The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
  • Patent number: 10800753
    Abstract: Tetrahydrothiophene and related heterocyclic analogs and related methods for GABA aminotransferase inactivation.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: October 13, 2020
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Hoang V. Le, Dustin D. Hawker
  • Patent number: 10588892
    Abstract: The present invention relates to a pharmaceutical composition comprising a physical mixture of sacubitril sodium and valsartan disodium, wherein the X-ray powder diffraction pattern of valsartan disodium comprises characteristic peaks at the following 2 theta (±0.2) angles: 4.70°, 9.29°, 22.34°, measured using a Cu K? radiation. The invention further relates to the use of said pharmaceutical composition as medicament in the treatment of heart failure.
    Type: Grant
    Filed: July 26, 2018
    Date of Patent: March 17, 2020
    Assignee: SYNTHON B.V.
    Inventors: Bohumil Dymacek, Marta Vivancos Martinez, Luis Nogueiras Nieto, Lisardo Alvarez Fernandez, Rohit Kumar, Jose Velada Calzada, Petr Mitas
  • Patent number: 10562866
    Abstract: The amorphous form of trisodium sacubitril valsartan and methods for the preparation thereof are disclosed herein.
    Type: Grant
    Filed: February 6, 2016
    Date of Patent: February 18, 2020
    Assignee: Mylan Laboratories Limited
    Inventors: Vellanki Sivaram Prasad, Arabinda Sahu, Siva Koteswara Rao Prathi, Lakshmana Rao Ampolu, Ramakoteswara Rao Jetti, Aggi Ramireddy Bommareddy, Neelima Bhagavatula, Nitin Ashok Shimpi
  • Patent number: 10508087
    Abstract: Novel crystalline forms of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl) propionate-(S)-3?-methyl-2?-(pentanoyl{2?-(tetrazol-5-ylate)biphenyl-4?-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.
    Type: Grant
    Filed: March 18, 2018
    Date of Patent: December 17, 2019
    Assignees: CRYSTAL PHARMATECH CO., LTD., SUZHOU PENGXU PHARMATECH CO., LTD.
    Inventors: Minhua Chen, Yanfeng Zhang, Chaohui Yang, Xiaoyu Zhang
  • Patent number: 10179143
    Abstract: Methods of using azide-modified biomolecules, such as fatty acids, carbohydrates and lipids, to treat a plant, an insect or an animal infected with a virus or to inhibit infectivity of a virus, such as the human immunodeficiency virus, are provided. Also provided are methods of labeling a virus, such as human immunodeficiency virus, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. Also, provided are methods of tracking a virus in vivo, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. The azide-modified biomolecules may be combined with a pharmaceutically acceptable excipient to produce a pharmaceutical composition, optionally containing another anti-viral agent and/or a delivery agent, such as a liposome.
    Type: Grant
    Filed: August 8, 2017
    Date of Patent: January 15, 2019
    Assignee: Life Technologies Corporation
    Inventors: Brian Agnew, Upinder Singh, Scott Grecian
  • Patent number: 10092537
    Abstract: Provided is a novel use of a plasminogen activator inhibitor-1 inhibitor (PAI-1 inhibitor) that is used as an active ingredient of an agent for controlling a tumor stem cell, an agent for enhancing the antitumor effect of an antitumor agent, an agent for tumor chemotherapy, a stem-cell protecting drug, or a hematopoietic disorder improving agent.
    Type: Grant
    Filed: April 15, 2014
    Date of Patent: October 9, 2018
    Assignee: RENASCIENCE CO., LTD.
    Inventors: Kiyoshi Ando, Takashi Yahata, Toshio Miyata
  • Patent number: 10039845
    Abstract: The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.
    Type: Grant
    Filed: June 30, 2017
    Date of Patent: August 7, 2018
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Martin G. Pomper, Sangeeta Ray, Ronnie C. Mease, Catherine Anne Foss
  • Patent number: 9914722
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: March 13, 2018
    Assignee: PTC Therapeutics, Inc.
    Inventors: Tianle Yang, Gary Mitchell Karp, Hongyan Qi
  • Patent number: 9694091
    Abstract: The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+PC3 PIP tumors.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: July 4, 2017
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Martin G. Pomper, Sangeeta Ray, Ronnie C. Mease, Catherine Anne Foss
  • Patent number: 9144575
    Abstract: Methods of using azide-modified biomolecules, such as fatty acids, carbohydrates and lipids, to treat a plant, an insect or an animal infected with a virus or to inhibit infectivity of a virus, such as the human immunodeficiency virus, are provided. Also provided are methods of labeling a virus, such as human immunodeficiency virus, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. Also, provided are methods of tracking a virus in vivo, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. The azide-modified biomolecules may be combined with a pharmaceutically acceptable excipient to produce a pharmaceutical composition, optionally containing another anti-viral agent and/or a delivery agent, such as a liposome.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: September 29, 2015
    Assignees: LIFE TECHNOLOGIES CORPORATION, THE JOHNS HOPKINS UNIVERSITY
    Inventors: Brian Agnew, David Graham, Upinder Singh, Scott Grecian
  • Publication number: 20150141464
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5 -mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Application
    Filed: November 20, 2012
    Publication date: May 21, 2015
    Inventors: Amy S. RIPKA, Jeffrey O. SAUNDERS
  • Publication number: 20150126568
    Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing hypertension and diabetic kidney disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of diabetes related renal complications, hypertension, albuminuria, Heart Diseases, ESRD, Kidney GFR complications, Vascular Disease, Ventricular Septal Defect, vascular dilation, high blood pressure, congestive heart failure (CHF), post-myocardial infarction (MI).
    Type: Application
    Filed: August 18, 2013
    Publication date: May 7, 2015
    Inventor: Mahesh Kandula
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Publication number: 20150099730
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 9, 2015
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Peter J. Connolly
  • Publication number: 20150094304
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
  • Publication number: 20150087829
    Abstract: The present invention relates to compounds of formula I wherein RS denotes F or CF3, Ra denotes H or C1-4-alkyl and Z denotes a leaving group or an optionally substituted or protected hydroxyl group, suitable as intermediates in the synthesis of indanyloxydihydrobenzofuranylacetic acids, which are GPR40 agonists, to a process for preparing these intermediates and to the process for preparing the GPR40 agonists making use of an asymmetric catalytic hydrogenation reaction in the presence of a transition metal catalyst and a chiral auxiliary.
    Type: Application
    Filed: September 24, 2014
    Publication date: March 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Georg DAHMANN, Holger WAGNER, Matthias ECKHARDT, Markus FRANK, Marco SANTAGOSTINO, Juergen SCHNAUBELT, Uwe STERTZ, Thorsten PACHUR
  • Publication number: 20150087617
    Abstract: The invention provides indole and indoline derivatives and slats thereof, compositions comprising them and uses thereof for the treatment of diseases and disorders.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 26, 2015
    Inventors: Abraham Nudelman, Marta Weinstock-Rosin
  • Publication number: 20150080412
    Abstract: The invention disclosed herein is directed to compounds of Formula (I) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula (I), or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a of a therapeutically effective amount of a selective PPAR? antagonist.
    Type: Application
    Filed: March 7, 2013
    Publication date: March 19, 2015
    Applicant: INCEPTION 2, INC.
    Inventors: Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Jill Melissa Baccei, Brian Andrew Stearns, Ryan Christopher Clark, Yen Pham Truong
  • Patent number: 8981110
    Abstract: The present invention provides novel process for preparation of olmesartan medoxomil (I) substantially free of olmesartan acid impurity (II) comprising, reacting trityl olmesartan medoxomil (III) with acid, filtering the precipitate of trityl alcohol, subjecting the filtrate to agitated thin film drying and recovering olmesartan medoxomil (I).
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: March 17, 2015
    Assignee: Lupin Limited
    Inventors: Rajendra Vishwanath Firke, Ujjwal Komalsing Sisodiya, Chandrakant Shriram Bhangale, Radhakrishna Bhikaji Shivdavkar, Himanshu Madhav Godbole, Girij Pal Singh
  • Patent number: 8981109
    Abstract: The present invention relates to a process for the preparation of pure Valsartan (I) substantially free from impurities of formulae (Ia), (Ib), and (Ic), which comprises: (i) condensing 2-(4?-bromomethylphenyl)benzonitrile of formula (II) with L-valine methyl ester hydrochloride of formula (V) in the presence of a base in a solvent to produce N-[(2?-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester of formula (VI); (ii) treating the compound VI of step (i) with acid followed by treating with base to produce pure compound VI substantially free from dimeric impurity of formula (Via); (iii) reacting the pure compound of formula (VI) with n-valeryl chloride in the presence of a base to produce pure N-valeryl-N-[(2?-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester (VII) substantially free from alkene impurity of formula (Vila); (iv) reacting the compound of formula (VII) with trialkyltin chloride and a metal azide in a solvent at a reflux temperature to produce N-(1-oxopentyl)-N-[[2?-(2-tributyltintetrazol-5-yl
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: March 17, 2015
    Assignee: Aurobindo Pharma Ltd
    Inventors: Raveendra Reddy Chinta, Gangadhara Bhima Shankar Nangi, Mahendar Reddy Nayini, Somappa Somannavar Yallapa, Shankar Reddy Budidet, Islam Aminul, Sivakumaran Meenakshisunderam
  • Publication number: 20150065516
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: October 29, 2014
    Publication date: March 5, 2015
    Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Halyan Wang
  • Publication number: 20150065506
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: August 13, 2014
    Publication date: March 5, 2015
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Patent number: 8969394
    Abstract: The invention is directed to thiophenecarboxamide derivatives of formulae I and II as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included. (Formulas I and II).
