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: Fluorinated silylated aromatic compounds, their intermediates, methods of use in treating diseases associated with deficiencies of cholinergic transmission in the central nervous system and methods for their preparation are disclosed.
Type:
Grant
Filed:
July 18, 1995
Date of Patent:
June 4, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Jean-Noel Collard, Jean-Marie Hornsperger
Abstract: Certain tetraarylethylenes reverse drug resistance in multi-drug resistant tumors. These compounds apparently function by inhibiting a p-glycoprotein pump which becomes activated in late stage tumor development and which is inherently present in tumors from certain origins.
Abstract: This invention relates to certain aristeromycin/adenosine derivatives which are useful in inhibiting AdoMet-dependent transmethylation and in the treatment of patients afflicted with neoplastic or viral disease states.
Type:
Grant
Filed:
November 1, 1994
Date of Patent:
May 28, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Esa T. Jarvi, James R. McCarthy, Nellikunja J. Prakash
Abstract: Antagonists of neurokinin A which are novel cyclic hexapeptide and octapeptide compounds are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.
Type:
Grant
Filed:
February 3, 1994
Date of Patent:
May 28, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Thomas J. Owen, Elizabeth M. Kudlacz, Scott L. Harbeson, Stephen H. Buck
Abstract: The present invention is new 3-(indol-3-yl)-propenoic acid derivatives and pharmaceutical compositions thereof. These new 3-indolyl-3-yl-prpopenoic acid derivatives are useful as NMDA antagonist.
Type:
Grant
Filed:
May 16, 1995
Date of Patent:
May 21, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Francesco G. Salituro, Bruce M. Baron, Boyd L. Harrison, Philip L. Nyce
Abstract: This invention relates to a process for the preparation of 10-(2-propynyl)-estr-4-ene-3,17-dione, whereby this compound is synthesized utilizing ketals prepared from the addition of 2,2-dimethyl-1,3-propanediol to the starting compound, 19-norandrost-5(10)-ene-3,17-dione (NAD). A new process for the addition of the propynyl group to steroid epoxides by means of higher order cuprates is also described herein.
Abstract: The present invention provides novel 5-(1-fluorovinyl)-1H-pyrimidine-2,4-dione derivatives which are useful as antineoplastic agents by themselves or in conjunctive therapy with the antineoplastic agent 5-fluorouracil.
Type:
Grant
Filed:
April 29, 1994
Date of Patent:
April 30, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
James R. McCarthy, Donald P. Matthews, Jeffrey S. Sabol
Abstract: This invention relates to a novel synthesis of 4-amino-5-hexenoic acid by thermal rearrangements, and to the novel intermediates produced thereby.
Abstract: This invention relates to certain hydroxy derivatives of 3,4-dihydro-2,5,7,8-tetraalkyl-2H-1-benzopyran-2-carboxylic acids and the lactones thereof, to the processes and intermediates useful for their preparation and to their use as free radical scavengers useful in the treatment of tissue damage implicated with free oxygen radicals.
Type:
Grant
Filed:
October 5, 1994
Date of Patent:
April 23, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
Abstract: Novel compounds which are chemically linked inhibitors of the proteases Elastase and Cathepsin G prevent connective tissue degradation associated with neutrophil induced inflammatory disease.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
April 23, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Michael R. Angelastro, Philippe Bey, Niall S. Doherty, Michael J. Janusz, Shujaath Mehdi, Norton P. Peet
Abstract: This invention relates to 5-chloro-2,3-dihydro-2,2-dimethylbenzofuran-7-carboxylic acid-octahydro-3-hydroxy-2,6-methano-2H-quinolizin-8-yl ester (I), a novel 5-HT.sub.3 -receptor antagonist, its method of preparation, and to its end-use application in the treatment or radio- and chemo-therapeutically-induced nausea and vomiting, in the treatment or pain associated with migraine, in the treatment of cognitive disorders, in treating hallucinatory endogenous psychoses or the type manifested in patients suffering from schizophrenia and mania, for irritable bowel syndrome, and to combat drug abuse.
Abstract: The present invention relates to a novel enantiospecific process for preparing (S)-1-[2(S)-(1,3-dihydro-1,3-dioxo-isoindo-2-yl)-1-oxo-3-phenylpropyl ]-1,2,3,4-tetrahydro-2-pyridine-carboxylic acid methyl ester which is a useful intermediate in the preparation of [4S-[4.alpha., 7.alpha.(R*), 12b.beta.]]-7-[(1-oxo-2(S)-thio-3-phenylpropyl) amino]-1,2,3,4,6,7,8,12b-octahydro-6-oxo-pyrido[2,1-a][2]benzazepine-4-car boxylic acid and [4S-[4.alpha., 7.alpha.(R*), 12b.beta.]]-7-[(1-oxo-2(S)-acetylthio-3-phenylpropyl)amino]-1,2,3,4,6,7,8, 12b-octahydro-6-oxo-pyrido[2,1-a][2]benzazepine-4-carboxylic acid and pharmaceutically acceptable salts thereof which is useful as an inhibitor of enkephali nase and angiotensin converting enzyme and to novel intermediates thereof.
Abstract: This invention relates to novel derivatives of 5H-dibenzo (a,d)cycloheptenes, to the processes for their preparation, to their muscarinic receptor antagonist properties and to their end-use application for treating Parkinson's Disease, tardive dyskinesia, and motion sickness.
Type:
Grant
Filed:
January 30, 1995
Date of Patent:
April 16, 1996
Assignee:
Merrell Pharmaceuticals, Inc.
Inventors:
Marcel Hibert, Luc Van Hijfte, Mary Richards, Paul Moser
Abstract: The present invention relates to a novel enantiospecific process for preparing (S)-1- 2(S)-(1,3-dihydro-1,3-dioxo-isoindo-2-yl)-1-oxo-3-phenylpropyl!-1,2 ,3,4-tetrahydro-2-pyridine-carboxylic acid methyl ester which is a useful intermediate in the preparation of 4S- 4.alpha., 7.alpha.(R*), 12b.beta.!!-7- (1-oxo-2(S)-thio-3-phenylpropyl)amino!-1,2,3,4,6,7,8,12b-oc tahydro-6-oxo-pyrido 2,1-a! 2!benzazepine-4-carboxylic acid and 4S- 4.alpha., 7.alpha.(R*), 12b.beta.!!-7- (1-oxo-2(S)-acetylthio-3-phenylpropyl)amino!-1,2,3,4,6,7,8, 12b-octahydro-6-oxo-pyrido 2,1-a! 2!benzazepine-4-carboxylic acid and pharmaceutically acceptable salts thereof which is useful as an inhibitor of enkephalinase and angiotensin converting enzyme and to novel intermediates thereof.
Abstract: The present invention is directed to a new class of piperidinyl medicinal agents which are useful for treating drug abuse.
Type:
Grant
Filed:
January 10, 1995
Date of Patent:
March 19, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Albert A. Carr, Richard C. Dage, John E. Koerner, Tung Li, Francis P. Miller, Thaddeus R. Nieduzak, Mark W. Dudley, . Christopher J. Schmidt, Robert A. Frank
Abstract: This invention relates to 1-aryl-3-pyridinyl-2-propene-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.
Type:
Grant
Filed:
November 17, 1993
Date of Patent:
March 19, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Robert J. Dinerstein, Michael L. Edwards, David M. Stemerick, Keith A. Diekema
Abstract: This invention relates to novel polyfluorinated alkyl derivatives of certain tripeptides, to the methods for their preparation, the intermediates therefore, to their use in inhibiting thrombin and lung tryptase and in their end-use application as anti-coagulants useful in treating thrombophlebitis and coronary thrombosis and in the treatment of asthma.
Type:
Grant
Filed:
May 22, 1995
Date of Patent:
March 12, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Bernhard Neises, Axel Ganzhorn, Celine Tarnus, Robert J. Broersma, Jr.
Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
Type:
Grant
Filed:
May 25, 1994
Date of Patent:
March 5, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
H. Michael Kolb, Joseph P. Burkhart, Michel J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin