Abstract: The invention provides the compounds 1,2-dideoxy-2-(hydroxymethyl)-1-(methylamino)-myo-inositol hydrochloride, 1,2-dideoxy-2-(hydroxymethyl)-1-(methylamino)-scyllo-inositol, 1,6-dideoxy-6-(hydroxymethyl)-1-(methylamino)-myo-inositol.
Abstract: The present invention is directed towards a process for producing a superior tasting pharmaceutical composition having porous granules produced through in situ gas generation using effervescence-producing ingredients. The method disclosed herein is especially suitable for producing superior tasting antacid tablets as well as superior tasting calcium supplements.
Type:
Grant
Filed:
January 19, 1994
Date of Patent:
August 1, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Deepak S. Phadke, Melissa P. Neddermeyer
Abstract: The present invention is directed to a new class of 2-optionally substituted-4-piperazine-benzothiophene derivatives of the formula ##STR1## in which Y is represented by hydrogen or C.sub.1-3 alkyl; R is represented by a substituent selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, --CF.sub.3, --OCF.sub.3, and --OH; R.sub.1 is represented by hydrogen, cycloalkyl, C.sub.1-6 alkyl, phenyl optionally substituted, phenylalkyl, or phenylamidoalkyl; X is represented by hydrogen, --(CH.sub.2).sub.n X.sub.1, CH=CHX.sub.1 or CHX.sub.2 --(CH.sub.2).sub.q --CH.sub.3 ; n is an integer from 0-2; q is either the integer 0 or 1; X.sub.1 is represented by --OH--,--OR.sub.2, --NR.sub.2 R.sub.3, --CO.sub.2 R.sub.2, --CONR.sub.2 R.sub.3, --CN, or --COR.sub.2 ; R.sub.2 and R.sub.3 are each independently represented by hydrogen, C.sub.1-4 alkyl, phenyl optionally substituted, phenylalkyl, or R.sub.2 and R.sub.3 together form a (CH.sub.2).sub.m cycloalkyl, where m=2- 6; X.sub.2 is --OR.
Type:
Grant
Filed:
September 15, 1993
Date of Patent:
July 25, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Ronald C. Bernotas, Jeffrey S. Sprouse, Hsien C. Cheng
Abstract: The present invention relates to 4-amino-.DELTA..sup.4 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with heating.
Type:
Grant
Filed:
February 25, 1994
Date of Patent:
July 25, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Philip M. Weintraub, Joseph P. Burkhart, Thomas R. Blohm
Abstract: This invention relates to neuroprotective 5-aryl-3H-1,2,4-triazol-3-ones and to their use in the treatment of neurodegenerative disorders such as cerebral ischemia, stroke, Alzheimer's disease, Parkinson's disease, and Huntington's disease.
Type:
Grant
Filed:
March 15, 1990
Date of Patent:
July 25, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Stephen M. Sorensen, John M. Kane, Francis P. Miller
Abstract: The present invention relates to certain novel mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and of ACE.
Type:
Grant
Filed:
November 9, 1993
Date of Patent:
July 4, 1995
Assignee:
Merrell Dow 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
Abstract: Agonists and Antagonist of bombesin are derivatives of naturally occurring bombesin possessing a methyl sulfide or a methyl amide bond connecting the two amino acids on the carboxy terminal end. Agonist and antagonist activities are 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. Use of these peptides include stimulating or antagonizing growth of tissues, especially lung, and a means for effecting treatment for digestional disorders. Treatment comprises administering to a patient in need thereof, an effective amount of a bombesin analog.
Abstract: Novel 5-acyl-2-(1H)pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.
Type:
Grant
Filed:
August 25, 1993
Date of Patent:
June 27, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Winton D. Jones, Richard C. Dage, Richard A. Schnettler
Abstract: Disclosed are Agonists and Antagonists of bombesin which are derivatives of naturally occurring bombesin possessing modified derivatives of phenylalanine. Agonist and antagonist activities are 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.Use of these peptides may be useful for stimulating or antagonising growth of tissues, especially lung, and of digestion. Treatment comprises administering to a patient in need thereof, an effective amount of a bombesin analog.
Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide derivatives which are useful as inhibitors of enkephalinase and ACE.
Abstract: The compound (R)-2-[(phenylisopropyl)amino]adenosine whose structure is given below: ##STR1## (R)-2-[(phenylisopropyl)amino]adenosine is about two orders of magnitude greater in its selectivity between the A-1 and A-2 adenosine receptors than its diastereoisomer. This compound is useful for lowering blood pressure.
Type:
Grant
Filed:
September 15, 1994
Date of Patent:
June 20, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Norton P. Peet, David R. Borcherding, Nelsen L. Lentz, Philip M. Weintraub, Philip R. Kastner
Abstract: The narrow poly- or mono-dispersed oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a recurring unit of from 3 to 50. These oligomers are water-soluble, preferably have a rigid backbone, have recurring units coupled by carbonyl linking moieties which have anionic groups, display predominantly linear geometry such that regular spacing between anionic groups exists in an aqueous medium, and are pharmaceutically-acceptable. The narrow poly- or mono-dispersed oligomers are useful for the treatment and/or diagnosis of AIDS and/or ARC or HSV.
Type:
Grant
Filed:
January 9, 1992
Date of Patent:
June 13, 1995
Assignees:
The Dow Chemical Company, Merrell Dow Pharmaceuticals, Inc.
Inventors:
Alan D. Cardin, William A. Fordyce, Michael J. Mullins, Thomas A. Chamberlin, Michael J. Fazio
Abstract: The present invention relates to novel 2-substitited indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.
Abstract: The adenosine derivatives represented by the following formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R is H or C.sub.1 -C.sub.7 alkyl,Q is the moiety of the formula ##STR2## wherein V is H or --COOHX is H, F, Cl, Br, andZ is H, F, Cl, or Br.These compounds are inhibitors of S-adenosylmethione decarboxylase and are useful for treating parasitic infections.
Abstract: This invention relates to 1-phenyl-3-aryl-2-propyne-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:
March 5, 1993
Date of Patent:
April 25, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Robert J. Dinerstein, Jeffrey S. Sabol, Keith A. Diekema
Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each selected from the group consisting of C.sub.1 -C.sub.2 lower alkyl; X is NH or S; and n is a whole number within the range of 1-4 inclusive; and when n=0, X is (CH.sub.2).sub.3 and the pharmaceutically acceptable salts thereof have been shown to be effective in treating tamoxifen resistant tumors.
Abstract: The present invention is directed to a new class of arylalkoxyphenoxy-imidazoline compounds and their use for the treatment of depression, anxiety, hypertension, and migraine headaches.
Type:
Grant
Filed:
February 9, 1994
Date of Patent:
April 18, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Jules Freedman, Bruce M. Baron, Mark W. Dudley
Abstract: This invention relates to an improvement in a process for making 2,6-di-tertiarybutyl-4-mercaptophenol and 4,4-isopropylidenedithio-bis-(2,6-di-tertiarybutylphenol) which comprises reduction of bis (3,5-di-tertiarybutyl-4-hydroxyphenyl)polysulfide with hydrogen gas at a temperature range of from about 20.degree. C. to about 90.degree. C. in the presence of a catalytic amount of cobalt-molybdenum catalyst.