Abstract: The invention relates to dihydroquinazolines and methods for the production thereof, the use thereof in the treatment and/or prophylaxis of diseases, in addition to the use thereof in the production of medicaments in the treatment and/or prophylaxis of diseases, especially for use as anti-viral agents, especially against cytomegalo viruses.
Inventors:
Tobias Wunberg, Judith Baumeister, Ulrich Betz, Mario Jeske, Gerald Kleymann, Thomas Lampe, Susanne Nikolic, Jürgen Reefschläger, Rudolf Schohe-Loop, Frank Süβmeier, Holger Zimmermann, Rolf Grosser, Kerstin Henninger, Guy Hewlett, Jörg Keldenich, Thomas Krämer, Peter Nell, Tse-I Lin
Abstract: The present invention relates to novel perfluorinated precursors for the production of F-18 labeled radiotracers for Positron Emission Tomography (PET) and processes for radiolabeling and purification using these precursors. The invention also comprises radiopharmaceutical kits using these precursors and processes.
Abstract: The present invention is directed to a polynucleotide sequence of the novel G-Protein Coupled Receptors EP3-11 OR EP3-12. The present invention provides polynucleotide sequences comprising the nucleic acid sequence SEQ ID NO: 20 or SEQ ID NO: 21 or nucleic acid sequences that hybridize to SEQ ID NO: 20 or SEQ ID NO: 21 or its complimentary strand having at least 40% sequence identity. The invention also provides the human EP3-11 or EP3-12 as targets for the identification of compounds useful for the treatment and prevention of cardiovascular diseases, inflammation, reproduction disorders and cancer as a result of relative quantification of the mRNA distribution in different human tissues by expression profiling. The invention also provides assays for the identification of compounds modulating EP3-11 or EP3-12.
Abstract: The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
Abstract: The present application relates to novel 3-phenylpropionic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.
Inventors:
Thomas LAMPE, Michael HAHN, Johannes-Peter STASCH, Karl-Heinz SCHLEMMER, Frank WUNDER, Sherif EL SHEIKH, Volkhart Min-Jian LI, Eva-Maria BECKER, Friederike STOLL, Andreas KNORR
Abstract: The present invention relates to processes for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate, i.e. the compound of the formula (I) and to a process for purifying the crude product of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate sulphinyldimethane (1:2) of the formula (II) is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
Abstract: The present application relates to novel substituted aryloxazole derivatives, a method for the production thereof, the use thereof for the treatment and/or prophylaxis of diseases and the use thereof for the production of drugs for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.
Inventors:
Peter Nell, Walter Hübsch, Barbara Albrecht-Küpper, Jorg Keldenich, Alexandros Vakalopoulos, Frank Süssmeier, Katja Zimmermann, Dieter Lang, Daniel Meibom
Abstract: The present application relates to novel, cyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.
Inventors:
Thomas Lampe, Eva-Maria Becker, Raimund Kast, Hartmut Beck, Mario Jeske, Joachim Schuhmacher, Friederike Stoll, Martina Klein, Metin Akbaba, Andreas Knorr, Johannes-Peter Stasch, Lars Bärfacker, Alexander Hillisch, Gunter Karig, Mark Meininghaus, Karl-Heinz Schlemmer, Rudolf Schohe-Loop
Abstract: The invention relates to the use of a radioactively labelled molecule specifically binding to ED-B fibronectin in a method of treatment for patients with Hodgkin lymphoma, in particular primary refractory Hodgkin lymphoma or recurrent Hodgkin lymphoma after chemotherapy, and for Hodgkin lymphoma patients scheduled for primary combined-modality therapy.
Abstract: The present invention relates to novel 1,4-diarylpyrimido[4,5-d]pyridazine-2,5-dione derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
Abstract: The present invention provides novel and advantageous processes for preparing and purifying chemical compounds such as pharmaceuticals. The processes comprise a nucleophilic substitution reaction with a moiety X wherein the leaving group L of a substrate S in the reaction is covalently attached to a purification moiety M. This concept offers a convenient and lime-saving way to purity the desired product S-X from non-reacted precursors S-L-M and by-products L-M.
Inventors:
John Cyr, Ananth Srinivasan, Mathias Berndt, Keith Graham, Dae Yoon Chi, Byoung Se Lee, So Young Chu, Song-Yi Lim, Sang Ju Lee, Jin-Sook Ryu, Seung Jun Oh
Abstract: The invention provides CTGF which is associated with the cardiovascular diseases and hematological diseases. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular diseases and hematological diseases. The invention also features compounds which bind to and/or activate or inhibit the activity of CTGF as well as pharmaceutical compositions comprising such compounds.
Inventors:
Stefan Golz, Holger Summer, Andreas Geerts, Ulf Brüggemeier, Barbara Albrecht-Küpper, Martina Klein, Sonja Steppan, Peter Ellinghaus, Donatella D'Urso, Michael Seewald, Hendrik Milting
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 drug delivery systems in the form of thin water-soluble films (wafers), which contain estradiol, or derivatives thereof, in low amounts. The wafers of the present invention are suitable for treating, alleviating or preventing a physical condition in a female mammal caused by insufficient endogenous levels of estrogen.
Abstract: The present application relates to novel 2-aminoethoxyacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.
Abstract: The invention provides pharmacological compositions comprising a stimulator or activator of the soluble guanylate cyclase (sGC) either alone or in combination for the treatment of hearing impairment i.e. hearing loss and tinnitus.
Abstract: This invention is directed to lipoxin A4 analogs of the following formula (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: This invention relates to novel 2,3-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 disorders, as a sole agent or in combination with other active ingredients.
Abstract: An injection device for a syringe, having a syringe body, a cannula with a needle, a plunger with a plunger rod, and an injection carriage for displacing the syringe body and the plunger, comprises at least one actuating element that acts on the injection carriage to carry out the injection procedure. The actuating element (120, 220, 320) cooperates with components which withdraw the needle (108, 208, 308) from the puncture site once the injection procedure has been completed, using a return stroke (H3) that is applied to the injection carriage. A single, targeted linear movement inserts the needle to a defined depth, injects the medicament and, once the injection has been completed, produces a return stroke which allows the needle to be withdrawn into the housing and thus out from the puncture site.