and tinnitus. The invention also provides methods of screening for such PDE-5 inhibitors for use in the preparation of medicaments for the treatment of hearing impairment i.e. hearing loss and tinnitus.
Abstract: This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.
Abstract: The present invention relates to the use of a specific compound, as described in detail below, having a high affinity to the peripheral benzodiazepine receptor for imaging cardiac and cardiovascular diseases for which inflammation and/or mitochondrial dysfunction and any other pathophysiological process leading to PBR activation are major contributing factor.
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: The invention relates to a preparation for restenosis prevention. The preparations for restenosis prevention known as yet do not reach sufficient active agent concentrations in the affected sections of the vascular walls as higher doses cause undesirable side effects. The present invention is a preparation to which at least one antihyperplastic agent is added that has a distribution ratio between butanol and water ?0.5. The lipophilic active agent is absorbed by the vascular wall fast and in sufficient quantity. The preparation may be a liquid that can pass through capillaries and may contain a contrast agent so that the active agent is transferred into the vascular wall without any additional effort while the usually required contrast radiograms are taken. The preparation may also be applied to a catheter.
Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly hyperproliferative diseases such as cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly hyperproliferative diseases such as cancer.
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: Compounds of a certain formula I in which R1, R2, R3 and R4 have the meanings indicated in the description are novel compounds expected to be useful in the therapy of (hyper)proliferative diseases and/or disorders responsive to induction of apoptosis.
Abstract: The present invention relates to a quinazoline derivative having the general formula (A): in which R1, R2, X, Y and Z are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).
Abstract: The invention relates to heteroaryloxy-substituted phenylaminopyrimidines, to methods for the production thereof, and to the use of the same for producing medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular diseases. The inventive compounds inhibit Rho-Kinase.
Abstract: The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
Inventors:
Martin Hendrix, Frank-Gerhard Böβ, Christina Erb, Timo Fleβner, Marja van Kampen, Joachim Luithle, Christoph Methfessel, Welf-Burkhard Wiese
Abstract: The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17?-hydroxy steroid dehydro-genase type 1.
Inventors:
Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Gabriele Moeller, Dominga Deluca, Jerzy Adamski, Walter Elger, Birgitt Schneider