Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 549/468)
  • Patent number: 9499507
    Abstract: The invention relates to a method for preparing 5-amino-benzoyl-benzofuran derivatives having the general formula in which R1 is hydrogen or an alkyl or aryl group and R2 is hydrogen, an alkyl, alkoxy or dialkylaminoalkoxy group. According to the invention, the compounds having formula I are prepared by hydrogenating a 5-nitro-benzofuran derivative having the general formula in which R1 and R2 have the same meaning as above in the presence of palladized charcoal as a catalyst and in an ether or a mixture of ether as a solvent, thus forming the desired compounds.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: November 22, 2016
    Assignee: SANOFI
    Inventors: Xavier Bon, Jean-Louis Delepine, Laure Jourdin, Denis Largeau, Philippe Vayron
  • Patent number: 9221778
    Abstract: The invention relates to a process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that from the compound of formula (II). The hydroxyl group is removed, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: December 29, 2015
    Assignee: SANOFI
    Inventors: Antal Friesz, Zsolt Dombrády
  • Patent number: 9193703
    Abstract: The invention relates to a novel process for preparation of N-[2-n-butyl-3-[4-[3-(di-n-butylamino)-propoxy]-benzoyl]-benzofuran-5-yl]methanesulfonamide (I) and pharmaceutical acceptable salts thereof, where a salt of (5-amino-2-butyl-1-benzofuran-3-yl){4-[3-(di-n-butylamino)propoxy]phenyl}methanone of formula (II)—where A is a mono- or dibasic acid forming an acid addition salt with the compound of formula (II), n is 1 if A is dibasic acid and n is 1 or 2 if A is a monobasic acid—is reacted with a mesylating reagent in a heterogen reaction, if desired, in the presence of a phase transfer catalyst. The invention also relates to the novel salts of compound of formula (II), for the preparation thereof and their use in the preparation of dronedarone.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: November 24, 2015
    Assignee: SANOFI
    Inventors: Antal Friesz, Csaba Huszar
  • Patent number: 9174958
    Abstract: This disclosure relates to a process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)-propoxy]-benzoyl}-1-benzofuran-5-yl]-methane-sulfonamide of formula I and its pharmaceutically acceptable salts, wherein one of the methylsulfonyl groups of the 2-n-butyl-3-[(di-n-butylamino-3-propoxy)-benzoyl]-5-bis-(methylsulfonamido)-benzofuran of formula II is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: November 3, 2015
    Assignee: SANOFI
    Inventor: Antal Friesz
  • Patent number: 9024046
    Abstract: The invention relates to a novel process for preparation of drohedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that a compound of formula (II) is reacted in the presence of a reductive agent with butyraldehyde and/or butanoic acid, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some hovel intermediary compounds and the preparation thereof.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: May 5, 2015
    Assignee: Sanofi
    Inventors: Antal Friesz, Csaba Huszar
  • Patent number: 8993620
    Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: March 31, 2015
    Assignee: Virginia Commonwealth University
    Inventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
  • Publication number: 20150065734
    Abstract: The present disclosure relates to processes for preparing dronedarone or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: August 26, 2014
    Publication date: March 5, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Johann Chan, Justin Vitale
  • Patent number: 8962869
    Abstract: The invention relates to a method for synthesizing benzofuran derivatives, in particular the dronedarone of formula (D), including carrying out a Fries rearrangement reaction using a sulfonamido-benzofuran ester intermediate.
    Type: Grant
    Filed: March 23, 2012
    Date of Patent: February 24, 2015
    Assignee: Sanofi
    Inventors: Bernard Grimaud, Pierre-Jean Grossi
  • Publication number: 20150031902
    Abstract: The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof which comprises oxidizing a compound of formula (IV) or a salt thereof with an oxidizing agent in an organic or inorganic solvent or solvent mixture, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (IV), and a process for the preparation thereof.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 29, 2015
    Applicant: SANOFI
    Inventors: Csaba Huszár, Adrienn Hegedus, Zsolt Dombrády
  • Publication number: 20150018568
    Abstract: The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof, characterized in that a compound of formula (II)—where L is leaving group—is reacted with compound of formula (III) and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 1, 2013
    Publication date: January 15, 2015
    Inventor: Antal Friesz
  • Patent number: 8927743
    Abstract: The present invention provides a process for obtaining dronedarone or salts thereof characterized in that in an organic phase comprising one or more non-polar solvents, 5-amino-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-2-n-butyl-benzofuran is reacted with methane sulfonyl chloride without the addition of a base. The invention also provides a process for obtaining intermediates of dronedarone environmentally friendly and industrially viable.
    Type: Grant
    Filed: October 18, 2011
    Date of Patent: January 6, 2015
    Assignee: Laboratorios Lesvi, S.L.
    Inventors: Ravindranath Vishnu Newadkar, Avinash Changdeo Gaikwad, Ajay Madhukar Harad
  • Publication number: 20150005515
    Abstract: The invention relates to a process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that from the compound of formula (II). the hydroxyl group is removed, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 1, 2015
    Inventors: Antal Friesz, Zsolt Dombrády
  • Patent number: 8884033
    Abstract: The disclosure relates to a process for preparing 5-aminobenzoylbenzofuran derivatives of formula I: in which R1 and R2 are as defined in the disclosure; by reduction of a 5-nitrobenzofuran derivative of formula II: using a hydrogen transfer agent, in the presence of palladium-on-charcoal as catalyst and in an ether or an ether mixture as solvent.
    Type: Grant
    Filed: January 16, 2013
    Date of Patent: November 11, 2014
    Assignee: Sanofi
    Inventors: Xavier Bon, Christine Biencourt, Corinne Leroy, Julia Mateos-Caro, Philippe Vayron
  • Patent number: 8871956
    Abstract: The invention relates to a method for preparing 3-keto-benzofurane derivatives of the general formula: Formula (I), where R is an alkyl or aryl group, R1 is hydrogen or an alkyl or aryl group, and R2 is a substituted alkyl or phenyl group. Said preparation method involves coupling a derivative of Formula III, where X is chlorine, bromine, or iodine or a sulfonate grouping: Formula (III) with a sulfonamide derivative of the formula R—SO2—NH2 in the presence of a basic agent and a catalytic system formed of a complex between a palladium compound and a ligand.
    Type: Grant
    Filed: March 30, 2011
    Date of Patent: October 28, 2014
    Assignee: Sanofi
    Inventors: Fréderic Bailly, Thomas Priem, Philippe Vayron
  • Publication number: 20140275093
    Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: October 16, 2013
    Publication date: September 18, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
  • Patent number: 8816103
    Abstract: The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)-propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula I: and pharmaceutically acceptable salts thereof wherein the acyl group of the benzofuran derivative of the general formula II: where R represents C1-4 alkyl-, C1-4 alkoxy- or aryl group, is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.
    Type: Grant
    Filed: January 14, 2013
    Date of Patent: August 26, 2014
    Assignee: Sanofi
    Inventors: Antal Friesz, Csaba Huszar
  • Publication number: 20140221431
    Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 7, 2014
    Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., Ltd
    Inventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
  • Publication number: 20140206761
    Abstract: There is provided a process for the preparation of a compound of formula II, wherein R1, R2, R3 and R4 are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone.
    Type: Application
    Filed: March 24, 2014
    Publication date: July 24, 2014
    Applicant: Cambrex Karlskoga AB
    Inventors: Lars O. HANSSON, Anders BERGH, Lars EKLUND
  • Patent number: 8772511
    Abstract: The invention relates to novel benzothiophene-, benzofuran-, and indole ureas and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning, and/or memory.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: July 8, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Timo Fleβner, Frank-Gerhard Böβ, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Dieter Lang, Joachim Luithle, Marja Van Kampen, Franz-Josef Van der Staay
  • Publication number: 20140171642
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.
    Type: Application
    Filed: February 19, 2014
    Publication date: June 19, 2014
    Applicant: BIONOMICS LIMITED
    Inventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
  • Publication number: 20140171444
    Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.
    Type: Application
    Filed: March 3, 2014
    Publication date: June 19, 2014
    Applicant: THE TEXAS A&M UNIVERSITY SYSTEM
    Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
  • Patent number: 8748636
    Abstract: The disclosure relates to a process for preparing benzofuran derivatives of general formula I: in which R, R1, and R2 are as defined in the disclosure; by coupling the hydroxylamine with a diketone of general formula III: in order to form an oxime that is then cyclized by heating in order to form the desired compound.
    Type: Grant
    Filed: January 16, 2013
    Date of Patent: June 10, 2014
    Assignee: Sanofi
    Inventors: Frederic Bailly, Xavier Bon, Philippe Vayron
  • Publication number: 20140128460
    Abstract: Inhibitors of EYA tyrosine phosphatase are provided herein, as well as pharmaceutical compositions and methods relating thereto.
    Type: Application
    Filed: March 6, 2013
    Publication date: May 8, 2014
    Applicant: CHILDREN'S HOSPITAL MEDICAL CENTER
    Inventor: Children's Hospital Medical Center
  • Publication number: 20140114081
    Abstract: The invention relates to a novel process for preparation of dronedarone (I) and pharmaceutically acceptable salts thereof where the compound of formula (II) or salt thereof is reacted with a compound of formula L-(CH2)3—CH3 (III), where L is a leaving group, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and the preparation thereof.
    Type: Application
    Filed: March 27, 2012
    Publication date: April 24, 2014
    Applicant: SANOFI
    Inventors: Antal Friesz, Zsolt Párkányi, Zsolt Dombrády
  • Publication number: 20140080904
    Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 20, 2014
    Applicant: Virginia Commonwealth University
    Inventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
  • Publication number: 20140081035
    Abstract: The invention relates to a novel process for preparation of N-[2-n-butyl-3-[4-[3-(di-n-butylamino)-propoxy]-benzoyl]-benzofuran-5-yl]methanesulfonamide (I) and pharmaceutical acceptable salts thereof, where a salt of (5-amino-2-butyl-1-benzofuran-3-yl) {4-[3-(di-n-butylamino)propoxy]phenyl}methanone of formula (II)—where A is a mono- or dibasic acid forming an acid addition salt with the compound of formula (II), n is 1 if A is dibasic acid and n is 1 or 2 if A is a monobasic acid—is reacted with a mesylating reagent in a heterogen reaction, if desired, in the presence of a phase transfer catalyst. The invention also relates to the novel salts of compound of formula (II), for the preparation thereof and their use in the preparation of dronedarone.
    Type: Application
    Filed: March 27, 2012
    Publication date: March 20, 2014
    Applicant: SANOFI
    Inventors: Antal Friesz, Csaba Huszar
  • Patent number: 8674119
    Abstract: The present invention relates to the scaled-up synthesis of biologically active compounds which display useful therapeutic activity in treating proliferative disorders. In particular the invention relates to process methods for the kilogram scale synthesis of a particular class of substituted benzofuran tubulin polymerisation inhibitors.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: March 18, 2014
    Assignee: Bionomics Limited
    Inventor: Bernard Luke Flynn
  • Patent number: 8658809
    Abstract: The subject of the present disclosure is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I: and the new intermediates of the preparation process.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 25, 2014
    Assignee: SANOFI
    Inventors: Antal Friesz, Mariann Csatarine Nagy
  • Publication number: 20140046078
    Abstract: The invention relates to a method for synthesizing benzofuran derivatives, in particular the dronedarone of formula (D), including carrying out a Fries rearrangement reaction using a sulfonamido-benzofuran ester intermediate.
    Type: Application
    Filed: March 23, 2012
    Publication date: February 13, 2014
    Applicant: SANOFI
    Inventors: Bernard Grimaud, Pierre-Jean Grossi
  • Publication number: 20140018554
    Abstract: The invention relates to a novel process for preparation of drohedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that a compound of formula (II) is reacted in the presence of a reductive agent with butyraldehyde and/or butanoic acid, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some hovel intermediary compounds and the preparation thereof.
    Type: Application
    Filed: March 27, 2012
    Publication date: January 16, 2014
    Applicant: SANOFI
    Inventors: Antal Friesz, Csaba Huszar
  • Publication number: 20140018553
    Abstract: The invention relates to a process for synthesizing benzofuran derivatives, in particular dronedarone of formula (D), comprising a step of Friedel-Crafts acylation starting from a sulfonamido-benzofuran ester intermediate.
    Type: Application
    Filed: March 23, 2012
    Publication date: January 16, 2014
    Applicant: SANOFI
    Inventors: Bernard Grimaud, Pierre-Jean Grossi
  • Patent number: 8613909
    Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.
    Type: Grant
    Filed: June 25, 2013
    Date of Patent: December 24, 2013
    Assignee: Virginia Commonwealth University
    Inventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
  • Publication number: 20130317100
    Abstract: The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
    Type: Application
    Filed: November 11, 2011
    Publication date: November 28, 2013
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Frank Richter, Erwin Schreiner, Samo Pirc, Anton Copar
  • Publication number: 20130302282
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Application
    Filed: October 21, 2011
    Publication date: November 14, 2013
    Applicant: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Publication number: 20130296296
    Abstract: The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted; R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted; R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted; R4 is hydrogen, halogen, methyl or methoxy; to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.
    Type: Application
    Filed: February 4, 2013
    Publication date: November 7, 2013
    Inventor: ASTRAZENECA AB
  • Publication number: 20130289106
    Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.
    Type: Application
    Filed: June 25, 2013
    Publication date: October 31, 2013
    Inventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
  • Publication number: 20130289287
    Abstract: The present invention provides a process for obtaining dronedarone or salts thereof characterized in that in an organic phase comprising one or more non-polar solvents, 5-amino-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-2-n-butyl-benzofuran is reacted with methane sulfonyl chloride without the addition of a base. The invention also provides a process for obtaining intermediates of dronedarone environmentally friendly and industrially viable.
    Type: Application
    Filed: October 18, 2011
    Publication date: October 31, 2013
    Applicant: LABORATORIOS LESVI, S.L.
    Inventors: Ravindranath Vishnu Newadkar, Avinash Changdeo Gaikwad, Ajay Madhukar Harad
  • Publication number: 20130281394
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: October 24, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
  • Publication number: 20130274325
    Abstract: The invention relates to fluorinated compounds and their use in the field of pathological syndromes of the cardiovascular system. Novel fluorinated benzofuran derivatives of amiodarone and pharmaceutically acceptable salts or solvates thereof and their use for the treatment of arrhythmias are described.
    Type: Application
    Filed: March 12, 2013
    Publication date: October 17, 2013
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards
  • Publication number: 20130261321
    Abstract: The subject of the present invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I: and the new intermediates of the preparation process.
    Type: Application
    Filed: May 30, 2013
    Publication date: October 3, 2013
    Inventors: Antal FRIESZ, Zsolt DOMBRADY, Mariann CSATARINE NAGY
  • Patent number: 8536350
    Abstract: The invention relates to a new process for the preparation of dronedarone and its salts, in particular a synthesis process which allows said compound and its salts to be obtained with good yields, high purity and in an industrially expedient manner; the invention also concerns a new synthesis intermediate.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: September 17, 2013
    Assignee: Laboratorio Chimico Internazionale S.p.A.
    Inventors: Mara Sada, Antonio Nardi, Stefano Maiorana
  • Publication number: 20130225673
    Abstract: A compound represented by the general Formula I: a pharmaceutically acceptable salt or ester thereof, a solvate thereof, a chelate thereof, a non-covalent complex thereof, a pro-drug thereof, a deuterated radio-labeled analog thereof, and mixtures of any of the foregoing, wherein: A-K are individually selected from carbon or nitrogen; X?—O, —NR1, or —S; R1-11 are individually selected from the group consisting of —H, C1-C6 alkyl, C6-C14 aryl, substituted C6-C14 aryl, C1-C14-alkoxy, halogen, hydroxyl, carboxy, cyano, C1-C6-alkanoyloxy, C1-C6-alkylthio, C1-C6-alkylsulfonyl, trifluoromethyl, hydroxy, C2-C6-alkoxycarbonyl, C2-C6-alkanoylamino, —O—R12, S—R12, —SO2—R12, —NHSO2R12 and —NHCO2R12, wherein R12 is phenyl, naphthyl, or phenyl or naphthly substituted with one to three groups selected from C1-C6-alkyl, C6-C10 aryl, C1-C6-alkoxy and halogen, and C4-C20 hydroxyheteroaryl wherein the heteroatoms are selected from the group consisting of sulfur, nitrogen, and oxygen.
    Type: Application
    Filed: October 6, 2011
    Publication date: August 29, 2013
    Applicant: J-PHARMA CO., LTD.
    Inventors: Michael F. Wempe, Hitoshi Endou
  • Publication number: 20130211102
    Abstract: The present invention relates to the scaled-up synthesis of biologically active compounds which display useful therapeutic activity in treating proliferative disorders. In particular the invention relates to process methods for the kilogram scale synthesis of a particular class of substituted benzofuran tubulin polymerisation inhibitors.
    Type: Application
    Filed: July 15, 2011
    Publication date: August 15, 2013
    Applicant: BIONOMICS LIMITED
    Inventor: Bernard Luke Flynn
  • Patent number: 8491872
    Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: July 23, 2013
    Assignee: Virginia Commonwealth University
    Inventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
  • Patent number: 8481763
    Abstract: A process is provided for preparing dronedarone or pharmaceutically acceptable salts thereof. The process comprises reacting 5-amino-2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)benzofuran (compound A) with methanesulfonyl chloride without any catalyst to provide crude dronedarone hydrochloride, which is purified to afford highly pure product. Then, the dronedarone hydrochloride can be converted to highly pure dronedarone through treatment with an alkaline solvent, the dronedarone can be further converted to other pharmaceutically acceptable salts of dronedarone. In this process, acylation between compound A and methanesulfonyl chloride is carried out successfully and the formation of the dimethylsulfonyl by-product is inhibited.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 9, 2013
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Xianshan Hou, Yongjiang Chen
  • Publication number: 20130172390
    Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.
    Type: Application
    Filed: September 14, 2012
    Publication date: July 4, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Markus Heil, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
  • Publication number: 20130165673
    Abstract: The invention relates to a method for preparing 3-keto-benzofurane derivatives of the general formula: Formula (I), where R is an alkyl or aryl group, R1 is hydrogen or an alkyl or aryl group, and R2 is a substituted alkyl or phenyl group. Said preparation method involves coupling a derivative of Formula III, where X is chlorine, bromine, or iodine or a sulfonate grouping: Formula (III) with a sulfonamide derivative of the formula R—SO2—NH2 in the presence of a basic agent and a catalytic system formed of a complex between a palladium compound and a ligand.
    Type: Application
    Filed: March 30, 2011
    Publication date: June 27, 2013
    Applicant: SANOFI
    Inventors: Fréderic Bailly, Thomas Priem, Philippe Vayron
  • Publication number: 20130165675
    Abstract: The disclosure relates to a process for preparing 5-aminobenzoylbenzofuran derivatives of formula I: in which R1 and R2 are as defined in the disclosure; by reduction of a 5-nitrobenzofuran derivative of formula II: using a hydrogen transfer agent, in the presence of palladium-on-charcoal as catalyst and in an ether or an ether mixture as solvent.
    Type: Application
    Filed: January 16, 2013
    Publication date: June 27, 2013
    Applicant: SANOFI
    Inventor: Sanofi
  • Publication number: 20130165674
    Abstract: The disclosure relates to a process for preparing benzofuran derivatives of general formula I: in which R, R1, and R2 are as defined in the disclosure; by coupling the hydroxylamine with a diketone of general formula III: in order to form an oxime that is then cyclized by heating in order to form the desired compound.
    Type: Application
    Filed: January 16, 2013
    Publication date: June 27, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Publication number: 20130131321
    Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; a
    Type: Application
    Filed: August 3, 2011
    Publication date: May 23, 2013
    Applicant: GRAFFINITY PHARMACEUTICALS GMBH
    Inventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul