Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/478)
  • Publication number: 20030162979
    Abstract: The invention relates to novel substituted sulphonylamino(thio)carbonyl compounds of the formula (I) 1
    Type: Application
    Filed: May 1, 2002
    Publication date: August 28, 2003
    Inventors: Klaus-Helmut Muller, Mark Wilhelm Drewes, Kurt Findeisen, Ernst Rudolf F. Gesing, Johannes R. Jansen, Rolf Kirsten, Joachim Kluth, Ulrich Philipp, Hans-Jochem Riebel, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6610729
    Abstract: The present invention relates to a hydroxamic acid derivative of the formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition containing the derivative or a salt thereof, and to pharmaceutical use thereof. The hydroxamic acid derivative and a pharmacologically acceptable salt thereof of the present invention have an inhibitory activity of TNF &agr; production, and are useful for, for example, the prophylaxis and treatment of the diseases such as autoimmune diseases and inflammatory diseases (e.g., sepsis, MOF, rheumatoid arthritis, Crohn's disease, cachexia, myasthenia gravis, systemic lupus erythematosus, asthma, I type diabetes, psoriasis and the like), and the like.
    Type: Grant
    Filed: November 22, 2000
    Date of Patent: August 26, 2003
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Tomokazu Gotou, Shinji Takeda, Kazuhiro Maeda, Tomohiro Yoshida, Naoki Sugiyama, Tadahiro Takemoto
  • Publication number: 20030144217
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Application
    Filed: August 21, 2002
    Publication date: July 31, 2003
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Roger D. Tung, Michael R. Hale, Christopher T. Baker, Andrew Spaltenstein, Eric S. Furfine, Istvan Kaldor, Wieslaw M. Kazmierski
  • Publication number: 20030022931
    Abstract: This invention relates to novel alkylxanthates of formulae 1 to 3 and use of alkylxanthates of formulae 1 to 6 in the integrated pest management, more specifically alkyl xanthates are used as insect growth regulatory for pest management in agricultural fields no or less environmental impact.
    Type: Application
    Filed: March 30, 2001
    Publication date: January 30, 2003
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Janapala Venkateswara Rao, Yenamandra Venkateswarlu, Kondapuram Vijaya Raghavan
  • Patent number: 6433009
    Abstract: A compound of the formula wherein R1 and R2 are as defined above, useful in the treatment and condition selected from the group consisting of meningitis and salpingitis, septic shock, disseminated intravascular coagulation, and/or adult respiratory distress syndrome, acute or chronic inflammation, arthritis, cholangitis, colitis, encephalitis, endocarditis, glomerulonephritis, hepatitis, myocarditis, pancreatitis, pericarditis, reperfusion injury, vasculitis, acute and delayed hypersensitivity, graft rejection, and graft-versus-host disease, auto-immune diseases including Type 1 diabetes mellitus and multiple sclerosis, periodonate diseases, interstitial pulmonary fibrosis, cirrhosis, systemic sclerosis, keloid formation, tumors which produce IL-1 as an autocrine growth factor, cachexia, Alzheimers disease, percussion injury, depression, atherosclerosis, osteoporosis in a mammal, including a human.
    Type: Grant
    Filed: October 31, 2000
    Date of Patent: August 13, 2002
    Assignee: Pfizer Inc
    Inventors: Mark Anthony Dombroski, James Frederick Eggler
  • Patent number: 6423740
    Abstract: The invention relates to a novel class of compounds that have structures related to certain naturally occurring or synthetic chalcones. The invention also relates to pharmaceutical compositions comprising the compounds and methods for treating certain disorders using the pharmaceutical compositions. The invention further relates to a process for synthesizing the novel class of compounds.
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: July 23, 2002
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Piero Valenti
  • Patent number: 6384248
    Abstract: The present invention deals with novel emulsifiers. The compounds are esters made by the reaction of sorbitol and meadowfoam acids. The introduction of the unsaturated highly stable meadowfoam acid portion of the molecule into the compounds of the present invention results in improved emulsification efficiency, improved oxidative stability and improved liquidity of the esters.
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: May 7, 2002
    Assignee: Fan Tech LTD
    Inventor: Anthony J. O'Lenick, Jr.
  • Patent number: 6362166
    Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: March 26, 2002
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Siegfried H. Reich, Thomas L. Little, Jr., Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine, Ted M. Bleckman
  • Patent number: 6303789
    Abstract: Compounds of the formula I in which R1, R2, R3, R4, R5, m and n have the meanings cited in the description, are novel effective PDE-inhibitors.
    Type: Grant
    Filed: December 7, 2000
    Date of Patent: October 16, 2001
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Thomas Bär
  • Publication number: 20010029265
    Abstract: Substituted tetrahydrofuran analogs of prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.
    Type: Application
    Filed: March 6, 2001
    Publication date: October 11, 2001
    Inventor: Robert D. Selliah
  • Patent number: 6175017
    Abstract: A process for the preparation of carbonates containing aromatic ester groups is disclosed. The process entails reacting aromatic monohydroxy componds with phosgene or with chlorocarbonic acid esters of aromatic monohydroxy compounds at a temperature of 50 to 350° C. and in the presence of active carbon as catalyst.
    Type: Grant
    Filed: August 18, 1993
    Date of Patent: January 16, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Josef Buysch, Norbert Schön, G{umlaut over (u)}nther Jeromin
  • Patent number: 6140516
    Abstract: Disclosed is a process for preparing novel trans-3-alkyloxy-4-hydroxytetrahydrofurans including racemic and substantially enantiomerically pure (3S,4S)-trans-3-alk(en)yloxy-4-hydroxytetrahydrofurans and (3R,4R)-trans-3-alk(en)yloxy-4-acyloxytetrahydrofurans. The disclosed process comprises the steps of reacting 3,4-epoxytetrahydrofuran with an alcohol under Lewis acid catalysis to obtain a racemic trans-3-alk(en)yloxy-4-hydroxytetrahydrofuran; contacting the trans-3-alk(en)yloxy-4-hydroxytetrahydrofuran with an acyl donor in the presence of a hydrolase enzyme to produce a mixture of a substantially enantiomerically pure (3S,4S)-trans-3-alk(en)yloxy-4-hydroxytetrahydrofuran and a substantially enantiomerically pure (3R,4R)-trans-3-alk(en)yloxy-4-acyloxytetrahydrofuran; and separating the components of the mixture by partitioning between water and a solvent immiscible with water.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: October 31, 2000
    Assignee: Eastman Chemical Company
    Inventors: Daniel John Bayston, Sharon Casson, James Matthew Lovell, Ronald Michael Scott
  • Patent number: 6013813
    Abstract: The present invention deals with the composition of matter and the utilization of certain novel sorbitol guerbet esters which are prepared by the reaction of a guerbet acid and a sorbitol as emulsifiers.
    Type: Grant
    Filed: August 24, 1998
    Date of Patent: January 11, 2000
    Assignee: Hansotech Inc
    Inventor: Anthony J. O'Lenick, Jr.
  • Patent number: 5886193
    Abstract: A support carrying a homocyclic or heterocyclic ring containing a first and second carbon atom wherein: (i) the first carbon atom is substituted by a nucleophilic group or a group convertible to a nucleophilic group on treatment with base; (ii) the second carbon atom is substituted by a hydroxy group, a hydroxy group protected by an acid labile protecting group, or a phosphate group substituted by an oligonucleotide; and (iii) the first and second carbon atoms are directly connected by a covalent bond; which is suitable for use in oligonucleotide synthesis. Methods for its preparation and use, and novel compounds for attachment to the support are described.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: March 23, 1999
    Assignee: Zeneca Limited
    Inventors: Michael Joseph McLean, Andrew John Garman
  • Patent number: 5880294
    Abstract: The present invention relates to D-pentofuranose derivatives represented by the following formulas (1) through (4): ##STR1## (wherein A represents a chlorobenzoyl group; R.sup.1 represents a hydrogen atom, an aliphatic lower acyl group, a substituted or unsubstituted benzoyl group; each of X and Y represents a lower alkyl group; Z represents an ethynyl group or tri-lower alkyl silylethynyl group; the sugar moiety in formula (1) represents xylose; and the sugar moiety of each of formulas (3) and (4) represents ribose). The present invention also relates to a process for preparing the compound (2) characterized by oxidizing the compound of formula (1) with a hypochlorite in the presence of a catalytic amount of 2,2,6,6-tetramethylpiperidinoxy compound, and these compounds are useful as intermediates in the synthesis of 3'-C-substituted ribonucleoside derivatives having excellent antitumor activities.
    Type: Grant
    Filed: January 6, 1998
    Date of Patent: March 9, 1999
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Makoto Nomura, Hideki Kazuno, Tsutomu Sato, Masato Washinosu, Motoaki Tanaka, Akira Matsuda, Tetsuji Asao
  • Patent number: 5874472
    Abstract: Compounds of formula (I) and salts, esters and amides thereof, wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.3-6 cycloalkyl group, a thiol group optionally substituted by a C.sub.1-6 alkyl group, or an amino group optionally substituted by one or two alkyl or alkenyl groups; R.sup.2 is H, C.sub.1-7 straight or branched chain alkyl, C.sub.3-6 cycloalkyl, C.sub.2-7 alkenyl or benzyl; A is a 5 or 6 membered aromatic carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or di C.sub.1-6 alkylamino; r is 0, 1 or 2; their use in medicine and in particular for conditions requiring inhibition of the NO Synthase enzyme, pharmaceutical formulations and processes for the preparation thereof are disclosed.
    Type: Grant
    Filed: March 18, 1996
    Date of Patent: February 23, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventors: Barry George Shearer, Karl Witold Franzmann, Harold Francis Hodson
  • Patent number: 5856323
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 5, 1999
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5856530
    Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.
    Type: Grant
    Filed: May 2, 1997
    Date of Patent: January 5, 1999
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Siegfried H. Reich, Thomas L. Little, Jr., Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine, Ted M. Bleckman
  • Patent number: 5750735
    Abstract: Carbapenem antibiotic compounds of the general formula: ##STR1## wherein the moiety ##STR2## is a 4, 5 or 6 membered mono, di- or tri-substituted oxygen or sulfur containing ring; wherein Z is oxygen, sulfur, sulfoxide and sulfone, pharmaceutical compositions thereof useful for the treatment of bacterial infections, processes for preparing the compounds and new intermediates useful in the process.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: May 12, 1998
    Assignee: American Cyanamid Company
    Inventors: Yang-I Lin, Panayota Bitha, Subas Sakya, Timothy W. Strohmeyer, Karen Bush, Carl Bernard Ziegler, Gregg Brian Feigelson
  • Patent number: 5693667
    Abstract: A compound, composition, and method for controlling Take-all disease of plants by applying a fungicide of the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 are carbons of a furan ring; A is selected from the group consisting of --C(X)-amine wherein the amine is substituted with a first and a second amine substituent or with an alkylaminocarbonyl and a hydrogen, --C(O)--SR.sub.3 ; --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ; Q is C, Si, Ge, or Sn; W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W may also be selected from --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.p --, and --O--; X is O or S; n is 0, 1, or 2; m is 0 or 1; p is 0, 1, or 2;wherein two R.sub.
    Type: Grant
    Filed: December 28, 1994
    Date of Patent: December 2, 1997
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
  • Patent number: 5668156
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: September 16, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William Robert Pilgrim
  • Patent number: 5648486
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: May 12, 1993
    Date of Patent: July 15, 1997
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5631389
    Abstract: The present invention relates to a new class of carbohydrate based nonionic surfactant, i.e., alkyl and alkenyl glycasuccinimide, and a process for their manufacture.
    Type: Grant
    Filed: April 30, 1996
    Date of Patent: May 20, 1997
    Assignee: Lever Brothers Company, Division of Conopco, Inc.
    Inventors: Robert Vermeer, Van Au, Bijan Harichian
  • Patent number: 5552066
    Abstract: Biodegradable compounds which are effective fabric conditioning molecules are described as having Formula I ##STR1## wherein R.sub.1 is a C.sub.1-4 alkyl or alkenyl, R.sub.2 and R.sub.3 are each independently a C.sub.7 -C.sub.30 straight or branched alkyl or alkenyl, R.sub.4 is a C.sub.1-4 alkyl or alkenyl or hydroxyalkyl and X is a water soluble anion.
    Type: Grant
    Filed: April 14, 1995
    Date of Patent: September 3, 1996
    Assignee: Lever Brothers Company, Division of Conopco, Inc.
    Inventors: Mohammad A. Rahman, Anthony Hung, Shang-Ren Wu
  • Patent number: 5530146
    Abstract: Furobenzopyran derivatives of the general formula (I): ##STR1## in which R.sup.1 is a lower alkyl group, R.sup.2 is a lower alkyl group, lower alkoxy group, halogen atom or lower alkyl group substituted by a halogen atom, R.sup.3 is a lower alkyl group, lower alkoxy group, halogen atom, lower alkyl group substituted by a halogen atom, phenoxy group or benzyloxy group, R.sup.4 is a hydrogen atom or lower alkyl group and m and n are any integers between 0 and 4, have an excellent herbicidal activity on weeds and are completely selective to crops such as paddy rice, soybeans and cotton.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: June 25, 1996
    Assignee: Mitsui Toatsu Chemicals, Incorporated
    Inventors: Kiyoshi Arai, Masayuki Ooka, Fumiaki Koizumi, Sadafumi Koda, Yasunaga Iwasaki, Yoshiro Kanemoto
  • Patent number: 5514679
    Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, hydroxy, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, alkylthioalkynyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy or cyanomethyl, nitro, difluoromethyl, trifluoromethyl or cyano;Y is alkylene of 3 to 9 carbon atoms;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkanoyl, alkanoyloxy, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, cyanomethyl, fluoroalkyl, cyano, phenyl, alkynyl, alkene, or halo;R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.
    Type: Grant
    Filed: May 13, 1994
    Date of Patent: May 7, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Theodore J. Nitz
  • Patent number: 5498775
    Abstract: This invention relates to the use of polyanionic benzylglycosides as smooth muscle cell proliferation inhibitors and as therapeutic compositions for treating diseases and conditions which are characterized by excessive smooth muscle proliferation, such as restenosis. The compounds of this invention are those of formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are, independently, H, SO.sub.3 M, or ##STR2## and each oligosaccharide group contains 1 to 3 sugar groups; M is lithium, sodium, potassium, or ammonium;n is 1 or 2;X is a halogen, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms;Y is carbonyl or sulfonyl;Z is alkyl from 1 to 12 carbon atoms, ##STR3## and X is as defined above; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 7, 1994
    Date of Patent: March 12, 1996
    Assignee: American Home Products Corporation
    Inventors: Sarah T. A. Novak, Richard M. Soll, John W. Ellingboe, Thomas T. Nguyen
  • Patent number: 5466827
    Abstract: Thioalkane .alpha.,.beta.-diketones have interesting organoleptic properties and are therefore suitable as aroma substances.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: November 14, 1995
    Assignee: Haarmann & Reimer GmbH
    Inventors: Heinz-Jurgen Bertram, Roland Emberger, Matthias Guntert, Peter Werkhoff
  • Patent number: 5434151
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: August 24, 1992
    Date of Patent: July 18, 1995
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5429756
    Abstract: Biodegradable compounds which are effective fabric conditioning molecules are described as having Formula I ##STR1## wherein R.sub.1 is a C.sub.1-4 alkyl or alkenyl, R.sub.2 and R.sub.3 are each independently a C.sub.7 -C.sub.30 straight or branched alkyl or alkenyl, R.sub.4 is a C.sub.1-4 alkyl or alkenyl or hydroxyalkyl and X is a water soluble anion.
    Type: Grant
    Filed: June 1, 1994
    Date of Patent: July 4, 1995
    Assignee: Lever Brothers Company, Division of Conopco, Inc.
    Inventors: Mohammad A. Rahman, Anthony P. C. Hung, Shang-Ren Wu
  • Patent number: 5412118
    Abstract: The present invention relates to liquid and powdered surfactant compositions comprising alkyl (alkyl glycosid) uronamide compounds. Compositions comprising these compounds have been found to provide significant benefits such as stable, aqueous foam (in shampoo compositions) and enhanced detergency and oily soil removal (in detergent compositions).
    Type: Grant
    Filed: October 12, 1993
    Date of Patent: May 2, 1995
    Assignee: Lever Brothers Company, Division of Conopco, Inc.
    Inventors: Robert Vermeer, Bijan Harichian, Van Au
  • Patent number: 5403857
    Abstract: The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; R.sup.2 and R.sup.3 together form -A.sup.2 -X.sup.2 -A.sup.3 - which defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl; A.sup.1 is a direct link to X.sup.1 or is (1-3C) alkylene; X.sup.1 is oxy, thio or imino; Ar is optionally substituted phenylene; R.sup.4 is (1-4C)alkyl, fluoro-(2-4C)alkyl or optionally substituted phenyl or a heterocyclic moiety; R.sup.5 is hydrogen or (1-4C)alkyl; and R.sup.6 is hydrogen, halogeno, trifluoromethyl, (1-4C)alkyl or (1-4C)alkoxy; or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
    Type: Grant
    Filed: February 1, 1994
    Date of Patent: April 4, 1995
    Assignees: Imperial Chemical Industries PLC, ICI-Pharma
    Inventors: Philip N. Edwards, Keith Oldham, David Waterson
  • Patent number: 5401861
    Abstract: A stereoselective process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates by contacting a lactol with an amine base in an inert solvent, adjusting the temperature and adding a sulfonating reagent.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: March 28, 1995
    Assignee: Eli Lilly and Company
    Inventor: Ta-Sen Chou
  • Patent number: 5358938
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl terahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiphenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: July 13, 1992
    Date of Patent: October 25, 1994
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Saijat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5324709
    Abstract: A tetrahydrofuran derivative represented by the following general formula [I]: ##STR1## wherein A represents direct bonding or a group represented by --B--CHR.sup.1 --(wherein B represents oxygen atom, sulfur atom or imino group; R.sup.1 represents hydrogen atom or an alkyl group); R represents hydrogen atom, halogen atom, hydroxyl group, an alkoxy group, benzyloxy group, an alkylsulfonyloxy group or a group represented by --O--COR.sup.2 (wherein R.sup.2 represents an alkyl group, a haloalkyl group, an alkenyl group, a cycloalkyl group, phenyl group, benzyl group, an alkoxy group, an alkylamino group or a dialkylamino group; X represents halogen atom; Y represents hydrogen atom or halogen atom) and the herbicide containing the same as the effective ingredient. The compounds of the present invention have exceedingly high herbicidal activity, and furthermore, the compounds are superior to the known similar compounds in terms of safety on crops. Thus, the compounds are useful as herbicides.
    Type: Grant
    Filed: November 20, 1992
    Date of Patent: June 28, 1994
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Natsume Bunji, Kyomura Nobuo, Suzuki Seiichi, Takahashi Yoji, Jikihara Tetsuo
  • Patent number: 5306831
    Abstract: Polyol impurities in a sorbitan ester mixture is removed by treating a polyol-containing sorbitan ester dissolved in a solution containing a hydrocarbon and a polar organic solvent with an aqueous metal halide salt solution.
    Type: Grant
    Filed: October 15, 1992
    Date of Patent: April 26, 1994
    Assignee: Shell Oil Company
    Inventors: Sharon M. Beshouri, Robert P. Adamski
  • Patent number: 5290956
    Abstract: This invention relates to latent thiol monomers and their use in the synthesis of polymers. In addition, this invention relates to novel polymers and graft copolymers formed with these latent thiol monomers.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: March 1, 1994
    Assignee: Rohm and Haas Company
    Inventors: William D. Emmons, Andrew W. Gross
  • Patent number: 5256798
    Abstract: A process for providing an alpha-anomer enriched ribofuranosyl sulfonate from a beta-anomer ribofuranosyl sulfonate; comprising treating a beta-anomer ribofuranosyl sulfonate or anomeric mixture thereof with a conjugate anion of a sulfonic acid source at elevated temperatures in an inert solvent.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: October 26, 1993
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Charles D. Jones
  • Patent number: 5256797
    Abstract: A process for separating an anomeric mixture of alpha and beta 2-deoxy-2,2-difluoro-D-ribofuranosyl-1-alkylsulfonates by contacting the anomeric mixture with a solvent; heating; adding a countersolvent; and lowering the temperature.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: October 26, 1993
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Timothy J. McCarthy
  • Patent number: 5252756
    Abstract: A stereoselective process for preparing 2-deoxy-2,2-difluoro-D-ribofuranosyl beta-anomer enriched aryl sulfonates or substituted arylsulfonates involving reacting a lactol with an acid scavenger and a sulfonating reagent in an inert solvent.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: October 12, 1993
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Charles D. Jones
  • Patent number: 5234950
    Abstract: The invention concerns a heterocyclic derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo-(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene, or a 6 membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X--A.sup.3 -- wherein each of A.sup.2 and A.sup.3 is (1-4C)alkylene and X is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
    Type: Grant
    Filed: January 3, 1992
    Date of Patent: August 10, 1993
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Philip N. Edwards, Jean-Marc M. M. Girodeau
  • Patent number: 5217991
    Abstract: Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from cycloalkyl and cycloalkylalkyl groups, wherein said cycloalkyl group contains three to about eight carbon atoms and the acyclic alkyl portion of said cycloalkylalkyl group contains one to about eight carbon atoms; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl: wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.
    Type: Grant
    Filed: May 28, 1992
    Date of Patent: June 8, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
  • Patent number: 5216013
    Abstract: Non-peptidyl compounds characterized generally as heterocyclic acyl aminodiol .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are compounds of the formula ##STR1## wherein R.sub.1 is selected from aryl and aralkyl groups represented by ##STR2## and wherein R.sub.1 may be further selected from heteroaryl and heteroaralkyl represented by ##STR3## wherein each of T and A is independently selected from N and CH; wherein n is a number selected from zero through five, inclusive; wherein X is selected from oxygen atom, methylamino and NH; wherein each of Y and Z is independently selected from chloro, fluoro, methoxy and dimethylamino; wherein Q is oxygen atom; and wherein each of T and A is independently selected from N and CH; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is selected from methyl and ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; wherein R.
    Type: Grant
    Filed: July 16, 1992
    Date of Patent: June 1, 1993
    Assignee: G. D. Searle & Co.
    Inventor: Gunnar J. Hanson
  • Patent number: 5206414
    Abstract: A process for the preparation of compounds of the general formula ##STR1## where R.sub.1 and R.sub.2 are identical or different and are hydrogen, C.sub.1 -C.sub.18 alkyl, phenyl, C.sub.1 -C.sub.4 alkyl-substituted phenyl, C.sub.7 -C.sub.9 phenylalkyl, C.sub.5 -C.sub.12 cycloalkyl or C.sub.1 -C.sub.4 alkyl-substituted C.sub.5 -C.sub.12 cycloalkyl,R.sub.3 is hydrogen or methyl,m is 0, 1, 2 or 3, andn is a number from 1 to 4 or 6, andA is as defined in the description,by reacting a compound of the formula II ##STR2## where m, R.sub.1 and R.sub.2 are as defined above, with a compound of the formula III ##STR3## where A and n are as defined in the description, which comprises carrying out the reaction in the presence of a catalyst which contains, as active material, an alkali metal compound of the formula IVM.sub.m An (IV)in whichM is Li, Na, K, Rb or Cs,m is the valency of An, andAn is a fluoride, hydroxide, phosphate, formate, acetate or --OR.sub.5 radical, andR.sub.
    Type: Grant
    Filed: April 29, 1992
    Date of Patent: April 27, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Samuel Evans, Paul Dubs, Milos Rusek, Zdenek Mazour, Arpad Major
  • Patent number: 5179123
    Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxgen, sulfur, --CH.dbd.CH--or --CH.dbd.N--; wherein R.sub.1 is alkyl, alkenyl or alkynyl of about 1 to 20 carbon atoms; wherein R is --CO.sub.2 R.sup.2, tetrazole, methylsulfonamide or benzenesulfonamide, wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation and R.sup.3 is hydroxyl or halogen, having utility as LTB.sub.4 synthesis inhibitors.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: January 12, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
  • Patent number: 5175298
    Abstract: The present invention provides processes and intermediates for one preparation of the hydroxy ethylene isostere dipeptide of leu-val which is itself useful in the preparation of renin inhibitory peptides. The process employs certain novel oxazolidenes.
    Type: Grant
    Filed: December 11, 1990
    Date of Patent: December 29, 1992
    Assignee: The Upjohn Company
    Inventor: Peter G. M. Wuts
  • Patent number: 5162364
    Abstract: A compound of formula (I): ##STR1## in which R, R.sub.1 and R.sub.2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA.sub.B receptors.
    Type: Grant
    Filed: June 11, 1991
    Date of Patent: November 10, 1992
    Assignee: Adir et Compagnie
    Inventors: Michel Debaert, Pascal Berthelot, Claude Vaccher
  • Patent number: 5112848
    Abstract: Substituted furan and pyrrole compounds which are useful in inhibiting lipoxygenase enzymes, particularly 5-lipoxygenase.
    Type: Grant
    Filed: April 19, 1990
    Date of Patent: May 12, 1992
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Bruce P. Gunn, James H. Holms, James B. Summers
  • Patent number: 5053430
    Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.
    Type: Grant
    Filed: September 22, 1989
    Date of Patent: October 1, 1991
    Assignee: Boehringer Ingelheim KG
    Inventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
  • Patent number: 5049676
    Abstract: A process for the preparation of optically active esters of 2-chloropropionic acid of the formula: ##STR1## from an optically active lactate of the formula: ##STR2## with inversion of configuration. COOR.sub.1 in formula I and formula II is a hydrolyzable group. The lactate of formula II is brought into contact with SOCl.sub.2, followed by decomposition of the chlorosulfite formed, the process being one in which at least the decomposition stage is carried out in the presence of an ether.
    Type: Grant
    Filed: May 30, 1990
    Date of Patent: September 17, 1991
    Assignee: Rhone-Poulenc Chimie
    Inventors: Pascal Metivier, Harivelo Rajoharisson