Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B, Y and Z have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treatment and prevention of diseases associated with microglia activation as well as pharmaceutical preparations that contain these compounds
Type:
Grant
Filed:
February 24, 2005
Date of Patent:
March 27, 2007
Assignee:
Schering AG
Inventors:
Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Monning, Herbert Schneider
Abstract: The process for making crystals of a 11 ?-benzaldoxim-estra-4,9-diene derivative having an average particle size of from 3 ?m to 25 ?m and a maximum particle size of 100 ?m, includes subjecting a supersaturated solution containing a special 11?-benzaldoxim-estra-4,9-diene derivative of formula (I) to a wet milling by a wet milling apparatus while crystallizing, In order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described and are part of the invention.
Abstract: 17-methylene-4-azasteroid compounds of formula I: wherein R20 denotes fluoro, chloro or bromo R20a denotes hydrogen, R10 and R4 each denote a hydrogen atom or a methyl group, and R1 and R2 each denote a hydrogen atom or together denote an additional bond, are useful for treating diseases or conditions caused by excessive androgen levels, such as acne, prostate diseases, alopecia and hirsutism, as well as gynecological conditions. Methods of synthesizing the new 17-methylene-4-azasteroid compounds are described.
Type:
Grant
Filed:
August 28, 2002
Date of Patent:
March 6, 2007
Assignee:
Schering AG
Inventors:
Bernd Menzenbach, Peter Droescher, Alexander Hillisch, Walter Elger, Hans-Udo Schweikert, Klaus Schoellkopf
Abstract: The invention provides formulations of GM-CSF that comprise chelating agents. The chelating agents stabilize the GM-CSF against N-terminal degradation and allow for rapid absorption of GM-CSF upon administration.
Type:
Application
Filed:
June 27, 2006
Publication date:
February 22, 2007
Applicant:
Schering AG
Inventors:
Dean Pettit, Claudia Jochheim, Catherine Scholz, Andreas Baumann
Abstract: A method for in vitro screening a group of test substances for a ligand using two assay systems, i.e. a cellular or tissue assay system and an enzymatic assay system, is described. First, those test substances are selected which have transcriptional ER-mediated activity measured by an ER-driven reporter gene in the cellular or tissue assay system with an EC50(ER)(half-maximally effective ligand concentration) lower than or equal to 10 nmol/l. Then in an enzymatic assay system the selected test substances having the required transcriptional ER-mediated activity are tested by measuring a physical-chemical interaction (recruitment) of SRC-1 and the ER in the presence of the test substances. The selected ligand activates the ER and induces interaction with the co-present SRC-1 with an E50(ER+SRC) higher than or equal to 100 nmol/l.
Type:
Grant
Filed:
November 20, 2001
Date of Patent:
January 23, 2007
Assignee:
Schering AG
Inventors:
Vladimir Patchev, Youriy Mitev, Siegmund Wolf, Gernot Langer
Abstract: A new process for the production of triiodotrimesic acid that is used as an intermediate product for the synthesis of x-ray contrast media is described.
Type:
Grant
Filed:
July 14, 2004
Date of Patent:
January 23, 2007
Assignee:
Schering AG
Inventors:
Heiko Schirmer, Ulrich Niedballa, Hannelore Niedballa, Johannes Platzek, Jose Luis Martin, Juan R. Harto, Jose Carretero
Abstract: The invention relates to macrocyclic metal complexes and their production and use for the production of conjugates with biomolecules. The conjugates are suitable as contrast media in NMR diagnosis and radiodiagnosis as well as for radiotherapy. High relaxivity is achieved by a special liganding of macrocyclic compounds, and a fine-tuning of the relaxivity is made possible.
Type:
Grant
Filed:
July 19, 2002
Date of Patent:
January 16, 2007
Assignee:
Schering AG
Inventors:
Johannes Platzek, Heribert Schmitt-Willich, Günther Michl, Thomas Frenzel, Detlev Sülzle, Hans Bauer, Bernd Radüchel, Hanns-Joachim Weinmann, Heiko Schirmer
Abstract: VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g.
Type:
Grant
Filed:
July 31, 2003
Date of Patent:
December 12, 2006
Assignee:
Schering AG
Inventors:
Andreas Huth, Ludwig Zorn, Martin Kruger, Stuat Ince, Karl-Heinz Thierauch, Andreas Menrad, Martin Haberey, Holger Hess-Stumpp
Abstract: This invention describes the new 17?-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with bases. The new compounds have an extraordinary strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
Type:
Grant
Filed:
September 24, 2004
Date of Patent:
December 12, 2006
Assignee:
Schering AG
Inventors:
Wolfgang Schwede, Arwed Cleve, Ulrich Klar, Gunter Neef, Kristof Chwalisz, Martin Schneider, Ulrike Fuhrmann, Holger Heb-Stumpp
Abstract: The process for making steroid crystals having a predetermined average particle size of from 1 ?m to 25 ?m and a maximum particle size that does not exceed a predetermined maximum value of 100 ?m, includes subjecting a supersaturated solution containing a steroid to a wet milling by wet milling apparatus while crystallizing, in order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described.
Abstract: Benzocycloheptenes of formula (I), in which R1, R2 and Y have the meanings that indicated herein, exhibit selective estrogenic activity on bones and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis:
Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula I in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z are as defined in the specification. The compounds are useful in treating malignant tumours, for example, ovarian, stomach, colon, breast, adeno-, head and neck carcinomas, acute lymphocytic and myelocytic leukemia. In addition, these compounds are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases such as psoriasis and arthritis. Methods of use and preparation of the compounds are also described.
Type:
Grant
Filed:
May 1, 2000
Date of Patent:
October 24, 2006
Assignee:
Schering AG
Inventors:
Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann, Jens Hoffmann, Rosemarie Lichtner
Abstract: The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.
Type:
Grant
Filed:
November 9, 1999
Date of Patent:
October 17, 2006
Assignees:
Schering AG, Novartis AG
Inventors:
Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch, Guido Bold, Paul William Manley, Pascal Furet, Jeanette Marjorie Wood, Jürgen Mestan, Jose Brüggen, Stefano Ferrari, Martin Krüger, Eckhard Ottow, Andreas Menrad, Michael Schirner
Abstract: The invention relates to vitamin D derivatives of general formula I, process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents.
Type:
Grant
Filed:
November 26, 2002
Date of Patent:
October 3, 2006
Assignee:
Schering AG
Inventors:
Andreas Steinmeyer, Katica Schwarz, Claudia Giesen, Martin Haberey, Marianne Fähnrich
Abstract: The invention relates to compounds of general formula I and their use for the production of pharmaceutical agents for treatment and prophylaxis of diseases that coincide with inflammatory, allergic and/or proliferative processes.
Type:
Grant
Filed:
December 19, 2003
Date of Patent:
September 26, 2006
Assignee:
Schering AG
Inventors:
Norbert Schmees, Manfred Lehmann, Hartmut Rehwinkel, Peter Strehlke, Stefan Jaroch, Heike Schaecke, Amdt J. G Schottelius
Abstract: The invention relates to quinoline and isoquinoline derivatives of general formula I and a process for their production, and their use as inflammation inhibitors.
Type:
Grant
Filed:
February 17, 2005
Date of Patent:
September 19, 2006
Assignee:
Schering AG
Inventors:
Stefan Jaroch, Manfred Lehmann, Norbert Schmees, Markus Berger, Hartmut Rehwinkel, Konrad Krolikiewicz, Werner Skuballa, Heike Schaecke, Arndt. J. G. Schottelius
Abstract: The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The new compounds are 16?- and 16?-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.
Type:
Grant
Filed:
February 4, 2000
Date of Patent:
September 19, 2006
Assignee:
Schering AG
Inventors:
Hermann Kuenzer, Rudolf Knauthe, Monika Lessl, Karl-Heinrich Fritzemeier, Christa Hegele-Hartung, Ulf Boemer, Gerd Mueller, Dirk Kosemund
Abstract: New tubular vascular implants (stents) that consist of biocompatible, thermoplastic material that have a shape memory and that contain at least one active ingredient are described. In addition, a process for their production and their use as vascular implants for prophylaxis of restenosis are described.
Type:
Grant
Filed:
November 21, 2001
Date of Patent:
August 8, 2006
Assignee:
Schering AG
Inventors:
Gesine Hildebrand, Johannes Tack, Helmut Kaeufer, Hans-Martin Wache, Thomas Mueller, Peter Ewert