Benzene Ring Bonded Directly To The Five-membered Hetero Ring Patents (Class 548/577)
  • Publication number: 20020137934
    Abstract: A new ligands that include a benzene ring in the backbone can be combined with a metal or metal precursor compound or formed into a metal-ligand complex catalyze a number of different chemical transformations, including olefin polymerization reactions. The ligands, complexes formed with the ligands and compositions including the ligands are useful catalysts, depending on the reaction.
    Type: Application
    Filed: September 18, 2001
    Publication date: September 26, 2002
    Applicant: Symyx Technologies
    Inventors: Anil Guram, Cheryl Lund, Howard W. Turner, Tetsuo Uno
  • Publication number: 20020120153
    Abstract: A method of producing a compound of the formula: 1
    Type: Application
    Filed: February 15, 2001
    Publication date: August 29, 2002
    Inventor: M. Mahmun Hossain
  • Publication number: 20020111367
    Abstract: The present invention is a series of compounds formed from phenyl substituted pyridine or benzene derivatives and their pharmaceutically acceptable salts. These compounds have shown high affinity as antagonists to the NK-1 receptor.
    Type: Application
    Filed: January 17, 2002
    Publication date: August 15, 2002
    Inventors: Michael Bos, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
  • Publication number: 20020099225
    Abstract: The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa inhibitors.
    Type: Application
    Filed: July 25, 2001
    Publication date: July 25, 2002
    Inventors: Jiacheng Zhou, Pasquale N. Confalone, Hui-Yin Li, Philip Ma, Lynette M. Oh, Lucius T. Rossano, Charles G. Clark, Chris Teleha
  • Patent number: 6417370
    Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogeno-alkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenyl-alkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups  in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their use as pesticides and herbicides.
    Type: Grant
    Filed: October 23, 2000
    Date of Patent: July 9, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark-Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
  • Patent number: 6417353
    Abstract: Amines are prepared by reacting aldehydes or ketones at elevated temperature under elevated pressure with nitrogen compounds selected from the group of ammonia, primary and secondary amines, and with hydrogen in the presence of a catalyst containing copper, wherein the catalytically active mass of the catalyst contains, before the reduction with hydrogen, 20 to 85% by weight of oxygen-containing compounds of zirconium, calculated as ZrO2, 1 to 30% by weight of oxygen-containing compounds of copper, calculated as CuO, 14 to 70% by weight of oxygen-containing compounds of nickel, calculated as NiO, 0 to 5% by weight of oxygen-containing compounds of molybdenum, calculated as MoO3, and 0 to 10% by weight of oxygen-containing compounds of aluminum, calculated as Al2O3.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: July 9, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Frank Funke, Joachim Wulff-Döring, Gerhard Schulz, Wolfgang Siegel, Andreas Kramer, Johann-Peter Melder, Arthur Höhn, Philipp Buskens, Wolfgang Reif, Jan Nouwen
  • Patent number: 6417371
    Abstract: The present invention relates to a process process for the preparation of the compound of the formula I where the compound of the formula III is reacted with oxalyl chloride and the product obtained is treated with hydrazine and an alkali metal hydroxide in the aqueous phase at elevated temperature, after treatment is complete a three-phase system is produced by addition of an ether and the compound of the formula I is obtained by acidifying the middle phase. The invention moreover relates to a polymorph of the compound of the formula I.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: July 9, 2002
    Assignee: Merckle GmbH
    Inventors: Thomas Kammermeier, Stefan Laufer, Philipp Merckle, Hans-Guenter Striegel
  • Publication number: 20020072614
    Abstract: Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
    Type: Application
    Filed: November 30, 2001
    Publication date: June 13, 2002
    Inventors: Juan Ignacio Luengo, John Duncan Elliott
  • Publication number: 20020065282
    Abstract: The present invention provides compounds of formula I 1
    Type: Application
    Filed: December 4, 2001
    Publication date: May 30, 2002
    Inventors: Guy Georges, Adelbert Grossmann, Tim Sattelkau, Wolfgang Schaefer, Ulrich Tibes
  • Patent number: 6380241
    Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: April 30, 2002
    Assignee: Abbott Laboratories
    Inventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen, Bruce G. Szczepankiewicz, Kenneth J. Henry, Gang Liu, Steven J. Wittenberger, Steven A. King
  • Patent number: 6355810
    Abstract: Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-COA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to HMG-CoA reductase and the distance between ligands is at least 10 Å. The multibinding compounds of this invention are useful in the treatment and prevention of hypercholesterolemia, hyperlipidemia, atherosclerosis and the like.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 12, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: John H. Griffin, Michael R. Leadbetter, Donald E. Schmidt, Jr.
  • Publication number: 20020019437
    Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): 1
    Type: Application
    Filed: July 31, 2001
    Publication date: February 14, 2002
    Inventors: David W. Boykin, M. Syed Rahmathullah, Richard R. Tidwell, James E. Hall
  • Publication number: 20020016347
    Abstract: Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1&bgr; and TNF-&agr; and may therefore be useful in the therapy of inflammatory diseases and conditions.
    Type: Application
    Filed: May 21, 2001
    Publication date: February 7, 2002
    Inventor: Anne Marie Horneman
  • Publication number: 20020002195
    Abstract: A compound of formula (I): 1
    Type: Application
    Filed: April 12, 2001
    Publication date: January 3, 2002
    Inventors: Jamin Huang, Scot Kevin Huber
  • Patent number: 6307061
    Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: October 23, 2001
    Assignee: Pfizer Inc.
    Inventors: Fumitaka Ito, Hiroshi Kondo
  • Patent number: 6274613
    Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, to a process for their preparation and to their use as pesticides.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: August 14, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Andrew Plant, Gerd Kleefeld, Thorsten Pötter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
  • Patent number: 6166013
    Abstract: Compounds having Formula I ##STR1## are useful for modulating the glucocorticoid receptor in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of treating immune, autoimmune, inflammatory, adrenal imbalance, cognitive and behavioral diseases in a mammal.
    Type: Grant
    Filed: July 30, 1999
    Date of Patent: December 26, 2000
    Assignee: Abbott Laboratories
    Inventors: Michael J. Coghlan, Jay R. Luly, Jeffrey M. Schkeryantz, Alan X. Wang
  • Patent number: 6132475
    Abstract: New p-diaminobenzene derivative compounds of the formula (I): ##STR1## and physiologically compatible water soluble salts thereof are described, wherein X represents oxygen, sulfur, selenium or N-R9. Compositions for dyeing keratin fibers including a combination of coupler and developer substance are described, in which the developer substance includes at least one of the new p-diaminobenzene derivative compounds.
    Type: Grant
    Filed: February 15, 1999
    Date of Patent: October 17, 2000
    Assignee: Wella Aktiengesellschaft
    Inventors: Laurent Chassot, Hans-Juergen Braun
  • Patent number: 6107508
    Abstract: The present invention relates to processes for the production of .alpha.-aryl-.beta.-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
    Type: Grant
    Filed: March 31, 1999
    Date of Patent: August 22, 2000
    Assignee: Dupont Pharmaceuticals Company
    Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
  • Patent number: 6096779
    Abstract: Amorphous piretanide having the following characteristics a) exothermic peaks at about 136.degree. C. and about 209.degree. C., b) an endothermic peak at about 207.degree. C., and c) a melting peak at about 225.degree. C. in differential thermal curves; d) a halopattern without diffraction peak in X-ray powder diffraction analysis; and e) characteristic absorptions at around 1700 cm.sup.-1 and 3200-3500 cm.sup.-1 in infra-red absorption spectrum, and having a superior solubility around neutrality and a high bioavailability effective in the manner of oral or injection administration. Methods of preparing amorphous piretanide are also described.
    Type: Grant
    Filed: November 20, 1997
    Date of Patent: August 1, 2000
    Assignee: Hoechst Pharmaceuticals & Chemicals K.K.
    Inventors: Yuji Chikaraishi, Yoshihisa Matsuda, Makoto Otsuka
  • Patent number: 6057342
    Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: May 2, 2000
    Assignee: Dupont Pharmaceutical Co.
    Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
  • Patent number: 6042620
    Abstract: New p-diaminobenzene derivative compounds of the formula (I): ##STR1## and physiologically compatible water soluble salts thereof are described, wherein X represents oxygen, sulfur, selenium or N-R9, wherein R9 represents hydrogen, an alkyl group, a hydroxyalkyl group, a phenyl group or an acetyl group; and the remaining R groups each represent variously hydrogen, hydroxy, amino, nitro, nitrile, alkyl, alkoxy, hydroxyalkyl, cyclic or aromatic groups, among others. Compositions for dyeing keratin fibers including a combination of coupler and developer substance are disclosed, in which the developer substance includes at least one of the new p-diaminobenzene derivative compounds.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: March 28, 2000
    Assignee: Wella AG
    Inventors: Hans-Juergen Braun, Laurent Chassot
  • Patent number: 5977357
    Abstract: A novel process for the preparation of compounds of formula I ##STR1## by aminolysis of a p-halophenyl alkyl ketone of formula II ##STR2## with a cyclic amine of formula III ##STR3## in water at a temperature of at least 130.degree. C., in which formulae X is a halogen atom and R.sub.1, R.sub.2 and R.sub.3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.
    Type: Grant
    Filed: June 1, 1998
    Date of Patent: November 2, 1999
    Assignee: Ciba Specialty Chemical Corporation
    Inventors: Rinaldo Husler, Rudolf Schwabe, Reto Luisoli
  • Patent number: 5968963
    Abstract: Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A.sub.2 (PLA.sub.2), and thereby useful in the treatment of intestinal cholesterol absorption and the disease states arising therefrom, such as hypercholesterolemia and coronary artery disease.
    Type: Grant
    Filed: March 4, 1996
    Date of Patent: October 19, 1999
    Assignee: Warner-Lambert Company
    Inventor: Reynold Homan
  • Patent number: 5958838
    Abstract: Arylheterocycles having the general formula (I): ##STR1## and process for preparing them. The arylheterocycles having the general formula (I) display high herbicidal activity.
    Type: Grant
    Filed: November 23, 1998
    Date of Patent: September 28, 1999
    Assignee: Isagro Ricerca S.r.l.
    Inventors: Franco Bettarini, Piero La Porta, Giovanni Meazza, Giampaolo Zanardi, Ernesto Signorini, Domenico Portoso
  • Patent number: 5912343
    Abstract: A compound comprising at least one cyclic amine, having an organolithium side-chain, defined according to formula (I) ##STR1## wherein Z is a lithium atom (Li); R.sub.1 is selected from the group consisting of organic groups containing from 1 to about 12 carbon atoms and a bridging bond; each R.sub.2 is independently selected from the group consisting of hydrogen, organic groups containing from 1 to about 12 carbon atoms, and a bridging bond; each R.sub.3 is independently selected from the group consisting of hydrogen and organic groups containing from 1 to about 12 carbon atoms; a is an integer from 4 to about 16; and b is an integer from 0 to about 12; and optionally including a bridge, formed by the selection of two of said bridging bonds, the bridge having 0 to about 6 carbon atoms between the bridging ring members.
    Type: Grant
    Filed: December 31, 1996
    Date of Patent: June 15, 1999
    Assignee: Bridgestone Corporation
    Inventors: David F. Lawson, William L. Hergenrother, Michael L. Kerns
  • Patent number: 5863947
    Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sup.2 is hydrogen, carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or aryl C.sub.1-6 alkyl,R.sup.3 is hydrogen, hydroxy or C.sub.1-4 alkoxy, andR.sup.4 is fluoro, trifluoromethyl, nitro, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkylthio, heteroaryl, optionally substituted aryl, optionally substituted aryl C.sub.1-6 alkyl, optionally substituted aryl C.sub.2-6 alkenyl, optionally substituted aryl C.sub.2-6 alkynyl, optionally substituted aryloxy, optionally substituted aryl C.sub.1-6 alkoxy, optionally substituted arylthio, optionally substituted aryl C.sub.1-6 alkylthio or --CONR"R'", --SO.sub.2 NR"R"", --NR"R'", --OCONR"R"' or --SONR"R'" where R" and R'" are each hydrogen, C.sub.1-6 alkyl or aryl C.sub.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: January 26, 1999
    Assignee: Eli Lilly and Company Limited
    Inventors: Stephen Richard Baker, Barry Peter Clark, John Goldsworthy, John Richard Harris
  • Patent number: 5824691
    Abstract: Guanidine derivatives of the formula: ##STR1## wherein Y is C--R.sup.1(in which R.sup.1 is hydrogen, lower alkyl, hydroxy, protected hydroxy, etc.,)R.sup.2 is pyrrolyl, tetrazolyl, pyrazolyl, etc.,R.sup.3 is hydrogen, lower alkoxy, hydroxy, protected hydroxy, etc.,Z is C--R.sup.4(in which R.sup.4 is hydrogen, carboxy, protected carboxy, nitro, halogen, hydroxy(lower)alkyl, etc.,), andW is R.sup.12(in which R.sup.12 is hydrogen, lower alkoxy, nitro, hydroxy or protected hydroxy)and pharmaceutically acceptable salts thereof which are useful as a medicament which are useful in inhibiting Na.sup.+ /H.sup.+ exchange in cells and in the prevention of cardiovascular diseases, cerebrovascular diseases, renal diseases, arteriosclerosis and shock.
    Type: Grant
    Filed: November 9, 1995
    Date of Patent: October 20, 1998
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Atsushi Kuno, Yoshikazu Inoue, Hisashi Takasugi, Hiroaki Mizuno, Kumi Yamasaki
  • Patent number: 5804595
    Abstract: The invention provides certain amino acid conjugates of substituted 2-phenyl-N-?1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.
    Type: Grant
    Filed: December 5, 1995
    Date of Patent: September 8, 1998
    Assignee: Regents of the University of Minnesota
    Inventors: Philip S. Portoghese, An-Chih Chang
  • Patent number: 5789600
    Abstract: An electrolytically polymerizable macromolecular compound which is advantageously usable as a surface modifier for a polar surface, as a compatibilizing agent for polymer alloys, as an adhesive primer, as an electrochromic substance, etc., a polymerizable monomer to be used for the production thereof, and a method for the production of an electrolytically polymerized film thereof are disclosed. The macromolecular compound has a repeating unit represented by the following general formula (2): ##STR1## wherein R.sub.1 represents a hydrogen atom or an alkyl group, A represents an electrolytically polymerizable group, and B represents a divalent group.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: August 4, 1998
    Assignee: YKK Corporation
    Inventors: Makoto Sakai, Masaki Wakabayashi, Akira Ishibashi
  • Patent number: 5756760
    Abstract: A 1-substituted-2-diphenylphosphinonaphthalene represented by formula (I): ##STR1## wherein at least one of R.sup.1, R.sup.2, R.sup.3, and R.sup.4, which may be the same or different, represents a lower alkyl group having 1 to 4 carbon atoms which may be substituted with an alkoxy group, a phenyl group or --OR.sup.6 (wherein R.sup.6 represents a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms or an alcohol-protective group), and the rest of them represent a hydrogen atom; A represents a single bond or a methylene group; and R.sup.5 represents a substituted or unsubstituted phenyl group; and a transition metal complex comprising the 1-substituted-2-diphenylphosphinonaphthalene as a ligand. The transition metal complex is useful as a catalyst in asymmetric synthesis.
    Type: Grant
    Filed: March 7, 1997
    Date of Patent: May 26, 1998
    Assignee: Takasago International Corporation
    Inventors: Sotaro Miyano, Tetsutaro Hattori, Yasuko Komuro, Hidenori Kumobayashi
  • Patent number: 5731434
    Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: March 24, 1998
    Assignee: Abbott Laboratories
    Inventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen
  • Patent number: 5679763
    Abstract: A composition exhibiting a second order nonlinear optical properties containing a non-centrosymmetric aromatic nonlinear optical compound possessing a delocalized resonance configuration as a guest in a host polyquinoline polymer matrix.
    Type: Grant
    Filed: February 24, 1995
    Date of Patent: October 21, 1997
    Assignee: Enichem S.p.A.
    Inventors: Kwan-Yue Alex Jen, Yongming Cai
  • Patent number: 5594024
    Abstract: A compound or Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 1 or 2; R.sup.1 and R.sup.2 are independently H (provided only one is H at the same time), --OH, CN, CH.sub.2 CN, 2- or 4-CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2 CHF.sub.2, CH.dbd.CF.sub.2, (CH.sub.2).sub.2 CF.sub.3, ethenyl, 2-propenyl, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, SSO.sub.2 CF.sub.3, COR, COOR, CON(R).sub.2, SO.sub.x CH.sub.3 (where, x is 0-2), SO.sub.x CF.sub.3, O(CH.sub.2).sub.x CF.sub.3, SO.sub.2 N(R).sub.2, CH.dbd.NOR, COCOOR, COCOON(R).sub.2, C.sub.1-8 alkyls, C.sub.3-8 cycloalkyls, CH.sub.2 OR, CH.sub.2 (R).sub.2, NRSO.sub.2 CF.sub.3, NO.sub.2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R.sup.3 is hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: January 14, 1997
    Assignee: The Upjohn Company
    Inventors: Kjell A. I. Svensson, Hakan V. Wikstrom, Per A. E. Carlsson, Anna M. P. Boije, R. Nicholas Waters, Clas A. Sonesson, Nils P. Stjernlof, Bengt R. Andersson, Lars O. Hansson
  • Patent number: 5591856
    Abstract: Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.
    Type: Grant
    Filed: January 10, 1995
    Date of Patent: January 7, 1997
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventors: David G. Wettlaufer, Peter A. Nemoto
  • Patent number: 5525734
    Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds on solid supports and synthetic compound libraries comprising pyrrolidine groups prepared by such methods.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: June 11, 1996
    Assignee: Affymax Technologies N.V.
    Inventors: Mark A. Gallop, Martin A. Murphy
  • Patent number: 5525735
    Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds and derivatives thereof on solid supports and synthetic compound libraries comprising pyrrolidine groups and derivatives thereof prepared by such methods.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: June 11, 1996
    Assignee: AFFYMAX Technologies NV
    Inventors: Mark A. Gallop, Martin A. Murphy
  • Patent number: 5514799
    Abstract: Nonlinear optical compounds having structures with delocalized resonance configurations corresponding to: ##STR1## wherein A.sub.1 and A.sub.2 are independently selected from electron withdrawing moieties; R.sub.1 and R.sub.2 are independently selected from aromatic rings, heteroaromatic rings and fused ring systems consisting of two or three aromatic or heteroaromatic rings; n and m are integers from one to five, and D.sub.1 and D.sub.2 are independently selected from hydrogen, electron donating groups and polymer attachment groups, with the proviso that at least one of D.sub.1 and D.sub.2 is an electron donating group. Polymers blended with, cured with, or having pendant side chains of the disclosed nonlinear optical materials and exhibiting second order nonlinear optical properties are also disclosed.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: May 7, 1996
    Assignee: Enichem S.p.A.
    Inventors: Pushkara R. Varanasi, Kwan-Yue A. Jen, King Y. Wong, Robert M. Mininni
  • Patent number: 5486609
    Abstract: A process for preparing carbocyclic m-aminohydroxyaromatics comprises reacting the corresponding o-- or m-halohydroxyaromatics or metal salts thereof with primary or secondary amines in the presence of a base and in the presence or absence of a diluent.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: January 23, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Robert Reinhardt, Helmut Reichelt, Roland Merger
  • Patent number: 5476850
    Abstract: There are described amino-substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## The compounds I are used for the treatment of cardiac arrhythmias and for the prevention of sudden heart death caused by arrhythmias and can therefore be used as antiarrhythmics. They are particularly suitable for those cases in which arrhythmias are a result of constriction of a coronary vessel, such as in angina pectoris or in acute cardiac infarct.
    Type: Grant
    Filed: December 5, 1994
    Date of Patent: December 19, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser
  • Patent number: 5444083
    Abstract: A pyrrolidine compound having the following formula and a pharmacologically acceptable salt thereof is disclosed. It is useful in the pharmaceutical field. ##STR1## in which X is hydrogen, a halogen, or a lower alkyl, Y is --(CH2)n--, n being zero, 1 or 2, --S(O)p--, p being zero, 1 or 2, --O--, or --NH-- and R is phenyl, a substituent-having phenyl, naphtyl, a substituent-having naphthyl, a heteroaryl or a substituent-having heteroaryl.
    Type: Grant
    Filed: January 22, 1990
    Date of Patent: August 22, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Motosuke Yamanaka, Tomonori Hoshiko, Shinji Suda, Naoki Yoneda, Nobuyuki Mori, Mitsumasa Shino, Hiroki Ishihara, Mamoru Saito, Toshiyuki Matsuoka
  • Patent number: 5386058
    Abstract: A method for producing polymethine dyes comprising the steps of:(a) reacting a 1,1-diaryl-2-metallo-ethene with an .omega., .omega.,-diaryl-polyalkene-aldehyde in an anhydrous solvent under an inert atmosphere; and(b) neutralizing the reaction mixture from step (a) with an acid, thereby producing a polymethine dye.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: January 31, 1995
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Roger A. Mader
  • 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: 5384320
    Abstract: Compounds of the formula ##STR1## wherein X is --CH.sub.2 --, --O-- or --S--, m is 1 to 3, n is 1 or 2 and R.sub.1 is hydrogen, C.sub.1 to C.sub.4 alkyl, aryl or aryl substituted with one or more substituents selected independently from the group consisting of halogen, nitro, cyano, C.sub.1 to C.sub.10 alkyl, C.sub.1 to C.sub.10 halosubstituted alkyl, C.sub.1 to C.sub.6 alkoxy, alkoxycarbonyl having from one to ten carbon atoms in the alkoxy moiety, aminocarbonyl, alkylaminocarbonyl having from one to ten carbon atoms in the alkyl moiety and dialkylaminocarbonyl having from one to ten carbon atoms in each of the alkyl moieties, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.
    Type: Grant
    Filed: December 10, 1993
    Date of Patent: January 24, 1995
    Assignee: Pfizer Inc
    Inventors: Kazuo Ando, Takafumi Ikeda
  • Patent number: 5364868
    Abstract: Amino-substituted benzoylguanidines, process for their preparation, their use as a medicament and medicament containing themBenzoylguanidines of the formula I ##STR1## are described in which R(1) or R(2) is an amino group --NR(3)R(4), where R(3) and R(4) are H or (cyclo)alkyl or R(3) is phenyl-(CH.sub.2).sub.p -- where p=0, 1, 2, 3 or 4, or phenyl, or R(3) and R(4) can also together be a methylene chain, and in which the other substituent R(1) or R(2) in each case is H, F, Cl, alkyl, alkoxy, CF.sub.3, C.sub.m F.sub.2m+1 --CH.sub.2 --, benzyl or phenoxy, and their pharmaceutically tolerable salts.The compounds according to the invention have very good antiarrhythmic properties, as occur, for example, in the case of oxygen deficiency symptoms.
    Type: Grant
    Filed: February 11, 1993
    Date of Patent: November 15, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Englert, Dieter Mania, Hans-Jochen Lang, Wolfgang Scholz, Wolfgang Linz, Udo Albus
  • Patent number: 5364830
    Abstract: Pressure or heat sensitive record materials with color-former sublimation problems reduced or eliminated whilst not reducing the color forming capability per unit weight of color former by providing what are in effect dimers of vinyl carbinols, with the vinyl carbinol residues, linked through the aryl groups of a diaryl amine.
    Type: Grant
    Filed: March 19, 1993
    Date of Patent: November 15, 1994
    Assignee: The Wiggins Teape Group Limited
    Inventors: Ivan Sheiham, Margaret P. Templey
  • Patent number: 5360930
    Abstract: Direct dyes having quaternary center with a long aliphatic chain, compositions containing those dyes, and the process of using them to dye hair are disclosed. These dyes have a higher affinity for hair and are more shampoo stable than conventional direct dyes, and produce pleasing uniform dyeing.
    Type: Grant
    Filed: January 10, 1994
    Date of Patent: November 1, 1994
    Assignee: Clairol Inc.
    Inventors: Alexander Chan, Yuh-Guo Pan
  • Patent number: 5338739
    Abstract: Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.
    Type: Grant
    Filed: March 10, 1994
    Date of Patent: August 16, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: David G. Wettlaufer, Peter A. Nemoto
  • Patent number: 5312930
    Abstract: This invention relates to optical elements capable of second harmonic generation and novel compositions for use in such optical elements comprising polar molecules placed in noncentrosymmetric configuration wherein such optical element has an electron donor moiety linked through a conjugated bonding moiety to an electron acceptor moiety which consists of a selected fluorinated sulfone, fluorinated ketone, fluorinated vinyl sulfone or fluorinated alkyl vinyl sulfone.
    Type: Grant
    Filed: December 31, 1992
    Date of Patent: May 17, 1994
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Lap T. Cheng, Andrew E. Feiring, Wilson Tam
  • Patent number: 5292893
    Abstract: A process is provided for catalytically reducing imines, oximes, hydrazones and related compounds. Moreover, there is provided a process for the catalytic asymmetric reduction of imines, oximes, hydrazones, and the like, using enantiomerically enriched catalysts, to provide chiral amine reaction products which are enriched in one enantiomer. Catalytic asymmetric reduction can also be carried out using an achiral precatalyst in combination with aThe U.S. Government has rights in this invention pursuant to NIH Grant Number GM 34917.
    Type: Grant
    Filed: November 14, 1991
    Date of Patent: March 8, 1994
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Christopher A. Willoughby