Ring In Alcohol Moiety Patents (Class 560/106)
  • Patent number: 5705167
    Abstract: Novel pharmaceutically/cosmetically-active aromatic polyenic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: April 26, 1995
    Date of Patent: January 6, 1998
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventors: Jean-Michel Bernardon, Philippe Nedoncelle
  • Patent number: 5703272
    Abstract: A process for preparing a carboxylic acid ester which includes subjecting a carboxylic acid and an alcohol or a phenol to an esterification reaction in the presence of a silica-titania catalyst. The silica-titania catalyst is prepared by adding an acidic solution containing a silicon compound and a titanium compound dissolved therein to a solution of a basic compound to bring about co-precipitation, in which the acidic solution is a nitric acid-acidic solution or a sulfuric acid-acidic solution, a ratio of the amount (gram equivalent) of nitric acid or sulfuric acid to the amount (mol) of the silicon compound in the acidic solution is 0.5 to 50 and the amount of the titanium compound in the acidic solution is such that a ratio of titania (TiO.sub.2) in the silica-titania catalyst is 1 to 50% by weight.
    Type: Grant
    Filed: September 3, 1996
    Date of Patent: December 30, 1997
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Mariko Abe, Shuji Ebata, Takafumi Abe, Hirofumi Higuchi
  • Patent number: 5661166
    Abstract: A Saishin N derivative represented by the following general formula: ##STR1## wherein X represents a carbonyl group or a >CH--ORx group, or X bonds to a carbon atom in Y or Z to represent a >C(ORx)--O-- group; Y and Z may be the same or different and each represents a carbonyl group or a >CH--ORy group, or each bonds to an oxygen atom in X to represent a >CH-- group; the broken line represents an optional bond; and Rx and Ry may be the same or different and each represents a hydrogen atom or an alkyl, alkenyl, aralkenyl, aralkyl, heterocyclic-alkyl or acyl group, is provided which is therapeutically usable as an antiulcer agent.
    Type: Grant
    Filed: March 13, 1995
    Date of Patent: August 26, 1997
    Assignee: Tokyo Tanabe Co. Ltd.
    Inventors: Susumu Yokura, Kiyokazu Murakami, Nobuo Takoi, Hiroyuki Iizuka, Eiji Ohtubo
  • Patent number: 5629346
    Abstract: Certain N-acetonylbenzamides exhibit low toxicity to plants are particularly useful for control of fungi, especially Phycomycetes.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 13, 1997
    Assignee: Rohm and Haas Company
    Inventors: H. Edwin Carley, Ashok K. Sharma, Colin Swithenbank
  • Patent number: 5616803
    Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: April 1, 1997
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takashi Nomoto, Masahiro Hayashi, Jun Shibata, Yoshikazu Iwasawa, Morihiro Mitsuya, Yoshiaki Iida, Katsumasa Nonoshita, Yasufumi Nagata
  • Patent number: 5606089
    Abstract: Compounds represented by the general formula (I), as well as intermediates for the synthesis of thereof: ##STR1## where R.sup.1 is a hydrogen atom or an acyl group; R.sup.2 is a lower alkyl group; R.sup.3 is a hydrogen atom or a lower alkyl group; R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; R.sup.2 and R.sup.4, when taken together, may form a 5-membered ring; R.sup.5 and R.sup.6, when taken together, may form a cycloalkyl group or a heterocyclic group in which at least one methylene on the ring of a cycloalkyl group is substituted by an oxygen atom, a sulfur atom or an alkyl-substituted nitrogen atom, provided that R.sup.6 is not present if the ring formed by R.sup.2 and R.sup.4 taken together is a benzofuran ring.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: February 25, 1997
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Kunio Tamura, Yoshiaki Kato, Mitsutaka Yoshida, Osamu Cynshi, Yasuhiro Ohba
  • Patent number: 5597839
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: January 28, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5583247
    Abstract: Ethylenically unsaturated monomers are protected from premature polymerization during manufacture and storage by the incorporation therein of an effective stabilizing amount of a 7-substituted quinone methide compound.
    Type: Grant
    Filed: April 14, 1995
    Date of Patent: December 10, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Nesvadba, Samuel Evans, Matthew E. Gande, Volker H. von Ahn, Roland A. E. Winter
  • Patent number: 5563292
    Abstract: Novel compounds of Formula 1 ##STR1## or a pharmaceutically acceptable salt or solvate thereof are disclosed. Also disclosed are pharmaceutical compositions containing compounds of Formula 1. Methods of treating allergy, inflammation and hyperproliferative skin diseases with compounds of Formula 1 are also disclosed.
    Type: Grant
    Filed: April 2, 1992
    Date of Patent: October 8, 1996
    Assignee: Schering Corporation
    Inventors: Neng-Yang Shih, Pietro Mangiaracina
  • Patent number: 5554641
    Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.
    Type: Grant
    Filed: March 20, 1995
    Date of Patent: September 10, 1996
    Inventors: David C. Horwell, Martyn C. Pritchard, Jennifer Raphy
  • Patent number: 5543559
    Abstract: The present invention is concerned with a process for the manufacture of optically active compounds of the formula ##STR1## wherein R signifies lower alkyl, lower alkoxy, phenyl, benzyl or --NR.sub.2.sup.1, R.sup.1 signifies lower alkyl, phenyl, benzyl or hydrogen and * signifies an optically active center, by asymmetrically hydrogenating an enol derivative of ketoisophorone of the formula ##STR2## wherein R has the significance given above, in the presence of a rhodium complex of an optically active diphosphine ligand.
    Type: Grant
    Filed: June 8, 1995
    Date of Patent: August 6, 1996
    Assignee: Hoffman-La Roche Inc.
    Inventors: Emil A. Broger, Yvo Crameri, Rudolf Schmid, Theodor Siegfried
  • Patent number: 5488133
    Abstract: Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid; n is an integer from 0 to 20;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy, acylamino, acetamidoalkyl, acetamidoaryl, --COO-alkyl, --COO-aryl, --COO-aralkyl, --CO-alkyl, --CO-aryl, --CO-heterocyclyl, cyano or heterocyclyl;R.sup.5 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, heterocyclyl, or a Z-CO.sub.2 -CR.sup.1 R.sup.2 (CR.sup.3 R.sup.4).sub.n group, wherein Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n are as defined above, m is an integer from 0 to 10, p is an integer from 0 to 10, and m+p.gtoreq.1 are useful as contrast agents in x-ray imaging compositions and methods.
    Type: Grant
    Filed: March 10, 1994
    Date of Patent: January 30, 1996
    Assignee: Eastman Kodak Company
    Inventors: Baldev Singh, Edward R. Bacon, Shaughnessy Robinson
  • Patent number: 5482523
    Abstract: Mannich condensation products prepared by the condensation of a compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl; R.sub.5 is hydrogen, alkyl, phenyl, aralkyl, alkaryl, or an acyl group of the formula: ##STR2## wherein R.sub.6 is alkyl, phenyl, aralkyl or alkaryl; R.sub.7 is alkyl; u is an integer from 1 to 10; n is an integer from 5 to 100; and x is an integer from 0 to 10;with an aldehyde and a nitrogen base selected from ammonia, lower alkylamine, a polyamine and mixtures thereof.The Mannich condensation products and their fuel soluble salts are useful as fuel additives for the prevention and control of engine deposits.
    Type: Grant
    Filed: November 2, 1994
    Date of Patent: January 9, 1996
    Assignee: Chevron Chemical Company
    Inventor: Richard E. Cherpeck
  • Patent number: 5472970
    Abstract: Allylaminoesters of the formula (I): ##STR1## in which: R.sub.1 is H or low-molecular-weight alkyl,R.sub.2 is low-molecular-weight alkyl, cycloalkyl, or low-molecular-weight phenylcycloalkyl, pyridyl or phenyl, low-molecular-weight phenylalkyl, low-molecular-weight diphenylalkyl, low-molecular-weight phenylalkenyl, in which the phenyl cycle may be mono-, di- or trisubstituted by chlorine atoms, low-molecular-weight alkyl radicals, low-molecular-weight alkoxy, or trifluoromethyl, acetamide or acetyloxy radicals, their racemic forms, their (S) enantiomers and their addition salts. Also, antiallergic drugs containing the same.
    Type: Grant
    Filed: September 19, 1994
    Date of Patent: December 5, 1995
    Assignee: Institut de Recherche Jouveinal S.A.
    Inventors: Alain P. Calvet, Agnes G. Grouhel, Jean-Louis Junien
  • Patent number: 5466872
    Abstract: Fuel compositions containing a major amount of hydrocarbons boiling in the gasoline or diesel range and an effective deposit-controlling amount of a poly(oxyalkylene) aromatic ether having the formula: ##STR1## where A.sub.1 is nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms; R.sub.1 and R.sub.2 are independently hydrogen, hydroxy, lower alkyl, or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl and each R.sub.3 and R.sub.4 is independently selected in each --O--CHR.sub.3 --CHR.sub.4 -- unit; R.sub.5 is hydrogen, alkyl having 1 to 100 carbon atoms, phenyl, aralkyl having 7 to 100 carbon atoms or alkaryl having 7 to 100 carbon atoms, or an acyl group of the formula: ##STR2## where R.sub.
    Type: Grant
    Filed: February 21, 1995
    Date of Patent: November 14, 1995
    Assignee: Chevron Chemical Company
    Inventor: Richard E. Cherpeck
  • Patent number: 5457108
    Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: October 10, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hanno Wild, Jutta Hansen, Jorg Lautz, Arnold Paessens
  • Patent number: 5439925
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: August 8, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
  • Patent number: 5412134
    Abstract: The protected cyclobutanone of the formula ##STR1## is treated with a dialkylaluminum chloride, an alkylaluminum dichloride, a trialkylaluminum compound, diphenylsilane in the presence of tris(triphenylphosphine) rhodium (I) chloride, or iridium tetrachloride to yield the corresponding diprotected cyclobutanol. This compound is useful as an intermediate in the preparation of antiviral agents.
    Type: Grant
    Filed: May 26, 1992
    Date of Patent: May 2, 1995
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Janak Singh, Gregory S. Bisacchi, Richard H. Mueller
  • Patent number: 5374766
    Abstract: This invention relates to a novel ester which presents as (CF 1) and a method for the production of the same as well as a process for hydrolysis and a method for the determination of an optical purity using this ester, and the object thereof is to provide an intermediate for the synthesis or various natural products, which has high stability, and the optical purity of which can readily be determined, according to the esterification of 1-oxo-5-hydroxymethyl-2-cyclohexene which is unstable to acids and alkalis.
    Type: Grant
    Filed: January 30, 1992
    Date of Patent: December 20, 1994
    Assignee: Nitto Denko Co., Ltd.
    Inventors: Shuji Senda, Eiichiro Fukuzaki, Yutaka Nakazono, Tetsuo Omata
  • Patent number: 5371284
    Abstract: Phenyl acetylenic acetals and thioacetals and their use in the treatment of allergy, asthma, inflammation, arthritis, hyperproliferative skin disease, psoriasis or contact dermatitis are disclosed. Also disclosed are intermediates useful for producing said phenyl acetylenic acetals and thioacetals.
    Type: Grant
    Filed: July 23, 1993
    Date of Patent: December 6, 1994
    Assignee: Schering Corporation
    Inventors: Richard J. Friary, Michael J. Green, Anil K. Saksena, Vera A. Seidl
  • Patent number: 5344638
    Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinwhereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently lower-alkyl, optionally substituted with halo;x is 1-3y is 1-4;n is 1-5;m is 1-15;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkylin an aqueous, pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 11, 1993
    Date of Patent: September 6, 1994
    Assignee: Sterling Winthrop Inc.
    Inventors: Carl R. Illig, Brent D. Douty
  • Patent number: 5312999
    Abstract: Propoxybenzene derivatives represented by the following formula ##STR1## wherein Ra represents a nitro group, an amino group which may have a protecting group or an --NHCH.dbd.C(COO--C.sub.1-6 -Alkyl).sub.2 group, Rb represents a hydrogen atom, a protecting group for the hydroxyl group or a substituted sulfonyl group and Xa and Xb, which may be the same or different, each represents a halogen atom, and processes for preparation thereof are disclosed. These derivatives are useful in preparing antibacterial agents.
    Type: Grant
    Filed: March 2, 1992
    Date of Patent: May 17, 1994
    Assignee: Daiichi Seiyaku Co., Ltd.
    Inventors: Toshihiro Fujiwara, Tutomu Ebata
  • Patent number: 5306837
    Abstract: Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one are described.
    Type: Grant
    Filed: July 15, 1993
    Date of Patent: April 26, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Toomas Mitt
  • Patent number: 5296003
    Abstract: Poly(oxyalkylene) hydroxyaromatic ethers having the formula: ##STR1## or a fuel-soluble salt thereof; where n is an integer from 5 to 100; x is an integer from 0 to 10; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms; R.sub.3 and R.sub.4 are each independently hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.5 is an acyl group of the formula: ##STR2## wherein y is 1, 2 or 3; R.sub.6 is a divalent hydrocarbyl radical, when y is 1, a trivalent hydrocarbyl radical, when y is 2, or tetravalent hydrocarbyl radical, when y is 3, said hydrocarbyl radicals having 1 to about 20 carbon atoms; and each Z is independently selected from the group consisting of: ##STR3## where each R.sub.7 is independently alkyl having 1 to 30 carbon atoms, phenyl, aralkyl having 7 to 36 carbon atoms or alkaryl having 7 to 36 carbon atoms.
    Type: Grant
    Filed: March 8, 1993
    Date of Patent: March 22, 1994
    Assignee: Chevron Research and Technology Company
    Inventor: Richard E. Cherpeck
  • Patent number: 5294616
    Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
    Type: Grant
    Filed: March 25, 1992
    Date of Patent: March 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
  • Patent number: 5292928
    Abstract: In a process for reacting a low molecular weight hydroxy compound with a carboxylic acid halide, a small amount of the acid halide is introduced into the reaction vessel and the remainder of the acid halide and the hydroxy compound are added gradually in an approximately stoichiometric ratio. The hydrogen halide formed is thus prevented from dissolving in the reaction medium. The heat of reaction to be dissipated is negligible.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: March 8, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Karlheinz Miltenberger
  • Patent number: 5283352
    Abstract: Catechol compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3 and X are as described herein are effective Catechol-O-methyltransferase inhibitors.
    Type: Grant
    Filed: December 7, 1992
    Date of Patent: February 1, 1994
    Assignee: Orion-yhtyma Oy
    Inventors: Reijo J. Backstrom, Kalevi E. Heinola, Erkki J. Honkanen, Seppo K. Kaakkola, Pekka J. Kairisalo, Inge-Britt Y. Linden, Pekka I. Mannisto, Erkki A. O. Nissinen, Pentti Pohto, Aino K. Pippuri, Jarmo J. Pystynen
  • Patent number: 5283358
    Abstract: Process for obtaining aryl esters by O-dealkylation of an alkyl aryl ether with an acyl halide in the presence of a catalyst chosen from hexaalkylguanidinium salts and tetraalkylphosphonium salts.The alkyl aryl ether corresponds preferentially to the formula Ar(OR).sub.n in which R denotes an alkyl group, in particular a methyl group, n is an integer from 1 to 6 and Ar represents a C.sub.6 to C.sub.14 aromatic radical, a coumarinyl group or a group of a number of phenyl radicals.This process allows also the obtention of aromatic polyester.
    Type: Grant
    Filed: December 10, 1992
    Date of Patent: February 1, 1994
    Assignee: Societe Nationale des Poudres et Explosifs
    Inventors: Roy A. Olofson, Ann P. Lawson, Heather L. Rayle
  • Patent number: 5266718
    Abstract: New ethanolamine benzoate compounds which can be used as medicaments and correspond to the formula: ##STR1## wherein R is as defined in the description, in the form of racemic compounds and enantiomers. These new compounds and their physiologically tolerable salts can be used therapeutically for treatment of insulin-resistance states.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: November 30, 1993
    Assignee: Adir et Compagnie
    Inventors: Michel Wierzbicki, Pierre Hugon, Jacques Duhault, Francoise Lacour, Michelle Boulanger
  • Patent number: 5264605
    Abstract: A process for preparing myoinositol polyphosphoric acid from myoinositol via a polyacylmyoinositol, a process for preparing a polysilyl-polyacylmyoinositol from a polyacylmyoinositol, and a process for preparing an optically active myoinositol polyphosphoric acid from the above product or a polysilylmyoinositol.
    Type: Grant
    Filed: February 20, 1991
    Date of Patent: November 23, 1993
    Assignee: Mitsui Toatsu Chemicals, Incorporated
    Inventors: Shoichiro Ozaki, Yutaka Watanabe
  • Patent number: 5256806
    Abstract: Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one are described.
    Type: Grant
    Filed: November 12, 1992
    Date of Patent: October 26, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Toomas Mitt
  • Patent number: 5256811
    Abstract: compounds of formula I ##STR1## wherein R.sup.1 represents a C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, C.sub.3-8 cycloalkyl(C.sub.1-8)alkyl, C.sub.1-8 hydroxyalkyl, C.sub.1-8 alkylthio, phenyl or substituted phenyl;R.sup.3 represents a C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, CO2(C.sub.1-8)alkyl, CO.sub.2 (C.sub.2-8) alkenyl, C.sub.1-8 alkylthio, (C.sub.1-2)alkyl CO.sub.2 (C.sub.1-8) alkyl or C.sub.1-8 aldehydroalkyl where the aldehyde function is protected by a suitable protecting group (for example, an acetal such as a dimethyl acetal);R.sup.4 represents a hydrogen atom, C.sub.1-8 alkyl or C.sub.2-8 alkenyl;Z represents a group (CH.sub.2).sub.n or a branched alkyl chain;n is 1 to 8;and each of a, b and c is independently a single or a double bond;can be prepared relatively easily and in good xxx at room temperature by reacting a compound of general formula II ##STR2## wherein R.sup.2, R.sup.3, R.sup.
    Type: Grant
    Filed: December 6, 1991
    Date of Patent: October 26, 1993
    Assignee: British Bio-Technology Limited
    Inventors: Richard S. Todd, Maxwell Reeve
  • Patent number: 5242936
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is at position 4 and either is an alkyl group of 1-6 C or is an --(CH.sub.2).sub.3 -- which is additionally linked to the phenyl at position 3 thereof;R.sub.2 is a lower alkyl of 1-3 C or is hydrogen;n.sub.1, n.sub.2 and n.sub.3 represent the number of CH.sub.2, C(R.sub.2).sub.2 and CH.sub.2 groups, respectively, wherein n.sub.1 is 2, 3, 4, 5, 6, 8, or 11, n.sub.2 is 0 or 1 and n.sub.3 is 0 andR.sub.4 is an alkyl residue of 1-12 C or is selected from phenyl and pyridyl; and their pharmaceutical compositions are useful in inhibiting the release of chemical mediators which cause allergic symptoms. Compounds, compositions, and methods for treatment of allergic conditions are disclosed.
    Type: Grant
    Filed: May 21, 1990
    Date of Patent: September 7, 1993
    Assignee: Frank M. Berger
    Inventors: Frank M. Berger, Joseph I. DeGraw, Jr., Howard L. Johnson
  • Patent number: 5238602
    Abstract: Compounds of the formula ##STR1## wherein n stands for the number 0 or 1; the rings A.sup.1, A.sup.2 and A.sup.3 represent 1,4-phenylene, 2-fluoro-1,4-phenylene or trans-1,4-cyclohexylene or one of these rings also represents a 2,5-disubstituted pyrimidine ring or a trans-2,5-disubstituted m-dioxane ring; X.sup.1 represents a single covalent bond, --COO--, --OOC--, --CH.sub.2 CH.sub.2 --, p--C.sub.6 H.sub.4 --, --CH.sub.2 CH.sub.2 --p-- C.sub.6 H.sub.4 --, --CH.sub.2 CH.sub.2 --p--C.sub.6 H.sub.4 --CH.sub.2 CH.sub.2 -- or, insofar as the rings A.sup.1 and A.sup.2 represent 1,4-phenylene, also --NON--; R.sup.2 represents 1E-alkenyl, 2Z-alkenyl, 3E-alkenyl, 4-alkenyl or alkenyloxy, with the proviso that the oxygen atom in alkenyloxy is linked with a saturated carbon atom; and R.sup.1 signifies 1E-alkenyl, 2Z-alkenyl, 3E-alkenyl, 4-alkenyl or, insofar as R.sup.2 represents alkenyloxy, also alkyl, their manufacture, as well as liquid crystalline mixtures and the use for electro-optical purposes.
    Type: Grant
    Filed: May 26, 1987
    Date of Patent: August 24, 1993
    Assignee: Hoffmann La Roche Inc.
    Inventors: Martin Petrzilka, Martin Schadt
  • Patent number: 5233076
    Abstract: A novel process and intermediates are disclosed for the preparation of the optically active compound ##STR1## wherein R.sup.3 is a protecting group. This cyclobutanone compound is used to prepare a compound of the formula ##STR2## having anti-viral activity.
    Type: Grant
    Filed: April 29, 1991
    Date of Patent: August 3, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Saleem Ahmad
  • Patent number: 5231221
    Abstract: Compounds of the formula ##STR1## can advantageously be prepared by reacting compounds the formula II ##STR2## in which the substituents R.sup.1 -R.sup.4 have the meanings given, with the anhydride of the formula III ##STR3## in the presence of dimethyl sulfoxide and the acid corresponding to the anhydride of the formula III.
    Type: Grant
    Filed: March 18, 1991
    Date of Patent: July 27, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Winfried Hertzsch, Gerhard Jahne
  • Patent number: 5214191
    Abstract: 2-Phenylalkanoate esters which are useful as inhibitors of human leukocyte elastase.
    Type: Grant
    Filed: May 22, 1990
    Date of Patent: May 25, 1993
    Assignee: Cortech, Inc.
    Inventors: Gary P. Kirschenheuter, Lyle W. Spruce, John C. Cheronis
  • Patent number: 5208366
    Abstract: An improved process is provided for the preparation of esters of polyhalophthalic acids, polyhalobenzoic acids, and polyhalophthalic anhydride useful as flame retardants for thermoplastic and thermosetting resins, which comprises the reaction of the above acids or anhydride with alcohols in the presence of certain metal and metallorganic compounds as catalysts. Also provided are certain esters per se.
    Type: Grant
    Filed: August 19, 1991
    Date of Patent: May 4, 1993
    Assignee: Elf Atochem North America, Inc.
    Inventors: Joseph M. Bohen, Anthony J. Mancuso
  • Patent number: 5206423
    Abstract: This invention provides process embodiments for acyloxylation of C.sub.1 -C.sub.4 alkylaromatic compounds to produce alpha-acyloxy C.sub.1 -C.sub.4 alkyl-substituted aromatic compounds, utilizing a palladium-tin catalyst which exhibits efficient oxidation selectivity and oxidation rate stability.Toluene is acetoxylated to benzyl acetate and benzylidene diacetate.
    Type: Grant
    Filed: November 6, 1991
    Date of Patent: April 27, 1993
    Assignees: Philip Morris Incorporated, Philip Morris Products Inc.
    Inventors: Robert L. Augustine, Setrak K. Tanielyan
  • Patent number: 5204217
    Abstract: A photosensitive composition containing a compound having a group represented by formula (I) or (II), said group, when irradiated with actinic radiation, forming a carboxylic acid or a sulfonic acid: ##STR1## where R.sub.1 represents hydrogen, an alkyl group, or an aryl group; andR.sub.2 to R.sub.6 may be the same or different and each represents hydrogen, a halogen, an alkoxyl group, an aryloxyl group, cyano group, or an alkyl group, provided that at least one of R.sub.2 to R.sub.6 represents an alkoxyl or aryloxyl group and two of R.sub.2 to R.sub.6 may link to form a ring.
    Type: Grant
    Filed: January 16, 1991
    Date of Patent: April 20, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Toshiaki Aoai, Mitsunori Ono
  • Patent number: 5198568
    Abstract: This invention relates to novel compositions of matter which are esters with enhanced water solubility, for use in aqueous enzymatic resolution reactions of racemic mixtures of these esters for producing the separate chiral isomers of the racemic mixture. The invention also relates to novel methods for preparing these esters. The importance of the production of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities. Of particular significance regarding the water soluble esters of this invention is that they are derivatized with groups which enhance their aqueous solubility and their reactivity with enzymatic resolving methods which are mediated in an aqueous environment.
    Type: Grant
    Filed: September 9, 1991
    Date of Patent: March 30, 1993
    Assignee: Sepracor, Inc.
    Inventors: Charles M. Zepp, Stephen A. Wald, David R. Dodds
  • Patent number: 5194668
    Abstract: Carboxylic acid esters and formamide are efficiently obtained by reacting carboxylic acid amides and formic acid esters, or by reacting carboxylic acid amides, alcohols and carbon monoxide in the presence of a dehydrated condensate of carboxylic acid amide with an alkali metal hydroxide or an alkaline earth metal hydroxide catalyst.
    Type: Grant
    Filed: June 8, 1990
    Date of Patent: March 16, 1993
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Hideo Ikarashi, Hirofumi Higuchi, Koichi Kida
  • Patent number: 5192799
    Abstract: Amine represented by the following formula (1), or their acid addition salts or their quaternary ammonium salts. ##STR1## The amines of formula (1) or their pharmaceutically acceptable acid addition salts or quaternary ammonium salts are useful for the treatment and prevention of heart diseases of animals, particularly arrhythima, myocardial infarction, angina pectoris and heart failure and psychoneurological diseases.
    Type: Grant
    Filed: June 5, 1992
    Date of Patent: March 9, 1993
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Keiichi Yokoyama, Noriaki Kihara, Joji Kamiya, Kanji Yoshihara, Masaaki Ishii, Akira Mizuchi, Kazutoshi Horikomi, Akira Awaya, Takuo Nakano
  • Patent number: 5189204
    Abstract: 3-(2-Trifluoro-1-hydroxyethyl)propenyl benzyl ether or derivatives thereof having the formula ##STR1## wherein R is a substituted or not substituted phenyl group and a mark * shows an asymmetric carbon atom, and derivatives thereof are provided, which are useful as a material for preparing liquid crystal compound.
    Type: Grant
    Filed: June 25, 1991
    Date of Patent: February 23, 1993
    Assignee: Showa Shell Sekiyu Kabushiki Kaisha
    Inventors: Tomoya Kitazumo, Takashi Yamazaki, Hitoshi Iwatsubo
  • Patent number: 5185459
    Abstract: Cyclobutanols of the formula ##STR1## wherein P is a hydroxy protecting group are useful intermediates in the preparation of antiviral compounds.
    Type: Grant
    Filed: May 26, 1992
    Date of Patent: February 9, 1993
    Assignee: E. R. Squibb & Sons Inc.
    Inventors: William A. Slusarchyk, Robert Zahler
  • Patent number: 5177109
    Abstract: Compounds, compositions and methods are described for treating a CNS disorder such as a cognitive disorder, epilepsy, depression, Parkinson's disease, Alzheimer's disease, a neurodegenerative disease or neurotoxic injury. Compound of interest are 2-amino-4,5-methyleneadipic acid compounds and derivatives defined by the formula I: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl, ##STR2## with each of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein each of X and Y is independently selected from hydroxyl, alkoxy, alkylthio, amino and ##STR3## with each of R.sup.6 and R.sup.7 being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein any of R.sup.1 through R.sup.
    Type: Grant
    Filed: July 19, 1991
    Date of Patent: January 5, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Roberto Pellicciari, Benedetto Natalini, Maura Marinozzi, Alexis A. Cordi, Joseph B. Monahan, Thomas H. Lanthorn
  • Patent number: 5171915
    Abstract: It is disclosed that aromatic compounds can be alkylated with mono-olefinic HVI-PAO dimer in contact with an acidic catalyst to produce novel alkylated aromatic compositions. It has been found that the novel HVI-PAO dimer alkylated aromatic compositions exhibit an extraordinary combination of properties relating to low viscosity with high viscosity index and low pour point which renders them very useful as lubricant basestock. Further, it has been found that the novel alkylaromatic compositions of the present invention show improved oxidative stability. Depending upon the substituent groups on the aromatic nucleus, useful lubricant additives can be prepared for improved antiwear, antioxidant and other properties. HVI-PAO dimer is prepared as a product or by-product from 1-alkene oligomerization using reduced chromium oxide on solid support.
    Type: Grant
    Filed: February 21, 1989
    Date of Patent: December 15, 1992
    Assignee: Mobil Oil Corporation
    Inventors: Thomas R. Forbus, Bruce P. Pelrine
  • Patent number: 5166397
    Abstract: This invention relates to a process for producing an optically active cyclobutylamine which comprises reacting a racemic modification of cyclobuthylamine represented by the following general formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 represent each a hydrogen atom or a protecting group; with an optically active N-acylphenylglycine to thereby give two corresponding diastereomeric salts, crystallizing the more difficultly soluble diastereomeric salt and isolating the corresponding optically active cyclobutylamine from the diastereomeric salt thus crystallized. The optically active substances of the compound of the above general formula [I] are useful as, for example, an intermediate in the synthesis of 9-[(1R, 2R, 3S)-2,3-bis(hydroxymethyl)-1-cyclobutyl]guanine which is expected as an antiviral agent.
    Type: Grant
    Filed: September 10, 1991
    Date of Patent: November 24, 1992
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Kazuhisa Narita, Masashi Nagai, Hideo Sugimura, Yukihiro Sagawa, Akira Shiozawa
  • Patent number: 5155271
    Abstract: The invention relates to a process for the preparation of compounds of the formula ##STR1## in which Q is substituted or unsubstituted C.sub.1 -C.sub.6 alkyl, A is a direct bond or a bridging member, s is the number 1 or 2, Z is a radical of the formula --CH.sub.2 CH.sub.2 OH, --CH.dbd.CH.sub.2 or --CH.sub.2 CH.sub.2 --Y, and Y is a leaving group, and the benzene or napthalene nucleus I can be further substituted, which comprises reacting compounds of the formula ##STR2## with compounds of the formulaQ--OH (3)in which A, s, Z and Q are as defined under formula (1), in the presence of hydrogenation catalysts, and then carrying out further conversion reactions where appropriate.The compounds obtained by the process according to the invention are suitable as intermediates for the preparation of reactive dyes.
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: October 13, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Peter Aeschlimann
  • Patent number: 5149843
    Abstract: Conjugated diene compounds of the general formula: ##STR1## which are industrially advantageous intermediates for preparing sarcophytol A useful as an anticarcinogenic promotor or antitumor agent are provided.
    Type: Grant
    Filed: June 7, 1991
    Date of Patent: September 22, 1992
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Hisao Takayanagi, Yasunori Kitano, Yasuhiro Morinaka