Abstract: Compounds of the formula I ##STR1## 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 gastro-intestinal region or for the treatment of diarrheal illnesses.
Type:
Grant
Filed:
November 9, 1998
Date of Patent:
January 18, 2000
Assignee:
Hoechst Marion Roussel Deutschland GmbH
Inventors:
Joachim Brendel, Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann
Abstract: The present invention relates certain mercaptoacetylamide disulfide derivatives of the formula ##STR1## useful in treating patients suffering from hypertriglyceridemia, atherosclerosis and hypercholestrolemia.
Type:
Grant
Filed:
November 24, 1997
Date of Patent:
January 11, 2000
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Gary A. Flynn, John F. French, Richard C. Dage
Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2)a-(X.sub.1).sub.b -Q.sub.1 -Q.sub.2 -C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radical or one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 -R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2, their preparation process and their use as pesticides.
Type:
Grant
Filed:
July 30, 1997
Date of Patent:
January 11, 2000
Assignee:
Hoechst Marion Roussel
Inventors:
Jacques Demassey, Michel Gohar, Christian Wehrey
Abstract: A subject of the invention is the compounds of formula (I): ##STR1## in which R represents a carboxylic acid remainder containing up to 18 carbon atoms the products of formula (I) can be used to prepare antibiotic products.
Type:
Grant
Filed:
April 20, 1998
Date of Patent:
January 4, 2000
Assignee:
Hoechst Marion Roussel
Inventors:
Alain Bonnet, Bernadette Chappert, Jacques Lagouardat
Abstract: This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase, and to novel processes for making the same. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient afflicted with a neutrophil associated inflammatory disease.
Type:
Grant
Filed:
November 22, 1996
Date of Patent:
December 28, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Timothy T. Curran, Joseph P. Burkhart, Michael R. Angelastro, Norton P. Peet, William A. Metz, Jr.
Abstract: Sulfonamide-substituted benzopyran derivatives, processes for their preparation, their use as a medicament, and pharmaceutical preparations comprising them Compounds of the formula I ##STR1## 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 diseases.
Type:
Grant
Filed:
November 2, 1998
Date of Patent:
December 28, 1999
Assignee:
Hoechst Marion Roussel Deutschland GmbH
Inventors:
Joachim Brendel, Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann
Abstract: This invention relates to compounds of the formula wherein X, Y, Z, m, n and p are as defined within, pharmaceutical compositions containing these compounds and to their use as antipsychotic agents, particularly in the treatment of schizophrenia. Depot derivatives of the compounds are useful for providing long acting effects of the compounds.
Type:
Grant
Filed:
April 8, 1999
Date of Patent:
December 28, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Mark G. Palermo, Lawrence L. Martin, Peter A. Nemoto
Abstract: The invention relates to the cytoplasmic expression of antibodies, antibody fragments and antibody fragment fusion molecules in E. coli. In particular, antibody fragment fusion molecules having an antibody moiety which is directed against tumors and an enzyme moiety which cleaves a nontoxic prodrug to give the toxic drug can be advantageously prepared in this way while retaining their respective functional properties.
Type:
Grant
Filed:
April 10, 1996
Date of Patent:
December 28, 1999
Assignee:
Hoechst Marion Roussel Deutschland GmbH
Inventors:
Martin Opper, Klaus Bosslet, Joerg Czech
Abstract: The present invention describes certain alkyloxyamino-substituted fluorenones which inhibit protein kinase C, as well as pharmaceutical compositions including these compounds and methods of using these compounds to control protein kinase C activity in mammals, including humans. More specifically, the present compounds are useful for the treatment of neoplastic disease states, disorders associated with abnormal blood flow (including hypertension, ischemia, atherosclerosis, coagulation disorders), and inflammatory diseases (including immune disorders, asthma, lung fibrosis, and psoriasis).
Type:
Grant
Filed:
April 18, 1997
Date of Patent:
December 21, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Winton D. Jones, Fred L. Ciske, Robert J. Dinerstein, Keith A. Diekema
Abstract: A subject of the invention is the compounds of general formula (I): ##STR1## in which R1=H, alkyl, acyl, R2 and R3=H, alkyl, R4=aryl, heteroaryl, X=O, CH2, Y=OH, O-alkyl or NRaRb, as well as the salts, their preparation processes, the intermediates of these processes, their use as medicaments and the pharmaceutical compositions containing them.
Abstract: The present invention relates to novel triptolide derivatives and a method of treating a patient suffering from an autoimmune disease comprising administering to a patient an effective amount of the novel triptolide derivatives.
Type:
Grant
Filed:
May 12, 1998
Date of Patent:
December 21, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Michel J. Jung, Mahinda Wickramaratne, Michael Hepperle
Abstract: The present invention comprises (4-Piperidinyl)-1H-2-Benzopyran derivatives useful as antipsychotic agents, their intermediates, pharmaceutical compositions and methods of making these compounds. These compounds are useful in treating psychosis.
Type:
Grant
Filed:
January 22, 1998
Date of Patent:
December 21, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Joseph T. Stupczewski, Kenneth J. Bordeau, Shelley L. Pavlek
Abstract: Compounds of the formula ##STR1## in all possible racemic, enantiomeric and diastereoisomeric forms and their non-toxic, pharmaceutically acceptable salts with acids and bases having antagonistic properties for angiotensin II receptors and a process and novel intermediates for their properties.
Type:
Grant
Filed:
May 1, 1998
Date of Patent:
December 21, 1999
Assignee:
Hoechst Marion Roussel
Inventors:
Francois Clemence, Michel Fortin, Jean-Luc Haesslein
Abstract: Novel N-(pyridinylamino)isoindolines and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the N-(pyridinylamino)isoindolines and related compounds, the intermediates or compositions thereof are disclosed.
Type:
Grant
Filed:
October 29, 1997
Date of Patent:
December 21, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Barbara E. Kurys, David M. Fink, Brian S. Freed, Gregory H. Merriman
Abstract: A compound of the formula ##STR1## wherein alc.sub.1, alc.sub.2 and alc.sub.3 are alkyl of up to 8 carbon atoms, n is an integer from 0 to 8, R.sub.1 and R.sub.
Type:
Grant
Filed:
September 28, 1998
Date of Patent:
December 14, 1999
Assignee:
Hoechst Marion Roussel
Inventors:
Alain Bonnet, Raphael Bouchet, Daniel Guilmard, Alain Mazurie
Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 7, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Peter A. Nemoto, John J. Tegeler
Abstract: Described herein are compounds of the general formula: ##STR1## a stereoisomer, solvate, or pharmaceutically acceptable salt thereof, wherein:R.sub.1 is H, halo, aryl or aryl substituted with one or two groups independently selected from halo, C.sub.1-4 alkyl, C.sub.1-4 -alkoxy, nitro, trifluoromethyl, trifluoromethoxy or cyano;R.sub.2 is C.sub.4-9 alkyl; phenyl or phenyl substituted with one or two groups selected independently from OH, cyano, halo, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, trifluoromethyl, trifluoromethoxy, nitro or phenyl; naphthyl;phenyl fused to a 5 or 6-membered heterocycle; the coumarin moiety ##STR2## wherein R.sub.3 and R.sub.4 are selected independently from H, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;or 1,2-methylenedioxy phenyl;with the proviso that R.sub.2 is not phenyl or 3,4-dimethoxyphenyl when R.sub.1 is H.Also described is their use as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia and anxiety.
Type:
Grant
Filed:
August 8, 1997
Date of Patent:
December 7, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Xin Wang, Jian-min Fu, Adi M. Treasurywala
Abstract: The invention relates to the preparation of the compound 4-(4-(4-(hydroxydiphenyl)-1-piperidinyl)-1-hydroxybutyl)-.alpha.,.alpha.-d imethylphenylacetic acid and its phosphorylated derivatives. These compounds can be prepared from .alpha.-(p-tert-butylphenyl)-4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-1-pi peridinylbutanol with the aid of fungi of the genus Cunninghamella or Absidia. The compounds according to the present invention can be used as pharmaceuticals for the treatment of allergic disorders, allergic rhinitis or asthma. Compounds of the formula II in which R.sup.1 is --CH.sub.2 --O--P(O)(OH).sub.2 and R.sup.2 is --OH; R.sup.1 is --CH.sub.3 and R.sup.2 is --O--P(O)(OH).sub.2 ; orR.sup.1 is --COOH and R.sup.2 is --O--P(O)(OH).sub.2 are produced by the process according to the present invention and are suitable as pharmaceuticals with antihistamine action.
Abstract: A nucleic acid sequence containing a sequence coding for a protein having a delta-5,7 sterol, delta-7 reductase activity, said nucleic acid being a DNA or an RNA, production process, strains of transformed yeasts and uses thereof.
Type:
Grant
Filed:
January 14, 1997
Date of Patent:
November 23, 1999
Assignee:
Hoechst Marion Roussel
Inventors:
Xavier Chenivesse, Catherine Duport, Eric Lecain, Denis Pompon
Abstract: The invention relates to the new products of formula (I): ##STR1## in which: R.sub.1 represents alkyl,A represents a sulphur or oxygen atom,R.sub.2 represents carboxy, tetrazolyl or alkyl, alkoxy, alkylthio substituted by a carboxy or a tetrazolyl,Hal.sub.1 is halogen, q represents an integer from 0 to 4,R.sub.3 is formyl, carboxy or tetrazolyl,Y represents phenyl substituted by a dioxol radical and optionally by a halogen atom, or by an alkyl or alkoxy radicalas well as all the possible racemic, enantiomeric and diastereoisomeric isomer forms, as well as the addition salts of said products of formula (I).