Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/304)
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Patent number: 8604063Abstract: The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.Type: GrantFiled: January 12, 2009Date of Patent: December 10, 2013Assignees: Centre National de Recherche Scientifique, Institut Curie, Universite Montpellier 2 sciences et TechniquesInventors: Jamal Tazi, David Grierson, Florence Mahuteau-Betzer, Pierre Roux
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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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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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Patent number: 8535903Abstract: The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity or as an enzymatic substrate for the detection of a nitroreductase activity and indicator of pH, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; U and V are N, N+R, CZ4, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic, preferably if U is CZ4, V is N or N+R and, if V is CZ4, U is N or N+R; and Z1, Z2, Z3 and Z4 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.Type: GrantFiled: July 29, 2010Date of Patent: September 17, 2013Assignee: BioMerieux, S.A.Inventors: Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
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Patent number: 8530461Abstract: 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: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
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Patent number: 8507536Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: August 10, 2012Date of Patent: August 13, 2013Assignee: Neurocrine Biosciences, Inc.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
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Publication number: 20130197228Abstract: The present invention relates to functionalised fluoroalkylfluorophosphate salts, in particular as ionic liquids, to the preparation thereof and to the use thereof.Type: ApplicationFiled: August 30, 2011Publication date: August 1, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Berthold Theo Hoge, Anne Julia Bader, Nikolai Mykola Ignatyev, Michael Schulte, Wolfgang Hierse, Waldemar Wiebe, Helge Willner
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Patent number: 8492410Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: February 6, 2013Date of Patent: July 23, 2013Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Patent number: 8470834Abstract: The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19, and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.Type: GrantFiled: August 19, 2009Date of Patent: June 25, 2013Assignees: Merck Sharp & Dohme Corp., Southern Research InstituteInventors: Cecil D. Kwong, F. George Njoroge, Subramaniam Ananthan, Feng Geng, Hollis S. Kezar, III, Joseph A. Maddry, John J. Piwinski, Robert C. Reynolds, John A. Secrist, III, Neng-Yang Shih
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Patent number: 8466161Abstract: The present invention relates to hydroxamate compounds of the following formula I, an isomer, pharmaceutically acceptable salt or hydrate thereof. The present invention also relates to a method for preparing the hydroxamate compounds, comprising allowing a compound of the following formula II to react with bromoaniline in the presence of an inorganic salt so as to prepare a compound of the following formula III.Type: GrantFiled: March 18, 2010Date of Patent: June 18, 2013Assignee: Chong Kun Dang Pharmaceutical Corp.Inventors: Sung Sook Lee, Kyung Joo Lee, Chang Sik Lee, Hyun Mo Yang, Do Hoon Kim, Dae Kyu Choi, Ho Jin Choi, Dal Hyun Kim, In Chang Hwang, Mi Jeong Kim, Byeong Hoon Han
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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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Patent number: 8461183Abstract: The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them. The compounds according to the invention are of quite particular therapeutic interest, notably for treating diabetes and/or dyslipidemias, as well as for preventing cardiovascular pathologies.Type: GrantFiled: May 26, 2009Date of Patent: June 11, 2013Assignee: GenfitInventors: Christophe Masson, Karine Caumont-Bertrand
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Publication number: 20130143910Abstract: A method and composition for treating cancer cells that targets fructose-1,6-biphosphataseenzymes (FBPs, type 1 and type 2) and/or their respective pathways. In one embodiment, inhibitors of FBPs or FBPs pathways are administered to a patient to treat brain cancer metastasis. In another embodiment, the present invention is particularly well suited for treating cancer cells that generally survive under glucose-independent conditions, or any other condition where cancer cells produce glucose via FBPs mediated pathways.Type: ApplicationFiled: November 14, 2012Publication date: June 6, 2013Inventor: Zhang Weihua
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Patent number: 8455398Abstract: Amide compounds, preparation methods and uses thereof. The structure of the compounds is represented as the general formula (I), in which the definitions of substituents are illuminated as description. The present amide compounds have broad spectrum activity of killing pests and are effective on lepidopteran pests including ostrinia nubilalis, sugarcane borer, adoxophyes orana fischer von reslerstamm, apple fruit borer, grapholitha inopinata, lymantri dispar l., cnaphalocrocis medinalis, ostrinia furnacalis, helicoverpa assulta, grapholitha inopinata, plutella xylostella, spodoptera exigua, prodenia litura etc., especially for plutella xylostella, spodoptera exigua. The present amide compounds can obtain good effect at very low dosage. At the same time, some compounds have good fungicidal activity which can be used to prevent rice blast, phytophthora infestans, cucumber downy mildew or grey mold of vegetables.Type: GrantFiled: June 3, 2009Date of Patent: June 4, 2013Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.Inventors: Changling Liu, Baoshan Chai, Hong Zhang, Jichun Yang, Zhinian Li, Yongwu Peng, Junfeng Wang, Jiao Wu, Shicun Ma, Miao Li
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Patent number: 8455654Abstract: A nanoscale pigment particle composition includes an organic benzimidazolone pigment, and a sterically bulky stabilizer compound, wherein the benzimidazolone pigment associates non-covalently with the sterically bulky stabilizer compound that is a substituted pyridine derivative; and the presence of the associated stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.Type: GrantFiled: July 18, 2011Date of Patent: June 4, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Rina Carlini, Darren Andrew Makeiff
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Patent number: 8450348Abstract: The present invention provides derivatives of squaric acid, in particular derivatives of 3,4-diamino-cyclobut-3-ene-1,2-dione and tautomers and isomers thereof, as a single stereoisomer or a mixture of stereoisomers, or as a pharmaceutically acceptable salt thereof. These compounds show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: GrantFiled: February 21, 2007Date of Patent: May 28, 2013Assignee: Forma TM, LLCInventors: Krishna K. Murthi, Roland Köstler, Chase Smith, Tilman Brandstetter, Arthur F. Kluge
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Publication number: 20130131056Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.Type: ApplicationFiled: January 15, 2013Publication date: May 23, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130119355Abstract: A styryl-based compound represented by Formula 1, a composition containing the styryl-based compound, and an organic light-emitting diode (OLED) including the styryl-based compound: The styryl-based compound may exhibit high heat resistance and thus an OLED including the same may have low driving voltage, high brightness, high efficiency, and long lifetime.Type: ApplicationFiled: September 11, 2012Publication date: May 16, 2013Applicant: SAMSUNG DISPLAY CO., LTD.Inventors: Sang-Hyun Han, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jin-O Lim, Soo-Yon Kim, Dae-Yup Shin, Jong-Hyuk Lee
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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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Patent number: 8426450Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor.Type: GrantFiled: May 23, 2012Date of Patent: April 23, 2013Assignee: Helsinn Healthcare SAInventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
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Publication number: 20130085278Abstract: The present invention provides methods for preparing 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine (compound A), which is useful for the treatment of depression and other CNS disorders. The present methods are useful for preparing compound A on large scale in manufacturing facilities.Type: ApplicationFiled: September 27, 2012Publication date: April 4, 2013Applicant: Hoffmann-La Roche IncInventor: Hoffmann-La Roche Inc
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Patent number: 8399492Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: November 11, 2011Date of Patent: March 19, 2013Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
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Patent number: 8389734Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: October 10, 2008Date of Patent: March 5, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Weichuan Caroline Chen, Paul Krenitsky, Andreas Termin, Dean Wilson
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Patent number: 8357808Abstract: The problem to be solved is to provide an important intermediate for production of an FXa inhibitor. The solution thereto is a process for industrially producing a compound (1) represented by the following formula (1): wherein Boc represents a tert-butoxycarbonyl group.Type: GrantFiled: September 9, 2011Date of Patent: January 22, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Takeo Koyama, Satoshi Kondo
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Patent number: 8338612Abstract: Because fluazinam is excellent as an active ingredient of pesticides and highly useful, it is desired to produce it efficiently in a proper form with simple operations at low cost in an environmentally friendly manner. The desired product is obtained in good yields with simple operations by using industrially advantageous reaction systems by a process comprising (1) a step of reacting ACTF and DCDNBTF in the presence of an alkali component, a solvent selected from the group consisting of ketones, nitriles, ethers and esters and a sufficient amount of water to substantially dissolve the alkali component, (2) a step of neutralizing or acidifying the reaction mixture with an acid and (3) a step of removing the solvent by distillation from the mixture containing fluazinam as the reaction product and the reaction solvent to precipitate crystals the product.Type: GrantFiled: July 29, 2008Date of Patent: December 25, 2012Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Shigeo Murai, Hiroshi Yoshizawa, Takeshi Ohshima, Katsuyoshi Murakami, Takayoshi Ando, Tadashi Nakamura, Norio Adachi, Akihiko Isogai
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Publication number: 20120316182Abstract: 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: June 8, 2012Publication date: December 13, 2012Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Jonathan Grey, Jianguo Cao, Zhijun Wang, Evan Rogers
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Patent number: 8329729Abstract: The invention provides named compounds of formula (I), wherein R4 is a N-substituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for the treatment of conditions mediated by M3 muscarinic receptors, such as chronic obstructive pulmonary disease is also disclosed.Type: GrantFiled: May 13, 2008Date of Patent: December 11, 2012Assignees: Astrazeneca AB, Pulmagen Therapeutics Synergy Ltd.Inventors: Richard James Bull, Rhonan Lee Ford, Antonio Mete
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Patent number: 8329705Abstract: The present invention relates to substituted [1,2,4]triazolo-[4,3-a]pyrazine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted [1,2,4]triazolo-[4,3-a]pyrazine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 29, 2010Date of Patent: December 11, 2012Assignee: ArQule, Inc.Inventor: Neil Westlund
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Publication number: 20120302551Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Indu T. Bharathan, Matthew Duffey, Amy Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
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Patent number: 8314130Abstract: The invention relates to certain compounds including substituted pyridines, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: October 1, 2009Date of Patent: November 20, 2012Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Junyi Zhang, Jun Jiang, Gary Bohnert, Nha Vo, Qinglin Che, Zhiqiang Xia, Lijun Sun
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Patent number: 8309735Abstract: The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and ? is a radical of formula (II) and their use for the inhibition of integrin.Type: GrantFiled: May 14, 2007Date of Patent: November 13, 2012Assignee: Shire Orphan Therapies GmbHInventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
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Patent number: 8288421Abstract: The invention relates to novel substituted 3-phenylamino-5-(3-aminophenyl)pyridines and corresponding pyrazines of formula (I), wherein A is CH or N, R1 represents C(?O)R9, S(?O)2R10, P(?O)(OR11)2, optionally substituted phenyl or optionally substituted heteroaryl, and the other substituents have the meaning described in the specification, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of neoplastic diseases and autoimmune diseases, and a method for the treatment of such a diseases.Type: GrantFiled: September 5, 2005Date of Patent: October 16, 2012Assignee: Basilea Pharmaceutica AGInventors: Martin Eberle, Felix Bachmann, Alessandro Strebel, Subho Roy, Goutam Saha, Godhuli Nandi
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Patent number: 8278336Abstract: The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: GrantFiled: November 21, 2008Date of Patent: October 2, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
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Publication number: 20120237589Abstract: The invention concerns lipid assemblies, liposomes having an outer surface comprising a mixture of anionic and cationic moieties; wherein at least a portion of the cationic moieties are imino moieties that are essentially charged under physiological conditions, and their use for serum resistant transfection of cells.Type: ApplicationFiled: July 2, 2010Publication date: September 20, 2012Applicant: MARINA BIOTECH, INC.Inventors: Steffen Panzner, Evgenios Siepi
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Patent number: 8247610Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, Y, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.Type: GrantFiled: October 17, 2008Date of Patent: August 21, 2012Assignees: Janssen Pharmaceutica N.V., Cellzome LimitedInventors: Chih Yung Ho, Yan Zhang, Umar S. M. Maharoof, John Harrison, Jeremy Major, Svenja Burckhardt, Alison Jones
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Publication number: 20120189614Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.Type: ApplicationFiled: July 10, 2010Publication date: July 26, 2012Applicant: Crobiotix, Inc.Inventors: Arnab Basu, Debra M. Mills, Norton P. Peet, John D. Williams
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Patent number: 8227492Abstract: The present invention relates to novel substituted sulfoximine derivatives of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.Type: GrantFiled: August 4, 2008Date of Patent: July 24, 2012Assignee: Cadila Healthcare LimitedInventors: Vrajesh B. Pandya, Pankaj Ramanbhai Patel
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Patent number: 8222634Abstract: The present invention relates to a novel anthracene derivative and an organic electronic device using the same. The organic electronic device according to the present invention shows excellent characteristics in efficiency, driving voltage, and life time.Type: GrantFiled: May 16, 2008Date of Patent: July 17, 2012Assignee: LG Chem, Ltd.Inventors: Dong-Hoon Lee, Jae-Chol Lee, Jae-Soon Bae, Jun-Gi Jang, Kong-Kyeom Kim, Dae-Woong Lee
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Publication number: 20120129205Abstract: The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity or as an enzymatic substrate for the detection of a nitroreductase activity and indicator of pH, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; U and V are N, N+R, CZ4, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic, preferably if U is CZ4, V is N or N+R and, if V is CZ4, U is N or N+R; and Z1, Z2, Z3 and Z4 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.Type: ApplicationFiled: July 29, 2010Publication date: May 24, 2012Applicant: bioMerieuxInventors: Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
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Patent number: 8178563Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: GrantFiled: May 4, 2007Date of Patent: May 15, 2012Assignee: IRM LLCInventors: Wenqi Gao, Jiqing Jiang, Yongqin Wan, Dai Cheng, Dong Han, Xu Wu, Shifeng Pan
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Patent number: 8163753Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.Type: GrantFiled: October 29, 2004Date of Patent: April 24, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidetsugu Tsubouchi, Hirofumi Sasaki, Motohiro Itotani, Yoshikazu Haraguchi, Shin Miyamura, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Kinue Ohguro, Takumi Sumida, Takeshi Hasegawa, Kazuho Tanaka, Isao Takemura
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Patent number: 8163930Abstract: The present invention relates to an improved process for the synthesis and purification of 3-chloro-N-(3-chloro-5-tri-fluoromethyl-2-pyridyl)-a,a,a-trifluoro-2,6-dinitro-p-toluidine (fluazinam) and other pyridinamines, which implements methyl isobutyl ketone (MIBK) as the reaction solvent. The process of the invention overcomes the drawbacks of prior art methods, by reducing the side reactions such as hydrolysis, eliminating the need for difficult and labor-intensive purification methods, and providing pure products in higher yields. The present invention relates to novel crystalline polymorphic forms fluazinam, and to mixtures of the polymorphs. The present invention also provides methods for preparing the novel polymorphs, as well as pharmaceutical compositions comprising same, and methods of using the polymorphs as pesticidal agents for combating noxious living organisms on agricultural and horticultural crops.Type: GrantFiled: November 23, 2006Date of Patent: April 24, 2012Assignee: Makhteshim Chemical Works Ltd.Inventors: Shlomi Cohen, Sharona Zamir
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Patent number: 8163778Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.Type: GrantFiled: November 24, 2008Date of Patent: April 24, 2012Assignee: Hoffmann-LA Roche Inc.Inventors: Wolfgang Haap, Paul Hebeisen, Eric Argirios Kitas, Bernd Kuhn, Peter Mohr, Hans Peter Wessel
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Patent number: 8134009Abstract: The invention relates to a process for the preparation of secondary nitroxide radicals from their corresponding secondary amines by oxidation with an organic peracid, comprising the steps a) adding to a reaction vessel a secondary amine, optionally together with an organic solvent and in one batch a base selected from the group consisting of alkali metal, alkaline earth metal or ammonium bicarbonates and alkaline earth metal or ammonium carbonates or mixtures thereof in the form of a solid together with water or as an aqueous slurry; b) dosing a peracid under stirring to the reaction mixture in an amount of 1.0 to 2.5 mol per mol of secondary amine; and c) isolating the organic phase.Type: GrantFiled: August 11, 2010Date of Patent: March 13, 2012Assignee: BASF SEInventors: Peter Nesvadba, Lucienne Bugnon, Martin Von Büren
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Patent number: 8133907Abstract: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12; R9 is selected from H —NR13C(O)R14 and —C(O)NR10R11; R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.Type: GrantFiled: July 14, 2006Date of Patent: March 13, 2012Assignee: Eli Lilly and CompanyInventors: Larry Chris Blaszczak, Brian Michael Mathes, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Brian Morgan Watson, Michael Robert Wiley
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Patent number: 8076370Abstract: Provided herein are substituted aromatic compounds, which are tRNA synthetase inhibitors, and hence can be used as antimicrobial agents. Compounds described herein can be used for the treatment or prevention of a condition caused by or contributed to by gram positive, gram negative, anaerobic bacteria or fungal organisms, more particularly against bacterium, for example, Staphylococci, Enterococci, Streptococci, Haemophilus, Moraxalla, Escherichia, Chlamydia, Mycoplasm, Legionella, Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus or Enterobactericeae, and fungal organisms, for example, Aspergillus, Blastomyces, Candida, Coccidiodes, Cryptococcus, Epidermophyton, Hendersonula, Histoplasma, Microsporum, Paecilomyces, Paracoccidiodes, Pneumocystis, Trichophyton, or Trichosporium. Processes for the preparation of these compounds, pharmaceutical compositions thereof, and methods of treating microbial infections are also provided.Type: GrantFiled: May 3, 2006Date of Patent: December 13, 2011Assignee: Ranbaxy Laboratories LimitedInventors: Biswajit Das, Jasbir Singh Arora, Shahadat Ahmed, Anish Bandyopadhyay, Rita Katoch, Santosh Haribhau Kurhade, Sujata Rathy, Soma Ghosh, Abhijit Datta Khoje, Arti Gujrati, Dilip J. Upadhyay
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Patent number: 8071616Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.Type: GrantFiled: January 25, 2010Date of Patent: December 6, 2011Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, William J. Scott, Bernd Riedl
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Publication number: 20110257183Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.Type: ApplicationFiled: April 22, 2011Publication date: October 20, 2011Inventors: Solomon Ungashe, Zheng Wei, J.J. Wright, Andrew Pennell, Brett Premack, Thomas Schall
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Patent number: 8039632Abstract: This invention relates to novel 2-amino-pyridine derivative useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: GrantFiled: November 12, 2007Date of Patent: October 18, 2011Assignee: Neurosearch A/SInventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Lene Teuber, Dan Peters, Dorte Strøbæk, Tina Holm Johansen, Palle Christophersen
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Patent number: 8034949Abstract: The present invention relates to a novel pyrrolidine compound, which has a potent antagonistic activity against central cannabinoid (CB1) receptor, having the formula [I]: wherein each of R1 and R2 is (A) optionally substituted aryl (or heteroaryl) group, or (B) both of the groups combine to form a group of the formula: one of R3 and R4 is hydrogen and another is hydrogen, hydroxyl, hydroxyalkyl, etc., or both of R3 and R4 combine to form oxo group, R5 is hydrogen or alkyl, Y is single bond, oxygen atom or a group of the formula: —N(R7)—, R6 is optionally substituted hydrocarbon group or optionally substituted cyclic group, R7 is alkyl or alkyloxycarbonylalkyl, provided that R6 is not 4-amino-5-chloro-2-methoxyphenyl group when Y is single bond and one of the R3 and R4 is hydrogen and another is hydroxymethyl, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 27, 2005Date of Patent: October 11, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yasunori Moritani, Shigeru Furukubu, Yasunori Tsuboi, Chieko Okagaki, Akira Oku, Naomitsu Hirano