Abstract: 7-fluoro-16-substituted 15-hydroxy PGI.sub.2 compounds which have saturated bond of the 13 position and which are useful as blood platelet anti-aggregating agents.
Type:
Grant
Filed:
September 8, 1986
Date of Patent:
July 14, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
George W. Holland, Hans Maag, Perry Rosen
Abstract: An improved process for preparing formaldoxime trimer is provided in which loss of the product is minimized and the prior art problems of long retention times to afford precipitation of the trimer which is difficult to filter and which occludes the undesirable salt of the acid that is difficult to remove. The method disclosed involved oximation of paraformaldehyde using dehydroxylamine sulfate and ammonia gas followed by steam stripping to recover formaldoxime and separate trimerization thereof followed by filtration recovery and drying.The formaldoxime trimer is produced in essentially quantitative yield and proceeds specifically by a procedure of steam stripping out the formaldoxime monomer from the synthesis liquor and allowing separate trimer formation and recovery. The product is free from inorganic salts and the mother liquor with formaldoxime monomer content, resulting from its recovery by filtration, does not represent a yield loss in that it is recyclable to the next synthesis reaction.
Abstract: Isocyanurate esters of thioalkanoamidophenols useful in the stabilization of organic materials normally susceptible to oxidative degradation are prepared by reacting an appropriate isocyanurate trithiol, which is a selected tris-mercapto alkanoic acid ester of tris-(2-hydroxyethyl) isocyanurate with an appropriate alkenyl compound, which is a selected N-alkenyl[4-amino-(mono- or dialkyl)phenol] or, where the alkano moiety is a sole methylene group, by reaction of tris-(2-hydroxyethyl) isocyanurate with an appropriate [mercapto-N-(mono- or di-alkyl]-4-hydroxyphenylalkanamide alkenoic] acid. In a preferred embodiment, the ester is 1,3,5-tris{2-hydroxy ethyl-[3-mercapto-(3',5'-di-tert-butyl-4'-hydroxypropionanilide)]propionat e}isocyanurate.
Type:
Grant
Filed:
February 10, 1986
Date of Patent:
July 14, 1987
Assignee:
Mallinckrodt, Inc.
Inventors:
Neil Dunski, Ali A. Bazzi, Henry J. Buehler
Abstract: A group of 4-substituted-5-nitroimidazoles is described, having effective antiprotozoal activity with much less mutagenicity than is shown by known 5-nitroimidazoles.
Abstract: Novel 2-(2-alkoxy-2-oxoethylidene)-1,2,3,4-tetrahydro-6-methyl-4-[2-(substituted )phenyl]-3,5-pyridinedicarboxylic acid dialkyl ester derivatives having novel inotropic and hypotensive activity, processes for their manufacture, pharmaceutical compositions, and methods for using said compounds and compositions are described.
Abstract: (Arylthio)pyridylalkanol derivatives of the formula: ##STR1## in which: Ar denotes an optionally substituted aryl radical,R denotes a hydrogen atom or an optionally substituted alkyl radical, an optionally substituted aryl radical or an optionally substituted aralkyl radical,R.sub.1 denotes an alkyl radical, and n equals 0, 1, 2, 3 or 4.
Type:
Grant
Filed:
February 26, 1985
Date of Patent:
June 30, 1987
Assignee:
Rhone-Poulenc Agrochimie
Inventors:
Pierre Place, Claude Anding, Jean-Claude Debourge
Abstract: Radiation sensitive silver halide photographic elements are disclosed which are protected from fog by quaternized aromatic oxatellurazinium salts. The aromatic oxatellurazinium salts can be initially incorporated in the photographic element as manufactured or during processing.
Type:
Grant
Filed:
August 25, 1986
Date of Patent:
June 30, 1987
Assignee:
Eastman Kodak Company
Inventors:
Rosemary Przyklek-Elling, Wolfgang H. H. Gunther, Roger Lok
Abstract: The invention relates to N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N-triazinylureas of the general formula ##STR1## wherein Q is selected from a radical ##STR2## Z is oxygen or sulfur, E is nitrogen or .dbd.CH--,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.3 alkoxy, andR.sub.3 and R.sub.4, each independently of the other, are hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 haloalkylthio, C.sub.1 -C.sub.4 alkylthio, halogen, C.sub.2 -C.sub.5 alkoxyalkyl, C.sub.2 -C.sub.5 alkoxyalkoxy or --NR.sub.5 R.sub.6, wherein R.sub.5 and R.sub.6 are hydrogen or C.sub.1 -C.sub.4 alkyl,and to the salts of these compounds with amines, alkali metal bases or alkaline earth metal bases or with quaternary ammonium bases. These compounds have good pre- and postemergence selective herbicidal and growth regulating properties.
Type:
Grant
Filed:
October 4, 1984
Date of Patent:
June 30, 1987
Assignee:
Ciba-Geigy Corporation
Inventors:
Josef Ehrenfreund, Werner Fory, Willy Meyer, Werner Topfl
Abstract: There is described a photographic system wherein development of an exposed photosensitive element with an aqueous alkaline photographic developing composition is effected in the presence of a compound which releases a quaternary in alkaline environment. Photographic products and processes utilizing such compounds are also disclosed.
Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
Type:
Grant
Filed:
May 14, 1986
Date of Patent:
June 30, 1987
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Marcia E. Christy, Gerald S. Ponticello
Abstract: A new class of organic superconductors having the formula (ET).sub.2 MX.sub.2 wherein ET represents bis(ethylenedithio)-tetrathiafulvalene, M is a metal such as Au, Ag, In, Tl, Rb, Pd and the like and X is a halide. The superconductor (ET).sub.2 AuI.sub.2 exhibits a transition temperature of 5 K. which is high for organic superconductors.
Type:
Grant
Filed:
May 29, 1985
Date of Patent:
June 23, 1987
Assignee:
The United States of America as represented by the United States Department of Energy
Inventors:
Jack M. Williams, Hsien-Hau Wang, Mark A. Beno
Abstract: This invention provides a benezene-fused heterocyclic compound of the formula: ##STR1## wherein R.sup.1 is halogen, nitro, amino, hydroxy, lower alkyl, lower alkoxy substituted by carboxy or protected carboxy, acylamino which may have lower alkyl on the amino moiety, or aryloxy which may have halogen,R.sup.2 is hydrogen or halogen,X is --O-- or ##STR2## in which R.sup.3 is hydrogen, lower alkyl or acyl and A is a group of the formula: ##STR3## in which R.sup.4 is hydrogen, lower alkenyl, lower alkynyl or alkyl which may have suitable substituent(s) selected from the groups consisting of hydroxy, acyl, lower alkoxy, di(lower)alkylamino, carboxy, protected carboxy and aryl; orR.sup.1 is hydrogen or lower alkoxy,R.sup.2 is hydrogen,X is ##STR4## in which R.sub.a.sup.3 is lower alkanoyl and A is a group of the formula: ##STR5## and pharmaceutically acceptable salts thereof.
Abstract: Hydroximic acids of 7-oxabicycloheptane substituted ether and thioether prostaglandin analogs are provided having the structural formula ##STR1## wherein Y is O or ##STR2## and including all stereoisomers thereof. The compounds are inhibitors of prostaglandin and biosynthesis and as such are useful, for example, as anti-allergy and antiinflammatory agents and also as antipsoriatic agents.
Type:
Grant
Filed:
July 23, 1986
Date of Patent:
June 16, 1987
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Ravi K. Varma, Eric M. Gordon, Ligaya M. Simpkins
Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistance to benzimidazole or thiophanate fungicides and/or cyclic imide fungicides.
Abstract: The compounds: ##STR1## in which R.sup.1 is hydrogen, halogen, hydroxy, or alkyl;R.sup.2 is substituted or unsubstituted pyridinyl, pyrazinyl, quinolinyl or quinoxalinyl and said substituents are alkyl, alkoxy, alkoxycarbonyl, halogen, cyano or nitro;R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, phenyl, halophenyl, methylphenyl, trifluoromethylphenyl, cyanophenyl or nitrophenyl; with the proviso that one of R.sup.5 and R.sup.6 is other than hydrogen;and n is an integer from 1 to 7;or a pharmaceutically acceptable salt thereof, are antipsychotic and anxiolytic agents.
Type:
Grant
Filed:
September 16, 1985
Date of Patent:
June 9, 1987
Assignee:
American Home Products Corporation
Inventors:
Magid A. Abou-Gharbia, Usha R. Patel, Reinhardt P. Stein
Abstract: An improved process for producing anthra[1,9-cd]-pyrazol-6(2H)-ones from 1,4-dichloro-5,8-disubstituted 9,10-anthracenediones. The process produces higher yields by using a new combination of protecting groups on the compounds which allows for easier and cleaner chromatographic resolution. The compounds produced have antibacterial, antifungal, antileukemic, and antitumor activity.
Type:
Grant
Filed:
May 5, 1986
Date of Patent:
June 9, 1987
Assignee:
Warner-Lambert Company
Inventors:
Vladimir G. Beylin, Om P. Goel, H.D. Hollis Showalter
Abstract: A process for preparing a 4-substituted pyridine product from a starting pyridine substituted in the 4-position by a leaving group susceptible to nucleophilic displacement when the starting pyridine is in quaternized form, comprises,quaternizing the starting pyridine under effective acidic conditions with acrylamide, N-monoalkylacrylamide or N-dialkylacrylamide,subjecting the resultant, corresponding quaternized starting pyridine, to a nucleophilic displacement reaction with a reagent which reacts with it to produce the corresponding quaternary salt of the 4-substituted pyridine product, anddequaternizing the latter under effective basic conditions to liberate the 4-substituted pyridine product.
Abstract: 7-Oxabicyclo(2.2.1)heptane hydroxamic acid derivatives are disclosed having the general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, aryl, aralkyl or alkenyl; R.sub.2 is hydrogen, lower alkyl, alkanoyl or aroyl; R.sub.3 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; and n is an integer from 0 to 9, with the proviso that when A is a single bond, n is an integer from 1 to 9; and including all stereoisomers and pharmaceutically acceptable salts thereof.These new compounds have been found to simultaneously inhibit the arachidonic acid enzymes cyclooxygenase and 5-lipoxygenase and are therefore useful as antiinflammatory, antiasthma and antipsoriatic agents.
Abstract: Corrosion of metal surfaces in contact with an aqueous medium is inhibited by incorporating a N-(hydrophobe aromatic)pyridinium compound such as N-(p-dodecylphenyl)-2,4,6-trimethylpyridinium sulfoacetate into the aqueous medium.