Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 546/159)
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Publication number: 20130203768Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: September 28, 2011Publication date: August 8, 2013Inventors: Michael Berger, Christopher Kern, Marko Eck, Jörg Schröder
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Patent number: 8497378Abstract: The present invention relates to the field of synthesizing anti-infective compounds. More particularly, the invention relates to synthesizing a family of quinolone compounds useful as anti-infective agents. The invention includes a process for preparing a quinolone compound wherein less than about 0.40% of dimeric impurity of the quinolone is produced.Type: GrantFiled: September 23, 2009Date of Patent: July 30, 2013Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Roger Hanselmann, Maxwell M. Reeve, Graham Johnson
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Publication number: 20130190500Abstract: This invention relates to a process for the preparation of 6-chloro-3-amino-2-(2-hydroxypropyl)-1-azanapthalene. It comprises treating 6-chloro-3-pyridylium-2-ethoxycarbonyl-1-azanaphthanlene bromide with morpholine at about 80° C., followed by treating the product thereof with methylmagnesium chloride.Type: ApplicationFiled: December 10, 2012Publication date: July 25, 2013Applicant: NEURON SYSTEMS, INC.Inventor: Neuron Systems, Inc.
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Publication number: 20130178499Abstract: The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: October 7, 2011Publication date: July 11, 2013Applicant: N30 PHARMACEUTICALS, INC.Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Patent number: 8471030Abstract: This invention concerns generally with a process for purifying crude pharmaceutical compositions, wherein the crude pharmaceutical composition comprises a sodium salt of Montelukast and more particularly relates to a process for the production of pharmaceutically pure preparations of Montelukast sodium using simulated moving bed technology, without requiring an intermediate acid formation step to separate isomers and to remove impurities.Type: GrantFiled: December 6, 2010Date of Patent: June 25, 2013Assignee: Orochem Technologies Inc.Inventors: Arun Kanti Mandal, Kamlesh Jayantilal Ranbhan, Ganesh Gurpur Pai, Abhilesh Agarwal, Rakesh Vikraman Nair Rema, Asha Oroskar
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Patent number: 8470852Abstract: The invention relates to substituted 2-amino-quinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: GrantFiled: August 26, 2011Date of Patent: June 25, 2013Assignee: Gruenenthal GmbHInventors: Sven Kühnert, Gregor Bahrenberg, Dagmar Kaulartz, Achim Kless, Wolfgang Schröder
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Patent number: 8466290Abstract: The present invention provides a STATS inhibitor containing as an active ingredient, a quinolinecarboxamide derivative represented by the formula (I) (in the formula, W represents a bond or an alkylene chain; X represents O, S, or NR34; and R1 to R8 and R34 each represent H, halogen, alkyl, phenyl, furyl, thienyl, or the like), or a pharmacologically acceptable salt thereof.Type: GrantFiled: July 10, 2009Date of Patent: June 18, 2013Assignees: Pharma IP General Incorporated Association, Pharma Design, Inc., Shizuoka Prefecture, Kumamoto Health Science University, Kabushiki Kaisha Yakult HonshaInventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Takane Yokotagawa, Osamu Takahashi, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
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Publication number: 20130150368Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R2, R4, R5, R6, R7, R8, R9, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 22, 2011Publication date: June 13, 2013Applicant: CYTOKINETICS, INC.Inventors: Luke W. Ashcraft, Gustave Bergnes, Scott Collibee, Chihyuan Chuang, Jeff Gardina, Bradley P. Morgan, Alex R. Muci, Xiangping Qian, Antonio Romero, Jeffrey Warrington, Zhe Yang
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Publication number: 20130150392Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.Type: ApplicationFiled: February 8, 2013Publication date: June 13, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: SUMITOMO CHEMICAL COMPANY, LIMITED
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Publication number: 20130150359Abstract: The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent.Type: ApplicationFiled: June 24, 2011Publication date: June 13, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Thomas Fuchss, Werner Mederski, Frank Zenke
