Chalcogen Attached Indirectly To Pyridine Or Partially Hydrogenated Pyridine Ring By Nonionic Bonding Patents (Class 546/266)
  • Patent number: 6127529
    Abstract: Bifuncitonal chelating pyridine compound and its use for conferring chelating properties on organic compounds. The pyridine compound has the structure ##STR1## where (i) n is an integer 1 or 2,(ii) R.sub.1, R.sub.2 and R.sub.3 represent groups that have no electrons capable of significantly delocalizing or resonating with the pyridine ring, such as hydrogen, alkyl or aralkyl having an aliphatic carbon atom next to the pyridine ring; at least two of R.sub.1, R.sub.2 and R.sub.
    Type: Grant
    Filed: September 13, 1991
    Date of Patent: October 3, 2000
    Assignee: Wallac Oy
    Inventors: Marek Kwiatkowski, Christian Sund, Jyrki Ylikoski, Veli-Matti Mukkala, Ilkka Hemmila
  • Patent number: 6090808
    Abstract: This subject invention relates to dimeric 4-phenylpiperidine, 4-phenyl-1,2,3,6-tetrahydropyridine, or 4-phenylpiperazine compounds or dimeric spirocyclic piperidine compounds having general formula (I), ##STR1## wherein n is 1-5; R.sup.1 to R.sup.4 are substituents; R.sup.5 and R.sup.6 each hydrogen or alkyl or form together an ethylene or propylene bridge; X is O, S, SO, SO.sub.2, CO or (CH.sub.2).sub.m, m being 0 or 1, X is NR.sup.7, R.sup.7 being H, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, or phenylalkyl, or X is CR.sup.8-- R.sup.9, wherein R.sup.8 and R.sup.9 are selected from hydroxy and the substituents defined under R.sup.7 ; and (i) Z.sup.1 is a substituent and Z.sup.2 is (CH.sub.2).sub.p wherein p is 0; and Y is N, C or CH; (ii) Z.sup.1 and Y are linked together via a single bond, thereby forming a spirocyclic junction; in which case Y is C; Z.sup.1 is O, S, (CH.sub.2).sub.q, q being 1, 2 or 3, or Z.sup.1 is CH.sub.2 O, CH.sub.2 S, CH.sub.2 CH.sub.2 O, CH.sub.2 CH.sub.2 S, CH.dbd.CH, CH.dbd.CHCH.
    Type: Grant
    Filed: May 6, 1998
    Date of Patent: July 18, 2000
    Assignee: H. Lundbeck A/S
    Inventors: Jens Perregaard, John W. Stenberg, Ejner K. Moltzen
  • Patent number: 6013802
    Abstract: The present invention describes a family of fluorescent indicators for metal cations. The indicators are fluorophore conjugates of pyridyl-based metal ion chelators. The indicators are very sensitive detection as quantification reagents for a variety of metals, in a variety of oxidation states, even in the presence of high concentrations of Ca.sup.2+, Na.sup.+, or K.sup.+ or other ions, such as is found in seawater, making them highly useful for assaying physiological samples, biological samples, or environmental samples.
    Type: Grant
    Filed: February 7, 1997
    Date of Patent: January 11, 2000
    Assignee: Molecular Probes, Inc.
    Inventors: Brian Matthew Hoyland, Michael A. Kuhn, Richard P. Haugland
  • Patent number: 5962479
    Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: October 5, 1999
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng Liang Chen
  • Patent number: 5958983
    Abstract: The present invention relates to polyaromatic compounds having useful antiviral activity against viruses of the herpes family, to a composition containing them, and to a method of using them for the treatment of herpes viruses infections.
    Type: Grant
    Filed: April 1, 1998
    Date of Patent: September 28, 1999
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael R. Barbachyn, Fred L. Homa, Antonio Monge, Esteban Santiago, Juan J. Martinez-Irujo, Maria Font
  • Patent number: 5925653
    Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH or S(O).sub.q where q=0, 1 of 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: July 20, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Rainer Preuss, Wolfgang Schaper, Martin Markl, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
  • Patent number: 5912350
    Abstract: Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents;G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent;R is hydrogen or an alkyl group;R.sub.1, X, Y, Z and T are organic or inorganic substituents; andR.sub.2 and R.sub.3 represent hydrogen or organic substituents; orNR.sub.2 R.sub.3 together represents a heterocyclic ring system;and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: June 15, 1999
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 5908931
    Abstract: The present invention relates particularly to novel preorganized hexadentate ligands that are suitable for completing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.
    Type: Grant
    Filed: December 14, 1990
    Date of Patent: June 1, 1999
    Assignee: Mallinckrodt Inc.
    Inventors: Raghavan Rajagopalan, William L. Neumann, Dennis L. Nosco
  • Patent number: 5861407
    Abstract: A class of substituted 1,2,3,6-tetrahydropyridine derivatives are disclosed that are ligands for dopamine receptor subtypes within the body. These compounds are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.
    Type: Grant
    Filed: February 21, 1997
    Date of Patent: January 19, 1999
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Ian Michael Mawer, Mark Peter Ridgill
  • Patent number: 5847218
    Abstract: The invention provides a novel sulfonium salt having a substituted or unsubstituted arylsulfonate anion. The novel sulfonium salt minimizes the influence of deactivation by basic compounds not only at a resist surface, but also at a resist-substrate interface, assists a resist to be configured to a definite pattern profile. When the sulfonium salt has an acid labile group, it is effective for increasing the dissolution contrast between exposed and unexposed areas. The sulfonium salt is useful in a chemically amplified positive resist composition which lends itself to fine patterning and features high resolution.
    Type: Grant
    Filed: March 4, 1997
    Date of Patent: December 8, 1998
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Youichi Ohsawa, Satoshi Watanabe, Junji Shimada, Katsuya Takemura, Shigehiro Nagura, Toshinobu Ishihara
  • Patent number: 5814645
    Abstract: The present invention pertains to new substituted nitrogen heterocycles of general formula (I) ##STR1## in which R.sup.1 and R.sup.2 independently of each other, stand for hydrogen or alkyl,X stands for oxygen, sulfur or an NR.sup.3 group,Y stands for carbon (C or CH) or nitrogen,Z stands for an electron-attracting group,T stands for the remainder of an unsaturated ring system broken possibly by other heteroatoms or heteroatom groups,Q stands for possibly substituted aryl or possibly substituted hetaryl, wherein R.sup.3 stands for hydrogen, alkyl or alkenyl, method for preparing them and their use as pesticides.
    Type: Grant
    Filed: August 18, 1997
    Date of Patent: September 29, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Johannes Kanellakopulos, Rainer Fuchs, Johannes Rudolf Jansen, Michael Schindler, Christoph Erdelen, Wolfgang Leicht, Ulrike Wachendorff-Neumann, Andreas Turberg
  • Patent number: 5739340
    Abstract: The invention relates to indolizine derivatives of general formula: ##STR1## in which: X denotes an --S or --SO.sub.2 -- group,each of R.sub.1 and R.sub.2, which are identical or different, denotes hydrogen, the methyl or ethyl radical or a halogen atom,R.sub.3 denotes hydrogen or a C.sub.1 -C.sub.4 alkyl radical,R.sub.4 denotes a precursor radical of a carboxyl group,R denotes a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or phenyl radical, and their use as intermediates for the preparation of pharmaceutically active aminoalkoxybenzenesulphonylindolizine derivatives.
    Type: Grant
    Filed: April 2, 1997
    Date of Patent: April 14, 1998
    Assignee: Elf Sanofi
    Inventors: Jean Gubin, Michel Renard
  • Patent number: 5714488
    Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein W is selected from the group consisting of optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are one or more groups independently selected from hydrogen, alkyl, halolalkyl, alkoxy, and halogen; Z is selected from the group consisting of N--OH, N--O--A--COM, CH--COM, and CH--CH.dbd.N--0--A--COM wherein A is selected from the group consisting of alkylene, alkenylene, cycloalkylene, and optionally substituted alkylphenyl wherein the alkyl portion is of one to six carbon atoms, and M is selected from the group consisting of a pharmaceutically acceptable, metabolically clearable group, --OR.sup.3, and --NR.sup.4 R.sup.
    Type: Grant
    Filed: September 17, 1996
    Date of Patent: February 3, 1998
    Assignee: Abbott Laboratories
    Inventors: Clint D. W. Brooks, Pramila Bhatia, Teodozyj Kolasa
  • Patent number: 5710170
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV). ##STR1## The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.
    Type: Grant
    Filed: December 10, 1996
    Date of Patent: January 20, 1998
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Daniel Guay, Yves Girard, Yves Ducharme, Marc Blouin, Pierre Hamel, Mario Girard
  • Patent number: 5710160
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV). ##STR1## The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.
    Type: Grant
    Filed: December 10, 1996
    Date of Patent: January 20, 1998
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Daniel Guay, Yves Girard, Yves Ducharme
  • Patent number: 5677454
    Abstract: Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents;G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent;R is hydrogen or an alkyl group;R.sub.1, X, Y, Z and T are organic or inorganic substituents; andR.sub.2 and R.sub.3 represent hydrogen or organic substituents; orNR.sub.2 R.sub.3 together represents a heterocyclic ring system;and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: October 14, 1997
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 5622977
    Abstract: Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is a substituted or unsubstituted alkyl; X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is hydrogen or alkyl; R.sup.2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 and R.sup.5, which may be the same or different, are each --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R.sup.6 is hydrogen or substituted or unsubstituted alkyl; R.sup.7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 22, 1997
    Assignee: Celltech Therapeutics Limited
    Inventors: Graham J. Warrellow, Ewan C. Boyd, Rikki P. Alexander, John C. Head
  • Patent number: 5618821
    Abstract: Compounds of the formula ##STR1## wherein Q is chosen from the group consisting of pyridyl, pyrazyl, pyrimidyl, quinolyl, indolyl and 7-azaindolyl or any of these substituted with one or two substituents;Y is an alkylene bridge of 3-9 carbon atoms;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.3 is alkoxycarbonyl, alkyltetrazolyl, substituted or unsubstituted phenyl or heterocyclyl, the N-oxide thereof, or a pharmaceutically acceptable acid addition salt thereof is an effective antipicornaviral agent.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: April 8, 1997
    Assignee: Sanofi, S.A.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz
  • Patent number: 5614634
    Abstract: Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,B means an alkylene group with 1-3 C atoms in the chain, a radical ##STR2## or a radical ##STR3## with R.sup.3 meaning a hydrogen atom, a carboxy or methoxycarbonyl group, A means groups ##STR4## --NH--CO--, --CO--NH--, --OCH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --COCH.sub.2 -- or --CHOH--CH.sub.2 --,X means N or CH,D means groups or ##STR5## and . . . . . means a single or double bond, as well as optionally their salts with physiologically harmless bases, process for their production and their pharmaceutical use.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: March 25, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5595958
    Abstract: Herbicidal 3-substituted pyridine compounds and derivatives thereof of the formula: ##STR1## wherein Ar is a substituted or unsubstituted 5- or 6-membered heteroaryl group having 1, 2 or 3 ring nitrogen atoms with the remainder of the ring atoms being carbon; a substituted or unsubstituted 5-membered heteroaryl group having a ring heteroatom of oxygen or sulfur with the remainder of the ring atoms being carbon; or a substituted or unsubstituted 5-membered heteroaryl group having one ring nitrogen atom and either an oxygen or sulfur ring heteroatom with the remainder of the ring atoms being carbon. Herbicidal compositions containing such 3-substituted pyridine compounds and derivatives thereof and methods of controlling undesirable vegetation employing these compounds and derivatives are also disclosed. The compounds in which XR is hydroxyl are also useful as intermediates for producing the disclosed 3-substituted pyridine derivatives.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: January 21, 1997
    Assignee: Zeneca Limited
    Inventors: Hsiao-Ling M. Chin, Nhan H. Nguyen, David B. Kanne, David L. Lee
  • Patent number: 5585327
    Abstract: 4-substituted pyridyl-3-carbinols of the formula ##STR1## wherein R is hydrogen, or an acyl, alkyl or carbamyl group exhibit desirable preemergent and postemergent herbicidal activity. Also disclosed are herbicidal compositions comprising such compounds and methods of controlling undesirable vegetation employing such compounds. The compounds wherein AR is hydroxyl serve as useful intermediates for the production of the alpha-benzyl substituted compounds as well as exhibiting herbicidal activity.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: December 17, 1996
    Assignee: Zeneca Limited
    Inventors: Hsiao-Ling Chin, Yi-Qiu Wei, Nhan H. Nguyen, Michael P. Ensminger, Linda Willitts, Derek P. Dagarin
  • Patent number: 5580888
    Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, wherein R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.6)--, where R.sup.6 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a group --(CH.sup.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1, 2 or 3; R.sup.5 is a hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 3, 1996
    Assignee: Celltech Therapeutics Limited
    Inventors: Graham J. Warrellow, Ewan C. Boyd, Rikki P. Alexander
  • Patent number: 5576443
    Abstract: Disclosed is a novel near-infrared absorbing dye of formula: ##STR1## wherein X.sup.1, X.sup.2 independently represents --CR.sup.8 R.sup.9 --, --S--, --Se--, --NR.sup.10 --, --CH.dbd.CH-- or --O--;n is an integer of 2 or 3;R.sup.1 and R.sup.2 independently represent alkyl of 1 to 10 carbons or substituted alkyl of 1 to 10 carbons;R.sup.3 represents a ring chosen from a set consisting of aryl, substituted aryl, and a heterocyclic ring of a type present in photographic emulsions;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl of 1-10 carbons, substituted alkyl of 1-10 carbons, R.sup.4 and R.sup.5 taken together or R.sup.6 and R.sup.7 taken together can represent atoms necessary to form a 5 or 6-membered aliphatic ring, an aromatic six-membered ring, an aromatic 10-membered ring, a substituted aromatic six-member ring or a substituted aromatic 10-member ring;R.sup.8, R.sup.
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: November 19, 1996
    Assignee: Sterling Diagnostic Imaging, Inc.
    Inventors: Dietrich M. Fabricius, Gregory C. Weed
  • Patent number: 5541213
    Abstract: A novel propenoic acid derivative which exhibits adenosine A1 antagonism is defined by the general formula (I): ##STR1## (wherein A represents an aromatic ring; R.sup.1 represents aryl or the like; R.sup.2, R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like; and R.sup.7 and R.sup.8 each represent lower alkyl or the like) or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: June 10, 1994
    Date of Patent: July 30, 1996
    Assignee: Eisai Co., Ltd.
    Inventors: Masayuki Matsukura, Keizoh Satoh, Naoki Yoneda, Makoto Kaino, Kazutoshi Miyake, Yoshiharu Daiku, Naoya Kishi, Fusayo Yoshida, Kenichi Nomoto, Toshiaki Ogawa, Tadanobu Takamura, Koichi Nose, Mikio Tomimatsu, Masanori Mizuno, Shigeto Negi, Shigeru Souda
  • Patent number: 5506227
    Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. 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.
    Type: Grant
    Filed: April 13, 1992
    Date of Patent: April 9, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
  • Patent number: 5466698
    Abstract: Substituted tetrahydropyridines and hydroxypiperidines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: November 14, 1995
    Assignee: Warner-Lambert Company
    Inventors: Shelly Glase, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
  • Patent number: 5457118
    Type: Grant
    Filed: April 20, 1994
    Date of Patent: October 10, 1995
    Assignee: Pfizer Inc.
    Inventors: Roger P. Dickinson, Kevin N. Dack, John Steele
  • Patent number: 5443820
    Abstract: Esters and amides of aminomethylenecyanoacetic acid I ##STR1## where R.sup.1 and R.sup.2 are each, independently of one another, phenyl, naphthyl, biphenylyl or five- or six-membered hetaryl with one, two or three nitrogens or one oxygen or one sulfur or one nitrogen and one oxygen or one nitrogen and one sulfur, which can be benzo-fused, it being possible for these radicals to be substituted by one to three C.sub.1 -C.sub.12 -alkyl groups, C.sub.1 -C.sub.12 -alkoxy groups, halogen atoms, cyano groups, hydroxyl groups or groups of the formulae COOR.sup.3, COR.sup.3, CONHR.sup.3, OCOR.sup.3 or NHCOR.sup.3, and whereR.sup.3 is C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.8 -cycloalkyl or phenyl,X is C.sub.2 -C.sub.30 -alkylene which can be interrupted by non-adjacent oxygens, or is C.sub.4 -C.sub.12 -alkenylene or C.sub.4 -C.sub.12 -alkynylene where the unsaturated bonds are not adjacent to the ester oxygens, or is C.sub.5 -C.sub.8 -cycloalkylene or phenylene, andY is O or NH.
    Type: Grant
    Filed: January 5, 1994
    Date of Patent: August 22, 1995
    Assignee: Basf Aktiengesellschaft
    Inventors: Martin Holderbaum, Alexander Aumueller, Hubert Trauth
  • Patent number: 5414003
    Abstract: Pyridinylmethyl-substituted pyridines and pyridones are prepared by reacting pyridine- or pyridone-substituted halogenopyridines with tetrazolylphenylboronic acids. The substances according to the invention can be used as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: May 9, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Peter Fey, Jurgen Dressel, Rudolf Hanko, Walter Hubsch, Thomas Kramer, Ulrich Muller, Matthias Muller-Gliemann, Martin Beuck, Hilmar Bischoff, Stefan Wohlfeil, Dirk Denzer, Stanislav Kazda, Johannes-Peter Stasch, Andreas Knorr, Siegfried Zaiss
  • Patent number: 5412114
    Abstract: The present invention relates to an improvement in the process for preparing a calixarene derivative in which the rotation of its benzene units are hindered and which comprises replacing all or a part of the hydrogen atoms of the hydroxyl groups of a calixarene derivative represented by the general formula: ##STR1## and is characterized by conducting the reaction in the presence of an alkaline earth metal. According to the present invention, an asymmetric calixarene derivative having a "cone" conformation can be selectively prepared by virtue of the template effect of the metal.
    Type: Grant
    Filed: February 9, 1993
    Date of Patent: May 2, 1995
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Seiji Shinkai, Tsutomu Matsuda, Takashi Arimura, Hirosuke Kawabata, Kozo Tachibana
  • Patent number: 5281606
    Abstract: New N-substituted 4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridines useful in the treatment of intestinal motility disorders, of the following general formula ##STR1## wherein A represents a group --E--G or --L--M, where --E-- is a straight or branched alkylene radical of from 2 to 4 carbon atoms,--G represents a radical selected from the group consisting of naphthyl mono-substituted with hydroxy or (C.sub.1 -C.sub.4)alkoxy; naphthyl di-substituted with hydroxy, (C.sub.1 -C.sub.4)alkoxy or (C.sub.1 -C.sub.4)alkyl; or naphthyl substituted with methylenedioxy,--L-- is a --Q--CH(OH)-- group wherein --Q-- is a straight or branched alkylene radical of from 1 to 3 carbon atoms, and--M represents a radical selected from the group consisting of naphthyl; naphthyl mono- or di-substituted with hydroxy, (C.sub.1 -C.sub.4)alkoxy or (C.sub.1 -C.sub.4)alkyl or naphthyl substituted with methylenedioxy; pyridyl; or (C.sub.1 -C.sub.4)alkyl-pyridyl,and their salts with mineral or organic acids.
    Type: Grant
    Filed: May 23, 1991
    Date of Patent: January 25, 1994
    Assignee: Sanofi
    Inventors: Umberto Guzzi, Costantino Palmieri, Tiziano Croci
  • Patent number: 5225561
    Abstract: Metal organic chemical vapor deposition (MOCVD) formation of copper oxide superconductor materials. Various source reagents of Group II elements suitable for high temperature superconductor (HTSC) material formation are described, including beta-diketonates, cyclopentadienyls, alkyls, perfluoroalkyls, alkoxides, perfluoroalkoxides, and Schiff bases, as well as complexes of such Group II compounds, utilizing monodentate or multidentate ligands to provide additional coordination to the Group IIA atom, so that the resulting complex is of enhanced volatility characteristics, and enhanced suitability for MOCVD applications. Also disclosed are methods of synthesizing such compounds and complexes, including a method of making Group II metal beta-diketonate compounds having enhanced thermal stability characteristics. Further disclosed are a vertical inverted reactor for chemical vapor deposition, and various methods of processing applied metal oxide films for enhanced HTSC character.
    Type: Grant
    Filed: September 12, 1990
    Date of Patent: July 6, 1993
    Assignee: Advanced Technology Materials, Inc.
    Inventors: Peter S. Kirlin, Duncan W. Brown, Robin A. Gardiner
  • Patent number: 5198443
    Abstract: Substituted 1,2,3,6-tetrahydropyridines are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: March 17, 1992
    Date of Patent: March 30, 1993
    Assignee: Warner-Lambert Company
    Inventors: Bradley W. Caprathe, Juan C. Jaen, Lawrence D. Wise
  • Patent number: 5175167
    Abstract: Hetarylalkenes of the general formula I ##STR1## where Ar is hetaryl,A is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.3 -alkyl or unsubstituted or monosubstituted, disubstituted or trisubstituted aryl or aralkyl, ##STR2## Z is whereR is hydrogen, C.sub.2 -C.sub.4 -acyl, unsubstituted or substituted benzoyl, C.sub.1 -C.sub.4 -alkylsulfonyl, unsubstituted or C.sub.1 -C.sub.4 -alkyl-substituted phenylsulfonyl or a radical R.sup.1,R.sup.1 is C.sub.1 -C.sub.4 -alkyl or unsubstituted or substituted phenyl or benzyland Hal is fluorine, chlorine, bromine or iodine,and B is unsubstituted or substituted mononuclear or dinuclear aryl, aralkyl or hetaryl,and their N-oxides and addition salts, the preparation of these substances, intermediates for this purpose and the preparation thereof, fungicides containing hetarylalkenes and a corresponding method for controlling harmful fungi.
    Type: Grant
    Filed: February 8, 1991
    Date of Patent: December 29, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernhard Zipperer, Manfred Lauer, Norbert Goetz, Thomas Zierke, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5153306
    Abstract: New and useful aromatic polyethers, which are high in glass transition temperatures, possess excellent mechanical properties, thermal resistance, solvent resistance, and generate fluorescence, are described. Also described are fluorescent resin compositions containing the aromatic polyethers. Processes for preparing the aromatic polyethers and the fluorescent resin compositions are also described.
    Type: Grant
    Filed: April 7, 1989
    Date of Patent: October 6, 1992
    Assignee: Idemitsu Kosan Company Limited
    Inventors: Shigeru Matsuo, Naoto Yakoh, Shinji Chino
  • Patent number: 5151436
    Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Het represents pyrid-3-yl, isoquinolin-4-yl, tetrahydroquinolin-3-yl, quinolin-3-yl, pyridazin-4-yl, pyrimid-5-yl, thiazol-5-yl, thieno[2,3-b]-pyridin-5-yl, pyrazin-2-yl, indol-3-yl and thieno[3,2-b]-pyridin-6-yl, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl, or two R.sup.1 substituents on the same nitrogen atom may together form an optionally substituted alkylene radical chain and salts thereof, processes for their preparation and compositions containing them are described.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: September 29, 1992
    Assignee: Rhone-Poulenc Sante
    Inventors: David C. Cook, Terance W. Hart, Iain M. Mc Lay, Malcolm N. Palfreyman, Brian W. Sharp, Roger J. A. Walsh
  • Patent number: 5130435
    Abstract: Vinyl ethers of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are identical to or different from one another, each being hydrogen, straight-chain or branched alkyl or alkenyl of up to 12 carbon atoms, cycloalkyl or cycloalkylene of from 5 to 8 carbon atoms, aryl, alkylaryl, alkenylaryl, aralkyl and aralkenyl of from 6 to 16 carbon atoms, halogen-substituted aryl or heterocyclyl, and in addition the radicals R.sup.1 and R.sup.2 or R.sup.1 and R.sup.3, together with the carbon atom to which they are bonded, can form a cycloalkane, cycloalkene or a heterocycle, and R.sup.4 is alkyl, alkylaryl or aralkyl, are prepared by eliminating an alcohol from an acetal/ketal of the formula ##STR2## where R.sup.1, R.sup.2, R.sup.3 and R.sup.
    Type: Grant
    Filed: August 9, 1990
    Date of Patent: July 14, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Hoelderich, Norbert Goetz, Leopold Hupfer
  • Patent number: 5120748
    Abstract: Substituted 1,2,3,6-tetrahydropyridines are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: June 28, 1991
    Date of Patent: June 9, 1992
    Assignee: Warner-Lambert Company
    Inventors: Bradley W. Caprathe, Juan C. Jaen, Lawrence D. Wise
  • Patent number: 5116990
    Abstract: There are provided 1H-pyrazolo[1,5-b]-1,2,4-triazole magenta couplers or 1H-pyrazolo[5,1-c]-1,2,4-triazole magenta couplers characterized by having at the 6-position a phenoxy group, on the ortho-position of which is an alkoxy group or an aryloxy group. A photographic material comprising the magenta coupler is excellent in color reproducibility and exhibits superior photographic characteristics in any of sensitivity, gradation, and color density.
    Type: Grant
    Filed: August 2, 1990
    Date of Patent: May 26, 1992
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keizo Kimura, Tadahisa Sato
  • Patent number: 5112386
    Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur, A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 --S(O).sub.n R.sup.3 groups; any two of the groups, A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.
    Type: Grant
    Filed: December 30, 1988
    Date of Patent: May 12, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Anthony Vivienne, John M. Clough, Paul deFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
  • Patent number: 5100460
    Abstract: Herbicides of formula: ##STR1## in which: n=0,1, 2f=0,1A is chosen from the groups ##STR2## in which: Ar is chosen from the groups ##STR3## B is chosen from optionally substituted C.sub.1 -C.sub.10 alkyl and C.sub.3 -C.sub.
    Type: Grant
    Filed: July 13, 1989
    Date of Patent: March 31, 1992
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Philippe Desbordes, Michel Euvrard
  • Patent number: 5079361
    Abstract: Cross-linking reagents which are highly specific for sulphydryl groups and react with thiols at an excellent rate. The essential feature of the reagents is at least one vinyl group conjugated with an armoatic nitrogen heterocycle. Particular examples include vinyl pyridines, vinyl pyrimidines and vinyl triazines.
    Type: Grant
    Filed: September 9, 1988
    Date of Patent: January 7, 1992
    Assignee: Celltech Limited
    Inventors: Rikki P. Alexander, Michael A. W. Eaton, Thomas A. Millican, Richard C. D. Titmas
  • Patent number: 5071860
    Abstract: Insecticidally active substituted heteroaryl phenyl ethers of the formula ##STR1## in which Het represents an optionally substituted heteroaromatic radical,X represents O, S, --CH.sub.2 --, --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.sub.2 --O--, ##STR2## Y represents O, --O--CH.sub.2 -- or S, Z represents an optionally substituted aromatic or heteroaromatic radical;m represents integers from 1-4n represents 0, 1, 2, 3, 4O represents 0, 1, 2, 3, 4, provided than n and o do not simultaneously represent 0p represents integers from 1-4,R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another represent hydrogen, C.sub.1 -C.sub.6 -alkyl which is optionally substituted; two radicals adjacent to one another can also, together with the C atoms to which they are bonded, form a saturated carbocyclic 5- or 6-ring,R.sup.1 represents identical or different radicals hydrogen, halogen, CN, C.sub.1-4 -alkyl, 1-5-halogeno-C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, 1-5-halogeno-C.sub.
    Type: Grant
    Filed: March 7, 1990
    Date of Patent: December 10, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Alig, Wilhelm Stendel, Michael Londershausen
  • Patent number: 5064842
    Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein:.alpha. and .beta. together represent a bond and additionally when B is an electron withdrawing group .alpha. can also represent OH and .beta. can represent hydrogen;Ar is an optionally substituted aryl or heteroaryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optioanlly substituted aryl or heteroaryl;A represents a group of formula --XR.sup.3 wherein X is a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q -- in which formula: Y represents --O--, --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 R.sup.6, R.sup.7 and R.sup.
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: November 12, 1991
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, Terence J. Ward, Albert Opalko
  • Patent number: 5032312
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 denotes a group R.sup.3 or R.sup.3 --A.sup.4 --Z.sup.3 -- and R.sup.2 denotes a group R.sup.4 or --Z.sup.4 --A.sup.5 --R.sup.4 ; m and n each individually stand for the number 0 or 1; A.sup.1, A.sup.2, A.sup.3, A.sup.4 and A.sup.5 each independently represent unsubstituted or halogen-, cyano- and/or methyl-substituted 1,4-phenylene in which optionally 1 CH group or 2 CH groups is/are replaced by nitrogen, trans-1,4-cyclohexylene in which optionally 2 non-adjacent methylene groups are replaced by oxygen and/or sulphur, 1-cyano-trans-1,4-cyclohexylene, bicyclo[2.2.2]octane-1,4-diyl, naphthalene-2,6-diyl, tetralin-2,6-diyl or trans-decalin-2,6-diyl; Z.sup.1, Z.sup.2, Z.sup.3 and Z.sup.4 each independently signify a single covalent bond, --COO--, --OOC--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2, --C.tbd.C--, --(CH.sub.2).sub.3 O--, --O(CH.sub.2).sub.3 -- or the trans form of --CH.dbd.CH--CH.sub.2 O-- or --OCH.sub.2 --CH.dbd.CH--; R.sup.3 and R.sup.
    Type: Grant
    Filed: March 2, 1990
    Date of Patent: July 16, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Stephen Kelly
  • Patent number: 5002957
    Abstract: Azaneophyl and silazaneophyl sulfides, processes for their preparation, agents containing them, and their use as pesticides.Compounds of the formula I, their optical isomers and mixtures thereof ##STR1## where M denotes C or Si,R.sup.1 denotes unsubstituted or substituted pyridyl, unsubstituted or substituted pyrimidyl, andwhen M=C- denotes unsubstituted or substituted pyridazinyl, unsubstituted or substituted pyrazinyl, unsubstituted or substituted 1,2,4-triazinyl, unsubstituted or substituted 1,2,4,5-tetrazinyl,R.sup.2, R.sup.3 independently or one another denote alkyl, alkenyl, haloalkyl, phenyl, or R.sup.2 and R.sup.3 denote an alkylene chain which - together with the quaternary central atom (M) - form an unsubstituted or fluorine-substituted ring having four to six ring members (when M=Si) or having three to six ring members (when M=C),R.sup.4 denotes H, F, --CN, --CCl.sub.3, --C.dbd.CH, (C.sub.1 -C.sub.4)alkyl, ##STR2## R.sup.
    Type: Grant
    Filed: March 23, 1989
    Date of Patent: March 26, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans H. Schubert, Gerhard Salbeck, Hans-Peter Krause, Werner Knauf, Anna Waltersdorfer, Manfred Kern
  • Patent number: 4997842
    Abstract: The present invention relates to the + or - pirmenol stereoisomers and to selected metabolites of pirmenol or (+,-)-cis-.alpha.-[3-(2,6-dimethyl-1-piperidinyl))propyl]-.alpha.-phenyl-2 -pyridinemethanol which are active as antiarrhythmic agents. The pharmacological use of the metabolites that is the present invention is as antiarrhythmic agents. Pharmaceutical compositions comprising the metabolites are also within the scope of the invention.
    Type: Grant
    Filed: February 8, 1990
    Date of Patent: March 5, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Timothy R. Hurley, Dino A. Sherwood, Peter W. K. Woo, Karl-Otto Vollmer, Egmont Schaller, Wolfgang Klemisch, Albrecht V. Hodenberg
  • Patent number: 4968341
    Abstract: Novel substituted aryloxyureas, processes for their production, and herbicides comprising them as active ingredients are provided.The substituted aryloxyureas exhibit an excellent herbicidal efficacy against weeds when applied, for example, to the weeds in a wide range of period from a preemergence stage to a growth stage.The substituted aryloxyureas of the invention have the excellent advantage of maintaining high safety on crops or crop plants in spite of their herbicidal efficacy.
    Type: Grant
    Filed: August 16, 1988
    Date of Patent: November 6, 1990
    Assignees: Kumiai Chemical Industry Co., Mitsui Petrochemical Industries, Ltd.
    Inventors: Isao Hashimoto, Tatsuyodihi Ishida, Kazutaka Tsuru, Yuji Yamada, Takeshige Miyazawa, Yasuo Nakamura, Susumu Katou, Katsuya Takahashi
  • Patent number: 4966902
    Abstract: Compounds of the formula (I) and their stereoisomers ##STR1## wherein A, B, C' and D independently of one another denote CH or N, in which at least one of the symbols A, B, C' or D must correspond to a nitrogen atom,X denotes CH.sub.2 or oxygen,R.sup.1 denotes a radical bonded to a carbon atom from the series comprising H, trialkylsilyl, halogen, nitro, cyano, alkenyl, alkynyl, amino, cycloalkyl, phenyl, phenxy, alkoxy, alkenyloxy, alkynyloxy, hydroxycarbonyl, alkylthio, cycloalkyloxy, alkylcarbonyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxy, halogenoalkylthio, halogenoalkoxyalkyl, alkylthioalkyl, alkoxyalkoxy, halogenoalkoxyalkoxy, alkenyloxyalkoxy, halogenoalkenyloxy, alkoxyalkylthio, alkylthioalkoxy, alkylthioalkylthio, halogenoalkoxycarbonyl, halogenoalkenyloxycarbonyl or dialkylamino or two radicals R.sup.1 when they are positioned ortho to one another together denote a methylenedioxy, ethylenedioxy or alkylene radical,R.sup.2 and R.sup.
    Type: Grant
    Filed: April 13, 1988
    Date of Patent: October 30, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans H. Schubert, Gerhard Salbeck, Hans-Peter Krause, Walter Luders, Werner Knauf, Anna Waltersdorfer, Manfred Kern
  • Patent number: 4948912
    Abstract: The present invention comprises a haloacetoxyalkyl ether having the formula: ##STR1## wherein R is H or a C.sub.1 -C.sub.4 substituted or unsubstituted alkyl group, R' is H or a C.sub.1 -C.sub.3 group, and X is chlorine or fluorine; aroyloxymethyl ethers having the formula:R--COOCH.sub.2 --O--CH.sub.2 --OOC--Rwherein the R is p-NO.sub.2 C.sub.6 H.sub.4, halogen substituted C.sub.6 H.sub.4, or other aromatics; the method of making such ethers and monoquaternary salts; and the method of alkylating amines, pyridines, or acetals or pyridine derivatives with such ethers to form quaternary ammonium salts; particularly HI-6, HGG-12, Toxogonin, and SAS-128.
    Type: Grant
    Filed: September 8, 1986
    Date of Patent: August 14, 1990
    Assignee: Southwest Research Institute
    Inventors: Robert E. Lyle, Jr., Donald J. Mangold, Nollie F. Swynnerton