Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/304)
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Publication number: 20110230465Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: September 16, 2010Publication date: September 22, 2011Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBHInventors: Timothy STAMMERS, Xavier BARBEAU, Pierre BEAULIEU, Megan BERTRAND-LAPERLE, Christian BROCHU, Paul J. EDWARDS, Pasquale FORGIONE, Cédrickx GODBOUT, Oliver HUCKE, Marc-André JOLY, Serge LANDRY, Olivier LEPAGE, Julie NAUD, Marc PESANT, Martin POIRIER, Maude POIRIER, Bounkham THAVONEKHAM
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Patent number: 8022018Abstract: Corrosion of metallic tubulars in an oil, gas or geothermal well may be inhibited by introducing into the well a dithiazine or dithiazine of the formula: wherein R is selected from the group consisting of a C1 to C12 saturated or unsaturated hydrocarbyl group or a C1 to C10 ?-hydroxy saturated or unsaturated hydrocarbyl group; R1 is selected from the group consisting of a C1-C24 straight chain or branched alkyl group or a C1-C24 arylalkyl; R2 is selected from the group consisting of X-R4-X, R4 being a C1-C6 alkyl group; and X is chlorine, bromine or iodine. The dithiazine may he isolated from a whole spent fluid formed by reaction of hydrogen sulfide and a triazine. Alternately, the whole spent fluid containing the dithiazine may be introduced into the well. The dithiazines of formulae (II) and (III) are quaternized derivatives of the dithiazine of formula (I).Type: GrantFiled: August 24, 2010Date of Patent: September 20, 2011Assignee: Baker Hughes IncorporatedInventor: Grahame Nigel Taylor
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Patent number: 8022017Abstract: Corrosion of metallic tubulars in an oil, gas or geothermal well may be inhibited by introducing into the well a dithiazine of the formula: wherein R is selected from the group consisting of a C1 to C10 saturated or unsaturated hydrocarbyl group or a C1 to C10 ?-hydroxy saturated or unsaturated hydrocarbyl group. The dithiazine may be isolated from a whole spent fluid formed by reaction of hydrogen sulfide and a triazine. Alternately, the whole spent fluid containing the dithiazine may be introduced into the well. In addition, the dithiazine or whole spent fluid may be formulated with at least one component selected from alkyl, alkylaryl or arylamine quaternary salts; mono or polycyclic aromatic amine salts; imidazoline derivative or a quaternary salt thereof; a mono-, di- or trialkyl or alkylaryl phosphate ester; or a monomeric or oligomeric fatty acid.Type: GrantFiled: December 21, 2009Date of Patent: September 20, 2011Assignee: Baker Hughes IncorporatedInventor: Grahame Nigel Taylor
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Patent number: 8003654Abstract: The invention relates to novel sulfonamide compounds of the formula (I) and their use as orexin receptor antagonists.Type: GrantFiled: April 10, 2007Date of Patent: August 23, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Cornelia Zumbrunn Acklin
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Publication number: 20110201816Abstract: The present inventors succeeded in isolating GWT1 (PfGWT1), which is one of the enzymes involved in GPI biosynthesis in the malaria parasite P. falciparum. In addition, the inventors revealed that degenerate mutant DNAs, with a lower AT content than the DNA encoding the PfGWT1 protein, can complement the phenotype of GWT1-deficient yeast. Based on the findings, the present invention provides the GWT1 protein of malaria parasites and the use of the protein in methods of screening for antimalarial drugs. The present invention also provides degenerate mutant DNAs encoding proteins involved in GPI biosynthesis, and which have a lower AT content than the original DNAs. The present invention also provides methods of screening for antimalarial drugs which use the degenerate mutant DNAs.Type: ApplicationFiled: March 4, 2011Publication date: August 18, 2011Applicant: EISAI R&D MANAGEMENT CO., LTDInventors: Katsura Hata, Kaoru Ogawa, Itaru Tsukada, Kazutaka Nakamoto, Koji Sagane, Keigo Tanaka, Kappei Tsukahara, Toshihiro Horii
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Publication number: 20110201818Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: September 24, 2008Publication date: August 18, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takashi Ichikawa, Benjamin Jones, Andre A. Kiryanov, Christopher McBride, Srinivasa Reddy Natala, Zhe Nie, Sheldon X. Cao, Betty Lam, Victoria Feher, Stephen W. Kaldor, Yan Liu, Jeffrey A Stafford
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Patent number: 7999109Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: December 17, 2009Date of Patent: August 16, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
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Patent number: 7977332Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: December 2, 2004Date of Patent: July 12, 2011Assignee: FMC CorporationInventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
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Publication number: 20110160460Abstract: The invention concerns novel ionic compounds with low melting point whereof the onium type cation having at least a heteroatom such as N, 0, S or P bearing the positive charge and whereof the anion includes, wholly or partially, at least an ion imidide such as (FXI0)N—(OX2F) wherein X1 and X2 are identical or different and comprise SO or PF, and their use as solvent in electrochemical devices. Said composition comprises a salt wherein the anionic charge is delocalised, and can be used, inter alia, as electrolyte.Type: ApplicationFiled: March 7, 2011Publication date: June 30, 2011Applicants: ACEP INC., CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE MONTREALInventors: Christophe Michot, Michel Armand, Michel Gauthier, Nathalie Ravet
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Patent number: 7951820Abstract: This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.Type: GrantFiled: July 25, 2006Date of Patent: May 31, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Ronald Knegtel, Hayley Binch, Julian M. C. Golec, Pan Li, Jean-Damien Charrier
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Publication number: 20110124873Abstract: The invention relates to bis(perfluoroalkyl)phosphinous acids, bis(perfluoroalkyl)thiophosphinous acids and derivatives, the synthesis thereof and the use thereof, in particular for the synthesis of air-stable metal complexes for catalytic processes.Type: ApplicationFiled: July 10, 2009Publication date: May 26, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Berthold Hoge, Anne Julia Bader, Boris Kurscheid, Nikolai Ignatyev, Emil Ferdinand Aust
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Patent number: 7943626Abstract: Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(arylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical compositions thereof, are provided for use as inhibitors of with MEK kinase.Type: GrantFiled: January 5, 2010Date of Patent: May 17, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, Stephen W. Kaldor
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Patent number: 7939666Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers.Type: GrantFiled: May 4, 2006Date of Patent: May 10, 2011Assignee: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
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Publication number: 20110098313Abstract: 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: October 20, 2010Publication date: April 28, 2011Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Patent number: 7932395Abstract: This invention provides compounds of Formula I, methods for their preparation and use for preparing compounds of Formula II wherein R1, R2, R3, R5, R6, X and n are as defined in the disclosure. This invention also discloses preparation of compounds of Formula III wherein R1, R2, R7, R8, R9 and n are as defined in the disclosure. This invention also pertains to certain compounds of Formula 4 and 6 used to prepare compounds of Formula I. wherein R1, R2, R5, X and n are as defined in the disclosure.Type: GrantFiled: October 13, 2009Date of Patent: April 26, 2011Assignee: E. I. du Pont de Nemours and CompanyInventor: Gary David Annis
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Patent number: 7932271Abstract: Provided is a compound capable of inhibiting production or secretion of ? amyloid protein. A compound represented by the following formula (1): (wherein, R1 represents a heterocyclic group which may have a substituent, R2 represents a cyclic hydrocarbon group which may have a substituent or a heterocyclic group which may have a substituent, R3 represents a cyclic hydrocarbon group which may have a substituent or a heterocyclic group which may have a substituent, R4 represents a hydrogen atom or a C1-6 alkyl group, and X represents —S—, —SO— or —SO2—); an N-oxide or S-oxide thereof; a salt thereof; or a solvate thereof; and a medicament containing any of them.Type: GrantFiled: June 29, 2004Date of Patent: April 26, 2011Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hideki Kubota, Takanori Yasukouchi, Satoru Miyauchi, Kayoko Motoki, Masanori Saito, Hitoshi Iimori
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Patent number: 7928264Abstract: The present invention relates to a compound of the formula [I]: wherein (a), in which —Y—, R4, R5 and R6 are4 R5 each as defined in the description, etc., R1 is hydrogen, halogen, lower alkyl, hydroxy, etc., R2 is hydrogen, lower alkyl or hydroxy(lower)alkyl, R3 is hydrogen or an amino protective group, 20R7 is hydrogen, lower alkyl, cyclo(lower)alkyl, lower R9 alkenyl, —Z—R9 or (b), in which —Z— is —0—, —S—, R9 —SO— or —SO2—, and each R9 is independently hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R8 is -D-E-R10, in which -D- is —CONHSO2— or —S02NHCO—, E is bond or lower alkylene, and R10 is halogen, cyano, carboxy, etc., or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of ulcer, overactive bladder, and the like.Type: GrantFiled: September 20, 2005Date of Patent: April 19, 2011Assignee: Astellas Pharma Inc.Inventors: Kouji Hattori, Susumu Toda, Kenichi Washizuka, Shinji Ito, Daisuke Tanabe, Takanobu Araki, Minoru Sakurai
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Patent number: 7923446Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: GrantFiled: May 31, 2007Date of Patent: April 12, 2011Assignee: Wyeth LLCInventors: Jason Shaoyun Xiang, Steve Yikkai Tam, Yonghan Hu, Phaik-Eng Sum, David Brian How, Darrin William Hopper, Matthew Douglas Vera, Joshua James Sabatini, Thomas Saltmarsh Rush, III, Elisabeth Ann Morris, Katy Evangelia Georgiadis
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Patent number: 7915443Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: November 16, 2007Date of Patent: March 29, 2011Assignee: Allergan, Inc.Inventors: Julie A. Wurster, Clarence Eugene Hull, III, Richard C. Yee, Sougato Boral, Shimiao Wang, Thomas C. Malone
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Patent number: 7906517Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.Type: GrantFiled: July 28, 2008Date of Patent: March 15, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yoshinori Nakamura, Norimitsu Hayashi, Takanori Higashijima, Hitoshi Kubota, Kozo Oka
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Publication number: 20110053975Abstract: 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: ApplicationFiled: January 12, 2009Publication date: March 3, 2011Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS, INSTITUT CURIE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUESInventors: Jamal Tazi, David Grierson, Florence Mahuteau-Betzer, Pierre Roux
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Publication number: 20110039860Abstract: Compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof is disclosed. The compounds are useful for treating diabetes, inflammation, atherosclerosis, hypertension, pain and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: April 27, 2009Publication date: February 17, 2011Inventors: Cangming Yang, Zhicai Wu, Rui Liang, Steven L Colletti
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Publication number: 20110034698Abstract: The present invention relates to oxonium salts having [(Ro)3O]+ cations and sulfonium salts having [(Ro)3S]+ cations, where Ro denotes straight-chain or branched alkyl groups having 1-8 C atoms or phenyl which is unsubstituted or substituted by Ro, ORo, N(Ro)2, CN or halogen, and anions selected from the group of [PFx(CyF2y+1?xHz)6?x]? anions, where 2?x?5, 1?y?8 and 0?z?2y+1, or anions selected from the group of [BFn(CN)4?n]? anions, where n=0, 1, 2 or 3, or anions selected from the group of [(Rf1SO2)2N]9? anions or anions selected from the group of [BFWRf24?w]? anions, to processes for the preparation thereof, and to the use thereof, in particular for the preparation of ionic liquids.Type: ApplicationFiled: October 20, 2010Publication date: February 10, 2011Inventors: Nikolai(Mykola) Ignatyev, German Bissky, Helge Willner
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Patent number: 7884079Abstract: A composition is provided having the formula where R1 and R2 are each independently H or a C1-C4 hydrocarbon; R3 is H, and R4 is a moiety capable of crossing the blood brain barrier selected from the group consisting of: an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate. The composition includes 4-aminopyridine and a transporter species which allows for improved transport of the aminopyridine across the blood brain barrier thereby reducing systemic side effects of aminopyridine administration.Type: GrantFiled: December 27, 2004Date of Patent: February 8, 2011Inventor: Landon C. G. Miller
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Publication number: 20110024725Abstract: 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: ApplicationFiled: May 16, 2008Publication date: February 3, 2011Inventors: Dong-Hoon Lee, Jae-Chol Lee, Jae-Soon Bae, Jun-Gi Jang, Kong-Kyeom Kim, Dae-Woong Lee
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Publication number: 20100317698Abstract: Compounds of formula (I): wherein: n represents an integer of from 1 to 6 inclusive, X represents an oxygen atom or an NR6 group, Y represents a carbon atom or a nitrogen atom, Z represents a carbon atom or a nitrogen atom, R1 and R2 represent a hydrogen atom or an alkyl or arylalkyl group, R3 and R4 represent a hydrogen atom or an alkyl group, R5 represents a hydrogen atom or an alkyl, halogen, hydroxy, alkoxy, cyano, nitro, acyl, alkoxycarbonyl, trihaloalkyl, trihaloalkoxy or optionally substituted amino group, R6 represents a hydrogen atom or an alkyl or arylalkyl group, Ra, Rb, Rc, Rd and Re are as defined in the description. Medicinal products containing the same which are useful as specific nicotinic ligands of ?4?2 receptors.Type: ApplicationFiled: January 30, 2007Publication date: December 16, 2010Applicant: LES LABORATOIRES SERVIERInventors: Solo Goldstein, Claude Guillonneau, Yves Charton, Brian Lockhart, Pierre Lestage
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Publication number: 20100298567Abstract: The invention relates to the nitration of aromatic or heteroaromatic compounds, wherein an activated aromatic or heteroaromatic compound and a nitration agent, optionally in the presence of a solvent, are mixed intensely in a microreactor, and wherein the proportion of the nitration agent to the activated aromatic or heteroaromatic compound, the concentration of nitration agent in the reaction mixture, and the temperature are selected at levels such high that the nitration begins autocatalytically, and wherein the nitration product is obtained after leaving the microreactor and, optionally after an after-reaction time outside the microreactor.Type: ApplicationFiled: January 12, 2006Publication date: November 25, 2010Applicant: LONZA AGInventors: Dominique Roberge, Laurent Ducry
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Patent number: 7820663Abstract: The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs in a mammal by administering an effective amount of a compound of Formula I.Type: GrantFiled: June 15, 2006Date of Patent: October 26, 2010Assignee: The Regents of the University of CaliforniaInventors: Derk J. Hogenkamp, Timothy B. C. Johnstone, Kelvin W. Gee
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Patent number: 7816389Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.Type: GrantFiled: January 11, 2007Date of Patent: October 19, 2010Assignee: Nabriva Therapeutics Forschungs GmbHInventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
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Patent number: 7812037Abstract: Compounds with antiplatelet aggregation and anticoagulant characteristics for the treatment of cardiovascular, cerebrovascular, and cardiovascular related diseases and symptoms, are described. The methods are directed to administering pharmaceutical compositions comprising aryl sulfonic pyridoxine and/or substituted pyridoxine analogs.Type: GrantFiled: October 28, 2005Date of Patent: October 12, 2010Assignee: Medicure International, Inc.Inventors: Wasimul Haque, James Diakur, Vinh Pham, Atiq Rehman, Tara Whitney, Mohammed Omar, Seng Yi, A. Qasim Khan
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Publication number: 20100234605Abstract: New methods for producing difluoromethylene-containing compounds with phenylsulfur trifluoride or a primary alkyl-substituted phenylsulfur trifluoride are disclosed. Also, new methods for producing trifluoromethyl-containing compounds with phenylsulfur trifluoride or primary alkyl-substituted phenylsulfur trifluoride are also disclosed.Type: ApplicationFiled: December 9, 2008Publication date: September 16, 2010Applicant: IM&T RESEARCH, INC.Inventors: Teruo Umemoto, Rajendra P. Singh
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Patent number: 7790892Abstract: A novel aromatic compound having an anthracene skeleton structure and an asymmetric molecular structure; and an organic electroluminescence device which comprises a cathode, an anode and an organic thin film layer comprising at least one layer containing a light emitting layer and sandwiched between the cathode and the anode in which at least one layer in the organic thin film layer contains the above novel aromatic compound singly or as a component of a mixture. The organic electroluminescence device exhibits a great luminance of emitted light, a great efficiency of light emission and a high purity of color, emits bluish light, is excellent in stability at high temperatures and has a long life. The organic electroluminescence device can be provided by utilizing the novel aromatic compound.Type: GrantFiled: April 17, 2003Date of Patent: September 7, 2010Assignee: Idemitsu Kosan Co., Ltd.Inventors: Hidetsugu Ikeda, Masahide Matsuura, Masakazu Funahashi, Chishio Hosokawa
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Patent number: 7786147Abstract: The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected.Type: GrantFiled: March 9, 2005Date of Patent: August 31, 2010Assignees: Medical College of Georgia Research Institute., University of Georgia Research Foundation, Inc.Inventors: Jerry J. Buccafusco, Alvin V. Terry, J. Warren Beach, Rammamohanna R. Jonnala
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Patent number: 7772435Abstract: Disclosed herein is a method comprising: (a) adding an aqueous solution comprising a quaternary ammonium salt to an organic solvent in a vessel under an inert atmosphere, thereby forming a first mixture comprising the quaternary ammonium salt and the solvent; and (b) mixing the first mixture at a temperature and for a time sufficient to remove water and a portion of the solvent from the first mixture, wherein the mixing is performed in an inert atmosphere and the temperature is less than the decomposition temperature of the quaternary ammonium salt.Type: GrantFiled: December 28, 2006Date of Patent: August 10, 2010Assignee: Sabic Innovative Plastics IP B.V.Inventors: Thomas Link Guggenheim, Paul Edward Howson, Farid Fouad Khouri, Lioba Maria Kloppenburg, Matthew Hal Littlejohn, Jacob Lee Oberholtzer, Juan Rodriguez Ordonez, Suresh R. Sriram, David Winfield Woodruff
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Patent number: 7754744Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: August 6, 2007Date of Patent: July 13, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
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Publication number: 20100164371Abstract: An electron transporting-injection compound, represented by following Formula 1: wherein each of the R1, the R2 and the R3 is selected from substituted or non-substituted aromatic group, substituted or non-substituted heterocyclic group, or of substituted or non-substituted aliphatic group, and at least one of the R2 and the R3 is selected from substituted or non-substituted heterocyclic group.Type: ApplicationFiled: December 15, 2009Publication date: July 1, 2010Inventors: Hyun Cheol JEONG, Dong Hee YOO, Jong Hyun PARK, Tae Han PARK, Kyung Hoon LEE
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Publication number: 20100168114Abstract: Methods for determining invertebrate- and insect-specific, such as mosquito-specific, residues of acetylcholinesterases are provided herein. The methods can be used to design pesticides and insecticides that are specific for the invertebrate or insect (e.g., mosquito) enzymes, resulting in reduced toxicity concerns for mammals. Compositions for inhibiting invertebrate and insect (e.g., mosquito) acetylcholinesterases and methods for preparing the same are also provided.Type: ApplicationFiled: December 18, 2009Publication date: July 1, 2010Inventor: Yuan-Ping Pang
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Publication number: 20100160391Abstract: The present invention provides conjugates comprising a substituted aminopyridine covalently attached to an organic molecule via an amide bond. Such conjugates find utility as substrates for amide hydrolases, where the substituted aminopyridine acts as a fluorescent reporter of amide hydrolase activity. As a result, the conjugates described herein can advantageously be used in assays to detect amide hydrolase activity based upon measuring the fluorescence of a substituted aminopyridine that is released after amide hydrolysis. The conjugates of the present invention are also particularly useful in screening assays, which enable the identification of inhibitory molecules for amide hydrolases and other enzymes. The identified amide hydrolase inhibitors can be used in the treatment of a variety of diseases and disorders associated with aberrant amide hydrolase activity.Type: ApplicationFiled: July 9, 2007Publication date: June 24, 2010Inventors: Bruce D. Hammock, Huazhang Huang, Kosuke Nishi
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Publication number: 20100144741Abstract: The invention relates to novel cyclic compounds of the formula (I), in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: November 22, 2007Publication date: June 10, 2010Inventors: Mathias Frederiksen, Rainer Martin Luond, Clive McCarthy, Henrik Moebitz, Jean-Michel Rondeau, Bernard Lucien Roy, Heinrich Rueeger
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Patent number: 7714095Abstract: Polyether polymers, such as polyetherimides, are prepared by the reaction of a dihydroxy-substituted aromatic hydrocarbon alkali metal salt, such as bisphenol A disodium salt, with a bis(N-(chlorophthalimido))aromatic compound, such as 1,3- and/or 1,4-bis(N-(4-chlorophthalimido))benzene, in a solvent such as o-dichlorobenzene and in the presence of a phase transfer catalyst such as a hexaalkylguanidinium chloride. Several embodiments may be employed to improve the method. They comprise employing substantially dry reagents, employing a high solids level in solvent, beginning with an excess of bis(N-(chlorophthalimido))-aromatic compound and incrementally adding alkali metal salt, employing alkali metal salt of small particle size, and using reagents of high purity.Type: GrantFiled: February 28, 2006Date of Patent: May 11, 2010Assignee: Sabic Innovative Plastics IP B.V.Inventors: Daniel Joseph Brunelle, Havva Yagci Acar, Farid Fouad Khouri, Thomas Link Guggenheim, David Winfield Woodruff, Norman Enoch Johnson
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Publication number: 20100113523Abstract: Disclosed herein are novel compounds and pharmaceutical compositions comprising these compounds. In some embodiments, the compounds are inhibitors of the tryptase enzyme and are useful for treating allergic rhinitis, asthma, vascular injury (e.g., restenosis and atherosclerosis), inflammatory bowel disease, arthritis, psoriasis, anaphylaxis, wounds, infections, and other allergy and inflammatory related diseases.Type: ApplicationFiled: October 29, 2009Publication date: May 6, 2010Inventors: Randall S. Alberte, William P. Roschek, JR.
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Publication number: 20100099710Abstract: The invention relates to compounds of general formula (I) wherein X, A, R1 and R2 are as defined herein for use as antiinflammatory agents capable of modulating the activity of a protein tyrosine kinase of the Src family.Type: ApplicationFiled: April 16, 2008Publication date: April 22, 2010Inventors: Lene Jensen, Jef Fensholdt
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Patent number: 7700623Abstract: An arylamidine derivative represented by the general formula (wherein R1 represents optionally protected or substituted amidino; and R2 and R3 are the same or different and each represents hydrogen or halogeno) or a salt of the derivative. The derivative and salt have potent activity against fungi including ones having tolerance to azole type drugs and further have high safety and excellent properties in a repeated dose toxicity test. They are hence useful as an excellent antifungal.Type: GrantFiled: June 28, 2005Date of Patent: April 20, 2010Assignee: Toyama Chemical Co., Ltd.Inventors: Kazuya Hayashi, Kazuto Kunitani, Sayuri Uehara, Teiichi Morita
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Patent number: 7691854Abstract: The invention relates to novel dihydropyridine derivatives, of Formula (I) processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: August 18, 2003Date of Patent: April 6, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenich, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
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Patent number: 7683097Abstract: The present invention provides compounds that are effective against inhibiting topoisomerase (i.e., topoisomerase I and/or topoisomerase II). These compounds are used for treating cell-proliferative disorders. In some instances, these compounds have anticancer activity, e.g., against multi-drug resistant cancers.Type: GrantFiled: May 25, 2005Date of Patent: March 23, 2010Assignee: Propharmacon Inc.Inventors: Martin A. Murphy, John Robert Schullek, John S. Ward, Gary C. Look, Brian Siesel
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Patent number: 7678811Abstract: 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 angogenesis disorders.Type: GrantFiled: July 10, 2007Date of Patent: March 16, 2010Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, William J. Scott, Bernd Riedl
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Publication number: 20100062937Abstract: Benzanilides of the formula: in which X represents hydrogen, halogen, nitro, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl or C1-6 alkylsulfonyloxy; Y represents halogen or C1-6 alkyl; R1 represents C1-6 alkyl, C1-6 alkylthio C1-6 alkyl, C1-6 alkylsulfinyl-C1-6 alkyl or C1-6 alkylsulfonyl-C1-6 alkyl; R2 represents hydrogen, C1-6 alkyl or C1-6 haloalkyl; R3 represents hydrogen or hydroxy; W represents CH or N; and Q represents optionally substituted phenyl or optionally substituted pyridyl wherein the substituent is at least one group selected from the group consisting of halogen, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl and C1-6 haloalkylsulfoxy; provided that when R3 is hydroxy, R2 is not C1-6 alkyl, or when R2 is C1-6 haloalkyl, R3 is hydroxy, W is CH, and the substituents of Q are two or more C1-6 haloalkyl. Insecticides comprising the benzanilides are herein provided.Type: ApplicationFiled: June 2, 2006Publication date: March 11, 2010Applicant: BAYER CROPSCIENCE AGInventors: Katsuaki Wada, Tetsuya Murata, Katsuhiko Shibuya, Eiichi Shimojo
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Publication number: 20100056584Abstract: 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: ApplicationFiled: November 12, 2007Publication date: March 4, 2010Applicant: NeuroSearch A/SInventors: Ulrik Svane Sorensen, Birgitte L. Eriksen, Lene Teuber, Dan Peters, Dorte Strobaek, Tina Holm, Palle Christophersen
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Publication number: 20100051924Abstract: A novel fluorene-containing compound and an organic electroluminescent device including an organic layer employing the same. The fluorene-containing compound has excellent electrical characteristics and an excellent charge transporting capability, and so can be used as a hole injecting material, hole transporting material, and/or emitting material that is suitable for all-color fluorescent and phosphorescent devices, such as red, green, blue, and white fluorescent and phosphorescent devices. Accordingly, an organic electroluminescent device employing the fluorene-containing compound has high efficiency, a low driving voltage, high brightness, and a long lifetime.Type: ApplicationFiled: August 25, 2009Publication date: March 4, 2010Applicant: Samsung Mobile Display Co., Ltd.Inventors: Seok-Hwan HWANG, Young-Kook Kim, Yoon-Hyun Kwak, Jeoung-In Yi, Chang-Ho Lee
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Patent number: 7662839Abstract: A compound of formula (I): or a salt, or chemically protected form thereof, wherein: R5 is an optionally substituted phenyl; A is ?wherein Q is N; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl, and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl, and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl, and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl, and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: Where RN? is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm-alkylene-R2 and the other of RP3 and RP4 is H, m and n can be 0 or 1, and m+n=1 or 2; and additionally, when RP3 is —Cm-alkylene-R2, m can also be 2 or 3, and m+n=1, 2, 3 or 4, and when R2 is tetrazol-5-yl, m+n may be 0; or where one of RP3 and RP4 is —O—CH2—R2, and the other of RP3 and RP4 is H, n is 0; RN is H or optionalType: GrantFiled: December 5, 2007Date of Patent: February 16, 2010Assignee: Asterand UK LimitedInventors: Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton