The Additional Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 514/337)
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Publication number: 20110086877Abstract: Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain in a subject, and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.Type: ApplicationFiled: October 1, 2010Publication date: April 14, 2011Inventors: SINA BAVARI, RICK GUSSIO, JAMES C. BURNETT
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Publication number: 20110082098Abstract: Novobiocin analogues are useful in methods of treating, inhibiting, and/or preventing cyst formation in autosomal dominant polycystic kidney disease (ADPKD) in a subject. The disclosure provides methods of treating ADPKD comprising administering a therapeutically effective amount of a coumarin-3-carboxamide novobiocin analogue. Accordingly, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of mTOR pathway phosphoproteins P-mTOR, P-Akt and P-S6K, or combinations thereof. Further, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of Hsp-90 client proteins CFTR, ErbB2, c-Raf and Cdk4, or combinations thereof.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: UNIVERSITY OF KANSASInventors: James P. Calvet, Brian S.J. Blagg, Shirin V. Sundar, Brenda S. Magenheimer
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Patent number: 7919509Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: February 27, 2009Date of Patent: April 5, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Hidefumi Ozawa, Ayako Tosaka, Koichi Yamazaki, Yuki Yamaguchi, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Publication number: 20110076318Abstract: Biocompatible intraocular implants include a retinoid component and a biodegradable polymer that is effective to facilitate release of the retinoid component into an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Inventors: Patrick M. Hughes, Orest Olejnik, Glenn Tony Huang, Joan-En Chang-Lin, Thierry Nivaggioli, JaneGuo Shiah, Michele Boix, Christian Sarrazin
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Patent number: 7915295Abstract: Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from —S(?O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(?O)ORx, —NRxOH; —C(?O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(?O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(?O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(?O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)q-O—Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, —S(?O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8?)n-D-(CR8R8?)m-; D is a bond, —NR9—, -0-, —S—, —S(=0)- or —S(=0)2-; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.Type: GrantFiled: December 30, 2004Date of Patent: March 29, 2011Assignee: Medivir ABInventors: Christian Sund, Nathalie Roue, Stefan Lindstrom, Dmitry Antonov, Christer Sahlberg, Katarina Jansson
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Publication number: 20110071193Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.Type: ApplicationFiled: September 22, 2010Publication date: March 24, 2011Applicant: Sergeant's Pet Care Products, Inc.Inventor: Larry Nouvel
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Publication number: 20110065676Abstract: The present invention is directed to a pharmaceutical composition comprising an effective amount of at least one PAR1 antagonist, at least one NAR agonist, optionally, an effective amount of at least one cardiovascular agent, and, optionally, a pharmaceutically acceptable carrier. The present invention also provides for the use of theses pharmaceutical compositions to treat various diseases associated with thrombosis.Type: ApplicationFiled: June 22, 2010Publication date: March 17, 2011Applicant: Schering CorporationInventors: Michael Sidney Perelman, Madhu Chintala
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Publication number: 20110065710Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: December 2, 2004Publication date: March 17, 2011Inventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
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Patent number: 7902228Abstract: Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.Type: GrantFiled: February 4, 2008Date of Patent: March 8, 2011Assignees: University of Iowa Research Foundation, The United States of America, National Institute of HealthInventors: David F. Wiemer, Jeffrey D. Neighbors, John A. Beutler
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Publication number: 20110052643Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: January 7, 2009Publication date: March 3, 2011Applicant: Synta Pharmaceuticals Corp.Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen, Lijun Sun
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Publication number: 20110044938Abstract: Compounds of a certain formula I, in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.Type: ApplicationFiled: August 15, 2007Publication date: February 24, 2011Applicant: NYCOMED GMBHInventors: Bjorn Bartels, Mathias Schmidt, Klaus Pekari, Thomas Beckers, Astrid Zimmermann, Volker Gekeler
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Publication number: 20110046139Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor.Type: ApplicationFiled: April 27, 2009Publication date: February 24, 2011Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
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Publication number: 20110039821Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: October 27, 2010Publication date: February 17, 2011Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
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Publication number: 20110021540Abstract: The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: January 27, 2011Applicant: ASTRAZENECA ABInventors: Johan Bylund, Maria Ek, Jorg Holenz, Martin H. Johansson, Annika Kers, Katja Narhi, Gunnar Nordvall, Liselotte Ohberg, Daniel Sohn, Jenny Viklund, Stefan Von Berg
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Publication number: 20110020457Abstract: A polymer-surfactant nanoparticle formulation, using the anionic surfactant aerosol OT (AOT) and polysaccharide polymer alginate, is used for sustained release of water-soluble drugs. The AOT-alginate nanoparticles are suitable for encapsulating doxorubicin, verapamil and clonidine, as well as therapeutic agents effective against dermal conditions such as psoriasis. The nanoparticles are also suitable for encapsulating photo-activated compounds such as methylene blue for use in photo-dynamic therapy of cancer and other diseases, and for treating tumor cells that exhibit resistance to at least one chemotherapeutic drug.Type: ApplicationFiled: August 14, 2007Publication date: January 27, 2011Inventors: Jayanth Panyam, Mahesh D. Chavanpatil
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Publication number: 20110021563Abstract: The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.Type: ApplicationFiled: November 18, 2008Publication date: January 27, 2011Applicants: Howard Florey Institute, St. Vincent's Institute of Medical ResearchInventors: Siew Yeen Chai, Michael William Parker, Anthony Lloyd Albiston, Frederick A.O. Mendelsohn, Keith Geoffrey Watson
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Publication number: 20110015185Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: ApplicationFiled: September 28, 2010Publication date: January 20, 2011Applicant: BIOVITRUM ABInventors: Gary Johansson, Peter Brandt, Björn M. Nilsson
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Patent number: 7872030Abstract: (R/S)-(?/+)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane or a physiologically acceptable salt thereof and/or (S)-(+)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane or a physiologically acceptable salt thereof are used for the manufacture of a medicament for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders.Type: GrantFiled: July 10, 2002Date of Patent: January 18, 2011Assignee: Merck Patent GmbHInventors: Gerd Bartoszyk, Herman Russ, Christoph Seyfried, Frank Weber
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Patent number: 7872011Abstract: The present invention relates to selective inhibitors of phosphoinositide (PI) 3-kinase ?, use of the selective inhibitors in anti-thrombotic therapy, and a method for screening compounds useful for the new anti-thrombotic therapy by detecting selective inhibitory activity of PI 3-kinase ? of the compound. The invention also relates to novel compounds that are inhibitors of PI 3-kinase.Type: GrantFiled: December 27, 2007Date of Patent: January 18, 2011Assignee: AstraZeneca ABInventors: Shaun P. Jackson, Alan D. Robertson, Vijaya Kenche, Philip Thompson, Hishani Prabaharan, Karen Anderson, Belinda Abbott, Isaac Goncalves, Warwick Nesbitt, Simone Shoenwaelder, Dilek Saylik
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Publication number: 20110009447Abstract: Substituted benzoic acid amides of formula (I) and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of benzoic acid amides are described.Type: ApplicationFiled: April 24, 2001Publication date: January 13, 2011Inventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch
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Publication number: 20110009455Abstract: The present invention relates to novel compounds of general formula (I) and uses thereof. The present invention relates to novel compounds of general formula (I) for use as glucokinase activators in the treatment of diabetes and obesity.Type: ApplicationFiled: February 5, 2009Publication date: January 13, 2011Applicant: Merck Patent GesellschaftInventors: Christoph Saal, Lars Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
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Patent number: 7868024Abstract: The invention relates to compounds of formula (I): Wherein X1, X2, X3, X4, Y and W are as described herein. The invention also relates to a preparation method and to a therapeutic application.Type: GrantFiled: July 17, 2009Date of Patent: January 11, 2011Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, André Malanda, Christian Maloizel
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Publication number: 20110002918Abstract: Treatment protocols for severe psoriasis include administering biologics, stopping all administration of the biologics after the severity of the psoriasis has reduced and has reached an equilibrium, mildness and/or a tolerable state of remission, and administering UV phototherapy. The biologics may include, for example, the biologics found in Amevive®, Enbrel®, Humira®, Raptiva®, and Remicade® and/or alefacept, etanercept, adalimumab, efalizumab, infliximab, and ustekinumab. The UV phototherapy may be repeated, for example daily, weekly, monthly, yearly, to keep the psoriasis in a mild state or in a tolerable state of substantial remission. Parameters for administering UV phototherapy may be determined based on skin tone, Fitzpatrick skin phenotype, the severity of the psoriasis, the area of exposure, and/or the MED.Type: ApplicationFiled: March 5, 2010Publication date: January 6, 2011Applicant: PHOTOMEDEXInventor: Jeffrey I. Levatter
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Publication number: 20110003861Abstract: 2-aryl and 2-heteroaryl 4h-1-benzopyran-4-one-6-amidino derivatives of formula (I) useful as pharmacological agents for the treatment of arthritis, cancer and related pain.Type: ApplicationFiled: March 6, 2008Publication date: January 6, 2011Applicant: ROTTAPHARM S.P.A.Inventors: Antonio Giordani, Ilario Verpilio, Sabrina Pucci, Roberto Artusi, Gianfranco Caselli, Marco Lanza, Laura Mennuni, Francesco Makovec, Lucio Claudio Rovati
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Publication number: 20100331370Abstract: Isobenzofuran analogs of sclerophytin A are prepared in a highly concise fashion via an aldol-cycloaldol sequence. The analogs exhibit IC50's as low as 1 ?M in growth inhibitory studies against KB3 cells using an MTT assay. Preferred analogs have one of the following structural formulas, where R is hydrogen or a substituted or unsubstituted lower alkyl group and Ar is a substituted or unsubstituted aryl group.Type: ApplicationFiled: June 30, 2010Publication date: December 30, 2010Inventor: Matthias C. McIntosh
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Publication number: 20100331323Abstract: The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Inventors: Daniel L. Comins, Florence F. Wagner, Pauline Ondachi
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Publication number: 20100324094Abstract: A method for synthesizing anti-leukemic epothilone analogues includes rigidifying a region between the macrolactone ring and the aromatic side-chain. The anti-leukemic compositions are non-naturally occurring epothilone analogue that are rigidified between the macrolactone ring and the aromatic side-chain.Type: ApplicationFiled: March 20, 2008Publication date: December 23, 2010Applicant: The University of ToledoInventors: Viranga Tillekeratne, Richard A. Hudson, Mamoun Alhamadsheh
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Publication number: 20100317699Abstract: The invention provides methods for the diagnosis and treatment of musculoskeletal disorders relating to the Hedgehog pathway, including but not limited to muscular dystrophy (e.g., Duchenne Muscular Dystrophy) using agents that agonize Sonic Hedgehog (shh), and thereby, the Hedgehog signaling pathway. Said agonizing agents include, e.g., the compounds of the invention (e.g., a compound of Formula I). The invention also provides methods of screening for agents that are capable of increasing the proliferation of muscle and/or muscle precursor cells.Type: ApplicationFiled: January 27, 2009Publication date: December 16, 2010Applicant: NOVARTIS AGInventors: Dustin Donald Armstrong, Shilpa Kadam
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Patent number: 7851490Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: GrantFiled: April 7, 2006Date of Patent: December 14, 2010Assignee: Neurosearch A/SInventors: Janus S. Larsen, Lene Teuber, Philip K. Ahring, Elsebet Østergaard Nielsen, Naheed Mirza
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Publication number: 20100311582Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.Type: ApplicationFiled: January 23, 2009Publication date: December 9, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Thomas Pitterna, Peter Renold, Ottmar Franz Hueter, Peter Maienfisch, Werner Zambach
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Publication number: 20100297073Abstract: Compounds having the formula I wherein wherein R1, R2, R3b, R4a, R4b, R4c and as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: May 20, 2010Publication date: November 25, 2010Inventors: Elbert Chin, Jim Li, Albert Sui-Ting Lui, Francisco Xavier Talamas
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Patent number: 7838537Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: November 30, 2007Date of Patent: November 23, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Marc-André Poupart, Pierre Louis Beaulieu, Jean Rancourt
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Publication number: 20100292227Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBHInventors: CHRISTIANE YOAKIM, MURRAY BAILEY, FRANCOIS BILODEAU, REBEKAH CARSON, LEE FADER, STEPHEN KAWAI, SEBASTIEN MORIN, CARL THIBEAULT, BRUNO SIMONEAU, SIMON SURPRENANT, YOULA TSANTRIZOS, STEVEN LAPLANTE
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Publication number: 20100292218Abstract: The present invention provides compounds of formulae Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va and the therapeutic use thereof. The present invention also includes methods of treating NF2-deficient or NF1-deficient cells or neurodegenerative diseases with radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va. Furthermore, the present invention is directed to methods of inhibiting the growth of NF2-deficient or NF1-deficient tumors. The methods comprise contacting NF2-deficient or NF1-deficient tumor cells with radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va. The present invention is also directed to the combinational use of radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va with at least one additional active agent, such as one or more HSP90 inhibitors.Type: ApplicationFiled: December 4, 2009Publication date: November 18, 2010Inventors: Ruihong CHEN, Allan E. Rubenstein, Jin-Chen Yu, Nicolas Winssinger, Sofia Barluenga
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Publication number: 20100292190Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: February 14, 2006Publication date: November 18, 2010Applicant: Bionomics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Patent number: 7829585Abstract: The present invention provides an antifungal agent that has superior antifungal action and is also superior in terms of physical properties, safety and metabolic stability. The present invention discloses a compound represented by the formula (I): (wherein X represents an oxygen atom, a sulfur atom or —NH—, R1 represents a hydrogen atom, a halogen atom, a cyano group, an amino group or a substituent, and R2 and R3 independently represent a hydrogen atom, a halogen atom, a hydroxyl group or a substituent, except for a case in which R2 and R3 are both hydrogen atoms), and an antifungal agent containing the above compound.Type: GrantFiled: March 29, 2006Date of Patent: November 9, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Kazutaka Nakamoto, Satoshi Inoue, Keigo Tanaka, Toru Haneda
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Publication number: 20100273824Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: January 18, 2008Publication date: October 28, 2010Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
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Publication number: 20100273830Abstract: An insecticidal compound of formula (I) in which G1, G2, and G3 together with the two carbon atoms to which G1 and G3 are attached, form a non-aromatic 4- or 5-membered ring system; wherein G1 is sulfur, SO, SO2, oxygen, a direct bond, NRa or CR5aR5b; G2 is sulfur, SO, SO2, oxygen, a direct bond, NRb or CR5cR5d; G3 is sulfur, SO, SO2, oxygen, a direct bond, NRc or CR5eR5f; with the provisos that a) not more than 1 group G can be a direct bond, b) not more than 2 G groups can be oxygen, sulfur, SO or SO2 and c) when 2 G groups are oxygen, SO, SO2 and/or sulfur the two groups are separated by a carbon atom; each of Z1 and Z2, which may be the same or different, represents oxygen or sulfur; D is phenyl or a 5- or 6-membered heteroaromatic ring and R1a, R1b, R5a, R5b, R5c, R5d, R5e, R5f, Ra, Rb Rc, R2, R3 and R20 are specified organic groups and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.Type: ApplicationFiled: July 14, 2008Publication date: October 28, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Roger Graham Hall, Olivier Loiseleur, Jagadish Pabba, Sitaram Pal, Andre Jeanguenat, Andrew Edmunds, Andre Stoller
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Publication number: 20100261727Abstract: 2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for ?-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimer's disease at an early stage by non-invasive techniques when they are labeled with radioisotopes: wherein R1-R4, V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight ?-amyloid peptide binding compound, generation of malignant high-molecular weight ?-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimer's disease.Type: ApplicationFiled: October 15, 2009Publication date: October 14, 2010Inventors: Dae Yoon Chi, Byoung Se Lee, Youjung Jung, Uthaiwan Sirion, Yoo Jin Lim, Yu Jin Bae, Heejun Kim, So Young Chu, Dae Hyuk Moon, Jin-Sook Ryu, Jae Seung Kim, Seung Jun Oh
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Publication number: 20100249176Abstract: The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: ApplicationFiled: October 23, 2008Publication date: September 30, 2010Inventors: James C. Barrow, Thomas S. Reger, Youheng Shu, Zhi-Qiang Yang
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Publication number: 20100249094Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: March 10, 2010Publication date: September 30, 2010Inventors: Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel
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Publication number: 20100240620Abstract: The present application relates to novel aryl-substituted 3-cyano-5-thiazolyl- and 3-cyano-5-thiadiazolyl-1,4-dihydropyridines, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.Type: ApplicationFiled: September 8, 2007Publication date: September 23, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Lars Barfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche
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Publication number: 20100234428Abstract: The invention relates to substituted 2-mercapto-3-aminopyridines, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Applicant: GRUNENTHAL GMBHInventors: Sven Kühnert, Beatrix Merla, Achim Kless, Gregor Bahrenberg, Wolfgang Schröder
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Patent number: 7795249Abstract: The present invention provides certain pyrazoline compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: December 19, 2007Date of Patent: September 14, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Ruth S. Adams, Matthew Duffey, Alexandra E. Gould, Paul D. Greenspan, Bheemashankar A. Kulkarni, Tricia J. Vos
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Publication number: 20100227888Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: May 19, 2010Publication date: September 9, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis
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Publication number: 20100226879Abstract: Compounds having the formula A-R wherein A is a hetereoaryl and R is Ia, Ib or Ic and wherein A, R, R1, R2a, R2b, R2c, R3a, R3b, R4, R5, R6, Ra, Rb, Rc, Rd, X, X1, X2 and n are as are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: March 5, 2010Publication date: September 9, 2010Inventors: Sarah C. Abbot, Alfred Sui-Ting Lui, Jim Li, Francisco Xavier Talamas
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Patent number: 7786120Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: August 25, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Julian M. C. Golec, Michael Mortimore
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Patent number: 7776900Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: GrantFiled: April 18, 2006Date of Patent: August 17, 2010Assignee: Neurosearch A/SInventors: Lene Teuber, Janus S. Larsen, Philip K. Ahring, Elsebet Østergaard Nielsen, Naheed Mirza
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Patent number: 7776888Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I are suitable for use as herbicides.Type: GrantFiled: December 29, 2003Date of Patent: August 17, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Renaud Beaudegnies, Andrew Edmunds, Christoph Lüthy, Roger Graham Hall, Sebastian Volker Wendeborn, Jürgen Schaetzer
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Publication number: 20100202986Abstract: A composition comprises a mixture of a silicone and a solvent. The composition further comprises a drug selected from the group of retinoids, retinyls, vitamin A esters, vitamin D analogues, and combinations thereof. The composition further comprises a salt of a dialkyl sulfosuccinate, such as dioctyl sodium sulfosuccinate (DOSS). The composition yet further comprises and a solubilizer. The salt of a dialkyl sulfosuccinate solubilizes the drug. The solubilizer solubilizes the salt of a dialkyl sulfosuccinate. The composition can be topically applied to a substrate, such as skin, for delivering the drug. Drugs with a wide solubility range are soluble and compatible in the composition without separation or crystallization of the drugs occurring.Type: ApplicationFiled: July 11, 2008Publication date: August 12, 2010Inventors: Victor Albert Raul, Linda Sue Nartker, Robert O. Huber