The -c(=x)x- Group Is In A Substituent Attached To The Ring Nitrogen Of The Five-membered Hetero Ring (e.g., Beta-pyrrolidyl Ethyl Ester Of Benzoic Acid, Etc.) Patents (Class 548/573)
  • Patent number: 9006457
    Abstract: The invention relates to reactive ionic liquids containing organic cations with groups or substituents which are susceptible to electrochemical reduction and anions obtained from fluoroalkyl phosphates, fluoroalkyl phosphinates, fluoroalkyl phosphonates, acetates, triflates, imides, methides, borates, phosphates and/or aluminates, for use in electrochemical cells, such as lithium ion batteries and double-layer capacitors.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: April 14, 2015
    Assignee: BASF SE
    Inventors: Michael Schmidt, Nikolai (Mykola) Ignatyev, William-Robert Pitner
  • Patent number: 8470871
    Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: June 25, 2013
    Assignee: Galderma Research & Development
    Inventors: Thibaud Biadatti, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
  • Patent number: 8460851
    Abstract: A salt represented by the formula (I): wherein Q1 and Q2 each independently represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents *—CO—O-La- or *—CH2—O-Lb-, * represents a binding position to —C(Q1)(Q2)-, La and Lb independently represent a C1-C15 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, ring W1 represents a C2-C36 nitrogen-containing heterocyclic group in which one or more —CH2— can be replaced by —O—, and Z1? represents an organic counter ion.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: June 11, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Satoshi Yamaguchi, Koji Ichikawa
  • Publication number: 20120190854
    Abstract: A method includes reacting an amino group, a composition including rhodium and an organic ligand, and a substrate having structural formula (I) in a reaction mixture. R1 is an organic group including a sp3 carbon atom bonded to CA. R2 is selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CA. R3 and R4 independently are selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CB. The method further includes forming a hydroaminated product in the reaction mixture.
    Type: Application
    Filed: April 5, 2012
    Publication date: July 26, 2012
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Akihiro Takemiya, Zhijian Liu, John F. Hartwig
  • Patent number: 8227507
    Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: July 24, 2012
    Assignee: Galderma Research & Development
    Inventors: Thibaud Biadatti, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
  • Patent number: 8211882
    Abstract: The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: July 3, 2012
    Inventors: Richard Delarey Wood, William J Welsh, Sean Ekins, Ni Ai
  • Publication number: 20110171576
    Abstract: A salt represented by the formula (I): wherein Q1 and Q2 each independently represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents *—CO—O-La- or *—CH2—O-Lb-, * represents a binding position to —C (Q1) (Q2)-, La and Lb independently represent a C1-C15 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, ring W1 represents a C2-C36 nitrogen-containing heterocyclic group in which one or more —CH2— can be replaced by —O—, and Z1? represents an organic counter ion.
    Type: Application
    Filed: January 6, 2011
    Publication date: July 14, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Satoshi YAMAGUCHI, Koji ICHIKAWA
  • Publication number: 20110045359
    Abstract: The invention relates to reactive ionic liquids containing organic cations with groups or substituents which are susceptible to electrochemical reduction and anions obtained from fluoroalkyl phosphates, fluoroalkyl phosphinates, fluoroalkyl phosphonates, acetates, triflates, imides, methides, borates, phosphates and/or aluminates, for use in electrochemical cells, such as lithium ion batteries and double-layer capacitors.
    Type: Application
    Filed: March 31, 2009
    Publication date: February 24, 2011
    Applicant: MERCK PATENT GESELLSCHAFT
    Inventors: Michael Schmidt, Nikolai (Mykola Ignatyev, William-Robert Pitner
  • Publication number: 20100298341
    Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Application
    Filed: December 11, 2008
    Publication date: November 25, 2010
    Inventors: Stephen A. Hitchcock, Wenyuan Qian, Albert Amegadzie
  • Patent number: 7807708
    Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: October 5, 2010
    Assignee: Galderma Research & Development
    Inventors: Thibaud Biadatti, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
  • Publication number: 20090239919
    Abstract: The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds.
    Type: Application
    Filed: March 6, 2009
    Publication date: September 24, 2009
    Inventors: Richard Delarey Wood, William J. Welsh, Sean Ekins, Ni Ai
  • Publication number: 20090163462
    Abstract: The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
    Type: Application
    Filed: June 11, 2008
    Publication date: June 25, 2009
    Applicant: deCODE genetics, ehf
    Inventors: Vincent SANDANAYAKA, Jasbir Singh, Mark Gurney, Bjorn Mamat, Peng Yu, Louis Bedell, Lei Zhao, Rama K. Mishra
  • Publication number: 20090010860
    Abstract: Disclosed is the use of the compounds of formula wherein Q is —OH; —OR7; —NH2; —NHR7; —NR7R8; or —N?R9; T is —COR5; —CN; or —SO2—(C6-C12)aryl; R1 is hydrogen; —OR7, —SR7; —NHR7; —NR7R8; C1-C22alkyl; C2-C12Alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl, C2-C11heteroaralkyl; C6-C10aryl; or C1-C9heteroaryl; R2 and R3 independently from each other are C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl, C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl; C3-C12cycloheteroalkyl; C2-C11heteroaralkyl, C6-C10aryl; or C1-C9heteroaryl; R4 is cyano; COR7, COOR7; CONH2; CONHR7; CONR7R8; SO2(C6-C12)aryl, C2-C12alk-1-enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl, C3-C5heterocycloalkyl, C6-C10aryl; or C1-C9heteroaryl; R5 is —COR7; —COOR7; —OR7; —SR7, —NHR7, —NR7R8; C2-C12alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12alkylphenyl; C1-C12alkoxy-C8-C10aryl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C
    Type: Application
    Filed: June 20, 2005
    Publication date: January 8, 2009
    Inventors: Barbara Wagner, Frank Bienewald, Heinz Wolleb, Olof Wallquist, Bernd Herzog, Thomas Ehlis, Jurg Haase
  • Publication number: 20080221322
    Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline.
    Type: Application
    Filed: October 31, 2007
    Publication date: September 11, 2008
    Applicant: AstraZeneca AB
    Inventors: Euan Alexander Arnott, John Crosby, Mathew Charles Evans, James Gair Ford, Martin Francis Jones, Kevin William Leslie, Ian Michael McFarlane, George Joseph Sependa
  • Patent number: 7312343
    Abstract: Compounds of formula I and a process for the preparation of such compounds are disclosed.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: December 25, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rudolf Schmid, Ulrich Zutter
  • Patent number: 7141560
    Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.
    Type: Grant
    Filed: January 17, 2002
    Date of Patent: November 28, 2006
    Assignee: Akzo Nobel N.V.
    Inventors: Niall Morton Hamilton, David Jonathan Bennett
  • Patent number: 6906046
    Abstract: Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-? and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: June 14, 2005
    Assignee: Celltech R & D Inc.
    Inventors: Randy W. Jackson, Ihab Darwish, Ted A. Baughman, J. Jeffry Howbert
  • Patent number: 6794511
    Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: September 21, 2004
    Assignee: G. D. Searle
    Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo, Clara I. Villamil
  • Patent number: 6749988
    Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.
    Type: Grant
    Filed: November 28, 2001
    Date of Patent: June 15, 2004
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
  • Publication number: 20040087791
    Abstract: Compounds of the formula I, in which M, A1, A2, K1 and K2 have the meanings given in the description are novel effective tryptase inhibitors.
    Type: Application
    Filed: August 6, 2003
    Publication date: May 6, 2004
    Inventor: Thomas Martin
  • Patent number: 6680336
    Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Grant
    Filed: February 15, 2002
    Date of Patent: January 20, 2004
    Assignee: ICOS Corporation
    Inventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Laurence E. Burgess, Stephen T. Schlachter
  • Publication number: 20030166963
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Application
    Filed: November 20, 2002
    Publication date: September 4, 2003
    Inventors: Li Deng, Jianfeng Hang, Liang Tang
  • Publication number: 20030149270
    Abstract: The present invention relates to novel processes for the preparation of optically active 3-aminocarboxylic acids and their esters, in particular processes for the preparation of optically active compounds of the formula IA or IB 1
    Type: Application
    Filed: December 6, 2002
    Publication date: August 7, 2003
    Inventors: Kai-Uwe Schoning, Martin Studer, Hans Jurg Kirner, Stephan Burkhardt
  • Publication number: 20020183386
    Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N-CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.
    Type: Application
    Filed: June 7, 2002
    Publication date: December 5, 2002
    Inventors: Karl E. Gierskcky, Johan Moan, Qian Peng, Harald Steen, Trond Warloe, Alf Bjorseth
  • Patent number: 6409995
    Abstract: Use of amino-substituted hydroxybenzophenones of the formula I in which the variables have the meanings explained in the description, as photostable UV filters in cosmetic and pharmaceutical preparations for protecting human skin or human hair from the sun's rays, alone or together with compounds which absorb in the UV region and are known per se for cosmetic and pharmaceutical preparations.
    Type: Grant
    Filed: April 20, 2000
    Date of Patent: June 25, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Thorsten Habeck, Frank Prechtl, Thomas Wünsch, Horst Westenfelder, Sylke Haremza, Thorsten Bach, Anja Spiegel
  • Patent number: 6407135
    Abstract: In accordance with the present invention, there are provided conjugates of nitric oxide scavengers (e.g., dithiocarbamates, or “DC”) and pharmacologically active agents (e.g., NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of nitric oxide overproduction induced thereby as a result of the co-production of nitric oxide scavenger (e.g., dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.
    Type: Grant
    Filed: December 3, 1999
    Date of Patent: June 18, 2002
    Assignee: Medinox, Inc.
    Inventors: Ching-San Lai, Tingmin Wang
  • Patent number: 6288063
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 27, 1998
    Date of Patent: September 11, 2001
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, David Ross Brittelli, William Riley Schoen, Sookhee Nicole Ha
  • Patent number: 6207828
    Abstract: This invention provides a convenient, new, one step process for the preparation of 2-(trihaloacetyl)-3-(substituted amino)-2-propenoates and related derivatives thereof by reaction of carbonyl compounds substituted with a trihaloacetyl group with an acetal in the presence of an organic acid. The resulting propenoates are useful as intermediates for the construction of trihalomethyl substituted heterocyclic compounds for use in pharmaceutical and agricultural applications.
    Type: Grant
    Filed: November 4, 1999
    Date of Patent: March 27, 2001
    Assignee: Rolm and Haas Company
    Inventor: Peter Osei-Gyimah
  • Patent number: 6075146
    Abstract: The invention relates to intermediates and processes for producing benzothiophenes employing hydroxylamines.
    Type: Grant
    Filed: July 28, 1998
    Date of Patent: June 13, 2000
    Assignee: Eli Lilly and Company
    Inventor: Erik Christopher Chelius
  • Patent number: 5939268
    Abstract: This invention features methods of synthesizing combinatorial libraries of chemical compounds, and combinatorial libraries of chemical compounds formed by the methods of this invention. Specifically, Diels-Alder chemistry is utilized to generate libraries of diverse molecules which are easily differentially functionalized with various chemical moities and in one aspect are configured to act as non-hydrolyzable peptidomimetics.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: August 17, 1999
    Assignee: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Patent number: 5916910
    Abstract: In accordance with the present invention, there are provided conjugates of nitric oxide scavengers (e.g., dithiocarbamates, or "DC") and pharmacologically active agents (e.g., NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of nitric oxide overproduction induced thereby as a result of the co-production of nitric oxide scavenger (e.g., dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.
    Type: Grant
    Filed: June 4, 1997
    Date of Patent: June 29, 1999
    Assignee: Medinox, Inc.
    Inventor: Ching-San Lai
  • Patent number: 5863903
    Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.
    Type: Grant
    Filed: March 14, 1995
    Date of Patent: January 26, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Karsten Lundgren, Ole Kirk
  • Patent number: 5686586
    Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis.In the formula, X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: November 11, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
  • Patent number: 5631369
    Abstract: Novel processes for producing compounds of formula I ##STR1## wherein R.sup.1 and R.sup.2 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; andn is 2 or 3;or a pharmaceutically acceptable salt thereof employing alkylacetate solvents are provided.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: May 20, 1997
    Assignee: Eli Lilly and Company
    Inventors: Douglas P. Kjell, Fred M. Perry
  • Patent number: 5594150
    Abstract: Process for the preparation of a hydroxylated secondary or tertiary amine compound having a hydroxyl function .beta. to the amine function, according to which a primary or secondary amine compound is reacted with a compound containing an epoxy function in the presence of a phase transfer catalyst.
    Type: Grant
    Filed: July 6, 1994
    Date of Patent: January 14, 1997
    Assignee: Chemoxal S.A.
    Inventors: Catherine David, Gilles Teral, Henry Ledon, Jean-Pierre Boiteux
  • Patent number: 5446192
    Abstract: .beta.-Aminoacrylic acid esters can be prepared by reacting acetic acid esters of the formulaH.sub.2 CR.sub.1 --COOR.sup.2 (II)with aminal esters of the formula ##STR1## at 0.5-10 bar and 50.degree.-170.degree. C. in an aprotic polar solvent. The radicals R.sup.1 to R.sup.7 are as defined in the description.
    Type: Grant
    Filed: March 3, 1993
    Date of Patent: August 29, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Helmut Kraus, Heinz-Ulrich Blank, Gerhard Marzolph
  • Patent number: 5423998
    Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.
    Type: Grant
    Filed: April 13, 1993
    Date of Patent: June 13, 1995
    Assignee: Ausimont S.r.l.
    Inventors: Carlo Venturello, Claudio Cavallotti
  • Patent number: 5344934
    Abstract: The present invention provides a process for preparing urethanes and carbonates from an amine or an alcohol, carbon dioxide and a hydrocarbyl halide. The amine or alcohol is reacted with carbon dioxide in a suitable solvent system and in the presence of an amidine or guanidine base, to form the ammonium carbamate or carbonate salt which is then reacted in a polar aprotic solvent with a hydrocarbyl halide. Polymer products can also be prepared utilizing this process or utilizing the resulting urethanes and carbonates under standard polymerization conditions.
    Type: Grant
    Filed: November 16, 1992
    Date of Patent: September 6, 1994
    Assignee: Monsanto Company
    Inventors: William D. McGhee, Dennis P. Riley, John J. Talley, Barry L. Parnas
  • Patent number: 5103007
    Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.
    Type: Grant
    Filed: October 27, 1989
    Date of Patent: April 7, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
  • Patent number: 5081245
    Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.
    Type: Grant
    Filed: August 18, 1989
    Date of Patent: January 14, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
  • Patent number: 5039673
    Abstract: Compounds are described of the formula (1) ##STR1## where: R.sup.1 is a hydrogen atom or a methyl group;X is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --, m is 2, 3 or 4 and n is 1; or X is trans --CH.dbd.CH--, m is zero and n is 3;Y is a saturated heterocyclic amino group;Alk is a C.sub.1-5 alkyl chain;l is zero or 1;p is zero, 1, 2, 3 or 4;R.sup.2 is a hydroxyl group or a group selected from --OCOR.sup.3, --CO.sub.2 R.sup.3, CONR.sup.3 R.sup.4, --SO.sub.2 NR.sup.3 R.sup.4, --NHCOR.sup.3, --NHSO.sub.2 R.sup.5, --SO.sub.2 R.sup.5, --SR.sup.5, --NR.sup.3 R.sup.4, --COR.sup.5, --NHCONR.sup.3 R.sup.4 and --NHCSNH.sub.2 ; and their physiologically acceptable salts, solvates and cyclodextrin complexes.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction and may be formulated for use as antithrombotic agents.
    Type: Grant
    Filed: August 22, 1989
    Date of Patent: August 13, 1991
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Harry Finch, Roger Hayes, Keith Mills, David F. Woodings
  • Patent number: 5010200
    Abstract: This invention provides novel insecticidally and acaricidally active pyrimidine derivatives of formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is selected from alkyl; alkenyl; alkynyl; haloalkyl; haloalkenyl; and cycloalkyl optionally substituted by alkyl or halogen;R.sup.2 is selected from alkyl; haloalkyl; alkoxy; alkylamino; dialkylamino; halogen; cycloalkyl optionally substituted by halogen or alkyl; and phenyl optionally substituted by alkyl, haloalkyl, halogen or alkoxy;R.sup.3 is selected from hydrogen and halogen;R.sup.4 is the residue of an alcohol of formula R.sup.4 -OH which forms an insecticidal ester when combined with chrysanthemic acid, permethrin acid or cyhalothrin acid; andX is selected from oxygen and sulphur.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: April 23, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: Edward McDonald, Roger Salmon, Alan J. Whittle, Michael G. Hutchings
  • Patent number: 4999361
    Abstract: The present invention provides compounds of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical, a C.sub.3 -C.sub.7 -cycloalkyl radical, a straight-chained or branched C.sub.2 -C.sub.12 -alkenyl radical or an unsubstituted or substituted C.sub.3 -C.sub.7 -mono- or bicycloalkenyl radical, an unsubstituted or singly or multiple substituted monocyclic aromatic or heteroaromatic radical, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained, branched, saturated or unsaturated C.sub.1 -C.sub.6 -aliphatic radicals or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and can optionally be substituted by a lower alkyl radical, a lower alkoxy radical or an oxygen atom, R.sub.4 is an unsubstituted or singly or multiple substituted monocyclic aromatic radical, an unsubstituted or substituted five- or six-membered heteroaromatic ring, R.
    Type: Grant
    Filed: February 27, 1989
    Date of Patent: March 12, 1991
    Assignee: Boehringer Mannheim GmbH
    Inventors: Christos Tsaklakidis, Herbert Leinert, Peter Freund
  • Patent number: 4988817
    Abstract: A process is provided for obtaining quaternary ammonium or phosphonium substituted carbonic acid esters. The first step involves reacting the hydroxyl predecessor compound of the ester with phosgene in an aprotic organic solvent to obtain a solution of chloroformate/hydrogen chloride complex. In a second step, the chloroformate/hydrogen chloride complex in solution is admixed with a salt whose conjugate anion, normally a phenol sulfonate, has structure L. During the admixing step, pH is maintained no lower than 6 until all reactants have been combined to form the product ester. Thereupon, pH is lowered to less than 5.5 to stabilize product against hydrolysis.
    Type: Grant
    Filed: November 16, 1988
    Date of Patent: January 29, 1991
    Assignee: Lever Brothers Company, Division of Conopco, Inc.
    Inventors: Stephen A. Madison, Jeffrey Bonn, Eddie N. Gutierrez
  • Patent number: 4987130
    Abstract: Substituted amino derivatives represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each stand for an acyclic hydrocarbon residue or an alicyclic hydrocarbon residue; R.sup.3 and R.sup.4 each stand for hydrogen or a hydrocarbon residue optionally containing hetero-atom(s); A stands for a carbon chain having two or more carbon atoms optionally containing ether linkage or sulfide linkage, which may be substituted and which may per se form a ring; X.sup.1 and X.sup.2 each stand for oxygen atom or sulfur atom; and Y stands for amino group or an organic residue bonded through nitrogen atom, which may form a ring by combining with a carbon atom constituting A; and their salts have anti-arrhythmic activity and are useful for prevention and treatment of a variety of arrhythmias.
    Type: Grant
    Filed: December 22, 1989
    Date of Patent: January 22, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Susumu Tsushima, Muneo Takatani, Minoru Hirata
  • Patent number: 4985561
    Abstract: A process is described for obtaining sulfophenyl quaternary ammonium or phosphonium substituted carbonic acid esters. These esters are prepared through sulfonation with sulfur trioxide of aromatic chloroformates followed by reaction of the sulfonated aromatic chloroformate with quaternary ammonium or phosphonium substituted alcohols. The resultant sulfophenyl esters are useful as bleach precursors in combination with peroxygen compounds such as sodium perborate or percarbonate.
    Type: Grant
    Filed: August 29, 1989
    Date of Patent: January 15, 1991
    Assignee: Lever Brothers Company, Division of Conopco, Inc.
    Inventors: Stephen A. Madison, Leonora M. Ilardi, Hans Cerfontain
  • Patent number: 4980378
    Abstract: Biodegradable absorption enhancers, especially useful in pharmaceutical formulations, are compounds having the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl, benzyl or 4-hydroxybenzyl; n is a whole number from 4 to 18 inclusive; R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 -C.sub.7 alkyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are combined to form a substituted or unsubstituted heterocycloalkyl radical having a total of 5 to 7 ring atoms, optionally including a hetero ring atom selected from oxygen, sulfur and nitrogen in addition to the indicated nitrogen atom, the substituents when present being one to three C.sub.1 -C.sub.7 alkyl radicals, which may be the same or different; and R.sub.3 and R.sub.4 are independently selected from hydrogen, methyl and ethyl.
    Type: Grant
    Filed: June 1, 1988
    Date of Patent: December 25, 1990
    Assignee: Odontex, Inc.
    Inventors: Ooi Wong, Toshiaki Nishiahta, Joseph H. Rytting
  • Patent number: 4931563
    Abstract: A process is provided for obtaining sulfophenyl quarternary ammonium or phosphonium substituted carbonic acid esters. The important step in this process involves reacting a phenyl quaternary ammonium or phosphonium substituted carbonic ester with oleum that contains from 0.5 to 33% sulfur trioxide. Amounts in excess of 33% sulfur trioxide lead to increased reaction times and, eventually, unacceptable product conversons.
    Type: Grant
    Filed: November 16, 1988
    Date of Patent: June 5, 1990
    Assignee: Lever Brothers Company
    Inventors: Stephen A. Madison, Leonora M. Ilardi
  • Patent number: 4925476
    Abstract: Nitrification inhibitors contain azole hemiaminal derivatives of the formula ##STR1## where R.sup.1 and R.sup.2 are each hydrogen, alkyl, aryl or halogen, R.sup.3 is alkyl, cycloalkyl, alkoxy, alkenyl, alkynyl, styryl, aryl, hetaryl or aralkyl, where the aromatic radical may be substituted, or is hydroxyl, A and B are each N or CR.sup.4, and R.sup.4 is hydrogen, alkyl, aryl or halogen.
    Type: Grant
    Filed: February 5, 1988
    Date of Patent: May 15, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Wagner, Norbert Rieber, Ernst-Heinrich Pommer, Juergen Dressel
  • Patent number: RE33907
    Abstract: A new class of anti-spasmodic thioester compounds having a heterocyclic ring containing the nitrogen atom of a secondary or tertiary amine or a bicycloheterocyclic ring system containing the nitrogen atom of a secondary or tertiary amine. These compounds have the general formula I ##STR1## wherein: =n is an integer from 0 to 2;R.sub.1 is aryl or cycloalkyl;=R.sub.2 is hydrogen or hydroxyl; andR.sub.
    Type: Grant
    Filed: August 15, 1989
    Date of Patent: April 28, 1992
    Assignee: United Pharmaceuticals, Inc.
    Inventor: William M. Davis