Abstract: The present invention relates to nucleotide-sugar-synthesizing enzymes (enzymes with nucleotidyltransferase or pyrophosphorylase activity) from nonparasitic protists, to a process for the preparation thereof and to the use thereof for preparing nucleotide-sugars. The enzymes according to the invention make possible or greatly simplify the enzymatic preparation of various nucleotide-sugars on the industrial scale from low-cost precursors. It is possible with the aid of the discovered enzymes to prepare, for example, GDP-fucose, GDP-mannose, UDP-glucose, UDP-glucosamine, UDP-galactose, UDP-galactosamine, UDP-N-acetylglucosamine and UDP-N-acetylgalactosamine in economic quantities.
Type:
Grant
Filed:
March 3, 1997
Date of Patent:
November 7, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Thomas Kiy, Lothar Elling, Maria Regina Kula
Abstract: Aminoalkyl and acylaminoalkyl ethers which are distinguished by high affinity for the bradykinin B.sub.2 receptor and improved solubility in water are described. These aminoalkyl and acylaminoalkyl ethers can be represented by the formula (I) ##STR1## in which R.sup.1,R.sup.2,R.sup.3 are alkyl, aryl, alkylaryl, halogen, hydrogen, cycloalkyl, CHO, CO--O-alkyl, COOH; R.sup.4, R.sup.5 are hydrogen, halogen, alkoxy, nitro, cyano, S-alkyl; n is a number from 1 to 8; R.sup.6 is hydrogen, alkyl, alkylalkenyl, alkylaryl; R.sup.7 is hydrogen and a substituted or unsubstituted acyl radical. A process for preparing the compounds of the formula (I) is likewise described.
Type:
Grant
Filed:
March 12, 1997
Date of Patent:
October 31, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Holger Heitsch, Adalbert Wagner, Klaus Wirth, Bernward Scholkens, Gerhard Nolken
Abstract: Novel oligonucleotide analogs of the formula [I] are described, ##STR1## in which A, B, D, G, L, P, Q, Q', R.sup.5, R.sup.6, X, Y, Z and n are as defined in the description, which have useful physical, biological and pharmacological properties, as well as a process for their preparation. Their application relates to use as inhibitors of gene expression (antisense oligonucleotides, ribozymes, sense oligonucleotides and triplex-forming oligonucleotides), as probes for the detection of nucleic acids and as auxiliaries in molecular biology.
Type:
Grant
Filed:
November 20, 1998
Date of Patent:
October 3, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Anuschirwan Peyman, Eugen Uhlmann, Gerhard Breipohl, Holger Wallmeier
Abstract: A compound of the formula ##STR1## where R.sup.1 is the radical of the formula II or III ##STR2## is suitable for the production of a pharmaceutical for the treatment of inflammations, carcinomatous diseases, or autoimmune diseases. A compound of the formula IV ##STR3## is suitable for the production of specific antibodies against a compound of the formula I for the discovery of specific-binding proteins from cell extracts, serum, blood, or synovial fluids, for the purification of proteins, for the modification of microtiter plates, or for the preparation of chromatography material, in particular of affinity chromatography material, and for use in diagnostics.
Type:
Grant
Filed:
April 22, 1999
Date of Patent:
September 19, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Stefan Mullner, Bernd Kirschbaum, Wilfried Schwab
Abstract: 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or dissorders whose course involves increased connective tissue or cartilage degradation.
Abstract: PNA synthesis using a base-labile amino protecting group Processes are described for preparing PNA oligomers, ##STR1## in which R.sup.0 is hydrogen, alkanoyl, alkoxycarbonyl, cycloalkanoyl, aroyl, heteroaroyl, or a group which favors the intracellular uptake of the oligomer, A and Q are amino acid residues, k and 1 are 0 to 20, n is 1-50, B is a nucleotide base which is customary in nucleotide chemistry, and Q.sup.0 is OH, NH.sub.2, or alkylamino which can be substituted by OH or NH.sub.2. In these processes, the amino acid residues and the structural components ##STR2## in which PG is a base-labile amino protecting group and B' is a nucleotide base which is protected on its exocyclic amino function, are coupled step-wise, in accordance with the solid-phase method, onto a polymeric support which is provided with an anchor group, and, after the construction is complete, the target compounds are cleaved from the polymeric support using a cleaving reagent.
Type:
Grant
Filed:
October 29, 1997
Date of Patent:
September 19, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Gerhard Breipohl, Eugen Uhlmann, Jochen Knolle
Abstract: The present invention is concerned with new hypolipidemic compounds, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis.Compounds of the formula (I): ##STR1## wherein R.sup.1 to R.sup.10 and X are as defined in the Specification and useful as hypolipidemic compounds.
Type:
Grant
Filed:
July 27, 1999
Date of Patent:
September 5, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Alfons Enhsen, Eugen Falk, Heiner Glombik, Siegfried Stengelin
Abstract: Substituted quinoline derivatives, processes for their preparation, and their use.Compounds of the formula I ##STR1## and their tautomeric forms, of the formula Ia ##STR2## in which m, n and the substituents X and R.sup.1 to R.sup.5 have the meanings mentioned, have an action against viruses.
Abstract: A novel polymer comprising oligo-p-phenylene units and having formula (A.sub.k B).sub.n is disclosed, wherein A and B have the following chemical structure: ##STR1## Y are identical or different and are each (E)--CR.sup.9 .dbd.CR.sup.10 --, --C.dbd.C-- or --CHR.sup.11 --CHR.sup.12 ;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12 are, independently of one another, identical or different in the individual structural elements and are each H, a straight-chain or branched alkyl group having from 1 to 22 carbon atoms, or an aryl or aryloxy group, or Br, Cl, F, CN or alkyloxycarbonyl having from 2 to 23 carbon atoms;k is from 1 to 25,n is from 1 to 200.The polymer of the present invention may be used as an electroluminescence material.
Type:
Grant
Filed:
September 18, 1997
Date of Patent:
September 5, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Willi Kreuder, Dieter Neher, Marcus Remmers
Abstract: Compounds of the formula I or salts thereof, in whichX is oxygen, --O--NR.sup.2 -- or --SO.sub.2 --NR.sup.2 --, and Y is N or CH,R.sup.1 is (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl or (C.sub.2 -C.sub.6)alkynyl, which are in each case optionally substituted, or, in the case where X=oxygen, also (subst.) phenyl,R.sup.2 is H, (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl or -alkynyl or (C.sub.3 -C.sub.6)cycloalkyl,R.sup.3 and R.sup.4 are H, (subst.) (C.sub.1 -C.sub.4)alkyl or (subst.) (C.sub.1 -C.sub.4)alkoxy or halogen, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)-alkylamino or di[(C.sub.1 -C.sub.4)alkyl]-amino,R.sup.5 is H or (C.sub.1 -C.sub.4)alkyl and R.sup.6 is hydrogen,may be prepared by reacting compounds of the formula II,R.sup.1 --X--R.sup.7 (II)with compounds of the formulae III, IV and VR.sup.8 --OCN (III)SO.sub.2 Cl.sub.2 (IV) ##STR1## where R.sup.7 and R.sup.8 are H, a quarternary ammonium ion or one equivalent of a metal cation.
Abstract: The promoter of the human endoglin gene, parts thereof, and compositions containing these are useful for high level control of gene expression, particularly in endothelial cells. The promoter, and promoter active portions of the promoter are shown to have unexpected activity and are particularly relevant for therapeutic use.
Abstract: New insulin derivatives of the formula II with an iso-electric point between 5 and 8.5, with improved stability in weakly acid aqueous medium and with a special action profile, and the physiologically tolerated salts of these insulin derivatives, for the treatment of diabetes mellitus; formula II is: ##STR1## in which R.sup.1 denotes H or H-Phe,R.sup.2 denotes a genetically encodable L-amino acid which contains no amide group,R.sup.30 represents the residue of a neutral genetically encodable L-amino acid,R.sup.31 represents a physiologically acceptable organic group which is basic in nature and has up to 50 carbon atoms, in whose structure 0 to 3 .alpha.-amino acids are involved and whose terminal carboxyl group which is present where appropriate can be free, in the form of an ester functionality, an amide functionality, a lactone or reduced to CH.sub.2 0H, andX represents a genetically encodable L-amino acid.
Abstract: Substituted bicyclic heteroaroylguanidines, a process for their preparation, their use as a medicament or a diagnostic agent, and a medicament containing them are described, as are the pharmaceutically tolerated salts thereof. A process for their preparation, and their use as medicines and diagnostic aids in cardiovascular diseases, is also described.
Type:
Grant
Filed:
November 18, 1998
Date of Patent:
July 25, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(ozy)yl, E is O or S; Y is --[CR(3).sub.2 ].sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z in Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.
Type:
Grant
Filed:
May 19, 1998
Date of Patent:
July 18, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David W. Laufer
Abstract: A biaxially oriented polypropylene film is described. The n-heptane-insoluble content of the film has a chain isotactic index, measured by .sup.13 C-NMR spectroscopy, of at least 97%. In addition, a process for the production of the polypropylene film and the use of the film are described.
Type:
Grant
Filed:
November 10, 1997
Date of Patent:
July 11, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Herbert Peiffer, Detlef Busch, Gunter Schlogl, Karl-Heinz Kochem, Thomas Dries, Andreas Winter
Abstract: Substituted 2-naphthoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing themSubstituted 2-naphthoylguanidines of the formula I ##STR1## having the meanings indicated in claim 1 for R1 to R8, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris. They also preventively inhibit the pathophysiological processes in the formation of ischemically induced damage, in particular in the production of ischemically induced cardiac arrhythmias.
Type:
Grant
Filed:
May 16, 1997
Date of Patent:
July 11, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Joachim Brendel, Heinz-Werner Kleemann, Heinrich Christian Englert, Hans Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Bansi Lal
Abstract: Compounds of formula I ##STR1## in which R(1) to R(8) and X have the meanings indicated in the specification, are useful for the production of medicaments having K.sup.+ channel-blocking action; in particular for the production of a medicament for the treatment or prophylaxis of stimulated gastric acid secretion; of ulcers of the stomach and of the intestinal region; of reflux esophagitis; of diarrhea; of all types of arrhythmias, including ventricular and supraventricular arrhythmias; and of reentry arrhythmias and for the prophylaxis of sudden heart death as a result of ventricular fibrillation.
Type:
Grant
Filed:
April 27, 1999
Date of Patent:
July 11, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Uwe Gerlach, Joachim Brendel, Hans Jochen Lang, Klaus Weidmann
Abstract: An inorganic material comprising an aerogel, a process for its preparation, and its use. The invention relates to a composite material comprising from 10 to 95% by volume of aerogel particles whose particle diameter is less than 0.5 mm and a phyllosilicate as inorganic matrix material.
Type:
Grant
Filed:
May 21, 1997
Date of Patent:
July 4, 2000
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Dierk Frank, Andreas Zimmermann, Helmut Stuhler
Abstract: Sulfuric acid which contains dilute organic phosphorus compounds and other impurities and is obtained, for example, during preparation of sulfonated arylphosphines, is purified by extraction with an amine which is sparingly soluble or insoluble in water.