Abstract: Method of producing compounds of formula
wherein
R1 is hydrogen or C1-C4-alkyl;
R2 is hydrogen, C1-C8-alkyl, C3-C6-cycloalkyl, or a radical —N(R3)R4; or R2 and R6 together are —CH2—CH2—S—;
R3 and R4 are hydrogen, C1-C4-alkyl, C3-C6-cycloalkyl or a radical —CH2B;
R6 is hydrogen, C1-C8-alkyl, aryl or benzyl;
or R3 and R6 together are —CH2—CH2—, —CH2—CH2—CH2—, —CH2—O—CH2—, —CH2—S—CH2— or —CH2—N(R5)—CH2—;
X is CH—CN; CH—NO2 or N—NO2;
A is an optionally substituted, aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical; and
B is optionally substituted phenyl, 3-pyridyl or thiazolyl;
characterised in that a compound of formula
wherein R2, R6 and X have the same significance as given above in formula (I), is reacted in the presence of a phase transfer catalyst and a base with a compound of f
Type:
Grant
Filed:
December 20, 2002
Date of Patent:
June 8, 2004
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
Gottfried Seifert, Thomas Rapold, Verena Gisin
Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.
Type:
Grant
Filed:
July 22, 1997
Date of Patent:
June 8, 2004
Assignee:
Pharmacia Corporation
Inventors:
Gary DeCrescenzo, Zaheer S. Abbas, John N. Freskos, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
September 6, 2000
Date of Patent:
June 1, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
Abstract: A process for the preparation of ruthenium compounds of the formula {Ru(dienyl)2} wherein “dienyl” represents a substituted pentadienyl or cycloheptadienyl group by reacting dichloro(2,7-dimethylocta-2,6-dien-1,8-diyl)-ruthenium with an appropriate diene in the presence of a primary or secondary alcohol capable of reducing Ru(IV) to Ru(II); and a carbonate of an alkaline material. These ruthenium compounds are useful as precursors of Ru catalysts.
Type:
Grant
Filed:
October 8, 2002
Date of Patent:
June 1, 2004
Assignee:
Firmenich SA
Inventors:
Albrecht Kurt Lutz Salzer, Frank Peter Herbert Podewils, Stefan Geyser
Abstract: Based on the discovery that the melting point and solubility of onium salts are affected by the asymmetry of the substitution on cation, and that the branched substituents effectively shield onium cations from electrochemical reduction, new onium salts are synthesized and high performance electrolytes based on these salts for electrochemical capacitor are provided. The composition of the new electrolyte comprises an onium salt or mixture of such onium salts dissolved in aprotic, non-aqueous solvents or mixture of such solvents. The electrolyte is able to perform at high rate of charge/discharge, at low ambient temperatures, and within wide operating voltage, due to the high solubility, low melting temperature, and the improved reduction stability of the new onium cations, respectively.
Type:
Grant
Filed:
May 10, 1999
Date of Patent:
June 1, 2004
Assignee:
The United States of America as represented by the Secretary
of the Army
Inventors:
Kang Xu, Shengping Ding, T. Richard Jow
Abstract: The present invention relates to 1-(aryloxy)propionoyl-2-arylsulfonyl hydrazines useful as hypoglycemic agents, and to a process for synthesis thereof. The present invention also relates to the synthesis of 1-(aryloxy)propionoyl-2-arylsulfonyl hydrazines as new hypoglycemic agents which may be useful in the treatment of diabetes.
Type:
Grant
Filed:
March 29, 2002
Date of Patent:
May 4, 2004
Assignee:
Council of Scientific & Industrial Research
Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula:
wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
Type:
Grant
Filed:
April 22, 2003
Date of Patent:
May 4, 2004
Assignee:
3-Dimensional Pharmaceuticals, Inc.
Inventors:
Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
Abstract: The invention relates to a process for the preparation of urea from ammonia and carbon dioxide in which the low-pressure carbamate stream formed in the further upgrading of the urea synthesis solution is stripped in a CO2-carbamate stripper in countercurrent contact with CO2, which results in the formation of a gas mixture consisting substantially of ammonia and carbon dioxide.
This gas mixture is preferably subsequently condensed in a high-pressure carbamate condenser and then returned to the synthesis zone.
Abstract: A method is provided for making aromatic-imide and aromatic-methylidynetrissulfonyl species by reaction of aromatic species with a reactant according to formula (I):
(X—SO2—)m—QH—(—SO2—R1)n (I)
wherein Q is C or N; wherein each X is independently selected from the group consisting of halogens, typically F or Cl; wherein each R1 is independently selected from the group consisting of aliphatic and aromatic groups, which may or may not be saturated, unsaturated, straight-chain, branched, cyclic, heteroatomic, polymeric, halogenated, fluorinated or substituted; wherein m is greater than 0; wherein m+n=2 when Q is N; and wherein m+n=3 when Q is C. Ar may be derived from an aromatic polymeric compound.
Abstract: In an industrial process for preparing organohalosilanes by reacting metallic silicon particles with an organohalide in the presence of a copper catalyst, a contact mass composed of the metallic silicon and the catalyst further contains an effective amount of a phosphonium compound having on the molecule at least one group of the formula: [R2R3R4P—]+Y− wherein R2, R3 and R4 each are a monovalent hydrocarbon group and Y is a halogen atom or acid group. The invention drastically increases the silane formation rate and the utilization of silicon without lowering the selectivity of useful silane.
Abstract: The present invention relates to crystalline forms of the sodium salt of 5-chloro-2-methoxy-N-(2-(4-methoxy-3-methylaminothiocarbonylaminosulfonylphenyl)ethyl)benzamide, processes for their preparation, their use, and pharmaceutical preparations comprising them.
Type:
Grant
Filed:
April 14, 2000
Date of Patent:
April 20, 2004
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Heinrich Christian Englert, Uwe Gerlach, Harald Schneider, Tobias Metzenthin
Abstract: Disclosed is a method for producing anthracene of formula (II) below by mixing a reaction mixture with a primary alcohol, wherein the reaction mixture is a reaction mixture obtained by reacting a metal hydride with an anthraquinone of formula (I):
Abstract: Siloxane bischloroformates are prepared in a continuous process by phosgenating siloxane bisphenols in a flow reactor using a substantial excess of phosgene and sodium hydroxide. While very high levels (>95%) of conversion of the siloxane bisphenol to the corresponding siloxane bischloroformate are achieved using a flow reactor according to the method of the invention, only more modest conversion (˜90%) of the siloxane bisphenol to the corresponding siloxane bischloroformate is attained when analogous batch processes are employed. The process holds promise for use in the manufacture of silicone-containing copolycarbonates which requires high purity siloxane bischloroformate intermediates.
Type:
Grant
Filed:
August 16, 2002
Date of Patent:
April 20, 2004
Assignee:
General Electric Company
Inventors:
James Manio Silva, David Michel Dardaris, Gary Charles Davis
Abstract: The present invention relates to a compound of formula (Ia) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders.
Type:
Grant
Filed:
October 17, 2002
Date of Patent:
April 13, 2004
Assignee:
Eli Lilly and Company
Inventors:
Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
Abstract: The present invention relates to a novel process for the preparation of N-methyl-N′-nitroguanidine by reacting nitroguanidine with aqueous methylamine solution buffered by the addition of inorganic or organic acids.
Abstract: The invention relates to a process for the chlorination of methylsilanes, which comprises reacting methylsilanes with chlorine in the presence of at least 0.1% by weight of hydrogen chloride, based on the weight of methylsilane of the formula (II), under the action of electromagnetic radiation which induces chlorination, chlorine being used in a substoichiometric amount based on the methylsilane of the formula (II), and the reaction being carried out at temperatures below the boiling point of the methylsilane of the formula (II). The invention further relates to an apparatus suitable for carrying out the chlorination of an industrial scale.
Type:
Grant
Filed:
October 18, 2002
Date of Patent:
April 13, 2004
Assignee:
Wacker-Chemie GmbH
Inventors:
Helmut Hollfelder, Siegfried Pflaum, Franz Riener
Abstract: The present invention provides carbanilides of formula (I),
wherein A, Q, R, X, Z and m are as defined herein. A plurality of processes for preparing these compounds is provided, along with methods of using the compounds to control microorganisms in crops and in the protection of materials. The compounds of the present invention also find use in controlling animal pests.
Type:
Grant
Filed:
May 30, 2002
Date of Patent:
April 6, 2004
Assignee:
Bayer Aktiengesellschaft
Inventors:
Hans-Ludwig Elbe, Bernd-Wieland Krüger, Robert Markert, Ralf Tiemann, Dietmar Kuhnt, Stefan Dutzmann, Klaus Stenzel, Christoph Erdelen, Martin Kugler, Hans-Ulrich Buschhaus
Abstract: Chloropropylsilanes are prepared via hydrosilation of olefinic halides with organosilicon hydrides, in the presence of neat platinum free copper containing catalysts. Organosilicon hydrides such as triethylsilane, olefinic halides such as allyl chloride, and catalysts such as copper acetate, copper chloride, copper sulphate, copper hydroxide, copper nitrate, and copper cyanide, can be used in the process.
Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula:
wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
Type:
Grant
Filed:
February 6, 2003
Date of Patent:
March 16, 2004
Assignee:
3-Dimensional Pharmaceuticals, Inc.
Inventors:
Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro