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
Abstract: The present invention relates to a novel process for preparing 1-(3-trialkylsilylphenyl)-2,2,2-trifluoromethyl ethanones which are useful for the treatment of Alzheimer's disease and senile dementia as disclosed by Schirlin, et al. in European Patent Application Publication No. 0 409 676, published Jan. 23, 1991.
Abstract: The present invention related to novel (R)-dimethyl N-tritylaspartate and novel (R)-alkyl N-trityl-4-oxo-5-phosphononorvalinate derivatives which are useful in the preparation of the class of beta-ketophosphonate NMDA antagonists.
Abstract: The present invention is directed to a class of 4,6-disubstituted tryptophan derivatives, 4,6-disubstituted kynurenines, their use as NMDA antagonists and to pharmaceutical compositions containing these compounds.
Type:
Grant
Filed:
July 17, 1995
Date of Patent:
August 20, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Michael G. Palfreyman, Ian A. McDonald, Francesco G. Salituro, Robert Schwarcz
Abstract: The oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a number average molecular weight of <10,000. These oligomers are water-soluble, have a rigid backbone with a predictable anion spacing, and are pharmaceutically-acceptable. The oligomers are useful for the treatment and/or diagnosis of HSV and HCMV.
Type:
Grant
Filed:
March 21, 1995
Date of Patent:
August 20, 1996
Assignees:
The Dow Chemical Co., Merrell Pharmaceuticals Inc.
Inventors:
Alan D. Cardin, Richard L. Jackson, Michael J. Mullins
Abstract: This invention relates to novel hydrazide acyl hydrazinium derivatives of certain 3,4-dihydro-2H-1-benzopyrans of the formula ##STR1## the stereoisomers and mixtures thereof, their inner salts, and the pharmaceutically acceptable salts thereof whereinR is H or C.sub.1-6 alkyl,R.sub.1 is C.sub.1-6 alkyl,R.sub.2 is H or --C(O)R,R.sub.3 and R.sub.4 are independently C.sub.1-6 alkyl;R.sub.5 is C.sub.1-6 alkyl, or ##STR2## with R.sub.8 being H or halogeno, n is zero, 1, 2, or 3 andis a halide, --S(O).sub.3 R.sub.6, or nothing when the inner salt is formedR.sub.6 is H, C.sub.1-6 alkyl, phenyl or 4-methylphenyl,to the intermediates, processes and techniques for their preparation, to their ability to manifest the property of being free radical scavengers, and to their end-use application in the treatment of disease conditions capable of being ameliorated by free radical scavengers.
Type:
Grant
Filed:
October 6, 1994
Date of Patent:
August 13, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
Abstract: Piperidinyl thiacyclic derivatives ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are defined in the specification. useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT.sub.2 receptors, pharmaceutical compositions and a methods of treatment using these compounds.
Type:
Grant
Filed:
May 24, 1995
Date of Patent:
July 30, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Albert A. Carr, John M. Kane, George D. Maynard, Hsien C. Cheng, Mark W. Dudley
Abstract: The invention is directed to a new class of antiarrhythmic agents of the formula: ##STR1## in which R is represented by hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, CF.sub.3, SR.sub.1, NHC(O)R.sub.2, NH.sub.2, or OH; R.sub.1 is hydrogen or C.sub.1-4 alkyl; R.sub.2 is C.sub.1-4 alkyl; X is represented by CO or CHOH; R.sub.3 and R.sub.4 are each independently represented by methyl, ethyl, n-propyl, or R.sub.3 and R.sub.4 together with the carbon atom to which they each are attached form a C.sub.5 or C.sub.6 cycloalkyl; and Alk is a C.sub.1-4 alkyl; or a pharmaceutically acceptable addition salt thereof.
Type:
Grant
Filed:
June 2, 1995
Date of Patent:
July 30, 1996
Assignee:
Merrell Pharmaceuticals, Inc.
Inventors:
Albert A. Carr, Richard C. Dage, David A. Hay, John E. Koerner, Tung Li
Abstract: This invention relates to novel purine nucleoside phosphorylase inhibitors, to the methods and intermediates for their preparation and to their use as immuno-suppressants, antilymphoma, antileukemic, antiviral and antiprotozoal agents.
Abstract: This invention relates to novel N-derivatives of 1-deoxy nojirimycin, to the method for their preparation and to their use in the treatment of diabetes and the use against retro-viruses, particularly in the treatment of acquired immuno-deficiency syndrome (AIDS).
Type:
Grant
Filed:
July 14, 1993
Date of Patent:
July 16, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Brigitte Lesur, Jean-Bernard Ducep, Charles Danzin
Abstract: This invention relates to substituted silyl alkylene amines, to the intermediates and processes useful for their preparation, to their pharmacological use as MAO-B inhibitors and to their end-use application in the treatment of Parkinson's Disease and senile dementia of Alzheimer's type.
Type:
Grant
Filed:
September 21, 1994
Date of Patent:
July 2, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Daniel G. Schirlin, Jean-Noel Collard, Charles Danzin
Abstract: This invention relates to certain 2,6-di-alkyl-4-silyl-phenols which are useful as inhibitors of LDL lipid peroxidation and as antiatherosclerotic agents.
Abstract: The present invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar-Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -C.sub.4 alkyl; or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;A is a bond, methylene or oxygen, sulfur or NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar-Y- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar-Y- group;R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ;R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; andn is an integer 1 to 3,which are useful as inhibitors of enkephalinase and ACE.
Abstract: This invention relates to substituted silyl alkylene amines, to the intermediates and processes useful for their preparation, to their pharmacological use as MAO-B inhibitors and to their end-use application in the treatment of Parkinson's Disease and senile dementia of Alzheimer's type.
Type:
Grant
Filed:
January 27, 1995
Date of Patent:
June 25, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Daniel G. Schirlin, Jean-Noel Collard, Charles Danzin
Abstract: The present invention relates to certain novel mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and of ACE.
Type:
Grant
Filed:
April 5, 1995
Date of Patent:
June 18, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Gary A. Flynn, Philippe Bey, Alan M. Warshawsky, Douglas W. Beight, Shujaath Mehdi, Eugene L. Giroux, Timothy P. Burkholder, Edward D. Daugs, John F. French