Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/341.1)
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Patent number: 9174942Abstract: Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R1, R4, and R5 are defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosuppression associated with an infectious disease.Type: GrantFiled: April 29, 2014Date of Patent: November 3, 2015Assignee: NewLink Genetics CorporationInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Nicholas N. Vahanian, Charles J. Link, Judith Lalonde, George Prendergast, Alexander Muller, William Malachowski
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Patent number: 9159499Abstract: The present invention relates to the use of at least one imidazol derivative of formula I or 1-(3,3,4,4,4-pentafluorobutyl)-1H-imidazole, 1-(3,3,4,4,4-pentafluorobutyl)-1,2,3-triazole or 1-(2?-thioethyl)ethylimidazole as additive in dye-sensitized solar cells and to special electrolyte formulations and a dye-sensitized solar cell comprising at least one compound of formula I or 1-(3,3,4,4,4-pentafluorobutyl)-1H-imidazole, 1-(3,3,4,4,4-pentafluorobutyl)-1,2,3-triazole or 1-(2?-thioethyl)ethylimidazole.Type: GrantFiled: August 20, 2012Date of Patent: October 13, 2015Assignee: Merck Patent GmbHInventors: Kentaro Kawata, Tomohisa Goto, Hiroki Yoshizaki
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Publication number: 20150140449Abstract: Provided are a nonaqueous solvent containing a compound with high conductivity and low viscosity and a high-performance power storage device using the nonaqueous solvent. The power storage device includes an ionic liquid. The ionic liquid contains an anion and a cation having a five-membered heteroaromatic ring having one or more substituents. At least one of the substituents is a straight chain formed of four or more atoms and includes one or more of C, O, Si, N, S, and P.Type: ApplicationFiled: November 11, 2014Publication date: May 21, 2015Inventors: Jun ISHIKAWA, Satoshi SEO, Rie YOKOI, Hiroshi KADOMA, Tomoya HIROSE
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Patent number: 8993768Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).Type: GrantFiled: May 10, 2012Date of Patent: March 31, 2015Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: John A. Beutler, Stuart F. J. LeGrice, Craig Thomas, Jian-Kang Jiang, Suhman Chung, Jennifer Wilson
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Publication number: 20150087833Abstract: An alkyl phenyl sulfide derivative represented by the general formula [I] or an agriculturally acceptable salt thereof, and a pest control agent containing the derivative or the salt as an active ingredient. [in the above formula, R1 is, for example, a C1˜C6 alkyl group which is mono- or poly-substituted with halogen atom; R2 is, for example, a halogen atom or a C1˜C6 alkyl group; R3 is, for example, a hydrogen atom or a halogen atom; and R4 is, for example, a hydrogen atom or a C1˜C12 alkyl group.] The derivative or the salt has an excellent pest control effect.Type: ApplicationFiled: April 11, 2013Publication date: March 26, 2015Applicants: IHARA CHEMICAL INDUSTRY CO., LTD., KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Kei Domon, Keiji Toriyabe, Yutaka Ogawa, Junichiro Bessho, Kei Kawamoto, Akira Watanabe, Masaaki Komatsu, Takeshi Matsuda, Seisuke Ito
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Publication number: 20150080445Abstract: Disclosed herein is a pharmaceutical composition comprising (3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl)methanol and methods of using the composition to treat chronic pain.Type: ApplicationFiled: November 21, 2014Publication date: March 19, 2015Inventor: Daniel W. Gil
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Patent number: 8975289Abstract: This invention describes new antifungal compounds that are aralkyl benzyl ethers of the formula (I): where Ar represents aryl, imidazolil, 1,2,4-triazolyl, benzimidazolil; R1, R2, R4 and R5 are independently hydrogen, halogen, C1-6 alkyl; R3 represents halogen, C1-6alkyl or O—R? where R? represents hydrogen or lower alkyl; R6 represents aryl, substituted aryl, trifluoromethyl, trichloromethyl or O—R? where R? represents hydrogen or lower alkyl; being the substituents of the aryl a halogen or a radical tetrazolyl; n and m represent independently an integer between 0 and 5; With the proviso that when Ar is imidazolil, R3 is chlorine, R6 is p-phenyl and R1, R2, R4 and R5 are hydrogen, n must be different from 2. When n and m are not 0 and 1, R3 or R6 can be represented by substituents not necessarily equal.Type: GrantFiled: August 27, 2010Date of Patent: March 10, 2015Assignee: Biolab Sanus Farmaceutical Ltda.Inventors: Artur Franz Keppler, Sérgio Luiz Sacurai, Marcio Henrique Zaim, Carlos Eduardo da Costa Touzarim
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Patent number: 8962599Abstract: Therapeutic compositions comprising substituted imidazole or imidazolium compounds may be used for a number of medical purposes, such as treatment of undesirable conditions or diseases, including disease or conditions related to bone, cancer, and/or pain.Type: GrantFiled: September 9, 2014Date of Patent: February 24, 2015Assignee: Antecip Bioventures II LLCInventor: Herriot Tabuteau
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Patent number: 8859160Abstract: The invention relates to a monomer (6, 14) carrying an imidazole-type heterocycle (3). According to the invention, the chemical structure of said monomer (6, 14) comprises at least one unit of formula (I) wherein R1 comprises an alkenyl grouping and R2 comprises a grouping for protecting one of the nitrogen atoms of the heterocycle. The invention also relates to a monomer carrying a benzimidazole-type heterocycle, and to protected polymers obtained from said monomers, deprotected polymers produced by the protected polymers, a proton exchange membrane based on deprotected polymers, and a fuel cell provided with said membrane. Furthermore, the invention relates to methods for producing the above-mentioned monomers and polymers.Type: GrantFiled: May 29, 2007Date of Patent: October 14, 2014Assignees: Peugeot Citroen Automobiles SA, CNRS (Centre National de la Recherche Scientifique)Inventors: Xavier Glipa, Bruno Ameduri, Louis Delon, Deborah Jones, Jacques Roziere, Guillaume Frutsaert
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Publication number: 20140287640Abstract: Disclosure of functionalized ionic liquids. Use of disclosed ionic liquids as solvent for carbon dioxide. Use of disclosed ionic liquids as flame retardant. Use of disclosed ionic liquids for coating fabric to obtain flame retardant fabric.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: Materials Modification IncInventors: Humcha Krishnamurthy Hariprakasha, Krishnaswamy Kasthuri Rangan, Tirumalai Srinivas Sudarshan
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Publication number: 20140272601Abstract: Salts with formula X?M+ wherein M+ is Li, Na, K, an ammonium, a phosphonium, an imidazolium, a pyridinium, or a pyrazolium and X? is an anion formed from covalent linking of two negative moieties to a positive onium-type core are provided. Also provided are electrolytes and batteries produced from these salts.Type: ApplicationFiled: November 16, 2012Publication date: September 18, 2014Inventors: Erlendur Jónsson, Michel Bernard Armand, Jens Patrik Johansson
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Publication number: 20140249181Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).Type: ApplicationFiled: May 10, 2012Publication date: September 4, 2014Applicant: The united States of America, as represented by the Secretary, Department of Health and Human ServInventors: John A. Beutler, Stuart F.J. LeGrice, Craig Thomas, Jian-Kang Jiang, Suhman Chung, Jennifer Wilson
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Publication number: 20140243362Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR? wherein R1 to R7 are as defined in claim 35.Type: ApplicationFiled: September 25, 2012Publication date: August 28, 2014Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le
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Publication number: 20140221330Abstract: An objective of the present invention is to provide a novel NDM (New Delhi metallo-?-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of ?-lactam antibiotics that have been inactivated as a result of decomposition by NDM.Type: ApplicationFiled: July 26, 2012Publication date: August 7, 2014Inventors: Akihiro Morinaka, Kazunori Maebashi, Takashi Ida, Muneo Hikida, Mototsugu Yamada, Takao Abe
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Patent number: 8791271Abstract: Process for preparing polymeric, ionic compounds comprising imidazolium groups, wherein an ?-dicarbonyl compound, an aldehyde, at least one amino compound having at least two primary amino groups, if appropriate an amino compound having only one primary amino group and a protic acid, where the carbonyl groups of the ?-dicarbonyl compound and of the aldehyde may, if appropriate, also be present as hemiacetal, acetal or hemiketal or ketal, are reacted with one another.Type: GrantFiled: December 10, 2009Date of Patent: July 29, 2014Assignee: BASF SEInventors: Michael Siemer, Sebastian Koltzenburg, Michael Klein
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Publication number: 20140190567Abstract: The present invention relates to the use of at least one imidazol derivative of formula I or 1-(3,3,4,4,4-pentafluorobutyl)-1H-imidazole, 1-(3,3,4,4,4-pentafluorobutyl)-1,2,3-triazole or 1-(2?-thioethyl)ethylimidazole as additive in dye-sensitized solar cells and to special electrolyte formulations and a dye-sensitized solar cell comprising at least one compound of formula I or 1-(3,3,4,4,4-pentafluorobutyl)-1H-imidazole, 1-(3,3,4,4,4-pentafluorobutyl)-1,2,3-triazole or 1-(2?-thioethyl)ethylimidazole.Type: ApplicationFiled: August 20, 2012Publication date: July 10, 2014Applicant: MERCK PATENT GMBHInventors: Kentaro Kawata, Tomohisa Goto, Hiroki Yoshizaki
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Publication number: 20140194620Abstract: The present invention relates to a precursor of positron emission tomography (PET) radioactive medical supplies, a preparation method thereof, and an application thereof, and more specifically, to a precursor having a tetravalent organic salt leaving group, a preparation method, and a method for preparing desired PET radioactive medical supplies in a high radiochemical yield within a short preparation time by introducing 18F using the same through a single step. The precursor having a tetravalent organic salt leaving group of the present invention can simplify the known complex multistep preparation of radioactive medical supplies into a single step, can save production costs because an excessive amount of a phase transfer catalyst is not required, facilitates separation of a compound after reaction, and enables rapid reaction velocity. The features are appropriate for the mass production of PET radioactive medical supplies by an automated synthesis system.Type: ApplicationFiled: May 11, 2012Publication date: July 10, 2014Applicant: FUTURECHEM CO., LTD.Inventors: Dae-Yoon Chi, Byoung-Se Lee, Chansoo Park, Min-Hyung Lee, Hyojin Cha, Woojin Cho, Heewon Kang, Kyunghun Kim
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Publication number: 20140178349Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.Type: ApplicationFiled: December 16, 2013Publication date: June 26, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono
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Patent number: 8748469Abstract: Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R1, R4, and R5 are defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine -2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.Type: GrantFiled: April 24, 2009Date of Patent: June 10, 2014Assignees: NewLink Genetics Corporation, Lankeanau Institute for Medical ResearchInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Nicholas N. Vahanian, Charles J. Link
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Patent number: 8722720Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.Type: GrantFiled: October 27, 2010Date of Patent: May 13, 2014Assignee: NewLink Genetics CorporationInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani
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Publication number: 20140127285Abstract: The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.Type: ApplicationFiled: October 28, 2013Publication date: May 8, 2014Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventor: Jung-Mo Ahn
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Patent number: 8673955Abstract: Imidazole derivatives of formula (I): wherein R1, R2a, R2b, A, V and W are as defined in the description, as inhibitors of fructose-1,6-bisphosphatase, their preparation process and their use in the prevention or treatment of diabetes, and other diseases where the inhibition of gluconeogenesis, control of blood glucose levels, reduction in glycogen stores, or reduction in insulin levels is beneficial and diseases related to the insulin resistance syndrome.Type: GrantFiled: July 19, 2006Date of Patent: March 18, 2014Assignee: Merck Patent GmbHInventors: Denis Carniato, Gérard Moinet, Gérard Botton, Annick Arbellot De Vacqueur, Annick Audet
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Patent number: 8673956Abstract: Imido-acid salts and compositions containing imido-acid salts are described herein. Methods of their preparation and use are also described herein. The methods of using the imido-acid salts include the reduction of volatile compounds from gas and liquid streams and the delivery of pharmaceutical agents to subjects.Type: GrantFiled: November 29, 2012Date of Patent: March 18, 2014Assignee: Board of Trustees of The University of AlabamaInventor: Jason E. Bara
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Publication number: 20140012012Abstract: A polyether compound containing oxirane monomer units in an average number per molecule of 10 to 100, wherein the polyether compound contains repeating units which are represented by the general formula (2) as at least part of the oxirane monomer units is provided. According to the present invention, it is possible to provide a polymer material which has suitable fluidity and is excellent in ion conductivity. (R1 to R4 respectively independently indicate a hydrogen atom or C1 to C3 alkyl group, and R2 and R3 may be bonded with each other. Further, X? is an anion which is comprised of 2 to 25 atoms.Type: ApplicationFiled: March 30, 2012Publication date: January 9, 2014Applicant: ZEON CORPORATIONInventors: Shigetaka Hayano, Yasuo Tsunogae
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Patent number: 8623942Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.Type: GrantFiled: March 9, 2010Date of Patent: January 7, 2014Assignee: Nippon Soda Co., Ltd.Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
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Patent number: 8592498Abstract: Disclosed herein are a reaction method and a production method of an organic compound which are capable of achieving high reaction selectivity according to the purpose and a high production rate of a target substance. The methods include at least two fluids, wherein at least one kind of the fluids is a fluid containing at least one organic compound and at least one kind of the fluids other than the above fluid is a fluid containing at least one reactant in the form of a liquid or solution, and the respective fluids join together in a thin film fluid foamed between processing surfaces arranged to be opposite to each other so as to be able to approach to and separate from each other, at least one of which rotates relative to the other, whereby an organic reaction is performed in the thin film fluid.Type: GrantFiled: September 11, 2008Date of Patent: November 26, 2013Assignee: M. Technique Co., Ltd.Inventor: Masakazu Enomura
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Patent number: 8541598Abstract: This invention relates to ionic liquid (ILs) solvents for chemical synthesis based on an alkyl-imidazolium cation core containing ionic liquids which have enhanced biodegradability and reduced toxicity relative to existing imidazolium bases ILs such as 1-butyl-3-methylimidazolium (bmmim) salts. Many of the described ILs produce a score of over 60% biodegradability over 28 days in a biodegradability test such as the Sturm Test, the Closed Bottle Test (OECD 301D) or the CO2 Headspace Test (ISO 14593). The ILs of the invention comprise an alkyl substituted imidazolium cationic core having a —C?OX— side chain in the 3-position of the imidazole ring, wherein X?O, NH, N or S and an associated counteranion characterized in that the —C?OX side chain comprises at least one ether linkage. The biodegradable and non-toxic IL may be used as green solvents for the chemical, pharmaceutical, biofuel and biomass industries. The ILs of the invention are particularly useful in hydrogenation, pericyclic and metathesis reactions.Type: GrantFiled: August 21, 2008Date of Patent: September 24, 2013Assignee: Dublin City UniversityInventors: Nick Gathergood, Saibh Morrissey, Bruce Pegot
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Patent number: 8492422Abstract: The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: September 15, 2011Date of Patent: July 23, 2013Assignee: Allergan, Inc.Inventors: Mohammad I. Dibas, Ken Chow, Liming Wang, Michael E. Garst, John E. Donello, Daniel W. Gil
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Publication number: 20130143939Abstract: Imido-acid salts and compositions containing imido-acid salts are described herein. Methods of their preparation and use are also described herein. The methods of using the imido-acid salts include the reduction of volatile compounds from gas and liquid streams and the delivery of pharmaceutical agents to subjects.Type: ApplicationFiled: November 29, 2012Publication date: June 6, 2013Applicant: BOARD OF TRUSTEES OF THE UNIVERSITY OF ALABAMAInventor: Board of Trustees of the University of Alabama
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Publication number: 20130123338Abstract: The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.Type: ApplicationFiled: May 12, 2011Publication date: May 16, 2013Applicant: Protiva Biotherapeutics, Inc.Inventors: James Heyes, Mark Wood, Alan Martin
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Patent number: 8399463Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.Type: GrantFiled: September 19, 2011Date of Patent: March 19, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 8338619Abstract: A method to obtain a new crystalline form of the Zoledronic acid, characterized by its X-rays diffractogram as well as by its spatial atomic distribution in the red crystalline and its curves of thermal analysis. There is also included a method to obtain this crystalline form, which includes the synthesis of the corresponding acid and the pharmaceutical composition this crystalline form comprises.Type: GrantFiled: February 4, 2010Date of Patent: December 25, 2012Assignee: Gador S.A.Inventors: Rafael Alberto Labriola, Dora Graciela Tombari, Adriana Vechhioli
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Patent number: 8318767Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: GrantFiled: December 15, 2011Date of Patent: November 27, 2012Assignees: Merck Sharp & Dohme Corp, Albany Molecular Research, Inc.Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Jian Liu, Michael M.-C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
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Publication number: 20120232286Abstract: An azole derivative according to the invention is represented by Formula (I), wherein each of Ra and Rb denotes a hydrogen atom, or a C1-C6 alkyl group, a C2-C6 alkenyl group or a C2-C6 alkynyl group; Ra and Rb may be substituted with Xa or Xb which is a halogen atom; each of na and nb denotes 0 or the number of Xa- or Xb-substituted hydrogen atoms among the hydrogen atoms in Ra or Rb; each Y denotes a halogen atom, a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C1-C4 alkoxy group, a C1-C4 haloalkoxy group, a phenyl group, a cyano group or a nitro group; m denotes 0 to 5; and A denotes a nitrogen atom or a methyne group. As a result, an azole derivative contained as an active ingredient in an agro-horticultural agent having an excellent controlling effect on diseases can be provided.Type: ApplicationFiled: December 7, 2010Publication date: September 13, 2012Applicant: KUREHA CORPORATIONInventors: Nobuyuki Araki, Toru Yamazaki, Nobuyuki Kusano, Eiyu Imai, Hisashi Kanno, Masaru Mori, Taiji Miyake
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Patent number: 8252944Abstract: There is provided a preparation process in which a N—H group of a heteroaromatic ring compound having a N—H group in its ring is converted directly to a N—Rf group at a high reaction efficiency without using a catalyst. The preparation process is a process for preparing a compound comprising a heteroaromatic ring structure having a N—Rf group (—Rf is a fluorine-containing organic group) in its ring and is characterized in that the heteroaromatic ring compound having a N—H group in its ring is allowed to react with fluoroalkene in the absence of an alkali metal.Type: GrantFiled: January 13, 2012Date of Patent: August 28, 2012Assignee: Daikin Industries, Ltd.Inventors: Yuzo Komatsu, Haruhiko Mohri, Hirokazu Aoyama
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Publication number: 20120196908Abstract: This invention describes new antifungal compounds that are aralkyl benzyl ethers of the formula (I): wherein: Ar represents aryl, imidazolil, 1,2,4-triazolyl, benzimidazolil; R1, R2, R4 and R5 are independently hydrogen, halogen, C1-6 alkyl; R3 represents halogen, C1-6alkyl or O—R? where R? represents hydrogen or lower alkyl; R6 represents aryl, substituted aryl, trifluoromethyl, trichloromethyl or O—R? where R? represents hydrogen or lower alkyl; being the substituents of the aryl a halogen or a radical tetrazolyl; n and m represent independently an integer between 0 and 5; With the proviso that when Ar is imidazolil, R3 is chlorine, R6 is p-phenyl and R1, R2, R4 and R5 are hydrogen, n must be different from 2. When n and m are not 0 and 1, R3 or R6 can be represented by substituents not necessarily equal.Type: ApplicationFiled: August 27, 2010Publication date: August 2, 2012Applicant: BIOLAB SANUS FARMACEUTICA LTDA.Inventors: Artur Franz Keppler, Sérgio Luiz Sacurai, Marcio Henrique Zaim, Carlos Eduardo da Costa Touzarim
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Publication number: 20120197005Abstract: The invention provides a method for producing a mixture of amorphous compounds, the method comprising supplying a solution containing the compounds; and allowing at least a portion of the solvent of the solution to evaporate while preventing the solute of the solution from contacting a nucleation point. Also provided is a method for transforming solids to amorphous material, the method comprising heating the solids in an environment to form a melt, wherein the environment contains no nucleation points; and cooling the melt in the environment.Type: ApplicationFiled: January 30, 2012Publication date: August 2, 2012Applicant: UCHICAGO ARGONNE, LLCInventors: Chris J. Benmore, Johann R. Weber
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Patent number: 8212053Abstract: There is provided a preparation process in which a N—H group of a heteroaromatic ring compound having a N—H group in its ring is converted directly to a N—Rf group at a high reaction efficiency without using a catalyst. The preparation process is a process for preparing a compound comprising a heteroaromatic ring structure having a N—Rf group (—Rf is a fluorine-containing organic group) in its ring and is characterized in that the heteroaromatic ring compound having a N—H group in its ring is allowed to react with fluoroalkene in the absence of an alkali metal.Type: GrantFiled: December 11, 2006Date of Patent: July 3, 2012Assignee: Daikin Industries, Ltd.Inventors: Yuzo Komatsu, Haruhiko Mohri, Hirokazu Aoyama
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Patent number: 8202513Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: GrantFiled: October 3, 2008Date of Patent: June 19, 2012Assignee: Bionomics LimitedInventors: Bernard Luke Flynn, Jonathan Bayldon Baell, Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Andrew John Harvey, Jorgen Alvar Mould, Dharam Paul
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Publication number: 20120116097Abstract: There is provided a preparation process in which a N—H group of a heteroaromatic ring compound having a N—H group in its ring is converted directly to a N—Rf group at a high reaction efficiency without using a catalyst. The preparation process is a process for preparing a compound comprising a heteroaromatic ring structure having a N—Rf group (—Rf is a fluorine-containing organic group) in its ring and is characterized in that the heteroaromatic ring compound having a N—H group in its ring is allowed to react with fluoroalkene in the absence of an alkali metal.Type: ApplicationFiled: January 13, 2012Publication date: May 10, 2012Applicant: DAIKIN INDUSTRIES, LTD.Inventors: Yuzo KOMATSU, Haruhiko MOHRI, Hirokazu AOYAMA
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Publication number: 20120088788Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: ApplicationFiled: December 15, 2011Publication date: April 12, 2012Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Jian Liu, Michael M.C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
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Patent number: 8153676Abstract: The invention relates to a compound of formula A-R—X or pharmaceutically acceptable salts thereof which can be used for producing a pharmaceutical preparation suitable for preventing or treating cancerous diseases, pathological consequences of alcohol abuse, viral hepatitis, steatohepatitis, acute and chronic pancreatitis, toxic renal diseases, hepatic insulin resistance in diabetes mellitus, hepatic damage in Wilson's disease and sideroses and/or ischaemic reperfusion damage, as an antidote against environmental toxins and medicament intoxication in order to extend the resistance time of medicaments in organisms, or for combating toxic side effects in the administration of chemotherapeutics. In the formula R is an aliphatic or aromatic C6- to C40-hydrocarbon radical which has a hydrophilic end A, and X is a radical having at least one free electron pair of a carbon or heteroatom and/or ?-electrons.Type: GrantFiled: April 27, 2007Date of Patent: April 10, 2012Inventors: Dieter Mueller-Enoch, Thomas Haehner
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Publication number: 20120071506Abstract: The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification, and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms.Type: ApplicationFiled: November 23, 2011Publication date: March 22, 2012Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20120042778Abstract: A sulfur dioxide absorbent comprising an ionic liquid comprised of alkyl ether-substituted imidazolium cation and an alkanesulfonate anion moieties possesses a high thermal/chemical stability, high SO2 absorption rate and low regeneration temperature, and is useful for an effective separation of SO2 from a combustion exhaust gas mixture or the like.Type: ApplicationFiled: April 20, 2011Publication date: February 23, 2012Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Kwang Deog JUNG, Hong Gon KIM, Chang Soo KIM, Hoon Sik KIM, Minserk CHEONG, Sung Yun HONG
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Patent number: 8119680Abstract: Novel compounds, compositions, and kits are provided. Methods of modulating A? levels, and methods of treating a disease associated with aberrant A? levels are also provided.Type: GrantFiled: September 3, 2010Date of Patent: February 21, 2012Assignee: Neurogenetic Pharmaceuticals, Inc.Inventors: Soan Cheng, Daniel D Comer, Long Mao, Guity P Balow, David Pleynet
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Publication number: 20120029041Abstract: 2-Aryl imidazoline derivatives are provided that are useful as anti-obesity agents or the like. A compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 each independently represent a hydrogen atom, halogen, C1-6alkyl, or the like; R3a, R3b, R4a and R4b each independently represent a hydrogen atom, C1-6alkyl, or haloC1-6alkyl; and Ar represents aryl, wherein the aryl may be substituted with 1 to 3 substituents such as halogen, cyano, C1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, haloC1-6alkyloxy, hydroxy, amino, monoC1-6alkylamino, diC1-6alkylamino, and C1-6alkyloxy-carbonyl.Type: ApplicationFiled: April 21, 2010Publication date: February 2, 2012Applicant: MSD K.K.Inventors: Yuji Haga, Minoru Moriya, Toshiyuki Takahashi
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Publication number: 20120020915Abstract: Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.Type: ApplicationFiled: January 13, 2011Publication date: January 26, 2012Applicants: QUEENS UNIVERSITY AT KINGSTON, THE SIR MORTIMER B. DAVIS JEWISH GENERAL HOSPITAL, OSTA BIOTECHNOLOGIES, INC.Inventors: Ajay Gupta, Hyman M. Schipper, Moulay Alaoui-Jamali, Walter A. Szarek, Kanji Nakatsu, Jason Z. Vlahakis
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Patent number: 8093403Abstract: The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I); and a Reformatsky reagent in a stable form suitable for the process. In the present invention, a compound represented by the general formula (I) is produced by reducing a specific ?-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.Type: GrantFiled: December 28, 2009Date of Patent: January 10, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun-Ichi Kawakami, Shigeru Nuwa, Shokyo Miki
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Publication number: 20120004230Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.Type: ApplicationFiled: September 19, 2011Publication date: January 5, 2012Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20110294862Abstract: A method for the prevention and treatment of hypotension and shock due to low peripheral resistance, comprising administering to a mammal in need thereof an effective amount of a certain imidazole derivative or pharmaceutically acceptable ester or salt thereof, and a method for the treatment of cardiopulmonary resuscitation, comprising administering to a mammal in need thereof an effective amount of a certain imidazole derivative or pharmaceutically acceptable ester or salt thereof.Type: ApplicationFiled: April 28, 2011Publication date: December 1, 2011Inventors: Riitta Heino, Tiina Leino, Tarja Lehtimäki