Two Double Bonds Between Ring Members Of The Diazole Ring (i.e., Pyrazole) Patents (Class 548/373.1)
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Patent number: 7674813Abstract: Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.Type: GrantFiled: June 19, 2008Date of Patent: March 9, 2010Assignee: WyethInventors: Lynn Resnick, Donna M. Huryn, Joan E. Sabalski, Joshua D. Berkowitz, Anthony Frank Kreft, Dennis Martin Kubrak, Thomas Joseph Caggiano, Koi Michele Morris
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Patent number: 7671072Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein R1, R2, and R3 are as defined herein; pharmaceutical compositions thereof; combinations thereof; and uses thereof in the treatment of, inter alia, conditions, diseases, and symptoms including, inter alia, Alzheimer's Disease, cancer, dementia, depression, diabetes, hair loss, schizophrenia, and stroke.Type: GrantFiled: November 15, 2004Date of Patent: March 2, 2010Assignee: Pfizer Inc.Inventors: John W. Benbow, Daniel W. Kung
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Publication number: 20100041726Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: October 1, 2009Publication date: February 18, 2010Inventors: Mark A. Seefeld, Meagan B. Rouse, Dirk A. Heerding
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Publication number: 20100035953Abstract: The invention relates to compounds of the formula I: wherein one of R5, R6 and R7 is and X1, X2, R1 to R15 and n are as defined in the description, and pharmaceutically acceptable salts and/or esters 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 modulated by PPAR ? and/or PPAR? agonists.Type: ApplicationFiled: October 21, 2009Publication date: February 11, 2010Inventors: Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Matthew Blake Wright
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Patent number: 7659298Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.Type: GrantFiled: June 21, 2006Date of Patent: February 9, 2010Assignee: sanofi-aventisInventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
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Patent number: 7655803Abstract: The invention relates to a process for the preparation of ionic liquids of general formula (cation)(R?—O—SO3). The process includes the step of treating the compound of formula (cation)(R—O—SO3) with an alcohol, or mixture of different alcohols, of the formula R?—OH optionally in the presence of a catalyst to form the desired ionic liquid and the by-product R—OH, which is optionally removed during the reaction or after completion of the reaction. The compound of formula (cation)(R—O—SO3) can be prepared by alkylating a tertiary or aromatic amine with a dialkylsulfate.Type: GrantFiled: October 28, 2005Date of Patent: February 2, 2010Assignee: Merck Patent GmbHInventors: Peter Wasserscheid, Roy Van Hal, Claus Hilgers
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Patent number: 7655666Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: GrantFiled: April 10, 2006Date of Patent: February 2, 2010Assignee: Novartis AGInventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
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Patent number: 7652149Abstract: The present invention relates to crystal forms of 4-[5-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-benzenesulfonamide and methods for preparation, interconversion, and isolation of such crystals.Type: GrantFiled: March 31, 2005Date of Patent: January 26, 2010Assignee: Pharmacia & Upjohn Company LLCInventor: Changquan Sun
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Publication number: 20100016396Abstract: The present invention aims to provide an agent for the prophylaxis or treatment of diabetes, which has a superior hypoglycemic action, and is associated with a fewer side effects such as body weight gain and the like. The present invention relates to an agent for the prophylaxis or treatment of diabetes comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof, or a prodrug thereof.Type: ApplicationFiled: January 28, 2008Publication date: January 21, 2010Inventor: Hiroshi Imoto
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Patent number: 7649009Abstract: Pyrazole amides are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: July 1, 2005Date of Patent: January 19, 2010Assignee: Merck & Co., Inc.Inventors: Teresa Beeson, Linda Brockunier, Emma R. Parmee, Subharekha Raghavan
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Patent number: 7645786Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.Type: GrantFiled: December 14, 2006Date of Patent: January 12, 2010Assignee: Pfizer Inc.Inventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
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Patent number: 7642264Abstract: The present invention relates to compounds of formula (Ia), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, R1, R2, R3 and R4 are as defined in the description and claims.Type: GrantFiled: March 22, 2007Date of Patent: January 5, 2010Assignee: Hoffman-La Roche Inc.Inventors: Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
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Patent number: 7632854Abstract: Compounds which are indazole derivatives and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them, as well as combinatorial libraries of indazole derivatives, as set forth in the specification, are disclosed; these compounds or compositions may be useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.Type: GrantFiled: November 17, 2004Date of Patent: December 15, 2009Assignee: Pfizer Italia S.r.l.Inventors: Katia Martina, Wolfgang Brill
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Patent number: 7625937Abstract: The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: September 26, 2007Date of Patent: December 1, 2009Assignee: Merck & Co., Inc.Inventors: Amjad Ali, James M. Balkovec, Donald W. Graham, Christopher F. Thompson, Nazia Quraishi
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Patent number: 7608635Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: August 10, 2006Date of Patent: October 27, 2009Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, Shijie Zhang, Zhenjian Du, Kevin Foley
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Patent number: 7598389Abstract: Novel silylated carboxamides of the formula (I) in which R, L, R1, R3, R3, R4 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms.Type: GrantFiled: November 6, 2004Date of Patent: October 6, 2009Assignee: Bayer Cropscience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Benoit Hartmann, Alexander Klausener, Jörg Nico Greul, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Publication number: 20090234135Abstract: The present invention relates to compositions of matter that are ionic liquids, the compositions comprising any of eleven cations combined with any of three fluorinated sulfonated anions. Compositions of the invention should be useful as solvents and, perhaps, as catalysts for many reactions, including aromatic electrophilic substitution, nitration, acylation, esterification, etherification, oligomerization, transesterification, isomerization and hydration.Type: ApplicationFiled: May 27, 2009Publication date: September 17, 2009Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Mark Andrew Harmer, Christopher P. Junk, Jemma Vickery
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Publication number: 20090216015Abstract: The present invention relates to novel base stable ionic liquids and uses thereof as solvents in chemical reactions, especially base catalysed chemical reactions and reactions comprising the use of strong basis.Type: ApplicationFiled: January 4, 2006Publication date: August 27, 2009Applicant: The Queen's University of BelfastInventors: Martyn J. Earle, Ute Frohlich, Susanne Huq, Suhas Katdare, Rafal Marcin Lukasik, Ewa Bogel, Natalia Vladimirovna Plechkova, Kenneth Richard Seddon
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Patent number: 7576115Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or is pharmaceutically acceptable salt of the compound or a solvate thereof.Type: GrantFiled: August 13, 2007Date of Patent: August 18, 2009Assignee: Nissan Chemical Industries, Ltd.Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
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Patent number: 7576116Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I: wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl; and wherein Ar is optionally substituted with one or more radicals selected from the group consisting of halo, C1-C4 alkyl, C1-C4 haloalkyl, azido, C1-C4 azidoalkyl, aryl, alkylaryl, haloaryl, haloalkylaryl, and combinations thereof, and R is selected from the group consisting of nitrile, acetonitrile, ethylnitrile, propylnitrile, carboxamide, amidine, tetrazole, oxime, hydrazone, acetamidine, aminoacetamide, guanidine, and urea. Also provided are methods of using the compounds for the treatment and prevention of cancer in humans.Type: GrantFiled: September 28, 2007Date of Patent: August 18, 2009Assignee: The Ohio State University Research FoundationInventor: Ching-Shih Chen
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Patent number: 7572797Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.Type: GrantFiled: November 3, 2006Date of Patent: August 11, 2009Assignee: Pfizer Inc.Inventors: Stephen Mark Denton, Karl Richard Gibson, Melanie Susanne Glossop, Mark Ian Kemp, Cedric Poinsard
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Patent number: 7569516Abstract: The present invention relates to a new class of plant growth regulators. In particular, the invention relates to 5-substituted-1-arylpyrazole-3-carboxylic acid derivative of general formula (I) and a method for treatment of plants with such compounds in order to induce growth regulating responses.Type: GrantFiled: December 15, 2004Date of Patent: August 4, 2009Assignee: Bayer CropScience AGInventors: Henricus Bastiaans, Gunter Donn, Nathalie Knittel, Arianna Martelletti, Richard Rees, Michael Schwall
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Patent number: 7566716Abstract: Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: May 18, 2006Date of Patent: July 28, 2009Assignee: Array Biopharma Inc.Inventors: Ellen Laird, George Topalov, Joseph P. Lyssikatos, Mike Welch, Jonas Grina, Josh Hansen, Brad Newhouse
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Publication number: 20090170883Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): (wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.Type: ApplicationFiled: November 12, 2008Publication date: July 2, 2009Applicants: KUMIAI CHEMICAL INDUSTRY CO., LTD., IHARA CHEMICAL INDUSTRY CO., LTD.Inventors: Keiji Toriyabe, Nobuo Takefuji, Minoru Itou, Tetsuya Hirade, Kiyotoshi Nishiyama, Mitsuharu Asahida, Yasunobu Maeda, Nobuhide Wada, Toyokazu Fujisawa, Hiroyuki Yano, Masaaki Komatsu, Osamu Tada
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Publication number: 20090133318Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein J is a phenyl optionally substituted with one to four substituents independently selected from R5; or J is a heterocyclic ring selected from the group consisting of J-1 to J-8; R4 is C4-C12 alkylcycloalkyl, C5-C12 alkenylcycloalkyl, C5-C12 alkynylcycloalkyl, C4-C12 cycloalkylalkyl, C5-C12 cycloalkylalkenyl, C5-C12 cycloalkylalkynyl, C4-C12 cycloalkenylalkyl or C4-C12 alkylcycloalkenyl; each optionally substituted with one to six substituents selected from CH3 and halogen; and R1a, R1b, R2, R3 and R5 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: November 18, 2005Publication date: May 28, 2009Inventor: George Philip Lahm
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Patent number: 7538134Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.Type: GrantFiled: June 14, 2006Date of Patent: May 26, 2009Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
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Patent number: 7528260Abstract: A method is disclosed for preparing compounds of Formula 1 by combining compounds of Formulae 2 and 3 and a sulfonyl chloride. Also disclosed are compounds of Formula 3, which are useful as starting materials for this method.Type: GrantFiled: December 6, 2005Date of Patent: May 5, 2009Assignee: E. I. du Pont de Nemours and CompanyInventors: Rafael Shapiro, Eric de Guyon Taylor, William T. Zimmerman
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Publication number: 20090111799Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R? is L-Lys, D-Lys, ?-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R? is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,Type: ApplicationFiled: July 24, 2008Publication date: April 30, 2009Applicant: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang
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Patent number: 7521471Abstract: The invention relates to 4-cyanopyrazole-3-carboxamide derivatives of formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8 are as described herein. Also disclosed and claimed are the method of preparation and therapeutic application of compound of formula (I).Type: GrantFiled: August 1, 2007Date of Patent: April 21, 2009Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Serge Martinez, Murielle Rinaldi-Carmona
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Publication number: 20090093484Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.Type: ApplicationFiled: December 21, 2006Publication date: April 9, 2009Inventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Patent number: 7511034Abstract: Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: GrantFiled: January 11, 2006Date of Patent: March 31, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
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Patent number: 7504518Abstract: Disclosed is a process for producing a blocked isocyanate compound represented by general formula (III): wherein R1, R2, Q1, and Q2 are as defined in the specification, characterized by comprising reacting a pyrazole compound (I) with an ethylenically unsaturated group-containing isocyanate compound (II) at a temperature in the range of 0° C. to 90° C. The production process can efficiently produce a high-purity blocked isocyanate compound without substantially producing by-products. In the production process, unlike the prior art technique, since there is no need to use any inert solvent such as toluene or xylene, safety to the human body and environment is excellent and the production processes and equipment can be simplified. The blocked isocyanate compound produced by the production process contains no residual inert solvent and is suitable for use in extensive fields such as various coating agents, adhesives, and molding materials.Type: GrantFiled: October 27, 2005Date of Patent: March 17, 2009Assignee: Showa Denko K.K.Inventors: Hideo Miyata, Masatoshi Murakami, Katsutoshi Ohno
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Patent number: 7495017Abstract: Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.Type: GrantFiled: May 1, 2007Date of Patent: February 24, 2009Assignee: Memory Pharmaceuticals CorporationInventors: Allen Hopper, Erik Kuester, Robert Dunn, Richard Conticello
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Publication number: 20090042961Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.Type: ApplicationFiled: May 8, 2008Publication date: February 12, 2009Inventors: Varghese John, Michel Maillard, Barbara Jagodzinska, Jose Aquino, Gary Probst, Jay Tung
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Patent number: 7485657Abstract: Disclosed are compounds of formula (I) The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and the pharmaceutical compositions comprising these compounds.Type: GrantFiled: May 3, 2005Date of Patent: February 3, 2009Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek Cogan, Ming-Hong Hao, Alan David Swinamer, Ronald A. Aungst
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Publication number: 20090030038Abstract: The present invention relates to new compounds of formula I. (I) wherein R1 to R12, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.Type: ApplicationFiled: May 22, 2006Publication date: January 29, 2009Applicant: ASTRAZENECA ABInventors: Chester Chu, Andrew Lister, Gunnar Nordvall, Carl Petersson, Didier Rotticci, Daniel Sohn, Stefan Von Berg
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Patent number: 7476687Abstract: Substituted furo[2,3-g]indazoles for lowering intraocular pressure and treating glaucoma are disclosed.Type: GrantFiled: November 24, 2004Date of Patent: January 13, 2009Assignee: Alcon, Inc.Inventors: Anura P. Dantanarayana, Jesse Albert May
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Publication number: 20090004140Abstract: The present invention discloses compounds of Formulae (I) and (II), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: June 25, 2008Publication date: January 1, 2009Inventors: YAO-LING QIU, Lu Ying, Yat Sun Or, Ce Wang, Jiang Long
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Publication number: 20080287506Abstract: Certain novel N,N-di(heteroarylalkyl)amine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein Ar Ar1, a, b, c, R, Rd, Re, Rf, Rg, Rh, R?, R3 and Rk 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: October 27, 2005Publication date: November 20, 2008Applicant: Bayer CropScience AGInventors: David M. Roush, John F. Chiarello, George Theodoridis, Hongyan Qi
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Patent number: 7452899Abstract: Compounds of Formula (I): inhibit the processing of APP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.Type: GrantFiled: July 29, 2004Date of Patent: November 18, 2008Assignee: Merck Sharp & Dohme LimitedInventors: Michela Bettati, Amanda Louise Boase, Ian Churcher, Tamara Ladduwahetty, Kevin John Merchant, Abdul Quddus
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Patent number: 7446121Abstract: Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (“HMG CoA reductase”) are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis are also described.Type: GrantFiled: November 18, 2005Date of Patent: November 4, 2008Assignee: Pfizer Inc.Inventor: Jeffrey A. Pfefferkorn
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Publication number: 20080234199Abstract: Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.Type: ApplicationFiled: November 22, 2006Publication date: September 25, 2008Inventor: Subba Reddy Katamreddy
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Publication number: 20080227787Abstract: There is provided a use of a compound of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description, and pharmaceutically-acceptable salts thereof, for the manufacture of a medicament for the treatment of a disease in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.Type: ApplicationFiled: March 2, 2005Publication date: September 18, 2008Inventors: Kristofer Olofsson, Benjamin Pelcman, Peter Nilsson, Anders Hallberg, Wesley Schaal
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Publication number: 20080214814Abstract: Stable ionic liquid complexes capable of maintaining stability at high temperatures, under acidic and highly oxidative conditions in the presence of a transition metal, and methods for determining the stability of stable ionic liquid complexes are provided. In accordance with the disclosure herein, the stable ionic liquid complexes are derived from pyrazole, pyrazine and 1,2,4-triazole.Type: ApplicationFiled: July 18, 2007Publication date: September 4, 2008Inventors: Zaiwei Li, Yongchun Tang, Jihong Cheng
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Patent number: 7417151Abstract: Generally disclosed are boron-based organic cations, a method for their manufacture, a method for their use in ionic liquids, and a method for their use as phase-transfer catalysts. More specifically, the boron-based organic cations have an charge of 1+, 2+, or 3+.Type: GrantFiled: December 10, 2004Date of Patent: August 26, 2008Assignee: The University of AkronInventor: Christopher J. Ziegler
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Publication number: 20080200478Abstract: This invention comprises antineoplastic curcumin derivatives and methods of preparation and use thereof. Particular reference is made to the following isomeric compounds wherein R1, R2, and R3 are selected from the group consisting of H, OH, OCH3, and COOH.Type: ApplicationFiled: October 29, 2007Publication date: August 21, 2008Inventor: Byron C. Robinson
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Publication number: 20080194640Abstract: A compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate thereof or a solvate thereof, which shows not only a C5a receptor antagonistic activity but also high activity in the biological availability, as compared to its racemate.Type: ApplicationFiled: February 7, 2006Publication date: August 14, 2008Inventors: Mitsuharu Nakamura, Seigo Ishibuchi, Tatsuyuki Ohtsuka, Hiroshi Sumichika, Sumie Sekiguchi, Takayuki Ishige, Naoko Ueda
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Publication number: 20080176848Abstract: Compounds of a certain formula (I) in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.Type: ApplicationFiled: March 14, 2006Publication date: July 24, 2008Applicant: Nycomed GmbHInventors: Thomas Maier, Thomas Bar, Thomas Beckers, Astrid Zimmermann, Siegfried Schneider, Volker Gekeler
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Patent number: 7396850Abstract: The present invention is directed to a compound, {2-Methyl-4-[3-methyl-1-(4-trifluoromethyl-phenyl)-1H-pyrazol-4-ylmethylsulfanyl]-phenoxy}-acetic acid and pharmaceutical uses thereof.Type: GrantFiled: December 31, 2003Date of Patent: July 8, 2008Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Nathan Bryan Mantlo, Daniel Ray Mayhugh, Guoxin Zhu