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:
December 1, 2006
Date of Patent:
April 8, 2008
Assignee:
Schering AG
Inventors:
Heiko Schirmer, Hannelore Niedballa, legal representative, Johannes Platzek, Jose Luis Martin, Juan R. Harto, Jose Carretero, Ulrich Niedballa
Abstract: The invention relates to the use of perfluoroalkyl-containing metal complexes that have a critical micelle formation concentration <10?3 mol/l, a hydrodynamic micelle diameter (2 Rh)>1 nm and a proton relaxivity in plasma (R1)>10 l/mmol·s as contrast media in MR imaging for visualization of intravascular thrombi.
Abstract: This invention relates to pyrimidine derivatives of general formula I in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases.
Type:
Grant
Filed:
October 18, 2004
Date of Patent:
March 4, 2008
Assignee:
Schering AG
Inventors:
Ulrich Luecking, Gerhard Siemeister, Martin Krueger, Rolf Jautelat
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:
June 13, 2006
Date of Patent:
February 12, 2008
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 relates to a new synthetic process for the production of key intermediates useful in the synthesis of epothilones or epothilone derivatives, to certain compounds used to produce these key intermediates and to a process to produce said compounds.
Type:
Grant
Filed:
April 21, 2005
Date of Patent:
February 5, 2008
Assignee:
Schering AG
Inventors:
Johannes Platzek, Orlin Petrov, Marc Willuhn, Klaus Dieter Graske, Werner Skuballa
Abstract: A sealable folding box in the shape of a parallelepiped or cube with attached bottom and cover flaps and an attachment flap—is provided with an attachment recess—is that is arranged on an edge of the folding box body that extends between these flaps. To this end, the folding-box body—seen in the lengthwise direction of the matrix—has a sealing flap on one end and a combination section on the other end. The combination section consists of an inside area and at least one outside area, whereby the inside area is an attachment flap—provided with an attachment recess—while the outside area is used to attach the combination section to the side wall with which it is in contact. With the invention, a folding box is provided that can be handled simply and reliably in production, storage and filling, that encloses the contents largely dust-tight and that can be marketed stacked or suspended.
Type:
Grant
Filed:
July 17, 2003
Date of Patent:
January 8, 2008
Assignees:
Schering AG, Carl Edelmann GmbH & Co. KG
Abstract: This invention relates to 2-heteroaryl-pyrimidine derivatives of general formula I or If as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.
Type:
Grant
Filed:
October 27, 2003
Date of Patent:
October 30, 2007
Assignee:
Schering AG
Inventors:
Ulrich Lücking, Martin Kruger, Rolf Jautelat, Olaf Prien, Gerhard Siemeister, Alexander Ernst
Abstract: Disclosed are methods and compositions for identifying malignant tumors that overexpress the c-erbB-2 oncogene. Assays useful for diagnosis and prognosis of neoplastic disease are provided which detect the external domain of c-erbB-2, the glycoprotein gp75 and quantitate the level of gp75 in the biological fluids of mammals carrying a tumor burden. Further disclosed are recombinant, synthetically and otherwise biologically produced novel proteins and polypeptides which are encoded by the external domain DNA sequence of the c-erbB-2 oncogene (the gp75 gene) or fragments thereof. Such gp75 proteins and polypeptides are useful as vaccines, therapeutically in the treatment of cancer either alone or in combination with chemotherapeutic agents. Also disclosed are antibodies to such gp75 proteins and polypeptides which are useful diagnostically and therapeutically. Still further disclosed are test kits embodying the assays of this invention.
Type:
Grant
Filed:
November 29, 1993
Date of Patent:
October 16, 2007
Assignee:
Schering AG
Inventors:
Miriam E. C. Hancock, John J. Monahan, Beatrice Claudia Langton
Abstract: The invention relates to a process for the production of 4-(17?-methyl-substituted 3-oxoestra-4,9-dien-11?-yl)benzaldehyde-(1E or 1Z)-oximes of general formula (I), in which R1 is a hydrogen atom, a C1-6-alkyl radical or a CnF2n+1 radical, whereby n is 1, 2 or 3, R2 is a C1-4-alkyl radical, X is an OH group in E- or Z-position, and Y is an OC1-6-alkyl group, an SC1-6-alkyl group or an OCH2CnF2+1 group, whereby n is 1, 2 or 3, which provides the target compounds of formula (I) with a high yield and good selectivity
Type:
Grant
Filed:
November 9, 2001
Date of Patent:
September 11, 2007
Assignee:
Schering AG
Inventors:
Gerd Schubert, Sven Ring, Bernd Erhart, Gerd Mueller
Abstract: This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
Type:
Grant
Filed:
October 13, 2005
Date of Patent:
September 11, 2007
Assignee:
Schering AG
Inventors:
John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
Abstract: The invention relates to substituted pentanols, a process for their production and their use as anti-inflammatory agents.
Type:
Grant
Filed:
October 5, 2004
Date of Patent:
July 3, 2007
Assignee:
Schering AG
Inventors:
Stefan Jaroch, Stefan Baeurle, Markus Berger, Konrad Krolikiewicz, Duy Nguyen, Hartmut Rehwinkel, Norbert Schmees, Werner Skuballa, Heike Schaecke
Abstract: This invention relates to pyrimidine derivatives of general formula I in which R1, R2, X, A and B have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.
Type:
Grant
Filed:
May 29, 2002
Date of Patent:
June 26, 2007
Assignee:
Schering AG
Inventors:
Thomas Brumby, Rolf Jautelat, Olaf Prien, Martina Schäfer, Gerhard Siemeister, Ulrich Lücking, Christoph Huwe
Abstract: The invention relates to a method for the production of 4-(17? substituted 3-oxoestra-4,9-dien-11?-yl)benzaldehyd-(1E or 1Z)-oximes of general formula (I), where R1?H, C1-6 alkyl or a CnF2n+1 group; R2?C1-4 alkyl, X=E- or Z-OH; and Y?O—C1-6 alkyl, S—C1-6 alkyl or O—CH2CnF2n+1, where n=1, 2 or 3, which produces the target compounds of formula (I) with high yield and selectivity.
Abstract: Cascade polymers, containing complex-forming ligands, optionally at least five ions of an element of atomic numbers 21–29, 39, 42, 44 or 57–83, as well as, if desired, cations of inorganic and/or organic bases, amino acids or amino acid amides, are valuable complexing compounds and complexes for diagnostics and therapy.
Type:
Grant
Filed:
September 30, 2004
Date of Patent:
April 24, 2007
Assignee:
Schering AG
Inventors:
Johannes Platzek, Heribert Schmitt-Willich, Heinz Gries, Gabriele Schuhmann-Giampieri, Hubert Vogler, Hanns-Joachim Weinmann, Hans Bauer
Abstract: Novel VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridones and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are selected.
Type:
Grant
Filed:
June 14, 2004
Date of Patent:
April 10, 2007
Assignee:
Schering AG
Inventors:
Andreas Huth, Martin Krueger, Ludwig Zorn, Stuart Ince, Rolf Bohlmann, Karl Heinz Thierauch, Andreas Menrad, Martin Haberey, Holger Hess-Stumpp
Abstract: New 17?-fluorosteroid compounds of formula (I) are disclosed: wherein R1 denotes H or methyl; R2 and R3 each denote H, Cl or methyl; and either a double bond or a single bond is present between C-6 and C-7 and also C-9 and C-10 of the steroid ring system respectively. These compounds have an activity profile with hybrid character so that they act as inhibitors for 5?-reductase and as high potency gestagens. Pharmaceutical compositions containing them are disclosed. They are suitable for treatment of conditions, which are caused by high levels of androgen in organs and tissues. These new compounds can be used in combination with other hormonal substances, such as estrogens, testosterone and other androgens, as contraceptives and for other applications.
Type:
Grant
Filed:
April 13, 2005
Date of Patent:
April 3, 2007
Assignee:
Schering AG
Inventors:
Ulrich Bothe, Peter Droescher, Walter Elger, Gudrun Reddersen, Bernd Menzenbach, Hans-Udo Schweikert, Alexander Hillisch, Birgitt Schneider
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: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.
Abstract: The invention relates to new unsaturated 14,15-cyclopropano-androstanes of the general formula (I) to their synthesis and to pharmaceutical compositions, containing these compounds. The compounds of formula (I) have gestagenic and/or androgenic activity.
Type:
Grant
Filed:
November 21, 2000
Date of Patent:
September 25, 2007
Assignee:
Schering AG
Inventors:
Sven Ring, Walter Elger, Guenter Kaufmann