Abstract: Novel pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the 1,2-benzisoxazoles and -benzisothiazoles and intermediates, or compositions thereof are disclosed.
Type:
Grant
Filed:
October 30, 1997
Date of Patent:
September 7, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
David M. Fink, Barbara E. Kurys, Gregory M. Shutske, John D. Tomer, IV
Abstract: The invention provides a pharmaceutical composition in solid unit dosage form, comprising, a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and, b) at least one inert ingredient.
Type:
Grant
Filed:
October 9, 1997
Date of Patent:
August 3, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Thomas T. Ortyl, Paul F. Skultety, Kristen C. Mitchell, Deepak S. Phadke, Faraneh Attarchi, Marguerite L. Pierce, Aaron W. Schoeneman, Joseph M. Schnitz
Abstract: The present invention relates to novel N-methyl-N-(4-(4-(1H-benzimidazol-2-yl)?1,4!diazepan-1-yl)-2-(aryl)butyl)b enzamide derivatives of the formula: ##STR1## stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Type:
Grant
Filed:
March 6, 1998
Date of Patent:
August 3, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
George D. Maynard, John M. Kane, Christopher R. Dalton, Braulio Santiago, Elizabeth M. Kudlacz, Larry D. Bratton
Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5, Y.sub.7, Y.sub.8 and Y.sub.9 are each nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.
Type:
Grant
Filed:
November 20, 1997
Date of Patent:
July 27, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful or the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.
Abstract: The present invention relates to novel substituted N-methyl-N-(4-(4-(1H-benzimidazol-2-yl-amino)piperidin-1-yl)-2-(aryl)butyl )benzamide derivatives of the formula: ##STR1## stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Type:
Grant
Filed:
January 6, 1997
Date of Patent:
July 13, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
George Daniel Maynard, John Michael Kane, Braulio Santiago, Elizabeth Mary Kudlacz, Larry Don Bratton, Christopher Robin Dalton
Abstract: A method of determining the degree of aggregation of the .beta.A4 peptide is disclosed. The method comprises reacting the protein with a suitable binding agent which is capable of binding the .beta.A4 peptide only in its non-aggregated state to form an amount of protein bound binding reagent. The amount of protein bound binding agent is then measured.
Type:
Grant
Filed:
July 17, 1996
Date of Patent:
July 6, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Shefali Goyal, Joseph W. Paul, Norbert G. Riedel, Sudhir R. Sahasrabudhe
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:
July 6, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: This invention relates to N-hydroxy-dibenz?b,e!oxepinalkylamines, N-hydroxy-dibenz?b,e!oxepinalkanoic acid amides and related heterocyclic analogues of the formula ##STR1## where X together with the carbon atoms to which it is attached forms a benzene or thiophene ring; W and Z are independently hydrogen, halogen, loweralkyl, or trifluoromethyl; R.sup.1 is hydrogen, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; R.sup.2 is loweralkyl, cycloalkyl, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; m is 0 or 1 and n is an integer of 0 to 4 or the pharmaceutically acceptable salts thereof. The compounds of this invention are useful as analgesics and topical antiinflammatory agents for the treatment of various dermatoses and agents for the treatment of conditions where accumulation of cyclooxygenase and/or lipoxygenase metabolites is a causative factor.
Type:
Grant
Filed:
February 27, 1998
Date of Patent:
June 29, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Richard C. Allen, Grover C. Helsley, R. Richard L. Hamer, Brian S. Freed, John I. White, Lawrence L. Martin
Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5 and Y.sub.9 are each nitrogen and Y.sub.7 and Y.sub.8 are a CH group,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.
Type:
Grant
Filed:
November 20, 1997
Date of Patent:
June 29, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
Abstract: This invention relates to novel Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3 and Y.sub.8 are CH, Y.sub.5, Y.sub.7 and Y.sub.9 are each independently nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.
Type:
Grant
Filed:
November 20, 1997
Date of Patent:
May 18, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
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:
March 30, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau
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:
March 30, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: 4,5-Dihydronaphth?1,2-c!isoxazole derivatives of the general formula: ##STR1## where A, X and n are defined herein are disclosed. Such compounds are useful as serotonin 5-HT.sub.3 antagonists. These compounds art useful for the treatment of anxiety, psychiatric disorders, nausea, vomiting and drug dependency.
Abstract: 2,3-dihydro-1H-isoindole derivatives of the formula ##STR1## where R.sub.1 -R.sub.5 and X are defined herein which are useful as serotonin reuptake inhibitors are disclosed. As such, these compounds may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.
Type:
Grant
Filed:
September 22, 1997
Date of Patent:
February 23, 1999
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
Gregory Michael Shutske, Kevin James Kapples
Abstract: 2,3-dihydro-1H-isoindole derivatives of the formula ##STR1## where R.sub.1 -R.sub.5 and X are defined herein which are useful as serotonin reuptake inhibitors are disclosed. As such, these compounds may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.
Type:
Grant
Filed:
September 22, 1997
Date of Patent:
February 23, 1999
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
Gregory Michael Shutske, Kevin James Kapples
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:
February 23, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme.
Abstract: There are disclosed various substituted 4-amino-3-pyridinol compounds of the formula below, ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
Type:
Grant
Filed:
June 2, 1998
Date of Patent:
February 9, 1999
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
Gregory Michael Shutske, Kevin James Kapples, John Dick Tomer, Nicholas Joseph Hrib, John Gerard Jurcak
Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
Type:
Grant
Filed:
January 8, 1997
Date of Patent:
February 9, 1999
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley