Abstract: Methods are provided for improving production of 3,5-diethyl-1,2-dihydro-1-phenyl-2-propylpyridine (DHP). In one illustrative embodiment, the methods involve controlling the rate of reaction and temperature of the reaction during formation of DHP. In another illustrative embodiment, the methods involve neutralizing the acid catalyst subsequent to DHP formation.
Type:
Grant
Filed:
February 10, 2006
Date of Patent:
December 19, 2006
Assignee:
Reilly Industries, Inc.
Inventors:
Martin Grendze, Ramiah Murugan, L. Mark Huckstep, Charles R. Hopper
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 conversion of a compound of formula II reaction of that compound with a compound of formula IV X—C(O)—Q,??(IV) wherein X is a leaving group, to form a compound of formula V and treatment of that compound in the presence of a base with catalytic amounts of cyanide ions.
Type:
Grant
Filed:
February 11, 2005
Date of Patent:
November 14, 2006
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
Hermann Schneider, Christoph Lüthy, Andrew Edmunds
Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for, and intermediates used in, their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
Type:
Grant
Filed:
November 12, 2002
Date of Patent:
October 31, 2006
Assignee:
AstraZeneca AB
Inventors:
Lilian Alcaraz, Timothy Johnson, Michael Stocks
Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula I in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z are as defined in the specification. The compounds are useful in treating malignant tumours, for example, ovarian, stomach, colon, breast, adeno-, head and neck carcinomas, acute lymphocytic and myelocytic leukemia. In addition, these compounds are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases such as psoriasis and arthritis. Methods of use and preparation of the compounds are also described.
Type:
Grant
Filed:
May 1, 2000
Date of Patent:
October 24, 2006
Assignee:
Schering AG
Inventors:
Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann, Jens Hoffmann, Rosemarie Lichtner
Abstract: There are provided novel compounds of formula (I) wherein R1, R2, R3, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease, CNS disorders and pain.
Type:
Grant
Filed:
July 26, 2002
Date of Patent:
October 10, 2006
Assignee:
Astrazeneca AB
Inventors:
Deborah Chen, David Cheshire, Stephen Connolly, Antonio Mete
Abstract: This invention relates to compounds of the formula wherein one of R5, R6 and R7 is and X1, X2, Y1 to Y4, R1 to R13 and m and n are defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.
Type:
Grant
Filed:
October 29, 2004
Date of Patent:
October 3, 2006
Assignee:
Hoffmann-la Roche Inc.
Inventors:
Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Matthew Blake Wright
Abstract: An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-? inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-?.
Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.
Abstract: The present invention relates to processes for the preparation of a compound of the formula wherein W is nitrogen or —CR3; R1 is halogen, haloalkyl, haloalkoxy, R4S(O)n— or —SF5; R2 is hydrogen or halogen; R3 is halogen; R4 is alkyl or haloalkyl; and n is 0, 1 or 2; and processes for using a compound of the formula (I) in the synthesis of compounds of the formula
Abstract: The invention relates to anthranilic acid amide derivatives of formula (I), wherein R1 represents H or lower alkyl, R2 represents H or lower alkyl, R3 represents perfluoro lower alkyl, and X is O or S, or an N-oxide or a tautomer thereof, to salts of such anthranilic acid amides, their N-oxides and their tautomers; processes for the preparation thereof, the application thereof for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age—related macular degeneration; a method for the treatment of such a disease in animals, especially in humans, and the use of such a compound—alone or in combination with one or more other pharmaceutically active compounds—for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.
Type:
Grant
Filed:
November 7, 2002
Date of Patent:
August 15, 2006
Assignee:
Novartis AG
Inventors:
Guido Bold, Pascal Furet, Paul W Manley
Abstract: The present invention relates to crystalline hydrates of substituted anilide derivatives, to their preparation, and to their use for controlling phytopathogenic fungi or undesired attack by insects or mites and/or for regulating the growth of plants.
Type:
Grant
Filed:
September 14, 2002
Date of Patent:
August 8, 2006
Assignee:
BASF Aktiengesellschaft
Inventors:
Matthias Bratz, August Wigger, Peter Erk, Hans Ziegler, Thomas Kröhl, Karl-Friedrich Jäger, Horst Mayer
Abstract: Oxycodone is manufactured in high yields and with a high purity using a composition including a thebaine component into 14-hydroxycodeinone and then reduction of 14-hydroxycodeinone to oxycodone.
Type:
Grant
Filed:
July 16, 2004
Date of Patent:
July 4, 2006
Assignee:
Acura Pharmaceuticals
Inventors:
Charles Auxilium Francis, Zhaiwei Lin, Christopher Arne Kaldahl, Kazimierz Grzegorz Antczak, Vijai Kumar
Abstract: The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt pro-drug or solvate thereof. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) and methods for the treatment or prevention of cancer comprising administering an effective amount of a compound of Formula (Ia).
Type:
Grant
Filed:
October 26, 2001
Date of Patent:
June 27, 2006
Assignee:
AstraZeneca
Inventors:
Francis Thomas Boyle, Keith Hopkinson Gibson, Kevin Michael Foote
Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Grant
Filed:
June 3, 2004
Date of Patent:
June 27, 2006
Assignee:
Pfizer Inc
Inventors:
Alan Daniel Brown, Justin Stephen Bryans, Charlotte Alice Louise Lane, Simon John Mantell
Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.
Type:
Grant
Filed:
June 9, 2004
Date of Patent:
June 13, 2006
Assignee:
Pfizer Inc
Inventors:
Simon Bailey, Elisabeth C. L. Gautier, Alan J. Henderson, Thomas V. Magee, Anthony Marfat, John P. Mathias, Dale G. McLeod, Sandra M. Monaghan, Blanda L. C. Stammen
Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.
Type:
Grant
Filed:
May 9, 2003
Date of Patent:
June 6, 2006
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Jr., Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
Abstract: A process of forming a d-tocotrienol from a (2S)-vinylchromane compound, through hydroboration of the (2S)-vinylchromane to provide an organoborane, followed by coupling the organoborane with a halogenated C-14 sidechain compound under conditions of palladium-catalyzed cross-coupling is taught. Methods for providing the (2S)-vinylchromane compound and the halogenated C-14 compound are disclosed.
Type:
Grant
Filed:
October 12, 2004
Date of Patent:
May 2, 2006
Assignee:
Yasoo Health, Inc.
Inventors:
Elias A. Couladouros, Andreas M. Papas, Vassilios I. Moutsos, Maria Lampropoulou
Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.
Abstract: A compound of the formula: wherein R1 and R2 each is H or a hydrocarbon group which may be substituted, or R1 and R2 form a 3- to 8-membered carbo or heterocyclic ring which may be substituted; R3 is H, a lower alkyl which may be substituted or an aromatic group which may be substituted; R4 is (1) an aromatic group which may be substituted, (2) an aliphatic hydrocarbon group substituted by an aromatic group which may be substituted, which hydrocarbon group may be further substituted or (3) an acyl; X and Y each is oxygen or sulfur which may be oxidized; and ring A is a benzene ring which may be further substituted, or a salt thereof, is useful for an agent for suppressing neurodegeneration.
Abstract: The invention is a process to hydrogenate an aryl-substituted pyridine, such as 2-phenyl-3-aminopyridine, without over-reducing the aryl ring using a specific Pt/C catalyst.
Type:
Grant
Filed:
January 5, 2004
Date of Patent:
February 7, 2006
Assignee:
Pfizer INC
Inventors:
Timothy James Norman Watson, Michael Girard Vetelino