Plural Six-membered Hetero Rings Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/332)
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Publication number: 20100261757Abstract: Certain novel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, b, c, T, W, Y R, Rf, Rg, Rh, Ri, Rj, Rk, Rm, Rn, and R 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: ApplicationFiled: January 15, 2007Publication date: October 14, 2010Inventors: John F. Chiarello, Harvey R. Wendt, Najing Zhang, George Theodoridis
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Publication number: 20100261758Abstract: Compounds of Formula (I) wherein R1 is aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R2 is defined heterocyclyl, R3 is alkyl, aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R4 is H or alkyl, or R3 and R4 together with the carbon atom to which they are attached are cycloalkyl fused with aryl, and their use as pharmaceuticals.Type: ApplicationFiled: March 28, 2007Publication date: October 14, 2010Applicant: NOVARTIS AGInventors: Luca Arista, Klemens Hogenauer, Niko Schmiedeberg, Gudrun Werner, Herbert Jaksche
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Patent number: 7807682Abstract: Compounds according to formula I wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C1-6 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated C1-12 hydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, 0, C(O), S, S(O), S(0)2, C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alkType: GrantFiled: November 30, 2007Date of Patent: October 5, 2010Assignee: Leo Pharma A/SInventor: Fredrik Bjorkling
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Publication number: 20100247544Abstract: Compositions are provided for promoting healing of tissue of a vertebrate organism. The compositions can be for internal administration of a therapeutically effective amount of pharmacologically active, protease inhibiting, aqueous media soluble polysulfonated materials in salt form and associated with a secondary material to reduce one or more of inflammation, bacterial proliferation, proteolytic activity, and cancerous cell growth. The compositions may additionally or alternatively be cross-linked so as to alter the solubility of these pharmacologically active salts or slow dissolution by providing biodegradable cross-linkers. Compositions for healing the tissue of a multicellular organism are provided that can include a polysulfonated material in a liquid mixture, as solid particles or constructs that may or may not biodegrade or deliver a pharmacologically relevant value.Type: ApplicationFiled: January 19, 2010Publication date: September 30, 2010Inventor: David John Vachon
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Publication number: 20100249139Abstract: The present invention relates to compounds of formula I wherein R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Patent number: 7803801Abstract: The present invention relates to an aminopyridine compound represented by the following general formula (I) or a salt thereof and an Syk inhibitor containing the compound or a salt thereof as an active ingredient. Here, X1, X2, X3, Z, Y1, Y2 represent a carbon atom or a nitrogen atom, R, R1, R5, R6 represent a hydrogen atom, an alkyl group, etc., and R7 represents a hydrogen atom, a halogen atom, a nitro group, a cyano group, —CpH2(p-1)(Ra1)(Ra2)—O—Ra3, —C(?O)—Rd1, a 5- or 6-membered saturated heterocyclic group, an aromatic heterocyclic group, —N(Rh1)(Rh2), etc. The aminopyridine compound of the present invention has not only high Syk inhibitory activity but also properties to selectively inhibit Syk.Type: GrantFiled: February 28, 2006Date of Patent: September 28, 2010Assignee: Japan Tobacco, Inc.Inventors: Yoshitoshi Kodama, Satoru Noji, Katsuaki Imamura, Ryo Mizojiri, Kenta Aoki, Hideo Takagi, Yuichi Naka, Goro Ito, Kiyotaka Shinoda, Akihito Fujiwara, Kazunori Kurihara, Masaru Tanaka
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Publication number: 20100227887Abstract: The present invention relates to pyridine-2-yl-carboxylic acid amides which act as metabotropic glutamate receptor antagonists. In particular, the present invention relates to pyridine-2-yl-carboxylic acid amides of formula I wherein R1, R2, R3, and R4 are as described in the specification.Type: ApplicationFiled: February 24, 2010Publication date: September 9, 2010Inventors: Georg Jaeschke, Eric Vieira, Juergen Wichmann
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Publication number: 20100222319Abstract: The disclosure relates to compounds of formula (I): wherein A, Z, Z?, L, R2 and R3 are as defined in the disclosure, to compositions comprising said compounds, and to methods for the manufacture and therapeutic use thereof.Type: ApplicationFiled: March 26, 2010Publication date: September 2, 2010Applicant: SANOFI-AVENTISInventors: Claude BERNHART, Monsif BOUABOULA, Pierre CASELLAS, Samir JEGHAM, Jèrome ARIGON, Romain COMBET, Sandrine HILAIRET, Pierre FRAISSE
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Publication number: 20100215661Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: ApplicationFiled: February 26, 2010Publication date: August 26, 2010Inventors: Nicola Mary ASTON, Paul Bamborough, Ann Louise Walker
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Patent number: 7781458Abstract: The invention provides compounds of formula I blocking phosphorylcholine biosynthesis by means of the selective blocking of the choline kinase enzyme in tumor cells or in cells affected by parasitic infection and therefore being applicable in the treatment of tumors and parasitic diseases or diseases produced by viruses and fungi in animals, including human beings; as well as to a method for preparing the compounds of the invention and certain intermediates of said method.Type: GrantFiled: January 11, 2005Date of Patent: August 24, 2010Assignees: Consejo Superior de Investigaciones Cientificas, Universidad de GranadaInventors: Juan Carlos Lacal Sanjuán, Joaquin Campos Rosa, Miguel Ángel Gallo Mezo, Antonio Espinosa Úbeda
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Publication number: 20100210593Abstract: There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.Type: ApplicationFiled: February 17, 2010Publication date: August 19, 2010Applicant: Syntrix Biosystems, Inc.Inventors: Dean Y. Maeda, John A. Zebala
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Patent number: 7776861Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.Type: GrantFiled: January 23, 2006Date of Patent: August 17, 2010Assignee: Purdue Pharma L.P.Inventors: Qun Sun, Xin Wen
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Publication number: 20100204277Abstract: The present invention is directed to methods of treating pest infestation by inhibiting metabolic processes of the pest such as for example, processes involved in invertebrate remodelling.Type: ApplicationFiled: April 5, 2007Publication date: August 12, 2010Applicant: HATCHTECH PTY LTD.Inventors: Vernon Morrison Bowles, Paul MacLeman
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Publication number: 20100197736Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.Type: ApplicationFiled: July 13, 2009Publication date: August 5, 2010Applicant: Japan Tobacco Inc.Inventors: Hisashi SHINKAI, Kimiya Maeda, Hiroshi Okamoto
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Publication number: 20100190788Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar1, Ar2, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.Type: ApplicationFiled: July 11, 2006Publication date: July 29, 2010Inventors: Olivier Defert, Philippe Van Rompaey, Petra Blom, Dirk Leysen, Gert De Wilde, Thomas Brown
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Publication number: 20100183513Abstract: The present invention relates to novel compounds of formula (II) that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating, or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.Type: ApplicationFiled: November 23, 2007Publication date: July 22, 2010Inventors: Wolfgang Froestl, Nampally Sreenivasachary, Sophie Lohmann, Maria Pilar Lopez Deber, Andreas Muhs, Maria Pihlgren Bosch
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Publication number: 20100184741Abstract: 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: ApplicationFiled: April 4, 2008Publication date: July 22, 2010Inventors: Neil Ashweek, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Yun-fei Zhu, Jinghua Yu, Graham Beaton
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Publication number: 20100179172Abstract: A novel pesticide is provided. The present invention provides a pesticide containing, as an active ingredient, an N-phenyl-methanamine derivative represented by the formula (I) or its salt: wherein R1 is alkyl which may be substituted, etc.; each of R2, R3, R4 and R6 which are independent of one another, is hydrogen, halogen, alkyl which may be substituted, etc.; R5 is haloalkyl or halogen; each of R7 and R8 which are independent of each other, is hydrogen, cyano, alkyl, etc.; R9 is alkyl, cycloalkyl, etc.; m is from 0 to 1 and n is from 0 to 4.Type: ApplicationFiled: June 20, 2008Publication date: July 15, 2010Applicant: Ishihara Sangyo Kaisha , Ltd.Inventors: Masayuki Morita, Kazuhiro Yamamoto, Toshihiko Ueki, Kumiko Azuma, Taku Hamamoto
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Publication number: 20100179186Abstract: This application provides a method for the use of select quaternary ammonium antagonists to alpha-7 nAChR for the treatment of cancer and HIV and AIDS.Type: ApplicationFiled: October 13, 2009Publication date: July 15, 2010Applicant: University of Kentucky Research FoundationInventors: Roger L. PAPKE, Peter A. CROOKS, Linda P. DWOSKIN, Gretchen Lopez HERNANDEZ, Zhenfa ZHANG, Jeffrey S. THINSCHMIDT, Guangrong ZHENG
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Publication number: 20100178247Abstract: A compound that recognizes and binds to the CA-IX protein has Formula I, II, III, or IV. The compounds may include a radioactive element for radioimaging or therapeutic applications. Thus, pharmaceutical compositions may be prepared with one or more of the compounds of Formula I, II, III, or IV.Type: ApplicationFiled: December 4, 2009Publication date: July 15, 2010Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
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Publication number: 20100179141Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.Type: ApplicationFiled: December 17, 2007Publication date: July 15, 2010Inventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, JR., Umar Faruk Mansoor
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Patent number: 7754738Abstract: This invention provides compounds of Formula (I), N-oxides and salts thereof wherein: A is O or S; B is a phenyl ring or a pyridine ring, each ring optionally substituted with 1 to 5 R; J is a pyrazole or a pyrrole heterocyclic ring system as defined herein; and; R1 is H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl each optionally substituted with one or more substituents selected from the group consisting of halogen, CN, NO2, hydroxy, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C2-C4 alkoxycarbonyl, C1-C4 alkylamino, C2-C8 dialkylamino and C3-C6 cycloalkylamino. Also disclosed are methods for controlling at least one invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of at least one compound of Formula I, an N-oxide or a salt thereof (e.g., as a composition described herein).Type: GrantFiled: June 10, 2003Date of Patent: July 13, 2010Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Robert James Pasteris, Thomas Martin Stevenson
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Publication number: 20100173888Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.Type: ApplicationFiled: June 17, 2009Publication date: July 8, 2010Inventors: Atli Thorarensen, John I. Trujillo, Wei Huang, Steve R. Turner, Simon Mantell, Ross Strang, Siew Kuen Yeap
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Publication number: 20100173937Abstract: Provided are methods of modulating, treating, reversing and/or preventing pain using tetrakis quaternary ammonium compounds, especially regarding pain of central and/or peripheral origin and/or pain which is nociceptive, neuropathic, somatic, visceral, and/or inflammatory in nature.Type: ApplicationFiled: December 7, 2009Publication date: July 8, 2010Applicants: University of Kentucky Research Foundation, University of UtahInventors: Joseph R. HOLTMAN, Peter A. Crooks, Linda P. Dwoskin, J. Michael McIntosh
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Publication number: 20100173942Abstract: PDE4 inhibition is achieved by novel nitroxide compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formulas I-III: wherein A, B, D, R1, R2, R3, R7, R8, R9, R10 and R6 are as defined herein.Type: ApplicationFiled: March 16, 2010Publication date: July 8, 2010Inventors: Richard A. Schumacher, Elizabeth Doorly Graham, Allen T. Hopper, Ashok Tehim
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Publication number: 20100168070Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: July 1, 2010Inventors: Niklas Heine, Klaus Fuchs, Christian Eickmeier, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
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Publication number: 20100168172Abstract: N-Substituted heteroaryl (substituted)alkyl sulfoximines are effective at controlling insects.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Gregory T. Whiteker, Nneka T. Breaux, John F. Daeuble
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Patent number: 7745445Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR?.Type: GrantFiled: May 13, 2005Date of Patent: June 29, 2010Assignee: IRM LLCInventors: Robert Epple, Mihai Azimioara
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Publication number: 20100160326Abstract: A novel pesticide is provided. The present invention provides a pesticide containing, as an active ingredient, a pyridyl-methanamine derivative represented by the formula (I) or its salt: wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, a heterocyclic group, etc.; each of R2 and R3 which are independent of each other, is hydrogen, halogen, cyano, nitro, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, a heterocyclic group, etc.; R4 is trifluoromethyl or chlorodifluoromethyl; R5 is hydrogen, halogen, cyano, nitro, alkyl, etc.; each of R6 and R7 which are independent of each other, is hydrogen, cyano, alkyl, haloalkyl, etc.; R8 is alkyl, cycloalkyl, alkoxyalkyl, alkoxyalkoxyalkyl, hydroxyalkyl, halogen, haloalkyl, cyano, nitro, etc.; and n is an integer of from 0 to 4.Type: ApplicationFiled: July 20, 2007Publication date: June 24, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Hirohiko Kimura, Masayuki Morita, Kazuhiro Yamamoto, Toshihiko Ueki, Kumiko Azuma, Taku Hamamoto
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Publication number: 20100150899Abstract: The present invention relates to new pyrazolinone scavengers of free radicals, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 10, 2009Publication date: June 17, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100152237Abstract: N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.Type: ApplicationFiled: February 26, 2010Publication date: June 17, 2010Applicant: University of Kentucky Research FoundationInventors: Peter A. CROOKS, Linda P. Dwoskin, Joshua Ayers, Vladimir Grinevich, Sangeetha Sumithran
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Patent number: 7732456Abstract: The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].Type: GrantFiled: March 4, 2005Date of Patent: June 8, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Norikazu Otake, Yuji Haga, Akira Naya, Sayaka Mizutani, Akio Kanatani
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Mono Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors
Publication number: 20100113511Abstract: Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.Type: ApplicationFiled: June 15, 2007Publication date: May 6, 2010Applicant: University of Kentucky Research FoundationInventors: Peter Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Zhenfa Zheng -
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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Publication number: 20100093802Abstract: 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: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: Millennnium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20100093707Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji NAKAMURA, Masayuki Morita, Tetsuo Yoneda, Kenji Izakura
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Publication number: 20100081661Abstract: Inhibitors of microbial heme oxygenase and their use for treatment of microbial infections and bioremediation. The inhibitors of microbial heme oxygenase are useful against a new class of antimicrobial agents to target infections that are persistently difficult to combat with the current spectrum of antimicrobial agents. Screening methods for selecting inhibitors of microbial heme oxygenase.Type: ApplicationFiled: July 24, 2007Publication date: April 1, 2010Applicant: UNIVERSITY OF MARYLAND, BALTIMOREInventors: Angela Wilks, Alexander MacKerrel, JR., Lena Furci, Pedro Lopes
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Publication number: 20100081673Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: September 28, 2009Publication date: April 1, 2010Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard HUTCHINSON, Nicholas Simon STOCK, Jeffrey Roger ROPPE, Jill Melissa SCOTT, Brian Andrew STEARNS, Yen Pham TRUONG, Deborah VOLKOTS, Timothy PARR
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Patent number: 7687067Abstract: A compound of general formula (I): A process for preparing this compound. An intermediate of general formula (II) for the preparation of a compound of general formula (I). A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: April 25, 2005Date of Patent: March 30, 2010Assignee: Bayer Cropscience S.A.Inventors: Pierre-Yves Coqueron, Darren James Mansfield, Philippe Desbordes, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier
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Publication number: 20100069439Abstract: Disclosed is a microorganism control agent containing not less than 1% by weight but less than 10% by weight of N,N?-hexamethylenebis(4-carbamoyl-1-decylpyridinium bromide), not less than 35% by weight but less than 60% by weight of at least one alcohol having 2 or 3 carbon atoms, water and an acid.Type: ApplicationFiled: November 13, 2007Publication date: March 18, 2010Applicant: Japan EnviroChemicals, Ltd.Inventor: Masaaki Nakabayashi
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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: 20100063045Abstract: Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof.Type: ApplicationFiled: March 28, 2008Publication date: March 11, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hasashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20100056509Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: October 20, 2009Publication date: March 4, 2010Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
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Publication number: 20100056576Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: August 31, 2009Publication date: March 4, 2010Inventors: Matthew T. BURGER, Wooseok HAN, Jiong LAN, Gisele NISHIGUCHI
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Publication number: 20100040692Abstract: The present invention relates to two-phase systems of a bioactive ingredient in particle form that has limited or no solubility in a liquid medium, which provides stability to the active ingredient that is similar to the active ingredient when in the solid state. The active ingredient may be capable of therapeutically treating for the presence of a cholinesterase inhibitor.Type: ApplicationFiled: August 15, 2008Publication date: February 18, 2010Applicant: SOUTHWEST RESEARCH INSTITUTEInventors: Hong Dixon, Joseph A. McDonough, Larry Allen Cabell, Patricia Underwood
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Publication number: 20100034784Abstract: The present invention provides a group of compounds found to increase the number of neurons derived from stem cells for use as a therapeutic agent in neurological conditions or diseases. In one embodiment of the present invention, the compounds are used to detect the mechanism by which the number of neurons is increased.Type: ApplicationFiled: July 9, 2009Publication date: February 11, 2010Applicant: NEURALSTEM, INC.Inventors: Judith KELLEHER-ANDERSSON, Karl K. JOHE
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Patent number: 7659272Abstract: 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: October 16, 2007Date of Patent: February 9, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C. B. Harriman, Zhan Shi, Chen Shaowu
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Publication number: 20100029689Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3, and R4 are as defined herein.Type: ApplicationFiled: July 2, 2009Publication date: February 4, 2010Applicants: MEMORY PHARMACEUTICALS CORPORATION, ROCHE PALO ALTO LLCInventors: Allen T. HOPPER, Joan Marie CAROON, Elbert CHIN, Robert F. DUNN, Sharada Shenvi LABADIE, Jim LI, Richard Allen SCHUMACHER, Francisco Xavier TALAMAS
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Publication number: 20100016367Abstract: A method of treating, inhibiting, or preventing an infection in a subject is described. The method comprises administering to the subject an effective amount of at least one bis-pyridinium compound. The bis-pyridinium compound comprises two aromatic ring structures. Each of the ring structures comprises a pyridine ring, and the ring structures are linked by a linker group of at least 8 atoms in length, said linker group being attached to the nitrogen atoms of the pyridine rings. At least one substituent on at least one of the ring structures is an alkyl group having at least 2 carbon atoms, and no substituent on either of the ring structures is —OH, —SH or an amine group.Type: ApplicationFiled: May 4, 2007Publication date: January 21, 2010Applicant: The University of SydneyInventors: Alfred Werner Widmer, Katrina Anne Jolliffe