Patents Examined by David E. Wheeler
  • Derivatives of 7-(.alpha.-hydroxy-substituted pyridyl carboxamido-.alpha. p h .DELTA..sup.3 -cephem-4-carboxylic acid
    Patent number: 4036834
    Abstract: Novel 7-(.alpha.-hydroxy-substituted pyridylcarboxamido-.alpha.-phenylacetamido)-3-substituted thiomethyl-.DELTA..sup.3 -cephem-4-carboxylic acid derivatives are disclosed. The compounds of this invention have high water solubility and show excellent antibacterial activities against various strains of Pseudomonas and Proteus.
    Type: Grant
    Filed: October 8, 1975
    Date of Patent: July 19, 1977
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Masuo Murakami, Masaru Iwanami, Ichiro Isaka, Yoshinobu Nagano, Masaharu Fujimoto, Tetsuya Maeda
  • 6.alpha., .beta.-Substituted penicillin derivatives
    Patent number: 4035359
    Abstract: Novel 6-methoxy and 6-thioalkyl-6-acylamido-penicillanic acids and their non-toxic pharmaceutically-acceptable salts, esters and amides which are useful as antibiotics. The products are prepared by treating an ester of 6-substituted-6-aminopenicillanic acid with an acylating agent followed by removal of the ester group. Also disclosed are novel intermediates.
    Type: Grant
    Filed: July 25, 1975
    Date of Patent: July 12, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Lovji D. Cama
  • 7 [.alpha.-Amino-.omega.-(2,3-methylenedioxy-phenyl)acylamido]cephalosporan ic acid derivatives
    Patent number: 4033956
    Abstract: Novel 7-[.alpha.-amino-.omega.-(2,3-methylenedioxyphenyl)acylamido] cephalosporanic acid derivatives are prepared which are useful as antibacterial agents.
    Type: Grant
    Filed: July 22, 1975
    Date of Patent: July 5, 1977
    Assignee: Richardson-Merrell Inc.
    Inventors: Raymond C. Erickson, Ronald E. Bambury
  • Cyclopenteno[1,2-h]quinol-4-one derivatives
    Patent number: 4033967
    Abstract: New cyclopenteno-quinolone derivatives of the formula ##STR1## wherein R is a saturated or unsaturated aliphatic hydrocarbyl, e.g., alkyl and alkenyl,X is hydrogen or alkyl, andY is halogen, azido, alkylthio, alkyl-sulfonyl, or nitrile or unsubstituted or substituted (e.g., alkyl mono or di-substituted) amino;And the pharmacologically compatible salts thereof; are outstandingly effective as bacteriostats in mammals.
    Type: Grant
    Filed: October 17, 1974
    Date of Patent: July 5, 1977
    Assignee: Boehringer Mannheim G.m.b.H.
    Inventors: Alfred Rhomberg, Herbert Berger, Kurt Stach, deceased, Werner Plattner, administrator, Wolfgang Vomel, Winfriede Sauer
  • 3-Hydroxymethyl-7.beta.-(2-alkoxy-or benzyloxyimino-2-arylacetamido)ceph-3-em-4-carboxylic acids and salts thereof
    Patent number: 4033950
    Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.
    Type: Grant
    Filed: March 24, 1976
    Date of Patent: July 5, 1977
    Assignee: Glaxo Laboratories Limited
    Inventors: Martin Christopher Cook, Gordon Ian Gregory, Janice Bradshaw
  • Thiacycl[2.2.2]azine carboxylic acids
    Patent number: 4033978
    Abstract: 3-Carboxy-5-substituted-thiacycl[2.2.2]azines of the formula: ##STR1## wherein R is phenyl or phenyl monosubstituted in the meta or para position with fluoro, chloro, lower alkyl of from 1 to 4 carbon atoms or lower alkoxy of from 1 to 4 carbon atoms, and the pharmaceutically acceptable salts thereof.These compounds are useful as anticomplimentary agents, specifically for the treatment of inflammatory conditions, auto-immune diseases, allergic reactions and vascular diseases.
    Type: Grant
    Filed: August 15, 1975
    Date of Patent: July 5, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Karl G. Untch, John O. Gardner
  • Nitrogen containing derivatives of cyclopenteno-quinolone compounds and bacteriostatic compositions
    Patent number: 4034096
    Abstract: New cyclopenteno-quinolone derivatives of the formula ##STR1## wherein R is a saturated or unsaturated aliphatic hydrocarbyl, e.g., alkyl and alkenyl,X is hydrogen or alkyl, andY is halogen, azido, alkylthio, alkyl-sulfonyl, or nitrile or unsubstituted or substituted (e.g., alkyl mono or di-substituted) amino;And the pharmacologically compatible salts thereof; are outstandingly effective as bacteriostats in mammals.
    Type: Grant
    Filed: July 14, 1975
    Date of Patent: July 5, 1977
    Assignee: Boehringer Mannheim G.m.b.H.
    Inventors: Alfred Rhomberg, Herbert Berger, Kurt Stach, deceased, by Werner Plattner, administrator, Wolfgang Vomel, Winfriede Sauer
  • Cephalosporin antibiotics
    Patent number: 4031083
    Abstract: Novel cephalosporin antibiotic derivatives.
    Type: Grant
    Filed: October 24, 1975
    Date of Patent: June 21, 1977
    Assignee: Yeda Research and Development Co., Ltd.
    Inventors: Fortuna Haviv, Abraham Patchornik, Janina Altman
  • Camptothecin analogues
    Patent number: 4031098
    Abstract: Camptothecin analogues showing more potent anti-tumor activity than a naturally occurring alkaloid camptothecin, which also exhibit an immunosuppressive activity, in which the 1-ethyl of camptothecin is replaced by various members of substitutents such as alkyls (except ethyl), alkenyls, alkynyls, aralkyls or aryloylalkyls; being produced from readily accessible starting materials on totally synthetic method newly developed by the present inventor.
    Type: Grant
    Filed: January 5, 1976
    Date of Patent: June 21, 1977
    Assignee: Shionogi & Co., Ltd.
    Inventor: Tsutomu Sugasawa
  • Dimeric anhydro-vinca derivatives
    Patent number: 4029663
    Abstract: Dimeric Vinca alkaloids are converted to three separable anhydro derivatives, useful as mitotic inhibitors or as intermediates for the preparation of other oncogenetically active alkaloids.
    Type: Grant
    Filed: July 10, 1975
    Date of Patent: June 14, 1977
    Assignee: Eli Lilly and Company
    Inventors: Gerald E. Gutowski, Jean C. Miller
  • 4(2' Isoquinolin-1-one)piperidines
    Patent number: 4029795
    Abstract: 1-(3-Aryloxy-2-hydroxypropyl)-4-(1-oxoisoquinolino)-piperidines, e.g. those of the formula ##STR1## R' = H, alkanoylaminoethenyl, carbamoyl, alkanoyl, CN, alkoxycarbonylamino-lower alkyl, halo, OH, alkanoylamino, alkyl, alkoxy, alkenyl, alkenyloxyR" = H, alkyl, alkoxy, alkenyl, alkenyloxy,R'" = alkanoylamino, NH.sub.2, NO.sub.2, alkyl, alkoxy, halo CF.sub.3, OH2-alkanoic acid esters and acid addition salts thereof are antihypertensive and antiarrhythmic agents.
    Type: Grant
    Filed: July 14, 1975
    Date of Patent: June 14, 1977
    Assignee: Ciba-Geigy Corporation
    Inventors: Kurt Eichenberger, Christian Egli, Hans Kuhnis, Oswald Schier
  • 1,4-Dithiin (and oxathiin)-yl cephalosporin derivatives, and compositions containing them
    Patent number: 4029781
    Abstract: New cephalosporin compounds of the formula: ##STR1## in which A is oxygen or sulphur, R.sub.1 is hydrogen or acetoxy and R.sub.2 is carboxy or a radical of the formula: ##STR2## in which the radical ##STR3## is a radical which can be easily removed enzymatically, and in which R.sub.3 is hydrogen or straight or branched chain C.sub.1-4 alkyl and R.sub.4 is straight or branched chain C.sub.1-4, alkyl or cyclohexyl, together with its diastereoisomeric forms and mixtures thereof, its acid addition salts and, where appropriate, its pharmaceutically acceptable non-toxic metal salts and addition salts with nitrogen-containing bases other than ammonia, exhibit valuable anti-bacterial properties, in particular against Gram-positive and Gram-negative bacteria.
    Type: Grant
    Filed: September 26, 1975
    Date of Patent: June 14, 1977
    Assignee: Rhone-Poulenc Industries
    Inventors: Christian Berger, Daniel Farge, Georges Gros, Mayer Naoum Messer, Claude Moutonnier
  • 3-Piperazinyl 1,2,4-benzothiadiazine 1,1-dioxide derivatives their compositions and method of use
    Patent number: 4029780
    Abstract: A compound of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group, and R.sub.2 represents a hydrogen or halogen atom or a trifluoromethyl group,And its pharmaceutically acceptable salt. The compound is prepared by reacting the corresponding 1,2,4-benzothiadiazine 1,1-dioxide with a piperazine compound or alkylating 1,2,4-benzothiadiazine 1,1-dioxide whose corresponding 3-position is substituted by a piperazinyl group. The above compound has superior antihypertensive activity separated from diuretic, antidiuretic and hyperglycemic activities, and is free from side-effects.
    Type: Grant
    Filed: October 28, 1975
    Date of Patent: June 14, 1977
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Haruki Nishimura, Masanao Shimizu, Naonobu Hatano, Katsuyoshi Nakatsuzi, Hiroaki Kinugasa, Hiroko Kon
  • Conversion of 4-lower alkyloxazole-5-carboxamide to 4-lower alkyl-5-cyanooxazoles
    Patent number: 4026901
    Abstract: A process is disclosed whereby 4-lower alkyl-5-cyanooxazoles, are obtained by vapor phase catalytic dehydration of 4-lower alkyloxazole-5-carboxamides.
    Type: Grant
    Filed: April 30, 1975
    Date of Patent: May 31, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: David Llewellyn Coffen
  • Cephalosporin antibiotics
    Patent number: 4026887
    Abstract: Novel cephalosporin antibiotic derivatives.
    Type: Grant
    Filed: October 24, 1975
    Date of Patent: May 31, 1977
    Assignee: Yeda Research & Development Co. Ltd.
    Inventors: Fortuna Haviv, Abraham Patchornik
  • 2-(5-Ethyl-6-bromothiazolo[3,2-b]-5-triazolyl)thiophosphonate esters, compositions and method of use
    Patent number: 4024252
    Abstract: A compound of the formula ##STR1## WHEREIN R.sub.1 is alkyl having 1 to 3 carbon atoms; is useful as insecticide.
    Type: Grant
    Filed: June 19, 1975
    Date of Patent: May 17, 1977
    Assignee: Nippon Soda Company Limited
    Inventors: Mitsuo Asada, Meiki Ando, Michihiko Matsuda, Tomio Yamada, Hitoshi Watanabe, Saburo Kano, Osami Nomura
  • (Carbamoyl)pyridino derivatives of ureidocephalosporins
    Patent number: 4024135
    Abstract: Ureido cephalosporin derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl; or certain heterocyclic groups; are disclosed. These compounds are useful as antibacterial agents.
    Type: Grant
    Filed: March 5, 1976
    Date of Patent: May 17, 1977
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner
  • 2-Aminomethyl- and 2-(2-aminoethyl)-substituted 4,5-diphenyloxazoles
    Patent number: 4020082
    Abstract: 2-Aminomethyl- and 2-(2-aminoethyl)-substituted 4,5-diphenyloxazoles of the general formula ##STR1## and salts thereof with non-toxic organic or inorganic acids having antiphlogistic, analgesic, anti-aggregant and local anaesthetic properties with low toxicity are provided, as well as processes for preparing them.
    Type: Grant
    Filed: August 5, 1975
    Date of Patent: April 26, 1977
    Inventor: Enzo Marchetti
  • 7.beta.-Acyloxy cephalosporins
    Patent number: 4020057
    Abstract: The compounds of this invention are cephalosporins having a 7.beta.-acyloxy group and 7.beta.-hydroxy intermediates for the preparation thereof. The compounds have antibacterial activity.
    Type: Grant
    Filed: June 18, 1975
    Date of Patent: April 26, 1977
    Assignee: SmithKline Corporation
    Inventor: John G. Gleason
  • 7-[.alpha.-Amino- .omega.-(3,4-methylenedioxyphenyl)acylamido]cephalosporanic acid derivatives
    Patent number: 4020060
    Abstract: Novel 7-[.alpha.-amino-.omega.-(3,4-methylenedioxyphenyl)acylamido]cephalosporan ic acid derivatives are prepared which are useful as antibacterial agents.
    Type: Grant
    Filed: July 22, 1975
    Date of Patent: April 26, 1977
    Assignee: Richardson-Merrell Inc.
    Inventors: Raymond C. Erickson, Ronald E. Bambury