The Five-membered Hetero Ring Consists Of Chalcogen, Plural Nitrogens, And Carbon Patents (Class 548/125)
  • Patent number: 5599793
    Abstract: This invention relates to L-arginine aldehyde derivatives, having the Formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: February 4, 1997
    Assignee: Eli Lilly and Company
    Inventors: Nickolay Y. Chirgadze, Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5589439
    Abstract: Herbicidal novel tetrazolinone derivatives of the formula: ##STR1## wherein R.sup.1 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, andR.sup.2 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, orR.sup.1 and R.sup.2 form, together with the nitrogen atom to which R.sup.1 and R.sup.2 are bonded, a 5- or 6-membered heterocyclic ring, optionally fused to a carbocyclic ring optionally and independently substituted by C.sub.1-4 alkyl, andR.sup.3 is a 5-membered heterocyclic radical containing at least one hereto atom selected from the group consisting of nitrogen, oxygen, and sulfur, optionally substituted by at least one substitutent selected from the group consisting of halogen, benzyl, phenyl, halogen-substituted phenyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkyl-sulfonyl and C.sub.
    Type: Grant
    Filed: July 28, 1995
    Date of Patent: December 31, 1996
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Koichi Moriya, Fritz Maurer, Seishi Ito, Katsuaki Wada, Kazuhiro Ukawa, Ryo Watanabe, Asami Ito, Natsuko Minegishi
  • Patent number: 5569655
    Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: October 29, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5567725
    Abstract: Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases which are characterized by an elevated secretion of glucose from the liver or by an elevated activity of the glucose-6-phosphatase system.
    Type: Grant
    Filed: February 14, 1995
    Date of Patent: October 22, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Horst Hemmerle, Gerrit Schubert, Peter Below, Andreas Herling, Hans-J org Burger
  • Patent number: 5532228
    Abstract: The invention discloses side-chain homologous vitamin D derivatives of formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, B, and D have the meanings defined in the specification and either (1) A is a direct bond between carbon atoms 20 and 22 and X is an oxy alkylene radical, --(CH.sub.2).sub.n O-- where n is 1 to 3; (2) A is a methylene bridge, --CH.sub.2 --, between carbon atoms 20 and 22 and X is either an alkylene radical, --(CH.sub.2).sub.n -- or an oxy alkylene radical, --(CH.sub.2).sub.n O--, where n is 1 to 3; or (3) if A is a direct bond and B and D together form a second bond, then X(R.sup.5) (R.sup.6) is ##STR2## The compounds possess proliferation-inhibiting and cell-differentiating activity.
    Type: Grant
    Filed: June 1, 1993
    Date of Patent: July 2, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Gunter Neef, Gerald Kirsch, Andreas Stein-Eyer, Katica Schwarz, Matthias Brautigam, Ruth Thieroff-Ekerdt, Petra Rach
  • Patent number: 5530117
    Abstract: The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: June 25, 1996
    Assignee: American Cyanamid Company
    Inventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross
  • Patent number: 5527813
    Abstract: The present invention relates to therapeutically active azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.
    Type: Grant
    Filed: March 2, 1994
    Date of Patent: June 18, 1996
    Assignee: Novo Nordisk A/S
    Inventors: Per Sauerberg, Preben H. Olesen
  • Patent number: 5525436
    Abstract: The subject invention relates to solid polymer electrolyte membranes comprising proton conducting polymers stable at temperatures in excess of 100.degree. C., the polymer being basic polymer complexed with a strong acid or an acid polymer. The invention further relates to the use of such membranes in electrolytic cells and acid fuel cells. Particularly, the invention relates to the use of polybenzimidazole as a suitable polymer electrolyte membrane.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: June 11, 1996
    Assignee: Case Western Reserve University
    Inventors: Robert F. Savinell, Morton H. Litt
  • Patent number: 5523312
    Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: June 4, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
  • Patent number: 5486531
    Abstract: The present invention relates to hydroxymethylfurazancarboxylic acid derivatives of the general formula I ##STR1## in which one of the radicals R.sup.1 and R.sup.2 represents hydroxymethyl and the other represents ##STR2## where X represents NR.sup.3 R.sup.4, OH or OR.sup.7, and R.sup.3, R.sup.4 and R.sup.7 are defined as indicated in claim 1, to processes for their preparation and to their use.
    Type: Grant
    Filed: March 7, 1994
    Date of Patent: January 23, 1996
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Helmut Bohn
  • Patent number: 5484772
    Abstract: This invention relates to L-arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.
    Type: Grant
    Filed: October 5, 1994
    Date of Patent: January 16, 1996
    Assignee: Eli Lilly and Company
    Inventors: Daniel J. Sall, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5482967
    Abstract: Novel compound represented by the formula: ##STR1## such as 6-Chloro-N-(2,6-diethoxyphenyl)-4-(2-methylphenyl-2-oxo-2H-1-benzopyran-3- acetamide: ##STR2## or a salt thereof. The compound has an excellent activity of inhibiting ACAT, lowering the cholesterol in blood and inhibiting tachykinin receptor. The present invention also relates to the production and use of the disclosed compound.
    Type: Grant
    Filed: September 2, 1993
    Date of Patent: January 9, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideaki Natsugari, Hitoshi Ikeda, Takenori Ishimaru, Takayuki Doi
  • Patent number: 5478934
    Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: December 26, 1995
    Inventors: Jun Yuan, Jan W. F. Wasley
  • Patent number: 5474995
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases, ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: January 10, 1994
    Date of Patent: December 12, 1995
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Ducharme, Jacques Y. Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
  • Patent number: 5468854
    Abstract: Conjugates of fluorescent labels with specific, selective, and high affinity ligands for receptors have been synthesized and used to directly measure binding to receptors. In the examples, fluorescein conjugates of the high-affinity benzodiazepine receptor ligands Ro 15-1788 and Ro 7-1986 were synthesized. The binding of these fluorescent ligands (BD 621, BD 623 and BD 607) to benzodiazepine receptors was characterized by direct fluorescence measurement. Both the equilibrium dissociation constants (K.sub.D) of BD 621 and BD 607 and the maximum number of binding sites (B.sub.max) estimated by fluorescence monitoring were consistent with values obtained by using radioligand binding techniques. The binding of BD 621 and BD 607 assessed by fluorescence measurement was reversible, abolished by photoaffinity labeling with Ro 15-4513, and unaffected by a variety of substances that do not bind to benzodiazepine receptors.
    Type: Grant
    Filed: July 22, 1993
    Date of Patent: November 21, 1995
    Assignee: Pharmaceutical Discovery Corporation
    Inventors: R. Tyler McCabe, Brian R. de Costa
  • Patent number: 5462963
    Abstract: The present invention involves photoprotective compositions which are useful for topical application to prevent damage to skin caused by acute or chronic exposure to ultraviolet light comprising chelating agents having the structure: ##STR1## wherein each --R.sup.1 is independently selected from the group consisting of alkyl, aryl, heteroaryl and heterocycle, or the --R.sup.1 's are covalently bonded together to form a cyclic alkyl or heterocyclic ring; --R.sup.2 and --R.sup.3 are --OR.sup.4, in which case there is no bond or a polar bond between --R.sup.2 and the nitrogen covalently bonded to --R.sup.3, each --R.sup.4 being independently selected from the group consisting of hydrogen, alkyl and aryl, except that both --R.sup.4 's are not methyl when both --R.sup.1 's are furyl; or --R.sup.2 is --O-- and is covalently bonded to the nitrogen which is covalently bonded to --R.sup.3, and --R.sup.3 is --O-- (there being a + charge on the nitrogen to which it is bonded) or nil;wherein the .alpha.
    Type: Grant
    Filed: August 2, 1991
    Date of Patent: October 31, 1995
    Assignee: The Procter & Gamble Company
    Inventors: Rodney D. Bush, Donald L. Bissett
  • Patent number: 5462694
    Abstract: A mesomorphic compound of the formula (I) according to claim 1 characterized by having at least one cyclic group selected from .beta. class including, e.g., thiazole-2,5-diyl, benzoxazole-2,5-diyl, indan-2,5-diyl, and quinoxaline-2,6-diyl and also having a linkage of Y.sup.1 (CH.sub.2).sub.m Y.sup.2, where Y.sup.1 and Y.sup.2 are --CH.sub.2 --, --O--, --COO-- or --OCO-- and m is 1-16, is suitable as a component for a liquid crystal composition providing improved response characteristics. A liquid crystal device is constituted by disposing the liquid crystal composition between a pair of substrates. The liquid crystal device is used as a display panel constituting a liquid crystal apparatus providing good display characteristics.
    Type: Grant
    Filed: August 30, 1994
    Date of Patent: October 31, 1995
    Assignee: Canon Kabushiki Kaisha
    Inventors: Yoko Kosaka, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura, Ikuo Nakazawa
  • Patent number: 5460669
    Abstract: The energetic salts of 3-nitramino-4-nitrofurazan have a desirable combination of desirable properties such as sufficiently high densities, and low or no hydrogen content. The salts are useful as ingredients in various propellant, explosive, gassifier, and pyrotechnic compositions. 3-Nitramino-4-nitrofurazan is itself a useful energetic compound and is also useful in the synthesis of still further energetic compounds.
    Type: Grant
    Filed: June 28, 1993
    Date of Patent: October 24, 1995
    Assignee: Thiokol Corporation
    Inventors: Rodney L. Willer, Robert S. Day, Dennis J. Park, deceased
  • Patent number: 5459264
    Abstract: A method for reducing an .alpha.,.beta.-unsaturated ketone of the present invention includes the step of treating the .alpha.,.beta.-unsaturated ketone with a silyl compound in the presence of a Lewis acid and alcohol to selectively reduce the carbonyl group of the .alpha.,.beta.-unsaturated ketone. According to this method, a deoxy-compound can be obtained from the .alpha.,.beta.-unsaturated ketone by selectively reducing the carbonyl group without reducing an .alpha.,.beta.-unsaturated bond.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: October 17, 1995
    Assignee: Shionogi Seiyaku Kabushiki Kaisha
    Inventors: Mitsuru Imuta, Makoto Kobayashi, Teruo Iizuka
  • Patent number: 5457122
    Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.
    Type: Grant
    Filed: July 13, 1993
    Date of Patent: October 10, 1995
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
  • Patent number: 5426109
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: August 27, 1992
    Date of Patent: June 20, 1995
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, Pierre Hamel
  • Patent number: 5424326
    Abstract: The present invention relates to phenyl-1,2,5-oxadiazolecarboxamide-2-oxides of the general formula I ##STR1## in which one of the radicals R.sup.1 and R.sup.2 represents ##STR2## and the other represents ##STR3## and R.sup.3 and R.sup.4 are defined as indicated in claim 1, to processes for their preparation and to their use for the treatment of disorders of the cardiovascular system, including angina pectoris and erectile dysfunctions.
    Type: Grant
    Filed: May 25, 1993
    Date of Patent: June 13, 1995
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Helmut Bohn
  • Patent number: 5405857
    Abstract: The present invention relates to hitherto unknown 3-substituted 1,2,3,4-oxatriazole-5-imine compounds which have proved to have biological effects making them suitable for treatment of cardiovascular diseases (blood clots), angina pectoris and asthma, a process for the preparation thereof and a pharmaceutical preparation comprising said compounds.
    Type: Grant
    Filed: July 19, 1993
    Date of Patent: April 11, 1995
    Assignee: A/S GEA Farmaceutisk Fabrik
    Inventors: Gunnar L. Karup, Herbert F. Preikschat, Tim N. Corell, Bodil G. Lissau, Finn P. Clausen, Soren B. Petersen, Borge I. F. Alhede
  • Patent number: 5405858
    Abstract: The invention relates to the new furazanylureas of the general formula (I) ##STR1## in which R.sup.1 represents hydrogen or fluorine,R.sup.2 represents hydrogen, fluorine or chlorine,R.sup.3 represents hydrogen, fluorine or chlorine andR.sup.4 represents phenyl which is substituted by trifluoromethyl and additionally monosubstituted to tetrasubstituted by fluorine and/or chlorine, and,in the event that R.sup.1 represents fluorine and/or R.sup.2 and/or R.sup.3 represent fluorine or chlorine, R.sup.4 furthermore also represents difluoromethyl, trifluoromethyl, chlorodifluoromethyl, trifluoroethyl, tetrafluoroethyl, chlorotrifluoroethyl, hexafluoropropyl, hexafluoropropenyl or trifluoromethylphenyl,which can be used as pesticides.
    Type: Grant
    Filed: March 10, 1993
    Date of Patent: April 11, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wilhelm Sirrenberg, Reinhard Lantzsch, Albrecht Marhold, Ulrike Wachendorff-Neumann, Alfred Elbert
  • Patent number: 5403851
    Abstract: This invention relates to novel substituted tryptamine and phenalkylamine and related compounds, pharmaceutical compositions thereof and methods of using said compounds and compositions for a number of pharmaceutical indications including (but not limited to): 1. central nervous system and psychiatric disorders (e.g., sleep disorders, epilepsy and other convulsive disorders, anxiety, psychiatric diseases, neurodegenerative diseases, fever); 2. chronobiological-based disorders (e.g., jet lag, delayed sleep syndrome, shift-work, seasonal affective disorder); 3. endocrine indications (e.g., contraception and infertility, precocious puberty, premenstrual syndrome, hyperprolactinemia, growth hormone deficiency); 4. cancer and other proliferative diseases; 5. immune system disorders and conditions associated with senescence; 6. ophthalmological diseases; 7. animal breeding (e.g., regulation of fertility, puberty, pelage color).
    Type: Grant
    Filed: April 5, 1994
    Date of Patent: April 4, 1995
    Assignee: Interneuron Pharmaceuticals, Inc.
    Inventors: Kay J. D'Orlando, Kenneth W. Locke, Emile M. Bellott, Richard L. Gabriel, Michael D. Nohrden, Yesh P. Sachdeva, Salah A. Zahr, Emile Al-Farhan, Subramaniam Krishnananthan
  • Patent number: 5399569
    Abstract: The present invention relates to 3-(cis-2,6-dimethylpiperidino)sydnone imine salts of the general formula I ##STR1## in which X denotes H.sub.2 PO.sub.4 or ##STR2## processes for their preparation and their use.
    Type: Grant
    Filed: May 10, 1993
    Date of Patent: March 21, 1995
    Assignee: Cassella AG
    Inventors: Karl Schonafinger, Eckard Kujath, Dieter Voegele
  • Patent number: 5389655
    Abstract: The present invention relates to phenylfuroxans of the general formula I ##STR1## in which one of the radicals R.sup.1 and R.sup.2 represents phenyl and the other represents ##STR2## where R.sup.3, R.sup.4 and n are defined as indicated in claim 1, processes for their preparation and their use.
    Type: Grant
    Filed: May 20, 1993
    Date of Patent: February 14, 1995
    Assignee: Cassella AG
    Inventors: Karl Schonafinger, Helmut Bohn
  • Patent number: 5384407
    Abstract: A compound of the formula ##STR1## V, W, Y, and Z are each independently C--H, oxygen, nitrogen, or sulfur; T is C--H or nitrogen;n is 0 or 1;R.sup.4 is hydrogen or one, two or three substituents independently selected from C.sub.1 -C.sub.4 -alkyl, halo-substituted C.sub.1 -C.sub.4 -alkyl, hydroxy-substituted C.sub.1 -C.sub.4 -alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 -alkoxy, mercapto, amino, mono-(C.sub.1 -C.sub.4 -alkyl)amino, di-(C.sub.1 -C.sub.4 -alkyl)amino, formamido, mono-(C.sub.1 -C.sub.4 -alkyl)amido, di-(C.sub.1 -C.sub.4 -alkyl)amido, cyano, nitro, C.sub.1 -C.sub.4 -alkoxycarbonyl, carboxyl, aminomethyl, mono-(C.sub.1 -C.sub.4 -alkyl)aminomethyl, di-(C.sub.1 -C.sub.4 -alkyl)aminomethyl, wherein free hydroxy and amino groups may be protected.
    Type: Grant
    Filed: March 30, 1994
    Date of Patent: January 24, 1995
    Assignee: Warner-Lambert Company
    Inventors: Edgardo Laborde, Mel Schroeder
  • Patent number: 5348968
    Abstract: The invention relates to a compound of formula (I): ##STR1## in which: R.sub.1 represents hydrogen or halogen, alkyl, alkoxy, cyano or aminocarbonyl or any one of the following: ##STR2## in which: m is equal to 1, 2 or 3,n is equal to 0, 1 or 2,T represents a CO or SO.sub.2,R.sub.4 or R.sub.5, which are identical or different, represent hydrogen or alkyl or phenyl,R.sub.2 represents hydrogen or alkyl, phenyl or acyl,R.sub.3 represents hydrogen, alkyl (optionally substituted by hydroxyl or phenyl) or alkoxycarbonyl,--X--Y.dbd. represents --N--C.dbd., --N--N.dbd.or else ##STR3## represents --O--N.dbd.; to its enantiomers, diastereoisomers and epimers and to its addition salts with a pharmaceutically acceptable acid.
    Type: Grant
    Filed: February 1, 1994
    Date of Patent: September 20, 1994
    Assignee: Adir et Compagnie
    Inventors: Gilbert Lavielle, Philippe Maillos, Olivier Muller, Michel Laubie, Tony Verbeuren, Jean-Jacques Descombes
  • Patent number: 5294628
    Abstract: Methyl .alpha.-arylacrylates substituted by a heterocyclic radical and having the general formula ##STR1## where R is alkyl, alkenyl, haloalkyl, cycloalkyl, alkoxy, alkylcarbonyl, alkoxycarbonyl, halogen or aryl, the aromatic ring being unsubstituted or substituted, Het is a five-membered heteroaromatic ring which is unsubstituted or substituted and has from one to three heteroatoms, and A is ethenylene, ethylene, methyleneoxy or methylenethio, and fungicides and pesticides containing these compounds.
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: March 15, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Franz Schuetz, Hans-Juergen Neubauer, Thomas Kuekenhoehner, Ulrich Schirmer, Peter Hofmeister, Christoph Kuenast, Eberhard Ammermann, Gisela Lorenz, Uwe Kardorff
  • Patent number: 5290756
    Abstract: Compounds of the formula: ##STR1## wherein X is hydrogen, halo, trihalomethyl, alkyl, nitroor cyano; X.sup.1 is hydrogen, halo, or trihalomethyl; R.sup.1 and R.sup.2 are hydrogen, alkyl phenyl or benzyl; n is 1 to 5, and Z is halo, cyano, nitro, trihalomethyl, methylthio, methylsulfinyl, methylsulfonyl, acetyl, phenyl, or heterocycle, and compositions containing these compounds exhibit herbicidal activity.
    Type: Grant
    Filed: June 8, 1982
    Date of Patent: March 1, 1994
    Assignee: Rohm and Haas Company
    Inventors: Colin Swithenbank, Ted Fujimoto
  • Patent number: 5281614
    Abstract: Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists.
    Type: Grant
    Filed: November 2, 1992
    Date of Patent: January 25, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Prasun K. Chakravarty, Linda L. Chang, William J. Greenlee, Dooseop Kim, Nathan B. Mantlo, Arthur A. Patchett
  • Patent number: 5271864
    Abstract: Ferroelectric liquid crystal compounds and compositions containing cyclohexenyl derivatives are provided. Specifically provided are compounds of formula: ##STR1## wherein R.sub.1 and R.sub.2 can be an alkyl, cycloalkyl, alkenyl, alkoxy, thioalkyl, alkylsilyl group having from one to about twenty carbon atoms. Y denotes --COO--, --OOC--, --CH.sub.2 O--, or --OCH.sub.2 --; and Ar.sub.1 and Ar.sub.2, independently of one another, can be selected from the group consisting of phenyl rings, halogenated phenyl rings and nitrogen-containing aromatic groups. In preferred embodiments the compounds of this invention contain at least one nitrogen-containing aromatic ring. Ar.sub.1 and Ar.sub.2 can be selected from 1,4-phenyl, mono- or dihalogenated 1,4-phenyl, 2,5-pyridinyl, 2,5-pyrimidyl, 2,5-pyrazinyl, 2,5-thiadiazole, 3,6-pyridazinyl and 1,4-cyclohexyl either or both be chiral racemic groups or chiral nonracemic groups.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: December 21, 1993
    Assignee: Displaytech, Inc.
    Inventors: Michael D. Wand, Rohini T. Vohra, Kundalika M. More, William N. Thurmes
  • Patent number: 5246952
    Abstract: Compounds of formula I ##STR1## wherein Z is thiazolyl or isothiazolyl, and X, R, R.sub.0, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumors.
    Type: Grant
    Filed: September 17, 1991
    Date of Patent: September 21, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Marc Lang
  • Patent number: 5221684
    Abstract: Hydroquinone diethers of the formula I ##STR1## where A.sup.1 and A.sup.2 are substituted or unsubstituted alkylene;R.sup.1 is hydrogen, halogen or alkyl;R.sup.2 is substituted or unsubstituted pyrazolyl or pyridyl;X is a substituted or unsubstituted 5-membered heteroaromatic radical, are prepared as described using the described intermediates, and are used as pesticides.
    Type: Grant
    Filed: October 8, 1991
    Date of Patent: June 22, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Christoph Nuebling, Hans Theobald, Wolfgang Krieg, Uwe Kardorff, Christoph Kuenast
  • Patent number: 5221680
    Abstract: Substituted 3-aminosydnonimines of the formula I ##STR1## and pharmacologically acceptable acid addition salts thereof, in which R.sup.1 denotes hydrogen or the radical --COR.sup.4,R.sup.2 denotes alkyl or phenyl alkyl having 1 to 4 C atoms in the alkyl group,R.sup.4 denotes, for example, an aryl radical, and processes and formulations for controlling or preventing cardiovascular diseases by administering an effective amount of such compounds to a host in need thereof.
    Type: Grant
    Filed: February 27, 1992
    Date of Patent: June 22, 1993
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn
  • Patent number: 5204475
    Abstract: The invention relates to pharmacologically active substituted 3-aminosydnone imines of the general formula I ##STR1## in which n denotes 0 or 1, and their pharmacologically acceptable salts and acid addition salts, and to a process for the preparation of the compounds according to the invention and their use.
    Type: Grant
    Filed: July 16, 1991
    Date of Patent: April 20, 1993
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just
  • Patent number: 5180825
    Abstract: Disclosed in a mitomycin derivative represented by the formula (I): ##STR1## wherein W is a heterocyclic group.
    Type: Grant
    Filed: November 13, 1991
    Date of Patent: January 19, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hitoshi Arai, Motomichi Kono, Masaji Kasai, Katsushige Gomi, Tadashi Ashizawa
  • Patent number: 5166166
    Abstract: The present invention relates to pharmacologically active substituted 3-dicyclohexylaminosydnone imines of the general formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which R.sup.1 denotes hydrogen or the radical --COR.sup.2 and R.sup.2 denotes (C.sub.1 to C.sub.4)-alkyl, (C.sub.1 to C.sub.4)alkoxy-(C.sub.1 to C.sub.4)alkyl, (C.sub.1 to C.sub.4) alkoxy, (C.sub.1 to C.sub.4)alkoxy-(C.sub.1 to C.sub.4 )alkoxy, (C.sub.5 to C.sub.7)cycloalkyl, phenyl, a phenyl radical which is mono-, di- or trisubstituted by 1 to 3 halogen atoms and/or 1 to 3 alkyl radicals having 1 to 4 C atoms and/or 1 to 3 alkoxy radicals having 1 to 4 C atoms, a nicotinoyl radical or an allylmercaptoacetyl radical, and to a process for the preparation of the compounds according to the invention and their use.
    Type: Grant
    Filed: July 16, 1991
    Date of Patent: November 24, 1992
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just
  • Patent number: 5154858
    Abstract: A nonlinear optical compound of the formula: ##STR1## and optionally a .pi. electron conjugated organic compound having an electron donative group and an electron attractive group, which has high conversion efficiency.
    Type: Grant
    Filed: November 20, 1991
    Date of Patent: October 13, 1992
    Assignee: Matsushita Electric Industrial Co., Ltd.
    Inventors: Katsuya Wakita, Nobuo Sonoda, Hisashi Minemoto, Tetsuji Kawakami, Tatsurou Kawamura, Yusuke Ozaki
  • Patent number: 5138064
    Abstract: Novel 3-pyrrolidinylthio-1-azabiycyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof have antimicrobial activity and are useful as medicaments in the treatment of infectious diseases caused by pathogenic microorganisms.
    Type: Grant
    Filed: February 6, 1990
    Date of Patent: August 11, 1992
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Masayoshi Murata, Hideo Tsutsumi, Keiji Matsuda, Kohji Hattori, Takashi Nakajima
  • Patent number: 5120732
    Abstract: Substituted 3-aminosydnone imines of the formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which A denotes, for example, --CH.sub.2 --,R.sup.1 denotes hydrogen or the radical --COR.sup.5,R.sup.2, R.sup.3 denote alkyl having 1 to 4 C atoms,R.sup.5 denotes, for example, an aliphatic radical having 1 to 4 C atoms,and methods for preparing such compounds by cyclization of a compound of the formula II ##STR2## and if desired subsequent acylation. The invention also includes formulations containing effective amounts of such compounds, and methods for administering same to patients for the control and prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: August 29, 1990
    Date of Patent: June 9, 1992
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just
  • Patent number: 5103007
    Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.
    Type: Grant
    Filed: October 27, 1989
    Date of Patent: April 7, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
  • Patent number: 5091398
    Abstract: The 1,2,3,4-oxatriazolium-5-olates of the formula I ##STR1## in which R.sup.1 denotes, for example, (C.sub.2 to C.sub.4)alkyl,R.sup.2 and R.sup.3 denotes (C.sub.1 to C.sub.4)alkyl have useful pharmacological properties.
    Type: Grant
    Filed: April 6, 1990
    Date of Patent: February 25, 1992
    Assignee: Cassella Aktiengellschaft
    Inventors: Karl Schonafinger, Helmut Bohn, Rudi Beyerle, Melitta Just
  • Patent number: 5081245
    Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.
    Type: Grant
    Filed: August 18, 1989
    Date of Patent: January 14, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
  • Patent number: 5079244
    Abstract: Substituted 3-aminosydnone imines of the general formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which A denotes an alkylene chain;X denotes one of the groups --O-- or --S--;R.sup.1 denotes e.g. hydrogen;R.sup.2 denotes e.g. an alkyl group,are prepared by cyclization of a compound of the formula II ##STR2## and, if appropriate, subsequent acylation, and have useful pharmacological properties.
    Type: Grant
    Filed: June 7, 1990
    Date of Patent: January 7, 1992
    Assignee: Cassella Aktiengesellschaft
    Inventors: Eckard Kujath, Christian Baumgartner, SchoKarl, Rudi Beyerle, Melitta Just, Helmut Bohn, Jorg Ostrowski
  • Patent number: 5077401
    Abstract: Herbicidal benzo-fused cyclic compounds of the formula ##STR1## wherein Q is ##STR2## Y is O or S, W is ##STR3## T is O, S, --NH-- or ##STR4## and R.sup.4 may represent, together with T, chlorine,Z is O or S,X is hydrogen or halogen,n is 0 or 1 andR is C.sub.3-6 cycloalkyl, and optionally substituted 5-membered heterocyclic group or an optionally substituted 6-membered heteroaromatic group which contains one to three nitrogen atoms,and salts thereof.
    Type: Grant
    Filed: October 6, 1989
    Date of Patent: December 31, 1991
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Shigeki Yagi, Hiroshi Miyauchi, Katsuhiko Shibuya
  • Patent number: 5051421
    Abstract: Benzo[b]thiophene derivatives of formula ##STR1## their tautomers and salts, in which the index n is 0, 1 or 2, alk is lower alkylene, Ar is phenyl, naphthyl or a monocyclic, five- or six-membered heteroaryl radical, wherein the aromatic radical is unsubstituted or is mono- or poly-substituted by lower alkyl, halo-lower alkyl, halogen and/or by nitro, and the ring A is unsubstituted or is mono- or poly-substituted by lower alkyl, lower alkoxy, lower alkylthio, lower alkanesulfinyl, lower alkanesulfonyl, halo-lower alkyl, halogen and/or by nitro, can be used, for example, as active ingredients in medicaments.
    Type: Grant
    Filed: January 18, 1990
    Date of Patent: September 24, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Pier G. Ferrini
  • Patent number: 5017213
    Abstract: Herbicidal 1-phenylpyrroles of the formula ##STR1## wherein each R.sup.1 represents methyl or together form a tetramethylene group,R.sup.2 represents hydrogen, C.sub.1-6 alkyl, cyclopropylmethyl, C.sub.1-4 alkoxy-C.sub.1-2 alkyl, C.sub.1-4 alkylthio-C.sub.1-2 alkyl, C.sub.1-4 alkylsulfinyl-C.sub.1-2 alkyl, C.sub.1-4 alkylsulfonyl-C.sub.1-2 alkyl, benzyl or phenylethyl which are optionally substituted by halogen, C.sub.3-4 alkenyl, C.sub.3-4 alkynyl, C.sub.3-4 haloalkenyl, C.sub.2-3 cyanoalkyl or carbmoylmethyl, thiocarbamoylmethyl, trimethylsilylmethyl, CH.sub.2 COOR.sup.3, ##STR2## or a C.sub.1-2 alkyl group which is connected with an optionally substituted 5-6 membered heterocyclic group, whereinR.sup.3 represents C.sub.1-6 alkyl or C.sub.5-6 cycloalkyl,R.sup.4 represents hydrogen, methyl, ethyl or cyclopropyl,R.sup.5 represents OR.sup.6 or N(CH.sub.3).sub.2, in whichR.sup.6 represents hydrogen, C.sub.1-5 alkyl, allyl, propargyl or benzyl, andn represents 0 to 1.
    Type: Grant
    Filed: July 7, 1989
    Date of Patent: May 21, 1991
    Assignee: Nihon Tokushu Noyaku Seizo K. K.
    Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Hiroshi Miyauchi, Tadao Asami
  • Patent number: 5007952
    Abstract: Herbicidally active pyrroles of the formula ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl, or one R.sup.1 together with the other R.sup.1 forms tetramethylene or butenylene,X represents hydrogen or halogen,Y represents O or S,n represents 0 or 1,R.sup.2 represents hydrogen or an organic radical.
    Type: Grant
    Filed: November 9, 1989
    Date of Patent: April 16, 1991
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Hiroshi Miyauchi, Tadao Asami