Abstract: A mini-proinsulin, in which the amino acid Arg bridges the A and the B chain instead of the C chain, shows insulin activity and is suitable for the preparation of pharmaceuticals for the treatment of diabetes mellitus. It can furthermore be converted into an insulin derivative simply using trypsin, the B chain of which is lengthened by Arg. This can be converted into insulin using carboxypeptidase B. Advantageously, however, the mini-proinsulin can also be converted to insulin directly in a one-pot process.
Type:
Grant
Filed:
March 10, 1995
Date of Patent:
April 5, 2005
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Michael Dörschug, Paul Habermann, Gerhard Seipke, Eugen Uhlmann
Abstract: The present invention relates to compounds of the formula I A—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:
May 13, 2002
Date of Patent:
March 15, 2005
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
Abstract: Use of inhibitors of cellular Na+/H+ exchanger (NHE) for the production of a medicament for the normalization of serum lipids
Type:
Application
Filed:
October 8, 2003
Publication date:
June 24, 2004
Applicant:
Hoechst Aktiengesellschaft
Inventors:
Hans Jochen Lang, Hans-Willi Jansen, Jan-Robert Schwark, Heinz-Werner Kleemann, Oliver Jung, Hans-Ludwig Schafer, Wolfgang Linz, Werner Kramer, Bernward Scholkens, Eugen Falk
Abstract: The present invention relates to compounds of the formulae I and Ia
in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their prodrugs, their preparation, their use, in particular as pharmaceutical active compounds, and pharmaceutical preparations comprising them. The compounds of the formula I are vitronectin receptor antagonists and can be employed, for example, as inhibitors of bone resorption and for the treatment of osteoporosis.
Type:
Grant
Filed:
June 15, 2000
Date of Patent:
April 20, 2004
Assignees:
Hoechst Aktiengesellschaft, Genentech
Inventors:
Anuschirwan Peyman, Jochen Knolle, Volkmar Wehner, Gerhard Breipohl, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek
Abstract: The present invention relates to 5-membered ring heterocycles of the formula I,
in which E, F, G, W, Y and Z have the meaning given in the patent claims, to their preparation and to their use as medicaments.
The novel compounds are used as vitronectin receptor antagonists and as inhibitors of bone reabsorption.
Type:
Grant
Filed:
February 21, 2002
Date of Patent:
September 16, 2003
Assignees:
Hoechst Aktiengesellschaft, Genentech, Inc.
Inventors:
Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Denis Carniato, Jean-Francois Gourvest, Tom Gadek, Robert McDowell
Abstract: Substituted 4-amino- and 4-alkoxy-cycloalkylpyrimidines, processes for their preparation, and their use as pesticides and fungicides
The invention relates to compounds of the formula
in which R1, R2, R3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.
Type:
Grant
Filed:
March 15, 1996
Date of Patent:
July 22, 2003
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lümmen, Werner Bonin
Abstract: The present invention relates to compounds of the formula I,
Type:
Application
Filed:
November 19, 2002
Publication date:
June 26, 2003
Applicant:
Hoechst Aktiengesellschaft and Genentech Inc.
Inventors:
Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
Abstract: Isolated cytohesin-PH peptides that can inhibit the beta-2 integrins from adhering, wherein the cytohesin-PH peptide has an amino acid sequence that comprises about a 140 amino acid domain from cytohesin-2. Assay kits comprising the peptides also are provided.
Abstract: Disclosed and claimed is an assay for identifying potential inhibitors of p-hydrophenylpyruvate dioxygenases (HPPD) from plants, in which an enriched HPPD from plants is incubated with a test substrate to be examined and the enzymatic activity of the enzyme is determined in comparison with the activity of the uninhibited enzyme. Also disclosed and claimed is a method of using the inhibitors of HPPD of a plant identified by the assay, such as their use as herbicides. Further disclosed and claimed are novel herbicidal active substances, including those of the formula (I)
which were found using the assay method according to the invention.
Abstract: The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.
Type:
Application
Filed:
April 24, 2002
Publication date:
April 3, 2003
Applicant:
Hoechst Aktiengesellschaft
Inventors:
Cenek Kolar, Jorg Czech, Klaus Bosslet, Gerhard Seemann, Hans-Harald Sedlacek, Dieter Hoffman
Abstract: The present invention relates to compounds of the formula I
Type:
Application
Filed:
May 13, 2002
Publication date:
February 6, 2003
Applicant:
Genentech, Inc. and Hoechst Aktiengesellschaft
Inventors:
Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
Abstract: Compounds of the formula I
in which B, D, E, R, W, Y, Z, b, c, d, e, f, g and have the meanings indicated in the claims, are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belongs to the group of integrins. The invention relates to the use of compounds of the formula I, and of pharmaceutical preparations which contain such compounds, for the treatment and prophylaxis of diseases which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or which are associated therewith or in which cell—cell or cell-matrix interactions play a part which are based on interactions of VLA-4 receptors with their ligands, for example of inflammatory processes, rheumatoid arthritis or allergic disorders, and it also relates to the use of compounds of the formula I for the production of pharmaceuticals for use in such diseases. It further relates to novel compounds of the formula I.
Type:
Grant
Filed:
September 27, 1999
Date of Patent:
February 4, 2003
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Hans Ulrich Stilz, Volkmar Wehner, Christoph Huels, Dirk Seiffge
Abstract: Spiro compounds of the formula I
in which &psgr; is C, Si, Ge or Sn and K1 and K2 independently of one another are conjugated systems, are suitable as materials in nonlinear optics.
Abstract: This invention relates to fluorophenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them. An embodiment of the invention embraces compounds of the formula I:
and the pharmaceutically tolerated salts thereof. The disclosed compounds are valuable inhibitors of the cellular sodium/proton exchanger (Na+ /H+ exchanger) . They are therefore outstandingly suitable for the treatment of all diseases attributable to increased Na+ /H+ exchange.
Type:
Grant
Filed:
December 20, 2001
Date of Patent:
January 7, 2003
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Jan-Robert Schwark, Hans-Jochen Lang, Heinz-Werner Kleemann, Andreas Weichert, Wolfgang Scholz, Udo Albus
Abstract: Five-membered heterocycles having biphenylsulfonyl substitution, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I
in which the symbols have the meanings indicated in the claims, have outstanding antiarrhythmic properties and exhibit a cardioprotective component. They can preventively inhibit or greatly decrease the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias. Moreover, they have a potent inhibitory action on the proliferation of cells.
Type:
Grant
Filed:
October 30, 2001
Date of Patent:
November 26, 2002
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Sabine Faber, Hans-Willi Jansen
Abstract: Mixtures of isomeric nonanols and decanols are obtained by joint aldol condensation of n-butanal and pentanals, and up to 1% by weight of 3-methylbutanal, hydrogenation of the aldol condensation product to the corresponding saturated alcohols, and separation from the reaction mixture of the components boiling at temperatures lower than those of the nonanols and decanols. The pentanals are mixtures of 60 to 90% by weight of n-pentanal and 10 to 40% by weight of 2-methylbutanal. The alcohol mixture is especially suitable for preparing ester plasticizers.
Type:
Grant
Filed:
May 8, 1995
Date of Patent:
November 19, 2002
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Helmut Bahrmann, Wilfried Fenske, Wolfgang Greb, Peter Heymanns, Peter Lappe, Thomas Müller, Jürgen Szameitat, Ernst Wiebus
Abstract: Compounds of the formula I and their salts, as defined in claim 1, are suitable as safeners for protecting crop plants against the phytotoxic side-effects of herbicides.
Type:
Grant
Filed:
January 29, 1998
Date of Patent:
November 19, 2002
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Xenia Holdgrün, Lothar Willms, Klaus Bauer, Klaus Trinks, Hermann Bieringer
Abstract: Poly(p-arylene-vinylenes) comprising repeating units of the formula (I),
where the symbols and indices have the following meanings:
Y1, Y2, Y3: identical or different, CH, N;
Aryl: an aryl group having from 4 to 14 carbon atoms;
R′, R″: identical or different, each a straight-chain or branched or cyclic alkyl or alkoxy group having from 1 to 20 carbon atoms, where one or more non-adjacent CH2 groups may be replaced by —O—, —S—, —CO—, —COO—, —O—CO—, —NR1—, —(NR2R3)+—A−, or —CONR4— and one or more H atoms may be replaced by F, or else CN, F, Cl or an aryl group having from 4 to 14 carbon atoms which may be substituted by one or more nonaromatic radicals R′;
R1, R2, R3, R4: identical or different, aliphatic or aromatic hydrocarbon radicals having from 1 to 20 carbon atoms or else H;
A−: a singly charged anion or its equivalent;
m: 0, 1 or 2;
n: 1, 2, 3,
Type:
Grant
Filed:
December 16, 1997
Date of Patent:
October 1, 2002
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Hubert Spreitzer, Willi Kreuder, Heinrich Becker, Harmannus Schoo, Robert Demandt