Abstract: The present invention is directed to esters of (+)-.alpha.-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol, pharmaceutical formulations, methods of making and methods of using these esters. These compounds antagonize the effects of serotonin at the 5HT.sub.2A receptor and are useful in treating various conditions such as, for example, psychoses such as schizophrenia.
Type:
Grant
Filed:
June 22, 1999
Date of Patent:
May 16, 2000
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Albert A. Carr, Raymond W. Kosley, Jr., Luc Van Hijfte
Abstract: The present invention is directed to esters of (+)-.alpha.-(2,3 Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, pharmaceutical formulations, methods of making and methods of using these esters. These compounds antagonize the effects of serotonin at the 5HT.sub.2A receptor and are useful in treating various conditions such as, for example, psychoses such as schizophrenia.
Type:
Grant
Filed:
July 25, 1997
Date of Patent:
February 22, 2000
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Albert A. Carr, Raymond W. Kosley, Jr., Luc Van Hijfte
Abstract: The present invention is directed to the use of (+)-.alpha.-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol in treating Depressive Disorders and Bipolar Disorders.
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: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol, and its use in the treatment of a number of disease states.
Type:
Grant
Filed:
November 13, 1998
Date of Patent:
December 21, 1999
Assignee:
Merrell Pharmaceuticals, Inc.
Inventors:
Albert A. Carr, John M. Kane, David A. Hay
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 present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-?2-(4-fluorophenyl)ethyl!-4-piperidine methanol, and its use in the treatment of a number of disease states.
Type:
Grant
Filed:
October 2, 1997
Date of Patent:
February 23, 1999
Assignee:
Merrell Pharmaceutical, Inc.
Inventors:
Albert A. Carr, John M. Kane, David A. Hay, Christopher J. Schmidt
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:
March 8, 1994
Date of Patent:
November 24, 1998
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: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-?2-(4-fluorophenyl)ethyl!-4-piperidine methanol, and its use in the treatment of a number of disease states.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
February 24, 1998
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Albert A. Carr, John M. Kane, David A. Hay, Christopher J. Schmidt
Abstract: Derivatives of 2,3-dihydro-5-benzofuranol, intermediates thereof, and processes useful for their preparation. These compounds are free radical scavengers and are useful in the treatment of conditions capable of being treated by free radical scavengers, such as stroke, nervous system trauma and reperfusion damage.
Type:
Grant
Filed:
December 22, 1994
Date of Patent:
February 24, 1998
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-vital agents.
Type:
Grant
Filed:
January 23, 1997
Date of Patent:
February 10, 1998
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Daniel Schirlin, Viviane Van Dorsselaer, Celine Tarnus
Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-viral agents.
Type:
Grant
Filed:
December 18, 1995
Date of Patent:
February 10, 1998
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Daniel Schirlin, Viviane Van Dorsselaer, Celine Tarnus
Abstract: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-?2-(4-fluorophenyl)ethyl!-4-piperidine methanol, and its use in the treatment of a number of disease states.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 23, 1997
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Albert A. Carr, John M. Kane, David A. Hay
Abstract: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-?2-(4-fluorophenyl)ethyl!-4-piperidine methanol, and its use in the treatment of a number of disease states.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 23, 1997
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Albert A. Carr, John M. Kane, David A. Hay
Abstract: This invention relates to a novel process for preparing 2,3-dihydro-benzofuranol derivatives and to the novel intermediates produced thereby.
Type:
Grant
Filed:
March 7, 1996
Date of Patent:
December 16, 1997
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Gilbert Marciniak, Richard A. Schnettler, Timothy A. Ayers, Damian J. Krysan
Abstract: The present invention is directed to a process for making (2S,5S)-5-fluoromethylornithine through the reaction of wet penicillin acylase with (2R,5R) and (2S,5S)-6-fluoromethyl-3-(phenylactyl)-amino-2-piperidone and the addition of an acid to the resulting product.
Abstract: Dipeptide compounds and analogs thereof having a phosphonomethyl moiety are disclosed. These compounds inhibit Endothelin Converting Enzyme and are thus useful in treating conditions responsive to inhibition of production of Endothelin.
Abstract: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol, and its use in the treatment of a number of disease states.
Type:
Grant
Filed:
January 13, 1995
Date of Patent:
October 1, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Albert A. Carr, John M. Kane, David A. Hay, Christopher J. Schmidt
Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-viral agents.
Type:
Grant
Filed:
June 30, 1993
Date of Patent:
September 24, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Daniel Schirlin, Viviane Van Dorsselaer, Celine Tarnus