Abstract: New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.
Type:
Grant
Filed:
September 30, 2005
Date of Patent:
September 28, 2010
Assignee:
DAC S.R.L.
Inventors:
Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
Abstract: This disclosure describes the molecular cloning of a pactamycin biosynthetic gene cluster from Streptomyces pactum ATCC 27456, characterization of individual genes in the gene cluster and the proteins encoded thereby as well as uses thereof. The pactamycin gene cluster is located within an 86.35 kilobases genetic locus and includes 53 open reading frames, 26 of which are considered to be the core cluster directly involved in the biosynthesis of pactamycin.
Abstract: The invention relates to compounds of formula (I) wherein A1 is C(R1R2)p; A2 is C(R6R7)q; p is 1 or 2; q is 1 or 2; each of R1, R2, R3, R4, R5, R6, R7 and R8 which may be the same or different, represents hydrogen, methyl or ethyl and R9 is C1-C4alkyl; R10 is hydrogen, halogen, C1-C3alkyl or C1-C3-haloalkyl, and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.
Type:
Grant
Filed:
December 20, 2005
Date of Patent:
June 29, 2010
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
Sebastian Volker Wendeborn, Renaud Beaudegnies, Andrew Edmunds, Christoph Luthy, Jurgen Schaetzer
Abstract: ??-Unsaturated sulfoxides of Formula I: are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.
Type:
Grant
Filed:
November 8, 2004
Date of Patent:
June 29, 2010
Assignee:
Temple University - Of The Commonwealth System of Higher Education
Inventors:
E. Premkumar Reddy, M. V. Ramana Reddy, Stanley C. Bell
Abstract: There is described a process for the purification of an impure preparation containing fentanyl by means of a reverse phase preparative chromatography process. A chromatographic column is loaded with a stationary phase, typically a silica particle having an organic ligand bound thereto. With a loading ratio of from about 50 to about 150 the impure preparation is acidified and passed through the column. The column is eluted with typically an aqueous solution of acetonitrile and the purified fentanyl is obtained in a specified cut.
Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Grant
Filed:
December 9, 2004
Date of Patent:
March 30, 2010
Assignee:
Merck Frosst Canada & Co.
Inventors:
Michael Boyd, Cheuk Lau, Christophe Mellon, Bruno Roy, John Scheigetz, Vouy Linh Truong
Abstract: The present invention is directed to novel pyridine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to ion channels such as potassium channels.
Abstract: The present invention relates to a novel process for the preparation of 2-amino-methylpyridine derivatives of the formula (I), comprising reacting in a first step 2-substituted pyridine derivatives of the formula (II), with a nitroalkane of the formula (III), in the presence of a base resulting in 2-nitromethylpyridine derivatives of the formula (IV) and hydrogenating these 2-nitromethylpyridine derivatives of the formula (IV) in a second step in the presence of a catalyst and in the presence of an acid, where in the formulae n, X, Y, R1, R2 and A are as defined in the description.
Abstract: A process for preparing ketones of the general formula (III) where R is an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted alkyl radical or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms, and R1 is an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms, by reacting alpha-oxo carboxylates of the general formula (I) wherein n and m is a number in the range from 1 to 6, M(m+) is a cation, and R has the meaning indicated for formula (III), with aryl bromides of the general formula (II) R1—Br ??(II) where R1 has the meaning indicated for formula (III), in the presence of two transition metals or compounds thereof as catalyst, is described.
Type:
Application
Filed:
February 19, 2009
Publication date:
September 3, 2009
Applicant:
SALTIGO GMBH
Inventors:
Alain Cotte, Matthias Gotta, Lukas Goossen, Felix Rudolphi, Christoph Oppel, Nuria Rodriguez Garrido
Abstract: The invention relates to compounds of formula (I) wherein A1 is C(R1R2)p; A2 is C(R6R7)q; p is 1 or 2; q is 1 or 2; each of R1, R2, R3, R4, R5, R6, R7 and R8 which may be the same or different, represents hydrogen, methyl or ethyl and R9 is C1-C4alkyl; R10 is hydrogen, halogen, C1-C3alkyl or C1-C3-haloalkyl, and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.
Type:
Application
Filed:
December 20, 2005
Publication date:
August 6, 2009
Applicant:
SYNGENTA CROP PROTECTION, INC.
Inventors:
Sebastian Volker Wendeborn, Renaud Beaudegnies, Andrew Edmunds, Christoph Luthy, Jürgen Schaetzer
Abstract: The invention relates to a process for preparing enantiomer-enriched 3-heteroaryl-3-hydroxypropanoic acid derivatives and 3-heteroaryl-1-aminopropan-3-ols, and to their use.
Type:
Grant
Filed:
September 24, 2003
Date of Patent:
June 30, 2009
Assignee:
Lanxess Deutschland GmbH
Inventors:
Frank Berendes, Markus Eckert, Nils Brinkmann, Claus Dreisbach, Ruth Meissner, Rainhard Koch
Abstract: Novel compounds for the prevention and treatment of dermatological disorders with an immunoallergic, hyperproliferative and inflammatory component, and a method of producing such compounds. The compounds are bioisosteres of substances with avenanthramide structures.
Abstract: The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur.
Type:
Grant
Filed:
August 30, 2004
Date of Patent:
March 17, 2009
Assignee:
Locus Pharmaceuticals, Inc.
Inventors:
Martha Kelly, Bruce D. Dorsey, Gary A. Flynn
Abstract: The present invention relates to a process for the preparation of compounds of formula (I) wherein the substituents are as defined in claim 1, by reaction of a compound of formula (II) wherein R3 is C1-C8alkyl or C3-C6cycloalkyl and R4 and R05 are as defined for formula (I), with a compound of formula (III) wherein R, R1, R2 and X1, are as defined for formula (I) in claim 1, in an inert solvent in the presence of a proton source.
Type:
Grant
Filed:
March 5, 2004
Date of Patent:
February 10, 2009
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
David Anthony Jackson, Martin Charles Bowden
Abstract: Novel biaryl compounds having the structural formula (I): are useful in a variety of pharmaceutical applications, whether human or veterinary, and also in cosmetics.
Abstract: The present invention relates to a process for the manufacture of compounds of formula Ia or Ib and pharmaceutically acceptable additional salts thereof, wherein R is lower alkyl. The compounds of formula Ia or Ib are valuable intermediate products for the manufacture of compounds that are pharmaceutically active as adenosine A2a receptor antagonist or metabotropic Glutamate receptor 2 antagonist. Such compounds are important in the regulation of many aspects of cellular metabolism and in the modulation of different central nervous system activities.
Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
Type:
Application
Filed:
July 2, 2008
Publication date:
November 27, 2008
Applicant:
CHEMOCENTRYX, INC.
Inventors:
SOLOMON UGASHE, Zheng Wei, J.J. Wright, Andrew Pennell
Abstract: The invention relates to novel substituted pyridyl ketones of the formula in which A, R, X, Y, Z and n are as defined in the disclosure, to processes for preparing these novel substances, and to their use as crop treatment agents, in particular as herbicides. The invention further relates to novel intermediates of the formulae and to processes for their preparation.
Type:
Grant
Filed:
April 16, 2003
Date of Patent:
October 21, 2008
Assignee:
Bayer CropScience AG
Inventors:
Hans-Georg Schwarz, Dorothee Hoischen, Kristian Kather, Klaus-Helmut Müller, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
Abstract: Process for preparing unsubstituted or nuclear-substituted ?-chloroalkyl pyridyl ketones and/or their hydrochlorides by reacting the corresponding unsubstituted or nuclear-substituted alkyl pyridyl ketone hydrochlorides with sulfuryl chloride at a reaction temperature of from ?25 to 70° C. (248 to 343 K) and a pressure of 0.05 to 0.2 MPa abs, in which the reaction is carried out in the presence of an unbranched or branched C1 to C10-alkanoic acid which is unsubstituted or monosubstituted to completely substituted by a radical selected from the group of fluorine, chlorine and bromine and whose melting point is below the chosen reaction temperature.
Abstract: The invention relates to the use of quaternary pyridium salts of formula (1) wherein R is NH2, CH3, or N(H)CH2OH group, and X is pharmaceutically acceptable counterion, for the preparation of vasoprotective agent for the treatment or prevention of conditions or diseases associated with dysfunction of vascular endothelium, oxidative stress, and/or insufficient production of endothelial prostacyclin PGI2, in particular but not exclusively if the above coincides with hypercholes terolemia, hypertriglyceridemia or low HDL level.
Abstract: A four-step process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone of the formula: starting from 2-methyl-5-ethylpyridine. 1-(6-Methylpyridin-3yl)-2-[4-(methylsulfonyl)phenyl]ethanone is an intermediate for preparing inhibitors.
Type:
Grant
Filed:
January 6, 2005
Date of Patent:
April 8, 2008
Assignees:
Lonza Ltd., Merck & Co. Inc.
Inventors:
David Kuo, James E. Leresche, Ralf Proplesch, Jean-Paul Roduit, Yves Bessard, Erich Armbruster
Abstract: A process is disclosed for preparing a heterocyclic aldehyde by oxidizing a heterocyclic alcohol with high selectivity and high yield. Specifically, the heterocyclic aldehyde is prepared by reacting a heterocyclic compound having at least one hydroxymethyl group bonded to a carbon atom of a heterocyclic ring with a hypohalogenous acid salt in the presence of a base to oxidize the hydroxymethyl group, wherein reaction is conducted in the co-presence of a 2,2,6,6-tetramethylpiperidine-1-oxyl derivative having at least two 2,2,6,6-tetramethylpiperidine-1-oxyl-4-yl groups.
Abstract: A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts thereof, where the variables are as defined further herein.
Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
Type:
Grant
Filed:
June 16, 2000
Date of Patent:
January 22, 2008
Assignee:
Astellas Deutschland GmbH
Inventors:
Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
Abstract: Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN—COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an ?,?-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.
Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
Type:
Grant
Filed:
January 5, 2005
Date of Patent:
September 25, 2007
Assignee:
Nicox S.A.
Inventors:
Eninnio Ongini, Valerio Chiroli, Francesca Benedini, Piero Del Soldato
Abstract: The invention relates to a process for preparing 2-halopyridinecarboxamides of primary aromatic monoamines I which have a substituent other than hydrogen in the ortho-position to the amino group by reaction of 2-halopyridinecarbonyl chloride II with the aromatic monoamine I, which comprises carrying out the reaction in a solvent mixture comprising water and at least one water-immiscible organic solvent in the presence of none or less than 10 mol %, based on the 2-halopyridinecarbonyl chloride II, of a base other than I or II.
Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
Type:
Grant
Filed:
May 21, 2003
Date of Patent:
July 3, 2007
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Paul Fleming, Geraldine C. B. Harriman, Zhan Shi, Shaowu Chen
Abstract: This invention provides a compound of the formula (I): wherein A represents a phenyl group or the like: B represents an aryl or the like: E represents a 1,4-phenylene group; R1 and R2 independently represent a hydrogen atom or the like: R3 and R4 independently represent a hydrogen atom or the like: R5 represents —CO2H or the like: R6 represents an alkyl group having from 1 to 6 carbon atoms or the like: X represents a methylene group or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
Abstract: The present invention is directed in part towards methods of modulating the function of calcium channels with pyridine- or 1,4-dihydropyridine-based compounds. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyridine- or 1,4-dihydropyridine-based compounds and pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
January 10, 2005
Date of Patent:
June 26, 2007
Assignee:
Vittal Mallya Scientific Research
Inventors:
Phani Kumar Pullela, Paramashivappa Rangappa, Srinivasa Rao Alapati, Pillarisetti V. Subbarao, Jeffrey A. Bibbs
Abstract: The invention relates to novel 1,4-dihydro-1,4-diphenylpyridine derivatives of formula (I) wherein the variable groups are as defined in the text and claims. Processes for their preparation, pharmaceutical compositions containing them, and methods of treatment of inflammatory processes, expecially chronic obstructive pulmonary diseases, using them are also disclosed and claimed.
Type:
Grant
Filed:
December 9, 2002
Date of Patent:
April 3, 2007
Assignee:
Bayer HealthCare AG
Inventors:
Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Kevin Nash, Mary Fitzgerald
Abstract: A starting product for the preparation of COX-2 inhibitors, notably the compound 1-(6-methylpyridine-3-yl)-2-[(4-(methylsulfonyl)phenyl]ethanone of the formula (I): A method for making the compound.
Type:
Grant
Filed:
January 13, 2000
Date of Patent:
November 28, 2006
Assignee:
Lonza AG
Inventors:
Erich Armbruster, Yves Bessard, David Kuo, James E. Leresche, Ralf Proplesch, Jean-Paul Roduit
Abstract: The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
Type:
Grant
Filed:
October 25, 2002
Date of Patent:
October 24, 2006
Assignees:
Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New York
Inventors:
Ronald Breslow, Sandro Belvedere, Leland Gershell, Thomas A. Miller, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
April 12, 2004
Date of Patent:
September 5, 2006
Assignee:
Amgen Inc.
Inventors:
Daniel Elbaum, Benny C. Askew, Jr., Shon Booker, Julie Germain, Gregory J. Habgood, Michael Handley, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Vinod F. Patel, Chester Chenguang Yuan, Joseph L. Kim, Guolin Cai, Guoqing Chen, Michael Croghan, Lucian V. Di Pietro, Celia Dominguez, Qi Huang, Leon M. Smith, II, Andrew Tasker, Ning Xi, Shimin Xu
Abstract: A process for the production of acetylopyridines of the formula (1): by reacting a pyridinecarboxylic ester of the formula (II): wherein R1 is C1-6-alkyl, with acetic acid in the gas phase in the presence of a catalyst. The active material of the catalyst is titanium dioxide and at least one alkali or alkaline earth metal oxide, and it is supported on an alumina-silica support having an apparent porosity of at least 50 percent. The process has the advantage of producing only small amounts of by-products (e.g, pyidine).
Abstract: The present invention relates to a novel antifungal antibacterial compound 2-methylheptylisonicotinate of formula 1 below obtained from natural sources and to a process for the isolation thereof.
Type:
Grant
Filed:
December 20, 2001
Date of Patent:
February 14, 2006
Assignee:
Council of Scientific and Industrial Research
Inventors:
Gojendra Nath Bordoloi, Babita Kumari, Nabibjyoti Bordoloi, Monoj Kanti Roy, Tarun Chandra Bora
Abstract: The present invention relates to a new process for preparing beta-ketoester compound of the following formula (1), which is a useful intermediate for the synthesis of such quinoline antibiotics as Ciprofloxacin, Levofloxacin, Gemifloxacin, Trovafloxacin, etc. The quinoline antibiotics obtained from the above compound of formula (1) show potent antibacterial activity, and so are advantageously used as a therapeutic agent for bacterial infections of humans or animals.
Abstract: A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.
Type:
Grant
Filed:
November 26, 2003
Date of Patent:
January 10, 2006
Assignee:
Wyeth
Inventors:
John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark, Wei Li
Abstract: The present invention provides processes useful in the preparation of certain ?3-adrenergic receptor agonists of the structural formula the pharmaceutically acceptable salts thereof, and the hydrates of said pharmaceutically acceptable salts, wherein HET is as described herein. The invention further provides intermediates useful in the preparation of such agonists, and processes useful in the production of such intermediates.
Type:
Grant
Filed:
October 9, 2003
Date of Patent:
July 19, 2005
Assignee:
Pfizer Inc,
Inventors:
Robert J. Chambers, Robert W. Dugger, Ming Kang, Yong Tao, John W. Wong
Abstract: The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX?) methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.
Type:
Grant
Filed:
January 4, 2001
Date of Patent:
April 19, 2005
Assignee:
Ferrer Internacional, S.A.
Inventors:
Rafael Foguet, Jorge Ramentol, Diego Fernandez-Cano, Miguel P. Armengol, Inés Petschen, Juan Sallares, Francesc X. Camps, Manuel M. Raga, Josep M. Castello
Abstract: The present invention is directed in part towards methods of modulating the function of calcium channels with pyridine- or 1,4-dihydropyridine-based compounds. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyridine- or 1,4-dihydropyridine-based compounds and pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
January 14, 2003
Date of Patent:
February 8, 2005
Assignee:
Vittal Mallya Scientific Research Foundation
Inventors:
Phani Kumar Pullela, Paramashivappa Rangappa, Srinivasa Rao Alapati, Pillarisetti V. Subbarao, Jeffrey A. Bibbs
Abstract: The invention relates to a process for preparing 2-halopyridinecarboxamides of primary aromatic monoamines I which have a substituent other than hydrogen in the ortho-position to the amino group by reaction of 2-halopyridinecarbonyl chloride II with the aromatic monoamine I, which comprises carrying out the reaction in a solvent mixture comprising water and at least one water-immiscible organic solvent in the presence of none or less than 10 mol %, based on the 2-halopyridinecarbonyl chloride II, of a base other than I or II.
Abstract: The invention relates to a salt formed of at least one AT1-receptor antagonist having at least one acidic center and of at least one cardiovascular ingredient having at least one basic center that can be used for treating cardiovascular diseases and conditions, their prophylaxis or delay of progression.
Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
Type:
Application
Filed:
April 15, 2004
Publication date:
December 23, 2004
Applicant:
The Regents of the University of Michigan
Abstract: Compounds of formula (I), wherein the substituents R1, R2, R3, R4 and Z and the suffixes n and m are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomers of those compounds are suitable for use as herbicides.
Type:
Application
Filed:
July 14, 2004
Publication date:
December 9, 2004
Inventors:
Jurgen Schaetzer, Martin Eberle, Jean Wenger, Sabine Berteina-Raboin, Kurt Nebel, Andre Stoller, Roger Graham Hall, Steven Scott Bondy, Daniel Dennis Comer, Julie Elizabeth Penzotti, Peter Diederik Jan Grootenhuis
Abstract: The invention relates to a process for the preparation of 5-arylnicotinaldehydes by reduction of the corresponding 5-arylnicotinic acids by catalytic hydrogenation in the presence of carboxylic anhydrides in which the catalyst used is a palladium/ligand complex, characterized in that the molar ratio between palladium and ligand is from 1:5 to 1:15 in the case of monodentate ligands and from 1:2.5 to 1:7.5 in the case of bidentate ligands.
Type:
Grant
Filed:
January 5, 2001
Date of Patent:
November 24, 2009
Assignee:
Merck Patent GmbH
Inventors:
Andreas Bathe, Heinz Bokel, Ralf Knieriemen, Christoph Muermann, Thomas Keil