Patents Examined by D. B. Springer
  • Patent number: 4675332
    Abstract: Novel acidic indole compounds having use as antiallergic agents, methods of synthesis, compositions, and uses are claimed.
    Type: Grant
    Filed: October 21, 1985
    Date of Patent: June 23, 1987
    Assignee: Warner-Lambert Company
    Inventors: David T. Connor, Paul C. Unangst, S. Russell Stabler
  • Patent number: 4672073
    Abstract: A diphenoxypropane derivative of the formula: ##STR1## wherein X is a halogen atom, Y is a hydrogen atom or a hydroxy group and Z is a tetrazolyl or carboxy group, has excellent antiasthmatic and antiinflammatory activities, and therefore the diphenoxypropane derivatives are useful as antiasthmatic or antiiflammatory agents.
    Type: Grant
    Filed: November 5, 1985
    Date of Patent: June 9, 1987
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Akira Nohara, Yoshitaka Maki
  • Patent number: 4670446
    Abstract: The invention provides the compounds of formula ##STR1## in which n equals 1 or 2,R denotes hydrogen, alkyl of 1 to 4 carbon atoms or phenyl,R.sub.1 denotes hydrogen, alkyl of 1 to 4 carbon atoms or alkenyl of 2 to 4 carbon atoms, X and Y, which may be identical or different, are each attached to the quinoline ring system in position 5, 6, 7 or 8, and each denote hydrogen or alkoxy of 1 to 3 carbon atoms. These compounds are useful in the treatment of cardiac arrhythmias.
    Type: Grant
    Filed: March 6, 1985
    Date of Patent: June 2, 1987
    Assignee: Rhone-Poulenc Sante
    Inventors: Michel Mestre, Christian Renault
  • Patent number: 4670452
    Abstract: There are provided benzopyrans of formula I ##STR1## wherein R.sub.6 and R.sub.7 together form the chain --CHOCH.dbd.(A.sub.1 E.sub.1)--O-- in which --O-- is attached to R.sub.7,R.sub.5 represents hydrogen,R.sub.8 represents propyl,A represents a single bond,A.sub.1 represents a single bond, phenylene or (CH.sub.2).sub.m,m represents an integer from 1 to 10 inclusive,E and E.sub.1, which may be the same or different, independently represent --COOH, 5H-tetrazolyl, or CONR.sub.24 R.sub.25, wherein R.sub.24 and R.sub.25, which may be the same or different, represent hydrogen or alkyl of C.sub.1 to C.sub.6 ;provided that when A.sub.1 represents a single bond, then E.sub.1 represents 5H-tetrazolyl or CONR.sub.24 R.sub.25, and their pharmaceutically acceptable salts, all of which are useful as anti-asthmatics.
    Type: Grant
    Filed: January 28, 1985
    Date of Patent: June 2, 1987
    Assignee: Fisons plc
    Inventors: Kenneth J. Gould, John L. Suschitzky
  • Patent number: 4670451
    Abstract: 3,4-Disubstituted benzoxa(thia)zole-2-one derivatives of the formula; ##STR1## wherein R.sub.1 is a halogen atom or methyl group, R.sub.2 is a methyl or ethyl group and X and Y are individually an oxygen or sulfur atom, and their preparation and use as a fungicide.
    Type: Grant
    Filed: May 20, 1985
    Date of Patent: June 2, 1987
    Assignee: Sumitomo Chemical Company, Ltd.
    Inventors: Tamon Uematsu, Satoru Inoue, Norihisa Yamashita
  • Patent number: 4668796
    Abstract: The invention relates to a process for resolving racemic mixtures of bicyclic imino-.alpha.-carboxylic esters into the components by crystallization of diastereomeric salts, which comprises preparing the salts of the racemic esters with optically active N-acylated R- or S-aminocarboxylic acid which contain a phenyl nucleus, recrystallizing them from an organic solvent, decomposing the precipitated, optically homogeneous diastereomeric salts in a manner known per se, and isolating the enantiomers and, where appropriate, converting the latter into the free acids by hydrolysis in a manner known per se. The invention also relates to optically pure compounds of the formula ##STR1## and to diastereomeric salts of these compounds, in which two of the radicals A, B.sup.1, B.sup.2 and C form a carbon chain and the others denote hydrogen, and R is an esterifying group.
    Type: Grant
    Filed: January 30, 1984
    Date of Patent: May 26, 1987
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rolf Geiger, Volker Teetz, Dietrich Langner
  • Patent number: 4668797
    Abstract: The invention relates to compounds of the formula I ##STR1## in which n denotes 0 or 1,R denotes hydrogen, alkyl or aralky, R.sup.1 denotes hydrogen or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, which each can be substituted by alkyl, alkoxy or halogen, arylalkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined in the aforegoing, a monocyclic or bicyclic sulfur or oxygen and/or nitrogen heterocyclic radical, or a side chain of a naturally occurring aminoacid, R.sup.
    Type: Grant
    Filed: September 27, 1985
    Date of Patent: May 26, 1987
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hansj/o/ rg Urbach, Rainer Henning, Volker Teetz, Hans Wissman, Reinhard Becker
  • Patent number: 4666935
    Abstract: Substituted maleimides of the formula in whichX represents hydrogen, chlorine or bromine,X.sup.1 represents chlorine or bromine,n represents 2, 3, 4 or 5 andR represents halogen, alkyl, optionally substituted aryl, aryloxy or cycloalkyl, halogenoalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, nitro, cyano, alkoxycarbonyl, alkylcarbonyl, carboxyl, carbonylamino, hydroxyl, alkoxy, halogenoalkoxy, acyloxy, sulphonylamino, alkylsulphonyl, alkylmercapto, marcapto, acylmercapto, halogenoalkylmercapto, amino, mono- or di-alkylamino or acylamino andm represents 1, 2, 3, 4 or 5,which possess fungicidal activity.
    Type: Grant
    Filed: February 8, 1984
    Date of Patent: May 19, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerhard Marzolph, Heinz U. Blank, Paul Reinecke, Wilhelm Brandes, Gerd Hanssler
  • Patent number: 4665189
    Abstract: There are described compounds of formula ##STR1## in which n is 0, 1 or 2, R.sup.1 is a hydrocarbyl group optionally substituted with an optionally substituted phenyl group and containing from 5 to 30 carbon atoms, R.sup.2 is optionally substituted phenyl or C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.6 where R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.7 where each R.sup.7 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.8 where R.sup.8 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.9 where R.sup.9 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, and R.sup.3, R.sup.4 and R.sup.5 are each selected from hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, C.sub.
    Type: Grant
    Filed: July 30, 1984
    Date of Patent: May 12, 1987
    Assignee: Lilly Industries Limited
    Inventors: Stephen R. Baker, William B. Jamieson, Alec Todd
  • Patent number: 4663461
    Abstract: A novel process for producing a 1-H-tetrazole-5-thiol of the formula: ##STR1## in which R.sup.1 is hydrogen; lower alkyl; lower alkyl substituted with a carboxylic acid, a carboxylic acid lower alkyl ester, or an hydroxy group; phenyl or phenyl substituted with a halogen, a lower alkyl group, or a lower alkoxy group; benzyl or benzyl substituted with a halogen, a lower alkyl group, or 1-3 alkoxy groups of 1-3 carbon atoms; or trichloroethyl,which process comprises:(a) reacting a sulfinyl or sulfonyl cyanide of the formula:RS(O).sub.n CNin whichn is 1 or 2 andR is alkyl; phenyl or phenyl substituted with a halogen, a lower alkyl group, or a lower alkoxy group; benzyl or benzyl substituted on the phenyl ring with a halogen, a lower alkyl group, or a lower alkoxy group; or an alicyclic group,with an azide of the formula R.sup.1 N.sub.5, in which R.sup.1 is as defined above, to form a 5-sulfinyl or sulfonyl-1-H-tetrazole of the formula: ##STR2## in which n is 1 or 2, andR and R.sup.
    Type: Grant
    Filed: January 7, 1985
    Date of Patent: May 5, 1987
    Assignee: American Home Products Corporation
    Inventors: Dieter H. Klaubert, John H. Sellstedt
  • Patent number: 4661606
    Abstract: Amino acids can be purified and/or concentrated by extracting aqueous mixtures such as fermentation broths by contacting an aqueous mixture containing amino acids with an organic solution containing a water insoluble extractant.
    Type: Grant
    Filed: June 6, 1984
    Date of Patent: April 28, 1987
    Assignee: Henkel Corporation
    Inventors: Francis W. Tuominen, Ronald R. Swanson, Phillip L. Mattison, Kenneth D. MacKay, Bradley W. Glorvigen
  • Patent number: 4659840
    Abstract: Provided is a method for preparing diaryl iodonium salts represented by the formula:[Ar.sub.1 --I.sup..sym. --Ar.sub.2 ]HSO.sub.4.sup..crclbar.wherein Ar.sub.1 and Ar.sub.2 respectively are an aryl group which may be substituted with an electron donor group and which may be the same or different which comprises subjecting a compound represented by the formula Ar.sub.1 --H wherein Ar.sub.1 is as defined above and a compound Ar.sub.2 --I wherein Ar.sub.2 is as defined above to a coupling reaction in a sulfuric acid solution containing an oxidizing agent and diluted with a diluting agent to a concentration of 85% by weight or less at a reaction temperature in the range from -20.degree. to +35.degree. C.
    Type: Grant
    Filed: March 8, 1984
    Date of Patent: April 21, 1987
    Assignee: Nippon Petrochemicals Co., Ltd.
    Inventors: Isoo Shimizu, Yasuo Matsumura, Yoshihisa Inomata
  • Patent number: 4659834
    Abstract: A process is disclosed for preparing a compound of the Formula (I) ##STR1## wherein R.sup.2 is trifluoromethyl or chloro;R.sup.3 is hydrogen or chloro; andX is halogen; wherein a compound of the Formula (II) ##STR2## wherein R.sup.5 is --CFCl.sub.2, --CF.sub.2 Cl, or --CCl.sub.3 ; andR.sup.6 is chloro or trichloromethyl;is fluoroinated either with a mixture of antimony (III) fluoride and antimony (V) chloride or bromide; or with antimony (V) fluoride; or with antimony (V) chloride and hydrogen fluoride.
    Type: Grant
    Filed: December 5, 1983
    Date of Patent: April 21, 1987
    Assignee: Alkaloida Vegyeszeti Gyar
    Inventors: Zoltan Salamon, Ilona Imre nee Virag, Magdolna Sebestyen
  • Patent number: 4659817
    Abstract: Compounds and methods featuring, in one aspect, compositions containing an organic boronic acid and one or more reporter groups.
    Type: Grant
    Filed: August 8, 1984
    Date of Patent: April 21, 1987
    Assignee: The Children's Medical Center Corporation
    Inventors: Paul M. Gallop, Mercedes Paz
  • Patent number: 4659706
    Abstract: Sulfinyl and sulfonyl substituted 3-benzazepine compounds are useful in treating gastrointestinal motility disorders. A particular compound of this invention is 8-hydroxy-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine.
    Type: Grant
    Filed: December 20, 1985
    Date of Patent: April 21, 1987
    Assignee: SmithKline Beckman Corporation
    Inventors: William E. Bondinell, Herbert S. Ormsbee, III
  • Patent number: 4658038
    Abstract: Analgesia-effecting 5-hydroxytryptophan derivatives are disclosed of the formulae: ##STR1## wherein R is selected from the group consisting of C.sub.2 -C.sub.16 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.16 alkenyl, C.sub.2 -C.sub.16 alkynyl, aryl containing up to 14 carbon atoms, and arylalkyl containing up to 20 carbon atoms;R.sup.2 and R.sup.2a are each H or R, as defined above;R.sup.3 and R.sup.3a are each H or alkyl containing from 1 to 4 carbons;R.sup.4 and R.sup.4a are each H or alkyl containing from 1 to 4 carbons;and their non-toxic, pharmacologically acceptable acid addition salts.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: April 14, 1987
    Assignees: Research Foundation for Mental Hygiene, Inc., Yeda Research and Development Co. Ltd.
    Inventors: Hadassah Tamir, Stephen E. Karpiak, Meir Wilchek
  • Patent number: 4658039
    Abstract: The new indole derivatives of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and denote hydrogen or lower alkyl,R.sup.3 denotes hydrogen, lower alkyl or halogen andR.sup.4 and R.sup.5 are identical or different and denote hydrogen, lower alkyl or optionally substituted aryl, and R.sup.4 and R.sup.5 can also represent lower alkenyl, andwhereinR.sup.2 and R.sup.5 can be linked by an alkylene bridge of the formula--CH.sub.2 --CH.sub.2 --CH.sub.2).sub.nin whichn represents the number 0 or 1, can be prepared by reacting an ammonium or phosphonium salt of the corresponding indolecarboxylic acid with a haloacetic acid allyl ester. The new compounds can be used to prepare acemetacin. The new indole derivatives possess a pharmacological action.
    Type: Grant
    Filed: November 21, 1985
    Date of Patent: April 14, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventor: Samir Samaan
  • Patent number: 4656190
    Abstract: Indene derivatives have been found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and are thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, and adult respiratory distress syndrome.
    Type: Grant
    Filed: November 14, 1983
    Date of Patent: April 7, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Tsung-Ying Shen, Shu S. Yang, San-Bao Hwang
  • Patent number: 4656292
    Abstract: 2,3-Dimethylmaleimido-alkyl or oxaalkyl haloacetates are useful in the preparation of polymers containing maleimide groups and quaternary ammonium groups which polymers are soluble in water. The polymers can be used as light-sensitive photographic recording materials which can be developed with water.
    Type: Grant
    Filed: June 17, 1985
    Date of Patent: April 7, 1987
    Assignee: Ciba-Geigy Corporation
    Inventor: Martin Roth
  • Patent number: 4652642
    Abstract: 9-Azido-6-halo-3-lower alkyl-2,3,4,5-tetrahydro-1H-3-benzazepines are prepared from their 9-amino congeners. The compounds are useful as photoaffinity probes for .alpha..sub.2 -adrenoceptor sites in biological samples.
    Type: Grant
    Filed: August 23, 1984
    Date of Patent: March 24, 1987
    Assignee: SmithKline Beckman Corporation
    Inventor: Robert M. DeMarinis