Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/352)
  • Patent number: 8633228
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: January 21, 2014
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • Publication number: 20140018397
    Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 16, 2014
    Applicant: Alkermes Pharma Ireland Limited
    Inventors: Sean Cunningham, Seamus Mulligan, Michael Myers
  • Patent number: 8623853
    Abstract: The present invention is directed, inter alia, to methods of treating NUT midline carcinoma (NMC) by administering compounds that promote increased histone acetylation. The invention also includes assay methods for determining the responsiveness of NMC to specific histone deacetylases and other compounds.
    Type: Grant
    Filed: July 21, 2009
    Date of Patent: January 7, 2014
    Assignees: The Brigham and Women's Hospital, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Christopher French, Jon Aster, Matthias Hofer, James Bradner
  • Publication number: 20140005212
    Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, R1b, R2a, R2b, R2c, A1, A2, and X are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: December 21, 2011
    Publication date: January 2, 2014
    Applicant: Purdue Pharma L.P.
    Inventors: Chiyou Ni, Minnie Park, Bin Shao, Laykea Tafesse, Jiangchao Yao, Mark Youngman, Xiaoming Zhou
  • Publication number: 20140005178
    Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).
    Type: Application
    Filed: August 12, 2013
    Publication date: January 2, 2014
    Applicant: Almirall, S.A.
    Inventors: Julio Cesar CASTRO PALOMINO LARIA, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Siliva Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
  • Publication number: 20140004044
    Abstract: The present disclosure provides novel compounds, including compounds that bind to potassium channels, methods for their manufacture, and methods for their use, including for the treatment of demyelinating diseases and/or in vivo imaging of the central nervous system to diagnose and/or assess the progression of MS or other diseases.
    Type: Application
    Filed: May 17, 2013
    Publication date: January 2, 2014
    Applicant: The University of Chicago
    Inventors: Pedro Brugarolas, Brian Popko, Daniel Appelbaum
  • Patent number: 8618142
    Abstract: A composition comprising: roflumilast having a purity of greater than or equal to 99% by weight, and N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight.
    Type: Grant
    Filed: April 10, 2013
    Date of Patent: December 31, 2013
    Assignee: Takeda GmbH
    Inventors: Bernhard Kohl, Bernd Mueller, Walter Palosch
  • Publication number: 20130345265
    Abstract: Dosage forms for oral administration of a PDE 4 inhibitor whose solubility is slight are described. They contain PVP as binder.
    Type: Application
    Filed: April 30, 2013
    Publication date: December 26, 2013
    Applicant: Takeda GmbH
    Inventors: Rango Dietrich, Klaus Eistetter, Hartmut Ney
  • Publication number: 20130345240
    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: August 16, 2013
    Publication date: December 26, 2013
    Applicant: CALCIMEDICA, INC.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20130345233
    Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.
    Type: Application
    Filed: August 27, 2013
    Publication date: December 26, 2013
    Applicant: Ingenium Pharmaceuticals GmbH
    Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
  • Patent number: 8614213
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: December 24, 2013
    Assignee: Novartis AG
    Inventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
  • Patent number: 8614229
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: December 24, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • Publication number: 20130330277
    Abstract: Disclosed herein are methods and compositions related to use of aminopyridines, such as fampridine, to improve impairments of patients with a demyelinating condition, such as MS.
    Type: Application
    Filed: August 12, 2013
    Publication date: December 12, 2013
    Applicant: ACORDA THERAPEUTICS, INC.
    Inventors: Andrew R. Blight, Ron Cohen
  • Publication number: 20130331411
    Abstract: The invention relates to the use of a compound of Formula I for the treatment of protease-activated receptor mediated diseases by the administration of a compound of Formula I or a prodrug or metabolite thereof.
    Type: Application
    Filed: September 23, 2011
    Publication date: December 12, 2013
    Applicants: BETH ISRAEL DEACONESS MEDICAL CENTER, THE BROAD INSTITUTE, INC.
    Inventors: Chris Dockendorff, Robert Flaumenhaft, Lawrence MacPherson
  • Patent number: 8604064
    Abstract: A method for the treatment of chronic obstructive pulmonary disease (COPD), including administering to a patient suffering from COPD, a therapeutically effective amount of roflumilast having a purity of greater than or equal to 99% by weight, and N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight.
    Type: Grant
    Filed: April 10, 2013
    Date of Patent: December 10, 2013
    Assignee: Takeda GmbH
    Inventors: Bernhard Kohl, Bernd Mueller, Walter Palosch
  • Patent number: 8603945
    Abstract: This disclosure relates to methods and compositions for modulating disease resistance in plants and transgenic plants.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: December 10, 2013
    Assignee: The Regents of the University of California
    Inventors: Colleen Marie Knoth, Thomas Eulgem, Thomas Girke
  • Patent number: 8598086
    Abstract: 3-Halo-6-(aryl)-4-iminotetrahydropicolinic acids having mono-, di- tri- and tetra-substituted aryl substituents in the 6-position, and their acid derivatives, are herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: December 3, 2013
    Assignee: Dow AgroSciences, LLC.
    Inventors: James M. Renga, Paul R. Schmitzer, Gregory T. Whiteker, Kim E. Arndt, Noormohamed M. Niyaz, Christian T. Lowe
  • Patent number: 8598213
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: December 3, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20130315897
    Abstract: The present invention is directed to methods of using combination therapies containing [2-({4-[(dimethylamino)iminomethyl]phenyl}carbonylamino)-5-methoxyphenyl]-N-(5-chloro(2-pyridyl))carboxamide for the treatment of thrombotic disease(s) and pharmaceutical compositions thereof.
    Type: Application
    Filed: May 8, 2013
    Publication date: November 28, 2013
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Uma Sinha, Stanley J. Hollenbach, Patrick Andre
  • Publication number: 20130317020
    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: Application
    Filed: August 2, 2013
    Publication date: November 28, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
  • Publication number: 20130310347
    Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 21, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
  • Publication number: 20130310426
    Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.
    Type: Application
    Filed: July 24, 2013
    Publication date: November 21, 2013
    Applicant: Acorda Therapeutics, Inc.
    Inventors: Andrew R. Blight, Ron Cohen
  • Publication number: 20130309199
    Abstract: The present invention relates to the use of an R-enantiomer of a compound according to the following formula (I) (I), wherein R1 or R2 is a group selected from H, —CH3, —CH2CH3, —CH2CH2CH3, and —CH2CH2CH2CH3 or can be taken together with another to give a cyclopropyl ring, a cyclobutyl ring, a cyclopentyl ring, or a cyclohexyl ring, R3 is a group selected from —COOH, —COOR6, —CONH2, —CONHR6, —CONR6R7, —CONHSO2R6, —COO—(CH2)3—CH2OH, —COO—(CH2)4—ONO2, —COO—PhOCH3—C2H2—COO—(CH2)4—ONO2, tetrazolyl, and a —COOH bioisostere, R4 or R5 is a group selected from —Cl, —F, —Br, —I, —CF3, —OCF3, —SCF3, —OCH3, —OCH2CH3, —CN, —CH?CH2, —CH2OH, and —NO2, R6 of R7 is a group selected from —CH3, —CH2CH3, —CH2CH2CH3, and —CH2CH2CH2CH3, and m or n is an integer selected from 0, 1, 2, and 3, or a nitro-variant of said compound, and pharmaceutically acceptable salts of said compound, preferably Tarenflurbil (R-Flurbiprofen), for use in the treatment of multiple sclerosis (MS).
    Type: Application
    Filed: November 3, 2011
    Publication date: November 21, 2013
    Inventors: Irmgard Tegeder, Gerd Geisslinger
  • Patent number: 8586607
    Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: November 19, 2013
    Assignee: Syddansk Universitet
    Inventors: Trond Ulven, Elisabeth Christiansen
  • Publication number: 20130303549
    Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.
    Type: Application
    Filed: July 10, 2013
    Publication date: November 14, 2013
    Inventors: Jean-Guy BOITEAU, Laurence CLARY, Corinne Millois BARBUIS
  • Publication number: 20130303526
    Abstract: The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: September 16, 2011
    Publication date: November 14, 2013
    Applicant: Purdue Pharma L.P.
    Inventors: Chiyou NI, Bin Shao, Laykea Tafesse, Jiangchao Yao, Jianming Yu, Xiaoming Zhou
  • Publication number: 20130289076
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
    Type: Application
    Filed: October 7, 2011
    Publication date: October 31, 2013
    Inventors: Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe, Marc Murtinell Pedemonte, Alberto Ortega Muñoz, Núrla Valls Vidal
  • Publication number: 20130289081
    Abstract: A derivative of nicotinic acid N-oxide is described having formula (I): that acts as inhibitor of enzyme 3-hydroxyanthranilate-3,4-dioxygenase (3HAO), and is thus able to reduce QUIN biosynthesis in vivo under excitotoxic or pathological conditions, said compound being at the same time also chemically stable towards auto-oxidation.
    Type: Application
    Filed: January 19, 2011
    Publication date: October 31, 2013
    Applicants: UNIVERSITA' DEGLI DI PARMA, UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Robert Schwarcz, Gabriele Costantino, Laura Amori
  • Patent number: 8563736
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: October 22, 2013
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Publication number: 20130274261
    Abstract: Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and a prostacyclin. Pharmaceutical formulations are also disclosed.
    Type: Application
    Filed: March 18, 2013
    Publication date: October 17, 2013
    Inventor: Arthur T. SANDS
  • Patent number: 8557851
    Abstract: The invention relates to pharmaceutical combinations of potassium channel openers and sodium channel inhibitors, for treating pains which are accompanied by an increase in muscle tone.
    Type: Grant
    Filed: March 12, 2009
    Date of Patent: October 15, 2013
    Assignee: MEDA Pharma GmbH & Co. KG
    Inventors: Istvan Szelenyi, Kay Brune, Robert Hermann, Mathia Locher
  • Patent number: 8557852
    Abstract: The present invention provides methods for preventing or treating a condition characterized by undesired thrombosis in a mammal using a crystalline polymorph form of a maleate salt of a compound of Formula I that has activity against mammalian factor Xa.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: October 15, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Craig Grant, James P. Kanter, Graeme Langlands
  • Publication number: 20130267566
    Abstract: Disclosed herein are methods and compositions related to the durable use of aminopyridines, such as 4-aminopyridine, to improve impairments of patients with a demyelinating condition, such as MS.
    Type: Application
    Filed: September 6, 2010
    Publication date: October 10, 2013
    Inventors: Andrew R. Blight, Ron Cohen
  • Publication number: 20130267516
    Abstract: Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: October 10, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Kristoffer Månsson, Lars Kristian Albert Blæhr
  • Patent number: 8551523
    Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: October 8, 2013
    Assignee: Acorda Therapeutics, Inc.
    Inventors: Andrew R. Blight, Ron Cohen
  • Patent number: 8552035
    Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: October 8, 2013
    Assignee: Pfizer Inc.
    Inventor: Paul V. Rucker
  • 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
  • Patent number: 8546563
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are 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: October 30, 2008
    Date of Patent: October 1, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
  • Publication number: 20130252818
    Abstract: An amorphous formulation of a herbicidal or pesticidal substance includes a composition of the formula [A]x[MpClq]y, the composition being an ionic liquid with a melting temperature below 150° C., wherein [MpClq] is a metal chloride, x is 1, 2, 3, or 4, p is 1, 2, 3, or 4, q is 1, 2, 3, 4, 5, 6, 7, 8, or 9, and y is 1 or 2, wherein each A is a cation that is a herbicidal or pesticidal substance or a cation precursor that is a herbicidal or pesticidal substance.
    Type: Application
    Filed: March 25, 2013
    Publication date: September 26, 2013
    Inventors: Katherine Lovejoy, Rico Del Sesto, Andrew Koppisch
  • Publication number: 20130253004
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: December 6, 2011
    Publication date: September 26, 2013
    Applicant: Amira Pharmaceuticals, Inc.
    Inventors: Thomas Jon Seiders, Bowei Wang, John Howard Hutchinson, Nicholas Simon Stock, Deborah Volkots
  • Publication number: 20130252975
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Application
    Filed: May 20, 2013
    Publication date: September 26, 2013
    Applicant: Amakem NV
    Inventors: Dirk Leysen, Oliver Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
  • 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
  • Publication number: 20130252924
    Abstract: The present invention relates to new therapies to treat pain and related diseases, as well as pharmaceutical compounds for use in said therapies.
    Type: Application
    Filed: November 11, 2011
    Publication date: September 26, 2013
    Applicant: AKRON MOLECULES GMBH
    Inventors: Josef Penninger, Graham Gregory Neely, Shane McManus, Henrik Nilsson
  • Patent number: 8541456
    Abstract: The application relates to specific combinations of Roflumilast and/or Roflumilast N-Oxide and a PPAR-agonist, as well as their use in the treatment of diabetes mellitus type 2.
    Type: Grant
    Filed: July 11, 2011
    Date of Patent: September 24, 2013
    Assignee: Takeda GmbH
    Inventors: Hans-Peter Kley, Guido Hanauer, Daniela Hauser, Beate Schmidt, Dirk Bredenbröker, Wilhelm Wurst, Jörg Kemkowski
  • Publication number: 20130243707
    Abstract: Topical compositions are disclosed that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder. A composition of the present invention comprises a Drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the Drug, the solvent system is a low alkanol system, and the composition is a single phase composition. Exemplary solvent systems are those for which one of the at least two solvent alcohols is polyethylene glycol, glycerin, butylene glycol, diproylene glycol, propylene glycol, ethanol, isopropanol, or a derivative thereof. Optionally the local inflammatory disorder is pseudofolliculitis barbae, dermatitis, psoriasis, wounds, or sunburn.
    Type: Application
    Filed: March 28, 2013
    Publication date: September 19, 2013
    Inventors: Monique Renata GREEN, Kenton FEDDE
  • Patent number: 8536206
    Abstract: The invention relates to novel processes for the preparation of high-purity roflumilast.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: September 17, 2013
    Assignee: Takeda GmbH
    Inventors: Bernhard Kohl, Bernd Mueller, Walter Palosch
  • Patent number: 8536165
    Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).
    Type: Grant
    Filed: August 8, 2008
    Date of Patent: September 17, 2013
    Assignee: Almirall, S.A.
    Inventors: Julio Cesar Castro Palomino Laria, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
  • Publication number: 20130237531
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 12, 2013
    Inventors: Guoxian Wu, Jiazhong Zhang, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, James Tsai
  • Patent number: 8530460
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 10, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Bernd Nosse, Niklas Heine, Gerald Juergen Roth
  • Patent number: 8530472
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, W, Y, R, R1, R2, R3 and R3? are as described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: September 10, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira