Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/298)
  • Patent number: 10519113
    Abstract: The present invention relates to a compound having the structure of formula (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where X, Y, Z, R, R1, R2, R3, R4, R5, and R6 are as described herein. The present invention also relates to compositions containing the compound having the structure of formula (I), and a method of treating cancer in a subject.
    Type: Grant
    Filed: August 17, 2017
    Date of Patent: December 31, 2019
    Assignee: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI
    Inventors: Arvin C. Dar, Ross L. Cagan, Alex P. Scopton, Masahiro Sonoshita
  • Patent number: 9879036
    Abstract: The present invention provides compounds that bind to mitochondrial aldehyde dehydrogenase-2 (ALDH2), methods of using said compounds to treat patients with Fanconi Anemia, and methods of preparing said compounds.
    Type: Grant
    Filed: February 19, 2015
    Date of Patent: January 30, 2018
    Assignee: Aviv Therapeutics, Inc.
    Inventors: Wenjin Yang, Yie-Teh Yu, Chun Jiang
  • Patent number: 9573900
    Abstract: The invention relates to polymorphs of deuterated omega-diphenylurea or salts thereof. In particular, the invention provides polymorphs of 4-(4-{3-[4-chloro-3-(trifluoromethyl)phenyl)-ureido]-phenoxy}-2-(N-1?,1?,1?-trideutero-methyl)picolinamide or its salt, namely, polymorphs of the compound as shown in formula (I) or its salt. The polymorphs are suited for preparing the pharmaceutical composition used for inhibiting phosphokinase (such as raf kinases).
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: February 21, 2017
    Assignee: Suzhou Zelgen Biopharmaceutical Co., Ltd.
    Inventor: Weidong Feng
  • Patent number: 9365558
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: June 14, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Lidet A. Negash
  • Patent number: 9133156
    Abstract: The present disclosure relates to a novel method for preparing selenyl-substituted aromatic aldehyde compounds by forming a selenolate nucleophile and performing a nucleophilic substitution reaction between the selenolate nucleophile and an aromatic aldehyde starting material.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: September 15, 2015
    Assignees: Sejong University Industry Academy Cooperation Foundation, Samsung Life Public Welfare Foundation
    Inventors: Dongyeol Lim, Do-Hyun Nam, Rashmi Dubey
  • Patent number: 9061982
    Abstract: The present invention relates to the preparation of oxovinylionol and its O-protected derivatives of the formula I in which R is hydrogen or an OH protecting group, for example a group Si(Ra)3, by reacting a compound of the general formula II in which R has the meanings given above for formula I, i.e. ?-vinyl ionol (formula II, R=hydrogen) or an O-protected derivative thereof (formula II, R?OH protecting group) with an oxidant in the presence of at least one transition metal, where the oxidant comprises at least one oxygen-containing compound which is selected from among hydrogen peroxide and organic hydroperoxides.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: June 23, 2015
    Assignee: BASF SE
    Inventors: Hansgeorg Ernst, Michael Puhl, Stefan Benson, Wolfgang Siegel
  • Publication number: 20150141467
    Abstract: Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Inventors: James Densmore Copp, Ann W. Newman, Anne Luong
  • Publication number: 20150133669
    Abstract: The present invention relates to new processes for the preparation of 2-cyclopentyl-6-methoxy-isonicotinic acid, which is a useful intermediate for the synthesis of pyridine-4-yl derivatives as immunomodulating agent. Moreover, the present invention also relates to new intermediates used in those processes.
    Type: Application
    Filed: May 21, 2013
    Publication date: May 14, 2015
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventor: Gunther Schmidt
  • Patent number: 9029401
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: May 12, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Publication number: 20150111929
    Abstract: The present invention provides an industrially suitable process for the preparation of substantially pure 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide or Sorafenib and its tosylate salt, with a suitable impurity profile and without requirement of any additional purification steps. The present invention also provides Sorafenib base (II) as stable crystalline Form-SSB. The present invention further relates to a process for the preparation of crystalline Sorafenib tosylate Form-I which is free from contamination of any other polymorphic form of Sorafenib tosylate, for e.g. Form II or Form III, and does not involve any seeding requirement for crystallization step.
    Type: Application
    Filed: December 31, 2012
    Publication date: April 23, 2015
    Inventors: Prashant Purohit, Sriram Rampalli, Mohanrao Seshagiri Vijaya Murali, Lavkumar Upalla
  • Publication number: 20150099766
    Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Michael MAUE, Isabelle ADELT, Wolfgang GIENCKE, Markus HEIL, Peter JESCHKE, Bernd-Wieland KRÜGER, Friedrich August MÜHLTHAU, Alexander SUDAU, Klaus RAMING, Ulrich EBBINGHAUS-KINTSCHER, Martin ADAMCZEWSKI, Arnd VOERSTE, Ulrich GÖRGENS, Tobias KAPFERER, Mark Wilhelm DREWES, Angela BECKER, Eva-Maria FRANKEN
  • Patent number: 9000163
    Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: April 7, 2015
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Masaaki Nagasawa, Kazuyasu Asami, Ryu Nakao, Nobuyuki Tanaka, Yoshiyuki Aida
  • Patent number: 8993557
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: John Lloyd, Jennifer X. Qiao, Heather Finlay, James Neels, Zulan Pi, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150080362
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 19, 2015
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Tamil Arasu, John David Baird, Wu Du, Olya Ginzburg, Yi Jin Kim Gorske, Jana Narasimhan, Srinivasa Peddi, Hongyan Qi, Sean Wesley Smith, Anthony Allan Turpoff, Richard Gerald Wilde, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang
  • Publication number: 20150057298
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, X, m, R2, Y, R3, Z, n, R4, A and B are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Inventors: William BUFFHAM, Hannah CANNING, Richard DAVENPORT, William FARNABY, Stephen MACK, Alka PARMAR, Susanne WRIGHT
  • Publication number: 20150051199
    Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.
    Type: Application
    Filed: October 31, 2012
    Publication date: February 19, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Christopher Charles Frederick Hamlett, Gilbert Ebai Besong, Gianni Chessari, Maria Grazia Carr, Alessia Millemaggi, David Norton, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson, Steven Douglas Hiscock
  • Patent number: 8957254
    Abstract: Process for synthesizing a chemical, in particular an agriculturally or pharmaceutically active compound, including: a first step comprising reacting a carboxylic acid halide with a vinyl ether to prepare a halogenated precursor of an alkenone; a second step comprising eliminating hydrogen halide from such precursor to form an alkenone, preferably by thermolysis under specific conditions; and a third step which uses the formed alkenone as a building block to synthesize the chemical. First step may be done in a liquid reaction medium comprising an alkenone or a halogenated alkenone precursor, or in a liquid reaction medium in turbulent state, specifically by creation of gas bubbles of the carboxylic acid halide herein. Second step may include a flash thermolysis, vacuum thermolysis, thermolysis under stripping with inert gas, and/or a thermolysis at a temperature from >90° C. to 120° C. Third step preferably comprises reacting the alkenone with a nitrogen-containing compound.
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: February 17, 2015
    Assignee: Solvay SA
    Inventors: Max Braun, Stefan Palsherm, Uta Claassen, Alain Lambert
  • Patent number: 8937088
    Abstract: A compound of Formula (I), salts thereof, prodrugs thereof, metabolites thereof, pharmaceutical compositions containing such a compound, and use of such compound and compositions to treat diseases mediated by multiple kinases, such as raf, VEGFR, PDGFR, FLT-3, and c-Kit.
    Type: Grant
    Filed: January 5, 2012
    Date of Patent: January 20, 2015
    Assignees: Astar Biotech LLC, Beta Pharma Canada Inc.
    Inventors: Zhaoyin Wang, Chunrong Yu
  • Patent number: 8933235
    Abstract: The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: January 13, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Zulan Pi, John Lloyd, Jennifer X. Qiao, Tammy C. Wang, George O. Tora
  • Patent number: 8933236
    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: Grant
    Filed: May 21, 2013
    Date of Patent: January 13, 2015
    Assignees: 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
  • Publication number: 20150005328
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 1, 2015
    Inventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
  • Publication number: 20140315958
    Abstract: The present invention relates to 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide monohydrate, to processes for its preparation, to pharmaceutical compositions comprising it and to its use in the control of disorders.
    Type: Application
    Filed: May 14, 2014
    Publication date: October 23, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alfons GRUENBERG, Juregen STIEHL, Katharina TENBIEF, Birgit KEIL
  • Patent number: 8865908
    Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 21, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Frederic Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
  • Patent number: 8865742
    Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: October 21, 2014
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Publication number: 20140309264
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK
  • Publication number: 20140296240
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Gary Mark COPPOLA, Yuki IWAKI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Gary Michael KSANDER, Muneto MOGI, Robert SUN
  • Patent number: 8841330
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: September 23, 2014
    Assignee: Bayer Healthcare LLC
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood
  • Patent number: 8791102
    Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: July 29, 2014
    Assignee: Exelixis, Inc.
    Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
  • Publication number: 20140206647
    Abstract: There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.
    Type: Application
    Filed: March 26, 2014
    Publication date: July 24, 2014
    Applicant: SYNTRIX BIOSYSTEMS, INC.
    Inventors: Dean Y. Maeda, John A. Zebala
  • Publication number: 20140200225
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 17, 2014
    Applicant: ORION CORPORATION
    Inventors: Rajeev GOSWAMI, Anil Kumar VUPPALA, Ramesh VELUDANDI, Ramesh SISTLA, Chakshusmathi GHADIYARAM, Muralidhara RAMACHANDRA
  • Patent number: 8778977
    Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: July 15, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
  • Patent number: 8759531
    Abstract: A fluoro-substituted deuterated diphenylurea compound, especially 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-2-(N-(methyl-d3))picolinamide, preparing method and use for treating or preventing tumor and relative diseases thereof.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: June 24, 2014
    Assignee: Suzhou Zelgen Biopharmaccceutical Co., Ltd.
    Inventors: Weidong Feng, Xiaoyong Gao, Xiaojun Dai
  • Patent number: 8741936
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: June 3, 2014
    Assignee: Intermune, Inc.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Patent number: 8722895
    Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
    Type: Grant
    Filed: April 9, 2013
    Date of Patent: May 13, 2014
    Assignee: Akebia Therapeutics, Inc.
    Inventors: Richard M. Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
  • Publication number: 20140128612
    Abstract: Methods and processes for preparation and production of deuterated ?-diphenylurea are disclosed. Especially, a kind of deuterated ?-diphenylurea compounds which can inhibit phosphokinase and the preparation method of N-(4-chloro-3-(trifluoromethyl)phenyl)-N?-(4-(2-(N-d3-methylcarbamoyl)-4-pridinyloxy)phenyl)urea are disclosed. The said deuterated diphenylurea compounds can be used for treating or preventing tumors and relative diseases.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Applicant: Suzhou Zelgen Biopharmaceutical Co., Ltd.
    Inventors: Weidong FENG, Xiaoyong GAO, Xiaojun DAI
  • Patent number: 8716283
    Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.
    Type: Grant
    Filed: April 1, 2009
    Date of Patent: May 6, 2014
    Assignees: University of Massachusetts, President and Fellows of Harvard College
    Inventors: Jon Goguen, Ning Pan, Kyungae Lee
  • Publication number: 20140107110
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 17, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
  • Publication number: 20140093513
    Abstract: The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.
    Type: Application
    Filed: May 24, 2013
    Publication date: April 3, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Chi B. Vu
  • Publication number: 20140094456
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 3, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
  • Patent number: 8686154
    Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: April 1, 2014
    Assignee: Emisphere Technologies, Inc.
    Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
  • Publication number: 20140088156
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Application
    Filed: February 14, 2012
    Publication date: March 27, 2014
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Publication number: 20140088158
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
  • Patent number: 8669369
    Abstract: Methods and processes for preparation and production of deuterated ?-diphenylurea are disclosed. Especially, a kind of deuterated ?-diphenylurea compounds which can inhibit phosphokinase and the preparation method of N-(4-chloro-3-(trifluoromethyl)phenyl)-N?-(4-(2-(N-d3-methylcarbamoyl)-4-pridinyloxy)phenyl)urea are disclosed. The said deuterated diphenylurea compounds can be used for treating or preventing tumors and relative diseases.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: March 11, 2014
    Assignee: Suzhou Zelgen Biopharmaceutical Co., Ltd.
    Inventors: Weidong Feng, Xiaoyong Gao, Xiaojun Dai
  • Patent number: 8669254
    Abstract: The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 11, 2014
    Assignee: Hoffman-La Roche Inc.
    Inventors: Paul Hebeisen, Stephan Roever
  • Patent number: 8669209
    Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: March 11, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
  • Publication number: 20140066421
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Application
    Filed: May 17, 2012
    Publication date: March 6, 2014
    Applicant: SOUTHWEST RESEARCH INSTITUTE
    Inventors: Stanton F. McHardy, Richard M. Corbett, Donald M. Maxwell, Michael W. Tidwell, Bismarck Campos, Christopher J. Bemben
  • Patent number: 8664248
    Abstract: The present invention relates to methods of treating hepatitis C infection, HIV infection, AIDS, or AIDS-related complex, or inhibiting HIV replication by administering a compound of Formula I wherein: X is H or OH; Y is H or OH; R1 is H or halogen (F, Cl, Br, I); R2 is H or halogen (F, Cl, Br, I); R3 is H, C1-6 alkyl, C1-6 fluoroalkyl, or benzyl; R4 is H, C1-6 alkyl, or benzyl; and R5 is H or C1-6 alkyl; or pharmaceutically acceptable salts thereof, to a mammal.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: March 4, 2014
    Assignee: TaiMed Biologics, Inc.
    Inventors: Brent Richard Stranix, Guy Milot, Jean-Emmanuel Bouchard
  • Publication number: 20140058104
    Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.
    Type: Application
    Filed: October 29, 2013
    Publication date: February 27, 2014
    Applicant: ZERIA PHARMACEUTICAL CO., LTD.
    Inventors: Masaaki NAGASAWA, Kazuyasu Asami, Ryu Nakao, Nobuyuki Tanaka, Yoshiyuki Aida
  • Publication number: 20140057926
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM
  • Publication number: 20140057916
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennnis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH