Patents Examined by G. Hendricks
  • Patent number: 4560695
    Abstract: This invention provides certain isoxazole and isothiazole derivatives, their pharmaceutical formulations, and their use in inhibiting aromatase and treating or preventing estrogen-dependent diseases in mammals.
    Type: Grant
    Filed: June 18, 1984
    Date of Patent: December 24, 1985
    Assignee: Eli Lilly and Company
    Inventors: Kenneth S. Hirsch, Charles D. Jones, Harold M. Taylor, Mark A. Winter
  • Patent number: 4560558
    Abstract: Disclosed are compounds of the formula: ##STR1## wherein X is hydrogen, loweralkyl, loweralkoxy or halo, Y is hydroxymethyl, carboxyl, carboxamido or carboloweralkoxy, and R is cyclohexyl, benzyl, norbornyl, loweralkyl, or a pharmaceutically acceptable salt thereof.The compounds are effective as diuretic agents.
    Type: Grant
    Filed: May 16, 1983
    Date of Patent: December 24, 1985
    Assignee: Abbott Laboratories
    Inventors: James A. Parks, Jacob J. Plattner
  • Patent number: 4556712
    Abstract: In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically active enantiomers can serve as important intermediates for both natural and unnatural opioids.
    Type: Grant
    Filed: March 18, 1983
    Date of Patent: December 3, 1985
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventor: Kenner C. Rice
  • Patent number: 4554006
    Abstract: Phenylpropylammonium salts of the formula ##STR1## where R.sup.1 denotes for instance alkyl or halogen, R.sup.2 denotes for instance alkyl or alkoxy, R.sup.3 denotes alkyl, alkenyl or alkynyl of up to 6 carbon atoms, R.sup.4 and R.sup.5 denote hydrogen or alkyl of up to 3 carbon atoms, m denotes one of the integers 0, 1, 2 and 3, n denotes one of the integers 0, 1 and 2, o denotes one of the integers 4, 5 and 6, X.sup..crclbar. denotes an anion, and the dashed bond may be hydrogenated when n is 0 or 1, and is hydrogenated when n is 2; the preparation of these compounds; and agents for regulating plant growth containing these compounds as active ingredients.
    Type: Grant
    Filed: December 8, 1980
    Date of Patent: November 19, 1985
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Buschmann, Bernd Zeeh, Johann Jung, Hubert Sauter
  • Patent number: 4549026
    Abstract: A process for the preparation of condensed triazoles of formula I ##STR1## in which R together with the triazole group form an aromatic group R.sub.1 is hydrogen or a hydrocarbon groupthe process comprisingreacting in a medium containing an organic phase a compound of formula II ##STR2## with a nitrite and an acid. The reaction is preferably carried out at a raised temperature.
    Type: Grant
    Filed: March 2, 1982
    Date of Patent: October 22, 1985
    Assignee: Sandoz Ltd.
    Inventors: Michel Deur, Istvan Toth
  • Patent number: 4547511
    Abstract: This invention relates to novel heterocyclic carboxamides which increase the activity of the immune system and to the preparation thereof. The invention is also concerned with pharmaceutical compositions containing the said compounds and methods of treatment therewith.
    Type: Grant
    Filed: February 22, 1982
    Date of Patent: October 15, 1985
    Assignee: Aktiebolaget Leo
    Inventors: Edgar Eriksoo, Eva B. Sandberg, Lars J. T. Stalhandske
  • Patent number: 4547523
    Abstract: A new polyether antibiotic has been isolated from fermentations of a new microorganism of the genus Streptomyces. This new microorganism is designated as N478-13 and it has ben named Streptomyces routienii Huang sp. nov., (ATCC 39446). The new antibiotic exhibits antibacterial activity against a variety of gram-positive bacteria; it can be used to control swine dysentery; and it promotes increased efficiency of feed utilization (i.e. promotes increased growth) in swine and ruminants.
    Type: Grant
    Filed: November 7, 1983
    Date of Patent: October 15, 1985
    Assignee: Pfizer Inc.
    Inventors: Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
  • Patent number: 4547494
    Abstract: A 7.beta.-{(Z)-2-(2-aminothiazol-4-yl)-2-[(2-pyrrolidon-3-yl)oxyimino]acetam ido}-3-(1-amino-1H-tetrazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof is useful as an antimicrobial agent.
    Type: Grant
    Filed: February 9, 1984
    Date of Patent: October 15, 1985
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Toyonari Oine, Yoshihisa Yamada, Mitsuyoshi Wagatsuma, Totaro Yamaguchi, Satoshi Ohshima
  • Patent number: 4544752
    Abstract: 3-Phenyl (or meta or para-substituted phenyl)-4-permissibly substituted-5-isothiazolecarboxylic acids, salts, esters and simple amides, used to lower uric acid levels in mammals.
    Type: Grant
    Filed: June 6, 1983
    Date of Patent: October 1, 1985
    Assignee: Eli Lilly and Company
    Inventors: James R. Beck, Robert P. Gajewski, Ronald E. Hackler
  • Patent number: 4542135
    Abstract: 9-Thia ergot cyclic peptide alkaloids produced by fermentation or synthetic methods have interesting anti-parkinson and other pharmacological activities.
    Type: Grant
    Filed: August 3, 1982
    Date of Patent: September 17, 1985
    Assignee: Sandoz Ltd.
    Inventors: Hans Kobel, Jean-Jacques Sanglier, Hans Tscherter, Georg Bolliger
  • Patent number: 4539328
    Abstract: Nematicidal 3-aryl-4-amino-5-isothiazole acids, esters and amides of the formula ##STR1## wherein A is selected from hydroxy, alkoxy, phenylmethoxy, and --NHR, where R is hydrogen, alkyl, 2-hydroxyethyl or 2-acetyloxyethyl; andZ is selected from hydrogen, halogen, alkyl, alkoxy, difluoromethoxy, thiomethyl, nitro, amino, and phenyl.
    Type: Grant
    Filed: March 25, 1983
    Date of Patent: September 3, 1985
    Assignee: FMC Corporation
    Inventors: William S. DiMenna, David M. Floyd
  • Patent number: 4536499
    Abstract: This disclosure describes novel compounds of the formula ##STR1## where m is 2, 3 or 4X is hydrogen or hydroxyR.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms or lower alkoxy having 1 to 4 carbon atoms, andR.sub.2 and R.sub.3 each independently represent lower alkyl as defined above, orR.sub.2 and R.sub.3 together with N represent ##STR2## wherein n is 1, 2 or 3, andR.sub.4 represents hydrogen or lower alkyl as defined above, andR.sub.5 represents hydrogen, lower alkyl, phenyl or phenyl substituted with fluoro, chloro, lower alkyl having 1 to 4 carbon atoms, or lower alkoxy having 1 to 4 carbon atoms, with the proviso that when X is hydroxy, m is 3 or 4,or a pharmaceutically acceptable acid addition salt thereof, which are useful in the treatment of diabetes by inhibiting or impeding post-prandial hyperglycemia.
    Type: Grant
    Filed: April 1, 1983
    Date of Patent: August 20, 1985
    Assignee: Sandoz, Inc.
    Inventors: Leonard J. Brand, Jeffrey Nadelson
  • Patent number: 4533672
    Abstract: This invention relates to indole derivatives which have anti-cancer activity. According to the invention there is provided an indole derivative of the formula I: ##STR1## in which X is an oxygen or sulphur atom, Ra is a phenyl radical which is optionally substituted by one or two groups selected from halogen atoms and 1-6C alkyl, 1-6C alkoxy and trifluoromethyl radicals and Rb is a hydrogen atom or a 2-6C alkoxycarbonyl radical. Manufacturing processes and pharmaceutical compositions are also described.
    Type: Grant
    Filed: October 24, 1983
    Date of Patent: August 6, 1985
    Assignee: Imperial Chemical Industries plc
    Inventors: Murdoch A. Eakin, Anthony J. Hayter, Barrington J. A. Furr
  • Patent number: 4532239
    Abstract: Basically-substituted pyridazines of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, independently of one another, denote hydrogen, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkoxyalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, alkoxy, hydroxyalkoxy, alkoxy-alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, phenalkoxy, alkanoyl, alkanoylamino and --NH--CO--R.sup.9, R.sup.9 representing morpholino, piperidino or 1-pyrrolididinyl, or an optionally substituted ureido radical, R.sup.4 denotes hydrogen or lower alkyl and W denotes hydrogen, chlorine or bromine; and the acid-addition salts thereof are useful alone or in pharmaceutical preparations for treating cardiac complaints, circulatory complaints and high blood pressure. Several methods for preparing the basically-substituted pyridazines are also provided.
    Type: Grant
    Filed: December 20, 1983
    Date of Patent: July 30, 1985
    Assignee: Cassella Aktiengesellschaft
    Inventors: Thomas Raabe, Helmut Bohn, Piero A. Martorana, Rolf-Eberhard Nitz
  • Patent number: 4528381
    Abstract: The invention provides a process for preparing triazoles comprising reacting a compound having the structural formula ##STR1## with a compound having the formulaR--ON.dbd.Oin the presence of C.sub.6 -C.sub.10 alkanol, wherein n is 0, 1 or 2, R is C.sub.6 -C.sub.10 alkyl and R.sup.1 is hydrogen or C.sub.1 -C.sub.10 alkyl.
    Type: Grant
    Filed: August 26, 1982
    Date of Patent: July 9, 1985
    Assignee: Uniroyal, Inc.
    Inventors: Richard A. Gencarelli, Edward L. Wheeler
  • Patent number: 4526892
    Abstract: Novel ergoline derivatives formed by reaction of an 8-carboxy ergoline with a carbodiimide and having hypotensive and antiprolatinic activity.
    Type: Grant
    Filed: December 9, 1982
    Date of Patent: July 2, 1985
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Patricia Salvati, Anna M. Caravaggi, Aldemio Temperilli, Germano Bosisio, Osvaldo Sapini, Enrico di Salle
  • Patent number: 4526977
    Abstract: 7-[2-(3-Amino-5-isoxazolyl)-2-alkyloxyiminoacetamido]-ceph-3-em-4-carboxyli c acid derivatives are antibacterial agents effective against gram-positive and gram-negative bacterium.
    Type: Grant
    Filed: April 7, 1983
    Date of Patent: July 2, 1985
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, John R. Potoski
  • Patent number: 4526980
    Abstract: Tetranitrodibenzo-1,3a,4,6a-tetrazapentalene is prepared from diaminobenzene by reacting diaminobenzene and lead dioxide in ethylacetate to produce diaminoazobenzene, isolating the product by silica-gel elution, reacting diaminoazobenzene with an inorganic azide in a dilute aqueous nitrous acid solution at a temperature not in excess of 10.degree. C. to produce diazidoazobenzene, isolating the product, heating diazidoazobenzene slowly to about 190.degree. C. until nitrogen stops evolving to form dibenzotetrazapentalene, isolating the product, nitrating dibenzotetrazapentalene with concentrated sulfuric acid and forming nitric at a temperature not in excess of about 65.degree. C. to product tetranitrodibenzo-1,3a,4,6a-tetrazapentalene.
    Type: Grant
    Filed: July 6, 1983
    Date of Patent: July 2, 1985
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Marguarite S. Chang, Robert R. Orndoff
  • Patent number: 4525358
    Abstract: New 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids, their amides and their salts, processes for the preparation thereof and therapeutic compositions. These compounds have the formula ##STR1## wherein Y=--OH or --NH.sub.2 ; X and X'=H, halogen, alkoxy or trifluoromethyl; m=1 or 2 and n=1 or 2.The amides of the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids are prepared either by reacting a 1-(diphenylmethyl)-piperazine with an omegahaloacetamide, or by reacting an alkali metal salt of an omega-[4-(diphenylmethyl)-1-piperazinyl]-alkanol with a 2-haloacetamide, or yet by reacting ammonia with a halide or alkyl ester of a 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid, whereas the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids are prepared by hydrolyzing the corresponding amide or lower alkyl ester.These compounds have in particular an antiallergic, spasmolytic and antihistaminic activity.
    Type: Grant
    Filed: May 17, 1983
    Date of Patent: June 25, 1985
    Assignee: UCB Pharmaceuticals, Inc.
    Inventors: Eugene Baltes, Jean de Lannoy, Ludovic Rodriguez
  • Patent number: 4524208
    Abstract: A process for preparing lysergic acid esters of the formula ##STR1## wherein R is alkyl of up to 3 carbon atoms, comprises reacting corresponding lysergic acid or isolysergic acid amides with corresponding alcohols at temperatures of 0.degree. to 65.degree. C. for 2 to 30 hours in the presence of an acid at a pH value of 0-1.
    Type: Grant
    Filed: May 26, 1983
    Date of Patent: June 18, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Gregor Haffer