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.
Abstract: Agonists of NPY which are derivatives of naturally occurring NPY. The agonism is confirmed using conventional competitive binding and biochemical assays and the use of these derivatives in a variety of conditions in which neuropeptide Y is implicated is also described.
Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.
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:
February 18, 1994
Date of Patent:
February 21, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Bernhard Neises, Axel Ganzhorn, Celine Tarnus, Robert J. Broersma, Jr.
Abstract: The present invention relates to compounds of the formula ##STR1## wherein A is methylene, oxygen, sulfur or N--B wherein B is R.sub.1 or COR.sub.2 wherein R.sub.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Z-- group wherein Ar is aryl and Z is a C.sub.0 -C.sub.4 alkyl and R.sub.2 is a --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Z group;R is hydrogen or a C.sub.1 -C.sub.4 alkyl; andX and Y are each independently hydrogen, nitro or amino, with the proviso that when X is nitro or amino, Y must be hydrogen, and when Y is nitro or amino, X must be hydrogen; andpharmaceutically acceptable salts thereof, which are inhibitors of Angiotensin Converting Enzyme.
Abstract: Certain Castanospermine ester derivatives of the formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are each independently hydrogen, C.sub.1-14 alkanoyl, C.sub.1-14 alkenoyl, cyclohexanecarbonyl, C.sub.1-8 alkoxyacetyl, ##STR2## naphthalenecarbonyl optionally substituted by methyl or halogen; phenyl (C.sub.2-6 alkanoyl) wherein the phenyl is optionally substituted by methyl or halogen; cinnamoyl; pyridinecarbonyl optionally substituted by methyl or halogen; dihydropyridine carbonyl optionally substituted by C.sub.1 -C.sub.10 alkyl; thiophenecarbonyl optionally substituted by methyl or halogen; or furancarbonyl optionally substituted by methyl or halogen; Y is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, trifluoromethyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylmercapto, cyano or dimethylamino; Y' is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or it is combined with Y to give 3,4-methylenedioxy; Y" is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halogen; with R, R.sub.1 and R.sub.
Type:
Grant
Filed:
April 1, 1993
Date of Patent:
January 31, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Sai P. Sunkara, Paul S. Liu, A. Stanley Tyms, Debra L. Taylor
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:
April 30, 1992
Date of Patent:
January 24, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Daniel G. Schirlin, Jean-Noel Collard, Charles Danzin
Abstract: Substituted (1.alpha., 2.beta., 3.alpha. or .beta.,4.alpha.,5.alpha. or .beta.)-2,3,4-trihydroxy-5-(hydroxymethyl)cyclopentylamines are inhibitors of alphamannosidase and alpha-fucosidase and are useful immunostimulants, antiviral and antimetastatic agents.
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 novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
Type:
Grant
Filed:
August 27, 1993
Date of Patent:
January 3, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
James R. McCarthy, Michael L. Edwards, Donald P. Matthews
Abstract: 2,3-Dihydro-1-(8-methyl-1,2,4-triazolo [4,3-b]pyridazin-6-yl)-4(1H)-pyridinone has been prepared in substantially pure form and has been found to be useful for alleviating bronchial spasms in mammals. Synthesis of this material through phenylselenyl intermediates is described.
Abstract: Drug-resistant malarial infection in humans can be effectively treated with standard antimalarial agents if administered in conjunction with desipramine.
Type:
Grant
Filed:
March 5, 1993
Date of Patent:
December 13, 1994
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Peter P. McCann, Albert Sjoerdsma, Alan J. Bitonti
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:
February 24, 1994
Date of Patent:
December 6, 1994
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Albert A. Carr, George D. Maynard, John M. Kane, Hsien C. Cheng, Mark W. Dudley
Abstract: The present invention relates to certain novel mercaptoacetylamido pyridazo[1,2]pyridazine, pyrazolo[1,2]pyridazine, pyridazo[1,2- a] [1,2]diazepine and pyrazolo[1,2- a ][1,2]diazepine derivatives useful as inhibitors of enkephalinase and of ACE.
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:
January 25, 1994
Date of Patent:
November 1, 1994
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Michael G. Palfreyman, Ian A. McDonald, Francesco G. Salituro, Robert Schwarcz, Bruce M. Baron