Polycyclo Ring System Having The Oxazine Ring As One Of The Cyclos Patents (Class 544/99)
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Publication number: 20110207711Abstract: The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.Type: ApplicationFiled: July 27, 2009Publication date: August 25, 2011Inventors: Jason Katz, James Jewell, Joon Jung, Solomon Kattar, Yongquan Hou, Rachel MacCoss, Satoru Ito
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Publication number: 20110207725Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)-group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: April 20, 2011Publication date: August 25, 2011Inventors: George W. Griesgraber, Tushar A. Kshirsagar, Azim A. Celebi, Sara J. Slania, Michael E. Danielson, Michael J. Rice, Joshua R. Wurst
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Publication number: 20110190486Abstract: The invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.Type: ApplicationFiled: March 25, 2011Publication date: August 4, 2011Applicant: ATTO-TEC GMBHInventors: Alexander Zilles, Jutta Arden-Jacob, Karl-Heinz Drexhage, Norbert Uwe Kemnitzer, Monika Hamers-Schneider
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Publication number: 20110186826Abstract: An electroluminescent material comprises the following structural unit: where X is selected from a group consisting of NR, O, S, SO, SO2, CR2, PR, POR, BR, SiR2; where R is a substituent group and Ar1 and Ar2 comprise aromatic rings; and, wherein Ar1 or Ar2 is fused to a further aryl system Ar3. An optical device comprises a first electrode for injection of positive charge carriers, a second electrode for injection of negative charge carriers and a layer located between the first and second electrode comprising the electroluminescent material.Type: ApplicationFiled: July 23, 2009Publication date: August 4, 2011Applicants: CAMBRIDGE DISPLAY TECHNOLOGY LIMITED, SUMATION COMPANY LIMITEDInventors: Annette Steudel, Thomas Pounds
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Publication number: 20110184168Abstract: Reactive fluorescent dyes compositions and methods of using same are disclosed. Squaraine nucleus, Nile Red nucleus, benzodioxazole nucleus, coumarin nucleus or aza coumarin nucleus dyes are disclosed having thiol-reactive groups. Squaraine nucleus, Nile Red nucleus, benzodioxazole nucleus, coumarin nucleus or aza coumarin nucleus dyes are disclosed that exhibit a fluorescence emission of at least about 575 nm. Biosensors are disclosed having a binding protein and a squaraine nucleus, Nile Red nucleus, benzodioxazole nucleus, coumarin nucleus or aza coumarin nucleus.Type: ApplicationFiled: June 22, 2009Publication date: July 28, 2011Applicant: Becton, Dickinson and CompanyInventors: J. Bruce PITNER, Douglas B. SHERMAN, K. Joseph THOMAS
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Patent number: 7943609Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)-group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: December 29, 2005Date of Patent: May 17, 2011Assignee: 3M Innovative Proprerties CompanyInventors: George W. Griesgraber, Tushar A. Kshirsagar, Azim A. Celebi, Sarah J. Slania, Michael E. Danielson, Michael J. Rice, Joshua R. Wurst
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Publication number: 20110111446Abstract: It is an object of the present invention to provide: a novel thiol-detecting reagent, which can be used in vivo and which solves the problem regarding the generation of background fluorescence due to hydrolysis; and a method for detecting thiol using the aforementioned reagent. The present invention provides a compound represented by the following formula (1): wherein each R2 independently represents an alkyl group containing 1 to 6 carbon atoms, a halogen atom, or a hydrogen atom.Type: ApplicationFiled: January 30, 2009Publication date: May 12, 2011Applicant: RIKENInventors: Hiroshi Abe, Yoshihiro Ito, Aya Shibata, Mika Ito
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Publication number: 20110065687Abstract: This application relates to certain novel polycyclic compounds that interact with quadruplex-forming regions of polynucleotides and thereby inhibit translation of genetic information into polypeptides. These compounds can thus provide anticancer and antibacterial and antiviral effects. The invention includes novel compounds and pharmaceutical compositions, and methods of using them to treat cancer and other conditions.Type: ApplicationFiled: April 17, 2008Publication date: March 17, 2011Inventors: Michael Schwaebe, Johnny Yasuo Nagasawa, Mustapha Haddach
