At 2-position And At 4- Or 6-position Patents (Class 544/309)
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Publication number: 20110166096Abstract: Disclosed are uracil derivatives of the formula (I): wherein R1, R2, R3, and X are as defined herein, and use thereof as therapeutic agents. The uracil derivatives are used in particular together with a cytostatic agent for suppressing or reducing resistance building up on cytostatic treatment.Type: ApplicationFiled: June 25, 2009Publication date: July 7, 2011Applicant: RESPROTECT GMBHInventors: Rudolf Fahrig, Kurt Eger, Martin Führer, Nicole Heinze, Matthias Klemm, Jörg-Christian Heinrich
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Patent number: 7968559Abstract: Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:Type: GrantFiled: April 5, 2010Date of Patent: June 28, 2011Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang
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Publication number: 20110130285Abstract: A composition for promoting root nodule formation, which can be easily applied to soil or plants, and enables efficient formation of root nodules, and a method for promoting root nodule formation using the composition are provided. A composition for promoting root nodule formation, which comprises a compound selected from the group consisting of a nucleoside, a nucleotide, and a nucleobase such as inosine, as an active ingredient, is applied to a leguminous plant to promote root nodule formation of the plant.Type: ApplicationFiled: November 30, 2010Publication date: June 2, 2011Inventors: Kazuhiko Watanabe, Daisuke Yokoi
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Publication number: 20110124619Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: ApplicationFiled: November 17, 2010Publication date: May 26, 2011Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Patent number: 7932376Abstract: This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide pyrimidine-based compound, preferably a P2Y12 receptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formulae I and Ia-Ic, or tautomers, salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae I and Ia-Ic.Type: GrantFiled: April 28, 2006Date of Patent: April 26, 2011Assignee: Inspire Pharmaceuticals, Inc.Inventors: James G. Douglass, III, Paul S. Watson, Sammy R. Shaver, Krzysztof Bednarski
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Patent number: 7923557Abstract: Disclosed herein is a regioselective synthesis of compounds represented by formula (I): or a salt, solvate, clathrate, or prodrug thereof, wherein X, Y, R2, R3, R4, R7, R8, R9, R10, m and n are defined as within.Type: GrantFiled: November 10, 2005Date of Patent: April 12, 2011Assignee: Synta Pharmaceuticals CorporationInventors: Shijie Zhang, Elena Kostik, Lijun Sun
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Patent number: 7906523Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.Type: GrantFiled: October 30, 2007Date of Patent: March 15, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
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Patent number: 7884202Abstract: Nucleobases are perfluoroalkylated in a one step process with a perfluoroalkyl halide in the presence of a sulfoxide, a peroxide and an iron compound. Compounds so produced are useful as medicinal drugs, intermediates for medicinal drugs and agricultural chemicals.Type: GrantFiled: November 6, 2006Date of Patent: February 8, 2011Assignees: Tosoh Corporation, Tosoh F-Tech, Inc., Sagami Chemical Research CenterInventors: Tetsu Yamakawa, Kyoko Yamamoto, Daisuke Uraguchi, Kenji Tokuhisa
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Publication number: 20110028337Abstract: The present invention provides modified nucleobase compounds, modified nucleic acid mimetic compounds and various uses thereof. In addition, the invention provides methods for nucleobase characterisation, SNP characterisation and nucleic acid sequencing.Type: ApplicationFiled: September 19, 2008Publication date: February 3, 2011Inventors: Mark Bradley, Juan J. Diaz-Mochon
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Publication number: 20110009607Abstract: The present invention provides a method for preparing a DNA fragment, in which a desired double-stranded DNA fragment having a sticky end is directly and easily obtained from an amplification product (an amplified fragment) after PCR without a restriction enzyme digestion. The method for preparing a DNA fragment having a sticky end of the present invention comprises: (i) a step of performing a PCR reaction using a template DNA and specific primers to obtain an amplified DNA fragment; and (ii) a step of performing a prescribed treatment on the amplified DNA fragment to dissociate a protecting group from the fragment.Type: ApplicationFiled: March 10, 2009Publication date: January 13, 2011Inventors: Makoto Komiyama, Akinori Kuzuya, Keita Tanaka
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Patent number: 7847097Abstract: The present invention relates to a process for preparing 1-alkyl-3-phenyluracils of the formula I where the variables R1 to R7 are as defined in the description by reacting 3-phenyluracils of the formula II and alkylating agents of the formula III R1-L1??III, with one another, wherein during the entire reaction the pH is kept in a range from 1 to 6 by adding base a little at a time.Type: GrantFiled: May 18, 2006Date of Patent: December 7, 2010Assignee: BASF AktiengesellschaftInventors: Joachim Gebhardt, Sandra Loehr, Michael Keil, Thomas Schmidt, Jan Hendrik Wevers, Helmut Zech, Rudolf Haeberle
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Patent number: 7807858Abstract: It was found that a fluoro derivative can be produced by reacting a hydroxy derivative with sulfuryl fluoride (SO2F2) in the presence of an organic base or in the presence of an organic base and “a salt or complex comprising an organic base and hydrogen fluoride”. According to the present production process, it is not necessary to use perfluoroalkanesulfonyl fluoride, which is not preferable in industrial use, and it is possible to advantageously produce optically-active fluoro derivatives, which are important intermediates of medicines, agricultural chemicals and optical materials, specifically 4-fluoroproline derivatives, 2?-deoxy-2?-fluorouridine derivatives, optically-active ?-fluorocarboxylate derivatives, and the like, even in a large scale.Type: GrantFiled: March 17, 2006Date of Patent: October 5, 2010Assignee: Central Glass Company, LimitedInventors: Akihiro Ishii, Takashi Ootsuka, Manabu Yasumoto, Hideyuki Tsuruta, Kenjin Inomiya, Koji Ueda, Kaori Mogi
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Patent number: 7807689Abstract: The present invention provides a compound of the formula: or stereoisomers or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, articles of manufacture comprising the same, and methods of using the same.Type: GrantFiled: March 15, 2005Date of Patent: October 5, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Luckner G. Ulysse
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Patent number: 7799914Abstract: The present invention provides a process for the preparation of a compound of formula (I): wherein X is halogen; Y is ZR1; Z is oxygen or sulphur; and R1 is C1-6 alkyl, C1-6 haloalkyl or C3-7 cycloalkyl; the process comprising either: a. hydrogenating a compound of formula (II): with a suitable transition metal catalyst in a C1-6 aliphatic alcohol, an ether, an ester or a hydrocarbon as solvent; or, b. conducting a one-pot hydrogenation of a compound of formula (III): wherein R2 is phenyl optionally substituted by chloro, C1-6 alkyl, C1-6 alkoxy or (C1-6 alkyl)2N; i. firstly at about 20° C. to form a compound of formula (IV): ii. and then at about 40° C.; both steps (i) and (ii) being carried out in the presence of a suitable catalyst and in the presence of a suitable solvent.Type: GrantFiled: March 29, 2005Date of Patent: September 21, 2010Assignee: AstraZeneca ABInventors: Ulf Larsson, Kajsa Radevik
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Patent number: 7795270Abstract: Deoxyuridine derivatives of the formula (I) where R1 is H or various substituents; D is —NHCO—, —CONH—, -0-, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is —O—, —S—, —CHR10—, —C(?O)—; J is —CH2—, or when G is CHR10 may also be —O— or —NH—; R10 is H, F, —CH3, —CH2NH2, —CH2OH; —OHR11 is H, F, —CH3, —CH2NH2, —CH2OH, —CH(OH)CH3, CH(NH3)CH3; or R10 and R11 together define an olefinic bond, or together form a —CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.Type: GrantFiled: January 6, 2005Date of Patent: September 14, 2010Assignee: Medivir ABInventors: Ian Gilbert, Corinne Nguyen, Gian Filippo Ruda, Alessandro Schipani, Ganasan Kasinathan, Nils-Gunnar Johansson, Dolores Gonzalez Pacanowska
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Patent number: 7795428Abstract: Compounds are provided for use with DPP-IV of the formula: 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: GrantFiled: August 7, 2007Date of Patent: September 14, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Jeffrey Alan Stafford, Zhiyuan Zhang, Bruce Elder, Paul Isbester, Grant Palmer, Jonathan S. Salsbury, Luckner Ulysse
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Patent number: 7790735Abstract: The present invention provides novel nucleoside and nucleotide derivatives that are useful agonist or antagonists of P1 and P2 receptors. For example, the present invention provides a compound of formula A-M, wherein A is modified adenine or uracil and M is a constrained cycloalkyl group. The adenine or uracil is bonded to the constrained cycloalkyl group. The compounds of the present invention are useful in the treatment or prevention of various diseases including airway diseases (through A2B, A3, P2Y2 receptors), cancer (through A3, P2 receptors), cardiac arrhythmias (through A1 receptors), cardiac ischemia (through A1, A3 receptors), epilepsy (through A1, P2X receptors), and Huntington's Disease (through A2A receptors).Type: GrantFiled: August 8, 2006Date of Patent: September 7, 2010Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A Jacobson, Victor E Marquez
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Patent number: 7781584Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.Type: GrantFiled: October 30, 2007Date of Patent: August 24, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
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Patent number: 7776869Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: October 14, 2005Date of Patent: August 17, 2010Assignee: Amgen Inc.Inventors: Stuart C. Chaffee, Brian K. Albrecht, Brian L. Hodous, Matthew W. Martin, David C. McGowan, Erin F. DiMauro, Gade Reddy, Victor J. Cee, Philip R. Olivieri, Anthony Reed, Karina Romero
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Publication number: 20100204456Abstract: Novel conjugates of 5-fluoro-uracil and novel 5-fluoro-uracil immunogens and monoclonal antibodies generated by these immunogens which are useful in immunoassays for the quantification and monitoring of 5-fluoro-uracil in biological fluids.Type: ApplicationFiled: April 26, 2010Publication date: August 12, 2010Inventors: Salvatore J. Salamone, Jodi Blake Courtney, Dennis Stocker
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Patent number: 7767811Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.Type: GrantFiled: June 5, 2006Date of Patent: August 3, 2010Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Patent number: 7767624Abstract: Disclosed are 3-heterocyclyl substituted benzoic acid derivatives of general formula (I), in which the variables R1 to R8 and X have the meanings indicated in claim 1, and the use thereof as herbicides or for desiccating/defoliating plants.Type: GrantFiled: July 22, 2003Date of Patent: August 3, 2010Assignee: BASF AktiengesellschaftInventors: Michael Puhl, Gerhard Hamprecht, Robert Reinhard, Ingo Sagasser, Werner Seitz, Cyrill Zagar, Matthias Witschel, Andreas Landes
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Patent number: 7745453Abstract: Compounds of Formula (1), pharmaceuticals containing the same, especially anti-HIV agents having anti viral activity, especially inhibitory activity against HIV integrase, wherein X represents either one of the following groups: (wherein, C ring is nitrogen-containing aromatic heterocyclic ring in which at least one atom in atoms neighboring the atom bound to the pyrimidine ring is unsubstituted nitrogen atom; R10 is hydrogen or lower alkyl; D ring is aryl or heteroaryl) Z1 and Z3 each is independently a single bond, O, S, S(?O) or SO2; Z2 is a single bond, lower alkylene or lower alkenylene; Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is lower alkyl, substituted lower alkyl or the like; R2 is a hydrogen atom or optionally substituted lower alkyl; or R1 and R2 may form, together with an adjacent atom, an optionally substituted heterocyclic ring, a pharmaceutically acceptable salt or a solvate thereof.Type: GrantFiled: December 21, 2004Date of Patent: June 29, 2010Assignee: Shionogi & Co., Ltd.Inventors: Hidenori Mikamiyama, Minamo Iwata, Yoshiyuki Taoda
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Patent number: 7737275Abstract: A process is described for preparing 3-phenyl(thio)uracils or 3-phenyldithiouracils of the formula I, by reacting a phenyl iso(thio)cyanate of the formula II with an enamine of the formula III and, if appropriate, in a further step, the resulting 3-phenyl(thio)uracil or 3-phenyldithiouracil of the formula I where R1=R1a, when R1=hydrogen, is reacted with an aminating agent of the formula IV to give 3-phenyl(thio)uracils or 3-phenyldithiouracils of the formula I where R1=amino where the variables R1, R1a, R2, R3, R4, X1, X2, X3, Ar, A and L1 are each as defined in claim 1.Type: GrantFiled: December 1, 2004Date of Patent: June 15, 2010Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Michael Puhl, Bernd Wolf, Michael Keil, Robert Reinhard, Werner Seitz, Guido Mayer
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Patent number: 7709493Abstract: Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:Type: GrantFiled: May 20, 2009Date of Patent: May 4, 2010Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang
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Publication number: 20100105030Abstract: The invention relates to non-natural bases and base pairs that expand the normal DNA-based encoding system. Compositions herein may comprise at least one non-natural base that may interact with another base via a Watson Crick-type hydrogen bonding geometry and/or a Hoogsteen-type hydrogen bonding geometry. The bases may be used in a molecular entity, such as an oligomer or any other entity wherein the bases are attached to a backbone. For example, they may be comprised in DNA, RNA, or PNA, or a variety of other nucleic acid-type systems.Type: ApplicationFiled: June 30, 2006Publication date: April 29, 2010Applicant: DAKO DENMARK A/SInventors: Jesper Lohse, Kenneth Heesche Petersen
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Publication number: 20100105562Abstract: The present invention relates to a crystalline form of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)-amino]sulfonyl]benzamide. The invention also relates to a process for the preparation of this crystalline form and to plant protection formulations which comprise this crystalline form of the phenyluracil.Type: ApplicationFiled: October 12, 2007Publication date: April 29, 2010Inventors: Thomas Schmidt, Joachim Gebhardt, Sandra Löhr, Michael Keil, Jan Hendrik Wevers, Peter Erk, Heidi Emilia, Gerhard Hamprecht, Werner Seitz, Guido Mayer, Bernd Wolf, Gerhard Cox, Alfred Michel, Cyrill Zagar, Robert Reinhard, Bernd Sievernich
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Patent number: 7704971Abstract: Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, ido, cyano, halo-substituted C1-4 alkyl, C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 alkynyl.Type: GrantFiled: September 1, 2006Date of Patent: April 27, 2010Assignee: SmithKlineBeecham CorporationInventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
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Publication number: 20100099159Abstract: There is disclosed nucleotides and nucleotide analogs having a protecting or “caging” group. There is further disclosed oligonucleotides and oligonucleotides analogs formed having a protecting or “caging” group. There is further disclosed a method for decaging the nucleotides and nucleotide analogs having a protecting or “caging” group and oligonucleotides and oligonucleotide analogs having a caging group.Type: ApplicationFiled: December 5, 2008Publication date: April 22, 2010Inventor: Alexander Deiters
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Publication number: 20100087641Abstract: The invention provides methods and materials for the conversion of cytosine to uracil. A nucleic acid, such a gDNA, is reacted with bisulfate, such as magnesium bisulfite, in the presence of a quaternary amine catalyst. Examples of suitable quaternary amine catalysts include but are not limited to quaternary ammonium compounds, quaternary alkyl ammonium salts, quaternary alkyl ammonium halides, quaternary methyl ammonium bromide, quaternary ammonium chloride, tetraethyl ammonium hydroxide, tetraethylammonium chloride, tetrabutyl ammonium chloride, tetrabutyl ammonium bromide. The invention also contemplates kits of premeasured ingredients for carrying out the methods of the invention either on an individual sample or on a plurality of samples.Type: ApplicationFiled: May 19, 2009Publication date: April 8, 2010Inventors: Victoria L. Boyd, Gerald Zon
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Patent number: 7642303Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.Type: GrantFiled: October 13, 2005Date of Patent: January 5, 2010Inventors: Thomas L. Shakely, James John Krutak
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Publication number: 20090326081Abstract: The invention relates to a polymeric material comprising crosslinked spherical particles that are obtained by photoinitiated precipitation polymerization of crosslinking monomer and optionally a further monomer in the presence of an initiator and a solvent. It also relates to a method for producing the material and a chromatography column containing the material.Type: ApplicationFiled: June 8, 2007Publication date: December 31, 2009Applicant: SEQUANT ABInventors: Knut Irgum, Fredrik Lime
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Publication number: 20090286818Abstract: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: ApplicationFiled: May 19, 2009Publication date: November 19, 2009Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20090275750Abstract: Methods of making compounds of the formula (I) wherein the variables are as defined herein. Also, methods of making compounds that may be used to inhibit dipeptidyl peptidase.Type: ApplicationFiled: September 15, 2006Publication date: November 5, 2009Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Paul R. Brodluahrer, Bruce Elder, Paul Isbester, Richard S. Fornicola, Philip B. Kisanga, Bingidimi I. Mobele, Grant J. Palmer, Maxwell M. Reeve, Jonathon S. Salsbury, Luckner Ulysse, Sripathy Venkatraman
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Patent number: 7592446Abstract: The present invention provides selenium derivatives of nucleosides, nucleoside phosphoramidites, nucleotides, nucleotide triphosphates, oligonucleotides, polynucleotides, and larger nucleic acids and methods for their synthesis. Selenium derivatives of both ribonucleic acids and deoxyribonulcleic acids, as well as methods for their synthesis, crystallization and uses in structural determinations, particularly by X-ray crystallographic techniques are disclosed. The selenium derivatives of the present invention are also useful as food supplements.Type: GrantFiled: March 22, 2002Date of Patent: September 22, 2009Assignee: Georgia State University Research Foundation, Inc.Inventor: Zhen Huang
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Patent number: 7572816Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.Type: GrantFiled: July 21, 2004Date of Patent: August 11, 2009Assignee: Auspex Pharmaceuticals, Inc.Inventors: Bruno Tse, Sepehr Sarshar
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Patent number: 7553840Abstract: Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:Type: GrantFiled: December 11, 2007Date of Patent: June 30, 2009Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang
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Patent number: 7547704Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.Type: GrantFiled: December 6, 2004Date of Patent: June 16, 2009Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, Universita Degli Studi di CagliariInventors: Paola LaColla, Richard Storer, Gilles Gosselin, Jean-Pierre Sommadossi
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Publication number: 20090124796Abstract: Provided is a simple and efficient production process of a nucleobase having a perfluoroalkyl group. A nucleobase (for example, uracils, cytosines, adenines, guanines, hypoxanthines, xanthines, or the like) is reacted with a perfluoroalkyl halide in the presence of a sulfoxide, a peroxide and an iron compound to produce a perfluoroalkyl-substituted nucleobase, which is useful as an intermediate for medical drugs, economically.Type: ApplicationFiled: November 6, 2006Publication date: May 14, 2009Inventors: Tetsu Yamakawa, Kyoko Yamamoto, Daisuke Uraguchi, Kenji Tokuhisa
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Publication number: 20090118224Abstract: To provide a novel anti-psychosocial stress agent which is highly safety and can be continuously taken, more particularly, a novel anti-psychosocial stress agent which prevents or alleviates psychosocial stress. The invention provides an anti-psychosocial stress agent containing, as an active ingredient, uridylic acid, uridine, or uracil. Since uridylic acid, uridine, or uracil, which is an active ingredient of the anti-psychosocial stress agent of the present invention, is inexpensively available and is a biological component, the agent exhibits high safety and can be continuously taken. Therefore, the anti-psychosocial stress agent of the present invention is effective for mitigating, alleviating, or relieving psychosocial stress, which is an issue in modern society. When the anti-psychosocial stress agent is taken before development of symptoms associated with psychosocial stress, the symptoms can be prevented.Type: ApplicationFiled: June 26, 2007Publication date: May 7, 2009Applicant: YAMASA CORPORATIONInventors: Kazuki Endo, Noriyuki Ashida
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Patent number: 7521396Abstract: The invention relates to compounds of the formula (I) in which Q, R1, R2, R3, R4, R5, R6, R7 are as defined in the disclosure, to processes for their preparation, and to their use as herbicides.Type: GrantFiled: April 22, 2003Date of Patent: April 21, 2009Assignee: Bayer CropScience AGInventors: Hans-Georg Schwarz, Roland Andree, Dorothee Hoischen, Joachim Kluth, Karl-Heinz Linker, Anton Vidal-Ferran, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Publication number: 20090081145Abstract: The present invention relates to an improved method of formation of disulfide bridges in substances bearing SH groups, in particular peptides, for example by formation of intramolecular disulfide bridges, in which a heterocyclic compound having at least one nitrogen atom (e.g. caffeine or a caffeine-like substance) is used for catalysis of the reaction. It was found, surprisingly, that addition of the heterocyclic substance increases both the yield and the purity of the product bearing disulfide bridges.Type: ApplicationFiled: December 23, 2006Publication date: March 26, 2009Applicant: AplaGen GmbHInventors: Karsten Knorr, Marco Emgenbroich, Carsten Bungener
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Patent number: 7501429Abstract: Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and/or epileptogenesis. Methods for preparing the compounds of the invention are also described.Type: GrantFiled: April 11, 2002Date of Patent: March 10, 2009Assignee: Queen's University at KingstonInventors: Donald F. Weaver, Buhendwa Musole Guillain, John R. Carran, Kathryn Jones
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Patent number: 7462625Abstract: GnRH receptor antagonists are disclosed that 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 A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: September 11, 2006Date of Patent: December 9, 2008Assignee: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
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Publication number: 20080300216Abstract: Deoxyuridine derivatives of Formula (I?); where A is O, S or CH2; B is O, S or CHR3; R1 is H, or various substituents; R2 is H, F; R3 is H, F, OH, NH2; or R2 and R3 together form a chemical bond; D is —NHCO—, —CONH—, —O—, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, or a stable monocyclic, bicyclic or tricyclic ring system have utility in the prophylaxis of treatment of parasitic diseases such as malaria.Type: ApplicationFiled: January 6, 2005Publication date: December 4, 2008Inventors: Ian Gilbert, Corinne Nguyen, Gian Filippo Ruda, Alessandro Schipani, Ganasan Kasinathan, Nils-Gunnar Johansson, Dolores Gonzalez Pacanowska
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Publication number: 20080262005Abstract: Compounds having utility as GnRH receptor antagonists and for treatment of a variety of sex-hormone related conditions in both men and women. Such compounds have the following structure (I): (I) wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6, R7, n and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of structure (I) 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: May 13, 2005Publication date: October 23, 2008Applicant: NEUROCRINE BIOSCIENCES, INC.Inventors: Yun-Fei Zhu, Zhiqiang Gou, Mi Chen, Liren Zhao
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Patent number: 7405221Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.Type: GrantFiled: September 23, 2003Date of Patent: July 29, 2008Assignee: Merck & Co., Inc.Inventors: Ihor E. Kopka, Bing Li, William K. Hagmann
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Publication number: 20080177064Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.Type: ApplicationFiled: October 30, 2007Publication date: July 24, 2008Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
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Patent number: RE42462Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: October 7, 1995Date of Patent: June 14, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: RE42477Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: March 27, 1997Date of Patent: June 21, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack