Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/352)
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Patent number: 8633228Abstract: 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: GrantFiled: June 29, 2009Date of Patent: January 21, 2014Assignee: Mitsui Chemicals Agro, Inc.Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
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Publication number: 20140018397Abstract: 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: ApplicationFiled: September 12, 2013Publication date: January 16, 2014Applicant: Alkermes Pharma Ireland LimitedInventors: Sean Cunningham, Seamus Mulligan, Michael Myers
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Patent number: 8623853Abstract: 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: GrantFiled: July 21, 2009Date of Patent: January 7, 2014Assignees: The Brigham and Women's Hospital, Inc., Dana-Farber Cancer Institute, Inc.Inventors: Christopher French, Jon Aster, Matthias Hofer, James Bradner
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Publication number: 20140005212Abstract: 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: ApplicationFiled: December 21, 2011Publication date: January 2, 2014Applicant: Purdue Pharma L.P.Inventors: Chiyou Ni, Minnie Park, Bin Shao, Laykea Tafesse, Jiangchao Yao, Mark Youngman, Xiaoming Zhou
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Publication number: 20140005178Abstract: 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: ApplicationFiled: August 12, 2013Publication date: January 2, 2014Applicant: 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
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Publication number: 20140004044Abstract: 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: ApplicationFiled: May 17, 2013Publication date: January 2, 2014Applicant: The University of ChicagoInventors: Pedro Brugarolas, Brian Popko, Daniel Appelbaum
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Patent number: 8618142Abstract: 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: GrantFiled: April 10, 2013Date of Patent: December 31, 2013Assignee: Takeda GmbHInventors: Bernhard Kohl, Bernd Mueller, Walter Palosch
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Publication number: 20130345265Abstract: Dosage forms for oral administration of a PDE 4 inhibitor whose solubility is slight are described. They contain PVP as binder.Type: ApplicationFiled: April 30, 2013Publication date: December 26, 2013Applicant: Takeda GmbHInventors: Rango Dietrich, Klaus Eistetter, Hartmut Ney
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Publication number: 20130345240Abstract: 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: ApplicationFiled: August 16, 2013Publication date: December 26, 2013Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130345233Abstract: 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: ApplicationFiled: August 27, 2013Publication date: December 26, 2013Applicant: Ingenium Pharmaceuticals GmbHInventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Patent number: 8614213Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.Type: GrantFiled: August 5, 2009Date of Patent: December 24, 2013Assignee: Novartis AGInventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
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Patent number: 8614229Abstract: 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: GrantFiled: August 27, 2008Date of Patent: December 24, 2013Assignee: 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
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Publication number: 20130330277Abstract: 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: ApplicationFiled: August 12, 2013Publication date: December 12, 2013Applicant: ACORDA THERAPEUTICS, INC.Inventors: Andrew R. Blight, Ron Cohen
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Publication number: 20130331411Abstract: 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: ApplicationFiled: September 23, 2011Publication date: December 12, 2013Applicants: BETH ISRAEL DEACONESS MEDICAL CENTER, THE BROAD INSTITUTE, INC.Inventors: Chris Dockendorff, Robert Flaumenhaft, Lawrence MacPherson
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Patent number: 8604064Abstract: 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: GrantFiled: April 10, 2013Date of Patent: December 10, 2013Assignee: Takeda GmbHInventors: Bernhard Kohl, Bernd Mueller, Walter Palosch
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Patent number: 8603945Abstract: This disclosure relates to methods and compositions for modulating disease resistance in plants and transgenic plants.Type: GrantFiled: July 23, 2009Date of Patent: December 10, 2013Assignee: The Regents of the University of CaliforniaInventors: Colleen Marie Knoth, Thomas Eulgem, Thomas Girke
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Patent number: 8598086Abstract: 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: GrantFiled: June 7, 2010Date of Patent: December 3, 2013Assignee: Dow AgroSciences, LLC.Inventors: James M. Renga, Paul R. Schmitzer, Gregory T. Whiteker, Kim E. Arndt, Noormohamed M. Niyaz, Christian T. Lowe
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Patent number: 8598213Abstract: 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: GrantFiled: July 6, 2012Date of Patent: December 3, 2013Assignee: H. Lundbeck A/SInventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
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Publication number: 20130315897Abstract: 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: ApplicationFiled: May 8, 2013Publication date: November 28, 2013Applicant: Millennium Pharmaceuticals, Inc.Inventors: Uma Sinha, Stanley J. Hollenbach, Patrick Andre
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Publication number: 20130317020Abstract: 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: ApplicationFiled: August 2, 2013Publication date: November 28, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Publication number: 20130310347Abstract: 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: ApplicationFiled: May 21, 2013Publication date: November 21, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
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Publication number: 20130310426Abstract: 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: ApplicationFiled: July 24, 2013Publication date: November 21, 2013Applicant: Acorda Therapeutics, Inc.Inventors: Andrew R. Blight, Ron Cohen
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Publication number: 20130309199Abstract: 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: ApplicationFiled: November 3, 2011Publication date: November 21, 2013Inventors: Irmgard Tegeder, Gerd Geisslinger
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Patent number: 8586607Abstract: 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: GrantFiled: July 23, 2009Date of Patent: November 19, 2013Assignee: Syddansk UniversitetInventors: Trond Ulven, Elisabeth Christiansen
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Publication number: 20130303549Abstract: 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: ApplicationFiled: July 10, 2013Publication date: November 14, 2013Inventors: Jean-Guy BOITEAU, Laurence CLARY, Corinne Millois BARBUIS
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Publication number: 20130303526Abstract: 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: ApplicationFiled: September 16, 2011Publication date: November 14, 2013Applicant: Purdue Pharma L.P.Inventors: Chiyou NI, Bin Shao, Laykea Tafesse, Jiangchao Yao, Jianming Yu, Xiaoming Zhou
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Publication number: 20130289076Abstract: 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: ApplicationFiled: October 7, 2011Publication date: October 31, 2013Inventors: Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe, Marc Murtinell Pedemonte, Alberto Ortega Muñoz, Núrla Valls Vidal
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Publication number: 20130289081Abstract: 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: ApplicationFiled: January 19, 2011Publication date: October 31, 2013Applicants: UNIVERSITA' DEGLI DI PARMA, UNIVERSITY OF MARYLAND, BALTIMOREInventors: Robert Schwarcz, Gabriele Costantino, Laura Amori
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Patent number: 8563736Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: GrantFiled: March 22, 2012Date of Patent: October 22, 2013Assignee: 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
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Publication number: 20130274261Abstract: 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: ApplicationFiled: March 18, 2013Publication date: October 17, 2013Inventor: Arthur T. SANDS
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Patent number: 8557851Abstract: 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: GrantFiled: March 12, 2009Date of Patent: October 15, 2013Assignee: MEDA Pharma GmbH & Co. KGInventors: Istvan Szelenyi, Kay Brune, Robert Hermann, Mathia Locher
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Patent number: 8557852Abstract: 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: GrantFiled: August 28, 2009Date of Patent: October 15, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Craig Grant, James P. Kanter, Graeme Langlands
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Publication number: 20130267566Abstract: 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: ApplicationFiled: September 6, 2010Publication date: October 10, 2013Inventors: Andrew R. Blight, Ron Cohen
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Publication number: 20130267516Abstract: 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: ApplicationFiled: November 21, 2011Publication date: October 10, 2013Applicant: LEO PHARMA A/SInventors: Kristoffer Månsson, Lars Kristian Albert Blæhr
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Patent number: 8551523Abstract: 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: GrantFiled: July 20, 2011Date of Patent: October 8, 2013Assignee: Acorda Therapeutics, Inc.Inventors: Andrew R. Blight, Ron Cohen
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Patent number: 8552035Abstract: 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: GrantFiled: February 27, 2012Date of Patent: October 8, 2013Assignee: Pfizer Inc.Inventor: Paul V. Rucker
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Patent number: 8546403Abstract: 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: GrantFiled: April 12, 2011Date of Patent: October 1, 2013Assignee: Calcimedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Patent number: 8546563Abstract: 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: GrantFiled: October 30, 2008Date of Patent: October 1, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
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Publication number: 20130252818Abstract: 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: ApplicationFiled: March 25, 2013Publication date: September 26, 2013Inventors: Katherine Lovejoy, Rico Del Sesto, Andrew Koppisch
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Publication number: 20130253004Abstract: 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: ApplicationFiled: December 6, 2011Publication date: September 26, 2013Applicant: Amira Pharmaceuticals, Inc.Inventors: Thomas Jon Seiders, Bowei Wang, John Howard Hutchinson, Nicholas Simon Stock, Deborah Volkots
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Publication number: 20130252975Abstract: 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: ApplicationFiled: May 20, 2013Publication date: September 26, 2013Applicant: Amakem NVInventors: Dirk Leysen, Oliver Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
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Publication number: 20130252922Abstract: 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: ApplicationFiled: October 27, 2011Publication date: September 26, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: Marion Hitchcock
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Publication number: 20130252924Abstract: The present invention relates to new therapies to treat pain and related diseases, as well as pharmaceutical compounds for use in said therapies.Type: ApplicationFiled: November 11, 2011Publication date: September 26, 2013Applicant: AKRON MOLECULES GMBHInventors: Josef Penninger, Graham Gregory Neely, Shane McManus, Henrik Nilsson
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Patent number: 8541456Abstract: 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: GrantFiled: July 11, 2011Date of Patent: September 24, 2013Assignee: Takeda GmbHInventors: Hans-Peter Kley, Guido Hanauer, Daniela Hauser, Beate Schmidt, Dirk Bredenbröker, Wilhelm Wurst, Jörg Kemkowski
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Publication number: 20130243707Abstract: 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: ApplicationFiled: March 28, 2013Publication date: September 19, 2013Inventors: Monique Renata GREEN, Kenton FEDDE
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Patent number: 8536206Abstract: The invention relates to novel processes for the preparation of high-purity roflumilast.Type: GrantFiled: July 12, 2012Date of Patent: September 17, 2013Assignee: Takeda GmbHInventors: Bernhard Kohl, Bernd Mueller, Walter Palosch
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Patent number: 8536165Abstract: 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: GrantFiled: August 8, 2008Date of Patent: September 17, 2013Assignee: 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
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Publication number: 20130237531Abstract: 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: ApplicationFiled: April 19, 2013Publication date: September 12, 2013Inventors: Guoxian Wu, Jiazhong Zhang, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, James Tsai
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Patent number: 8530460Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: GrantFiled: December 14, 2012Date of Patent: September 10, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Bernd Nosse, Niklas Heine, Gerald Juergen Roth
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Patent number: 8530472Abstract: 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: GrantFiled: September 27, 2012Date of Patent: September 10, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira