Patents Examined by Ethel G. Love
  • Patent number: 4465686
    Abstract: Disclosed and claimed is the cardiotonic use of 1-R.sub.1 -5-(3-R'-4-R"-phenyl)-6-R-2(1H)-pyridinones (II), where R.sub.1 is hydrogen, lower-alkyl or lower-hydroxyalkyl, R is lower-alkyl or hydrogen, and, R' and R" are each hydrogen, amino or hydroxy, at least one of R' or R" being other than hydrogen, or where R' is nitro when R" is hydroxy, or pharmaceutically acceptable acid-addition salts thereof where at least one of R' and R" is amino. Also disclosed and claimed are 1-R.sub.1 -5-(3-R'-4-R"-phenyl)-6-R-2(1H)-pyridinones (I), where R.sub.1, R' and R" are defined as above and R is lower-alkyl and acid-addition salts thereof where at least one of R' and R" is amino. Also shown and claimed is the process which comprises reacting 1-R.sub.1 -1,2-dihydro-2-oxo-5-(3-R'-4-R"-phenyl)-6-R-nicotinonitrile, where R.sub.
    Type: Grant
    Filed: April 26, 1982
    Date of Patent: August 14, 1984
    Assignee: Sterling Drug Inc.
    Inventors: George Y. Lesher, Chester J. Opalka, Jr., Donald F. Page, Ruthann M. McGarry
  • Patent number: 4465869
    Abstract: The specification describes a process for the production of a 4-alkoxymethyl-1,3-dioxolan in good yield, in high purity and in a simple manner by reacting an alkyl glycidyl ether with a carbonyl compound in the presence of an acid catalyst. The 4-alkoxymethyl-1,3-dioxolan is useful as an intermediate for the production of an .alpha.-monoalkyl glyceryl ether by hydrolysis.
    Type: Grant
    Filed: July 19, 1982
    Date of Patent: August 14, 1984
    Assignee: Kao Corporation
    Inventors: Naotake Takaishi, Kouichi Urata, Yoshiaki Inamoto
  • Patent number: 4465672
    Abstract: New S-adenosylmethionine salts have been prepared which are stable indefinitely with time, even at elevated temperatures.The new salts correspond to the formula: ##STR1## in which X is the equivalent of an organic sulphonic acid of pK less than 2.5,and possess therapeutic activity in numerous fields of human therapy.
    Type: Grant
    Filed: August 16, 1982
    Date of Patent: August 14, 1984
    Assignee: Bioresearch S.p.A.
    Inventor: Federico Gennari
  • Patent number: 4464359
    Abstract: 3'-Deoxyadenosine 5'-triphosphate is oligomerized to form (2'-5')-oligo (3'-deoxyadenylate) by incubation with adenosine triphosphate: (2'-5')-oligo adenosine adenyl transferase, in the presence of an inert support carrying a double stranded polynucleotide. The (2'-5')-oligo (3'-deoxyadenylate) is digested with a suitable phosphatase to remove the terminal phosphate groups. The thus produced corresponding 3'-deoxyadenosine compound is an anti-viral material effective against Herpes Simplex infection and effective in inhibiting the transformation of cells infected with Epstein Barr virus.
    Type: Grant
    Filed: April 10, 1981
    Date of Patent: August 7, 1984
    Assignee: Research Corporation
    Inventors: Robert J. Suhadolnik, Joseph M. Wu, Paul Doetsch, Earl E. Henderson
  • Patent number: 4464361
    Abstract: Adenosine derivatives of the general formula: ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## in which R.sup.5 and R.sup.6 are each hydrogen, alkoxy or arylthio and R.sup.7 is hydrogen or halogen, or a group of the formula: ##STR3## and R.sup.2, R.sup.3 and R.sup.4 are each hydrogen or alkanoyl, and pharmaceutically acceptable salt thereof.These derivatives and salts thereof are useful as antihypertensives, bradycardiacs, etc. The method of production thereof and pharmaceutical compositions based on those adenosine derivatives or salts are also described.
    Type: Grant
    Filed: April 14, 1982
    Date of Patent: August 7, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Sadao Ohki, Fumiko Hamaguchi, Tatsuo Nagasaka, Hiroyuki Kikuchi
  • Patent number: 4464389
    Abstract: Pentaerythritol retinoates and monobenzal acetals thereof such as (E)-2.sub..alpha. -phenyl-5.sub..alpha. -hydroxy-methyl-5.sub..beta. -retinoyloxymethyl-1,3-dioxane, (E)-2.sub..alpha. -phenyl-5.sub..beta. -hydroxymethyl-5.sub..alpha. -retinoyloxymethyl-1,3-dioxane, and pentaerythritol monoretinoate are disclosed. These retinoids are useful as chemopreventive agents and as therapeutic agents for treating nonmalignant skin disorders.
    Type: Grant
    Filed: October 20, 1982
    Date of Patent: August 7, 1984
    Assignee: SRI International
    Inventor: Marcia I. Dawson
  • Patent number: 4462993
    Abstract: The invention relates to novel aminoacridine-.alpha.,.beta.-(D)- and -(L)-N-glycoside derivatives, the salts thereof and to a novel process for the preparation of such compounds and salts. The novel compounds have the formula I ##STR1## wherein R is hydrogen or a group of the formula II ##STR2## wherein n=0 or 1, p=1 or 2, A.sup.-p is an anion, preferably halogenide, R.sup.1 is hydrogen or a methyl group andR.sup.2 is hydrogen or a sugar residue, or R is dimethylamine,and the two substituentsX and X.sup.1 are identical or different and stand for hydrogen, a group of the formula II, dimethylamine, halogen, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group, for a nitro-, cyano-, carbomethoxy-, carbamoyl-, phenyl- or a C.sub.1-4 alkylphenyl group,with the restriction that at least one of the substituents R, X and X.sup.1 represents a group of formula II with R.sup.2 =sugar residue, andR.sup.3 is hydrogen or a C.sub.1-5 alkyl group.
    Type: Grant
    Filed: March 1, 1982
    Date of Patent: July 31, 1984
    Assignee: Biogal Gyogyszergyar
    Inventors: Antal Kovacs, Andras Liptak, Pal Nanasi, Lorant Janossy, Istvan Csernus, Janos Erdei, Istvan Kaszab, Kalman Polya, Andras Neszmelyi
  • Patent number: 4460604
    Abstract: A class of 4-amine-4-arylcyclohexanones, their ketals, and acid addition salts have been synthesized and found to be useful for relieving pain in animals. Their analgesic activity appears to be of high order, and in addition some exhibit narcotic antagonist activity that is useful in modifying the cardiovascular, respiratory, and behavioral depression caused by other analgesics. Several show mixed analgesic and narcotic antagonist activity. Preferred compounds of the class are 4-(m-hydroxyphenyl)-4-dimethylaminocyclohexanone ethylene ketal, and 4-(m-hydroxyphenyl)-4-(n-butylmethylamino)cyclohexanone ethylene ketal as free bases and as their hydrochloride salts.Processes for synthesis and intermediates are described. Unit dosage forms and therapeutic treatments are disclosed.
    Type: Grant
    Filed: October 22, 1980
    Date of Patent: July 17, 1984
    Assignee: The Upjohn Company
    Inventor: Daniel Lednicer
  • Patent number: 4459418
    Abstract: A new method for the preparation of acetals of long chain fatty aliphatic aldehydes and polyols containing four or more hydroxyl groups which produces the acetals in a relatively pure form by reaction in a mutual solvent, preferably a C.sub.1 to C.sub.4 fatty carboxylic acid. The `clean` acetals are useful emulsifying agents and their esters and polyalkoxy substituents are useful dispersants and surfactants for aqueous compositions.
    Type: Grant
    Filed: April 15, 1980
    Date of Patent: July 10, 1984
    Assignee: Imperial Chemical Industries
    Inventor: James N. Greenshields
  • Patent number: 4459304
    Abstract: 2-Anilino-3,5-dinitro-benzotrifluorides of the formula ##STR1## in which X is O, S, SO or SO.sub.2,n is 1, 2, 3 or 4,R.sup.1 is haloalkyl, haloalkoxyalkyl, phenyl, halophenyl, haloalkylphenyl, haloalkoxyphenyl, haloalkylmercaptophenyl or haloalkylsulphonyl, andR.sup.2 each independently is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl or haloalkoxyalkyl, orXR.sup.1 and R.sup.2, when in the ortho-position relative to one another, together with the two adjacent carbon atoms of the phenyl nucleus, form an optionally halogen-substituted dioxanyl ring, orprovided X represents S, SO or SO.sub.2, R.sup.1 can represent unsubstituted alkyl in addition to the aforementioned radicals,which possess arthropodicidal, nematicidal, fungicidal and bactericidal properties.
    Type: Grant
    Filed: March 28, 1979
    Date of Patent: July 10, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alfons Hartmann, Erich Klauke, Ingeborg Hammann, Peter Roessler, Volker Paul
  • Patent number: 4459417
    Abstract: This invention is a novel chemical particularly concerned with N-dealkylation of secondary amines as found in amino-cylitols of which spectinomycin is an example. Separation and further alkylation also comprise the present invention process.
    Type: Grant
    Filed: February 23, 1983
    Date of Patent: July 10, 1984
    Assignee: The Upjohn Company
    Inventor: Richard C. Thomas
  • Patent number: 4458067
    Abstract: An N.sup.6,O.sup.2' -diacyladenosine-3',5'-cyclic phosphoric ester alkali metal salt can be obtained with ease and in a high yield by reacting an adenosine-3',5'-cyclic phosphoric ester alkali metal salt with a carboxylic anhydride having 4 or less carbon atoms at a temperature of 70.degree. C. or above.
    Type: Grant
    Filed: December 30, 1981
    Date of Patent: July 3, 1984
    Assignee: Kikkoman Corporation
    Inventors: Nobuyuki Yamaji, Kyoko Tahara, Motohiko Kato
  • Patent number: 4456614
    Abstract: The present invention concerns chemical compounds of the general formula: ##STR1## in which: R.sub.1 and R.sub.2 may be identical or different and represent a hydrogen or halogen atom or else a lower alkyl, lower alkoxy, nitro or acetyl group andR represents a lower alkyl or lower aralkyl group, such as benzyl.These compounds are useful in therapy for the treatment of hypertension and cardiac arrhythmia.
    Type: Grant
    Filed: April 2, 1981
    Date of Patent: June 26, 1984
    Assignee: Pierre Fabre S.A.
    Inventors: Gilbert Mouzin, Henri Cousse, Pol Vilain
  • Patent number: 4455420
    Abstract: A compound, 4-Amino-7-(5-deoxy-beta-D-ribofuranosyl)-5-iodo-7H-pyrrolo[2,3-d] pyrimidine, as well as process to produce this compound, are disclosed. The compound is useful as a muscle relaxant.
    Type: Grant
    Filed: January 13, 1983
    Date of Patent: June 19, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Rymantas Kazlauskas
  • Patent number: 4455435
    Abstract: Leuco Crystal Violet Lactone is prepared by condensing one molar proportion of each of N,N-dimethylaniline, p-dimethylaminobenzaldehyde, and m-dimethylaminobenzoic acid with 0-1 molar proportion of urea and 1-4 molar proportions of a strong acidic condensing agent.
    Type: Grant
    Filed: January 22, 1979
    Date of Patent: June 19, 1984
    Assignee: American Cyanamid Company
    Inventors: John P. Dundon, Erwin Klingsberg
  • Patent number: 4450171
    Abstract: 6(R)-[2-(8'-acyloxy-2'-methyl-6'-methyl (or hydrogen)-polyhydronaphthyl-1')-ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H- pyran-2-ones are prepared by acylation of the corresponding 8'-hydroxy compounds. The products are strong inhibitors of the biosynthesis of cholesterol.
    Type: Grant
    Filed: June 14, 1982
    Date of Patent: May 22, 1984
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Robert L. Smith, Alvin K. Willard
  • Patent number: 4447600
    Abstract: Nucleoside or glucose derivatives of N-acetylneuraminic acids are provided, which have immunological activity, are clinically useful, as an immuno suppressive, in particular to treat autoimmune disease such as collagenosis disease without causing any serious side-effects and may be prepared by subjecting a halide of N-acetylneuraminate derivative together with a nucleoside or a glucose to Koenigs-Knorr reaction.
    Type: Grant
    Filed: May 20, 1982
    Date of Patent: May 8, 1984
    Assignee: Kanto Ishi Pharmaceutical Co., Ltd.
    Inventors: Haruo Ogura, Kimio Furuhata, Toshiaki Osawa, Satoshi Toyoshima, Yoshiyasu Shitori, Masayoshi Ito
  • Patent number: 4444784
    Abstract: 6(R)-[2-(8'-acyloxy-2'-methyl-6'-methyl (or hydrogen)-polyhydronaphthyl-1')-ethyl]-4 (R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones are prepared by acylation of the corresponding 8'-hydroxy compounds. The products are strong inhibitors of the biosynthesis of cholesterol.
    Type: Grant
    Filed: December 18, 1980
    Date of Patent: April 24, 1984
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Robert L. Smith, Alvin K. Willard
  • Patent number: 4438275
    Abstract: Benzyl esters of the formula ##STR1## in which n is 1,2,3,4, or 5,R.sup.2 is hydrogen, C.sub.1-4 -alkyl, cyano or ethynyl,R.sup.3 is radical of a carboxylic acid customary in pyrethroids or pyrethroid-like compounds, andat least one R.sup.1 is fluoroalkoxy or fluoroalkylmercapto, or two together are fluoromethylene- or fluoroethylene-dioxy, and the others, if present, are hydrogen or various radicals,which possess arthropodicidal properties. Various alcohols, amines, aldehydes, halides, and the like, corresponding to the alcohol moieties of the esters are also synthesized.
    Type: Grant
    Filed: July 30, 1981
    Date of Patent: March 20, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Lantzsch, Albrecht Marhold, Wolfgang Behrenz, Ingeborg Hammann
  • Patent number: 4436667
    Abstract: This invention relates to the preparation of cyclopropane carboxylic acid ester derivatives, which are useful as pesticides.There is provided a process for preparing a mixture of cis-isomers of a compound of formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from chlorine, bromine and methyl, consisting predominantly of the 1R cis S- and 1S cis R- isomers, which process comprises dissolving a mixture of 1S cis S- and 1R cis R- isomers of the compound of formula I, alone or in the presence of 1R cis S- and 1S cis R-isomers, in an organic amine base containing from 5 to 7 carbon atoms and being a secondary amine containing two branched alkyl groups or a tertiary amine, crystallizing out from a resulting solution of cis- isomers of formula I in the organic amine base a 1:1 mixture of the 1R cis S- and 1S cis R- isomers, and evaporating off the organic amine base.
    Type: Grant
    Filed: April 10, 1981
    Date of Patent: March 13, 1984
    Assignee: Shell Internationale Research Maatschappij B. V.
    Inventor: Michael J. Bull