Abstract: A subject of the invention is the products of formula (I):
in which:
R1 and R2 represent in particular cyano and trifluoromethyl,
R3 represents in particular alkyl, alkenyl or alkynyl, substituted in particular by nitrooxy or carbonyloxy,
R4 and R5 represent in particular methyl optionally substituted by fluorine,
X and Y represent in particular oxygen, as well as their salts and isomers.
Type:
Grant
Filed:
September 28, 1998
Date of Patent:
June 5, 2001
Assignee:
Hoechst Marion Roussel
Inventors:
Andre Claussner, Francois Goubet, Jean-Georges Teutsch
Abstract: A subject of the invention is the compounds of formula (I):
in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.
Type:
Grant
Filed:
November 29, 1999
Date of Patent:
May 29, 2001
Assignee:
Hoechst Marion Roussel
Inventors:
Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
Abstract: The invention relates to a novel process for preparing compounds of the formula (IV) or (I):
from the racemic alkoxyfuranone of the formula (II):
R1 and R2 being as defined in the description, to the novel compounds of the formula (IV) as well as to the intermediate compounds of this process, and to the use of the compounds of the formula (IV) or (I) in the process for the synthesis of compounds which inhibit interleukin-1beta converting enzyme.
Type:
Grant
Filed:
February 1, 2000
Date of Patent:
May 22, 2001
Assignee:
Hoechst Marion Roussel
Inventors:
Raphael Bouchet, Francis Brion, Colette Colladant, Jacques Lagouardat
Abstract: Novel spiro[cyclopent[b]indole-piperidines], intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the spiro[cyclopent[b]indole-piperidines] and intermediates, or compositions thereof are disclosed.
Abstract: A reagent for immunologically detecting rheumatism containing as an antigen at least one mammalian protein selected from among ezrin, radixin and moesin and/or a peptide composed of at least nine consecutive amino acid residues found in the amino acid sequences of ezrin, radixin and moesin; and a method of detecting autoantibodies present in the serum of a rheumatic. An immunological reaction using this reagent enables precritical or early diagnosis of rheumatism. An immunological detection using the above autoantigenic proteins is convenient and reliable as an early serodiagnostic method based on rheumatism-specific antigens.
Type:
Grant
Filed:
January 22, 1999
Date of Patent:
May 1, 2001
Assignees:
Dade Behring Marburg GmbH, Hoechst Marion Roussel Ltd.
Abstract: The subject of the invention is the products of formula (I):
in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.
Type:
Grant
Filed:
February 2, 1999
Date of Patent:
April 24, 2001
Assignee:
Hoechst Marion Roussel
Inventors:
Serge Bernard, Denis Carniato, Jean-Francois Gourvest, Jean-Georges Teutsch, Jochen Knolle, Hans-Ulrich Stilz, Volkmar Wehner, Sarah C. Bodary, Thomas R. Gadek, Robert S. McDowell, Robert M. Pitti
Abstract: A subject of the invention is a modified yeast strain in which the acetyl-CoA pregnenolone acetyltransferase (APAT) activity is eliminated by altering the gene coding for this activity with resultant stabilization of 3&bgr;-hydroxysteroids.
Type:
Grant
Filed:
February 1, 1999
Date of Patent:
April 17, 2001
Assignee:
Hoechst Marion Roussel
Inventors:
Tilman Achstetter, Gilles Cauet, Eric Degryse
Abstract: The invention concerns steroid compounds of general formula (I) in which n=2, 3, either R1 and R2═H, (C1-C4) alkyl, or R1 and R2 form with nitrogen a heterocyclic compound, X═OH optionally esterified, Y═(C1-C4)alkyl, and their additive salts, the method for preparing them, their application as medicine and the pharmaceutical compositions containing them.
Type:
Grant
Filed:
October 4, 1999
Date of Patent:
March 27, 2001
Assignee:
Hoechst Marion Roussel
Inventors:
Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
Abstract: The object is to provide a promoting agent for bone formation, a therapeutic method for bone formation and a process for preparing a promoting agent for bone formation.
A promoting agent for bone formation which comprises at least one of kistrin, echstatin, a peptide or polypeptide containing the amino acid sequence ArgGlyAsp in the molecule such as a peptide represented by Gly-Arg-Gly-Asp-Ser or a compound represented by the following general formula (IX) and so on, as well as a biologically acceptable salt thereof
wherein R16 represents —N(R20)2 (R20 represents a hydrogen atom or a C1-C4 alkyl group), R17 represents a hydrogen atom or a C1-C4 alkyl group, R18 represents a hydrogen atom, a C1-C4 alkyl group and so on, R19 represents OH, NH2 and so on, Y represents —NH—, —O— or a direct bond, a represents 1-3, b represents 1 or 2, c represents 0 or 1 and d represents 0 or 1.
Type:
Grant
Filed:
April 20, 1999
Date of Patent:
February 27, 2001
Assignee:
Hoechst Marion Roussel
Inventors:
Kazuyuki Kitamura, Osamu Komiyama, Mizuho Inazu, Roland Baron, Thomas R. Gadek, Hans-Ulrich Stilz, Volkmar Wehner, Jochen Knolle, Robert S. McDowell
Abstract: 5-Membered ring heterocycle of the formula I,
in which D includes a COOR15, CON(CH3)R15 or CONHR15 radical and R15 includes a 6-24 member bicyclic or tricyclic radical, compositions, preparation and use as inhibitors of thrombocyte aggregation, metastasization of carcinoma cells, binding of osteoclasts to bone surfaces and for the treatment of tromboses.
Type:
Grant
Filed:
July 28, 1999
Date of Patent:
February 20, 2001
Assignee:
Hoechst Marion Roussel
Inventors:
Gerhard Zoller, Otmar Klingler, Bernd Jablonka, Melitta Just, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig, Hans-Ulrich Stilz
Abstract: Compounds of the formula I
having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal illnesses.
Type:
Grant
Filed:
August 4, 1998
Date of Patent:
February 6, 2001
Assignee:
Hoechst Marion Roussel Deutschland GmbH
Inventors:
Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann, Joachim Brendel
Abstract: The present invention is new 3-(heterocyclic)-propenoic acid derivatives and pharmaceutical compositions thereof. These new 3-(heterocyclic)-propenoic acid derivatives are useful as NMDA antagonist.
Abstract: DNA sequences coding for human polypeptides with protease activity and capable of inducing apoptosis, related to the interleukin-1beta converting enzyme are disclosed.
Type:
Grant
Filed:
March 15, 1999
Date of Patent:
January 30, 2001
Assignee:
Hoechst Marion Roussel
Inventors:
Anita Diu, Chi Faucheu, Thierry Hercend, Jean Louis Lalanne, David J Livingston, Michael Su
Abstract: Compounds useful as preventive and therapeutic agents for bone and cartilage diseases; and drug compositions containing the same. The compounds are polyhydroxyphenol derivatives of general formula (I)
and quinione analogues derived therefrom (wherein R1 is alkyl, optionally substituted benzyl or optionally substituted aryl; R2 is hydrogen, alkyl, alkenyl or optionally substituted benzyl; R3 is hydrogen, alkyl, alkenyl, optionally substituted benzyl, hydroxyl, alkoxy, alkenyloxy or optionally substituted benzyloxy; R4 is hydrogen, alkyl, alkenyl, optionally substituted benzyl or hydroxyl; and R5 and R6 are each independently hydrogen, alkyl, alkenyl or optionally substituted benzyl). The polyhydroxyphenol derivatives and the quinone analogues exhibit a potent inhibitory activity against bone resorption and are useful as preventive and therapeutic agents for bone and cartilage diseases.
Abstract: An expression cassette, operable in a recombinant host, comprising a heterologous DNA coding sequence encoding a protein, which is functional, alone or in cooperation with one or more additional proteins, of catalyzing an oxidation step in the biological pathway for conversion of cholesterol into hydrocortisone, which step is selected from the group consisting of:
the conversion of cholesterol to pregnenolone;
the conversion of pregnenolone to progesterone;
the conversion of progesterone to 17&agr;-hydroxyprogesterone;
the conversion of 17&agr;-hydroxyprogesterone to cortexolone;
the conversion of cortexolone to hydrocortisone, and the corresponding control sequences effective in said host.
Type:
Grant
Filed:
June 17, 1998
Date of Patent:
January 9, 2001
Assignee:
Hoechst Marion Roussel
Inventors:
Herman Slijkhuis, Eric Bastiaan Smaal, Gerardus Cornelis Maria Selten
Abstract: A cosmetic or pharmaceutical composition containing a dermatologically effective amount of at least one liposome containing a compound of the formula ##STR1##