Abstract: Disclosed is a method for producing an amide compound represented by the formula (3) below and having an excellent control activity against a harmful arthropod, which is characterized in that an aniline compound represented by the formula (1) below and an aldehyde compound represented by the formula (2) below are reacted in a solvent in the presence of an oxidizing agent such as oxygen or a peroxide. (In the formulae below, R1, R2 and R3 independently represent a C1-C6 alkyl group which may be substituted by a halogen atom, or the like; and R4, R5, R6 and R7 independently represent a halogen atom or the like.
Type:
Grant
Filed:
April 9, 2008
Date of Patent:
February 21, 2012
Assignee:
Sumitomo Chemical Company, Limited
Inventors:
Yoshihiko Nokura, Hiroshi Ikegami, Markus Jachmann
Abstract: The invention relates to a process for preparing the compound of formula 1, a valuable intermediate product in the synthesis of the pharmaceutical active substance dabigatran etexilate.
Abstract: To provide a process for producing a specific anthranilamide compound or its salt. To provide a process for producing an anthranilamide compound represented by the formula (I) or its salt: wherein each of R1a and R3 which are independent of each other, is halogen or haloalkyl; R2 is cyclopropyl alkyl or cyclobutyl alkyl; and Hal is a chlorine atom or a bromine atom, which comprises a step of selectively halogenating a compound represented by the formula (II): wherein R1a, R2 and R3 are as defined above.
Abstract: Compounds of formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
Type:
Grant
Filed:
May 22, 2007
Date of Patent:
January 31, 2012
Assignee:
Eli Lilly and Company
Inventors:
Michael Gregory Bell, Robert Anthony Doti, Matthew Scott Dowling, Michael James Genin, Peter Ambrose Lander, Tianwei Ma, Nathan Bryan Mantlo, Jason Matthew Ochoada, Lindsay Scott Stelzer, Ryan Edward Stites, Alan M Warshawsky
Abstract: The present invention relates to a high assayed esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention further provides an improved and commercially viable process for preparation of high assayed esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides an improved process for preparation of pure amorphous esomeprazole magnesium. The present invention further provides an improved and commercially viable process for preparation of substantially enantiomerically pure esomeprazole in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. The present invention also provides solid form of esomeprazole calcium salt, its polymorphs (form 1, form 2 and amorphous form) and processes for their preparation thereof.
Abstract: This invention provides a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, theremostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.
Type:
Grant
Filed:
April 17, 2009
Date of Patent:
January 31, 2012
Assignee:
Hanmi Holdings Co., Ltd.
Inventors:
Tae Hee Ha, Hee Sook Oh, Won Jeoung Kim, Chang Hee Park, Eun Young Kim, Young Hoon Kim, Kwee Hyun Suh, Gwan Sun Lee
Abstract: A compound of formula (I): wherein A1 represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; X represents —C(R3)— or nitrogen; when X represents —C(R3)—, R2 represents hydrogen and R1 represents fluorine, R3 represents hydrogen or fluorine, when X represents —C(R3)— and R2 and R1 each represent hydrogen, R3 represents hydrogen, hydroxy, methoxy or fluorine, when X represents —C(R3)— and R2 represents hydroxy, methoxy, —CO2CH3 or —CO2CH2CH3, R1 and R3 each represent hydrogen, when X represents nitrogen, R1 and R2 each represent hydrogen; and Y represents H or methyl; or a physiologically functional derivative thereof.
Type:
Grant
Filed:
April 12, 2006
Date of Patent:
January 10, 2012
Assignee:
Glaxo Group Limited
Inventors:
Colin David Eldred, David House, Graham George Adam Inglis, Simon John Fawcett MacDonald, Philip Alan Skone
Abstract: An object of the present invention is to provide a novel compound which has a potent inhibitory effect on FXa and exhibits an excellent antithrombotic effect when orally administered.
Abstract: A salt of a compound of formula (I) may be made with methanesulfonic acid. The salt and salts with other acids may be prepared by recovering from methyl tert-butyl ether (MTBE).
Abstract: A compound of general formula (I): A process for preparing this compound. A compound of general formula (II): A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
Type:
Grant
Filed:
May 17, 2006
Date of Patent:
December 6, 2011
Assignee:
Bayer Cropscience AG
Inventors:
Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
Abstract: The present invention provides a process for preparing the amorphous rabeprazole sodium. The process comprises the following steps: (a) Contacting rabeprazole sodium compound with a solvent system to thereby obtain a clear solution under a first temperature, wherein said solvent system is a mixture of at least two categories of organic solvents; (b) Stirring said clear solution of step (a) under a second temperature for a certain time period to obtain a solution containing resultant separated solid, wherein said second temperature is equal to or lower than said first temperature; (c) Filtering said solution containing resultant separated solid obtained from step (b) to obtain a wet solid; and (d) Drying said wet solid to obtain an amorphous rabeprazole sodium compound.
Abstract: A compound of general formula (I) A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
Type:
Grant
Filed:
November 24, 2008
Date of Patent:
December 6, 2011
Assignee:
Bayer SAS
Inventors:
Pierre-Yves Coqueron, Philippe Desbordes, Darren James Mansfield, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Alain Villier, Pierre Genix
Abstract: The present invention relates to the mono-sulfate salt, crystalline forms A and B of the mono-sulfate salt, an amorphous form of the mono-sulfate salt, hemi-sulfate salts, and a crystalline form A of the hemi-sulfate salt of the compound 2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine.
Type:
Grant
Filed:
December 17, 2007
Date of Patent:
November 22, 2011
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Thomas Cleary, Alexander Glomme, Olaf Grassmann, Shan-Ming Kuang, Roland Meier, Doreen Miller, Regina Moog, Franziska E. Rohrer, Jason Yang
Abstract: 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid of formula (5) or a salt thereof, is prepared by reacting reacting 2-bromo-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine of formula (3) or a salt thereof, with a metal cyanide, to obtain 2-cyano-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine of formula (4) or a salt thereof, and hydrolyzing the 2-cyano-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine of formula (4) or a salt thereof.
Type:
Grant
Filed:
November 8, 2010
Date of Patent:
November 15, 2011
Assignee:
Daiichi Sankyo Company, Limited
Inventors:
Hiroshi Nagasawa, Koji Sato, Tsutomu Yagi, Yasuo Kitani
Abstract: The invention provides a compound of formula (I): (where R1, Q, A and R2 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Pyridine-alkynyl Compound”); pharmaceutical compositions comprising an effective amount of a Pyridine-alkynyl Compound; and methods for treating or preventing a condition such as pain, urinary incontinence, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, a seizure, stroke, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia or depression in an animal comprising administering to an animal in need thereof an effective amount of a Pyridine-alkynyl Compound.
Abstract: There is provided a heterocycle-substituted pyridine derivative's salt or a crystal thereof. The present invention provides an acid addition salt of 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-yl amine or a crystal thereof as well as process for producing the same.
Abstract: Described herein are compounds that are useful as ROCK inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including cardiovascular, inflammatory, neurological, or proliferative diseases or disorders.
Type:
Grant
Filed:
May 10, 2007
Date of Patent:
November 15, 2011
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jeremy Green, Jingrong Cao, Upul Bandarage, Jon Come, Craig Marhefka
Abstract: The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
Type:
Grant
Filed:
April 17, 2008
Date of Patent:
November 8, 2011
Assignee:
Bristol-Myers Squibb Company
Inventors:
Timothy F. Herpin, George C. Morton, Robert P. Rehfuss, R. Michael Lawrence, Michael A. Poss, Jacques Y. Roberge, Timur Gungor
Abstract: It is an object of the present invention to provide (1) a process for manufacturing alkali metal salts of 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1H-benzimidazole which are useful as gastric acid secretion inhibitors, anti-ulcer agents and other drugs and (2) salts of 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1H-benzimidazole with amines which are intermediates for the production of the alkali metal salts, and a process for manufacturing the same. According to the present invention, disclosed are salts represented by the following formula (I): (wherein A+ represents an isopropylammonium ion, sec-butylammonium ion or cyclopentylammonium ion).