The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 558/178)
  • Publication number: 20140275573
    Abstract: An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: LUNG BIOTECHNOLOGY INC.
    Inventors: Vijay Sharma, Hitesh Batra, Sudersan Tuladhar
  • Publication number: 20140017797
    Abstract: This invention concerns isotopically coded or non-isotopically coded affinity-tags for analysis of certain target molecules in complex samples, in particular for mass spectrometric analysis of proteomic samples. The affinity-tags have the following general formula X-SPACER-OPO3H2, wherein X is a functional group or moiety capable of reacting with a functional group of a protein, peptide, DNA, lipid, sugar and/or steroid. These phosphate affinity tags (‘PTAG’) are capable of high but reversible binding to metal-oxides like TiO2. Due to this property, tagged sample fractions can be isolated from non-tagged sample fraction by affinity chromatography. The binding of organophosphate to metal-oxides remains intact during multiple washings of preferably acidic solutions to remove non-specifically bound components. PTAG's are also envisaged wherein X is selected such that it is capable of binding proteins, peptides, nucleic acid molecules, lipids, carbohydrates, steroids and the like.
    Type: Application
    Filed: December 13, 2011
    Publication date: January 16, 2014
    Applicant: De Staadt der Nederlanden, vert doorde minister van VWS
    Inventor: Jamila Willhelmina Zomer-Elhadari
  • Patent number: 8492593
    Abstract: Amido-fluorophosphite compounds and catalyst systems comprising at least one amido-fluorophosphite ligand compound in combination with a transition metal are described. Moreover, the use of amido-fluorophosphite containing catalysts for transition metal catalyzed processes, especially to the hydroformylation of various olefins to produce aldehydes are also described.
    Type: Grant
    Filed: August 16, 2011
    Date of Patent: July 23, 2013
    Assignee: Eastman Chemical Company
    Inventor: Thomas Allen Puckette
  • Publication number: 20130046112
    Abstract: Amido-fluorophosphite compounds and catalyst systems comprising at least one amido-fluorophosphite ligand compound in combination with a transition metal are described. Moreover, the use of amido-fluorophosphite containing catalysts for transition metal catalyzed processes, especially to the hydroformylation of various olefins to produce aldehydes are also described.
    Type: Application
    Filed: August 16, 2011
    Publication date: February 21, 2013
    Applicant: Eastman Chemical Company
    Inventor: Thomas Allen Puckette
  • Publication number: 20120294900
    Abstract: Provided are compositions and methods for modulating quorum sensing in microbes. The compounds are AI-2 analogs and as such have structures similar to 4,5-dihydroxy-2,3-pentanedione that can act as agonists/antagonists of quorum sensing. The compounds are useful for modulating quorum sensing in bacteria and can be used in methods for prophylaxis or therapy of bacterial infections and for reduction of biofilms.
    Type: Application
    Filed: March 26, 2012
    Publication date: November 22, 2012
    Applicant: UNIVERSITY OF MARYLAND, COLLEGE PARK
    Inventors: Herman Sintim, William E. Bentley, Varnika Roy, Jacqueline Smith
  • Publication number: 20120129968
    Abstract: The invention relates to a liquid bis(acyl)phosphine oxide of formula (I): wherein R is C1-C18 alkyl, and wherein R is optionally substituted as described herein. The invention also relates to radiation curable compositions comprising liquid bis(acyl)phosphine oxide of formula (I).
    Type: Application
    Filed: June 21, 2011
    Publication date: May 24, 2012
    Inventor: Timothy Edward Bishop
  • Publication number: 20120046247
    Abstract: This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.
    Type: Application
    Filed: August 16, 2011
    Publication date: February 23, 2012
    Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
  • Publication number: 20110294151
    Abstract: Described herein are substrates composed of a base coated with a fluorophore-labeled calcium phosphate coating. The substrates are useful in culturing and studying the activity of a variety of cells. The substrates described herein can be used for both solution- and image-based analysis of cultured cells. New methods for producing and using such coated substrates are also disclosed.
    Type: Application
    Filed: July 29, 2010
    Publication date: December 1, 2011
    Inventors: Hongwei Hanna Rao, Jian Tan
  • Publication number: 20110286962
    Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
    Type: Application
    Filed: May 26, 2011
    Publication date: November 24, 2011
    Inventors: Jean-Pierre SOMMADOSSI, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
  • Patent number: 7935686
    Abstract: Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of making prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of using prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: May 3, 2011
    Assignee: XenoPort, Inc.
    Inventor: Mark A. Gallop
  • Publication number: 20100204184
    Abstract: The invention concerns novel phosphonate derivatives, preparation method, use thereof as ligands modulating T ?9?2 lymphocyte activity and pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 14, 2010
    Publication date: August 12, 2010
    Applicants: LABORATOIRES MAYOLY SPINDLER, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER II
    Inventors: Jean-Louis Montero, Ibrahim Zgani, Chantal Menut, Valérie Gallois
  • Patent number: 7749985
    Abstract: Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.
    Type: Grant
    Filed: July 21, 2009
    Date of Patent: July 6, 2010
    Assignee: XenoPort, Inc.
    Inventors: Mark A. Gallop, Feng Xu, Thu Phan, Usha Dilip, Ge Peng
  • Patent number: 7494985
    Abstract: Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of making prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of using prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.
    Type: Grant
    Filed: November 3, 2005
    Date of Patent: February 24, 2009
    Assignee: XenoPort, Inc.
    Inventor: Mark A. Gallop
  • Patent number: 7186703
    Abstract: The present invention discloses novel phospho-derivatives of branched-chain lipophilic molecules useful for permeabilizing biological barriers and for inhibiting tumor growth. The invention further discloses pharmaceutical compositions comprising said molecules and their uses.
    Type: Grant
    Filed: August 1, 2001
    Date of Patent: March 6, 2007
    Assignee: D-Pharm Ltd.
    Inventors: Alexander Kozak, Marina Vinnikova, Michael Polyak, Eliezer Beit-Yannai, Dalia Reznitsky-Cohen, Alexander Senderikhin
  • Patent number: 7101864
    Abstract: The present invention relates to compositions useful for treating or controlling disease states or conditions associated with zinc containing proteinases, especially metalloproteinases. The active ingredient in these compositions is an alpha-oxo- or alpha-thixophosphpnate of formula (I). Out of the phosphonates of formula (I), some are known and others are new. The novel compounds constitute another aspect of the invention.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: September 5, 2006
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Eli Breuer, Reuven Reich, Claudio Salomon
  • Publication number: 20040182279
    Abstract: A lightfast colorant and a lightfast ink composition include a lightfast colorant that is derived by covalently binding a benzophenone derivative and a conventional colorant and that imparts effective lightfastness and long-term storage stability to an ink composition that is prepared with the same.
    Type: Application
    Filed: March 18, 2004
    Publication date: September 23, 2004
    Applicant: Samsung Electronics Co., Ltd.
    Inventors: Kyung-hoon Lee, Seung-min Ryu, Yeon-kyoung Jung
  • Publication number: 20030236212
    Abstract: The invention relates to novel Acyl coenzyme-A mimics, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The Acyl coenzyme-A mimics, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, bacterial infection and impotence. In certain embodiments, the Acyl coenzyme-A mimics, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Application
    Filed: April 10, 2003
    Publication date: December 25, 2003
    Inventors: Jean-Louis Dasseux, Carmen Daniela Oniciu
  • Patent number: 6596711
    Abstract: Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)methylphosphinic acid; ii) (S)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iii) (R)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iv) (3-amino-2-hydroxypropyl)difluoromethylphosphinic acid; and v) (3-amino-2-oxopropyl)methylphosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.
    Type: Grant
    Filed: March 1, 2001
    Date of Patent: July 22, 2003
    Assignee: AstraZeneca AB
    Inventors: Kosrat Amin, Thomas Elebring, Peter Guzzo, Thomas Olsson, Marianne Swanson, Sverker Von Unge
  • Patent number: 6585780
    Abstract: Phosphinato-substituted propane- and butanepolycarboxylic acids and derivatives thereof are useful as crosslinking agents for cellulosic materials to render them wrinkle resistant and/or iron free in a durable press process.
    Type: Grant
    Filed: January 10, 2001
    Date of Patent: July 1, 2003
    Assignee: Rhodia Inc.
    Inventors: Johnson D. Koola, Lanny E. Todd
  • Patent number: 6506739
    Abstract: Bis-(N,N′-bis-(2-haloethyl)amino)phosphoramidates, pharmaceutical compositions containing them, methods of treatment using them, and processes for their preparation. The compounds possess anti-tumor activities or are capable of being modified to have anti-tumor activities; and this invention relates to the use of the compounds in methods for the treatment of tumors and, especially, for the treatment of cancer.
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: January 14, 2003
    Assignee: Telik, Inc.
    Inventors: R. Jason Herr, Robert T. Lum, Steven R. Schow, Fanying Meng, Michael R. Kozlowski, Pavel Zhichkin
  • Patent number: 6459003
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: October 1, 2002
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Publication number: 20020058644
    Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme.
    Type: Application
    Filed: December 21, 2000
    Publication date: May 16, 2002
    Inventors: Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Cheuk Kun Lau, Chun Sing Li, Patrick Roy, Michel Therien, John Scheigetz, Zhaoyin Wang
  • Publication number: 20020026049
    Abstract: Compounds of the formula I 1
    Type: Application
    Filed: May 31, 2001
    Publication date: February 28, 2002
    Inventors: Jean-Pierre Wolf, Gebhard Hug
  • Patent number: 6329547
    Abstract: The present invention provides compounds represented by the following general formula [I] and salts thereof, which are useful as therapeutic agents for glaucoma, wherein R1 is H, lower alkyl or phenyl, and the phenyl can be substituted by lower alkyl, hydroxy, lower alkoxy, halogen, nitro or phenyl; R2 and R3, being the same or different, are H, halogen or lower alkyl; R4 and R5, being the same or different, are H, lower alkyl or carboxyl or ester thereof; and R6 is carboxyl or phosphono or ester thereof.
    Type: Grant
    Filed: November 22, 2000
    Date of Patent: December 11, 2001
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Eiichi Shirasawa, Koji Konomi, Masaki Ichikawa, Hiroshi Suhara
  • Patent number: 6255518
    Abstract: A method for the preparation of a fluorinated Phosphonate having the formula (RO)2PO CFR′R″ comprises treating a phosphonate of the formula (RO)2PO CHR′R″, or a metal salt thereof, with fluorine. R is an alkyl group R′ is hydrogen or alkyl and R″ is hydrogen, alkyl or another group.
    Type: Grant
    Filed: March 20, 2000
    Date of Patent: July 3, 2001
    Assignee: F2 Chemicals, Limited
    Inventors: Richard Dickinson Chambers, John Hutchinson
  • Patent number: 5973180
    Abstract: The present invention relates to an improved process for the preparation of an acyl derivative of O,S-dialkyl phosphoroamidothioate by reacting an O,S-dialkyl phosphoroamidothioate with an acylating agent in the presence of an acid, wherein the improvement resides in adding a C.sub.4 to C.sub.8 aliphatic alcohol, following completion of the acylation reaction, to the mixture of the N-acyl-O,S-dialkyl phosphoroamidothioate, the acylating agent and the acid. In an embodiment of the present invention, the acylation reaction is conducted in the absence of a solvent. The aliphatic alcohol is easily recovered and can be reused in a subsequent acylation reaction.
    Type: Grant
    Filed: August 31, 1998
    Date of Patent: October 26, 1999
    Assignee: Bayer Corporation
    Inventors: Vijay C. Desai, David T. Erdman, Klaus Jelich, Peter E. Newallis
  • Patent number: 5807846
    Abstract: The present invention is directed to compounds useful for the regulation of cholesterol of Formula I, methods for using them and pharmaceutical compositions thereof, ##STR1## wherein Ar and Ar.sup.1 are each independently selected from unsubstituted or substituted phenyl which substituents are from 1-5 in number and are each independently selected from alkyl, alkoxy, hydroxy, halogen, nitro, trifluoromethyl, COOH, and COOalkyl;X is --NH--, --O--, --S--, or --(CH.sub.2).sub.0-4 --, andR is hydrogen, alkyl, or phenyl.
    Type: Grant
    Filed: June 24, 1997
    Date of Patent: September 15, 1998
    Assignee: Warner-Lambert Company
    Inventors: William Howard Roark, Bruce David Roth
  • Patent number: 5698540
    Abstract: A liquid pesticidal composition including Acephate and one or more N-alkyl-2-pyrrolidones, and methods for stabilizing and inhibiting decomposition of Acephate by adding one or more N-alkyl-2-pyrrolidones to Acephate. The storage stability of Acephate bulk or Acephate in an Acephate-containing liquid pesticidal composition is improved by addition of the N-alkyl-2-pyrrolidone(s).
    Type: Grant
    Filed: February 10, 1995
    Date of Patent: December 16, 1997
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yasuyuki Katayama, Toshiro Ohtsubo
  • Patent number: 5686633
    Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.
    Type: Grant
    Filed: December 31, 1991
    Date of Patent: November 11, 1997
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Eric Vieira, Hugh Stephen Laver
  • Patent number: 5684174
    Abstract: A method for purifying O,S-dimethyl N-acetyphosphoramidothioate, which is characterized by subjecting a crude crystal of O,S-dimethyl N-acetylphosphoramidothioate to recrystallization by using a two-phase solvent system comprising water and an organic which is an aromatic hydrocarbon, an aliphatic carboxylic acid ester or aliphatic ketone, wherein the amount of water is 0.1 to 2 parts by weight and the amount of the organic solvent is 1 to 20 parts by weight to 1 part by weight of the crude O,S-dimethyl N-acetylphosphoramidothioate.
    Type: Grant
    Filed: September 26, 1996
    Date of Patent: November 4, 1997
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yoji Sakito, Mamoru Shirahata, Yujiro Kiyoshima, Kazuya Minamisaka, Atukazu Iwata
  • Patent number: 5616769
    Abstract: A method for purifying O,S-dimethyl N-acetyphosphoramidothioate, which is characterized by subjecting a crude crystal of O,S-dimethyl N-acetylphosphoramidothioate to recrystallization by using a two-phase solvent system comprising water and an organic which is an aromatic hydrocarbon, an aliphatic carboxylic acid ester or aliphatic ketone, wherein the amount of water is 0.1 to 2 parts by weight and the amount of the organic solvent is 1 to 20 parts by weight to 1 part by weight of the crude O,S-dimethyl N-acetylphosphoramidothioate.
    Type: Grant
    Filed: September 21, 1995
    Date of Patent: April 1, 1997
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yoji Sakito, Mamoru Shirahata, Yujiro Kiyoshima, Kazuya Minamisaka, Atukazu Iwata
  • Patent number: 5616745
    Abstract: New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6 R represents a radical ##STR2## (R.sub.1 and R.sub.2 : aliphatic radical containing 12 to 22 carbon atoms; R: hydrogen atom or alkyl radical optionally substituted with phenyl), or a radical ##STR3## (X=CH.sub.2, CO; R.sub.3 and R.sub.4 aliphatic radical containing 11 to 21 carbon atoms), their preparation and their use.The lipopolyamines of general formula (I) are especially useful as vectors for the transfection of eukaryotic cells.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 1, 1997
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Jean-Paul Behr, Jean-Philippe Loeffler
  • Patent number: 5574025
    Abstract: The compounds disclosed inhibit the prenylation of several proteins. These compounds are potent inhibitors of famesyl-protein transferase and geranylgeranyl-protein transferase. Further contained in this invention are chemotherapeutic compositions containing these prenyl-transferase inhibitors and methods for their production.
    Type: Grant
    Filed: October 26, 1994
    Date of Patent: November 12, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Charles A. Omer
  • Patent number: 5532402
    Abstract: Disclosed herein is a process for producing an optically active hydroxyalkylphosphonate represented by the formula (4), which comprises asymmetrically hydrogenating an oxoalkylphosphonate represented by the formula (1) using, as a catalyst, a ruthenium-optically active phosphine complex represented by the formula (2).
    Type: Grant
    Filed: March 13, 1995
    Date of Patent: July 2, 1996
    Assignee: Takasago International Corporation
    Inventors: Ryoji Noyori, Masato Kitamura, Makoto Tokunaga
  • Patent number: 5508273
    Abstract: Compounds represented by the formula I: ##STR1## are disclosed as agents for use in treating bone wasting diseases.
    Type: Grant
    Filed: December 30, 1993
    Date of Patent: April 16, 1996
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Scott Beers, Elizabeth A. Malloy, Charles Schwender
  • Patent number: 5504236
    Abstract: The preparation of .alpha.-carbonylphosphine oxides by oxidizing an .alpha.-hydroxyalkyl phosphine oxide with an organic hydroperoxide or of an organic peroxy acid in the presence of a compound of a Group IV to Group VIII metal in the periodic table, and novel .alpha.-hydroxybenzyl phosphine oxides..alpha.-Carbonylphosphine oxides are used as photoinitiators for polymerizable compositions.
    Type: Grant
    Filed: September 7, 1993
    Date of Patent: April 2, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Martin Fischer, Eckhard Hickmann, Rudolf Kropp, Jochen Schroeder, Beate Trentmann
  • Patent number: 5488043
    Abstract: The present invention relates to a method for stabilizing acephate which comprises adding a sodium salt of condensed phosphate and/or a synthetic silicic acid in which the surface silanol groups being alkylsilylated to acephate or acephate-containing dry pesticidal formulation and a stabilized acephate having added a sodium salt of condensed phosphate and/or a synthetic silicic acid in which the surface silanol groups being alkylsilylated.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: January 30, 1996
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Masahiro Yamada, Yasuyuki Katayama, Toshiro Ohtsubo
  • Patent number: 5463181
    Abstract: The present invention relates to certain inhibitors of farnesyl:protein transferase which are useful as antineoplastic agents.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: October 31, 1995
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: David M. Stemerick
  • Patent number: 5459149
    Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: October 17, 1995
    Assignee: Roussel Uclaf
    Inventors: John E. Robinson, George S. Cockerill
  • Patent number: 5451573
    Abstract: Substituted cyclohexane derivatives for the treatment of diseases Esters of cyclohexane derivatives of the formula I ##STR1## in which A--B, R.sup.3, R.sup.4, R.sup.5, Y and Z have the meanings indicated, for use as inhibitors of the glucose-6-phosphatase system of the liver in mammals are described. The compounds are suitable for the production of pharmaceutical preparations.
    Type: Grant
    Filed: September 7, 1993
    Date of Patent: September 19, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Horst Hemmerle, Peter Schindler, Roland Utz, Robert Rippel, Andreas Herling
  • Patent number: 5352822
    Abstract: The present invention discloses pesticidally active compounds of formula (II) ##STR1## or a salt thereof, wherein Q is an monocyclic aromatic ring, or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each ring system being optionally substituted, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; R.sup.2, R.sup.3 , R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; and R.sup.1 is selected from hydrogen and C.sub.1-8 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy and X.sup.1 is hydrogen, fluoro or chloro.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: October 4, 1994
    Assignee: Roussel Uclaf
    Inventors: Robert J. Blade, George S. Cockerill, John E. Robinson
  • Patent number: 5242908
    Abstract: The use of a compound of the formula I ##STR1## in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R.sup.1 and R.sup.2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R.sup.1 and R.sup.2 together form a cyclic diester, R.sup.3 and R.sup.4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.
    Type: Grant
    Filed: February 1, 1991
    Date of Patent: September 7, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Anuschirwan Peyman, Eugen Uhlmann, Karlheinz Budt, Jochen Knolle, Irvin Winkler, Matthias Helsberg
  • Patent number: 5210110
    Abstract: Silylated acylphosphine oxides of formula I ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 are defined in the specification, are highly suitable as photoinitiators for the photopolymerization of compounds which can be polymerized by means of free radicals, namely ethylenically unsaturated compounds.
    Type: Grant
    Filed: November 18, 1991
    Date of Patent: May 11, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Werner Rutsch, Rinaldo Husler
  • Patent number: 5200546
    Abstract: There are disclosed novel compounds of the formula: ##STR1## wherein, x is --CH.sub.2 --, --CHF--, --CF.sub.2, --CHOH-- or --C(O)--;R.sup.6 is hydrogen, benzyl, pentafluorophenyl, nitrophenyl, 1-benzotriazolyl or 1-succinimidoyl;Fmoc is 9-fluorenylmethyloxycarbonyl; and* indicates a chiral carbon atom.The Formula (I) compounds are useful in synthesizing peptides. There are also disclosed novel synthesis methods which include the step of hydrogenating a compound of the Formula ##STR2## wherein R.sup.4 and R.sup.5 are C.sub.1-8 lower alkyl, to give a compound of the formula ##STR3## wherein R.sup.4 and R.sup.5 are as defined above. The compounds of formula (II) are useful as intermediates in preparing certain formula (I) compounds.
    Type: Grant
    Filed: September 30, 1991
    Date of Patent: April 6, 1993
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Terrence R. Burke, Jr., Benjamin B. Lim
  • Patent number: 5166144
    Abstract: The invention relates to new O-halogenocyclobutyl S-alkyl (di)thiophosphoric acid ester-amides of the general formula (I) ##STR1## in which A represents fluorine or chlorine,B represents hydrogen or alkyl,X represents oxygen or sulphur,R.sup.1 represents hydrogen, alkyl, --COH (formyl) or --CO-alkyl (acyl) which is optionally substituted by halogen,R.sup.2 represents hydrogen or alkyl, andR.sup.3 represents alkyl or alkoxyalkyl,which can be used as agents for combating pests.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: November 24, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Kruger, Dietmar Bielefeldt, Karl-R. Gassen, Jurgen Hartwig, Wilhelm Stendel, Christoph Erdelen
  • Patent number: 5164383
    Abstract: O-Halogenocyclopentyl S-alkyl (di)thiphosphoric(phosphonic) acid ester derivatives of the general formula (I) ##STR1## in which R.sup.1 represents alkyl, alkoxy or the radical ##STR2## R.sup.3 represents hydrogen or alkyl and R.sup.4 represents hydrogen, alkyl, --COH (formyl) or optionally halogen-substituted --CO-alkyl (acyl),R.sup.2 represents alkyl or alkoxyalkyl andX represents oxygen or sulphur,can be used as pesticides.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: November 17, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Kruger, Michael Negele, Jurgen Hartwig, Christoph Erdelen, Wilhelm Stendel
  • Patent number: 5100654
    Abstract: A phosphorylated derivative of L-dopa of the formula ##STR1## wherein when X is ##STR2## wherein Z is --CH.sub.2, N, S or a linkage other than oxygen which renders the phosphate group resistant to hydrolysis by phosphatase enzymes in tissues and biological fluids,then Y is OQ, wherein Q is H or an alkyl with one to twelve carbon atoms, orwherein X is OQ, then Y is ##STR3## wherein R' is hydrogen or a pharmaceutically acceptable cation and R is a moiety which increases hydropobicity. The phosphorylated derivative of L-dopa is useful as an agent to increase the melanin content in mammalian skin and hair.
    Type: Grant
    Filed: April 7, 1989
    Date of Patent: March 31, 1992
    Assignee: Yale University
    Inventors: John M. Pawelek, Michael P. Osber
  • Patent number: 5047158
    Abstract: Hydrocarbon compositions, including oligomers and polymers, for use in improving the thermo-oxidative stability and the dispersancy and viscosity index improvement (for high molecular weight) properties of fuels and lubricating oils are disclosed. These compositions are adducts of sulfur mono- and diimides having one of the following formulae: ##STR1## wherein R is a hydrocarbycontaining at least 18 carbon atoms, in which X.dbd. can be O.dbd., S.dbd., Y'--N.dbd., i is 0 or 1, --Y and Y'-- can be ##STR2## wherein R' is hydrocarbyl or hydrocarbyloxy, R" is hydrocarbyl, R'" and R"" are hydrocarbyloxy, and each of R', R", R'", and R"" is from from 1 to 20 carbon atoms.
    Type: Grant
    Filed: August 10, 1989
    Date of Patent: September 10, 1991
    Assignee: Exxon Chemical Patents Inc.
    Inventor: Stanley J. Brois
  • Patent number: 5037813
    Abstract: A compound of Formula (I):R.sup.1 (CA.dbd.CA.sup.1).sub.x --C(.dbd.X)NR.sup.2 R.sup.3(I)where R.sup.1 is alkyl optionally substituted by a group selected from alkoxy, alkenyl, alkynyl, alkenyloxy, alkynyloxy, aryl, aryloxy, arylalkoxy and cycloalkyl fused to an aryl ring; x=1 or 2; X=O or S; each A and A.sup.1 is independently hydrogen, alkyl or haloalkyl; R.sup.2 is alkyl, alkenyl or cycloalkyl any of which may be substituted by halo, alkenyl, alkyl, cycloalkyl, alkynyl, dioxalanylalkyl or alkoxy; and R.sup.3 is selected from groups (A) to (D):(A) --Y.dbd.X.sup.1 --(R.sup.4).sub.a where X.sup.1 is O or S, Y is phosphorus or carbon, R.sup.4 is hydrogen, alkyl, alkoxy, acyl or CO.sub.2 R.sup.5 is alkyl or aryl, and a is 1 or 2.(B) --S(R.sup.6)(O).sub.bwhere R.sup.6 alkyl, aryl, aryloxy, alkoxy, thioalkoxy, thioaryl, alkythio, alkoxythio or arylthio and b is 0, 1 or 2(C) --S(O).sub.c NR.sup.7 R.sup.8where c is 0, 1 or 2, R.sup.7 is --COR.sup.9 or --CO.sub.2 R.sup.9 where R.sup.
    Type: Grant
    Filed: December 11, 1986
    Date of Patent: August 6, 1991
    Assignee: Burroughs Wellcome Co.
    Inventors: Malcolm H. Black, Robert J. Blade, Robert J. Peek
  • Patent number: 4977293
    Abstract: Monoethylenically unsaturated compounds whose polymers are useful as polymeric photoinitiators are of formula Ar.sup.1 COC(R.sup.1)(R.sup.2)R.sup.3 where R.sup.1 is (C.sub.1 -C.sub.10 alkyl or alkoxy, R.sup.2 is C.sub.1 -C.sub.10 alkyl, --X--O--R.sup.4 -OCOC(R.sup.5).dbd.CH.sub.2 (II) --X--NH--R.sup.6 --OCOC(R.sup.5).dbd.CH.sub.2 (III), or --CH.sub.2 [OCH.sub.2 CH(OH)CH.sub.2 ].sub.a OCOC(R.sup.5).dbd.CH.sub.2 (IIIA) or R.sup.1 and R.sup.2, together with the attached carbon, denote C.sub.4 -C.sub.8 cycloalkyl, R.sup.3 is a C.sub.6 -C.sub.20 aromatic group, OH tert. amino,--OCOC(R.sup.5).dbd.CH.sub.2 (VI) or --OCH.sub.2 CH(OH)CH.sub.2 OCOC(R.sup.5).dbd.CH.sub.2 (VIA), R.sup.4 is C.sub.1 14 C.sub.4 alkylene, which may be substituted by --OH or by C.sub.2 -C.sub.20 acyloxy, R.sup.5 is H or C.sub.1 -C.sub.4 alkyl, R.sup.6 is C.sub.1 to C.sub.4 alkylene, X is a group of formula R.sup.7 CO-- or ##STR1## where R.sup.7 is C.sub.1 -C.sub.4 alkylene, R.sup.8 is C.sub.1 to C.sub.4 alkyl, and is 0 or 1, Ar.sup.1 is a C.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: December 11, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Kevin B. Hatton, Edward Irving, Josephine M. A. Walshe, Anne Mallaband