Abstract: The present invention relates to compounds of formula (I) wherein R1 is as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
Type:
Grant
Filed:
December 13, 2005
Date of Patent:
August 12, 2008
Assignee:
Hoffman-La Roche Inc.
Inventors:
Markus Boehringer, Daniel Hunziker, Bernd Kuhn, Bernd Michael Loeffler, Hans Peter Marty, Patrizio Mattei, Robert Narquizian
Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.
Type:
Grant
Filed:
May 30, 2006
Date of Patent:
June 10, 2008
Assignee:
Ortho McNeil Pharmaceutical, Inc.
Inventors:
Peter J. Connolly, William V. Murray, Steven K. Wetter, Sigmond Johnson, Victor T. Bandurco, Jacqueline Bussolari
Abstract: A process for hydrogenating nitrile functions present in organic compounds over at least one heterogeneous catalyst, in which the hydrogenation is carried out in the presence of an ionic liquid, is described.
Type:
Grant
Filed:
December 20, 2004
Date of Patent:
June 3, 2008
Assignee:
BASF Aktiengesellschaft
Inventors:
Verena Weiskopf, Till Gerlach, Kirsten Wenz
Abstract: The present invention provides isolated N-methyl-3-(3-methylphenoxy)-3-phenylpropylamine hydrochloride, and preparation thereof as well as of N-methyl-3-(4-methylphenoxy)-3-phenylpropylamine hydrochloride and of N-methyl-3-phenoxy-3-phenylpropylamine hydrochloride. The invention further provides the use of the above compounds as reference markers and/or reference standards during the synthesis of Atomoxetine. Also provided is a method of limiting the amounts of the impurities 3FT (3-fluorotoluene), 4FT (4-fluorotoluene), and FB (fluorobenzene) in the 2-fluorotoluene starting material used in the synthesis of Atomoxetine Hydrochloride. The purity of the Atomoxetine Hydrochloride product is ensured by determining the amounts of 3FT, 4FT, and FB in the 2-fluorotoluene starting material with the marker 3-ATM HCl.
Type:
Grant
Filed:
June 28, 2005
Date of Patent:
May 27, 2008
Assignee:
Teva Pharmaceutical Fine Chemicals S.r.l.
Abstract: The present invention is to prepare efficiently 2?-amino-5?-hydroxypropiophenone corresponding to the AB-ring part of camptothecin (CPT) skeleton and a tricyclic ketone corresponding to the CDE-ring part in order to provide efficiently CPT by the total synthesis, which is a starting material for irinotecan hydrochloride and various kinds of camptothecin derivatives, and to provide stably CPT and its derivatives.
Abstract: Provided herein are processes for conversion of methane to acetic acid. In one embodiment, the processes are for direct, selective conversion of methane to acetic acid in a single step.
Abstract: The present invention provides the diaminophenyladamantane derivatives with antitumor activities and the preparation method therefore. The method includes a step of reacting an aromatic diol with at least one 5-halo-2-nitrophenol in the presence of at least one inorganic base in an organic solvent with a relatively high boiling point.
Type:
Grant
Filed:
April 21, 2005
Date of Patent:
April 29, 2008
Assignee:
National Taiwan University of Science & Technology
Abstract: The present invention relates to novel dihydronaphthalene compounds, compositions, methods for using the same, and processes for preparing the same. The present invention also relates to novel total synthesis approaches for preparing these compounds. In addition, the present invention relates to methods of producing quantities of isomers of these compounds and separating and purifying them using chiral separation techniques. The present invention also relates to methods of producing quantities of a single isometric compound without the need for chiral separation techniques.
Type:
Grant
Filed:
July 27, 2005
Date of Patent:
April 22, 2008
Assignee:
Amgen Inc.
Inventors:
Qi Yan, Carlos Orihuela, Bo Shen, Ying Chen, Xin Wang, John Ng, Ruizhi Ji, Pengzu Zhou
Abstract: The present invention relates to halogenated 4-aminophenols and to halogenated 4-(phenyidiazenyl)phenols, to a process for their preparation and to the use of the halogenated 4-hydroxyphenols for preparing active ingredients, especially in pharmaceuticals and agrochemicals.
Type:
Grant
Filed:
September 3, 2004
Date of Patent:
April 15, 2008
Assignee:
LANXESS Deutschland GmbH
Inventors:
Karen Peilstöcker, Albrecht Marhold, Jens-Peter Joschek
Abstract: A process is described for the preparation of N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenyl-propaneamine comprising substitution of the sulfonyloxy group of the compound of the formula in which the substituents R and R? have the meanings stated in the description, in a solvent comprising an ionic liquid, to yield the tertiary amine of the formula and the subsequent deprotection thereof.
Type:
Grant
Filed:
October 6, 2005
Date of Patent:
April 15, 2008
Assignee:
Chemi SPA
Inventors:
Stefano Turchetta, Umberto Ciambecchini, Pietro Massardo
Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
Abstract: Provided are processes for preparing tomoxetine comprising reacting N-methyl-3-hydroxy-3-phenylpropylamine with dimethylsulfoxide (DMSO) and 2-fluorotoluene in the presence of an alkali base to form tomoxetine. Also provided is the conversion of said tomoxetine into atomoxetine or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
June 28, 2005
Date of Patent:
April 8, 2008
Assignee:
Teva Pharmaceutical Fine Chemicals S.r.l.
Inventors:
Eugenio Castelli, Giuseppe Lo Monaco, Silvia Mantovani, Paola Daverio, Paolo Riva, Alessandra Vailati, Stefano Bianchi
Abstract: The invention provides a method for manufacturing a tertiary amine, including reacting a tertiary amine with an alcohol and a primary or secondary amine in a reactor loaded with a film type catalyst, controlling the superficial velocity of liquid in the reactor at 0.1 cm/s or more.
Abstract: 3(4),7(8)-bis(aminomethyl)bicyclo[4.3.0]nonane and a process for its preparation, wherein bicyclo[4.3.0]nona-3,7-diene is reacted with synthesis gas in a homogeneous organic phase in the presence of transition metal compounds of Group VIII of the Periodic Table containing complex-bound organophosphorus compounds, and excess organophosphorus compound, at temperatures of 70 to 160° C. and pressures of 5 to 35 MPa, and the 3(4),7(8)-bisformylbicyclo[4.3.0]nonane thus obtained is reductively aminated.
Abstract: A process for preparing long chain internal fatty tertiary amines, quaternary amines and amine oxides via the selection of long chain internal olefins.
Type:
Grant
Filed:
November 10, 2005
Date of Patent:
March 11, 2008
Assignee:
Procter & Gamble Company
Inventors:
Corey James Kenneally, Jeffrey John Scheibel
Abstract: The invention relates to substituted amino compounds, to processes for their preparation, to pharmaceutical formulations containing these compounds and to the use of these substances in the preparation of pharmaceutical formulations, especially for the treatment or inhibition of depression, anxiety, pain and urinary incontinence, and to related methods of treating or inhibiting these disorders.
Type:
Grant
Filed:
January 16, 2007
Date of Patent:
March 11, 2008
Assignee:
Gruenenthal GmbH
Inventors:
Petra Bloms-Funke, Elmar Friderichs, Ivars Graudums, Hagen-Heinrich Hennies, Achim Kless, Klaus Schiene, Oswald Zimmer
Abstract: Thyronamine derivatives and analogs, methods of using such compounds, and pharmaceutical compositions containing them are disclosed. Methods of preparing such compounds are also disclosed.
Type:
Grant
Filed:
June 17, 2005
Date of Patent:
March 4, 2008
Assignees:
The Regents of the University of California, Oregon Health & Science University
Inventors:
Thomas S. Scanlan, Matthew E. Hart, David K. Grandy, James R. Bunzow
Abstract: A process for the preparation of compounds of formula (I): HO-A-ONO2??(I) wherein A is a C2-C6 alkylene chain, the compounds of formula (I) being synthesized by nitration of the corresponding alkanediols with “stabilized” nitric acid is herein disclosed. The process is safer to operators and allows to obtain advantageous yields on an industrial scale.
Abstract: The invention relates to a continuously operated process for the purification by distillation of the 1,2-propylene glycol formed as by-product in the synthesis of propylene oxide, wherein the mixture formed in the synthesis which contains the 1,2-propylene glycol is separated in a dividing wall column into low-, intermediate- and high-boiling fractions and the 1,2-propylene glycol is taken off as intermediate boiler at the side offtake of the column.
Type:
Grant
Filed:
July 22, 2003
Date of Patent:
February 19, 2008
Assignee:
BASF Aktiengesellschaft
Inventors:
Peter Bassler, Hans-Georg Goebbel, Joaquim Henrique Teles, Peter Rudolf