Nitro Bonded To Carbon In Acid Moiety Patents (Class 560/20)
  • Publication number: 20040082805
    Abstract: The present invention provides a compound which has cytokine production inhibitory activity and is useful for the treatment of diseases which is associated with cytokine.
    Type: Application
    Filed: September 29, 2003
    Publication date: April 29, 2004
    Inventors: Yoshihito Eguchi, Ken-cihi Chiba, Masaki Goto, Hiroshi Obaishi, Yoshikazu Kuboi
  • Patent number: 6727098
    Abstract: A novel achiral biaryl-type compound and a circular dichroism (CD) color fixing agent are provided. Furthermore, a method for determining an absolute configuration of a chiral compound is carried out by introducing the above achiral biaryl-type compound into the chiral compound.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: April 27, 2004
    Assignee: Kanazawa University
    Inventors: Tomihisa Ohta, Shinzo Hosoi
  • Patent number: 6699463
    Abstract: Compounds of Formula I Each R is independently linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy or one R is H and the other R is linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy; R1 is selected from the group consisting of COCH3, CO2R3, CONH2, CONH(R4)2, CN, COX(CH2)n-N—(R2)(R4)(R3), and the quaternized salt form of the formula COX(CH2)n-N—(R2)(R4)(R3)+Y−; X is O or NH; n is an integer of 1 to 5; Y is an anion; and R2, R3 and R4 are independently linear or branched C1 to C20. Hair care formulations and other compounds containing compounds of Formula I, and methods for protecting hair and substrates such as polymers, textiles, fabrics, leathers and paints using the compounds herein.
    Type: Grant
    Filed: April 10, 2002
    Date of Patent: March 2, 2004
    Assignee: EM Industries
    Inventor: Ratan K. Chaudhuri
  • Patent number: 6686496
    Abstract: The compounds of the invention which encompasses a class of compounds having the property of anti-carcinogenic activity against human myeloma r comprising 4-oxo-2-butenoic acid compounds and 3-hydrazino-2,4-dioxobutanoic acid compounds and more specifically those novel derivatives: 4-(4-Chloro-phenyl)-2-(N′-fluoren-9-ylidene-hydrazino)-4-oxo-but-2-enoic acid methyl ester (OF-07); 2-{N′-[(2-Bromo-phenyl)-phenyl-methylene]-hydrazino}-4-oxo-4-phenyl-but-2-enoic acid methyl ester (OF-09); 2-{N′-[(4-Dimethylamino-phenyl)-phenyl-methylene]-hydrazino}-4-oxo-4-phenyl-but-2-enoic acid methyl ester (OF-10) and 2-{N′-[1-(4-Chloro-phenyl)-ethylidene]-hydrazino}-4-oxo-4-phenyl-but-2-enoic acid methyl ester (OF-20) and the use of 2-(N′-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester (OF-06); 4-(4-Ethoxy-phenyl)-2-(N′-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-butyric acid methyl ester (OF-13); 4-b
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: February 3, 2004
    Assignee: University of Central Florida
    Inventors: D. Howard Miles, Solodnikov Sergey Yurjevich, Krasnykh Olga Petrovna, Korotkova Tatiana Alexandrovna, Elena A. Goun
  • Patent number: 6656737
    Abstract: An organic compound useful for detecting the total quantity of isocyanate in an environmental sample is provided. The compound is 9-anthrcenylmethyl-1-piperazinecarboxylate (PAC), an isocyanate derivatizing agent. A process for producing PAC and methods for detecting a particular isocyanate monomer or the total isocyanate in environmental samples using PAC & related isocyanate derivatizing agents are also provided.
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: December 2, 2003
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventor: Robert P. Streicher
  • Publication number: 20030220517
    Abstract: A novel process affords &ohgr;-ketocarboxylic acid derivatives of the formula (I) 1
    Type: Application
    Filed: March 14, 2003
    Publication date: November 27, 2003
    Inventor: Albrecht Marhold
  • Patent number: 6630598
    Abstract: A process of reacting a nitroaniline compound of formula (2): with an acid anhydride or acid halide is carried out in the presence of an alkali metal compound or an alkaline earth metal compound to produce an acylnitroaniline derivative. The process further includes the step of reacting the resulting product with a compound of formula (5); R2—Y to produce an N-acylnitroaniline derivative of formula (1): The N-acylnitroaniline derivative of formula (1) is a useful intermediate for the production of pharmaceuticals.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: October 7, 2003
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Tomoyasu Yoshida
  • Publication number: 20030119902
    Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.
    Type: Application
    Filed: August 28, 2002
    Publication date: June 26, 2003
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
  • Patent number: 6555703
    Abstract: The invention relates to a process for forming a carboxylic benzyl ester comprising reacting a dibenzyl ether with a carboxylic acid in the presence of a heteropolyacid and forming a carboxylic acid benzyl ester.
    Type: Grant
    Filed: August 31, 2001
    Date of Patent: April 29, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Pieter Ooms, Bernd-Ulrich Schenke
  • Patent number: 6538150
    Abstract: The present invention relates to a compound of the formula (I) The compound according to the invention is suitable for the preparation of herbicidal active substances such as sulfonylureas.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: March 25, 2003
    Assignee: Aventis CropScience GmbH
    Inventors: Klaus Lorenz, Hans-Joachim Ressel, Lothar Willms
  • Publication number: 20030055279
    Abstract: Benzyl carboxylates can be prepared by reacting dibenzyl ethers with carboxylic acids and optionally carboxylic anhydrides in the presence of one or more, preferably one, acids applied to a support as catalyst.
    Type: Application
    Filed: August 21, 2002
    Publication date: March 20, 2003
    Inventors: Pieter Ooms, Bernd-Ulrich Schenke, Martin Sturmann
  • Patent number: 6531624
    Abstract: A process for producing a benzoylacrylic acid derivative (formula 1) in high yield through a small number of steps and a simple purification step. The process comprises reacting 2,4,5-trifluoro-3-methyl-6-nitrobenzoyl chloride with a compound (formula 2) to yield an aminoacrylic acid derivative (formula 1) and then reacting the aminoacrylic acid derivative (formula 1) with an amine derivative represented by R2—NH2, wherein R2 is a cycloalkyl group or the like.
    Type: Grant
    Filed: May 18, 2001
    Date of Patent: March 11, 2003
    Assignees: Asahi Glass Company Ltd., Katayama Seiyakusyo Co., Ltd.
    Inventors: Naoto Morita, Takashi Inagaki
  • Publication number: 20020183518
    Abstract: Y—X—C(R′)═C(R″)COOR″′  (A1)
    Type: Application
    Filed: November 27, 2001
    Publication date: December 5, 2002
    Applicant: ONTOGEN CORPORATION
    Inventors: Adnan M. M. Mjalli, Xiaodong Cao, Edmund J. Moran
  • Publication number: 20020165096
    Abstract: Compounds of formula I 1
    Type: Application
    Filed: June 21, 2001
    Publication date: November 7, 2002
    Inventors: Juergen Schaetzer, Alain De Mesmaeker, Shy-Fuh Lee
  • Patent number: 6403638
    Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: June 11, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
  • Patent number: 6369194
    Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: April 9, 2002
    Assignee: Yale University
    Inventor: Harry H. Wasserman
  • Publication number: 20020040159
    Abstract: Methods for preparing substituted aromatic carboxylic acid esters are described.
    Type: Application
    Filed: December 6, 2001
    Publication date: April 4, 2002
    Applicant: EASTMAN CHEMICAL COMPANY
    Inventors: Neil W. Boaz, M. Todd Coleman, Timothy R. Hightower
  • Patent number: 6348619
    Abstract: A carboxylic acid ester is prepared by a process comprising: reacting an aldehyde and an alcohol in a liquid phase in the presence of molecular oxygen as indicated by the following reaction: RCHO+R′OH+O2→RCOOR′+H2O in the presence of a catalyst comprising at least palladium and an element X, wherein X is bismuth, lead or a combination thereof, supported on a carrier, wherein the catalyst has an acid strength, pKa, of more than 4.8 and shows an ammonia chemical adsorption amount at 0° C. of 0-150 &mgr;mol/g-catalyst.
    Type: Grant
    Filed: January 25, 1999
    Date of Patent: February 19, 2002
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Yasukazu Yoshida, Yuji Mikami, Motomu Oh-Kita
  • Patent number: 6337418
    Abstract: Methods for preparing substituted aromatic carboxylic acid esters are described. In particular, the invention relates a method for preparing a nitro-substituted aromatic carboxylic acid ester: Additionally the invention relates to a method for preparing a thioether-substituted aromatic carboxylic acid ester: Such aryl esters are useful in the preparation of various agrochemicals and agrochemical intermediates.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: January 8, 2002
    Assignee: Eastman Chemical Co.
    Inventors: Neil W. Boaz, M. Todd Coleman, Timothy R. Hightower
  • Patent number: 6329377
    Abstract: The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: December 11, 2001
    Assignee: Cephalon, Inc.
    Inventor: Sankar Chatterjee
  • Publication number: 20010037042
    Abstract: Process for the coupling of
    Type: Application
    Filed: March 6, 2001
    Publication date: November 1, 2001
    Inventors: Adriano Indolese, Anita Schnyder
  • Patent number: 6310245
    Abstract: The invention relates to 2-benzoylcyclohexane-1,3-diones of the formula I where R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR5, —OCOR6, —OSO2R6, —SH, —S(O)nR7, —SO2OR5, —SO2NR5R8, —NR8SO2R6 or —NR8COR6; R3 is hydrogen, alkyl, haloalkyl, alkenyl or alkynyl; R4 is hydrogen, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, —COR9, —CO2R9, —COSR9 or —CONR8R9; X is oxygen or sulfur; Z is oxygen or NR8; m is 0 or 1; n is 0, 1 or 2; R5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R6 is alkyl or haloalkyl; R7 is alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R8 is hydrogen or alkyl; R9 is alkyl, alkenyl, alkynyl, phenyl or benzyl; R10 is alkyl, haloalkyl, alkenyl or alkynyl; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring which is linked in the 2-position; where m is 1 if R3 is
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: October 30, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Uwe Kardorff, Regina Luise Hill, Michael Rack, Wolfgang von Deyn, Stefan Engel, Martina Otten, Matthias Witschel, Ernst Baumann, Joachim Rheinheimer, Guido Mayer, Ulf Misslitz, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 6284894
    Abstract: A process for the preparation of an allylic aromatic compound in which an aromatic amine is reacted first with a nitrite and then with an allylic olefin having an eliminatable terminal substituent. Novel allylic derivatives of disubstituted benzene compounds are also described.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: September 4, 2001
    Assignee: Nycomed Imaging AS
    Inventors: Fredrik Ek, Lars Goran Wistrand
  • Patent number: 6284910
    Abstract: The post-translational addition of a farnesyl moiety to the Ras oncoprotein is essential for its membrane localization and is required for both its biological activity and ability to induce malignant transformation. The present invention describes design and synthesis of a farnesylpyrophosphate (FPP) analog, 8-anilinogeranyl pyrophosphate (AGPP) that is transferred to Ras by farnesyltransferase (FTase), in which the &ohgr;-terminal isoprene unit of the farnesyl group has been replaced with an aniline functionality. AGPP potently inhibited FTase activity in vitro (IC50=0.6 &mgr;M) and is highly selective showing little inhibitory activity against either geranylgeranyl-protein transferase type I (GGTase I) (IC50=31 &mgr;M) or the utilization of FPP by the enzyme squalene synthase (IC50=1000 &mgr;M). Kinetic analyses suggest that AGPP acts as a competitive inhibitor of FTase with respect to FPP.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: September 4, 2001
    Assignee: University of Kentucky Research Foundation
    Inventors: Hans Peter Spielmann, Douglas A. Andres, Kareem A. H. Chehade
  • Patent number: 6258982
    Abstract: The present invention relates to a hydrogenation process for the preparation of aromatic amino compounds containing directly on the aryl ring or in a side chain one or more entities that may also undergo hydrogenation, such as carbon multiple bonds, nitrile groups, imino groups or carbonyl groups. The preparation is carried out by catalytic hydrogenation of the corresponding aromatic nitro compounds in the presence of a phosphorus-modified noble metal catalyst. The invention relates also to the use of modified noble metal catalysts for the hydrogenation of aromatic nitro compounds containing carbon multiple bonds and/or substituted by nitrile, imino or carbonyl groups.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: July 10, 2001
    Assignee: Novartis AG
    Inventors: Peter Baumeister, Urs Siegrist, Martin Studer
  • Patent number: 6255517
    Abstract: The present invention relates to a thymol derivative represented by following Chemical Formula 1, pharmaceutically acceptable salts or esters thereof, and anti-cancer agents comprising the same as an active ingredient.
    Type: Grant
    Filed: October 14, 1999
    Date of Patent: July 3, 2001
    Inventors: Ok Pyo Zee, Young Hoon Jung, Kang Ro Lee, Hyung In Moon, Hyung Geun Baek, Min Jung Lee, Dae Keun Kim
  • Patent number: 6251944
    Abstract: The present invention relates to a class of compounds represented by Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 integrin.
    Type: Grant
    Filed: April 8, 1999
    Date of Patent: June 26, 2001
    Assignee: G. D. Searle & Company
    Inventors: Barbara B. Chen, Helen Y. Chen, Glen J. Gesicki, Richard A. Haack, James W. Malecha, Thomas D. Penning, Joseph G. Rico, Thomas E. Rogers, Peter G. Ruminski, Mark A. Russell, Stella S. Yu
  • Patent number: 6162943
    Abstract: Process for the preparation of .alpha.-alkoxy-.alpha.-trifluoromethyl-arylacetic esters of the formula (I) ##STR1## wherein R is a component selected from the group consisting of C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.6 -C.sub.10 -aryl and C.sub.1 -C.sub.6 -halogenoalkyl, R' is selected from the group consisting of C.sub.1 -C.sub.4 -alkyl, X is selected from the group consisting of halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.6 -C.sub.10 -aryl or C.sub.1 -C.sub.4 -alkoxy and nitro, and n is zero or an integer from 1 to 3.
    Type: Grant
    Filed: April 16, 1999
    Date of Patent: December 19, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Norbert Lui, Albrecht Marhold
  • Patent number: 6147224
    Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.
    Type: Grant
    Filed: October 1, 1998
    Date of Patent: November 14, 2000
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
  • Patent number: 6057269
    Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: May 2, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz, Olaf Menke, Markus Menges
  • Patent number: 6054457
    Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: December 9, 1997
    Date of Patent: April 25, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
  • Patent number: 6043360
    Abstract: The instant invention provides intermediates and processes for the preparation of compounds of formula IV ##STR1## wherein: n is 0, 1, or 2;R is hydrogen or C.sub.1 -C.sub.4 alkyl;X.sup.1 is hydrogen, cyano, 4-hydroxybenzoyl, 4-halobenzoyl, or 4-(C.sub.1 -C.sub.4 alkoxy)benzoyl;Y is NR.sup.4 R.sup.5, 4-hydroxyphenyl, or 4-(C.sub.1 -C.sub.4 alkoxy)phenyl;and R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.4 alkyl.
    Type: Grant
    Filed: April 29, 1998
    Date of Patent: March 28, 2000
    Assignee: Eli Lilly and Company
    Inventors: Tony Yantao Zhang, John Paul Gardner
  • Patent number: 6030803
    Abstract: Dibenzodihydropyridinecarboxylic esters are provided which comply with formula (1) or (2), wherein: R.sub.1 is substituted alkyl or cyano; R.sub.2 and R.sub.3 are independently hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; R.sub.4 is hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; R.sub.5 and R.sub.6 are independently alkyl, alkoxy or another substituent which is relatively resistant to oxidation; m and n are integers from 0 to 4; wherein, if m or n is at least 2, two groups R.sub.5 or R.sub.6 may be linked together; and Z is oxygen or sulphur. The new compounds are used in a method as chemiluminogenic reagents for detecting the presence of peroxidase activity at extremely low levels (10.sub.-20 moles). A kit containing the dibenzodihydropyridine-carboxylic esters for use in assaying peroxidase activity has also been described.
    Type: Grant
    Filed: January 7, 1999
    Date of Patent: February 29, 2000
    Assignee: De Staat der Nederlanden, vertegenwoordigd door de Minister van Welzijn, Volksgeszonheid en Cultuur
    Inventors: Marjorie Jacquemijns, Gijsbert Zomer
  • Patent number: 6002041
    Abstract: Particularly pure di-C.sub.1 -C.sub.4 -alkyl 5-nitro-isophthalates are obtained in good yield and in a simple process by dissolving 5-nitro-isophthalic acid in a mixture of a C.sub.1 -C.sub.4 -alkyl alcohol and a solvent which is miscible or only partially miscible with water, heating in the presence of a strong acid, thus forming a second, aqueous phase, crystallizing out, after the esterification reaction has ended, the di-C.sub.1 -C.sub.4 -alkyl 5-nitro-isophthalate formed from the organic phase by cooling and removing the aqueous phase before or after the di-C.sub.1 -C.sub.4 -alkyl 5-nitro-isophthalate is separated off.
    Type: Grant
    Filed: May 6, 1998
    Date of Patent: December 14, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Rauchschwalbe, Bernhard Beitzke, Helmut Fiege
  • Patent number: 5985919
    Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: November 16, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Grote, Reinhard Kirstgen, Bernd Muller, Hubert Sauter, Albrecht Harreus, Hartmann Konig, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Franz Rohl
  • Patent number: 5981573
    Abstract: A compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: [wherein each of Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 is an aryl group or an aromatic heterocyclic group; A.sup.1 is a C.sub.2-6 chain hydrocarbon group or a group represented by --A.sup.1a --W.sup.1 --A.sup.1b -- (wherein W.sup.1 is an oxygen atom, a sulfur atom, an ethynylene group, a cyclopropylene group or a group represented by --NR.sup.W --; A.sup.2 is a C.sub.2-8 chain hydrocarbon group; each of X and Y is an oxygen atom, a sulfur atom, a carbonyl group or a group represented by --CHR.sup.a -- or by --NR.sup.b --, or X and Y together represent a vinylene group or an ethynylene group; each of R.sup.1, R.sup.2, R.sup.3, R.sup.7 and R.sup.8 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkenyl group or a lower alkoxy group; each of R.sup.4 and R.sup.
    Type: Grant
    Filed: August 4, 1998
    Date of Patent: November 9, 1999
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
  • Patent number: 5952381
    Abstract: The present invention relates to a class of compounds represented by Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: September 14, 1999
    Assignee: G. D. Searle & Co.
    Inventors: Barbara B. Chen, Helen Y. Chen, Glen J. Gesicki, Richard A. Haack, James W. Malecha, Thomas D. Penning, Joseph G. Rico, Thomas E. Rogers, Peter G. Ruminski, Mark A. Russell, Stella S. Yu
  • Patent number: 5952386
    Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: September 14, 1999
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
  • Patent number: 5905164
    Abstract: Amine compounds of general formula (I), ##STR1## wherein: each R.sup.1 independently represents an alkyl group; each R.sup.2 independently represents an alkyl group; each group X independently represents a polyalkylene polyol moiety wherein hydroxyl groups of the polyol moiety are optionally alkylated but not including a group X which includes an ethyleneoxy or di(ethyleneoxy) moiety; n and m independently represent 1, 2 or 3; and each Q is independently selected from hydrogen or halogen atoms, and alkyl, acyl, nitro, cyano, alkoxy, hydroxy, amino, alkylamino, sulphinyl, alkylsulphinyl, sulphonyl, alkylsulphonyl, sulphonate, amido, alkylamido, alkoxycarbonyl, halocarbonyl and haloalkyl groups, processes for their preparation and intermediate compounds are described. Compounds of general formula (I) are useful as radiation curing agents in polymerisation processes.
    Type: Grant
    Filed: February 27, 1998
    Date of Patent: May 18, 1999
    Assignee: Lambson Fine Chemicals Limited
    Inventors: David George Anderson, Robert Stephen Davidson, Neil Richard Cullum, Elizabeth Sands
  • Patent number: 5885990
    Abstract: Substituted amidinonaphthyl ester compounds effective for treatment of thrombosis are represented by the following formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1## wherein R.sub.1 represents (4,5-dihydro-1H-imidazol-2-yl)amino group, (4,5-dihydro-1,3-thiazol-2-yl)amino group, amidino group, morpholinomethyl group, nitro group, amino group, dimethylamino group, ##STR2## R.sub.3 represents hydrogen, methoxy group, hydroxyl group, acetylamino group, morpholino group, piperidino group, 1-pyrrolidinyl group or dimethylamino group,m represents 0-4,R.sub.4 represents hydrogen or methyl group,R.sub.2 represents NH.sub.2 CO(CH.sub.2).sub.n --, 2-(carbamoyl)vinyl group or R.sub.5 OOC(CH.sub.2).sub.n --,R.sub.5 represents dimethylcarbamoylmethyl group, hydrogen or lower alkyl group, andn represents 0-2.
    Type: Grant
    Filed: June 12, 1997
    Date of Patent: March 23, 1999
    Assignee: Torii Pharmaceutical Co., Ltd.
    Inventors: Toyoo Nakayama, Hiroyuki Kawamura, Hiroyuki Uchiyama
  • Patent number: 5808131
    Abstract: Disclosed is a liquid urethane containing adduct; a process for the preparation thereof; and applications therewith. More specifically this invention relates to a stable adduct which is a liquid at room temperature and which contains a plurality of urethane linkages, and yet which is substantially free of any isocyanate functionality or isocyanate-reactive functionality. Such adducts can be used as quenchants, lubricants, or surfactants.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: September 15, 1998
    Assignee: The Dow Chemical Company
    Inventors: Henri J. M. Gruenbauer, Camiel F. Bartelink, Martin Moeller
  • Patent number: 5773656
    Abstract: Known (R)-1-aryl-alkylamines of the formula ##STR1## in whichR.sup.1 and Ar have the meanings indicated in the description, are prepared by a new process, which comprisesa) reacting a racemate of an ethyl or methyl 2-aryl-alkanoate of the formula ##STR2## with ammonia in the presence of a lipase which is suitable for the cleavage of esters, in the presence of a diluent,b) separating off from the reaction mixture the resulting (R)-2-aryl-alkanamide of the formula ##STR3## and then reacting it with sodium hypochlorite or sodium hypobromite in the presence of water.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: June 30, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventor: Uwe Stelzer
  • Patent number: 5763719
    Abstract: A fullerene derivative of the formula I ##STR1## where the symbols and indices have the following meanings: F is a fullerene radical of the formula (C.sub.20+2m), where m is a number from 1 to 50R.sup.1 to R.sup.8 are identical or different and are each H, CO.sub.2 R.sup.9, CN, COR.sup.10, Cl, Br, I, F, OR.sup.11, C.sub.1 -C.sub.20 -alkyl, phenyl or H, R.sup.1 -R.sup.4 and/or R.sup.5, R.sup.7 can also be part of a cycloalipathic, cycloaromatic or cycloheteroaromatic system which in turn is substituted by C.sub.1 -C.sub.20 -alkyl, aryl, carboxyl, carbonyl, alkoxy, aryloxy, halogen, nitro, alcohol or amine, or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, R.sup.3 and R.sup.4 can together be ##STR2## where R.sup.15 -R.sup.18 are each H, C.sub.1 -C.sub.20 -alkyl, F, Cl, Br, I or phenyl, andAR is the radical of a fused cyclo-aromatic system, and n is from 1 to 20 and a process for its preparation.
    Type: Grant
    Filed: September 15, 1995
    Date of Patent: June 9, 1998
    Assignee: Hoechst AG
    Inventors: Andreas Gugel, Pavel Belik, Klaus Mullen
  • Patent number: 5756810
    Abstract: A process for preparing t-butyl 4-(hydroxymethyl)-3-nitrobenzoate from t-butyl 4-(acetoxymethyl)-3-nitrobenzoate which comprises reacting t-butyl 4-(acetoxymethyl)-3-nitrobenzoate with hydrazine or hydrazine hydrate in a lower alkanol at 0.degree.-50.degree. C.
    Type: Grant
    Filed: September 11, 1996
    Date of Patent: May 26, 1998
    Assignee: Pharmacopeia, Inc.
    Inventors: John J. Baldwin, Michael H. J. Ohlmeyer, Ian Henderson
  • Patent number: 5728864
    Abstract: A liquid crystal compound of the formula (1) ##STR1## wherein R is a linear alkyl group having 6 to 12 carbon atoms,both X and Y are hydrogen atoms or one of X and Y is a fluorine atom and the other is a hydrogen atom,A is --CF.sub.3 or --C.sub.2 F.sub.5,m is an integer of 2 to 4,n is an integer of 2 to 4, andC* is an asymmetric carbon,having a ferrielectric phase in its phase sequence, or a ferrielectric liquid crystal composition containing the liquid crystal compound of the formula (1) having a ferrielectric phase, may be injected between substrates provided with nonlinear active elements, such as thin film transistors or diodes formed on each pixel, to form an active matrix liquid crystal display device.
    Type: Grant
    Filed: April 12, 1996
    Date of Patent: March 17, 1998
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Yuki Motoyama, Tomoyuki Yui, Masahiro Johno, Maki Ito, Takahiro Matsumoto, Hiroshi Mineta
  • Patent number: 5726205
    Abstract: This document describes O-acyl-4-phenyl-cycloalkanols of general formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between them denote 5- to 7-membered saturated, monocyclic, heterocyclic rings which may optionally also be interrupted by an oxygen or sulphur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl or alkynyl having up to 17 carbon atoms, and also processes for preparing them, pharmaceutical compositions containing these compounds and the use of these pharmaceutical compositions which intervene in cholesterol biosynthesis.
    Type: Grant
    Filed: January 17, 1997
    Date of Patent: March 10, 1998
    Assignee: Karl Thomae GmbH
    Inventors: Eberhard Woitun, Roland Maier, Peter Muller, Rudolf Hurnaus, Michael Mark, Bernard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
  • Patent number: 5721234
    Abstract: Novel glutamate receptor antagonists represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof, whereinZ is an alicyclic fused ring having 5 to 7 carbon atoms;R.sup.1 is hydrogen, an alkyl or an arylalkyl; andA is O, CH.sub.2, NR.sup.4, CH.sub.2 NR.sup.4, CN, tetrazole or CO wherein R.sup.4 is hydrogen, alkyl, hydroxyalkyl, aminoalkyl or aralkyl, wherein(i) when A is O, CH.sub.2, NR.sup.4 or CH.sub.2 NR.sup.4 then B is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, hydroxyalkyl, alkoxy, aminoalkyl, heterocyclic, alkylheterocyclic, heterocyclic-methyl, heterocyclic-ethyl, alkylcarbonyl, cycloalkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclic-carbonyl, alkylheterocyclic-carbonyl, or when A is NR.sup.4 or CH.sub.2 NR.sup.4 then B is a naturally occurring .alpha.-amino acid moiety joined by an amide bond or B joins with R.sup.4 and the nitrogen to form a four to seven membered heterocyclic ring, provided that when Z is a fused cyclohexyl ring and R.sup.
    Type: Grant
    Filed: October 23, 1995
    Date of Patent: February 24, 1998
    Assignee: Warner-Lambert Company
    Inventors: Christopher Franklin Bigge, Daniel Martin Retz
  • Patent number: 5719306
    Abstract: The present invention provides compounds of the formula Ar.sup.1 --Q--Ar.sup.2 --Y--R--Z and pharmaceutically acceptable salts thereof wherein Ar.sup.1 and Ar.sup.2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD and asthma.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 17, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Nizal Samuel Chandrakumar, Barbara Baosheng Chen, Michael Clare, Bipinchandra Nanubhai Desai, Stevan Wakefield Djuric, Stephen Hermann Docter, Alan Frank Gasiecki, Richard Arthur Haack, Chi-Dean Liang, Julie Marion Miyashiro, Thomas Dale Penning, Mark Andrew Russell, Stella Siu-tzyy Yu
  • Patent number: 5719307
    Abstract: Polyurethane-urea elastomers are made using as a chain extender 2-methyl-1,3-propanediol-bis-p-aminobenzoate which is the reduction product from hydrogenating 2-methyl-1,3-propanediol-bis-p-nitrobenzoate. The latter composition is preferably made by esterifying p-nitrobenzoic acid and 2-methyl-1,3-propanediol using a stoichiometric excess of the diol initially, adequate to render the reaction mixture processible, and after converting to a nonvolatile form sufficient diol to form diester with substantially all of the acid, removing free diol by distillation while continuing the esterification of unreacted acid and transesterification of monoester formed to diester. This process, which can be applied broadly to esterification of other nitroaromatic acids with other aliphatic diols, produces high yields of diester without needing extraneous solvent for processibility and with only water as a by-product.
    Type: Grant
    Filed: May 7, 1996
    Date of Patent: February 17, 1998
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Kevin Rodney Lassila, Jeremiah Patrick Casey
  • Patent number: 5717109
    Abstract: The present invention provides compounds of formula ##STR1## in which R represents an organic group, or a pharmaceutically acceptable metabolically labile ester or amide thereof, or a pharmaceutically acceptable salt thereof, which are useful as antagonists of one or more of the actions of L-glutamate at metabotropic excitatory amino acid receptors.
    Type: Grant
    Filed: July 10, 1995
    Date of Patent: February 10, 1998
    Assignee: Eli Lilly and Company
    Inventors: M. Brian Arnold, Thomas J. Bleisch, David R. Helton, Mary Jeanne Kallman, Paul L. Ornstein, Darryle D. Schoepp, Joseph P. Tizzano