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Patent number: 7906506Abstract: Substituted fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) with a —CH(—R2)— group in the fused ring at the 2-position of the imidazo ring and a —CH(—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: July 12, 2007Date of Patent: March 15, 2011Assignee: 3M Innovative Properties CompanyInventors: George W. Griesgraber, Sarah C. Johannessen Slania
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Patent number: 7892345Abstract: The invention accordingly relates to a method for preparing transparent C.I. Pigment Violet 23 by salt kneading a Pigment Violet 23-crude in the presence of a crystalline salt and an organic liquid. Said method is characterized in that the organic liquid is propylene carbonate.Type: GrantFiled: February 28, 2008Date of Patent: February 22, 2011Assignee: Clariant Finance (BVI) LimitedInventors: Wolfgang Hoyer, Leonhard Unverdorben
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Patent number: 7884099Abstract: The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given.Type: GrantFiled: November 12, 2008Date of Patent: February 8, 2011Assignee: Cumbre IP Ventures, L.P.Inventors: Charles Z. Ding, Yafei Jin, Keith Combrink, In Ho Kim
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Publication number: 20110021450Abstract: Provided is a medicinal composition, in particular, a medicinal composition for treatment and/or prevention which has a high therapeutic effect on infection with a parasitic protozoa and a selective toxicity thereto and exhibits a life-prolonging effect and so on. A medicinal composition which contains as the active ingredient a benzo[a]phenoxazine compound represented by General formula (1) or a salt compound of the same, in particular, an agent for treating and/or preventing infection with a protozoa such as malaria, leishmaniasis, African trypanosomiasis, Chagas disease, toxoplasmosis, lymphatic filariasis, babesiosis or coccidium disease; and a novel compound which is contained therein as the active ingredient.Type: ApplicationFiled: March 11, 2009Publication date: January 27, 2011Applicants: HOSHI UNIVERSITY, SYNSTAR JAPAN CO., LTD., SWISS TROPICAL AND PUBLIC HEALTH INSTITUTEInventors: Masataka Ihara, Jian-Feng Ge, Chika Arai, Mei Yang, Isamu Itoh, Reto Brun
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Publication number: 20110014196Abstract: The invention relates to compounds comprising a plurality of enzyme substrates suitably linked and further carrying one or more cargo entities. In particular such compounds have the structure (substrate)n-linker-(cargo)m wherein “substrate” is a substrate specific for an enzyme-type protein; n is 2 or more; “linker” is a linking unit consisting of 1 to 300 atoms; “cargo” is a drug, a label detectable by a fluorescence detector, magnetic resonance imaging (MRI), positron emission tomography (PET) or scintigraphy, or a functional group which can be transformed into a drug or a detectable label; and m is 1 or more. The invention further relates to a corresponding molecular shuttles having the structure (fusion protein)n-linker-(cargo)m wherein “fusion protein” is a proteinaceous binding entity fused to an enzyme-type protein for which specific substrates exist. The proteinaceous binding entity is designed to bind to a target structure in vitro or in vivo, for example a cellular receptor.Type: ApplicationFiled: October 2, 2008Publication date: January 20, 2011Applicant: COVALYS BIOSCIENCES AGInventors: Andreas Brecht, Florent Beaufils
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Publication number: 20110009536Abstract: The present invention is directed to a new C.I. Pigment Violet 37 in rod-like form, a process for its preparation and its use for coloring high molecular weight organic material. The C.I. Pigment Violet 37 in rod-like form having a length of 0.5 to 30 ?m, a width of 0.05 to 1 ?m, especially 0.100 to 0.500 ?m and an average thickness of 0.01 to 0.200 ?m, especially 0.03 to 0.100 ?m.Type: ApplicationFiled: December 4, 2007Publication date: January 13, 2011Applicant: CIBA CORPORATIONInventors: Marc Maurer, Niklaus Raetzo
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Publication number: 20100323396Abstract: A reagent for measuring platelets comprising Nile Blue hydrogensulfate, or Nile Blue and an acid, a reagent kit for measuring platelets comprising the reagent for measuring platelets, and a method for measuring platelets using the reagent or reagent kit.Type: ApplicationFiled: February 17, 2009Publication date: December 23, 2010Inventors: Yuhgi Suzuki, Keiko Moriyama, Yusuke Mori, Hiroki Takeshita
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Publication number: 20100297684Abstract: Novel, activatable dyes, such as photoactivatable dyes, e.g., oxazine dyes, are described. Some of the dyes are targeting dyes that can, e.g., target biomolecules, such as polypeptides, proteins, or nucleic acids. Upon activation, such as by irradiation, the novel dyes rapidly turn on their fluorescence and emit light, such as near-IR light with spatial and temporal precision.Type: ApplicationFiled: September 12, 2008Publication date: November 25, 2010Inventor: Stephen C. Miller
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Publication number: 20100298308Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.Type: ApplicationFiled: November 14, 2006Publication date: November 25, 2010Inventors: Dianqing (Dan) Wu, Dakai Liu, James J. Donegan
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Patent number: 7816519Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.Type: GrantFiled: November 16, 2006Date of Patent: October 19, 2010Assignee: Life Technologies CorporationInventors: Zhenjun Diwu, Jixiang Liu, Kyle Gee
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Patent number: 7816406Abstract: The present invention provides quinolone analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing quinolone analogs, and methods of using the same.Type: GrantFiled: September 16, 2005Date of Patent: October 19, 2010Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Fabrice Pierre, Collin Regan, Michael Schwaebe, Johnny Y. Nagasawa, Peter Chua
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Publication number: 20100222302Abstract: The invention relates to novel chimeric antibiotics of formula I wherein R1 is CH2NHCOR5, heteroarylmethyl, heteroaryloxymethyl or heteroarylaminomethyl; R2 is H, OH, OSO3H, OPO3H2, OCH2OPO3H2, OCOCH2CH2COOH, OCOR6; R3 is H or halogen; R4 is (C1-C3)alkyl, (C1-C3)haloalkyl or cycloalkyl; R5 is alkyl or haloalkyl; and R6 is the residue of a naturally occurring amino acid or of dimethylaminoglycine. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).Type: ApplicationFiled: August 7, 2006Publication date: September 2, 2010Inventors: Christian Hubschwerlen, Philippe Panchaud, Christine Sigwalt, Jean-Luc Specklin
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Publication number: 20100210452Abstract: This invention provides a convenient method for converting imines and other electrophiles into heterocyclic ring systems. The process does not require the use of metallic reagents, and is catalyzed by an organic heterocyclic carbene catalyst. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. Chiral heterocyclic carbene catalysts of the invention and methods of using these catalysts produce chiral heterocycles in high enantiomeric and diastereomeric excess.Type: ApplicationFiled: April 23, 2007Publication date: August 19, 2010Applicant: The Regents of the University of CaliforniaInventors: Jeffrey Bode, Ming He, Justin Struble
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Patent number: 7749994Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.Type: GrantFiled: August 14, 2006Date of Patent: July 6, 2010Assignees: Genentech, Inc., Hoffman-LaRoche, Inc. (US Only), F. Hoffman-LaRoche, AG (EX-US)Inventors: Thomas E. Rawson, Brian Safina, Jennafer Dotson, Aihe Zhou, Ignacio Aliagas-Martin, Jason Halladay, Jun Liang, Matthias Rueth, Bing-Yan Zhu, Frederick Brookfield, Michael Prime, Birong Zhang, Jun M. Li
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Publication number: 20100119709Abstract: Compositions and methods useful for imparting coloration to various substrates including plastics, paper, wood, fabrics, fibers and textiles. Materials comprising water-soluble colorants including an amidine group and a chromophore moiety are contacted with a substrate, and the substrate permitted to dry to provide substantially water-proof coloration on the substrate. In one embodiment an ink, coating, or dye is an aqueous composition comprising one or more amidines as provided herein, which is contained within a vessel that includes a gas at an effective level of pressure to enable the gas to react with an amidine as herein provided, to provide and maintain the amidine substantially in its protonated form prior to application of the aqueous composition to a desired substrate.Type: ApplicationFiled: November 8, 2008Publication date: May 13, 2010Inventor: Sean Michael Ragan
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Patent number: 7695930Abstract: The present invention relates to methods for the detection, identification and/or quantification of microorganisms with peptidase activity using enzymatic substrates with the following general formula:Type: GrantFiled: July 22, 2008Date of Patent: April 13, 2010Assignee: BiomerieuxInventors: Arthur James, John Perry, Annette Rigby, Stephen Stanforth
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Publication number: 20100081654Abstract: Compounds with cancer cell specific lethality are provided. In particular, RAS-selective lethal compounds and compositions are provided. Also provided are methods of screening for such compounds and methods of treating a condition in a mammal, by administering to the mammal a therapeutically effective amount of such compounds or compositions.Type: ApplicationFiled: August 21, 2009Publication date: April 1, 2010Inventors: Brent R. Stockwell, Wan Seok Yang, Rohitha SriRamaratnam
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Publication number: 20100069376Abstract: The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen; R4 is H, (C1-C3)alkyl, or cycloalkyl; R5 represents piperidin-4-yl or R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; n is 0 or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula I. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).Type: ApplicationFiled: November 23, 2007Publication date: March 18, 2010Applicant: Actelion Pharmaceuticals, Ltd.Inventors: Christian Hubschwerlen, Philippe Panchaud, Jean-Luc Specklin
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Patent number: 7652134Abstract: The present invention relates to methods of preparing compounds having formula (1), (2), (5), and ((6A)-(6D)) comprising contacting the corresponding ester, an amine with formula NHR1R2, and a Lewis acid having formula MLn, wherein L is a halogen atom or an organic radical, n is 3-5, and M is a group III elemental atom, a group IV elemental atom, As, Sb, V or Fe, wherein A, B, V, X, Z, W, R1, R2, R5, Z1, Z2, Z3, Z4, Z5, Z6, Z7, and Z8 are substituents. Z4, Z5, Z6, Z7, and Z8 are substituents.Type: GrantFiled: June 9, 2005Date of Patent: January 26, 2010Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Fabrice Pierre, Collin Regan, Michael Schwaebe, George Petros Yiannikouros, Michael Jung
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Publication number: 20100003763Abstract: Reactive fluorescent dyes compositions and methods of using same are disclosed. Squaraine nucleus, Nile Red nucleus, benzodioxazole nucleus, coumarin nucleus or aza coumarin nucleus dyes are disclosed having thiol-reactive groups. Squaraine nucleus, Nile Red nucleus, benzodioxazole nucleus, coumarin nucleus or aza coumarin nucleus dyes are disclosed that exhibit a fluorescence emission of at least about 575 nm. Biosensors are disclosed having a binding protein and a squaraine nucleus, Nile Red nucleus, benzodioxazole nucleus, coumarin nucleus or aza coumarin nucleus.Type: ApplicationFiled: June 22, 2009Publication date: January 7, 2010Applicant: Becton, Dickinson and CompanyInventors: J. Bruce Pitner, Douglas B. Sherman, Arounaguiry Ambroise, K. Joseph Thomas
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Publication number: 20090325946Abstract: The present invention relates to novel phenolic and catecholic amines of Formula I, to processes for their preparation, pharmaceutical compositions containing them, to their use in therapy and to their use in radiolabeled form as PET- or SPECT ligands.Type: ApplicationFiled: June 24, 2009Publication date: December 31, 2009Applicant: H. Lundbeck A/SInventors: Ask PUSCHL, Morten JORGENSEN, Benny BANG-ANDERSEN
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Patent number: 7629458Abstract: The invention provides a method for preparing levofloxacin hemihydrate, comprising: maintaining levofloxacin at a first elevated temperature in a first solvent; adding a polar solvent to precipitate the levofloxacin hemihydrate, wherein the polar solvent comprises water; and recovering the levofloxacin hemihydrate. The invention also provides a method of converting a levofloxacin form to levofloxacin hemihydrate, comprising storing one or more forms selected from the group consisting of Forms A, B, C, F, G and H for a sufficient time to permit the one or more forms to convert to levofloxacin hemihydrate.Type: GrantFiled: October 3, 2002Date of Patent: December 8, 2009Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Valerie Niddam-Hildesheim, Neomi Gershon, Ehud Amir, Shlomit Wizel
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Patent number: 7612063Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.Type: GrantFiled: January 14, 2008Date of Patent: November 3, 2009Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terence Moran
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Publication number: 20090229059Abstract: Disclosed are oxazine disulfide dyes of formula (1) D1-(Z1)r-Y1—S-A, wherein A is hydrogen; or a radical of formula (1a)*—S—Y2-(Z2)r-D2; Y1 and Y2 independently from each other are unsubstituted or substituted, straight-chain or branched, interrupted or uninterrupted C—1—C—10alkylene; C5-C10cycloalkylene; C5-C10arylene; or —C5-C10arylene-(C1-C10alkylene); Z1 and Z2 independently from each other are *—(CH2)p—C(O)—**; *—(CH2CH2—O)S—**; *—(CH2)p—C(O)O—**; *—(CH2)p—OCO—**; *—(CH2)P—N(R1)—**; formula 1(g); —(CH2)p—CON(R1)—**; *—(CH2)p—(R1)NC(O)—**; , 0-; —S—; —S(O)—; —S(O)2—; or a cationic biradical of a substituted or unsubstituted aromatic or heteroaromatic compound of the formula (1a); (1b); (1c); (1d); or (1e); wherein the asterix * indicates the linkage to D1 and/or D2; the asterix ** indicates the linkage to Y1 and/or Y2; W1 is N or a radical of CR5; R1, R2, R3, R4 and R5 independently from each other are hydrogen; C1-C14alkyl; C2-C14alkenyl; C5-C10aryl; C5-C10aryl-(C1-C10alkyl); or —C1-C10alkyl(C5-C10aryl);Type: ApplicationFiled: September 27, 2006Publication date: September 17, 2009Inventors: Christian Cremer, Olof Wallquist
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Publication number: 20090226948Abstract: The present invention relates to a time temperature indicator for indicating temperature change over time, comprising an immobilized enzyme and a substrate of the enzyme, wherein the reaction of the substrate catalyzed by the enzyme produces a reaction product in a time and temperature dependent manner and wherein the formation of the reaction product can be detected by monitoring a physical characteristic of the substrate and/or the product which is linked to its concentration. The invention further relates to a method of time temperature indication comprising the step of an enzyme-catalyzed reaction, a method of printing the enzyme-based time temperature indicator on a packaging material or a label, a printing ink or printing ink concentrate comprising components of the enzyme-based time temperature indicator and a packaging material or a label comprising the enzyme-based time temperature indicator.Type: ApplicationFiled: August 3, 2005Publication date: September 10, 2009Inventors: Hans Reichert, Peter Simmendinger, Thomas Bolle
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Publication number: 20090215761Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, W, X, Z, B, L, R1, R3, R4 and R5 are substituents. The present invention also relates to methods for using such compounds.Type: ApplicationFiled: June 30, 2008Publication date: August 27, 2009Applicant: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Fabrice Pierre, Michael Schwaebe
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Publication number: 20090192298Abstract: The present disclosure relates, according to some embodiments, to compositions, systems, and methods for preparing and using fluorescent through-bond energy transfer cassettes.Type: ApplicationFiled: November 13, 2008Publication date: July 30, 2009Inventor: Kevin Burgess
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Publication number: 20090137575Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.Type: ApplicationFiled: December 17, 2008Publication date: May 28, 2009Inventors: Duane A. Burnett, Wen-Lian Wu
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Patent number: 7514427Abstract: HIV inhibitory compounds of formula: salts and stereoisomers thereof, wherein R1 and R2 are hydrogen or optionally substituted C1-10alkyl; R3 is n is 1, 2 or 3; R3a is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, aminocarbonyl, C 1-4alkyloxycarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C1-4alkylcarbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het; or R3 is a monocyclic or bicyclic aromatic heterocyclic ring system, wherein one, two, three or four ring members are nitrogen, oxygen and sulfur, and wherein the remaining ring members are carbon atoms; and wherein each of said heterocyclic ring systems may optionally be substituted; X is —NR7—, —O— or —S—; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.Type: GrantFiled: January 10, 2006Date of Patent: April 7, 2009Assignee: Tibotec Pharmaceuticals, Ltd.Inventors: Bart Rudolf Romanie Kesteleyn, Pierre Jean-Marie Raboisson, Wim Van De Vreken, Maxime Francis Jean-Marie Ghislain Canard
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Publication number: 20090012071Abstract: The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound as the only active agent or in combination with one or more other active agents.Type: ApplicationFiled: April 23, 2008Publication date: January 8, 2009Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Barton James Bradbury, Milind Deshpande, Akihiro Hashimoto, Ha Young Kim, Edlaine Lucien, Godwin Pais, Michael John Pucci, Qiuping Wang, Jason Allan Wiles
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Publication number: 20090005371Abstract: Fused [1,2]imidazo[4,5-c] ring compounds, e.g., fused [1,2]imidazo[4,5-c]quinolines and [1,2]imidazo[4,5-c]naphthyridines, with a substituent, e.g., a substituted alkoxy substituent, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: February 10, 2006Publication date: January 1, 2009Inventors: Michael J. Rice, Bryon A. Merrill, Philip D. Heppner
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Patent number: 7470683Abstract: Compounds of formula I, of trans relative configuration: wherein: X represents an oxygen atom or an NR2 group, Y represents a group selected from —CH2—, —(CH2)2— and —CH?CH—, R1 and R2, which may be the same or different, each represents a hydrogen atom or a group selected from alkyl, cycloalkyl and cycloalkylalkyl, in racemic form or in the form of optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof. Medicinal products containing the same which are useful in the treatment of disorders of the central nervous system that involve the dopaminergic system.Type: GrantFiled: September 25, 2007Date of Patent: December 30, 2008Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Mark Millan, Mauricette Brocco
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Patent number: 7462717Abstract: The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising themType: GrantFiled: August 19, 2003Date of Patent: December 9, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Encarnacion Matesanz-Ballesteros, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Petrus Megens
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Publication number: 20080269192Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)-group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: December 29, 2005Publication date: October 30, 2008Applicant: Coley Pharmaceutical Group, Inc.Inventors: George W. Griesgraber, Tushar A. Kshirsagar, Azim A. Celebi, Sarah J. Slania, Michael E. Danielson, Michael J. Rice, Joshua R. Wurst
