The Hetero Ring Has At Least Seven Members Patents (Class 514/431)
  • Patent number: 10959430
    Abstract: Compositions and methods for repelling coleopterans. The compositions contain a substrate and an anti-aggregation pheromone intermixed within the substrate. The pheromone may be verbenone, methyl salycylate, wintergreen oil, or combinations thereof.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: March 30, 2021
    Assignee: ISCA TECHOLOGIES, INC.
    Inventors: Agenor Mafra-Neto, Josue Isaias Ponce, William H. Urrutia, Carmem R. Bernardi, Rodrigo Oliveira Da Silva
  • Patent number: 10351576
    Abstract: The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: July 16, 2019
    Assignee: Novartis AG
    Inventors: Donatella Chianelli, Xiaodong Liu, Valentina Molteni, John Nelson, Jason Roland, Paul Vincent Rucker, David Charles Tully
  • Patent number: 9950661
    Abstract: A light source unit including a light source that emits light into a vehicle interior through a lens of a room light, a substrate on which the light source is mounted, the substrate being mounted on a base member of the room light, an engagement portion that engages with, among a plurality of mounting seats that are provided on the base member and that have different protrusion heights, an upper side mounting seat, the engagement portion being provided on the substrate and on a circumference of an imaginary circle formed about the light source, and a clearance portion that is capable of avoiding interference with, among the plurality of mounting seats, a lower side mounting seat, the clearance portion being provided in the substrate and on the circumference of the imaginary circle formed about the light source.
    Type: Grant
    Filed: July 5, 2016
    Date of Patent: April 24, 2018
    Assignee: HONDA MOTOR CO., LTD.
    Inventors: Takeshi Udo, Kenichi Takizawa, Yoshiaki Hirato, Naoki Nakanishi
  • Patent number: 9433603
    Abstract: The present invention relates to the use of 3-(R)-[3-(2-methoxyphenylthio)-2-(S)-methylpropyl]amino-3,4-dihydro-2H-1,5-benzoxathiepine or a pharmaceutically acceptable salt thereof for preventing and/or treating cardiotoxic effects caused by chemotherapy and/or radiation.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: September 6, 2016
    Assignee: PIERRE FABRE MEDICAMENT
    Inventors: Bernard Vacher, Bruno Le Grand
  • Patent number: 9309213
    Abstract: C3-functionalized-cyclopentanyltetrahydrofuranyl carbamates that inhibit HIV proteolytic enzymes and processes for preparing the compounds are described. Compositions comprising the disclosed compound and methods of using the compounds and/or compositions for treating patients infected with HIV are also described.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: April 12, 2016
    Assignee: Purdue Research Foundation
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Bruno D. Chapsal
  • Patent number: 9243006
    Abstract: The present invention provides multi-thiol mercaptoalkoxysilane compositions and methods of making multi-thiol mercaptoalkoxysilane compositions having the formula: wherein the R3 group, and the R4 group are independently an alkoxy, a halogen, an alkyl, an aryl, a heteroaryl, a heterocycle or derivatives thereof and n is an integer between 1 and 30.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: January 26, 2016
    Assignee: Southern Methodist University
    Inventors: David Y. Son, Abby R. Jennings
  • Publication number: 20150119345
    Abstract: Provided herein are methods for treating or preventing gastrointestinal and/or liver infections utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists. Also provided herein are methods for increasing the levels of an enteroendocrine peptide or hormone in an individual suffering from a gastrointestinal infection or liver infection utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists.
    Type: Application
    Filed: October 28, 2014
    Publication date: April 30, 2015
    Applicant: LUMENA PHARMACEUTICALS, INC.
    Inventors: Bronislava GEDULIN, Michael GREY
  • Publication number: 20150045396
    Abstract: The present invention provides a prophylactic or therapeutic agent for giant cell tumors occurring in a bone and soft tissue or for chondrosarcoma, which comprises a non-steroidal anti-inflammatory agent or thiazolidine derivative as an active ingredient, and the like
    Type: Application
    Filed: March 18, 2013
    Publication date: February 12, 2015
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Akihiko Takeuchi, Hiroyuki Tsuchiya
  • Publication number: 20140336148
    Abstract: The present invention relates to novel pharmaceutical combinations with synergistic action of diacerein or a pharmaceutically acceptable salt of diacerein and non-steroidal inflammatory drugs, having analgesic, anti-inflammatory, antipyretic, and osteoarthritis-treating activities.
    Type: Application
    Filed: December 25, 2012
    Publication date: November 13, 2014
    Inventors: Umit Cifter, Ali Turkyilmaz, Nur Pahlivan Akalin, Sibel Zenginer, Onur Mutlu
  • Publication number: 20140323412
    Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 30, 2014
    Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
  • Publication number: 20140308241
    Abstract: Described are biomarkers including TOX useful for the diagnosis or prognosis of T cell malignancy. A level of a biomarker is determined in a sample from a subject and compared to a control level, wherein an increased level of the biomarker in the sample relative to the control level indicates that the subject has T cell malignancy. The T cell malignancy may be a cutaneous T cell lymphoma (CTCL) such as mycosis fungoides or Sezary syndrome.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 16, 2014
    Inventors: Youwen Zhou, Yuanshen Huang, Yang Wang, Ming-wan Su
  • Publication number: 20140243281
    Abstract: Provided herein are pediatric dosage forms for use in the treatment of a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of the pediatric dosage form comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are said pediatric dosage form for use in the treatment of a pediatric liver disease, for use in decreasing the levels of serum bile acids or hepatic bile acids, for use in the treatment of pruritis, for use in reducing liver enzymes or bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: August 28, 2014
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
  • Publication number: 20140235692
    Abstract: The present invention relates to the use of 3-(R)-[3-(2-methoxyphenylthio)-2-(S)-methylpropyl]amino-3,4-dihydro-2H-1,5-benzoxathiepine or a pharmaceutically acceptable salt thereof for preventing and/or treating cardiotoxic effects caused by chemotherapy and/or radiation.
    Type: Application
    Filed: September 13, 2012
    Publication date: August 21, 2014
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Bernard Vacher, Bruno Le Grand
  • Publication number: 20140206743
    Abstract: The present invention relates to the use of 3-(R)-[3-(2-methoxyphenylthio)-2-(S)-methyl-propyl]amino-3,4-dihydro-2H-1,5-benzoxathiepine or one of the pharmaceutically acceptable salts thereof for treating cancer and particularly in preventing and/or treating cancerous metastases.
    Type: Application
    Filed: September 12, 2012
    Publication date: July 24, 2014
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Bernard Vacher, Bruno Le Grand
  • Patent number: 8778895
    Abstract: The invention relates to novel insecticidal active compound combinations comprising, firstly, cyclic ketoenols or other acaricidally active compounds and, secondly, further insecticidally active compounds from the group of the anthranilamides, which combinations are highly suitable for controlling animal pests, such as insects and unwanted acarids.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: July 15, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Christian Funke, Thomas Bretscheneider, Reiner Fischer, Rüdiger Fischer, Heike Hungenberg, Wolfram Andersch, Wolfgang Thielert, Anton Kraus
  • Publication number: 20140066489
    Abstract: Method of exposing agricultural substrates (plant matter 10, animal matter 12) to agrochemicals (A); method of decreasing or preventing sub-surface geological matter (20, 22) contamination resulting from exposing agricultural substrates to agrochemicals; composition [(A)/(T)] 30 used therein; article-of-manufacture including the composition. Includes exposing agricultural substrates to composition including combination (mixture) of an agrochemical and at least one transforming agent capable of decreasing or eliminating concentration of the agrochemical which contacts sub-surface geological matter (at temporally varying times, and at spatially varying depths). Before entering sub-surface geological matter, transforming agent exhibits inactivity for decreasing agrochemical concentration, and inactivity for affecting or/and interfering with agrochemical functionality with respect to agricultural substrates.
    Type: Application
    Filed: November 10, 2013
    Publication date: March 6, 2014
    Applicant: Yeda Research and Development Co. Ltd.
    Inventors: Brian BERKOWITZ, Ishai Dror
  • Publication number: 20130338093
    Abstract: Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 19, 2013
    Publication date: December 19, 2013
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventor: Lumena Pharmaceuticals, Inc.
  • Publication number: 20130217673
    Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of mixed monoamine reuptake inhibitor locally at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least thirty days. In some embodiments, the relief can be for at least at least fifty days, at least one hundred days, at least one hundred and twenty days, at least one hundred and thirty, at least one hundred fifty days or at least one hundred and eighty days.
    Type: Application
    Filed: February 22, 2012
    Publication date: August 22, 2013
    Applicant: Warsaw Orthopedic, Inc
    Inventor: Jared T. Wilsey
  • Publication number: 20130108573
    Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: May 2, 2013
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventor: Lumena Pharmaceuticals, Inc.
  • Publication number: 20130109671
    Abstract: Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: May 2, 2013
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventor: Lumena Pharmaceuticals, Inc.
  • Patent number: 8410292
    Abstract: Disclosed are englerins and derivatives (I) thereof useful in the treatment of a number of cancers, particularly renal cancer, as well as pharmaceutical compositions and method of treating a patient with the use of these derivatives. The englerins, for example Englerin A and Englerin B, can be isolated from the plant Phyllanthus engleri or produced by synthetic methods. An example of the englerin derivative is 2?-chloroenglerin A, which has the structure (II), wherein double bond ‘a’ is E, Z, or a mixture of E and Z.
    Type: Grant
    Filed: December 30, 2008
    Date of Patent: April 2, 2013
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: John A. Beutler, Ranjala Ratnayake, David Covell, Tanya R. Johnson
  • Publication number: 20130059807
    Abstract: Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.
    Type: Application
    Filed: February 22, 2012
    Publication date: March 7, 2013
    Applicant: Satiogen Pharmaceuticals, Inc.
    Inventors: Bronislava Gedulin, Andrew A. Young, Howard E. Greene
  • Patent number: 8372878
    Abstract: There are described compounds of general formula (I) and isomeric forms thereof wherein n is 0, 1, 2 or 3, saturated or unsaturated; most preferably at least one of R1 to R5 represents halogen; at least one of R1, R2, R3, R4 and R5 is selected from —S—R or —COOR, or two or more Of R1-R5 comprise a linking group such as —S—(CH2)mS—, where m is 1, 2 or 3 and R is selected from alkyl having 1 to 5 carbon atoms, cycloalkyl having 3-6 carbon atoms, hydroxy, and aryl having 6 to 10 carbon atoms, such groups being optionally substituted, and when R1 is selected from —S—R, then at least one of R2, R3 and R5 is most preferably selected from halogen; and R1, R2, R3, R4 and R5 are otherwise the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and pharmacologically acceptable sal
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: February 12, 2013
    Assignee: Anamar AB
    Inventors: Torbjorn Lundstedt, Elisabeth Seifert, Per Lek, Arne Boman
  • Publication number: 20130034536
    Abstract: Provided herein are methods and compositions comprising bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists for the treatment of pancreatitis or prevention of pancreatitis.
    Type: Application
    Filed: August 3, 2012
    Publication date: February 7, 2013
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventor: Bronislava GEDULIN
  • Publication number: 20120329781
    Abstract: The instant invention relates to a combination, particularly a synergistic combination, of an alpha-2-delta ligand and a dual serotonin-noradrenaline re-uptake inhibitor (DSNRI) or one or both of a selective serotonin re-uptake inhibitor (SSRI) and a selective noradrenaline re-uptake inhibitor (SNRI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 27, 2012
    Inventors: David James Dooley, Mark John Field, Richard Griffith Williams
  • Patent number: 8278355
    Abstract: The invention provides for the use of isovaline or a pharmaceutically acceptable salt thereof for the treatment of Pain in a mammalian subject in some preferred embodiments, the invention provides for the treatment of acute and chronic Pain syndromes where other drug therapies have limited efficacy or unacceptable toxicity in said subject.
    Type: Grant
    Filed: September 12, 2007
    Date of Patent: October 2, 2012
    Assignee: Therexcell Pharma Inc.
    Inventors: Ernest Puil, Bernard Ansel MacLeod, Thomas Michael Stokes, Wei Liu
  • Publication number: 20120238563
    Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.
    Type: Application
    Filed: June 4, 2012
    Publication date: September 20, 2012
    Inventors: Jose Maria CID-NÚÑEZ, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Publication number: 20120208859
    Abstract: The invention pertains to compound of Formula (I) wherein X, Y, Z, R1, R2, R3, R4, A and A? are as described hereinabove. Formula (I) and (II) compounds can be used in pharmaceutical compositions, useful for the treatment of diseases.
