Abstract: The invention relates to novel epothilone derivatives of general formula (I), wherein R8 means a halogen atom, especially a fluorine or chlorine atom, and the remaining substituents have the meanings given in the description. The novel compounds are suitable for producing medicaments.
Type:
Grant
Filed:
December 7, 2001
Date of Patent:
August 26, 2003
Assignee:
Schering AG
Inventors:
Ulrich Klar, Werner Skuballa, Bernd Buchmann, Wolfgang Schwede, Michael Schirner
Abstract: Competitive progesterone antagonists, including two novel steroids, viz., 11&bgr;,19-[4-(cyanophenyl)-o-phenylene]-17&bgr;-hydroxy-17&agr;-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one and 11&bgr;,19-[4-(3-pyridinyl)-o-phenylene]-17&bgr;-hydroxy-17&agr;-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one, inhibit formation of endometrial glands at below their ovulation inhibiting dose and the abortive dose, and thus achieve oral contraception in females without adversely affecting the menstrual cycle and without risk of aborting a previous implanted fertilized egg or a fetus.
Type:
Grant
Filed:
November 28, 2001
Date of Patent:
August 19, 2003
Assignee:
Schering AG
Inventors:
Krzystof Chwalisz, Walter Elger, Karin Schmidt-Gollwitzer, Eckhard Ottow
Abstract:
The invention relates to a method for producing epothilone B and derivatives, and to intermediate products for this method. According to the novel method, the epothilone B or derivatives are produced in high yields from the C1-C6, C7-C10 and C11-C20-fragments 2, 3 and 4 that can be obtained economically and diastereomerically purely (the variable radicals having the meanings given in the description ).
Type:
Grant
Filed:
June 1, 2001
Date of Patent:
August 12, 2003
Assignee:
Schering AG
Inventors:
Johann Mulzer, Andreas Mantoulidis, Elisabeth Öhler
Abstract: The invention relates to 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production of these new intermediate products in the synthesis and the use for the production of epothilones or epothilone derivatives.
Type:
Application
Filed:
August 5, 2002
Publication date:
August 7, 2003
Applicant:
Schering AG
Inventors:
Jurgen Westermann, Johannes Platzek, Orlin Petrov
Abstract: This invention describes the use of estrogen receptor (ER)&bgr;-selective agonists for the production of a pharmaceutical agent for triggering somatotropic and/or organotropic effects in the CNS, the circulatory system, the skeletal system and/or the immune system in the aging male and female organism (anticatabolic therapy).
Type:
Application
Filed:
October 17, 2002
Publication date:
July 10, 2003
Applicant:
Schering AG
Inventors:
Walter Elger, Gudrun Reddersen, Birgitt Schneider, Alexander Hillisch, Olaf Peters, Dirk Kosemund, Gerd Muller
Abstract: The invention provides a stable pharmaceutical composition containing biologically active human interferon-&bgr; (IFN-&bgr;), preferably IFN &bgr;1b produced in a bacterial host, dissolved in an aqueous-based solution containing a glycine buffer at a pH of about 2.0 to about 4.0. The invention of also provides stable IFN-&bgr; lyophilizates prepared from biologically active IFN-&bgr;, dissolved in an aqueous-based solution containing a glycine buffer at a pH of about 2.0 to about 4.0.
Type:
Application
Filed:
July 9, 2002
Publication date:
June 26, 2003
Applicant:
Schering AG
Inventors:
Michael McCaman, Susanne Ottoboni, Erno Pungor
Abstract: The invention relates to new C13-substituted estra-1,3,5(10)-trien-3-yl sulfamates of general formula I,
wherein R1 represents an acyl residue, oxycarbonyl residue, aminocarbonyl residue, sulfonyl residue, or aminosulfonyl residue, and R15 represents ethyl, methods of preparing same, and pharmaceutical compositions containing these compounds.
The compounds of the invention of general formula I inhibit the activity of steroid sulfatase (EC 3.1.6.2) and do not exhibit any estrogenic effect.
Type:
Grant
Filed:
September 6, 2000
Date of Patent:
June 24, 2003
Assignee:
Schering AG
Inventors:
Sigfrid Schwarz, Gerd Müller, Dirk Kosemund, Margit Richter, Olaf Peters, Ina Scherlitz-Hofmann, Thomas Michel, Walter Elger, Gudrun Reddersen, Birgitt Schneider
Abstract: The invention relates to a device for magnetic separation of pharmaceutical preparations, their starting or intermediate products that contain a separation space, in which a magnetic gradient field prevails and which has an inlet and an outlet, whereby the device is embodied in the form of an attachment filter for injection instruments or infusion instruments.
Type:
Application
Filed:
December 19, 2002
Publication date:
June 12, 2003
Applicant:
Schering AG
Inventors:
Werner Weitschies, Thomas Rheinlander, Wolfgang Ebert, Bernard Better
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:
Application
Filed:
July 19, 2002
Publication date:
June 12, 2003
Applicant:
Schering AG
Inventors:
Johannes Platzek, Heribert Schmitt-Willich, Gunther Michl, Thomas Frenzel, Detlev Sulzle, Hans Bauer, Bernd Raduchel, Hanns-Joachim Weinmann, Heiko Schirmer
Abstract: Provided are methods for inducing an increase in the number of CD4+ T-lymphocytes in HIV-infected patients by administering human GM-CSF. The GM-CSF may be administered concurrently with at least one antiretroviral agent.
Abstract: The invention relates to new quinoline, isoquinoline and phthalazine derivatives as antagonists of the gonadotropin-releasing hormone.
Type:
Application
Filed:
February 21, 2002
Publication date:
June 5, 2003
Applicant:
Schering AG
Inventors:
Peter Strehlke, Peter Droescher, Ulrich Buehmann, Norbert Schmees, Peter Muhn, Holger Hess-Stumpp, Ronald Kuhne, Eckhard Guenther, Emmanual Polymeropoulos, Antonius Ter Laak
Abstract: A solid pharmaceutical agent formulation that contains (2R)-1-((4-chloro-2-(ureido)phenoxy)methyl)carbonyl-2-methyl-4-(4-fluorobenzyl)piperazine or a salt thereof is described.
Type:
Application
Filed:
October 18, 2002
Publication date:
May 8, 2003
Applicant:
Schering AG
Inventors:
Heiko Kranz, Christoph Volkel, Ralph Lipp, Johannes Tack, Herbert Wiesinger
Abstract: This invention describes the use of metal complexes that have a plasma protein bond of at least 10% as imaging diagnostic agents for locating an infarction or a necrosis using lasting positive visualization.
Type:
Application
Filed:
October 7, 2002
Publication date:
April 3, 2003
Applicant:
Schering AG
Inventors:
Johannes Platzek, Ulrich Speck, Ulrich Niedballa, Bernd Raduchel, Hanns Weinmann, Wolfgang Ebert
Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B and Y 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 treating and for preventing diseases that are associated with microglia activation, as well as pharmaceutical preparations that contain these compounds.
Type:
Application
Filed:
July 5, 2002
Publication date:
March 20, 2003
Applicant:
Schering AG
Inventors:
Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning, Herbert Schneider, Bernd Elger