Abstract: This invention relates to new 19-nor-17&agr;-pregna-1,3,5(10)-trien-17&bgr;-ols with a 21,16&agr;-lactone ring with a long-chain substituent in 11&bgr;-position of general formula II 1
Type:
Application
Filed:
March 27, 2003
Publication date:
December 11, 2003
Applicant:
Schering AG
Inventors:
Gerd Mueller, Jens Hoffmann, Karl-Heinrich Fritzemeier, Alexander Hillisch
Abstract: Disclosed and claimed are methods for oral contraception, or a hormone replacement therapy, or for treating breast cancer, in a patient in need thereof involving administering to the patient, at a dosage of no greater than 200 &mgr;g/day per 70 kg subject, a compound having Formula (I):
wherein X in combination with K form a steroidal ring and R5 is a sulphamate group that has of the formula:
wherein each of R1 and R2 is H.
Type:
Grant
Filed:
January 5, 2001
Date of Patent:
November 25, 2003
Assignees:
Sterix Limited, Schering AG
Inventors:
Barry Victor Lloyd Potter, Michael John Reed, Walter Elger, Gudrun Roddersen, Heinrich-Thomas Proske
Abstract: The invention relates to a method for representing compounds of the general formula (1). The invention further relates to the hitherto unknown compounds of general formulas (5, 6 and 7) in the form of intermediate products and to the use of 4,4-dimethyl-3&bgr; hydroxypregna-8,14-diene-21-carboxylic acid esters of the general formula (1) for producing 4,4-dimethyl-5&agr;-cholesta-8,14,24-triene-3&bgr;-ol (2).
Abstract: To provide a novel apoptosis inducer, and a method of screening an apoptosis inducer. For example, an apoptosis inducer comprising inhibiting HDAC6 such as an antisense oligonucleotide to the gene of histone deacetylase 6 (HDAC6), and anti-cancer agent comprising this apoptosis inducer, and the present invention also provides a method of screening an apoptosis inducer that inhibits HDAC6, and more specifically a method of screening an apoptosis inducer said method comprising the steps of (1) determining whether or not a test substance inhibits histone deacetylase 6 (HDAC6) by using deacetylation of an acetylated substance that can be a substrate for histone deacetylase 6 (HDAC6) or decrease in the expression of histone deacetylase 6 (HDAC6) as an index; and (2) confirming, when inhibition is present, whether it induces apoptosis of the cell in vitro and/or in vivo.
Abstract: The invention relates to conjugates that consist of macrocyclic metal complexes with biomolecules and their production. The conjugates are suitable as contrast media in NMR diagnosis and radiodiagnosis as well as as agents 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:
November 6, 2003
Applicant:
Schering AG
Inventors:
Johannes Platzek, Heribert Schmitt-Willich, Gunther Michl, Thomas Frenzel, Detlev Sulzle, Hans Bauer, Bernd Raduchel, Hans-Joachim Weinmann, Henko Schirmer
Abstract: Improved metal complex-containing pharmaceutical agents are described which, as an additive, contain one or more complexing agents and/or one or more weak metal complex(es) or mixtures thereof.
Type:
Application
Filed:
June 16, 2003
Publication date:
November 6, 2003
Applicant:
Schering AG
Inventors:
Heinz Gries, Ulrich Speck, Hanns-Joachim Weinmann, Hans Peter Niendorf, Wolfgang Seifert
Abstract: The invention relates to the calcium complex of [[(4R)-4-[bis[(carboxy-.kappa.O)methyl]amino-.kappa.N]-6,9-bis[(carboxy-.kappa.O)methyl]-1-[(4,4-diphenylcyclohexyl)oxy]-1-hydroxy-2-oxa-6,9-diaza-1-phosphaundecan-11-ylic-acid.kappa.N6,.kappa. N9,.kappa.011]1-oxidato(6-)]-, tetrahydrogen (MS-325) and its salts, pharmaceutical agents that contain these complexes, for the production of agents for the reduction of effects that are caused by heavy metals as well as processes for their production.
Type:
Application
Filed:
January 15, 2003
Publication date:
October 30, 2003
Applicant:
Schering AG
Inventors:
Johannes Platzed, Ulrich Nieballa, Guenter Michl
Abstract: The invention relates to (ethylene)-(propylene)-triaminepentaacetic acid derivatives that are substituted on both the ethylene bridge and the propylene bridge, as well as conjugates of these compounds with biomolecules. The compounds and conjugates are suitable as agents for NMR diagnosis and radiodiagnosis as well as for radiotherapy.
Abstract: The invention relates to 17&agr;-alkyl-17&bgr;-oxy-estra-1,3,5(10)-trienes that have an antiestrogenic action with general formula I. In addition, the invention also relates to 17-oxo-estra-1,3,5(10)-trienes as well as 17&bgr;-hydroxy-estra-1,3,5(10)-trienes as intermediate products in the production of the estratrienes according to the invention. The invention also relates to the use of 17&agr;-alkyl-17&bgr;-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations that contain at least one 17&agr;-alkyl-17&bgr;-oxy-estratriene as well as at least one pharmaceutically compatible vehicle.
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:
Application
Filed:
March 31, 2003
Publication date:
October 9, 2003
Applicant:
Schering AG
Inventors:
Krzystof Chwalisz, Walter Elger, Karin Schmidt-Gollwitzer, Eckhard Ottow
Abstract: A near infrared fluorescent contrast agent comprising a compound having three or more sulfonic acid groups in a molecule, and a method of fluorescence imaging comprising introducing the near infrared fluorescent contrast agent of the present invention into a living body, exposing the body to an excitation light, and detecting near infrared fluorescence from the contrast agent. The near infrared fluorescent contrast agent of the present invention is excited by an excitation light and emits near infrared fluorescence. This infrared fluorescence is superior in transmission through biological tissues. Thus, detection of lesions in the deep part of a living body has been made possible. In addition, the inventive contrast agent is superior in water solubility and low toxic, and therefore, it can be used safely.
Abstract: This invention describes C1-C6-epothilone fragments and an efficient process for the production of C1-C6-fragments of epothilones and derivatives thereof.
Type:
Application
Filed:
December 23, 2002
Publication date:
September 18, 2003
Applicant:
Schering AG
Inventors:
Ulrich Klar, Markus Berger, Bernd Buchmann, Wolfgang Schwede, Werner Skuballa
Abstract: This invention relates to a quick-release tablet formulation with >99.19% pure fludara (high-purity fludara) as an active ingredient in a defined composition of residual contaminants.
Type:
Application
Filed:
December 20, 2002
Publication date:
September 18, 2003
Applicant:
Schering AG
Inventors:
Wolfgang Heil, Ulf Tistam, Ralph Lipp, Johannes-Wilhelm Tack
Abstract: This invention describes a safe method for the production of sulfamoyl chloride from chlorosulfonyl isocyanate and formic acid in the presence of a amide catalyst, taming the hazardous nature of this reaction by circumventing heat accumulation processes, as well as the sulfamoylation of alcohols and phenols with the resulting sulfamoyl chloride in N,N-dimethyl acetamide or N-methyl pyrrolidone thereby avoiding the formation of side-products which were inevitable with the methods of the prior art using dimethyl formamide or dichloromethane as a solvent. The current invention allows industrial scale applications and describes as an example the process of manufacture of the biologically active compound 17&bgr;-Hydroxyestra-1,3,5(10)-triene-3-yl sulfamate.
Type:
Application
Filed:
December 23, 2002
Publication date:
September 11, 2003
Applicant:
Schering AG
Inventors:
Jens Geisler, Frank Schneider, Fernando Lopez Holguin, Kai Lovis
Abstract: This invention relates to 11&bgr;-(para-substituted)phenyl-estra-1,3,5(10)-trienes with a straight-chin or branched-chain, optionally partially or completely halogenated alkyl radical or alkenyl radical in each case with up to 5 carbon atoms, an ethinyl radical or prop-1-inyl radical in 8&bgr;-position.
Type:
Application
Filed:
October 15, 2002
Publication date:
September 11, 2003
Applicant:
Schering AG
Inventors:
Nico Brauer, Olaf Peters, Alexander Hillisch, Christa Hegele-Hartung, Peter Muhn
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