    Type: Application
    Filed: October 13, 2009
    Publication date: August 16, 2012
    Applicant: ALLOSTEM THERAPEUTICS LLC
    Inventors: Uday R. Khire, Mahendra Devichand Chordia
  • Patent number: 8188141
    Abstract: The present invention provides compounds having formula (I): (I) wherein n, R1-R5, Ra-Rb, Q, Y1 and Y2 are as defined herein; and additionally provides methods for the synthesis thereof, compositions thereof, and methods for the use thereof in the treatment of various disorders including cancer, metastasis and disorders involving increased angiogenesis.
    Type: Grant
    Filed: September 23, 2005
    Date of Patent: May 29, 2012
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Mihirbaran Mandal, David C. Dorn, Malcolm A. S. Moore
  • Patent number: 8183234
    Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidinocarbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.
    Type: Grant
    Filed: June 30, 2010
    Date of Patent: May 22, 2012
    Assignee: Piramal Life Sciences Limited
    Inventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More, Anil Ghate, Jacqueline Trivedi, Sapna Parikh
  • Patent number: 8173637
    Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: May 8, 2012
    Assignee: Handa Pharmaceuticals, LLC
    Inventors: Fang-yu Liu, Zhi-qun Shen
  • Publication number: 20120035170
    Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.
    Type: Application
    Filed: August 22, 2011
    Publication date: February 9, 2012
    Inventors: José Maria Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Publication number: 20120015925
    Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.
    Type: Application
    Filed: May 16, 2011
    Publication date: January 19, 2012
    Applicant: ASAHI KASEI PHARMA CORPORATION
    Inventors: Takehiko SASAHARA, Mitsunobu MOHRI, Ken-ichi KASAHARA
  • Publication number: 20110294767
    Abstract: Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.
    Type: Application
    Filed: May 26, 2011
    Publication date: December 1, 2011
    Applicant: Satiogen Pharmaceuticals, Inc.
    Inventors: Bronislava Gedulin, Andrew A. Young, Howard E. Greene
  • Patent number: 8067459
    Abstract: The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of cancer or precancerous conditions.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: November 29, 2011
    Assignee: ArQule, Inc.
    Inventors: Mark Ashwell, Manish Tandon, Jean-Marc Lapierre, Syed Ali, Yanbin Liu, Chiang J. Li
  • Publication number: 20110281855
    Abstract: The present invention provides a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol. The present invention further provides a method of treating pain and pain related conditions by administering to a patient in need thereof, a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol.
    Type: Application
    Filed: April 21, 2011
    Publication date: November 17, 2011
    Applicant: GRUENENTHAL GMBH
    Inventor: RAMESH SESHA
  • Publication number: 20110275695
    Abstract: The invention relates to crystalline forms of zotepine hydrochloride, including the crystalline hydrochloride salt of zotepine and two cocrystals of zotepine hydrochloride with benzoic acid. The preparation and characterization of these crystalline forms of zotepine hydrochloride is described. The invention also relates to the therapeutic use of the crystalline forms of zotepine hydrochloride to treat central nervous system disorders and to pharmaceutical compositions containing them.
    Type: Application
    Filed: June 11, 2009
    Publication date: November 10, 2011
    Applicant: BIONEVIA PHARMACEUTICALS, INC.
    Inventors: Isabel Kalofonos, Dimitris Kalofonos, William Martin-Doyle, Jason Hanko, Eric J. Hagen
  • Patent number: 8030345
    Abstract: The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
    Type: Grant
    Filed: July 8, 2005
    Date of Patent: October 4, 2011
    Assignee: Cadila Healthcare Limited
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Brijesh Srivastava
  • Publication number: 20110224276
    Abstract: Optical isomers of phenylpropionic acid drugs are a mixture having R-type optical isomer and S-type optical isomer at a ratio of 10:1-1:10 by weight, wherein the ratio of 1:1 is excluded. A use of the optical isomers includes that the R-type optical isomer is used for manufacturing anti-inflammatory and analgesic drugs and the mixture having the R-type optical isomer and the S-type optical isomer at a ratio of 10:1-1:10 by weight, wherein the ratio of 1:1 is excluded, is used for manufacturing anti-inflammatory and analgesic drugs. The therapeutic indexes of anti-inflammatory and analgesic drugs of the present optical isomers are all higher than those of the S-type optical isomers and the racemate.
    Type: Application
    Filed: November 20, 2009
    Publication date: September 15, 2011
    Inventors: Tao Wang, Yan Geng, Zonggui Wang, Hongzhang Sun
  • Publication number: 20110213012
    Abstract: The present invention is directed, inter alia, to methods of treating NUT midline carcinoma (NMC) by administering compounds that promote increased histone acetylation. The invention also includes assay methods for determining the responsiveness of NMC to specific histone deacetylases and other compounds.
    Type: Application
    Filed: July 21, 2009
    Publication date: September 1, 2011
    Applicants: THE BRIGHAM AND WOMEN'S HOSPITAL, INC., DANA-FARBER CANCER INSTITUTE
    Inventors: Christopher French, Jon Aster, Matthias Hofer, James Bradner
  • Publication number: 20110207604
    Abstract: A species of Burkholderia sp with no known pathogenicity to vertebrates but with pesticidal activity (e.g., plants, insects, fungi, weeds and nematodes) is provided. Also provided are natural products derived from a culture of said species and methods of controlling pests using said natural products.
    Type: Application
    Filed: February 24, 2011
    Publication date: August 25, 2011
    Applicant: MARRONE BIO INNOVATIONS
    Inventors: Ratnakar Asolkar, Marja Koivunen, Pamela Marrone, Ana-Lucia Cordova-Kreylos, Huazhang Huang
  • Publication number: 20110206636
    Abstract: The use of sesquiterpenes and, in particular sesquiterpene lactone endoperoxides, such as artemisinin and analogs thereof, for the treatment of hepatitis C virus infections. Artemisinin, analogs of artemsisnin and some crude Artemisia extracts were tested in vitro against DNA-viruses, retro-viruses and Flavivirida, (an important family of human and animal RNA pathogens). These compounds were also screened for anti-tumor activity. Strong activity of artemisinin was noticed against the bovine viral diarrhea virus (BVDV). As pestiviruses, such as BVDV, share many similarities with hepatitis C virus (HCV), we can conclude that endoperoxides in general and artemisinin more specifically have efficacy as treatments for hepatitis C viral infections.
    Type: Application
    Filed: October 21, 2010
    Publication date: August 25, 2011
    Applicant: Kemin Foods, LLC
    Inventors: Benedikt Sas, Johan Van Hemel, Jan Vandenkerckhove, Eric Peys, Johan Neyts
  • Patent number: 7994210
    Abstract: The present invention relates to methods of treating of Down syndrome in a person using compounds of the invention.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: August 9, 2011
    Assignee: Axonyx, Inc.
    Inventor: Gosse B. Bruinsma
  • Patent number: 7973030
    Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.
    Type: Grant
    Filed: February 25, 2005
    Date of Patent: July 5, 2011
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Takehiko Sasahara, Mitsunobu Mohri, Ken-Ichi Kasahara
  • Patent number: 7964631
    Abstract: Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-?) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-? activity, in particular inflammations.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: June 21, 2011
    Assignee: Piramal Life Sciences Limited
    Inventors: Bansi Lal, Somesh Sharma, Usha Ghosh, Swati Bal-Tembe, Tulsidas More, Pravin Gagare, Sunil Jadhav, Shashikant Patil, Asha Kulkarni-Almeida, Sapna Parikh, Radha Bhaskar Panicker, Anagha Damre, Ravindra Gupte
  • Publication number: 20110144094
    Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Application
    Filed: February 16, 2011
    Publication date: June 16, 2011
    Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Patent number: 7956085
    Abstract: This invention relates to Novel 1,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: June 7, 2011
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Wendelin Frick, Heiner Glombik, Stefan Theis, Hubert Heuer, Hans-Ludwig Schaefer, Werner Kramer
  • Publication number: 20110118330
    Abstract: Compounds that inhibit proteolytic enzymes of Human Immunodeficiency Virus (HIV) are described. Preparation of the inhibitors, pharmaceutical compositions containing them, and uses of the compounds or compositions for the treatment of HIV infections are also described.
    Type: Application
    Filed: July 8, 2009
    Publication date: May 19, 2011
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventor: Arun K. Ghosh
  • Publication number: 20110092564
    Abstract: Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said composition are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC).
    Type: Application
    Filed: February 26, 2009
    Publication date: April 21, 2011
    Inventors: Ernest Puil, Bernard A. Macleod, Richard Wall
  • Patent number: 7923468
    Abstract: This invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives which are substituted with cyclohexyl groups, method for producing the same, drugs containing said compounds and use thereof.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: April 12, 2011
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Wendelin Frick, Heiner Glombik, Stefan Theis, Hubert Heuer, Hans-Ludwig Schaefer, Werner Kramer