Abstract: Anhydrous polymorphic form-I of anti cancer drug, Lenalidomide whose chemical name is 3-(4-amino-1-oxo-1, 3-dihydro-isoindole-2-yl)-piperidine-2,6-dione, is disclosed. Alternate methods for making anhydrous polymorphic form-I of Lenalidomide are also disclosed.
Abstract: Disclosed herein is {[5-(3-fluorophenyl)-3-hydroxypyridine-2-carbonyl]-amino}acetic acid and the ester and amide prodrugs thereof, that can stabilize hypoxia inducible factor-2 alpha (HIF-2?) and thereby provide a method for treating cancer. Further disclosed are compositions which comprise {[5-(3-fluorophenyl)-3-hydroxypyridine-2-carbonyl]-amino}acetic acid and/or a prodrug thereof which can be used to treat cancer.
Abstract: An effluent produced in oxidation of a cellulosic material with an oxidizing agent in the presence of an N-oxyl compound and a bromide and/or iodide is deionized by electrodialysis to an inorganic salt concentration of less than 0.4%, whereby the N-oxyl compound in the effluent is concentrated and recovered. The N-oxyl compound thus recovered can be reused in oxidation of a cellulosic material. Preferably, the effluent is subjected to reduction treatment and ion exchange resin treatment prior to the electrodialysis.
Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
Type:
Grant
Filed:
November 28, 2011
Date of Patent:
October 21, 2014
Assignee:
Mapi Pharma Ltd.
Inventors:
Ehud Marom, Michael Mizhiritskii, Shai Rubnov
Abstract: The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
Type:
Grant
Filed:
October 5, 2010
Date of Patent:
October 14, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Stephane L. Bogen, Yao Ma, Yaolin Wang, Brian Robert Lahue, Latha G. Nair, Manami Shizuka, Matthew Ernst Voss, Margarita Kirova-Snover, Weidong Pan, Yuan Tian, Bheemashankar A. Kulkarni, Craig R. Gibeau, Yuan Liu, Giovanna Scapin, Diane Rindgen, Ronald J. Doll, Timothy J. Guzi, Danny J. Hicklin, Amin Nomeir, Gerald W. Shipps, Jr., Malcolm MacCoss
Abstract: Disclosed are a polymorphs I-VI of N-(6-(4-chlorophenoxy)hexyl)-N?-cyano-N?-(4-pyridyl)guanidine or of a solvate thereof, a preparation method thereof, and a use thereof as a biological active ingredient. The polymorphs are useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation.
Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Type:
Grant
Filed:
July 18, 2011
Date of Patent:
September 30, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Eugene Richard Hickey, Doris Riether, Monika Ermann
Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3, R3a have meanings given in the description.
Type:
Grant
Filed:
December 7, 2012
Date of Patent:
September 30, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer
Abstract: The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(?O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.
Type:
Grant
Filed:
November 23, 2011
Date of Patent:
September 30, 2014
Assignee:
Pierre Fabre Medicament
Inventors:
Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Christophe Pignier
Abstract: The present invention describes a process for preparing a cyclooxygenase-2 selective inhibitor. It provides a synthetic procedure for the said substance namely 5-chloro-3-(4-methylsulphonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine of formula (I). The invention also relates to preparation of a new intermediate of formula (IV) and a process to prepare it. Furthermore, the invention describes a process for preparing another key intermediate of formula (II). Compounds of formula (IV) and formula (II) are useful intermediates in synthesis of the said cyclooxygenase-2 inhibitor.
Abstract: The present invention refers to compounds of formula (I): as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or chemoprevention of cancer, aging related diseases or processes, diabetes and neurodegenerative diseases.
Type:
Grant
Filed:
May 10, 2011
Date of Patent:
September 16, 2014
Assignees:
Ikerchem, S.L., Universidad del Pais Vasco
Inventors:
Fernando Pedro Cossio Mora, Leire Lidia Arias Echeverría, Yosu Ion Vara Zalazar, Eneko Aldaba Arévalo, Eider San Sebastián Larzabal, Aizpea Zubia Olascoaga
Abstract: The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
Type:
Grant
Filed:
May 13, 2013
Date of Patent:
September 9, 2014
Assignee:
Novartis AG
Inventors:
Stephanie Kay Dodd, Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
Abstract: The invention relates to a process for obtaining compounds derived from tetrahydro-?-carboline, specifically tadalafil and intermediate products from the synthesis, comprising the reaction between piperonal and an alkyl ester of D-tryptophan as a salt, and in the absence of any other component, followed by haloacetylation and a final cyclization with methylamine.
Type:
Grant
Filed:
February 10, 2012
Date of Patent:
September 9, 2014
Assignee:
Interquim, S.A.
Inventors:
Xavier Berzosa Rodríguez, Francisco Marquillas Olondriz
Abstract: The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.
Abstract: This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.
Type:
Grant
Filed:
June 9, 2011
Date of Patent:
September 2, 2014
Assignee:
Technion Research & Development Foundation Limited
Inventors:
Gennady Nisnevich, Mark Gandelman, Kseniya Kulbitski
Abstract: Disclosed are: a ligand for an asymmetric synthesis catalyst; and a process for producing an ?-alkenyl cyclic compound using the ligand. Specifically disclosed are: a ligand for an asymmetric synthesis catalyst, which is represented by any one of formulae (1) to (4) [wherein R1 represents —Cl or —Br; R2 represents —CH3 or —CF3; and R3 represents —CH2—CH?CH2 or —H]; and a process for producing an ?-alkenyl cyclic compound using the ligand.
Type:
Grant
Filed:
October 1, 2010
Date of Patent:
September 2, 2014
Assignee:
National University Corporation Nagoya University
Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds;
Type:
Grant
Filed:
May 27, 2011
Date of Patent:
August 26, 2014
Assignee:
The Royal Institution for the Advancement of Learning/McGill University
Inventors:
Youla S. Tsantrizos, Joris Wim De Schutter, Yih-Shyan Lin
Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
Type:
Grant
Filed:
December 7, 2012
Date of Patent:
August 5, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn