The Hetero Ring Is Five-membered Patents (Class 549/29)
  • Patent number: 5244595
    Abstract: 1. A mesomorphic compound represented by the following formula 8 I]: ##STR1## wherein R.sub.1 and R.sub.2 respectively denote a straight chain or branch chain allyl group having 1-18 carbon atoms, wherein --CH.sub.2 -- in the alkyl group may be substituted by ##STR2## on condition that hetero atoms are not adjacent each other, R.sup.2 may be hydrogen atom, halogen atom, cyano group and trifluoromethyl group; n is 0 or 1, with the proviso that A.sup.1 denotes a single bond, ##STR3## when n is 0, A.sup.1 denotes a single bond when n is 1; A.sup.2 denotes any one of ##STR4## and X.sup.1, X.sup.2, Z.sup.1 and Z.sup.2 denote independently any one of hydrogen atom, halogen atom, cyano group and trifluoromethyl group, with proviso that X.sup.1, X.sup.2, Z.sup.1 and Z.sup.2 may not be all hydrogen atoms; Y denotes any one of ##STR5## a single bond.
    Type: Grant
    Filed: July 15, 1991
    Date of Patent: September 14, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Yoko Yamada, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura
  • Patent number: 5223591
    Abstract: Initiators for cationic polymerization by thermal activation, photochemical activation (UV-irradiation) or activation by electron bombardment are compounds wherein a heterocyclic, aryl substituted or aryl ring is fused to a sulfonium moiety in combination with a non-nucleophilic anion. During the activation of the initiator, a carbon-sulfur bond is broken leading to formation of a sulfide and a carbonium ion within the same molecule. The carbonium ion initiates the polymerization.
    Type: Grant
    Filed: November 25, 1991
    Date of Patent: June 29, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Johan Nyander, Sonny Jonsson, Bjorn Elman, Ann-Britt Pettersson, Per-Erik Sundell, Sven Gothe, Jan-Erik Nystrom
  • Patent number: 5214204
    Abstract: The present invention provides certain (substituted carbocyclic aryl)amidoalkyl-and (substituted heterocyclic aryl)amidoalkyl-N-Hydroxy urea compounds which inhibit lipoxygenase enzyme activity and are thus useful in the treatment of allergic and inflammatory disease states.
    Type: Grant
    Filed: July 19, 1991
    Date of Patent: May 25, 1993
    Assignee: Abbott Laboratories
    Inventors: Joseph F. Dellaria, Dee W. Brooks, Jimmie L. Moore, Kevin J. Sallin
  • Patent number: 5196224
    Abstract: Flavoring and perfume compositions as well as flavored foodstuffs and allied products and also perfumed products characterized by a content of one or more substituted thiophenes with the formula ##STR1## wherein none, one or two of the dotted lines represent a double bond with the proviso that no cumulated double bonds are present.
    Type: Grant
    Filed: June 20, 1991
    Date of Patent: March 23, 1993
    Assignee: Naarden-International N.V.
    Inventors: Henry L. A. Van den Heuvel, Paulus P. J. M. Jaegers
  • Patent number: 5176845
    Abstract: A mesomorphic compound represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 respectively denote a linear or branched alkyl group having 3-18 carbon atoms capable of including one or more methylene groups which can be replaced with at least one species of ##STR2## with the proviso that --O-- cannot directly be connected to --O--, and R.sup.2 can also be halogen, --CN or --CF.sub.3 ; X denotes ##STR3## --CH.sub.2 O-- or --OCH.sub.2 ; A denotes ##STR4## and m and n are respecitvely 0 or 1 with the proviso that m+n=0 or 1. The mesomorphic compound is effective for providing a ferroelectric liquid crystal composition showing an improved low-temperature operation characteristic and a decreased temperature-dependence of response speed.
    Type: Grant
    Filed: June 10, 1991
    Date of Patent: January 5, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Yoko Yamada, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura
  • Patent number: 5159067
    Abstract: Compounds of the general formula: ##STR1## wherein A, B, and C are hydrogen, halogen, or azido; D is hydrogen, halogen, azido, or OH; A and B or C and D can be replaced with a double bond; R is an aldohexose, aldohexosamine, or N-acetyl aldohexosamine, R.sub.1 and R.sub.2 are hydrogen or alkyl groups of from C.sub.1 to C.sub.10 ; W is oxygen or sulfur; X is oxygen, sulfur, or CH.sub.2 ; Y is a purine or pyrimidine base, and Z is carbon, sulfur, or oxygen. Y can be any purine or pyrimidine base, natural or synthetic, which combines with a sugar to form a biologically active nucleoside. In combination with an appropriate pharmaceutical carrier, the compositions have enhanced activity or increased intracellular absorbment over the parent nucleoside as a function of the 5'-O-diphosphosugar.
    Type: Grant
    Filed: July 10, 1989
    Date of Patent: October 27, 1992
    Assignees: University of Georgia Research Foundation Inc., University of Alabama at Birmingham Research Foundation, Inc.
    Inventors: Raymond F. Schinazi, Jean-Pierre Sommadossi, Chum K. Chung
  • Patent number: 5118441
    Abstract: A mesomorphic compound represented by the following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 respectively denote a linear or branched alkyl group having 1-18 carbon atoms capable of having a substituent; X denotes any one of a single bond, --O--, ##STR2## Y denotes ##STR3## or --CH.sub.2 O--; and Z denotes any one of --O--, ##STR4## .
    Type: Grant
    Filed: April 11, 1990
    Date of Patent: June 2, 1992
    Assignee: Canon Kabushiki Kaisha
    Inventors: Shosei Mori, Takeshi Togano, Takao Takiguchi, Takashi Iwaki, Yoko Yamada
  • Patent number: 5116530
    Abstract: A mesomorphic compound represented by the following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 respectively denote a linear or branched alkyl group having 1-18 carbon atoms capable of having a substituent; X.sub.1 denotes any one of a single bond, --O--, ##STR2## X.sub.2 denotes any one of a single bond, --O--, ##STR3## Z.sub.1 denotes any one of ##STR4## --CH.sub.2 O-- and --CH.dbd.C(CN)--; and A.sub.1 denotes --A.sub.2 -- or --A.sub.2 --A.sub.3 -- wherein A.sub.2 and A.sub.
    Type: Grant
    Filed: October 16, 1989
    Date of Patent: May 26, 1992
    Assignee: Canon Kabushiki Kaisha
    Inventors: Takeshi Togano, Takao Takiguchi, Yoko Yamada, Masanobu Asaoka, Kenji Shinjo
  • Patent number: 5112990
    Abstract: A ruthenium catalyzed method to synthesize cyclic sulfate compounds from the corresponding cyclic sulfites, and the cyclic sulfate reaction products obtained by this method. These cyclic sulfates further react with selected nucleophiles to give various substituted products. The method is an efficient means for the synthesis of chiral building blocks from tartaric acid enantiomers in high yields using an overall two-stage, one-pot reaction procedure. The chiral compounds can be transformed by nucleophilic reactions into chiral building blocks useful for the synthesis of natural biologically active products, such as antibiotics and pheromones.
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: May 12, 1992
    Assignee: Massachusetts Institute of Technology
    Inventors: K. Barry Sharpless, Yun Gao
  • Patent number: 5086187
    Abstract: Compounds of the general formula, including isomers and tautomers thereof: ##STR1## wherein: R.sup.1 to R.sup.5 are as defined in the text; the compounds have herbicidal and plant growth regulating properties; including compositions containing them, methods for using them and intermediates for making them.
    Type: Grant
    Filed: May 31, 1990
    Date of Patent: February 4, 1992
    Assignee: Dunlena Pty. Limited
    Inventors: Janet E. Anderson-McKay, Andris J. Liepa
  • Patent number: 5084476
    Abstract: The compounds of the formula ##STR1## wherein X and Y are independently --CH.sub.2 -- or >C(CH.sub.3).sub.2 ; Z is --CHR.sup.8 --, >CO, >CR.sup.8 OR.sup.7, --CHR.sup.8 --CHR.sup.8 --, --CHOR.sup.7 --CH.sub.2 --, --CO--CHOR.sup.7 or --CHOR.sup.7 --CHOR.sup.7 --; R.sup.1 is a 5- or 6-membered, monocyclic heterocyclic group which optionally can be C-substituted by halogen, lower-alkyl, lower-alkoxy, acyloxy, nitro, hydroxy, amino, lower-alkylamino or di-lower-alkylamino and/or which can be substituted on a ring --NH-- group by lower-alkyl; R.sup.2 and R.sup.3 are independently hydrogen, lower-alkyl, trifluoromethyl or halogen and one of R.sup.2 and R.sup.3 always is trifluoromethyl or lower-alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy or halogen; R.sup.6 is hydrogen, lower-alkyl or --OR.sup.7 ; R.sup.7 is hydrogen, lower-alkyl or acyl; R.sup.8 is hydrogen or lower-alkyl; and R.sup.7 and R.sup.
    Type: Grant
    Filed: August 17, 1989
    Date of Patent: January 28, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Ekkehard Weiss
  • Patent number: 5023342
    Abstract: A ruthenium catalyzed method to synthesize cyclic sulfate compounds from the corresponding cyclic sulfites, and the cyclic sulfate reaction products obtained by this method. These cyclic sulfates further react with selected nucleophiles to give various substituted products. The method is an efficient means for the synthesis of chiral building blocks from tartaric acid enantiomers in high yields using an overall two-stage, one-pot reaction procedure. The chiral compounds can be transformed by nucleophilic reactions into chiral building blocks useful for the synthesis of natural biologically active products, such as antibiotics and pheromones.
    Type: Grant
    Filed: May 26, 1988
    Date of Patent: June 11, 1991
    Assignee: Massachusetts Institute of Technology
    Inventors: K. Barry Sharpless, Yun Gao
  • Patent number: 4987132
    Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.
    Type: Grant
    Filed: August 16, 1988
    Date of Patent: January 22, 1991
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Toshiyasu Mase, Hiromu Hara, Hitoshi Nagaoka, Takumi Takahashi, Takeshi Suzuki, Kenichi Tomioka, Toshimitsu Yamada
  • Patent number: 4981868
    Abstract: This invention relates to novel 3-heteroaryl-2-fluoro-1-olefins and their pharmacological use as dopamine beta-hydroxylase DBH inhibitors in the treatment of DBH mediated conditions such as hypertension.
    Type: Grant
    Filed: July 25, 1989
    Date of Patent: January 1, 1991
    Assignee: Merrell Dow Pharmaceutical
    Inventors: James R. McCarthy, Donald P. Matthews, Charlotte L. Barney
  • Patent number: 4925931
    Abstract: N-Homocysteine thiolactonyl retinamido cobalamin is useful for decreasing the induction of chemically-induced tumors in animals. It is also useful for inhibiting weight gain.
    Type: Grant
    Filed: July 14, 1988
    Date of Patent: May 15, 1990
    Inventor: Kilmer S. McCully
  • Patent number: 4866181
    Abstract: A process for preparing optically active alcohols by reducing ketones using mono- or diisopinocampheylhaloboranes as reducing agents.
    Type: Grant
    Filed: December 17, 1987
    Date of Patent: September 12, 1989
    Assignee: Aldrich-Boranes, Inc.
    Inventor: Herbert C. Brown
  • Patent number: 4847376
    Abstract: The present invention provides a lipase substrate of the general formula: ##STR1## wherein A is an alkylene or alkenylene radical containing up to 16 carbon atoms, R and R.sub.1, which can be the same or different, each signify an alkyl, alkenyl or acyl radical containing up to 20 carbon atoms or an optionally alkyl-substituted aryl or aralkyl radical containing up to 8 carbon atoms in the alkyl moiety and wherein one of R and R.sub.1 can also be a hydrogen atom, X is the residue of an aromatic hydroxy or thiol compound, and each Y and Z, independently from each other, is --S-- or --O--, Z also --CH.sub.2 --.The present invention also provides a process and a reagent for the optical determination of lipase.
    Type: Grant
    Filed: May 1, 1986
    Date of Patent: July 11, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ulrich Neumann, Martina Junius, Hans-Georg Batz
  • Patent number: 4840951
    Abstract: Naphthalene derivative of the formula: ##STR1## wherein Ring A is a substituted or unsubstituted benzene ring; each of R.sup.1 and R.sup.2 is a group of the formula: --OR.sup.5, --NHR.sup.5 or ##STR2## or either one of R.sup.1 and R.sup.2 is a lower alkoxy group and the other one is a group of the formula: --OR.sup.5, --NHR.sup.5 or ##STR3## each of R.sup.3 and R.sup.4 is a lower alkoxy group, or one of R.sup.3 and R.sup.4 is a lower alkoxy group and the other is a hydrogen atom; R.sup.5 is a substituted alkyl group, a heterocyclic group, a cycloalkyl group, an alkyl group of at least 5 carbon atoms or alkenyl group; and each of R.sup.6 and R.sup.7 is hydrogen atom or a lower alkyl group and salts thereof are disclosed. Said naphthalene derivative (I) and its salts have excellent hypolipidemic activity and are useful for treatment or prophylaxis of hyperlipidemia and/or arteriosclerosis.
    Type: Grant
    Filed: June 17, 1987
    Date of Patent: June 20, 1989
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tameo Iwasaki, Kohki Takashima
  • Patent number: 4797456
    Abstract: Water-soluble sulfonium salts are converted, without the elimination of odorous volatile by-products, to water-insoluble products useful as binders in coating formulations by heating a water-soluble cyclic sulfonium salt in which the sulfonium sulfur is bonded only to aliphatic carbons.
    Type: Grant
    Filed: December 9, 1982
    Date of Patent: January 10, 1989
    Assignee: The Dow Chemical Company
    Inventors: Ritchie A. Wessling, Donald L. Schmidt, Kiyoshi I. Aikawa
  • Patent number: 4695634
    Abstract: Hypoglycemic 5-furyl and 5-thienyl derivatives of oxazolidine-2,4-dione and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; and intermediates useful in the preparation of said compounds.
    Type: Grant
    Filed: August 6, 1986
    Date of Patent: September 22, 1987
    Assignee: Pfizer Inc.
    Inventor: Rodney C. Schnur
  • Patent number: 4692513
    Abstract: Alpha-L-Aspartyl-D-heteroaromatic-substituted glycine esters and amides are disclosed to be useful as high intensity sweeteners. These compounds can be used to sweeten a variety of foods, beverages and other oral products.
    Type: Grant
    Filed: December 20, 1985
    Date of Patent: September 8, 1987
    Assignee: The Procter & Gamble Company
    Inventors: Robert B. Blum, John M. Gardlik, John M. Janusz, George P. Rizzi
  • Patent number: 4680291
    Abstract: The present invention provides propenylamines useful as anti-mycotic agents.
    Type: Grant
    Filed: August 18, 1978
    Date of Patent: July 14, 1987
    Assignee: Sandoz Ltd.
    Inventors: Helmut Hamberger, Adrian Stephen, Anton Stutz, Peter Stutz
  • Patent number: 4501903
    Abstract: The invention is a method of increasing the yield of chloromethylthiophene produced by the addition of concentrated aqueous formaldehyde solution to a mixture of thiophene and concentrated hydrochloric acid and passing in a rapid stream of gaseous hydrogen chloride. The improvement comprises increasing the rate of addition of the gaseous hydrogen chloride from about 0.6 moles per mole of thiophene per hour to about 1.5 moles per mole of thiophene per hour to increase product yield.
    Type: Grant
    Filed: July 5, 1983
    Date of Patent: February 26, 1985
    Assignee: Stauffer Chemical Company
    Inventor: Stanley B. Mirviss
  • Patent number: 4482568
    Abstract: Tetramethylene sulfoxide and its substituted derivatives have been found to be exceptionally potent inhibitors of oxidation of alcohols by liver alcohol dehydrogenases.
    Type: Grant
    Filed: October 17, 1983
    Date of Patent: November 13, 1984
    Assignee: University of Iowa Research Foundation
    Inventors: Bryce V. Plapp, Vijay K. Chadha
  • Patent number: 4466903
    Abstract: 2-Alkylidene-1,3-dioxolanes and 2-(1-alkylalkylidene)-1,3-dioxolanes are employed as acid acceptors in methylchloroform, trichloroethylene or mixtures thereof. The preferred acid acceptor is 2-methylene-1,3-dioxolane.In another aspect of the invention, aliphatic aldehyde hydrazone is employed to stabilize 2-alkylidene-1,3-dioxolane and 2-(1-alkylalkylidene)-1,3-dioxolane. The preferred aliphatic aldehyde hydrazone is acetaldehyde dimethylhydrazone.
    Type: Grant
    Filed: June 16, 1983
    Date of Patent: August 21, 1984
    Assignee: PPG Industries, Inc.
    Inventor: Steven E. Pamer
  • Patent number: 4465833
    Abstract: A novel ethynylation process is disclosed which provides an expanded series of novel ethylnyl-terminated aromatic compounds having base sensitive substituents and which facilitates the economic preparation of prior art ethynyl-substituted aromatic compounds.
    Type: Grant
    Filed: October 15, 1980
    Date of Patent: August 14, 1984
    Assignees: Hughes Aircraft Company, Hughes Aircraft Company
    Inventors: Kreisler S. Y. Lau, Robert H. Boschan
  • Patent number: 4463177
    Abstract: m-Hydroxyphenyl substituted compounds of formula ##STR1## where R is an organic radical and R.sup.1 is hydroen or an organic radical are prepared by dehydrohalogenating a compound of formula ##STR2## (where X is chlorine or bromine, and R and R.sup.1 have the above meanings). Preferred novel starting materials of formula (II) are of the formula ##STR3## (where R.sup.1 and X are as above, n is 2,3 or 4, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl(lower)alkyl or aryl(lower)alkyl).
    Type: Grant
    Filed: November 26, 1982
    Date of Patent: July 31, 1984
    Assignee: John Wyeth & Brother Limited
    Inventor: Robin G. Shepherd
  • Patent number: 4418231
    Abstract: 2-Alkylidene-1,3-dioxolanes and 2-(1-alkylalkylidene)-1,3-dioxolanes are employed as acid acceptors in methylchloroform, trichloroethylene or mixtures thereof. The preferred acid acceptor is 2-methylene-1,3-dioxolane.In another aspect of the invention, aliphatic aldehyde hydrazone is employed to stabilize 2-alkylidene-1,3-dioxolane and 2-(1-alkylalkylidene)-1,3-dioxolane. The preferred aliphatic aldehyde hydrazone is acetaldehyde dimethylhydrazone.
    Type: Grant
    Filed: August 7, 1981
    Date of Patent: November 29, 1983
    Assignee: PPG Industries, Inc.
    Inventor: Steven E. Pamer
  • Patent number: 4416826
    Abstract: Peresters of the formula: ##STR1## wherein R is an alkyl group; and ##STR2## light-absorbing chromophore group; and use thereof as photoinitiators are provided.
    Type: Grant
    Filed: October 29, 1980
    Date of Patent: November 22, 1983
    Inventor: Douglas C. Neckers
  • Patent number: 4367339
    Abstract: There are provided di- tri- and tetrasubstituted N-nitroaniline compounds and inorganic and organic salts thereof which are effective for increasing axillary branching, improving canopy and enhancing flowering of herbaceous ornamental plants and graminaceous crops, leguminous crops, cotton and sunflowers. The salts are also effective as yield enhancing agents and lodging inhibitors for the crops.
    Type: Grant
    Filed: August 18, 1980
    Date of Patent: January 4, 1983
    Assignee: American Cyanamid Company
    Inventors: Thomas D. O'Neal, Prithvi R. Bhalla, Barrington Cross
  • Patent number: 4356313
    Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acids and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
    Type: Grant
    Filed: February 19, 1981
    Date of Patent: October 26, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Gerald E. Stokker, Norman P. Gould
  • Patent number: 4356314
    Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acids, and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
    Type: Grant
    Filed: February 19, 1981
    Date of Patent: October 26, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Gerald E. Stokker, Norman P. Gould
  • Patent number: 4348525
    Abstract: [Hydroxy(organosulfonyloxy)iodo]arenes are synthesized in neutral organic solvents by the reaction of ring-substituted [hydroxy(organosulfonyloxy)iodo]benzenes with iodoarenes via ligand transfer. The produced compounds are reacted with (triorganosilyl) arenes or (trihalosilyl)arenes in neutral organic solvents to produce diaryliodonium salts. The diaryliodonium salt synthesis proceeds in regiospecific fashion, aryliodination occurring at the point of attachment of the silicon atom in the silylarenes.
    Type: Grant
    Filed: April 9, 1981
    Date of Patent: September 7, 1982
    Assignee: The University of Akron
    Inventors: Gerald F. Koser, Richard H. Wettach
  • Patent number: 4341795
    Abstract: Asymmetrical N-substituted bis-carbamoyl sulfide compounds exhibit exceptional broad spectrum pesticidal activity coupled with extremely low mammalian toxicity and phytotoxicity.
    Type: Grant
    Filed: December 1, 1975
    Date of Patent: July 27, 1982
    Assignee: Union Carbide Corporation
    Inventor: Wei C. Liang
  • Patent number: 4341894
    Abstract: Sensitizers for photoconductive compositions and elements are disclosed. The sensitizers are 2,4,6 tri substituted pyrylium dye salts wherein at least one of said substituents is a 5 or 6 membered heterocyclic ring having at least one atom selected from the group consisting of N, O and S.
    Type: Grant
    Filed: April 26, 1979
    Date of Patent: July 27, 1982
    Assignee: Eastman Kodak Company
    Inventors: Michael T. Regan, George A. Reynolds, Donald P. Specht, James A. VanAllan
  • Patent number: 4337354
    Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acid and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
    Type: Grant
    Filed: February 19, 1981
    Date of Patent: June 29, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Gerald E. Stokker, Norman P. Gould
  • Patent number: 4332952
    Abstract: Hypoglycemic 5-furyl and 5-thienyl derivatives of oxazolidine-2,4-dione and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; and intermediates useful in the preparation of said compounds.
    Type: Grant
    Filed: April 23, 1981
    Date of Patent: June 1, 1982
    Assignee: Pfizer Inc.
    Inventor: Rodney C. Schnur
  • Patent number: 4317922
    Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)-oxy]alkano ic and cycloalkanoic acids and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
    Type: Grant
    Filed: February 19, 1981
    Date of Patent: March 2, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Gerald E. Stokker, Norman P. Gould
  • Patent number: 4316043
    Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)-oxy]alkano ic and cycloalkanoic acids and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
    Type: Grant
    Filed: December 19, 1980
    Date of Patent: February 16, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Gerald E. Stokker, Norman P. Gould
  • Patent number: 4302593
    Abstract: An intermolecular compound of an amino acid containing a sulfonic acid group and a carboxylic acid group with a sulfoxide in which the amino acid is at least moderately soluble.A method which comprises reacting an amino acid containing a sulfonic acid group and a carboxylic acid group with a sulfoxide in which the amino acid is at least moderately soluble.A method for recovering an amino acid containing a sulfonic acid group and a carboxylic acid group from an admixture of the amino acid with other ingredients by adding thereto a sulfoxide in which the amino acid is moderately soluble, with the sulfoxide being added in a sufficient amount to solubilize the amino acid, separating an intermolecular compound of the amino acid with the sulfoxide, and then recovering the amino acid from its intermolecular compound.
    Type: Grant
    Filed: March 31, 1980
    Date of Patent: November 24, 1981
    Inventor: Orville G. Lowe
  • Patent number: 4282227
    Abstract: 3,4-Dihydroxyphenyltetrahydrothieno[2,3-c] or [3,2-c] pyridines are prepared by cyclization of a N-thienylmethyl-2-(3',4'-dimethoxyphenyl)-ethanolamine. These compounds have renal vasodilating activity. A species is 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydrothieno[2,3-c]pyridine and its pharmaceutically acceptable acid addition salts or esters.
    Type: Grant
    Filed: May 22, 1980
    Date of Patent: August 4, 1981
    Assignee: SmithKline Corporation
    Inventor: L. Martin Brenner
  • Patent number: 4264625
    Abstract: Bis-[N-Alkyl-N-arylcarbamate] sulfide compounds exhibit outstanding miticidal and insecticidal activity, coupled with substantially reduced mammalian toxicity, and phytotoxicity.
    Type: Grant
    Filed: October 26, 1978
    Date of Patent: April 28, 1981
    Assignee: Union Carbide Corporation
    Inventor: Themistocles D. J. D'Silva
  • Patent number: 4251666
    Abstract: A method of producing thiophene, residing in interacting diacetylene with sodium sulphide in a mixture of an aprotic polar solvent with water, in a weight ratio 50-90:50-10, respectively, or in water at a temperature of 20.degree.-100.degree. C. The method ensures quantitative yield of thiophene with a high degree of purity (more than 99.0% by gas-liquid chromatography). The method is technologically simple and does not require complicated equipment.
    Type: Grant
    Filed: November 26, 1979
    Date of Patent: February 17, 1981
    Inventors: Mikhail G. Voronkov, Boris A. Trofimov, Vasily V. Krjuchkov, Svetlana V. Amosova, Jury M. Skvortsov, Anatoly N. Volkov, Anastasia G. Malkina, Roman Y. Mushy
  • Patent number: 4174447
    Abstract: A decarboxylation process for coupling aromatic compounds wherein cyclic hydrocarbons and heterocyclic compounds having at least one labile ring hydrogen are reacted with the mono silver salts of aromatic carboxylic acids, or mono silver salts of unsaturated compounds such as .alpha.,.beta.-ethylenically unsaturated acid compounds, or silver trifluoroacetate, or the mono silver salts are reacted with themselves, by heating to temperatures of 100.degree. to 500.degree. C. at pressures of 0.1 to 10 atmospheres, or by irradiating the reactants with ultraviolet light of 200 to 400 nanometers at temperatures of -30.degree. to 150.degree. C. The resulting dimers, trimers, polysubstituted polyphenyls, polyheterocyclics and trifluoromethylated aromatics are useful as heat transfer media, as intermediates for high molecular weight polymers, pesticides and petroleum additives, and as scintillation counters.
    Type: Grant
    Filed: February 26, 1975
    Date of Patent: November 13, 1979
    Assignee: Standard Oil Company (Indiana)
    Inventor: Ellis K. Fields