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Patent number: 7435823Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: January 24, 2005Date of Patent: October 14, 2008Assignee: Amgen Inc.Inventors: Michele Potashman, Tae-Seong Kim, Steven Bellon, Shon Booker, Yuan Cheng, Joseph L. Kim, Andrew Tasker, Ning Xi, Shimin Xu, Jean-Christophe Harmange, George Borg, Matthew Weiss, Brian L. Hodous, Russell Graceffa, William H. Buckner, Craig E. Masse, Deborah Choquette, Matthew W. Martin, Julie Germain, Lucian V. DiPietro, Stuart C. Chaffee, Joseph J. Nunes, John L. Buchanan, Gregory J. Habgood, David C. McGowan, Douglas A. Whittington, Daniel La, Vinod F. Patel
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Patent number: 7432372Abstract: The invention provides novel fluorinated resorufin compounds that are of use in a variety of assay formats. Also provided are methods of using the compounds and kits that include a compound of the invention and instructions detailing the use of the compound in one or more assay formats.Type: GrantFiled: November 1, 2004Date of Patent: October 7, 2008Assignee: Invitrogen CorporationInventors: Robert Hardy Batchelor, Yue Ge, Iain D. Johnson, Wai-Yee Leung, Jixiang Liu, Brian Patch, Peter Aaron Emrys Smalley, Thomas Harry Steinberg
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Patent number: 7425628Abstract: The invention provides a process for preparing levofloxacin hemihydrate, comprising: (A) dissolving levofloxacin in a solvent selected from the group consisting of acetonitrile, acetonitrile:H2O, dimethyl sulfoxide, dimethyl sulfoxide:H2O, methyl ethyl ketone, methyl ethyl ketone:H2O, butanol, butanol:H2O, and mixtures thereof at an elevated temperature; and (B) crystallizing levofloxacin hemihydrate.Type: GrantFiled: November 27, 2002Date of Patent: September 16, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Valerie Niddam-Hildesheim, Neomi Gershon, Eduard Schwartz
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Patent number: 7420054Abstract: The present invention relates to novel enzymatic substrates with the following general formula: where R1, R2, R3, R4, R5, R6, A and X are as defined in claim 1, the reaction media comprising the same and the use thereof for the detection and/or identification and/or quantification of microorganisms expressing at least one peptidase activity.Type: GrantFiled: May 13, 2004Date of Patent: September 2, 2008Assignee: bioMerieuxInventors: Arthur James, John Perry, Annette Rigby, Stephen Stanforth
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Patent number: 7402579Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, W, X, Z, B, L, R1, R3, R4 and R5 are substituents. The present invention also relates to methods for using such compounds.Type: GrantFiled: April 14, 2006Date of Patent: July 22, 2008Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Fabrice Pierre, Michael Schwaebe
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Publication number: 20080167296Abstract: HIV inhibitory compounds of formula: salts and stereoisomers thereof, wherein R1 and R2 are hydrogen or optionally substituted C1-10alkyl; R3 is n is 1, 2 or 3; R3a is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, aminocarbonyl, CI 4alkyloxycarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C1-4alkylcarbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het; or R3 is a monocyclic or bicyclic aromatic heterocyclic ring system, wherein one, two, three or four ring members are nitrogen, oxygen and sulfur, and wherein the remaining ring members are carbon atoms; and wherein each of said heterocyclic ring systems may optionally be substituted; X is —NR7—, —0— or —S—; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.Type: ApplicationFiled: January 10, 2006Publication date: July 10, 2008Inventors: Bart Rudolf Romanie Kesteleyn, Pierre Jean-Marie Raboisson, Wim Van De Vreken, Maxime Francis Jean-Marie Ghislain Canard
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Patent number: 7381720Abstract: The present invention relates to methods for ameliorating a cell proliferative disorder using quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents.Type: GrantFiled: May 10, 2006Date of Patent: June 3, 2008Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terrance Moran
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Patent number: 7354916Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.Type: GrantFiled: July 30, 2004Date of Patent: April 8, 2008Assignee: Cylene PharmaceuticalsInventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terence Moran