    Type: Grant
    Filed: August 10, 2007
    Date of Patent: March 3, 2015
    Assignee: Merck Frosst Canada Ltd.
    Inventors: Marc Blouin, Jason Burch, Yongxin Han, Christophe Mellon
  • Patent number: 8969341
    Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: March 3, 2015
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20150057238
    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 26, 2015
    Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Leonard Mitchell, Peter Johnson, Naomi Went
  • Patent number: 8933102
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I).
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: January 13, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Lehua Chang, Scott D. Edmondson
  • Patent number: 8933241
    Abstract: A method for producing high-purity olmesartan medoxomil is provided in which a solvent containing water is used in steps of tritylation and DMDO esterification of olmesartan.
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: January 13, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventor: Shigeo Yanagihara
  • Publication number: 20150011754
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: September 17, 2014
    Publication date: January 8, 2015
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
  • Publication number: 20150011553
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: July 3, 2014
    Publication date: January 8, 2015
    Inventors: Ulrich GÖRGENS, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • Patent number: 8927709
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: January 6, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20150005345
    Abstract: The present invention features benzhydrol-pyrazole derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cancers, inflammatory disorders, or autoimmune disorders.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 1, 2015
    Inventors: Anthony D. Keefe, Richard W. Wagner, Matthew Clark, Ying Zhang, Diana Gikunju, John Cuozzo, Heather Thomson
  • Publication number: 20140378516
    Abstract: Embodiments of the present disclosure, in one aspect, relate to a beta-lactamase inhibitor, pharmaceutical compositions including a beta-lactamase inhibitor, methods of treatment of a condition (e.g., infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Inventors: Yu Chen, Derek Nichols, Adam R. Renslo, Priyadarshini Jaishankar, Erica M.W. Lauterwasser
  • Publication number: 20140378457
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson, Bruce E. Tomczuk
  • Publication number: 20140378430
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Alan Naylor
  • Patent number: 8916710
    Abstract: The present invention relates to a process for preparing tetrazole-substituted anthranilic acid diamide derivatives of the formula (I) in which R1, R2, R3, R4, Q and Z have the meanings given in the description, by reacting pyrazole acids with anthranilic esters.
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: December 23, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Sergii Pazenok, Frank Volz, Norbert Lui, Arnd Neeff, Sylvia Szywalski
  • Publication number: 20140371067
    Abstract: The present invention relates to a method of controlling weeds at a locus, said method comprising application to the locus of a weed controlling amount of a herbicidal composition comprising a compound of Formula (I), or an agronomically acceptable salt of said compounds wherein X, R1, R2, R4 and R5 are as defined herein. The invention further relates novel herbicidal compounds, to herbicidal compositions comprising said compounds and to their use for controlling weeds, in particular in crops of useful plants.
    Type: Application
    Filed: December 20, 2012
    Publication date: December 18, 2014
    Applicant: SYNGENTA LIMITED
    Inventors: Glynn Mitchell, Alison Clare Elliott
  • Publication number: 20140371240
    Abstract: The invention relates to compounds of the general formulae (I) and (II) in which the radicals A1, A2, A3, A4, M1, M2, M3, Q, R1, T, W1 and W2 have the meaning given in the description and to the use of the compounds for controlling animal pests. The invention furthermore relates to processes and intermediates for preparing the compounds of formula (I).
    Type: Application
    Filed: December 17, 2012
    Publication date: December 18, 2014
    Inventors: Michael Maue, Tobias Kapferer, Friedrich August Muehlthau, Olga Malsam
  • Publication number: 20140357801
    Abstract: A nitrile rubber coupled via bisdihydropyrazole groups is produced by reacting a nitrile rubber which is based on conjugated dienes, ?,?-unsaturated nitriles and optionally further copolymerizable monomers as monomers, may have been hydrogenated and has covalently bonded tetrazole groups with a bifunctional ene compound in which the ene groups can each be reacted with the tetrazole groups to give dihydropyrazole groups.
    Type: Application
    Filed: May 21, 2014
    Publication date: December 4, 2014
    Applicant: LANXESS Deutschland GmbH
    Inventors: Sven BRANDAU, Andreas KAISER, Uwe WESTEPPE, Christopher BARNER-KOWOLLIK, Christoph DUERR, Paul LEDERHOSE
  • Publication number: 20140350010
    Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Application
    Filed: November 28, 2012
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20140343017
    Abstract: Provided is a highly safe and effective compound represented by the following general formula (1) or a salt thereof which acts on tubulin and has an anticancer effect, wherein Ar represents an aryl group or a heteroaryl group; Z1, Z2, Z3, and Z4 each independently represent CH, a nitrogen atom, an oxygen atom, or a sulfur atom; R1 represents a hydrogen atom, a halogen atom, an alkyl group, or the like; R2 and R3 are the same or different and each represent a hydrogen atom, a halogen atom, a carboxyl group, or the like; n units of R4 are the same or different and each represent a hydrogen atom, an alkyl group, or the like; and n represents a number of 0 to 4.
    Type: Application
    Filed: January 24, 2013
    Publication date: November 20, 2014
    Applicant: Kabushiki Kaisha Yakult Honsha
    Inventors: Takashi Ikeda, Masahiro Ono, Satoshi Ueno, Ryuta Yamazaki, Takashi Yaegashi, Takeshi Matsuzaki
  • Publication number: 20140342906
    Abstract: Tetrazol-5-yl- and triazol-5-yl-aryl compounds of the general formula (I) as herbicides are described. In this formula (I), X, Z, W and R are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A and B are N and CY. Q is cyanoalkylcarbonyl or isoxazolyl.
    Type: Application
    Filed: January 10, 2013
    Publication date: November 20, 2014
    Inventors: Ralf Braun, Lothar Willms, Ines Heinemann, Isolde Haeuser-Hahn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger
  • Publication number: 20140329676
    Abstract: The present invention relates to the use of anthranilic acid diamide derivatives with heteroaromatic and heterocyclic substituents of formula (I) wherein R1, R2, R3, R4, R5, R6, n, A, Q have the meanings as given in the description—for controlling animal pests, such as insects and/or unwanted acarids and/or nematodes in transgenic crops and to methods particularly useful for controlling insects, and/or acarids and/or nematodes and/or increasing crop yield in those crops.
    Type: Application
    Filed: December 17, 2012
    Publication date: November 6, 2014
    Inventors: Rüdiger Fischer, Heike Hungenberg, Bill Striegel, Steven Riniker
  • Patent number: 8877938
    Abstract: A compound of an angiotensin receptor antagonist (ARB), a neutral endopeptidase inhibitor (NEPi) and one or more monovalent cations are useful for the treatment of hypertension and/or heart failure. ARB includes S—N-valeryl-N-{[2?-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine in the anion form, NEPi includes (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester in the anion form and cation includes monovalent cations such as Na+. The compound includes trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3?-methyl-2?-(pentanoyl{2?-(tetrazol-5-ylate)biphenyl-4?-ylmethyl}amino)butyrate] hemipentahydrate.
    Type: Grant
    Filed: November 8, 2006
    Date of Patent: November 4, 2014
    Assignee: Novartis Pharmaceuticals Corporation
    Inventors: Lili Feng, Sven Erik Godtfredsen, Bin Hu, Yugang Liu, Piotr Karpinski, Paul Allen Sutton, Mahavir Prashad, Michael J. Girgis, Thomas J. Blacklock
  • Patent number: 8871792
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: October 28, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20140316142
    Abstract: The present invention relates to an improved process for the preparation of angiotensin receptor antagonists and intermediates thereof. Particularly the present invention relates to an improved process for the preparation of N-(1-oxopentyl)-N-[[2?-(1H-tetrazol-5-yl)[1,1?-biphenyl]-4-yl]methyl]-L-valine of Formula 1 via a phosphite salt of Formula-4.H3PO3 preferably a phosphite salt of Formula-4?.
    Type: Application
    Filed: September 18, 2012
    Publication date: October 23, 2014
    Applicant: ALKEM LABORATORIES LTD.
    Inventors: Mahendranath Narasimha Rao Rao, Lokesh Ravilla, Shridhara Kanakamajalu, Sundarraja Kothapalli Rao, Kuppuswamy Nagarajan
  • Patent number: 8865755
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: October 21, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Robert Murray McKinnell, Brooke Blair
  • Patent number: 8859600
    Abstract: Acetone solvate crystals of trityl olmesartan medoxomil are provided.
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: October 14, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Hiroshi Kiyota, Hideaki Ishikawa
  • Publication number: 20140288090
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Application
    Filed: November 20, 2012
    Publication date: September 25, 2014
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Amy S. Ripka, Jeffrey O. Saunders
  • Publication number: 20140288042
    Abstract: This invention relates to compounds of Formula I having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R represents a fused bicyclic or spirocyclic aliphatic diamine and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 25, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim
  • Publication number: 20140275152
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Brian W. Metcalf, Zhe Li