Chalcogen Bonded Directly To A Ring Carbon Of The 1,3-diazine Ring Of The Quinazoline Ring System Patents (Class 514/266.3)
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Naphthamide Derivatives As Multi-Target Protein Kinase Inhibitors and Histone Deacetylase Inhibitors
Publication number: 20100298358Abstract: Isolated compounds of formula I: and stereoisomers, enantiomers, diastereomers, and pharmaceutically acceptable salts thereof are described, as well as processes for production, and methods of use of these compounds and compositions thereof for the treatment of diseases associated with abnormal protein kinase activities and/or abnormal histone deacetylase activities including, for example, inflammatory diseases, autoimmune diseases, cancer, neurological and neurodegenerative diseases, cardiovascular diseases, metabolic disease, allergies and asthma and/or hormone-related diseases.Type: ApplicationFiled: May 21, 2010Publication date: November 25, 2010Applicant: Shenzhen Chipscreen Biosciences Ltd.Inventors: Xian-Ping LU, Zhibin Li, Song Shan, Jindi Yu, Zhiqiang Ning -
Publication number: 20100292209Abstract: The invention relates to screening for compounds and compositions that modulate neurotrophic factor signaling as reflected by modulation of factor-induced neurite outgrowth. The compounds and compositions are useful in the treatment of a variety of disorders. The invention also provides methods for preparing compounds for treatment of such disorders.Type: ApplicationFiled: March 28, 2008Publication date: November 18, 2010Applicants: Massachusetts Institute of Technology, The General Hospital Corporation d/b/a Massachuset ts General HospitalInventors: Letian Kuai, Stephen J. Haggarty
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Publication number: 20100292159Abstract: This invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory conditions.Type: ApplicationFiled: March 20, 2007Publication date: November 18, 2010Applicant: UNIVERSITY OF QUEENSLANDInventor: Maree Therese Smith
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Patent number: 7834023Abstract: Compounds of formula I are provided: wherein Ar1 and Ar2 are substituted aromatic rings and L1 and L2 are independent divalent linking groups. The compounds are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.Type: GrantFiled: September 17, 2007Date of Patent: November 16, 2010Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Carroll Anna Crew, legal representative, Shawn M. Bauer, Anjali Pandey
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Publication number: 20100285960Abstract: A method for regulating the release rate of microencapsulated actives comprising: 1a) addition or subtraction of piperonylbutoxide (PBO), component B) to 2a) formulations A) comprising at least one microencapsulated active having agrochemical activity, optionally PBO outside the microcapsule, 3a) dilution by water of component A) and/or component B) until the active application dose, the ratio by weight PBO/active ranges from 0.1 to 80, the PBO subtraction being feasible only when the PBO is present outside the microcapsule of the formulation A).Type: ApplicationFiled: December 23, 2008Publication date: November 11, 2010Applicant: ENDURA S.p.A.Inventors: Carlotta Gobbi, Lucio Bassetti, Valerio Borzatta
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Publication number: 20100267752Abstract: The present invention discloses 3-hydroquinazolin-4-one derivatives for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cancer, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.Type: ApplicationFiled: October 14, 2009Publication date: October 21, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Andrei Glushkov, Dmitry Koltun, Elena Mayboroda, Eric Parkhill, Natalya Vasilevich, Jeff Zablocki
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Publication number: 20100267633Abstract: The invention relates to substituted N-(4-oxo-3,4-dihydroquinazolin-2-yl)butanamid derivatives which modulate androgen receptors to treat conditions such as: osteoporosis, peridontal disease, bone fracture, frailty, and sarcopenia.Type: ApplicationFiled: September 22, 2006Publication date: October 21, 2010Inventors: Barbara Hanney, Yuntae Kim, Helen J. Mitchell, Jeffrey D. Musselman, James J. Perkins
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Publication number: 20100261741Abstract: The present invention is directed to quinazolinone 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: June 28, 2010Publication date: October 14, 2010Applicant: MerckInventors: James C. Barrow, Rowena V. Cube, Phung Le Ngo, Kenneth E. Rittle, Zhiqiang Yang, Steven D. Young
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Publication number: 20100256120Abstract: The invention concerns a compound of the Formula I wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen and R4 is, (1-6C)alkyl or (1-6C)alkoxy; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: August 7, 2006Publication date: October 7, 2010Inventors: Dearg Sutherland Brown, Ian Alun Nash, Steve Swallow
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Publication number: 20100255116Abstract: A fungicidal composition is provided. A fungicidal composition comprising synergistically effective amounts of (a) a carboxylic acid amide derivative of the formula (I) or its salt: wherein B is a heterocyclic group which may be substituted; each of R1 and R2 which are independent of each other, is alkyl; X is halogen, alkyl or alkoxy; and n is an integer of from 0 to 5, and (b) at least one fungicidal compound selected from the group consisting of an azole compound, an anilinopyrimidine compound, a triazolopyrimidine compound, a strobilurin compound, an N-halogenothioalkyl compound, a pyridinamine compound, a bicarbonate, an inorganic sulfur compound, a dithiocarbamate compound, an organic chlorine compound, a dicarboxyimide compound, an amine compound, a phenylpyrrole compound, a benzophenone compound, a dinitrobenzene compound, a piperidine compound, a morpholine compound, etc.Type: ApplicationFiled: October 20, 2008Publication date: October 7, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Shigeru Mitani, Shintaro Tsukuda
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Patent number: 7807686Abstract: The present invention relates to 2-(4-oxo4H-quinazolin-3-yl) acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.Type: GrantFiled: March 10, 2006Date of Patent: October 5, 2010Assignee: N.V. OrganonInventors: Jeffrey Letourneau, Christopher Riviello, Koc-Kan Hoc, Jui-Hsiang Chan, Michael Ohlmeyer, Patrick Jokiel, Irina Neagu, John Richard Morphy, Susan Elizabeth Napier
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Publication number: 20100249158Abstract: The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: July 3, 2008Publication date: September 30, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Klaus Fuchs, Niklas Heine, Christian Eickmeier, Sandra Handschuh, Cornelia Dorner-Ciossek, Stefan Hoerer
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Publication number: 20100216823Abstract: The invention provides compounds of formula (I): wherein m, n, X, R1, A, B, R2 and R3 have the meanings given in the specification, and pharmaceutically acceptable salts, solvates, polymorphs and prodrugs thereof. The compounds are PDE7 inhibitors and have a number of therapeutic applications, particularly in the treatment of pain, especially neuropathic pain.Type: ApplicationFiled: May 16, 2008Publication date: August 26, 2010Inventors: David James Rawson, Nigel Alan Swain, Lesa Watson
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Publication number: 20100216738Abstract: The present invention relates to the use of active substance combinations which consist firstly of a known dihydrofuranone derivative and secondly of further known pesticidal active substances, which active substance combinations are used for controlling animal pests, in particular from the order of the mites.Type: ApplicationFiled: June 27, 2008Publication date: August 26, 2010Applicant: BAYER CROPSCIENCE AGInventors: Reiner Fischer, Emmanuel Salmon, Heike Hungenberg, Jingquan Guo
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Publication number: 20100204167Abstract: The novel active compound combinations comprising a compound of the formula (I-1) or (I-2) and the active compounds (1) to (26) listed in the description have very good insecticidal and acaricidal properties.Type: ApplicationFiled: July 6, 2007Publication date: August 12, 2010Inventors: Reiner Fischer, Wolfram Andersch, Thomas König, Anton Kraus, Emmanuel Salmon, Heike Hungenberg
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Publication number: 20100197706Abstract: The present invention relates to derivatives of 1-oxo-1,2-dihydroisoquinoline-5-carboxamides and of 1-oxo-3,4-dihydroquinazoline-8-carboxamides, to the preparation thereof and to the therapeutic use thereof.Type: ApplicationFiled: January 26, 2010Publication date: August 5, 2010Applicant: SANOFI-AVENTISInventors: Michel EVERS, Arielle GENEVOIS-BORELLA, Andreas KARLSSON, Jean-Luc MALLERON
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Publication number: 20100197705Abstract: There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile having structural formula I(B) and to a method of preparing it. There is further a process or method for the manufacture of a pharmaceutically active quinazolinone compounds of the formula I wherein the symbols have the meanings given in the description, said process comprising reacting a compound of the formula II, wherein R4* is R1*—C(?O)— wherein R1* is independently selected from the group of meanings of R1 as defined for a compound of the formula I so that R1* and R1 are identical to or different from each other, or R4* is especially H, and R1 and R3, R5 and R6 are as defined for a compound of the formula I, or a salt thereof, under simultaneous or sequential condensation and cyclisation conditions with an aniline compound of the formula III, wherein R2 and m are as defined for a compound of the formula I. Further reactions and related embodiments are also claimed and disclosed.Type: ApplicationFiled: January 6, 2010Publication date: August 5, 2010Inventors: Weichun Chen, Hong-Yong Kim, Jessica Liang, Michael Mutz, Mahavir Prashad, Christopher Towler, Ruoqiu Wu
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Publication number: 20100189685Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: May 23, 2008Publication date: July 29, 2010Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Tove Bolken, Dennis E. Hruby
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Publication number: 20100190746Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: November 20, 2009Publication date: July 29, 2010Applicant: ICAGEN, INC.Inventors: Grant A. McNaughton-Smith, James B. Thomas, JR., George S. Amato
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Patent number: 7763628Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: GrantFiled: April 17, 2007Date of Patent: July 27, 2010Assignee: Cytokinetics, Inc.Inventors: Jeffrey T. Finer, Gustav E Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng
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Publication number: 20100173874Abstract: The invention features methods and devices for local delivery of agents that modify glutamate-mediated neurotransmission to the inner ear for treatment of inner ear disorders caused by glutamate-induced hearing loss and/or tinnitus.Type: ApplicationFiled: July 30, 2009Publication date: July 8, 2010Inventors: Jean-Luc Puel, Remy Pujol, Yves Christen
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Publication number: 20100168042Abstract: The invention relates to novel insecticidal active compound combinations comprising, firstly, cyclic ketoenols or other acaricidally active compounds and, secondly, further insecticidally active compounds from the group of the anthranilamides, which combinations are highly suitable for controlling animal pests, such as insects and unwanted acarids.Type: ApplicationFiled: March 9, 2010Publication date: July 1, 2010Applicant: BAYER CROPSCIENCE AGInventors: Christian Funke, Thomas Bretscheneider, Reiner Fischer, Rüdiger Fischer, Heike Hungenberg, Wolfram Andersch, Wolfgang Thielert, Ánton Kraus
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Publication number: 20100168089Abstract: An in vitro method of screening for candidate compounds for the preventive or curative treatment of acne entails determination of the ability of a compound to inhibit the expression or the activity of TACE, and also to the administration of inhibitors of the expression or of the activity of this enzyme, in the treatment of acne.Type: ApplicationFiled: December 17, 2009Publication date: July 1, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: JÉRÔME AUBERT, ISABELLE CARLAVAN, JOHANNES VOEGEL
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Patent number: 7745452Abstract: The present invention is directed to quinazolinone compounds of the formula I: wherein R1, R2, R3, X1, X2 X3 are defined herein. These compounds are antagonists of T-type calcium channels, and 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: GrantFiled: March 8, 2006Date of Patent: June 29, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Rowena V. Cube, Phung Le Ngo, Kenneth E. Rittle, Zhiqiang Yang, Steven D. Young
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Publication number: 20100160315Abstract: This invention relates to novel 2,3-diamino-quinazolinone derivatives having medical utility, to use of the 2,3-diamino-quinazolinone derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2,3-diamino-quinazolinone derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.Type: ApplicationFiled: May 22, 2008Publication date: June 24, 2010Applicant: Neuro Search A/SInventors: Carsten Jessen, William Dalby Brown, Joachim Demnitz, Dorte Strobaek, Mads P.G. Korsgaard, Palle Christophersen
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Patent number: 7741332Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.Type: GrantFiled: April 26, 2007Date of Patent: June 22, 2010Assignee: Icagen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, Jr.
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Publication number: 20100152213Abstract: The invention relates to a series of dual inhibitors of enzymes PDE7 and PDE4, having formula (I) and to the use thereof in the production of pharmaceutical compositions for the treatment of inflammatory and/or autoimmune processes.Type: ApplicationFiled: March 14, 2008Publication date: June 17, 2010Inventors: Carmen Gil Ayuso-Gontan, Tania Castaño Calduch, Nuria Campillo Martin, Sara Ballester Jareño, Carol González Garcia, Francisco Javier Hernández Torres
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Publication number: 20100152209Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.Type: ApplicationFiled: November 3, 2006Publication date: June 17, 2010Applicant: Hydra Biosciences Inc.Inventors: Jayhong A. Chong, Christopher Fanger, Glenn R. Larsen, William C. Lumma, JR., Anu Mahadevan, Peter Meltzer, Magdalene M. Moran, Amy Ripka, Dennis John Underwood, Manfred Weigele, Xiaoguang Zhen
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Publication number: 20100144747Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: September 29, 2009Publication date: June 10, 2010Inventors: Hans ALLGEIER, Yves AUBERSON, David CARCACHE, Philipp FLOERSHEIM, Christel GUIBOURDENCHE, Wolfgang FROESTL, Jörg KALLEN, Manuel KOLLER, Henri MATTES, Joachim NOZULAK, David ORAIN, Johanne RENAUD
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Publication number: 20100144693Abstract: The present invention relates generally to the field of treatment and prophylaxis of retinal degenerative diseases. More particularly, the present invention contemplates a method for preventing, reducing the risk of development of, or otherwise treating or ameliorating the symptoms of, age-related macular degeneration (AMD) or related retinal conditions in mammals and in particular humans. The present invention further provides therapeutic compositions enabling dose-dependent or dose-specific administration of agents useful in the treatment and prophylaxis of age-related macular degeneration or related retinal degenerative conditions.Type: ApplicationFiled: April 13, 2007Publication date: June 10, 2010Applicant: PRANA BIOTECHNOLOGY LIMITEDInventors: Ashley Bush, Colin Louis Masters, Penelope Jane Huggins, Jack Gordon Parsons, Gaik Beng Kok, Vijaya Kenche, Mariana El Sous
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Publication number: 20100143299Abstract: This invention provides the treatment of viral infections with a 4,6-disubstituted or 2,4,6-trisubstituted quinazoline derivative represented by the structural formula [(I)] wherein: R2 is selected from the group consisting of hydrogen, NR?R? and C1-7 alkyl; —A is selected from the group consisting of a bond, O, S(O)n, C1-7 alkylene, C2-7 alkenylene and C2-7 alkynylene; R4 is selected from the group consisting of C1-7 alkyl, C2-7 alkenyl, C3-10cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted alkyl and cycloalkyl-alkyl; —Y is selected from the group consisting of a single bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene; n is 0, 1 or 2; and R6 is selected from the group consisting of halogen, heteroaryl and aryl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-?/-oxide, a solvate or a pro-drug thereof.Type: ApplicationFiled: July 20, 2007Publication date: June 10, 2010Applicant: Gilead Sciences, Inc.Inventors: Ling-Jie Gao, Piet André Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe, William John Watkins, Lee Shun Chong
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Publication number: 20100113391Abstract: [Problem] Provided is a compound, which exhibits a P2Y12 inhibitory action and is useful as a medical drug, particularly, as a platelet aggregation inhibitor. [Means for Solution] The inventors have eagerly investigated P2Y12 inhibitors. As a result, the inventors have found that a bicyclic heterocyclic compound such as quinazolinedione, isoquinolone, and the like having an amino group substituted with lower alkyl, cycloalkyl, or lower alkylene-cycloalkyl at the specific position exhibits an excellent platelet aggregation inhibitory action, thereby completing the present invention. Since the compound of the invention exhibits excellent P2Y12 inhibitory action and platelet aggregation inhibitory action, it is useful as a platelet aggregation inhibitor.Type: ApplicationFiled: April 17, 2008Publication date: May 6, 2010Applicant: Astellas Pharma Inc.Inventors: Yuji Koga, Takao Okuda, Takashi Kamikubo, Michihito Kageyama, Hiroyuki Moritomo
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Patent number: 7709491Abstract: The invention relates to substituted quinazolines and to methods for the production thereof, in addition to the use thereof in the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, especially against cytomegaloviruses.Type: GrantFiled: October 25, 2003Date of Patent: May 4, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Tobias Wunberg, Judith Baumeister, Mario Jeske, Susanne Nikolic, Frank Süβmeier, Holger Zimmermann, Rolf Grosser, Kerstin Henninger, Guy Hewlett, Jörg Keldenich, Dieter Lang, Tse-I Lin
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Patent number: 7709479Abstract: The use of a compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O) or S(O)2, NH or NR12 where R12 is hydrogen or C1-6 alkyl; R5 is selected from a group NHC(O)OR9, NHC(O)R9, NHS(O)2R9, C(O)R9, C(O)OR9, S(O)R9, S(O)OR9, S(O)2OR9, C(O)NR10 R11, S(O)NR10R11 S(O)ONR10R11, where R9, R10 or R11 are various specified organic groups; R6 is hydrogen, optionally substituted hydrocarbyl or optionally substituted heterocyclyl; R7 and R8 are various specified organic groups, and R1, R2, R3, R4 are independently selected from halogeno, cyano, nitro, C1-3alkylsulphanyl, —N(OH)R13— (wherein R7 is hydrogen, or C1-3alkyl), or R15X1— (wherein X1 represents a direct bond, —O—, —CH2—, —OCO—, carbonyl, —S—, —SO—, —SO2—, —NR16CO—, —CONR16—, —SO2NR16—, —NR17SO2— or —NR18— (wherein R16, R17 and R18 each independently represents hydrogen, C1-3alkyl or C1-3alkoxy C2-3alkyl), and R9 is hydrogen, optionally substituted hydrocarbyl, optionally substituted heterocyclyl or optionally substituted alkoxyType: GrantFiled: September 18, 2000Date of Patent: May 4, 2010Assignee: AstraZenecaInventors: Andrew Austen Mortlock, Nicholas John Keen, Frederic Henri Jung, Andrew George Brewster
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Publication number: 20100105654Abstract: A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structures VA, VB, VIIA and VIIB where the values of the variables are defined herein.Type: ApplicationFiled: October 23, 2009Publication date: April 29, 2010Inventors: Rustum S. BOYCE, Natalia Aurrecoechea, Daniel Chu, Aaron Smith, Christopher R. Conlee, Brian D. Thompson, Judith de Armas Kuntz, David L. Musso, Kevin K. Barvian, Stephen A. Thomson, William R. Swain, Kien S. Du, Brian A. Chauder, Jason D. Speake, Michael J. Bishop
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Publication number: 20100105670Abstract: Disclosed is a fungicidal mixture comprising (a) at least one compound selected from the compounds of Formula 1 N-oxides, and salts thereof, wherein G, D, R1 and R5 are defined in this specification, and (b) the compound of Formula 2 and optionally (c) one or more compounds described in the disclosure. Also disclosed is a fungicidal composition comprising a fungicidally effective amount of the aforesaid mixture and at least one additional component selected from the group consisting of surfactants, solid diluents or liquid diluents. Further disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of the aforesaid mixture (e.g., as a composition described herein).Type: ApplicationFiled: November 15, 2007Publication date: April 29, 2010Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Wonpyo Hong, Thomas Paul Selby
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Patent number: 7696215Abstract: The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen or halogeno; and R4 is isoxazolyl; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: GrantFiled: February 23, 2006Date of Patent: April 13, 2010Assignee: AstraZeneca ABInventors: Ian Alun Nash, Jonathan Erle Finlayson, Caroline Rachel Thompson
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Publication number: 20100074895Abstract: Methods are provided for treating cancer metastasis by administering a therapeutic composition targeting a kinase substrate cascade.Type: ApplicationFiled: October 31, 2007Publication date: March 25, 2010Inventors: Emanuel F. Petricoin, III, Mariaelena Pierobon, Valerie Calvert, Lance A. Liotta
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Publication number: 20100068197Abstract: Disclosed are compounds of Formula I effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: July 9, 2009Publication date: March 18, 2010Applicant: Myriad Pharmaceuticals, Inc.Inventors: MARK B. ANDERSON, J. Adam Willardsen, Warren S. Weiner, Kazuyuki Suzuki, Robert J. Halter, In Chul Kim, Matthew Reeder, Ashantai Yungai
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Publication number: 20100063073Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: ApplicationFiled: August 25, 2009Publication date: March 11, 2010Inventors: Jeffrey T. Finer, Gustave Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng
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Publication number: 20100029695Abstract: A medicament safe and free from side effects, for the prevention or treatment of dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen, which suppresses the progress of the condition and improves the quality of life of the patient, which medicament treats dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen by including a quiazoline derivative having the formula (I) or (II) or its pharmaceutically acceptable salt as an effective ingredient:Type: ApplicationFiled: October 9, 2009Publication date: February 4, 2010Applicant: Asubio Pharma Co., Ltd.Inventors: Harukazu Fukami, Yoshiaki Tomimori, Yoshiaki Fukuda, Naohiro Watanabe
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Publication number: 20090325987Abstract: The present invention provides Quinazolinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.Type: ApplicationFiled: June 16, 2009Publication date: December 31, 2009Applicant: Glenmark Pharmaceuticals, S.A.Inventors: Meyyappan Muthuppalniappan, Abraham Thomas, Sukeerthi Kumar, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay, Srinivas Gullapalli
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Patent number: 7638520Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atheroscelerosis.Type: GrantFiled: November 21, 2006Date of Patent: December 29, 2009Assignee: SmithKline Beecham, plcInventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
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Publication number: 20090318478Abstract: The invention discloses quinazoline derivatives or salts thereof, which possess PDE9-inhibiting activity and are useful as treating agents of dysuria and the like, the derivatives being represented by the formula (I) in the formula, R1 stands for phenyl or aromatic heterocyclic group which are optionally substituted with 1-3 substituents selected from halogen, C1-6 alkyl, C1-6 haloalkyl containing 1-6 halogen atoms and C1-6 alkoxy; and n is an integer of 1-3.Type: ApplicationFiled: July 24, 2007Publication date: December 24, 2009Inventors: Akira Asagarasu, Shuichiro Sato, Makoto Okada
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Patent number: 7625908Abstract: A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.Type: GrantFiled: November 11, 2004Date of Patent: December 1, 2009Assignee: AstraZeneca ABInventors: Laurent Francois Andre Hennequin, Robert Hugh Bradbury, Jason Grant Kettle
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Publication number: 20090291973Abstract: This invention relates to novel quinazoline derivatives having medical utility, to use of the quinazoline derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the quinazoline derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.Type: ApplicationFiled: November 17, 2006Publication date: November 26, 2009Applicant: NeuroSearch A/SInventors: William Dalby Brown, Lene Teuber, Tino Dyhring, Dorte Strøbæk, Carsten Jessen
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Publication number: 20090285782Abstract: This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR?R?, C1-7 alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7 alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7 alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R? and R? are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.Type: ApplicationFiled: July 20, 2007Publication date: November 19, 2009Applicant: Gilead Sciences, Inc.Inventors: Ling-Jie Gao, Piet André Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe, William John Watkins, Lee Shun Chong
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Patent number: 7618977Abstract: Medicaments for the treatment of dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen, having quinazolidone derivatives of formula I or II that are herein defined, are disclosed.Type: GrantFiled: February 22, 2001Date of Patent: November 17, 2009Assignee: Asubio Pharma Co., Ltd.Inventors: Harukazu Fukami, Yoshiaki Tomimori, Yoshiaki Fukuda, Naohiro Watanabe
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Publication number: 20090281128Abstract: The present invention relates to compounds of formula I: useful as inhibitors of caspases. The present invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for preparing the compounds, and methods of using the compounds and compositions in the treatment of various diseases, conditions, or disorders.Type: ApplicationFiled: May 12, 2009Publication date: November 12, 2009Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Ronald Knegtel, Michael Mortimore, John Studley, David Millan
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Publication number: 20090280081Abstract: The role of the JAK/STAT signal transduction pathway cellular mechanisms that lead to the onset and progression of degenerative joint diseases or disorders such as osteoarthritis (OA) is disclosed. Certain known effective OA therapeutics such as hymenialdisine, debromohymenialdisine, and its variants and derivatives are shown to function as JAK3-specific inhibitors, which downregulate steady state mRNA levels of key cellular components involved in cartilage degradation. Another JAK3-specific inhibitor, not previously known as an OA therapeutic, is shown to downregulate steady state mRNA levels of various cellular components involved in cartilage degradation in a manner identical to that of the known OA therapeutics.Type: ApplicationFiled: May 1, 2007Publication date: November 12, 2009Applicant: Genzyme CorporationInventor: George Vasios