Patents Examined by Anne Marie T. Tighe
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Patent number: 3962242Abstract: Nitrofuryl-triazolo[4,3-b]pyridazine compounds of the formula ##SPC1##WhereinR.sub.1 is lower alkoxy radical or a saturated 5- or 6-membered heterocyclic ring attached via a cyclic nitrogen atom, which heterocyclic ring can also contain, in addition to said cyclic nitrogen atom, a cyclic oxygen atom or an optionally lower alkylated cyclic nitrogen atom and R.sub.2 is a hydrogen atom or R.sub.1 and R.sub.2 together represent an additional valency bond,Are outstandingly effective as bacteriostats and are particularly useful in the treatment of bacterial infections in the urinary tract.Type: GrantFiled: January 30, 1975Date of Patent: June 8, 1976Assignee: Boehringer Mannheim G.m.b.H.Inventors: Herbert Berger, Rudi Gall, Max Thiel, Wolfgang Vomel, Winfriede Sauer
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Patent number: 3954754Abstract: This invention provides aminopyridazine derivatives of formula I, ##SPC1##whereinR.sub.1 is amino, or an ##EQU1## group, wherein each of R.sub.3 and R.sub.4 is alkyl of 1 to 4 carbon atoms, orR.sub.3 and R.sub.4 together with the carbon atom to which they are bound, form a cycloalkylidene radical of 5 to 12 carbon atoms,R.sub.2 is hydrogen or methyl,A is a --(CH.sub.2).sub.n -- group,Whereinn is 0 or an integer from 1 to 7, or an >N--CO--R.sub.5 group,WhereinR.sub.5 is alkyl or alkenyl of 1 to 16 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, 1-adamantyl, or a --(CH.sub.2).sub.m --R.sub.6 group,Whereinm is 0 or an integer from 1 to 4, andR.sub.Type: GrantFiled: July 3, 1974Date of Patent: May 4, 1976Assignee: Sandoz Ltd.Inventor: Erhard Schenker
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Patent number: 3950361Abstract: A process for purifying beta-lactones, which comprises contacting a beta-lactone selected from the group consisting of alpha, alpha-dimethyl-beta-propiolactone, beta-propiolactone and a mixture of these with a solid alkaline earth metal hydroxide.Type: GrantFiled: July 12, 1971Date of Patent: April 13, 1976Assignee: Teijin Ltd.Inventors: Yasuo Taneda, Tadakazu Tsutada
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Patent number: 3950334Abstract: O-alkyl-S-alkyl-O[6-alkyl- or 6-halo-pyridazin-(3)-yl]-(thiono)thiolphosphoric acid esters of the formula ##SPC1##In whichR and R', which may be identical or different, are each alkyl with 1 to 4 carbon atoms,R" is alkyl with 1 to 3 carbon atoms or halogen, andX is oxygen or sulfur,Which possess insecticidal and acaricidal properties.Type: GrantFiled: November 11, 1974Date of Patent: April 13, 1976Assignee: Bayer AktiengesellschaftInventors: Hans-Jochem Riebel, Lothar Rohe, Ingeborg Hammann, Wolfgang Behrenz
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Patent number: 3948912Abstract: New nitroimidazolyl-triazolo-pyridazines of the formula: ##SPC1##WhereinZ is methyl or amino which can be substituted by lower alkyl,And the pharmacologically compatible acid-addition salts thereof, exhibit outstanding anti-microbial activity against bacteria and protozoa, and also systemic effectiveness.Type: GrantFiled: March 17, 1975Date of Patent: April 6, 1976Assignee: Boehringer Mannheim G.m.b.H.Inventors: Herbert Berger, Rudi Gall, Kurt Stach, Wolfgang Vomel, Rita Hoffmann
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Patent number: 3948916Abstract: New diglycidyl compounds of mononuclear, five-membered or six-membered, unsubstituted or substituted, hydroxyalkylated N-heterocyclic compounds, produced by addition of formaldehyde or acetaldehyde to mononuclear, five-membered or six-membered, unsubstituted or substituted, N-heterocyclic compounds, for example hydantoin or dihydrouracil, to monohydroxyalkyl compounds, and subsequent glycidylation of the OH group and NH group to give the corresponding glycidyl compounds.Type: GrantFiled: September 13, 1973Date of Patent: April 6, 1976Assignee: Ciba-Geigy AGInventors: Daniel Porret, Jurgen Habermeier, Willy Fatzer, Dieter Baumann
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Patent number: 3948897Abstract: A facile process for the production of Ftorafur [1-(tetrahydro-2-furanyl)-5-fluorouracil] which comprises reacting 2,4-bis-trimethylsilyl uracil with 2-chlorotetrahydrofuran to produce 1-tetrahydro-2-furanyluracil at low temperatures in a dry non-aqueous solvent, e.g. a halogenated hydrocarbon solvent such as methylene chloride. Subsequently the desired final product is produced by direct fluorination of the uracil ring as the last step utilizing a fluorinating agent such as trifluoromethylhypofluorite. This step is conducted in the cold and again in the presence of a halogenated hydrocarbon solvent such as chloroform. Ftorafur has been utilized as a pyrimidine analog for the management of carcinoma in the breast and large intestine and with less side effects than 5-fluorouracil (5-FU).Type: GrantFiled: October 9, 1973Date of Patent: April 6, 1976Assignee: The United States of America as represented by the Secretary of Health, Education and WelfareInventors: Leroy B. Townsend, Robert A. Earl
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Patent number: 3948904Abstract: Novel cephalosporin and penicillin antibiotic derivatives.Type: GrantFiled: June 24, 1974Date of Patent: April 6, 1976Assignee: Yeda Research & Development Co. Ltd.Inventors: Abraham Patchornik, Fortuna Haviv
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Patent number: 3947444Abstract: A process for producing N.sub.1 -(dihydroxyalkyl)-5-substituted uracils of the formula: ##SPC1##WhereinR.sub.1 is hydrogen, methyl, a trihalomethyl, a halogen,R.sub.2 is 1,4-dihydroxybutyl-2,1,4-dihydroxypentyl-2,2,5-dihydroxypentyl-1,Characterized by reducing N.sub.1 -(butyrolactone)uracils of the formula: ##SPC2##WhereinR.sub.1 is hydrogen, methyl, a trihalomethyl, a halogen,A is: ##SPC3##With an alkali metal boron hydride in an aqueous or aquo-alcoholic solution at a temperature ranging from 15.degree. to 50.degree.C.Type: GrantFiled: June 21, 1973Date of Patent: March 30, 1976Inventors: Solomon Aronovich Giller, Regina Abramovna Zhuk, Anna Eduardovna Berzinya, Laima Avgustovna Sherinya
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Patent number: 3947443Abstract: 1,3-Bis(halomethyl)phenobarbitals are prepared by reacting phenobarbital with formaldehyde and a chlorine source or a bromine source at a temperature of -10.degree. to 200.degree.C in the presence of a Lewis acid catalyst, the formaldehyde and bromine or chlorine source being employed in at least approximately twice the molar amounts of phenobarbital. These compounds are useful anticonvulsant agents.Type: GrantFiled: May 17, 1974Date of Patent: March 30, 1976Assignee: The Kendall CompanyInventor: Julius A. Vida
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Patent number: 3947437Abstract: Disclosed are novel substituted pyridazinyloxy(thio)phenyl ureas and derivatives thereof. The compounds of the instant invention are useful as herbicides and can be formulated to provide herbicidal compositions.Type: GrantFiled: January 22, 1974Date of Patent: March 30, 1976Assignee: The Dow Chemical CompanyInventor: Howard Johnston
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Patent number: 3947517Abstract: In the synthesis of tetracyclines, a critical step is the stereospecific or stereoselective introduction of a hydroxyl group at the C-12(a) position, a novel method for the introduction of this critical hydroxy group is disclosed. Additionally, synthetic procedures for obtaining tetracycline precursors are discussed.Type: GrantFiled: December 29, 1972Date of Patent: March 30, 1976Assignee: Research CorporationInventors: Hans H. Muxfeldt, Jeffrey Michael
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Patent number: 3947464Abstract: The d,l-phenylpropanolamine racemate is split with optically active thiazolidine-4-carboxylic acids of the formula: ##EQU1## where R.sub.1 R.sub.2 are hydrogen, alkyl of 1 to 8 carbon atoms, cycloalkyl, aryl or alkylene of at least 2 carbon atoms or R.sub.1 and R.sub.2 together form a ring of alkyl or alkylene with 4 to 12 carbon atoms and AC is acyl, especially benzoyl, tosyl, nitrophenylsulfenyl, acetyl or preferably formyl.Type: GrantFiled: November 27, 1973Date of Patent: March 30, 1976Assignee: Deutsche Gold- und Silber-Scheideanstalt vormals RoesslerInventors: Friedrich Asinger, Heribert Offermanns
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Patent number: 3946046Abstract: Process for resolving a racemic mixture of an oxo-type prostaglandin intermediate by (a) converting the oxo compound by reaction with an optically active ephedrine to a mixture of oxazolidine diastereomers, (b) separating at least one oxazolidine diastereomer from said mixture, (c) hydrolyzing said oxazolidine to free the optically active oxo compound, and (d) recovering said optically active oxo compound.Type: GrantFiled: December 15, 1972Date of Patent: March 23, 1976Assignee: The Upjohn CompanyInventor: Robert C. Kelly
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Patent number: 3946031Abstract: Novel 2-substituted-1,2,4-thiadiazolo-[ 2,3-a]-benzimidazoles of the formula ##SPC1##And the pharmaceutically acceptable salts thereof; and process for their preparation. These 2-substituted-1,2,4-thiadiazole-[2,3-a]-benzimidazoles are useful as fungistatic and fungicidal agents.Type: GrantFiled: November 14, 1974Date of Patent: March 23, 1976Assignee: Syntex Inc.Inventor: Colin C. Beard
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Patent number: 3946030Abstract: An improved process for the production of 2-mercaptoarylthiazoles comprising reacting a primary aryl amine and sulfur with selected nitrogen-containing compounds including thiourea, urea, cyanamide, metal cyanamide salts, dicyanodiamide, ammonium thiocyanate, and the like, in the presence or absence of carbon disulfide.Type: GrantFiled: August 1, 1974Date of Patent: March 23, 1976Assignee: Phillips Petroleum CompanyInventor: Howard W. Bost
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Patent number: 3944569Abstract: This invention relates to a class of phthalein indicator dyes useful as optical filter agents in photographic processes to protect a selectively exposed photosensitive material from further exposure during processing in the presence of incident light. Such dyes comprise 3,3-disubstituted phthalides and 3,3-disubstituted naphthalides wherein the 3,3 substituents are p-hydroxy carbocyclic aryl radicals wherein one or both of the radicals possess a --CH.sub.2 --NRR' group ortho to the p-hydroxy group and the --CH.sub.2 --NRR' group(s) is capable of rendering the indicator dye substantially non-diffusible in aqueous solution.Type: GrantFiled: August 27, 1973Date of Patent: March 16, 1976Assignee: Polaroid CorporationInventors: Stanley M. Bloom, Elbert M. Idelson, Myron S. Simon, David P. Waller
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Patent number: 3944550Abstract: Vitamin E orotate which is useful in medicines and cosmetics, is produced by esterifying vitamin E with an orotyl halide or orotic anhydride or with orotic acid in the presence of phosphorous oxychloride.Type: GrantFiled: September 27, 1973Date of Patent: March 16, 1976Assignee: Kanebo Ltd.Inventors: Kyotaro Hasunuma, Masahiro Kurokawa, Takashi Abe
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Patent number: 3940354Abstract: Cephalosporon compounds of the formula ##SPC1##In the form of racemic mixtures or optically active isomers or in the form of their cis or trans isomers or mixtures thereof wherein R is selected from the group consisting of phenyl substituted with at least one hydroxyl and sydnone optionally substituted with phenyl, R' is selected from the group consisting of hydrogen and R", R" is an ester group easily removable by acid hydrolysis or hydrogenolysis, R.sub.1 and R.sub.2 are alkyl of 1 to 3 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, Y is selected from the group consisting of amino and Y', Y' is hydrogen and NHCOOZ, Z is straight or branched alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable addition salts with organic and inorganic acids and bases where appropriate with the proviso that when Y is amino, R' is hydrogen and when Y is amino or NHCOOZ, R is phenyl which have antibacterial activity and their preparation.Type: GrantFiled: January 25, 1974Date of Patent: February 24, 1976Assignee: Roussel-UCLAFInventors: Jacques Martel, Rene Heymes, Andre Lutz
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Patent number: 3937707Abstract: 6-Substituted derivatives of 1-phenazinol 5,10-dioxide which possess broad spectrum anti-microbial activity are disclosed.Type: GrantFiled: July 22, 1974Date of Patent: February 10, 1976Assignee: Hoffmann-La Roche Inc.Inventors: Willy Leimgruber, Manfred Weigele