Patents Examined by Cecilia M. Jaisle
  • Patent number: 9051275
    Abstract: The present invention relates to polymorphs and solvates of the hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine (P027), processes for their preparation, and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 4, 2011
    Date of Patent: June 9, 2015
    Assignee: Laboratories Del Dr. Esteve, S.A.
    Inventors: Ramón Berenguer Maimó, Jorge Medrano Rupérez, Jordi Benet Buchholz, Laura Puig Fernandez, Laia Pellejà Puxeu
  • Patent number: 9040537
    Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts thereof, the N-oxides thereof and the salts of the N-oxides thereof, where the radical A is of the formula A, wherein # denotes the point of attachment to the remainder of formulae I or II, and wherein A1 is N or C—RA1, A2 is N or C—RA2, A3 is N or C—RA3, A4 is N or C—RA4 and A5 is N or C—RA5, provided that one or two of the variables A1, A2, A3, A4 or A5 is N; RA1, RA5, if present, are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-haloalkyl and the like; RA2, RA4, if present, are H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; RA3, if present, is H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; where W is N or C—RW and V is N or C—RV, provided that one of the variables W or V is N; Rt and Rw, if present, are H, halogen, methyl, C1-haloalkyl and the like; Ru and Rv, if present, are H, halogen, C1-C4-alkyl, C1-C3-haloalkyl and the like; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkyl
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: May 26, 2015
    Assignee: BASF SE
    Inventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Wolfgang Von Deyn, Douglas D. Anspaugh, Deborah L. Culbertson
  • Patent number: 9012632
    Abstract: Provided is a method whereby a heteroaromatic ring aryl can be very rapidly methylated at a high yield. In an N-alkyl-2-pyrrolidinone, a heteroaromatic ring aryltrialkylstannan is cross-coupled with methyl iodide in the presence of a palladium complex, a phosphine ligand, a cuprous halide, a carbonic acid salt and/or an alkali metal fluoride to thereby rapidly methylate the heteroaromatic ring aryl. (Formula shows a case wherein the heteroaromatic ring aryl is a pyridyl group.
    Type: Grant
    Filed: December 25, 2009
    Date of Patent: April 21, 2015
    Assignee: Riken
    Inventors: Masaaki Suzuki, Hisashi Doi, Hiroko Koyama
  • Patent number: 9012639
    Abstract: The invention relates to copper(I) complexes of the formula A wherein X=Cl, Br or I (independently of one another); N*?E=a bidentate ligand, wherein E=a phosphinyl group including a phosphorus atom or an arsenyl group including an arsenic atom, wherein the phosphinyl group or the arsenyl group is combined with R in the form of R2E (where R=alkyl, aryl, alkoxy, or phenoxy; N*=imine function which is part of an aromatic group selected from pyridyl, pyrimidyl, pyridazinyl, triazinyl, oxazolyl, thiazolyl and imidazolyl, the aromatic group optionally having at least one substituent to increase the solubility of the copper(I) complex in an organic solvent; and ?=at least one carbon atom which is likewise part of the aromatic group. The carbon atom is located directly adjacent both to the imine nitrogen atom, coordinating to Cu in the case of a bridging ligand and to the phosphorus or arsenic atom.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: April 21, 2015
    Assignee: Cynora GmbH
    Inventors: Hartmut Yersin, Uwe Monkowius, Tobias Fisher, Thomas Hofbeck, Thomas Baumann, Tobias Grab
  • Patent number: 9012451
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 2, 2012
    Date of Patent: April 21, 2015
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Konstanze Hurth, Timothy John Ritchie
  • Patent number: 9000158
    Abstract: In an embodiment, the present invention provides a process for preparing (?)-6-(4-aminophenyl)-5-methylpyridazin-3-(2H)-one, which process comprises: a) reacting racemic 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone of formula II with a chiral tartaric acid derivative to obtain a diastereomeric salt of (?)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone and the chiral tartaric acid derivative; and b) reacting the diastereomeric salt with a base to obtain (?)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone. The (?)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone may be used to prepare levosimendan.
    Type: Grant
    Filed: July 12, 2010
    Date of Patent: April 7, 2015
    Assignee: Cipla Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Ashwini Amol Sawant
  • Patent number: 8993562
    Abstract: The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. Compounds of formula (I) are useful for treating or preventing diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: March 31, 2015
    Assignee: Ferrer Internacional, S.A.
    Inventors: José Luís Falcó, Albert Palomer, Antonio Guglietta
  • Patent number: 8993754
    Abstract: Provided is an iridium complex having a substructure represented by the following formula (1), which is a luminescent element material capable of luminescence with high brightness/high efficiency and excellent in durability and can be used in a luminescent element, etc.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: March 31, 2015
    Assignee: National Institute of Advanced Industrial Science and Technology
    Inventor: Hideo Konno
  • Patent number: 8987446
    Abstract: The invention relates to bimetallic complexes in which the ligand contains a salophen unit which complexes copper, manganese or cobalt and a phenanthroline unit which complexes palladium and the two systems are linked by a continuous conjugated system. The invention further relates to the use of these bimetallic complexes as catalysts for the oxidative carbonylation of aromatic hydroxy compounds to form diaryl carbonates, a process for preparing diaryl carbonates using the bimetallic complex as catalyst and also diaryl carbonates prepared by oxidative carbonylation of aromatic hydroxy compounds using the bimetallic complexes of the invention as catalysts.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Christoph Gürtler, Thomas Ernst Müller, Pieter Ooms, Johann Rechner, Friedhelm Risse, Angelina Prokofieva, Franco Doro, Burkhard Köhler, Walter Leitner, Aurel Wolf
  • Patent number: 8962625
    Abstract: A pyridazinone compound represented by the formula (I) has excellent effect on weed control and is useful as an active ingredient of herbicides.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: February 24, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Toshiyuki Kiji, Takafumi Fusaka
  • Patent number: 8962834
    Abstract: The invention relates to compounds of formula wherein the substituents are as described in claim 1. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: February 24, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Helmut Jacobsen, Synese Jolidon, Thomas Luebbers
  • Patent number: 8957073
    Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: May 11, 2011
    Date of Patent: February 17, 2015
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
  • Patent number: 8946222
    Abstract: Phenoxymethyl compounds that inhibit at least one phosphodiesterase 10 are described as are pharmaceutical compositions containing such compounds an methods for treating various CNS disorders by administering such compounds to a patient in need thereof.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: February 3, 2015
    Assignee: FORUM Pharmaceuticals Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Patent number: 8946221
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, L1, L2, X, Y, Q and Z have defined meanings.
    Type: Grant
    Filed: August 13, 2010
    Date of Patent: February 3, 2015
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Laurence Anne Mevellec, Ludo E. J. Kennis, Josephus Carolus Mertens, Jacobus A. J. Van Dun, Maria V. F. Somers, Walter B. L. Wouters
  • Patent number: 8940743
    Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: January 27, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Marcel Frans Leopold De Bruyn, Gregor James MacDonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck
  • Patent number: 8937067
    Abstract: Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: January 20, 2015
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
  • Patent number: 8937073
    Abstract: Disubstituted tetrahydrofuranyl compounds of general formula I of which the following are exemplary:
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: January 20, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Birgit Jung, Raimund Kuelzer
  • Patent number: 8933090
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
    Type: Grant
    Filed: October 19, 2010
    Date of Patent: January 13, 2015
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
  • Patent number: 8927549
    Abstract: Embodiments of the present invention provide adamantyl benzamide derivatives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) in a subject are also provided.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: January 6, 2015
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Dharma Rao Polisetti, Suparna Gupta, Soren Ebdrup
  • Patent number: 8927540
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4?, have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: January 6, 2015
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat