The Nitrogen Is Bonded Directly At 4- Or 6-position Patents (Class 544/317)
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Publication number: 20110275652Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.Type: ApplicationFiled: July 15, 2011Publication date: November 10, 2011Inventors: Jiri Zemlicka, Shaoman Zhou, John C. Drach
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Publication number: 20110268720Abstract: The disclosure provides an extended release formulation of 5-fluorocytosine. In another aspect, a method of treating a fungal disease is provided. The method comprises administering to a subject in need thereof a fungus-treating effective amount of a composition comprising 5-fluorocytosine. In yet another aspect, a method of treating a cancer is provided. The method comprises administering to a subject in need thereof a sufficient amount of an expression vector to induce expression of cytosine deaminase which is capable of converting 5-fluorocytosine to 5-fluorourcail in cells of the cancer and a cancer-treating effective amount of a composition comprising 5-fluorocytosine.Type: ApplicationFiled: June 30, 2009Publication date: November 3, 2011Applicant: TOCAGEN INC.Inventors: Harry E. Gruber, Douglas J. Jolly, Kay Olmstead
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Publication number: 20110269732Abstract: The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational change in the protein AuroraB and whose binding constant for the two-step process is given as Ki*. Finally, this invention also relates to compounds having the features of the pharmacophore.Type: ApplicationFiled: October 14, 2009Publication date: November 3, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Julian M.C. GOLEC, John POLLARD, James WESTCOTT, Hayley Marie BINCH, Michael Paul MORTIMORE, Daniel David ROBINSON
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Publication number: 20110269706Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.Type: ApplicationFiled: January 7, 2010Publication date: November 3, 2011Applicant: Northlake Biosciences LLCInventors: Yu Chen, Yi Chen
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Publication number: 20110263627Abstract: This present disclosure is related to the field of N3-substituted-N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: April 20, 2011Publication date: October 27, 2011Applicant: DOW AGROSCIENCES LLCInventors: Timothy A. Boebel, Beth Lorsbach, Timothy P. Martin, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
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Patent number: 8044040Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-? expression utilizing compounds of the present invention are also disclosed.Type: GrantFiled: July 16, 2007Date of Patent: October 25, 2011Assignees: Bristol-Myers Squibb Company, Pharmacopeia, Inc.Inventors: Gulzar Ahmed, Axel Metzger, Ian Henderson, David J. Diller, Jun Wen, Stephen T. Wrobleski, Katerina Leftheris, Chunjian Liu
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Publication number: 20110257396Abstract: An improved process for the manufacture of Lamivudine. The process involves: (a) resolution of racemic lamivudine (intermediate of formula IX) to cis (±) lamivudine of formula (XII) by forming a crystalline salt and separating the product from an organic solvent by fractional crystallization; (b) resolution of cis (±) lamivudine to cis (?) isomer involving formation of S-Binol adduct of formula XIV.Type: ApplicationFiled: September 10, 2007Publication date: October 20, 2011Applicant: Lupin LimitedInventors: Girij Pal Singh, Dhananjai Srivastava, Srinivas Ayyalasomayajula Satya, Manmeet Brijkishore Saini, Harishchandra Sambhaji Jadhav, Aparna Murlidharan Warrier, Nilesh Bhimsingh Dumre
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Publication number: 20110257397Abstract: There is provided a method for resolving a compound of formula III, in the cis configuration: There is also provided a process for producing optically active compound of formula I or II: wherein: R1, R2, R3 are as defined herein, the method and process involving the production, recovery and conversion of diastereomeric salts.Type: ApplicationFiled: June 22, 2011Publication date: October 20, 2011Inventors: Alex CIMPOIA, Dan Simion, Joana R. Simion
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Publication number: 20110245458Abstract: Disclosed is a peptide nucleic acid monomer as well as a corresponding peptide nucleic acid molecule. The monomer comprises a terminal amino group and a terminal group A. The terminal amino group and the terminal group A are connected by an aliphatic moiety. The main chain of this aliphatic moiety is free of groups that are charged under physiological conditions. The terminal group A is one of —COOH, —COOR3, —COX, —COSR3, —CN, —CONH2, —CONHR3, —CONR3, R4, with R3 and R4 being H or an aliphatic, alicyclic, aromatic, arylaliphatic or arylalicyclic group, and X being a halogen atom. The terminal amino group is substituted by an aliphatic group with a main chain of at least two carbon atoms and optionally 0 to a bout 2 heteroatoms selected from the group N, O, S, Se and Si. The main chain has a polar head group Z.Type: ApplicationFiled: September 3, 2008Publication date: October 6, 2011Applicant: NANYANG TECHONOLOGICAL UNIVERSITYInventors: Chuan Fa Liu, Yun Zeng, Xiao Wei Lu
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Publication number: 20110245497Abstract: Cis(±)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone is reacted with S(+)-1,1?-binaphthyl-2,2?-diyl hydrogen phosphate in methanol to obtain diastereomeric compounds. The diastereomeric compounds are subjected to selective crystallization to obtain (2R-Cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone 1,1?-binaphthyl-2,2?-diyl hydrogen phosphate. (2R-Cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone 1,1?-binaphthyl-2,2?-diyl hydrogen phosphate is treated with hydrochloric acid in water to obtain (2R-cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone.Type: ApplicationFiled: December 8, 2008Publication date: October 6, 2011Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Ayyalasomayajula Satya Srinivas
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Publication number: 20110236952Abstract: The invention relates to compounds of formula (I?): in which A, L2, M and B are as defined in the description.Type: ApplicationFiled: September 22, 2009Publication date: September 29, 2011Applicant: CIS BIO InternationalInventors: Emmanuel Bourrier, Michel Laget, Laurent Lamarque, Norbet Tinel, Eric Trinquet, Hervé Bazin
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Publication number: 20110229918Abstract: The invention relates to a precursor for producing sintered metallic components, a method for producing the precursor and the production of the components. The object of the invention is to disclose possibilities of being able to produce sintered metallic components, which render possible an increased physical density and a reduced shrinkage on the fully sintered component. With a precursor according to the invention for the production of sintered metallic components, a coating layer is formed on a core, which is formed from respectively one particle of a first metallic powder. The coating layer is formed with a second powder and a binder. The first powder thereby has a particle size d90 of at least 50 ?m and the second powder has a particle size d90 of less than 25 ?m. The precursor is powdery.Type: ApplicationFiled: November 7, 2008Publication date: September 22, 2011Applicant: COVALYS BIOSCIENCES AGInventors: Nicole Schneider-Han-Marra, Andreas Brecht
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Publication number: 20110230472Abstract: It is an object of the present invention to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused azole compound shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 25, 2009Publication date: September 22, 2011Applicant: Shionogi & Co., Ltd.Inventors: Yasunori Mitsuoka, Manami Masuda, Daisuke Taniyama
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Patent number: 8022221Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: February 12, 2009Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Victor J. Cee, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
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Patent number: 8013154Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.Type: GrantFiled: September 26, 2008Date of Patent: September 6, 2011Inventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
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Publication number: 20110213148Abstract: The present invention discloses a co-crystal compound of optical devices. The co-crystal compound is crystallized out with hydrogen bonding by a temperature fluctuation method after mixing small organic molecules without optoelectronic properties and organic molecules having heterocyclic rings with optoelectronic properties. The photoluminescence (PL) intensity of this hydrogen-bonded co-crystal compound according to the present invention can vary with a variety of the small organic molecules without optoelectronic properties, so as to modulate the PL intensity.Type: ApplicationFiled: May 11, 2010Publication date: September 1, 2011Applicant: NATIONAL CENTRAL UNIVERSITYInventors: Tu Lee, Pu-Yun Wang
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Publication number: 20110207157Abstract: The invention relates to new proteins called alkylcytosine transferases (ACTs) derived from O6-alkylguanine-DNA alkyltransferase, and to substrates for ACTs specifically transferring a label to these ACTs and to fusion proteins comprising these. The substrates according of the invention are substituted cytosines of formula (I) wherein R1 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to OCH2—; R2 is a linker; and L is a label or a plurality of same or different labels. The invention further relates to methods of transferring label L from these substrates of formula (I) to ACTs and ACT fusion proteins. The system of ACT-compound of formula (I) is particularly suitable for double labelling studies together with the known system O6-alkylguanine-DNA alkyltransferase (AGT)-benzylguanines.Type: ApplicationFiled: July 24, 2007Publication date: August 25, 2011Applicant: Ecole Polytechnique Federale de LausanneInventors: Arnaud Gautier, Kai Johnsson, Maik Kindermann, Alexandrc Juillerat, Florent Beaufils
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Patent number: 7989446Abstract: The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient.Type: GrantFiled: September 22, 2010Date of Patent: August 2, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Masaya Kato, Norifumi Sato, Minoru Okada, Tetsuyuki Uno, Nobuaki Ito, Yasuhiro Takeji, Hisashi Shinohara, Masahiro Fuwa
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Patent number: 7968703Abstract: There is provided a method for resolving a compound of formula III, in the cis configuration: There is also provided a process for producing optically active compound of formula I or II: wherein: R1, R2, R3 are as defined herein, the method and process involving the production, recovery and conversion of diastereomeric salts.Type: GrantFiled: March 7, 2005Date of Patent: June 28, 2011Assignee: SHIRE Canada Inc.Inventors: Alex Cimpoia, Dan Simion, Ioana R. Simion, legal representative
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Publication number: 20110152300Abstract: This present disclosure is related to the field of 2-aldoximino-5-fluoropyrimidines and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Timothy A. Boebel, Beth Lorsbach, Timothy P. Martin, W. John Owen, Michael T. Sullenberger, Chenglin Yao
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Publication number: 20110137034Abstract: The invention relates to a process for the preparation of stable lamivudine polymorph form and to a composition comprising thereof.Type: ApplicationFiled: September 1, 2008Publication date: June 9, 2011Applicant: Hetero Research FoundationInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash chander Reddy
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Patent number: 7951789Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.Type: GrantFiled: December 27, 2007Date of Patent: May 31, 2011Assignees: Idenix Pharmaceuticals, Inc., L'Université Montpellier IIInventors: Jean-Pierre Sommadossi, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
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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: 7947698Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.Type: GrantFiled: March 21, 2008Date of Patent: May 24, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Andy Atuegbu, Vadim Markovtsov, Somasekhar Bhamidipati, Rajinder Singh, Vanessa Taylor, Sambaiah Thota, Jeffrey Wayne Clough, David Carroll, Hui Li, Robin Cooper
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Publication number: 20110112294Abstract: Compounds of the formula I wherein: R1 is independently H, —OR3, —NHR4; C1-C4 alkyl; or, when n is 2, adjacent R1 together define an olefinic bond; R2 is H; or when the gem R1 is C1-C4 alkyl, that R2 may also be C1-C4 alkyl; or when the gem R1 is —OR3, that R2 may also be —C(?O)OH or a pharmaceutically acceptable ester thereof; R3 is independently H, or a pharmaceutically acceptable ester thereof; R4 is independently H or a pharmaceutically acceptable amide thereof; R5 and R6 are H or an amine prodrug moiety n is 1, 2 or 3; and pharmaceutically acceptable salts thereof; have utility in the treatment or prophylaxis of HIV, especially reverse transcriptase mutants which allow an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.Type: ApplicationFiled: December 30, 2010Publication date: May 12, 2011Applicant: Medivir ABInventors: Xiao-Xiong ZHOU, Christer Sahlberg
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Patent number: 7939660Abstract: A novel process for preparing emtricitabine, and more particularly a process for preparing emtricitabine involving the formation and isolation of intermediate compounds in salified form, is described.Type: GrantFiled: April 6, 2009Date of Patent: May 10, 2011Assignee: Archimica S.r.l.Inventors: Giorgio Bertolini, Maurizio Deleo, Marco Frigerio, Massimo Losa, Maurizio Velati
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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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Publication number: 20110070192Abstract: Processes for the preparation of racemic and optically active nucleoside analogs of formula (A) are described. These compounds are useful as anti-infective agents, antisense therapeutic agents and hybridization assay probes.Type: ApplicationFiled: November 8, 2004Publication date: March 24, 2011Inventors: Bruno Tse, Borcherng Hong, Wei-Hung Chen, Yea-Fen Jiang, Shuo-Cang Zhang, Subramanian Marappan, Sepehr Sarshar
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Publication number: 20110053891Abstract: This present disclosure is related to the field of 5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: August 5, 2010Publication date: March 3, 2011Applicant: Dow AgroSciences LLCInventors: Timothy A. Boebel, Kristy Bryan, Peter L. Johnson, Beth Lorsbach, Timothy P. Martin, Kevin G. Meyer, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
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Publication number: 20110053918Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: June 27, 2008Publication date: March 3, 2011Inventors: Zhaoning Zhu, William J. Greenlee, Robert D. Mazzola, JR., Jun Qin, Xianhai Huang, Anandan Palani
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Publication number: 20110046104Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: October 30, 2009Publication date: February 24, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Paul Mortimore, Julian M.C. Golec, Daniel David Robinson, John Studley
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Publication number: 20110046370Abstract: Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient. Since the novel indole compound exhibits superior inhibitory activity for various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.Type: ApplicationFiled: August 17, 2010Publication date: February 24, 2011Applicant: Korea Institute of Science and TechnologyInventors: Tae Bo Sim, Young Jin Ham, Kyung Ho Yoo, Chang Hyun Oh, Jung Mi Hah, Hwan Kim, Hwan Geun Choi, Jung-Hun Lee
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Patent number: 7893073Abstract: The invention relates to novel 3,4-dihydropyrimidin-2(1H)-one derivatives having the formula processes for their preparation, and their use in compositions, and in the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: February 15, 2005Date of Patent: February 22, 2011Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Barbara Albrecht, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
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Publication number: 20110039872Abstract: The present application describes deuterium-enriched capecitabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: October 27, 2010Publication date: February 17, 2011Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20110039798Abstract: The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS.Type: ApplicationFiled: July 9, 2008Publication date: February 17, 2011Applicant: EASTERN VIRGINIA MEDICAL SCHOOLInventors: Gustavo F. Doncel, Keykavous Parang, Hitesh Kumar Agarwal
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Patent number: 7888367Abstract: Compounds of the formula (I) wherein: R1 is independently H1—OR3, —NHR4; C1-C4 alkyl; or, when n is 2, adjacent R1 together define an olefinic bond; R2 is H; or when the gem R1 is C1-C4 alkyl, that R2 may also be C1-C4 alkyl; or when the gem R1 is —OR3, that R2 may also be —C(?O)OH or a pharmaceutically acceptable ester thereof; R3 is independently H, or a pharmaceutically acceptable ester thereof; R4 is independently H or a pharmaceutically acceptable amide thereof; R5 and R6 are H or an amine prodrug moiety n is 1, 2 or 3; and pharmaceutically acceptable salts thereof; have utility in the treatment or prophylaxis of HIV, especially reverse transcriptase mutants which allow an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.Type: GrantFiled: July 5, 2006Date of Patent: February 15, 2011Assignee: Medivir ABInventors: Xiao-Xiong Zhou, Christer Sahlberg
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Publication number: 20110034492Abstract: This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: DOW AGROSCIENCES LLCInventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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Publication number: 20110034491Abstract: This present disclosure is related to the field of 5-fluoro-2-oxopyrimidine-1-(2H)-carboxylates and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Inventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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Publication number: 20110034493Abstract: This present disclosure is related to the field of N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: DOW AGROSCIENCES LLCInventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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Publication number: 20110034490Abstract: This present disclosure is related to the field of N1-acyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: DOW AGROSCIENCES LLCInventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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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: 20110009620Abstract: The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient.Type: ApplicationFiled: September 22, 2010Publication date: January 13, 2011Inventors: Masaya Kato, Norifumi Sato, Minoru Okada, Tetsuyuki Uno, Nobuaki Ito, Yasuhiro Takeji, Hisashi Shinohara, Masahiro Fuwa
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Patent number: 7863270Abstract: The invention relates to cyclic hydrazone compounds and compositions including the cyclic hydrazone compounds according to formula (I): The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.Type: GrantFiled: May 12, 2006Date of Patent: January 4, 2011Assignee: Synta Pharmaceuticals Corp.Inventors: Zachary Demko, Lijun Sun, Howard P. Ng
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Publication number: 20100324290Abstract: The present invention relates to a stable crystalline Form I of lamivudine. The present invention further relates to a process for the preparation of the stable crystalline Form (I) of the stable crystalline Form (I) of lamivudine.Type: ApplicationFiled: April 30, 2008Publication date: December 23, 2010Applicant: RANBAXY LABORATORIES LIMITEDInventors: Sayeed Mukhtar, Vishwesh Pravinchandra Pandya, Shivanand Shrishailacpa Kokatnur
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Publication number: 20100324010Abstract: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: ApplicationFiled: October 14, 2008Publication date: December 23, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yasuhiro Imaeda, Takanobu Kuroita, Yoshiyuki Fukase, Shinkichi Suzuki, Michiko Amano
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Publication number: 20100317612Abstract: The subjects of the present invention are the method of preparation of 4-furfurylcytosine and/or its derivatives, its use in the manufacture of anti-aging compositions and an anti-aging composition. As 4-furfurylcytosine and/or its derivatives possesses a series of biological properties it might be use as a composition having excellent anti-aging effect to prevent the sagging of skin and loss of luster and to improve sufficiently its aesthetic appearance without significantly change the growth rate and the total growth ability of the skin. Optimal methods of manufacturing this compound, while at the same time obtaining the highest possible process efficiency, with particular emphasis on its utility in the pharmaceutical and cosmetic industries are presented.Type: ApplicationFiled: November 25, 2008Publication date: December 16, 2010Applicant: INSTYTUT CHEMII BIOORGANICZNEJ PANInventors: Jan Barciszewski, Wojciech T. Markiewicz, Eliza Wyszko, Maria Markiewicz, Monika Nowak, Katarzyna Rolle, Ewelina Adamska, Marcin K. Chimielewski
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Publication number: 20100311970Abstract: The present invention relates to a process for the preparation of substituted 1,3-oxathiolanes. The present invention specifically relates to a process for the preparation of lamivudine.Type: ApplicationFiled: April 30, 2008Publication date: December 9, 2010Applicant: RANBAXY LABORATORIES LIMITEDInventors: Neera Tewari, Dinesh Shashidharan Nair, Hashim Nizar Poovanathil Nagoor Meeran, Mohan Prasad
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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