Abstract: New thyroid receptor ligands are provided which have the general formula I:
wherein
R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl;
R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen;
R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH;
n is an integer from 0 to 4; and
m is an integer from 1 to 4.
In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
Abstract: The invention relates to novel hydroxamic acid derivatives, to a plurality of processes for their preparation and to their use as pesticides.
Type:
Grant
Filed:
May 14, 2002
Date of Patent:
November 23, 2004
Assignee:
Bayer Aktiengesellschaft
Inventors:
Bernd-Wieland Krüger, Herbert Gayer, Peter Gerdes, Fritz Maurer, Ulrich Heinemann, Martin Vaupel, Astrid Mauler-Machnik, Ulrike Wachendorff-Neumann, Gerd Hänssler, Karl-Heinz Kuck
Abstract: Stereoselective process for the industrial synthesis of compounds of formula (I):
wherein R represents linear or branched (C1-C6)alkyl.
Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.
Abstract: The present invention is directed to an analytical method for measuring the concentration of an N-(phosphonomethyl)iminodiacetic acid (“NPMIDA”) substrate, an N-(phosphonomethyl)glycine product, formaldehyde, formic acid, N-methyl-N-(phosphonomethyl)glycine (“NMG”), N-methyl-aminomethylphosphonic acid (MAMPA) or aminomethylphosphonic acid (“AMPA”)) in an aqueous mixture thereof, using infrared spectroscopy. The present invention is also directed to a process for oxidizing an N-(phosphonomethyl)iminodiacetic acid substrate to form a N-(phosphonomethyl)glycine product, and as part of the process, measuring the concentration of at least one reactant, product or byproduct of the oxidation reaction using the analytical method of the present invention and controlling the oxidation process in response to the measurement taken.
Type:
Grant
Filed:
May 17, 2002
Date of Patent:
November 16, 2004
Assignee:
Monsanto Technology LLC
Inventors:
David R. Eaton, Walter Gavlick, Gary Klopf, Arnold Hershman, Denis Forster
Abstract: Polymerizable compounds are prepared and/or worked up using at least one liquid ring pump by a process in which a working liquid which contains a material stream from the preparation and/or working-up of the polymerizable compound is used in a liquid ring pump.
Type:
Grant
Filed:
September 4, 2002
Date of Patent:
November 16, 2004
Assignee:
BASF Aktiengesellschaft
Inventors:
Gerhard Nestler, Jürgen Schröder, Nicole McGlone
Abstract: Ethanol is dehydrogenated in the presence of hydrogen over a dehydrogenation catalyst, for example, a copper on silica catalyst. The liquefiable products present in the resulting intermediate reaction product mixture are selectively hydrogenated over a suitable catalyst, such as 5% ruthenium on carbon, so as selectively to hydrogenate reactive carbonyl-containing by-products to the corresponding alcohols. Butan-2-one and n-butyraldehyde are thereby hydrogenated to 2-butanol and n-butanol respectively. A two stage distillation procedure is then used to purify the selectively hydrogenated product. A first distillate of ethyl acetate, ethanol and water produced in the first distillation zone is redistilled in the second distillation zone, thereby producing a bottom product comprising, typically, from about 99.8 mol % to about 99.
Type:
Grant
Filed:
June 5, 2001
Date of Patent:
October 26, 2004
Assignee:
Davy Process Technology Limited
Inventors:
Stephen William Colley, Christopher Richard Fawcett, Colin Rathmell, Michael William Marshall Tuck
Abstract: An ultraviolet radiation absorbent for thermoplastic polymer materials such as polyethylene terephthalate or polycarbonate contains cyclic imino ester compound of a specified structure in an amount of over 99.5 weight % and less than 100 weight % and having an acid value in the range of 1×10−3-1 and/or a chlorine ion content in the range of 1×10−1-1×103 ppm.
Type:
Grant
Filed:
November 12, 2002
Date of Patent:
October 26, 2004
Assignees:
Takemoto Yushi Kabushiki Kaisha, Teijin DuPont Films Japan Limited
Abstract: The invention relates to a method for hydrogenation of aromatic urethanes, which contain one or more aromatic rings and one or more urethane groups bonded directly and/or indirectly to one aromatic ring or to different aromatic rings, using hydrogen in the presence of a supported catalyst, which contains ruthenium as active metal. The catalyst support of the catalyst to be used according to the invention has a BET surface ranging from larger than 30 m2/g to smaller than 70 m2/g and more than 50% of the pore volume of the catalyst support is represented by macropores with a pore diameter of larger than 50 nm and less than 50% is represented by mesopores with a pore diameter of 2 to 50 nm. The method is suitable in particular for hydrogenation of dibutyl 4,4′-methylenedicarbanilate to dibutyl 4,4′-methylenedicyclohexylcarbamate with a trans-trans isomer content of <30%, preferably of <20%, particularly preferably of 5 to 15%.
Type:
Grant
Filed:
December 31, 2002
Date of Patent:
October 26, 2004
Assignee:
Degussa AG
Inventors:
Norbert Finke, Ranier Lomoelder, Christian Lettmann, Guido Stochniol
Abstract: Process for the carbonylation of optionally substituted ethylenically unsaturated compounds by reaction with carbon monoxide and a coreactant in the presence of a catalyst system. The catalyst system includes
(a) a source of Pt group metal cations,
(b) a certain bidentate diphosphine composition.
Abstract: Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.
Abstract: Compounds able to chelate paramagnetic metal ions and the use thereof as contrast agents in the technique known as “Magnetic Resonance Imaging” (M.R.I.).
Type:
Grant
Filed:
August 27, 2002
Date of Patent:
October 12, 2004
Assignee:
Bracco Imaging S.p.A.
Inventors:
Christoph De Haen, Andrea Beltrami, Enrico Cappelletti, Luciano Lattuada, Mario Virtuani
Abstract: The present invention relates to a process for the preparation of both the phenyl pyrazine derivative 2,6-diamino-3-(2,3,5-trichlorophenyl)pyrazine and an intermediate in the synthesis of 2,6-diamino-3-(2,3,5-trichlorophenyl)pyrazine, 2-{[Cyano-(2,3,5-trichlorophenyl)-methyl]-amino}-acetamidine or a salt thereof.
Abstract: The invention relates to the preparation of compounds (I)
in which A═H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III)
a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)-Het, where Ar=phenyl, M═H or cation and Het=heterocycle from formula (I), to give compounds (I) (A═H), or
b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A═H), or
c) reaction of (III) with cyanates and amines (VII) of the formula HNR3-Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A═H) and optional acylation if A is to be other than H.
Type:
Grant
Filed:
November 5, 2002
Date of Patent:
September 14, 2004
Assignee:
Hoechst Schering AgrEvo GmbH
Inventors:
Gerhard Schnabel, Jan Vermehren, Lothar Willms
Abstract: A process for producing fomesafen from acifluorfen comprises the steps of (a) converting acifluorfen to its acid chloride, (b) coupling the acid chloride so formed with methanesulphonamide to form crude fomesafen and (c) purifying the crude fomesafen, characterized in that each of the steps is carried out in a single common solvent, which is preferably a chloroalkane. Preferably the steps are telescoped together so that there is no isolation of the product for any step until fomesafen is obtained.
Type:
Grant
Filed:
June 20, 2002
Date of Patent:
September 14, 2004
Assignee:
Syngenta Limited
Inventors:
Stephen Martin Brown, Brian David Gott, James Peter Muxworthy
Abstract: An ester compound of formula (1)
can be produced by making a compound given by formula (2):
react with an alkali metal salt of acetic acid in the presence of an aromatic hydrocarbon, and the obtained ester compound of formula (1) react with an alkali metal hydroxide and water to give a 3-phenoxypropanol compound of formula (3):
Abstract: A process for producing a carboxylic acid having (n+1) carbon atoms, which includes carbonylating an alcohol having n carbon atoms, and/or an ester of the alcohol and the carboxylic acid in each alkyl group with carbon monoxide in the presence of a catalytic system containing a rhodium catalyst. The process uses a reaction medium for the carbonylation that includes: (1) a rhodium catalyst, (2) an organic halide corresponding to said alcohol, (3) an ester of the alcohol and the carboxylic acid, (4) the carboxylic acid, optionally (5) water, a haloid acid, an inorganic halogen salt or an acetate, and (6) a cocatalyst selected from arginine, N-acetyl alanine, or nitrogen- and oxygen-containing organic compounds.
Type:
Grant
Filed:
October 4, 2002
Date of Patent:
August 31, 2004
Assignee:
China Petrochemical Development Corporation
Inventors:
Chia Jung Tsai, Yao Lung Liu, Hsi Chin Tsai
Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.
Type:
Grant
Filed:
October 1, 2001
Date of Patent:
August 17, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
Abstract: Synergistic immixtures of ascorbic acid with at least one monosaccharide ester of ascorbic acid and/or at least one metal salt of phosphorylated ascorbic acid more effectively increase the synthesis of epidermal ceramides in human skin, especially types IV to VII ceramides, as well as improve the barrier function, moisture content and/or suppleness/surface appearance of the skin and which otherwise combat/prevent intrinsic aging thereof and are useful for the treatment of dermatitis.
Abstract: The invention relates to a process for the preparation of heterocycles, characterised in that the following components:
i) a propargyl derivative of the general structural formula I
a wherein Het is an optionally substituted hetero atom and A is a substituted or unsubstituted aromatic entity, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkyne, an acceptor group or a nitrile;
(ii) a compound of the general structural formula II,
B—X II,
wherein B is an electron-deficient substituted or unsubstituted aromatic entity with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic entity with or without an acceptor group, an electron-deficient olefin and/or alkyne, a metal complex, and X is a leaving group;
(iii) a nucleophile of the general structural formula III,
Y—Cn—Z III,
wherein Y and/or Z, each