Chalcogen Bonded Directly At 4-position Patents (Class 544/287)
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Publication number: 20110077233Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: October 25, 2010Publication date: March 31, 2011Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
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Publication number: 20110077245Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R3, L, X, Y and Z have defined meanings.Type: ApplicationFiled: December 3, 2010Publication date: March 31, 2011Inventors: Marcel Jozef Maria Van der Aa, Albertus Henricus Maria Theresia Van Heertum, Jacobus Alphonsus Josephus van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20110071148Abstract: The compounds according to formula VIII, their pharmaceutically acceptable acid or base addition salts, and the uses thereof is disclosed. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for the preparing a medicament for modulating estrogen related receptor (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity, etc. The definition of the groups of the formula is defined as the description.Type: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Applicant: Guangzhou Institute of Biomedicine and Health, Chinese Academy of SciencesInventors: Ke Ding, Chiwai Wong, Zhanfang Kang, Xi Zhou
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Publication number: 20110065671Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bi-cyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.Type: ApplicationFiled: May 18, 2009Publication date: March 17, 2011Inventors: Joel M. Harris, Santhosh Francis, Bernard R. Neustadt, Craig D. Boyle, Hong Liu, Jinsong Hao, Andrew Starnford, Samuel Chackalamannil, William J. Greenlee
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Publication number: 20110065703Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.Type: ApplicationFiled: March 12, 2008Publication date: March 17, 2011Inventor: Jay Jie-Qiang Wu
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Patent number: 7906521Abstract: The present invention relates to compounds useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: September 17, 2004Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Richard Isaacs
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Publication number: 20110053932Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFR?, PDGFR?, PKC?, p38, Src, SIK, Syk, Tie2 and TrkB kinases.Type: ApplicationFiled: June 18, 2008Publication date: March 3, 2011Inventors: Taebo Sim, Truc Ngoc Nguyen, Baogen Wu, Yun He, Yongping Xie, Xing Wang, Guobao Zhang, Nathanael Schiander Gray
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Patent number: 7893260Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3. Suitable compounds include but are not limited to, for example, substituted quinazolin-4-ones of formula I.Type: GrantFiled: November 3, 2006Date of Patent: February 22, 2011Assignee: Hydra Biosciences, Inc.Inventors: Jayhong A. Chong, Christopher Fanger, Glenn R. Larsen, William C. Lumma, Jr., Magdalene M. Moran, Amy Ripka, Dennis John Underwood, Manfred Weigele, Xiaoguang Zhen
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Patent number: 7893071Abstract: The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is selected from the group consisting of H, halo, alkyl, haloalkyl, —NH2, hydroxy and alkoxy; R2 is selected from the group consisting of optionally substituted bicyclic, optionally substituted aryl, and R6 is H, or C1-C8 alkyl; R19 is optionally substituted aryl; and m is 0-6.Type: GrantFiled: April 22, 2002Date of Patent: February 22, 2011Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
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Publication number: 20110039823Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.Type: ApplicationFiled: April 11, 2008Publication date: February 17, 2011Applicant: Actelion Pharmaceuticals LtdInventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110009435Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as anti-inflammatory agents.Type: ApplicationFiled: May 19, 2008Publication date: January 13, 2011Applicant: Pfizer, Inc.Inventors: Mark E. Schnute, Peter G. Ruminski, Cathleen E. Hanau, Joseph W. Stobach, Jeffery Carroll, Kirby Sample
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Patent number: 7863283Abstract: The present invention relates to sulphoximine-substituted quinazoline derivatives of the formula (I), processes for their preparation and their use as a medicament for the treatment of various diseases.Type: GrantFiled: June 13, 2008Date of Patent: January 4, 2011Assignee: Bayer Schering Pharma AGInventors: Duy Nguyen, Arne von Bonin, Michael Haerter, Hartmut Schirok, Anne Mengel, Martina Schaefer, Oliver von Ahsen
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Publication number: 20100323887Abstract: Disclosed are compounds of Formula 1, wherein X is O or S; Y is O or S; and R1, R2, R3 and R4 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: January 30, 2009Publication date: December 23, 2010Applicant: E.I. DU Pont De Nemours and CompanyInventors: Caleb William Holyoke, JR., My-Hanh Thi Tong, Reed Aaron Coats, Wenming Zhang, Stephen Frederick McCann, Dominic Ming-Tak Chan
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Patent number: 7851623Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-[(4-fluoro-2-methy-1-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline starting from a compound of Formula IX: wherein R4 is a protecting group; or an intermediate there between, using process steps, reagents and conditions as described.Type: GrantFiled: October 31, 2007Date of Patent: December 14, 2010Assignee: AstraZeneca ABInventors: Euan Alexander Arnott, John Crosby, Matthew Charles Evans, James Gair Ford, Martin Francis Jones, Kevin William Leslie, Ian Michael McFarlane, George Joseph Sependa
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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: 20100298357Abstract: The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.Type: ApplicationFiled: December 23, 2009Publication date: November 25, 2010Applicant: AstraZeneca ABInventor: James MCCABE
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Patent number: 7829574Abstract: Substituted quinazoline compounds of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and X are defined herein. It also discloses a pharmaceutical composition containing one of these compounds.Type: GrantFiled: May 9, 2008Date of Patent: November 9, 2010Assignee: Hutchison MediPharma Enterprises LimitedInventors: Wei-Guo Su, Weihan Zhang, Xiaoqiang Yan, Yumin Cui, Yongxin Ren, Jifeng Duan
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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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Patent number: 7816527Abstract: Kits including novel fluorescent derivitization reagents for labeling an aldehyde- and/or ketone-containing target substance in a sample are described. In one embodiment kits are provided the novel fluorescent derivitization reagents of which have the following formula: wherein Q is carbonyl, thiocarbonyl, or sulfonyl, and R5 is -L-Z; L is arylene, or a C1-6 perfluoroalkylene; Z is a carbonyl hydrazide, hydrazide, sulfonyl hydrazide, or a thiocarbonyl hydrazide; R11-R14 are independently H, C1-16 alkyl, C1-6 alkylamino, amino, or halogen; and R21-R24 are independently H, C 1-6 alkyl, C 1-6 alkoxy, C1-6 perfluoroalkyl, C1-6 alkylamino, di(C2-12-alkyl)amino, amino, carboxy, cyano, halogen, hydroxy, nitro, phenyl, sulfo, or -L-Z. The kits and reagents described are particularly useful for labeling glycoproteins or glycopeptides, nucleic acids, and lipopolysaccharides in electrophoresis gels.Type: GrantFiled: July 15, 2005Date of Patent: October 19, 2010Assignee: Life Technologies CorporationInventors: Richard P. Haugland, Thomas H. Steinberg, Wayne F. Patton, Zhenjun Diwu
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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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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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Patent number: 7799526Abstract: A phosphoprotein detection reagent that selectively binds phosphoamino acids. Methods of generating and employing the reagent are also provided, as are methods of detecting modulation of protein phosphorylation are disclosed. Methods of detecting a change in state of a cell are also disclosed. Additionally, a kit for the detection of phosphoproteins is also disclosed.Type: GrantFiled: November 21, 2003Date of Patent: September 21, 2010Assignee: The University of North Carolina at Chapel HillInventor: Alan Howe
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Patent number: 7799795Abstract: Provided herein are compounds of the formula where A1, A2, A3, A4, L, Q, R1, R2, R3, R4, Rx, Ry, Rz, X, Y1, Y2, Y4 and Z are as described herein, and compositions thereof that are useful in the treatment of inflammatory and immune conditions and diseases. In particular, the invention provides aryl nitrile compounds which modulate the expression and/or function of a chemokine receptor.Type: GrantFiled: June 26, 2006Date of Patent: September 21, 2010Assignee: Amgen Inc.Inventors: Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Julio C. Medina, Jeffrey T. Mihalic, George R. Tonn
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Publication number: 20100234404Abstract: Compounds and compositions for modulating the activity of p38 kinases are provided, including p38?, and p38? kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.Type: ApplicationFiled: May 28, 2010Publication date: September 16, 2010Inventors: Hengyuan Lang, Jiong Lan, Yungeng Fang
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Publication number: 20100204227Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.Type: ApplicationFiled: October 29, 2009Publication date: August 12, 2010Inventors: George W. MULLER, Alexander L. Ruchelman
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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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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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Patent number: 7750154Abstract: The invention concerns a compound of the Formula (I) wherein m is 0-2 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is halogeno, trifluoromethyl or (1-6C)alkyl; R3 is hydrogen, halogeno or (1-6C)alkyl; and R4 is (3-6C)cycloalkyl; 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: October 22, 2004Date of Patent: July 6, 2010Assignee: AstraZeneca ABInventors: Dearg Sutherland Brown, Ian Alun Nash
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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: 20100144766Abstract: A compound in combination with a pharmaceutically acceptable carrier, the compound having a formula: wherein: R1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl, and lower alkoxy; R2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy; and R3 is a member of the group consisting of hydrogen and lower alkenoxy-carbonyl; and n is either 1 or 2; and pharmaceutically acceptable salts thereof; for use in treatment of or prevention of skeletal muscle fibrosis and/or for inducing skeletal muscle regeneration.Type: ApplicationFiled: January 21, 2008Publication date: June 10, 2010Inventors: Mark Pines, Arnon Nagler
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Publication number: 20100144707Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.Type: ApplicationFiled: March 27, 2006Publication date: June 10, 2010Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Brian Kirk, Siya Ram, Paul Sweetnam
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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: 20100137586Abstract: There is provided a compound of formula (III), and a process for preparing a compound of formula (V) comprising converting a compound of formula (III) to the compound (V), wherein (X) is fluoro, chloro, bromo or iodo. There is also provided a process for preparing a compound of formula (XI) comprising converting a compound of formula (X) to the compound (XI). The compounds (V) and (XI) so prepared may be used in a process for preparing gefitinib.Type: ApplicationFiled: April 16, 2008Publication date: June 3, 2010Applicant: CIPLA LIMITEDInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Srinivas Laxminarayan Pathi
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Publication number: 20100113488Abstract: The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: ApplicationFiled: December 19, 2007Publication date: May 6, 2010Inventors: Nicholas Ronald Wurtz, Eldon Scott Priestley, Daniel L. Cheney, Peter W. Glunz, Xiaojun Zhang, Brandon Parkhurst, Vladimir Ladziata, Luciano Mueller
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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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Patent number: 7705005Abstract: The invention disclosed herein relates to compounds of formula (I) where the various groups are defined herein, and which are useful for treating inflammatory diseases such as atherosclerosis.Type: GrantFiled: January 25, 2007Date of Patent: April 27, 2010Assignee: Glaxo Group LimitedInventor: Colin Andrew Leach
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Patent number: 7671200Abstract: Quinazolinones of formulae (a, b, c and d) are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: GrantFiled: June 28, 2007Date of Patent: March 2, 2010Assignee: Cytokinetics, Inc.Inventors: Jeffrey Finer, Gustave Bergnes, Bainian Feng, Whitney Smith, John Chabala
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Publication number: 20100048898Abstract: A process for synthesizing 7-alkynyl-4-aminoquinazolines from 7-haloquinazolines is disclosed. In one specific synthesis, 4-[N-3-chloro-4-fluorophenyl)]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butynyl]-6-[N-methyl acrylamide]quinazoline is prepared from 7-chloro-6-nitro-3H-quinazolin-4-one. Also disclosed is an intermediate useful in the syntheses of 7-alkynyl-4-ammoquinaozolines and a process for making the intermediate. The 7-alkynyl-4-aminoquinaozolines prepared by processes of the invention are useful as pharmaceutically active compounds.Type: ApplicationFiled: March 2, 2007Publication date: February 25, 2010Inventor: Eric N. Jacobsen
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Publication number: 20100041664Abstract: The present invention provides novel bicyclic lactams derivatives, and analogues thereof, of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, B, C, W, Y, Z1, Z2, Z3, Z4, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: ApplicationFiled: December 17, 2007Publication date: February 18, 2010Inventors: Nicholas Ronald Wurtz, Eldon Scott Priestley, Daniel L. Cheney, Xiaojun Zhang, Brandon Parkhurst, Vladimir Ladziata
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Publication number: 20100029658Abstract: The present invention relates to novel quinoxaline, quinazoline and phthalazine derivatives as well as multimeric derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds for the treatment and prevention of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in treating and preventing neurodegenerative diseases.Type: ApplicationFiled: August 22, 2006Publication date: February 4, 2010Inventors: Moshe Gavish, Jehuda Arieh Veenman, Alex Shterenberg, Ilan Marek
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Publication number: 20100016342Abstract: Provided herein are solid forms comprising 3-(2,5-dimethyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione. Pharmaceutical compositions comprising the solid forms and methods for treating, preventing and managing various disorders are also disclosed.Type: ApplicationFiled: September 25, 2008Publication date: January 21, 2010Inventors: Louise M. Cameron, George W. Muller, Hon-Wah Man
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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: 7635700Abstract: Provided are 5-substituted quinazolinone compounds, for example, of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use for treating angiogenesis or cytokine related disorders, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: September 26, 2007Date of Patent: December 22, 2009Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Patent number: 7625909Abstract: 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 structure IA, IB, and IC where the values of the variables are defined herein.Type: GrantFiled: May 21, 2004Date of Patent: December 1, 2009Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: 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: 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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Patent number: RE41894Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxy-alkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 arylType: GrantFiled: March 5, 2008Date of Patent: October 26, 2010Assignee: Boehringer Ingelheim Canada Ltd.Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Elise Ghiro, Nathalie Goudreau, Marc-Andre Poupart, Jean Rancourt, Youla S. Tsantrizos, Anne-Marie Faucher, Teddy Halmos, Dominik M. Wernic