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Patent number: 8461182Abstract: PROBLEM To provide a novel compound, a pharmaceutically acceptable salt or a hydrate thereof useful for preventing or treating for depression, anxiety disorders (such as generalized anxiety disorder, posttraumatic stress disorder, panic disorder, obsessive-compulsive disorder or social anxiety disorder), attention deficit disorder, mania, manic-depressive illness, schizophrenia, mood disorders, stress, sleep disorders, attacks, memory impairment, cognitive impairment, dementia, amnesia, delirium, obesity, eating disorder, appetite disorder, hyperphagia, bulimia, cibophobia, diabetes, cardiovascular diseases, hypertension, dyslipidemia, myocardial infarction, movement disorder (such as Parkinson's disease, epilepsy, convulsion or tremor), drug abuse, drug addiction or sexual dysfunction, based on a melanin-concentrating hormone receptor (MCH receptor) antagonistic action. SOLUTION A compound, a pharmaceutically acceptable salt or a hydrate thereof represented by the formula (I).Type: GrantFiled: September 30, 2009Date of Patent: June 11, 2013Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Kosuke Kanuma, Naoki Miyakoshi, Madoka Kawamura, Tsuyoshi Shibata
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Patent number: 8461339Abstract: The invention provides kinase inhibitor compounds of the formula (1): or salts, solvates, tautomers or N-oxides thereof; wherein X is O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; m is 0-2; n is 0-1; q is 0-2; A is C1-6 alkylene optionally interrupted by O; R1 is halogen, cyano, nitro, an optionally substituted acyclic C1-6 hydrocarbon group, optionally substituted C3-7 cycloalkyl, optionally substituted phenyl, optionally substituted five membered heteroaryl, NR2R3, Ra—Rb, O—Rb or C(O)NR2R8; R4 is fluorine, chlorine, methyl or cyano; R2 is hydrogen or optionally substituted C1-4 alkyl; R3 is Ra—Rb; or NR2R3 forms a 4 to 7 membered non-aromatic heterocyclic ring; Ra is a bond, C(X2), C(X2)X1, SO, SO2 or SO2NRc; Rb is hydrogen or an optionally substituted 3 to 7-membered carbocyclic or heterocyclic ring or an optionally substituted C1-12 acyclic hydrocarbon group; Rc is hydrogen or a C1-4 hydrocarbon group; Rd is O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2Type: GrantFiled: July 15, 2009Date of Patent: June 11, 2013Assignee: Sentinel Oncology LimitedInventors: Robert George Boyle, David Winter Walker
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Patent number: 8455648Abstract: The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: April 24, 2009Date of Patent: June 4, 2013Assignee: Abbott GmbH & Co. KGInventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Wilfried Hornberger
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Patent number: 8445512Abstract: The invention relates to substituted quinoline-3—Carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: GrantFiled: August 26, 2011Date of Patent: May 21, 2013Assignee: Gruenenthal GmbHInventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder
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Patent number: 8440595Abstract: Fungicidal compounds of the general formula (I), wherein the substituents are as defined in claim 1.Type: GrantFiled: September 3, 2008Date of Patent: May 14, 2013Assignee: Syngenta Crop Protection LLCInventors: Laura Quaranta, Fiona Murphy Kessabi, Renaud Beaudegnies, Hans-Georg Brunner, Fredrik Cederbaum
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Publication number: 20130116234Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.Type: ApplicationFiled: November 1, 2012Publication date: May 9, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8436016Abstract: The present invention is directed to fused heterocyclic compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: October 13, 2009Date of Patent: May 7, 2013Inventors: Scott D. Kuduk, Christina Ng Di Marco
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Publication number: 20130098770Abstract: Copper plating baths containing a leveling agent that is a reaction product of one or more of certain pyridine compounds with one or more epoxide-containing compounds, that deposit copper on the surface of a conductive layer are provided. Such plating baths deposit a copper layer that is substantially planar on a substrate surface across a range of electrolyte concentrations. Methods of depositing copper layers using such copper plating baths are also disclosed.Type: ApplicationFiled: October 24, 2011Publication date: April 25, 2013Applicant: Rohm and Haas Electronic Materials LLCInventors: Zuhra I. NIAZIMBETOVA, Maria Anna Rzeznik
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Publication number: 20130102632Abstract: The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: December 6, 2012Publication date: April 25, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Patent number: 8426598Abstract: The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: July 31, 2009Date of Patent: April 23, 2013Assignee: Merck, Sharp & Dohme, Corp.Inventors: Scott D. Kuduk, Christina Ng Di Marco
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Patent number: 8420670Abstract: The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors.Type: GrantFiled: August 22, 2008Date of Patent: April 16, 2013Assignees: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Wilhelm Amberg, Michael Ochse, Wilfried Braje, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
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Patent number: 8415475Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.Type: GrantFiled: December 4, 2007Date of Patent: April 9, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, David Francis Alain Lançois, Ismet Dorange, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
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Patent number: 8415272Abstract: Compounds of the general Formula (1) wherein the substituents are as defined in claim 1, are useful as fungicides.Type: GrantFiled: January 8, 2009Date of Patent: April 9, 2013Assignee: Syngenta Crop Protection LLCInventors: Fiona Murphy Kessabi, Laura Quaranta, Renaud Beaudegnies, Hans-Georg Brunner, Fredrik Cederbaum
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Patent number: 8410134Abstract: The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.Type: GrantFiled: March 22, 2008Date of Patent: April 2, 2013Assignee: Shire Orphan Therapies GmbHInventors: Christoph Gibson, Thomas Tradler, Karsten Schnatbaum, Jochen Pfeifer, Elsa Locardi, Dirk Scharn, Matthias Paschke, Ulf Reimer, Uwe Richter, Gerd Hummel, Ulrich Reineke
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Patent number: 8410274Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: GrantFiled: January 26, 2012Date of Patent: April 2, 2013Assignee: Vertex PharmaceuticalsInventors: Patricia Hurter, William Rowe, Christopher Ryan Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
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Patent number: 8404849Abstract: The present invention relates to the process for producing modulators of cystic fibrosis transmembrane conductance regulator (CFTR).Type: GrantFiled: May 20, 2011Date of Patent: March 26, 2013Assignee: Vertex PharmaceuticalsInventors: Lifang Sun, Khisal Ahmed Alvi, Caroline Joyce Decker, Yongmin Li
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Patent number: 8404713Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, Z and n have defined meanings, the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary ammonium salts and the stereochemically isomeric forms thereof, and their use for the treatment of PARP-mediated disorders.Type: GrantFiled: October 22, 2008Date of Patent: March 26, 2013Assignee: Janssen Pharmaceutica NVInventors: Patrick René Angibaud, Laurence Françoise Bernadette Marconnet-Decrane, Jorge Eduardo Vialard, Laurence Anne Mevellec, Christophe Meyer, Pierre-Henri Storck
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Patent number: 8399674Abstract: The present invention relates to 2-aminoquinolines of formula I wherein R1, R2 and R3 are as defined in the specification, as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.Type: GrantFiled: January 27, 2012Date of Patent: March 19, 2013Assignee: Hoffman-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Patent number: 8394828Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to quinoline-derived amides that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.Type: GrantFiled: July 16, 2008Date of Patent: March 12, 2013Assignee: Janssen Pharmaceutica, NVInventors: Ellen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
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Patent number: 8394959Abstract: The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.Type: GrantFiled: April 6, 2012Date of Patent: March 12, 2013Assignee: Wyeth LLCInventors: Qinghong Lu, Mannching Sherry Ku, Warren Chew, Gloria Cheal, Anthony F. Hadfield, Mahmoud Mirmehrabi
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Patent number: 8394958Abstract: The present invention relates to compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: GrantFiled: November 21, 2008Date of Patent: March 12, 2013Assignee: Bayer Pharma AGInventors: Markus Berger, Hartmut Rehwinkel, Thomas Zollner, Ekkehard May, Jorma Hassfeld, Heike Schacke
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Patent number: 8394829Abstract: Provided are compounds of Formula I: wherein X is: R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.Type: GrantFiled: May 9, 2011Date of Patent: March 12, 2013Assignee: Gilead Sciences, Inc.Inventors: William R. Baker, Shaopei Cai, Joshua Aaron Kaplan, Musong Kim, Jennifer Alissa Loyer-Drew, Stephane Perreault, Gary Phillips, Lafe J. Purvis, II, Marcin Stasiak, Kirk K. Stevens, Josh Van Veldhuizen
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Publication number: 20130059852Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).Type: ApplicationFiled: April 8, 2011Publication date: March 7, 2013Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
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Patent number: 8389727Abstract: The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment therewith.Type: GrantFiled: October 21, 2010Date of Patent: March 5, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Beili Zhang, Mariusz Krawiec, Brian Luisi, Ales Medek
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Publication number: 20130053375Abstract: Disclosed are quinoline compounds having the formula: wherein R1, R2 and A are as defined herein, and methods of making and using the same.Type: ApplicationFiled: May 6, 2011Publication date: February 28, 2013Inventors: Michael Jonathan Bury, Linda N. Casillas, Adam Kenneth Charnley, Michael P. DeMartino, Xiaoyang Dong, Patrick Eidam, Pamela A. Haile, Philip Anthony Harris, Ami Lakdawala Shah, Bryan W. King, Robert W. Marquis, JR., John F. Mehlmann, Joseph J. Romano, Clark A. Sehon
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Patent number: 8383836Abstract: Psoralen compounds of Formula (I): wherein (N+ Aryl) is a member selected from the group consisting of nitrogen containing aromatic heterocycles of formulae (i)-(iii): wherein Z is a group of formula: wherein R is C1-C30 hydrocarbyl, which may be linear, branched or cyclic and contains from 1 to 15 carbon-carbon double bonds, which may be conjugated or unconjugated with one another or may include an aryl ring, and may contain one or more substituents; R1 is hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, alkene-aryl, alkene-heteroaryl, alkene-heterocyclyl, alkene-cycloalkyl, fused cycloalkylaryl, fused cycloalkylheteroaryl, fused heterocyclylaryl, fused heterocyclyheteroaryl, alkylene-fused cycloalkylaryl, alkylene-fused cycloalkylheteroaryl, alkylene-fused heterocyclylaryl, alkylene-fused heterocyclyheteroaryl; n is an integer from 1 to 8 and X is a pharmaceutically acceptable counter ion; and their use in methods for the treatment of a cell proliferatType: GrantFiled: April 20, 2010Date of Patent: February 26, 2013Assignees: Duke University, Immunolight, LLCInventors: Eric Toone, David Gooden, Tuan Vo-Dinh, Frederic A. Bourke, Jr.
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Patent number: 8378106Abstract: A method is described for preparing argatroban monohydrate obtained from (2R,4R)-1-[NG-nitro-N2-(3-methyl-8-quinolinesulphonyl)-L-arginyl]-4-methyl-2-piperidine carboxylic acid by suitably treating crude argatroban. The method either comprises preparation of argatroban monohydrate in a continuous step or an intermediate step of isolating a purified argatroban. Also obtainable from argatroban monohydrate is anhydrous argatroban, shown to have new physico-chemical characteristics. The described argatroban synthesis and purification process hence enables three different forms of argatroban, not previously described, to be obtained, each with distinctive physico-chemical characteristics and in particular enables argatroban monohydrate to be obtained with high yield and with high purity, being therefore a product suitable for use as active principle in proprietary medicines.Type: GrantFiled: April 6, 2009Date of Patent: February 19, 2013Assignee: Lundbeck Pharmaceuticals Italy S.p.A.Inventors: Jacopo Zanon, Giovanna Libralon, Andrea Nicole′
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Publication number: 20130041046Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Applicant: SENOMYX, INC.Inventors: Catherine TACHDJIAN, Xiao Qing TANG, Donald S. KARANEWSKY, Guy SERVANT, Xiaodong LI, Feng ZHANG, Qing CHEN, Hong ZHANG, Timothy James DAVIS, Vincent DARMOHUSODO, Melissa Sue WONG, Victor SELCHAU
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Publication number: 20130040931Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).Type: ApplicationFiled: January 14, 2011Publication date: February 14, 2013Applicant: Amgen Inc.Inventors: Nick A. Paras, James Brown, Yuan Cheng, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Ana Elena Minatti, Thomas Nixey, Timothy Powers, Christopher M. Tegley, Qiufen Xue, Bryant Yang, Wenge Zhong
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Patent number: 8372865Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: GrantFiled: December 15, 2009Date of Patent: February 12, 2013Assignee: Roche Palo Alto LLCInventors: Jacob Berger, Joan Marie Caroon, Nancy Elisabeth Krauss, Keith Adrian Murray Walker, Shu-Hai Zhao, Francisco Javier Lopez-Tapia
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Patent number: 8367702Abstract: As a result of extensive studies on NAD(P)H oxidase inhibitors, the present inventors found that a quinolone derivative having, at the 2-position, an alkyl group substituted with a heteroatom or the like has an excellent NAD(P)H oxidase inhibitory activity, and accomplished the present invention. The compound of the present invention has a reactive oxygen species production inhibitory activity based on the NAD(P)H oxidase inhibitory activity, and therefore can be used as an agent for preventing and/or treating diabetes, impaired glucose tolerance, hyperlipidemia, fatty liver, diabetic complications and the like.Type: GrantFiled: September 25, 2008Date of Patent: February 5, 2013Assignee: Astellas Pharma Inc.Inventors: Kenichi Onda, Kenichiro Imamura, Fumie Sato, Hiroyuki Moritomo, Yasuharu Urano, Yuki Sawada, Naoki Ishibashi, Keita Nakanishi, Kazuhiro Yokoyama, Shigetada Furukawa, Kazuhiro Momose
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Patent number: 8367833Abstract: Disclosed is a process for producing 6-aryloxyquinoline derivatives useful as insecticides or fungicides for agricultural and horticultural use. The process comprises a cyclization reaction step of reacting an anthranilic acid derivative represented by general formula (1) with a kenone in the presence of an acid to obtain a quinolone derivative and a condensation reaction step of reacting the quinolone derivative with a halogen compound or an acid anhydride to obtain a quinoline derivative.Type: GrantFiled: July 13, 2009Date of Patent: February 5, 2013Assignees: Nippon Kayaku Co., Ltd., Meiji Seika Pharma Co., Ltd.Inventors: Yasuhito Kato, Shizuo Shimano, Akinori Morikawa, Hiroki Hotta, Kazumi Yamamoto, Nozomu Nakanishi, Nobuto Minowa, Hiroshi Kurihara
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Publication number: 20130029994Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: July 20, 2012Publication date: January 31, 2013Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
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Patent number: 8362253Abstract: Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.Type: GrantFiled: March 6, 2012Date of Patent: January 29, 2013Assignee: Vertex Pharmaceutical IncorporatedInventors: John DeMattei, Yushi Feng, Cristian L. Harrison, Adam R. Looker, Praveen Mudunuri, Stefanie Roeper, Yuegang Zhang
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Publication number: 20130018064Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I, wherein ring A, B1, B2, B3, L, R1, R4, ring Z, m and p of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: November 19, 2010Publication date: January 17, 2013Applicant: Amgen Inc.Inventors: Nick A. Paras, Yuan Cheng, Timothy Powers, James Brown, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Qiufen Xue, Bryant Yang
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Patent number: 8350028Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein R1 and R2 are as described herein and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists, useful for the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.Type: GrantFiled: March 5, 2009Date of Patent: January 8, 2013Assignee: Hofmann-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Patent number: 8349866Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of 1H-imidazo[4,5-c]quinolin-4-amines and 1H-imidazo[4,5-c]quinolin-4-amine-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: GrantFiled: July 31, 2009Date of Patent: January 8, 2013Inventor: Chongxi Yu
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Publication number: 20120329796Abstract: The present invention relates to compound (I) wherein: means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a —CN group, a hydroxyl group, a —COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a —NO2 group, a —NRiR2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n? is 1 or 2, R? is a hydrogen atom, a halogen atom or a group chosen among a (Ci-C3)alkyl group, a hydroxyl group, a —COOR1 group, a —NO2 group, a —NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (Ci-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a —CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating pathological or nonpathological conditions linked with premature aging.Type: ApplicationFiled: June 14, 2010Publication date: December 27, 2012Applicants: SOCIETE SPLICOS, UNIVERSITE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Jamal Tazi, Florence Mahuteau, Romain Najman, Didier Scherrer, Julien Santo
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Publication number: 20120329830Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein ring A, B1, B2, B3, L, R1, R4, R5 and m of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: November 19, 2010Publication date: December 27, 2012Applicant: Amgen Inc.Inventors: Yuan Cheng, Timothy Powers, Kate Ashton, James Brown, Scott Harried, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Thomas Nixey, Nick A. Paras, Steve F. Poon, David J. St. Jean, JR., Qiufen Xue, Wenge Zhong
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Patent number: 8338411Abstract: The present invention relates to the adenosine A3 receptor ligands of the general formula (I), within them favourably to the antagonists, to their salts, solvates, N-oxides and isomers, to the pharmaceutical compositions containing the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the use of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the preparation of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, as well as to the new intermediates of the general formula (II), (VI), (XI), (XII) and (XV), and to the preparation thereof.Type: GrantFiled: December 4, 2009Date of Patent: December 25, 2012Assignee: SanofiInventors: Edit Susan, Kinga Boer, Zoltan Kapui, Geza Timari, Sandor Batori, Zoltan Szlavik, Endre Mikus, Judit Vargane Szeredi, Michel Finet, Katalin Urban Szabo, Tibor Szabo