Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 514/338)
  • 2,3-DIHYDROBENZO(1,4) DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEM DISEASES
    Publication number: 20130281486
    Abstract: Compounds of formula I wherein X, Z, R1-R4, and m are as defined in the claims, exhibit alpha2C antagonistic activity, and are thus useful as alpha2C antagonists. Methods for the treatment of diseases and conditions of the peripheric system and the central nervous system are also disclosed.
    Type: Application
    Filed: June 14, 2013
    Publication date: October 24, 2013
    Inventors: David DIN BELLE, Patrik HOLM, Arto KARLJALAINEN, Arto TOLVANEN, Gerd WOHLFAHRT, Petteri RUMMAKKO
  • THERAPEUTIC COMPOUNDS
    Publication number: 20130281434
    Abstract: Compounds of formula I?: or salts thereof are provided. Pharmaceutical compositions comprising a compound of formula I?, processes for preparing compounds of formula I?, intermediates useful for preparing compounds of formula I? and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal are also provided.
    Type: Application
    Filed: April 19, 2013
    Publication date: October 24, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Cyclic benzimidazole derivatives useful as anti-diabetic agents
    Patent number: 8563746
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: October 19, 2009
    Date of Patent: October 22, 2013
    Assignees: Merck Sharp & Dohme Corp, Metabasis Therapeutics, Inc.
    Inventors: Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion, Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka
  • Oral tablet compositions of dexlansoprazole
    Patent number: 8563035
    Abstract: Oral tablet compositions of dexlansoprazole or pharmaceutically acceptable salts or hydrated forms thereof having a gradual release and processes for the manufacture of the tablet composition and its use in the treatment of gastrointestinal disorders.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: October 22, 2013
    Inventors: Umit Cifter, Ali Turkyilmaz, Ibrahim Murat Uzer, Alper Terkinli, Levent Oner
  • Imidazolothiadiazoles for use as protein kinase inhibitors
    Patent number: 8563550
    Abstract: There is provided compounds of formula (I), wherein Z, M, R1, X, R2, R3 and B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein kinase (e.g. a PIM family kinase or PI3-K) is desired and/or required, and particularly in the treatment of cancer.
    Type: Grant
    Filed: September 29, 2008
    Date of Patent: October 22, 2013
    Inventors: Paolo Pevarello, Ana Maria Garcia Collazo, Ana Belen Garcia Garcia
  • SOLID DOSAGE FORM COMPRISING PROTON PUMP INHIBITOR AND SUSPENSION MADE THEREOF
    Publication number: 20130273168
    Abstract: A solid, rapidly gelling oral pharmaceutical dosage form, as well as an aqueous formulation prepared thereof, comprising a) an acid sensitive proton pump inhibitor as active ingredient distributed in a multitude of enteric coated pellets, and b) a suspension modifying granulate. Furthermore, the invention relates to an improved process for the manufacture and the use of such formulation in medical treatment, including prevention of gastrointestinal disorders in humans.
    Type: Application
    Filed: June 5, 2013
    Publication date: October 17, 2013
    Inventors: Eva PERSSON, Eva TROFAST
  • VIRAL POLYMERASE INHIBITORS
    Publication number: 20130274179
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.
    Type: Application
    Filed: April 11, 2013
    Publication date: October 17, 2013
    Applicant: Biota Scientific Management Pty Ltd
    Inventors: Silas Bond, Rosliana Halim, Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding
  • ORALLY DISINTEGRATING TABLET
    Publication number: 20130273157
    Abstract: A orally disintegrating tablet is obtained by tableting fine granules showing controlled release of lansoprazole and an additive, which is capable of suppressing breakage of the fine granules during tableting, and can control the release of lansoprazole for a long time, and can maintain a therapeutically effective concentration for a prolonged time, and shows superior disintegration property in the oral cavity.
    Type: Application
    Filed: December 26, 2011
    Publication date: October 17, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shiro Ishii, Yutaka Ebisawa, Takayuki Okabe
  • HETEROCYCLIC PYRAZOLE COMPOUNDS, METHOD FOR PREPARING THE SAME AND USE THEREOF
    Publication number: 20130274255
    Abstract: The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.
    Type: Application
    Filed: April 12, 2012
    Publication date: October 17, 2013
    Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGY
    Inventors: Chu-Bin LIAO, Chao-Cheng CHIANG, Huei-Ru YANG, Yuan-Chun LIAO, Paonien CHEN
  • ORAL FORMULATION FOR DEXLANSOPRAZOLE
    Publication number: 20130273171
    Abstract: A stable formulation of dexlansoprazole for treating a digestive disorder, and methods of manufacturing the same.
    Type: Application
    Filed: November 18, 2010
    Publication date: October 17, 2013
    Applicant: HANDA PHARMACEUTICALS, LLC
    Inventors: Zhiqun Shen, Yu Zhang, Enjun Fu, MIn Michael He, Fang-yu Liu
  • NOVEL INHIBITORS OF BACTERIAL BIOFILMS AND RELATED METHODS
    Publication number: 20130274256
    Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.
    Type: Application
    Filed: October 11, 2012
    Publication date: October 17, 2013
    Applicant: SEQUOIA SCIENCES, INC.
    Inventor: Sequoia Sciences, Inc.
  • GENETIC POLYMORPHISMS ASSOCIATED WITH VENOUS THROMBOSIS, METHODS OF DETECTION AND USES THEREOF
    Publication number: 20130274195
    Abstract: The present invention is based on the discovery of genetic polymorphisms that are associated with venous thrombosis. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.
    Type: Application
    Filed: December 24, 2012
    Publication date: October 17, 2013
    Inventors: CELERA CORPORATION, LEIDEN UNIVERSITY MEDICAL CENTER (LUMC) Acting on Behalf of ACADEMIC HOSPITAL LEIDEN
  • VIRAL POLYMERASE INHIBITORS
    Publication number: 20130274218
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.
    Type: Application
    Filed: April 11, 2013
    Publication date: October 17, 2013
    Applicant: Biota Scientific Management Pty Ltd
    Inventors: Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding, Silas Bond, Rosliana Halim
  • 4,5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections
    Patent number: 8557848
    Abstract: The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: October 15, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin X. Chen, Srikanth Venkatraman, F. George Njoroge, Stuart B. Rosenblum, Charles A. Lesburg, Jose S. Duca, Neng-Yang Shih, Francisco Velazquez, Gopinadhan N. Anilkumar, Qingbei Zeng, Joseph A. Kozlowski
  • Solid dispersions containing kinase inhibitors
    Patent number: 8557995
    Abstract: A solid dispersion comprises, in essentially non-crystalline form, a kinase inhibitory compound, e.g., N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a cancer.
    Type: Grant
    Filed: June 7, 2011
    Date of Patent: October 15, 2013
    Assignee: AbbVie Inc.
    Inventors: Jonathan M. Miller, Rajeev Gokhale, Eric A. Schmitt, Yi Gao, Justin Lafountaine, Lloyd Dias
  • ACTIVE ENANTIOMER OF DODECYL 2-(N,N-DIMETHYLAMINO)-PROPIONATE
    Publication number: 20130267562
    Abstract: 2R-dodecyl 2-(N,N dimethylamino)-propionate (R-DDAIP) provides an unexpectedly improved activity in facilitating transport of a pharmaceutically active compound across biological membranes and tissues, compared to S-DDAIP of the same enantiomeric purity, or racemic DDAIP. Purified S-DDAIP is also provided.
    Type: Application
    Filed: November 30, 2011
    Publication date: October 10, 2013
    Applicant: NEXMED HOLDINGS, INC
    Inventors: Bassam B. Damaj, Richard Martin
  • Treatment of Addiction and Impulse-Control Disorders Using PDE7 Inhibitors
    Publication number: 20130267502
    Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 10, 2013
    Inventors: Gregory A. Demopulos, George A. Gaitanaris, Roberto Ciccocioppo
  • INDOLE, INDAZOLE AND BENZIMIDAZOLE ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS
    Publication number: 20130267529
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, Z, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Application
    Filed: June 6, 2013
    Publication date: October 10, 2013
    Inventors: Michael Patrick Dillon, Nancy Elizabeth Krauss
  • Method of producing a PPI-containing pharmaceutical preparation
    Publication number: 20130266658
    Abstract: The present invention relates to a method of producing a pharmaceutical preparation that contains a proton pump inhibitor and optionally a non-steroidal anti-inflammatory drug in the form of pellets. The invention further relates to pharmaceutical preparations obtainable by said method, in particular those with a defined dissolution profile.
    Type: Application
    Filed: May 29, 2013
    Publication date: October 10, 2013
    Inventors: Gerd Weiß, Thomas Profitlich, Karl Schwitzer, Cornelia Wagner, Manfred Schwitzer, Bernhard Huber
  • HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS
    Publication number: 20130267510
    Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: December 6, 2011
    Publication date: October 10, 2013
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large
  • Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid and administration thereof
    Patent number: 8552034
    Abstract: A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.
    Type: Grant
    Filed: April 7, 2011
    Date of Patent: October 8, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Marinus Jacobus Verwijs, Rossitza Gueorguieva Alargova, Ritu Rohit Kaushik, Irina Nikolaevna Kadiyala, Christopher Young
  • Substituted 4-(indazolyl)-1,4-dihydropyridines and methods of use thereof
    Patent number: 8551989
    Abstract: This invention relates to novel 4-(indazolyl)-1,4-dihydropyridine of the following formula (I) derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: October 8, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Karen Engel
  • Benzimidazole derivatives: preparation and pharmaceutical applications
    Patent number: 8551988
    Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: October 8, 2013
    Assignee: Mei Pharma, Inc.
    Inventors: DiZhong Chen, Hong Yan Song, Eric T. Sun, Niefang Yu, Yong Zou
  • CHEMOKINE RECEPTOR ANTAGONISTS
    Publication number: 20130261129
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Application
    Filed: March 29, 2013
    Publication date: October 3, 2013
    Applicant: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Wei, Lijuan Jane Wang
  • INDAZOLE DERIVATIVES USEFUL AS ERK INHIBITORS
    Publication number: 20130261125
    Abstract: The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Inventors: Gerald W. Shipps, JR., Xiaohua Huang, Yongqi Deng, Liang Zhu, Alan B. Cooper, Binyuan Sun, Abdelghani Achab, Sie-Mun Lo
  • Substituted bicyclic imidazole derivatives as gamma secretase modulators
    Patent number: 8546440
    Abstract: The present invention is concerned with novel substituted bicyclic imidazole derivatives of Formula (I) wherein R0, R1, R3, R4, X, A1, A2, A3, A4, Y1, Y2 and Y3 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said novel compound as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: October 1, 2013
    Assignee: Janssen Pharmaceuticals, Inc.
    Inventors: Henricus Jacobus Maria Gijsen, Gregor James MacDonald, François Paul Bischoff, Gary John Tresadern, Andrés Avelino Trabanco-Suárez, Sven Franciscus Anna Van Brandt, Didier Jean-Claude Berthelot
  • Compounds that modulate intracellular calcium
    Patent number: 8546403
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: April 12, 2011
    Date of Patent: October 1, 2013
    Assignee: Calcimedica, Inc.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Viral polymerase inhibitors
    Patent number: 8546389
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: October 1, 2013
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
  • Antibacterial Compounds
    Publication number: 20130252938
    Abstract: The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Application
    Filed: March 21, 2013
    Publication date: September 26, 2013
    Applicant: Biota Europe Ltd.
    Inventors: Christopher James Lunniss, James T. Palmer, Gary Robert William Pitt, David Davies, Lorraine Claire Axford
  • Modulators of Aldhehyde Dehydrogenase Activity and Methods of Use Thereof
    Publication number: 20130253010
    Abstract: The present invention provides compounds that function as modulators of aldehyde dehydrogenase activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Application
    Filed: December 17, 2012
    Publication date: September 26, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Che-Hong Chen, Daria Mochly-Rosen, Wenjin Yang
  • METHOD FOR MANUFACTURING MEDICINAL COMPOUNDS CONTAINING DABIGATRAN
    Publication number: 20130251811
    Abstract: The invention relates to an improved process for preparing a new medicament formulation of the active substance dabigatran etexilate of formula I in the form of the methanesulphonic acid salt thereof, and this new medicament formulation as such.
    Type: Application
    Filed: May 21, 2013
    Publication date: September 26, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Guido Bernhard Edmund RADTKE
  • SUBSTITUTED PHENOXYPYRIDINES
    Publication number: 20130252922
    Abstract: The present invention relates to substituted phenoxypyridine compounds of general formula (I) in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: October 27, 2011
    Publication date: September 26, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventor: Marion Hitchcock
  • METHOD FOR SCREENING COMPOUNDS FOR TREATING SEPSIS TARGETING NOD2 SIGNALLING PATHWAY AND COMPOSITION FOR TREATING SEPSIS COMPRISING NOD2 SIGNALLING PATHWAY INHIBITORS
    Publication number: 20130251702
    Abstract: Methods for screening compounds for treating sepsis are disclosed. The present methods and compositions are targeting NOD2 mediated signaling pathway and the agents identified by the present methods are qualified as drug candidates for clinical development. Further Methods and composition for treating sepsis are disclosed.
    Type: Application
    Filed: March 21, 2013
    Publication date: September 26, 2013
    Applicant: SNU R&DB FOUNDATION
    Inventors: Doo Hyun CHUNG, Sae Jin OH, Ji Hyung KIM
  • COMPOSITION COMPRISING A BENZIMIDAZOLE AND PROCESS FOR ITS MANUFACTURE
    Publication number: 20130251791
    Abstract: The invention provides new benzimidazole compositions, comprising: (a) a core containing said benzimidazole active ingredient; (b) an intermediate layer; and (c) an enteric layer; said core being substantially free of binder. The invention also provides a process for manufacturing the composition of the invention.
    Type: Application
    Filed: May 16, 2013
    Publication date: September 26, 2013
    Inventors: Pawan Seth, Benoit Schmitt
  • NOVEL FUSED PYRAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
    Publication number: 20130252944
    Abstract: The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Application
    Filed: July 11, 2011
    Publication date: September 26, 2013
    Inventors: Christelle Bolea, Sylvain Celanire, Lam Tang, Philip Jones, Nigel J. Liverton, Richard Soll, Jingchao Dong, Zhiyu Lei, Fuqing Liu, Yanling Kong, Yi Ju, Haoyong Zhang, Jieping Wei, Qiaoxin Wei, Minxiang Zhang, Yunfu Luo
  • PROCESS FOR PREPARING ORALLY ADMINISTERED DABIGATRAN FORMULATIONS
    Publication number: 20130251810
    Abstract: The invention relates to an improved process for preparing a new medicament formulation of the active substance dabigatran etexilate of formula I in the form of the methanesulphonic acid salt thereof, and this new medicament formulation as such.
    Type: Application
    Filed: May 20, 2013
    Publication date: September 26, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Sabine LANDERER, Thomas FRIEDL
  • Inhibitors of the human aldosterone synthase CYP11B2
    Patent number: 8541404
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: September 24, 2013
    Assignee: ElexoPharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Modulators of ATP-binding cassette transporters
    Patent number: 8541453
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: September 24, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
  • Ketolide compounds having antimicrobial activity
    Patent number: 8541420
    Abstract: The invention relates to ketolide compound of Formula-I and the pharmaceutically acceptable salts thereof having antimicrobial activity. The invention also provides pharmaceutical compositions containing the compounds of invention and methods of treating or preventing microbial infections with the compound of invention.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: September 24, 2013
    Assignee: Wockhardt Ltd.
    Inventors: Bharat Kalidas Trivedi, Mahesh Vithalbhai Patel
  • COMPOUNDS FOR ENHANCING ARGINASE ACTIVITY AND METHODS OF USING SAME
    Publication number: 20130245070
    Abstract: The present invention relates to a method for enhancing arginase activity in a damaged or injured cell. In other aspects, the invention provides a method for treating a disorder that can be treated by enhancing arginase activity in a human in need thereof, the method comprising administering to the human an effective amount of a compound that enhances arginase activity. Such disorders include ischemia, hypoxia, neurodegenerative disease or condition, stroke or trauma of the nervous system. In yet another aspect, the invention provides methods for promoting regeneration of a neural cell in a human in need thereof.
    Type: Application
    Filed: March 9, 2012
    Publication date: September 19, 2013
    Applicant: THE RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK
    Inventors: Rajiv R. Ratan, Marie T. Filbin
  • Modulators of ATP-Binding Cassette Transporters
    Publication number: 20130245011
    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 (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: May 6, 2013
    Publication date: September 19, 2013
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • MULTIPLE PPI DOSAGE FORM
    Publication number: 20130245071
    Abstract: Herein provided are dosage forms (variously referred to as “formulations”) comprising a PPI that is released from the dosage form as a first and a second dose. Each dose of PPI is present in an amount sufficient to raise the plasma levels of the PPI to at least 100 ng/ml.
    Type: Application
    Filed: April 30, 2013
    Publication date: September 19, 2013
    Inventors: Rajneesh Taneja, Majid Vakilynejad
  • ORALLY DISINTEGRATING TABLET
    Publication number: 20130243859
    Abstract: The present invention relates to a multi-layer orally disintegrating tablet having (1) an enteric fine granule-containing layer containing a proton pump inhibitor and (2) an acetylsalicylic acid-containing layer, which shows high stability of the active ingredients (proton pump inhibitor, aspirin) and expresses the pharmacological effects of the active ingredients stably and rapidly after administration.
    Type: Application
    Filed: December 2, 2011
    Publication date: September 19, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Yasushi Mima, Tetsuya Kawano, Yumiko Ishii
  • INDAZOLE, BENZISOXAZOLE, AND BENZISOTHIAZOLE KINASE INHIBITORS
    Publication number: 20130245015
    Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Application
    Filed: May 3, 2013
    Publication date: September 19, 2013
    Inventors: YUJIA DAI, STEVEN K. DAVIDSEN, ANNA M. ERICSSON, KRESNA HARTANDI, ZHIQIN JI, MICHAEL R. MICHAELIDES
  • INSECTICIDAL COMPOUNDS
    Publication number: 20130245072
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, A5, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 19, 2013
    Applicant: SYNGENTA CORP PROTECTION LLC
    Inventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
  • CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    Publication number: 20130245003
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a? and I-A.a? in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: March 25, 2013
    Publication date: September 19, 2013
    Applicant: Abbott GmbH & Co. KG
    Inventors: Andreas Kling, Wilfried Hornberger, Helmut Mack, Achim Moeller, Volker Nimmrich, Dietmar Seemann, Wilfried Lubisch
  • MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
    Publication number: 20130245010
    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 (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 19, 2013
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
    Publication number: 20130245063
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 19, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. Whitten, Jonathan Grey, Jianguo Cao, Zhijun Wang, Evan Rogers
  • NITROBENZOTHIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATIONS THEREOF
    Publication number: 20130245008
    Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.
    Type: Application
    Filed: November 18, 2011
    Publication date: September 19, 2013
    Applicant: SANOFI
    Inventor: Alain Pellet
  • Compounds
    Patent number: 8536169
    Abstract: The invention is directed to certain novel compounds directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: September 17, 2013
    Assignee: Glaxo Group Limited
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Joelle Le, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst