Patents Assigned to Hoechst Aktiengesellschaft
  • Phenyl.-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or diagnostic agent, and also a medicament containing them
    Patent number: 6025349
    Abstract: Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or diagnostic agent, and also a medicament containing them.Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## in which the substituents have the meanings stated in the description, and their pharmaceutically suitable salts, are described. They are obtained by reacting a compound II ##STR2## with guanidine, in which R(1) to R(5) and R(A), R(B), R(C) and R(D) have the stated meaning, and L is a leaving group which easily undergoes nucleophilic substitution. Compounds I are excellent cardiovascular therapeutic agents.
    Type: Grant
    Filed: July 20, 1998
    Date of Patent: February 15, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Substituted benzyloxy-carbonylguanidines, a process for their preparation, their use as a medicament or diagnostic, and a medicament containing them
    Patent number: 6022899
    Abstract: There are described compounds of the formula I ##STR1## in which the substituents R(1) to R(7) and X have the meanings shown in the claims, and their pharmaceutically tolerable salts. These are effective inhibitors of the cellular sodium proton antiporter (Na.sup.+ /H.sup.+ exchanger). They are therefore outstandingly suitable for the treatment of all diseases which can be attributed to increased Na.sup.+ /H.sup.+ exchange.
    Type: Grant
    Filed: January 9, 1998
    Date of Patent: February 8, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans-Jochen Lang, Udo Albus, Wolfgang Scholz
  • Hypolipidemic 1,4-benzothiazepine-1,1-dioxides
    Patent number: 6020330
    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 a defined in the specification and are useful as hypolipidemic compounds.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: February 1, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Alfons Enhsen, Eugen Falk, Heiner Glombik, Siegfried Stengelin
  • Preparation having increased in vivo tolerability
    Patent number: 6020315
    Abstract: A preparation having increased in vivo tolerability comprising a glycosyl-Y[--C(.dbd.Y)--X--].sub.p --W(R).sub.n --X--C(.dbd.Y)-active compound, sugar or sugar alcohol and, optionally divalent ions, and a pharmaceutically tolerable carrier.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: February 1, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Klaus Bosslet, Jorg Czech, Manfred Gerken, Rainer Straub, Matthias Blumrich
  • Use of isoxazole and crotonamide derivatives for the treatment of carcinomatous disorders
    Patent number: 6020372
    Abstract: The compound of the formula I or II ##STR1## is suitable for the production of a pharmaceutical for the treatment of carcinomatous disorders, where R.sup.1 is (C.sub.3 -C.sub.5)-cycloalkyl, (C.sub.2 -C.sub.6)-alkenyl or (C.sub.2 -C.sub.6)-alkynyl, R.sup.2 is CF.sub.3, OCF.sub.3, SCF.sub.3, OH, NO.sub.2, halogen, benzyl, phenyl, CN or O-phenyl, R.sup.3 is (C.sub.1 -C.sub.4)-alkyl, halogen or a hydrogen atom and X is a --CH group or a nitrogen atom.
    Type: Grant
    Filed: November 13, 1998
    Date of Patent: February 1, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wilfried Schwab, Jorg Czech, Klaus Boslett
  • Process for the preparation of aldehydes employing catalyst compositions based on rhodium complexes containing diphosphine ligands
    Patent number: 6020532
    Abstract: A process for preparing aldehydes by hydroformylating olefinically unsaturated compounds in the presence of a water-insoluble catalyst composition comprising rhodium complexes containing diphosphine ligands, wherein the diphosphine ligands present are compounds of the formula (I) ##STR1## wherein R.sup.1 is selected from the group consisting of carboxylate (COO.sup.-), sulfonate (SO.sub.3.sup.-), phosphonate (PO.sub.3.sup.2-) and 2-anmino ethtanebisphosphonate, R.sup.
    Type: Grant
    Filed: July 9, 1998
    Date of Patent: February 1, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Helmut Bahrmann, Peter Lappe, Thomas Muller
  • 3-hydroxypyridine-2-carboxamidoesters, their preparation and their use as pharmaceuticals
    Patent number: 6020350
    Abstract: There are described 3-hydrixypyridine-2-carboxamidoesters of the formula ##STR1## their preparation, their use for the inhibition of collagen biosynthesis and their use as pharmaceuticals for the treatment of fibrotic disorders.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: February 1, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Klaus Weidmann, Karl-Heinz Baringhaus, Georg Tschank, Martin Bickel
  • Hollow extrusion using internal coolant
    Patent number: 6019934
    Abstract: The process according to the invention for producing large-bore thick-walled pipes made of polyethylene comprises extruding the polymer composition out of an annular die 3 and subsequently cooling the melt 7 emerging from the die 3 using water as the coolant from the outside, the melt 7 emerging from the die being additionally also cooled with water from the inside. In order to ensure the internal cooling, according to the invention floating plugs 11 and 12 are inserted, which plugs are fixed in their physical position relative to the extrusion die 3 by means of retaining elements.
    Type: Grant
    Filed: February 4, 1997
    Date of Patent: February 1, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Ulrich Schulte
  • Process for the preparation of chiral, nonracemic (4-aryl-2,5-dioxoimidazolidin-1-yl) acetic acids
    Patent number: 6018053
    Abstract: The present invention relates to a process for the preparation of chiral, nonracemic compounds of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings indicated in claim 1 and which are useful intermediates for the preparation of pharmaceutical active compounds in which, for resolution, a salt is formed from the racemic compound of the formula I and a chiral, nonracemic amino compound. It furthermore relates to compounds of the formula I and esters thereof.
    Type: Grant
    Filed: June 19, 1997
    Date of Patent: January 25, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Holla, Gerhard Beck, Bernhard Kammermeier, Berndt Kulitzscher, Jurgen Michalowsky
  • G cap-stabilized oligonucleotides
    Patent number: 6013639
    Abstract: Oligonucleotides of the formula5'-(CAP)-(Oligo)-(CAP)-3'are disclosed where (oligo) is a nucleotide sequence of from 10 to 40 nucleotides in length, and CAP is G.sub.m, where m is an integer of from zero to ten, the two CAP's which are present in the molecule can be defined independently of each other and must be different in the case where m is zero at the 5' or 3' end and the end of the Oligo sequence is other than guanine. The oligonucleotides can be synthesized chemically. The oligonucleotides are used to diagnose or treat cancer, restenosis, a disease caused by a virus, a disease affected by integrins or cell-cell adhesion receptor or a disease triggered by diffusible factors.
    Type: Grant
    Filed: January 31, 1996
    Date of Patent: January 11, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Anuschirwan Peyman, Eugen Uhlmann
  • Vitronectin receptor antagonists, their preparation and their use
    Patent number: 6011045
    Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: January 4, 2000
    Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them
    Patent number: 6011063
    Abstract: Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(5) have the meanings given in the claims, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and for infarct treatment and also for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes in the formation of ischemically induced damage, in particular in the illicitation of ischemically induced cardiac arrhythmias.
    Type: Grant
    Filed: June 3, 1997
    Date of Patent: January 4, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
  • Use of isoxazole and crotonamide derivatives for the modulation of apoptosis
    Patent number: 6011051
    Abstract: Compounds of the formula I or II ##STR1## are suitable for the production of pharmaceuticals for the modulation of apoptosis. These compounds can be employed for the treatment of infarct, stroke, neurodegeneration or hypertrophic disorders.
    Type: Grant
    Filed: July 23, 1997
    Date of Patent: January 4, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Stefan Mullner, Claudia Dax
  • Modified cycloolefin copolymer
    Patent number: 6008298
    Abstract: Polymer alloy comprising a) one or more cycloolefin copolymers and b) one or more types of core/shell particles having a diameter of 0.01 to 0.7 micrometer.
    Type: Grant
    Filed: January 22, 1998
    Date of Patent: December 28, 1999
    Assignees: Hoechst Aktiengesellschaft, Mitsui Petrochemical Ind., Ltd.
    Inventors: Wilfried Hatke, Frank Osan, Otto Herrmann-Schonherr
  • Preparations stimulating nail growth
    Patent number: 6007798
    Abstract: A nail varnish comprising a compound having a vasodilating action and a water-insoluble film-forming agent is suitable for treatment of growth disturbances of the nail.
    Type: Grant
    Filed: February 11, 1998
    Date of Patent: December 28, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Manfred Bohn, Karl Theodor Kraemer, Horst Ulbricht
  • Process for the oxidation of organic compounds in the presence of bis- and tris- (.mu.-oxo)-dimanganese complex salts as catalyst
    Patent number: 6008387
    Abstract: Disclosed and claimed are oxidation reactions involving, as a catalyst, a bis- and/or tris-(.mu.-oxo)-dimanganese complex salt of the formula I[LMn(.mu.-O).sub.a (.mu.-OAc).sub.b MnL].sup.x A.sub.y (I)Ac is a C.sub.2 -C.sub.8 -acyl group,a is 1, 2 or 3,b is 0 when a is 2 or 3 or b is 2 when a is 1,x indicates the number of positive charges and is 2 or 3,A is a singly or doubly negatively charged anion,y is the number of anions A required to balance the positive charges andL is a ligand, such as N,N-bis(2-pyridylmethyl)-N-methylamine or N,N,N',N'-tetrakis(2-pyridyl(methyl)-N-methylamine or N.sub.1 N.sub.1 N.sub.1, N.sup.1 -tetrakis(2-pyridylmethyl)-1,2-ethylenediamine.
    Type: Grant
    Filed: January 2, 1997
    Date of Patent: December 28, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ahmed Tafesh, Matthias Beller
  • Imino compounds, process for their preparation and their use as victronectin antagonists
    Patent number: 6005117
    Abstract: There are described imino derivatives of formula (I)R.sup.1 --Y--A--B--D--E--F--G (I)their preparation and their use as medicaments. The compounds according to the invention may be used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: December 21, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
  • Phenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them
    Patent number: 6005010
    Abstract: Compounds of the formula ##STR1## where T is ##STR2## and R(A), R(B), R(C), R(D), R(E), R(F), x and y have the meanings indicated in the claims, and their pharmaceutically acceptable salts are effective inhibitors of the cellular sodium-proton antiporter (Na.sup.+ /H.sup.+ exchanger). These compounds are therefore outstandingly suitable for treatment of all illnesses which are to be attributed to increased Na.sup.+ /H.sup.+ exchange.
    Type: Grant
    Filed: August 20, 1997
    Date of Patent: December 21, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Andreas Weichert, Hans-Willi Jansen, Wolfgang Scholz
  • Ortho-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent, and a medicament comprising them
    Patent number: 6001881
    Abstract: Benzoylguanidines of the formula I ##STR1## in which: R(1) to R(4) have the meanings given in the claims, are antiarrhythmic pharmaceuticals, having a cardioprotective component, which are also valuable for the prevention of ischemically induced damage, in particular in association with the triggering of ischemically induced cardiac arrhythmias. As a consequence of inhibiting the cellular Na.sup.+ /H.sup.+ exchange mechanism, they are used for treating acute or chronic damage triggered by ischemia. In addition to this, they are notable for their strong inhibitory effect on the proliferation of cells. They are suitable for preventing the genesis of high blood pressure.
    Type: Grant
    Filed: June 4, 1997
    Date of Patent: December 14, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
  • Fluoroalkyl/alkenyl-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them
    Patent number: 5998481
    Abstract: There are described benzoylguanidines of the formula I ##STR1## having the definitions of R(1) to R(4) indicated in the text, and their pharmaceutically tolerable salts. They are obtained by reaction of a compound II ##STR2## with guanidine. They are outstanding agents for the treatment of disorders of the cardiovascular system.
    Type: Grant
    Filed: February 24, 1998
    Date of Patent: December 7, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Andreas Weichert, Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz