Sulfonamides (i.e., Q-(o=)s(=o)-hnh, Wherein Q Is A Substituent And Wherein Any Substituent Replacing One Or Both Hydrogens Shown Will Be Referred To As E) Patents (Class 564/80)
  • Patent number: 10173993
    Abstract: A one pot single step process is described for the synthesis of a compound, including a labeled compound, containing a sulfonyl functional group comprising the step of mixing together a silane, an SO2 source, an electrophilic compound, an activating compound and optionally a metal catalyst. A process for producing tracers from a labeled sulfonyl containing compound prepared by the described process is also included.
    Type: Grant
    Filed: December 8, 2016
    Date of Patent: January 8, 2019
    Assignee: Commissariat a l'Energie Atomique et aux Energies Alternatives
    Inventors: Niklas von Wolff, Joëlle Char, Thibault Cantat
  • Patent number: 9353050
    Abstract: A process for the preparation of isosulfan blue (Active Pharmaceutical Ingredient) is provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon mild oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: May 31, 2016
    Assignee: Apicore US LLC
    Inventors: Ravishanker Kovi, Satyam Nampalli, Peter Xavier Tharial
  • Patent number: 9276241
    Abstract: The case for a molten salt battery is used for a molten salt battery containing as an electrolyte a molten salt containing sodium ions. The case is formed of aluminum or an aluminum alloy containing 90% by mass or more of aluminum.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: March 1, 2016
    Assignee: SUMITOMO ELECTRIC INDUSTRIES, LTD.
    Inventors: Koji Nitta, Shoichiro Sakai, Shinji Inazawa, Chihiro Hiraiwa, Atsushi Fukunaga, Masatoshi Majima
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Patent number: 8993630
    Abstract: The present invention relates to substituted sulphonamido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: March 31, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ingo Hartung, Marion Hitchcock, Florian Puhler, Gerhard Siemeister, Roland Neuhaus
  • Patent number: 8969552
    Abstract: The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH?N—, —CH?CH— or —N?CH—; A is CH2, O or S; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition salts
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: March 3, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Patent number: 8889906
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: November 18, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Patent number: 8884058
    Abstract: The present invention relates to the preparation of (R)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
    Type: Grant
    Filed: April 23, 2013
    Date of Patent: November 11, 2014
    Assignee: Ardea Biosciences
    Inventors: Andreas Maderna, Jean Michel Vernier
  • Publication number: 20140315954
    Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Inventors: Geoffrey C. WINTERS, Alexander L. Mandel, BRADLEY J. HEDBERG
  • Publication number: 20140309206
    Abstract: The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 16, 2014
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
  • Patent number: 8859765
    Abstract: The present invention provides efficient and economical methods for synthesis of (?)-2-exo-morpholinoisoborne-10-thiol, its enantiomer, and related chiral catalysts. Novel compounds and methods of asymmetric synthesis are also disclosed.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: October 14, 2014
    Assignee: ScinoPharm Taiwan, Ltd.
    Inventors: Ping-Yu Wu, Julian Paul Henschke
  • Patent number: 8859814
    Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: October 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
  • Patent number: 8841483
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: April 11, 2007
    Date of Patent: September 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Pramod Joshi, Paul Krenitsky, Jesus Gonzalez, III, Jian Wang, Dean Wilson, Andreas Termin
  • Publication number: 20140256701
    Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 11, 2014
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins, Sean Turner
  • Patent number: 8829052
    Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: September 9, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
  • Patent number: 8808742
    Abstract: This invention relates to compositions, methods for preparing the compositions and methods for treating or preventing diseases, comprising administering the compositions.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: August 19, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Barry D. Quart, Colin Edward Rowlings
  • Patent number: 8808961
    Abstract: An embodiment of the composition contains any of compounds of the formula A-LG in which A represents any of residues of general formula (A-1) below and LG represents any of groups that are cleaved to generate acids of the formula A-H when acted on by an acid. The composition further contains at least one of a compound that generates an acid when exposed to actinic rays or radiation and a compound that generates an acid when heated.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: August 19, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Tomotaka Tsuchimura, Takeshi Kawabata, Takayuki Ito
  • Patent number: 8809584
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: August 19, 2014
    Assignee: Institut Univ. de Ciencia i Tecnologia, S.A.
    Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
  • Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Publication number: 20140206741
    Abstract: The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.
    Type: Application
    Filed: April 12, 2012
    Publication date: July 24, 2014
    Applicant: Sichuan Guokang Pharmaceutical Co., Ltd
    Inventors: Luyun Zhang, Fang Yang, Wanqi Shi, Ping Zhang, Ying Li, Shufan Yin
  • Patent number: 8772343
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I):(I) or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R3, R4 and R5 are as defined in the description. Nav1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: July 8, 2014
    Assignee: Pfizer Limited
    Inventors: Andrew Simon Bell, Alan Daniel Brown, Russell Andrew Lewthwaite, Manuel Perez-Pacheco, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Patent number: 8759399
    Abstract: Aromatic N-halosulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to release active halogen ions has been utilized in a range of biocidal and fungicidal applications. This disclosure deals with the use of halo active aromatic sulfonamide organic compounds as odor control and/or biocidal agents in a cleaning solution for use with bovines and other dairy animals.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: June 24, 2014
    Inventors: David J. Schneider, Charles A. Schneider
  • Patent number: 8759577
    Abstract: Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: June 24, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventor: Stuart Dimock
  • Patent number: 8754237
    Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: June 17, 2014
    Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: James Elliot Bradner, Ralph Mazitschek, Weiping Tang, Stuart L. Schreiber
  • Publication number: 20140155637
    Abstract: The present invention relates to a novel enantioselective method of preparing (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-5 methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide.
    Type: Application
    Filed: May 24, 2012
    Publication date: June 5, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Peter Fey, Agathe Christine Mayer
  • Publication number: 20140148498
    Abstract: The instant invention provides methods and compositions for the treatment and prevention of Marfan syndrome and related diseases, disorders and conditions. The invention further provides pharmaceutical compositions and kits for the treatment and prevention of Marfan syndrome and related diseases, disorders and conditions.
    Type: Application
    Filed: April 13, 2012
    Publication date: May 29, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Harry C. Dietz, Jefferson J. Doyle, Jennifer Pardo Habashi, Tammy Holm
  • Patent number: 8729138
    Abstract: The present invention relates to a mixture of polyfluoroalkylsulfonamido alkyl amines including at least one polyfluoroalkylsulfonamido alkyl amine and its analog, a di(polyfluoroalkylsulfonamido alkyl)amine. The invention also relates to polyfluoroalkylsulfonamido alkyl halide intermediate used to make the aforementioned mixture.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: May 20, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Alexander Borisovich Shtarov, Volodymyr B. Pashovych
  • Patent number: 8648116
    Abstract: This invention concerns N-(2-arylamino) aryl sulfonamide compounds which are inhibitors of MEK including crystalline polymorphic forms which exhibit a specific powder x-ray diffraction profile and/or a specific differential scanning calorimetry profile. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein, including the use in the treatment and/or prevention of cancer, hyperproliferative diseases and inflammatory conditions. The invention also concerns methods of making the compounds and compositions described herein.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: February 11, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Michel Vernier, Colin Edward Rowlings, Jean-Luc Girardet, Stuart Dimock, Barry Quart, Jeffrey N. Miner
  • Patent number: 8614201
    Abstract: Certain heterocyclic amide compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPA1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: December 24, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Didier Jean-Calude Berthelot, Henricus Jacobus Maria Gijsen, Mirko Zaja, Jason Rech, Alec Lebsack, Bryan Branstetter, Wei Xiao, J. Guy Breitenbucher
  • Patent number: 8609897
    Abstract: The present invention is directed to a novel trifluoromethylsulfonamide derivative which inhibits the processing of APP by the putative ?-secretase and thus is useful in the treatment or prevention of Alzheimer's disease. This compound possesses favorable pharmacokinetic properties in higher species (rhesus) and thus can be dosed on an intermittent dosing regiment (e.g., once weekly). When dosed on such a regiment the compound exhibits significant and continuous A? lowering without the manifestation of Notch associated gastrointestinal toxicity for extended periods, e.g., 7 days. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew Daniels, Jed Hubbs, Thomas Miller
  • Patent number: 8609839
    Abstract: Camphor-derived compounds are disclosed, which are represented as the following formula (I): wherein R1, R2, R3, and R4 each are defined as described in the specification. In addition, a method for manufacturing the camphor-derived compounds and application thereof are disclosed.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: December 17, 2013
    Assignee: National Tsing Hua University
    Inventors: Biing-Jiun Uang, Bo-Yao Yang
  • Publication number: 20130317000
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 28, 2013
    Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INC
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Patent number: 8569378
    Abstract: The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G1, G2, G3 and G8 are each independently selected from —N? etc., Ring G6 is selected from divalent aryl etc., A is selected from amino etc., G4 is selected from oxygen etc., G5 is selected from oxygen etc., G7 is selected from —CH2— etc., and R2 is selected from C1-6 alkyl etc.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: October 29, 2013
    Assignees: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Toshiyuki Sakai, Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
  • Publication number: 20130261339
    Abstract: Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
    Type: Application
    Filed: May 30, 2013
    Publication date: October 3, 2013
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventor: Stuart DIMOCK
  • Patent number: 8536229
    Abstract: The invention provides compounds of formula I wherein n, A, R, R?, R?, RO, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: September 17, 2013
    Assignee: Novartis AG
    Inventors: Fabrizio Gasparini, Yves Auberson, Silvio Ofner, Terance W Hart, Kaspar Zimmerman
  • Patent number: 8530521
    Abstract: A compound having the structure wherein Y is selected from the group consisting of —C(O)OR2, —C(O)NHR8, —C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: September 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Robert K. Baker, Kathleen M. Rupprecht, Michael Man-Chu Lo, Brent Whitehead
  • Patent number: 8524778
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl sulfonamides and related compounds (collectively referred to herein as ‘BPSAAA compounds’), as described herein, and including, for example, biphenyl-4-sulfonic acid (hydroxyalkyl-phenyl)-amides and related compounds.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: September 3, 2013
    Assignee: PIMCO 2664 Limited
    Inventors: Iain Robert Greig, Robert Jurgen Van't Hof, Stuart Hamilton Ralston
  • Patent number: 8518998
    Abstract: The present invention relates to the use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides of the formula I, wherein A and R1 to R6 have the meanings indicated in the claims, for treating pain and for manufacturing a medicament for the treatment of pain.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: August 27, 2013
    Assignee: Sanofi-aventis Deutschland GmbH
    Inventors: Karl Rudolphi, Martin Michaelis, Hans Guehring
  • Patent number: 8501992
    Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: August 6, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kyoung S. Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
  • Publication number: 20130184238
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 18, 2013
    Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
  • Publication number: 20130184342
    Abstract: The technology described herein relates to methods of inducing cell death. The technology described herein further relates to treating conditions including cancers and autoimmune diseases comprising administering inhibitors of double strand break repair. Also described herein are inhibitors of double strand break repair and methods of screening for such inhibitors.
    Type: Application
    Filed: March 13, 2013
    Publication date: July 18, 2013
    Applicant: THE JACKSON LABORATORY
    Inventor: THE JACKSON LABORATORY
  • Patent number: 8487098
    Abstract: A synergistic antimicrobial composition containing flumetsulam and an isothiazolone biocide chosen from among 4,5-dichloro-2-n-octyl-4-isothiazolin-3-one, 2-n-octyl-4-isothiazolin-3-one and N-n-butyl-1,2-benzisothiazolin-3-one. A synergistic antimicrobial composition containing diclosulam and an isothiazolone biocide chosen from 4,5-dichloro-2-n-octyl-4-isothiazolin-3-one and 2-n-octyl-4-isothiazolin-3-one.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: July 16, 2013
    Assignee: Dow Global Technologies LLC
    Inventor: Emerentiana Sianawati
  • Patent number: 8466316
    Abstract: Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: June 18, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventor: Stuart Dimock
  • Publication number: 20130150574
    Abstract: The present invention provides efficient and economical methods for synthesis of (?)-2-exo-morpholinoisoborne-10-thiol, its enantiomer, and related chiral catalysts. Novel compounds and methods of asymmetric synthesis are also disclosed.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 13, 2013
    Applicant: Scinopharm Taiwan, LTD.
    Inventor: Scinopharm Taiwan, LTD.
  • Patent number: 8461175
    Abstract: The invention relates to a compound of formula (I), where: R1 is a phenyl group optionally substituted by one or more halogen atoms; R2 is: a hydrogen atom or a halogen atom or a cyano group; a —C(?O)Y group where Y is a hydrogen atom, or a —NH2 or —OR3 group; a —C(?S)NH2 group; a —C(?NH)NH—OH group; a —CH2OH or —CH2F group; a —CH?N—OH group; a —CH?CH2 or —C?C—R3 group; a H or H R1 group being a hydrogen or (C1-C4)alkyl group; R3 is a hydrogen atom or (C1-C4)alkyl group; and R4 is a —NH2, (C1-C4)alkyl, (C1-C4)fluoroalkyl or (C3-C7)cycloalkyl group.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: June 11, 2013
    Assignee: Sanofi-Aventis
    Inventors: Georges Delettre, Stéphanie Deprets, Frank Halley, Laurent Schio, Fabienne Thompson
  • Patent number: 8461209
    Abstract: The invention provides a sulfonyl malonamide derivative, or a pharmacologically acceptable salt thereof or a solvate thereof, that has therapeutic and/or preventive effects(s) on various diseases due to its agonist action at AT2 receptor, and is useful as a pharmaceutical agent for the treatment and/or prevention of diseases involving the renin-angiotensin-aldosterone system (RAAS).
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: June 11, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Tomohiro Yoshida, Hiroshi Sakashita, Atsushi Numata, Saori Tahara, Hisashi Kawasumi
  • Publication number: 20130004509
    Abstract: The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of BRAF. In particular embodiments, the invention concerns mutations in a BRAF sequence that confer resistance to a BRAF inhibitor. Identification of such mutations in a BRAF sequence allows the identification and design of second-generation BRAF inhibitors. Methods and kits for detecting the presence of a mutant BRAF sequence in a sample are also provided.
    Type: Application
    Filed: February 22, 2011
    Publication date: January 3, 2013
    Inventor: Levi Garraway
  • Publication number: 20120330019
    Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 27, 2012
    Inventors: Xiangdong Alan Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Piyasena Hewawasam, Andrew Charles Good, Yan Chen, Jeffrey Allen Campbell
  • Publication number: 20120295881
    Abstract: The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: July 11, 2012
    Publication date: November 22, 2012
    Applicant: Abbott GmbH & Co. KG
    Inventors: Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Frauke Pohlki, Charles W. Hutchins