Ring Oxygen In The Bicyclo Ring System Patents (Class 546/115)
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Patent number: 7816353Abstract: Compounds of formula III: wherein R5a, R3, X, Y, Q, R1a and R1b are as defined in the specification, pharmaceutically acceptable salts thereof, and methods of use thereof.Type: GrantFiled: October 22, 2004Date of Patent: October 19, 2010Assignee: Exelixis, Inc.Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew Tsuhako, John M. Nuss, Wei Xu
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Publication number: 20100261725Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 26, 2009Publication date: October 14, 2010Applicant: CALCIMEDICA, INC.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Patent number: 7812164Abstract: The invention provides novel derivatives of cyclopamine having the following formula:Type: GrantFiled: December 27, 2007Date of Patent: October 12, 2010Assignee: Infinity Pharmaceuticals, Inc.Inventors: Brian Austad, Mark L. Behnke, Alfredo C. Castro, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Martin Tremblay
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Publication number: 20100255005Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: May 28, 2008Publication date: October 7, 2010Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
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Publication number: 20100249078Abstract: Certain tetracyclic compounds are described, which may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: May 23, 2008Publication date: September 30, 2010Applicant: The Scrips Research InstituteInventor: Dale L. Boger
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Publication number: 20100247514Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: May 5, 2008Publication date: September 30, 2010Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Theodros Asberom, Xianhai Huang, Xiaohong Zhu, Mark D. McBriar, Dmitri A. Pissarnitski, Zhiqiang Zhao, Ruo Xu, Hongmei Li, Anandan Palani, Johannes H. Voigt, Robert D. Mazzola, JR., John Clader, Hubert Josien, Jun Qin
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Publication number: 20100249417Abstract: Disclosed is 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate, which has strong antibacterial activity. The compound is highly safe and useful as an original drug for pharmaceutical preparations. Also disclosed is a method which is useful for producing 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate.Type: ApplicationFiled: November 25, 2008Publication date: September 30, 2010Applicants: Toyama Chemical Co., Ltd., Taisho Pharmaceutical Co., Ltd.Inventors: Taro Kiyoto, Masahiro Takebayashi, Yasutaka Baba, Muneo Syoji, Toshiya Noguchi, Fumihito Ushiyama, Hiroki Urabe, Hiromasa Horikiri
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Publication number: 20100239551Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating chan-nel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSSI1E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.Type: ApplicationFiled: January 4, 2008Publication date: September 23, 2010Applicant: IRM LLCInventors: David C. Tully, Arnab K. Chatterjee, Agnes Vidal, Badry Bursulaya
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Publication number: 20100234419Abstract: The invention relates to substituted 3-aminoisoxazolopyridines, to processes for their preparation, to medicaments containing these compounds and to the use of these compounds in the preparation of medicaments.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Applicant: GRUNENTHAL GMBHInventors: Sven KÜHNERT, Gregor Bahrenberg, Wolfgang Schröder
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Patent number: 7790729Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: May 19, 2006Date of Patent: September 7, 2010Assignee: Methylgene Inc.Inventors: Oscar Mario Saavedra, Stephen William Claridge, Lijie Zhan, Franck Raeppel, Arkadii Vaisburg, Stephane Raeppel, Robert Deziel, Michael Mannion, Nancy Z. Zhou, Ljubomir Isakovic
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Patent number: 7790753Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.Type: GrantFiled: April 17, 2006Date of Patent: September 7, 2010Assignee: sanofi-aventisInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Corinne Veronique
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Publication number: 20100222352Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.Type: ApplicationFiled: September 25, 2006Publication date: September 2, 2010Applicant: YALE UNIVERSITYInventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
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Publication number: 20100222338Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Wenge Zhong, Stephen Hitchcock, Brian K. Albrecht, Michael D. Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Dean Hickman, Daniel Horne, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig E. Masse, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Holger Monenschein, Thomas Nguyen
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Publication number: 20100197679Abstract: Bicyclic nitrogen containing compounds and their use as antibacterialsType: ApplicationFiled: April 17, 2008Publication date: August 5, 2010Inventors: Christopher Barfoot, David Thomas Davies, Timothy James Miles, Neil David Pearson
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Patent number: 7767667Abstract: It has now been found that certain novel heterocyclic derivitives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)?C(R7)N(R8)—, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)?C(R12)C(R13)?C(R14) 1 12, -, where R,R,R6, R7, R8, RI1, R R13, R14, and X are described. 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 compatable 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: GrantFiled: August 22, 2008Date of Patent: August 3, 2010Assignee: FMC CorporationInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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Patent number: 7737161Abstract: The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.Type: GrantFiled: January 29, 2009Date of Patent: June 15, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Hidenori Akatsuka, Toru Iijima, Tatsuya Watanabe, Jun Murakami, Takashi Mitsui
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Publication number: 20100144717Abstract: The present invention relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation.Type: ApplicationFiled: December 15, 2006Publication date: June 10, 2010Inventors: Janelle Comita-Prevoir, Mark Cronin, Bolin Geng, Andrew Aydon Godfrey, Folkert Reck
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Publication number: 20100143251Abstract: The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus.Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Inventors: Gilles D. Tamagnan, David Alagille, Herve Da Costa
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Publication number: 20100120838Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: ApplicationFiled: January 20, 2010Publication date: May 13, 2010Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta M. Micula, Seong Heon Kim, De-Yi Yang, Razia Rizvi
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Publication number: 20100120839Abstract: There is provided compounds of formula I, wherein R1, R2, A1, A2, A3 and A4 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.Type: ApplicationFiled: April 21, 2008Publication date: May 13, 2010Inventors: Kiyo No, Andrei Sanin, Gasse Kromann
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Patent number: 7709483Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: GrantFiled: March 29, 2007Date of Patent: May 4, 2010Assignee: Glaxo Group LimitedInventors: Graham Elgin Jones, Timothy James Miles, Neil David Pearson
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Publication number: 20100105659Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: March 19, 2008Publication date: April 29, 2010Applicant: ARRAY BIOPPHARMA INC.Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Ronald Jay Hinklin, Ajay Singh
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Publication number: 20100099663Abstract: The present invention is directed to a compound of formula I, wherein R1, R2, R3, X, A, m and n are as herein defined, the process for its preparation and its use thereof as a medicament.Type: ApplicationFiled: December 21, 2009Publication date: April 22, 2010Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Manfred SCHUDOK, Armin HOFMEISTER
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Patent number: 7700616Abstract: The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus.Type: GrantFiled: May 8, 2007Date of Patent: April 20, 2010Assignee: Molecular Neuroimaging, LLC.Inventors: Gilles D. Tamagnan, David Alagille, Herve Da Costa
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Publication number: 20100093733Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
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Publication number: 20100081650Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.Type: ApplicationFiled: November 17, 2009Publication date: April 1, 2010Inventors: Jeffrey Michael Axten, Robert A. Daines, David Thomas Davies, Timothy Francis Gallagher, Graham Elgin Jones, William Henry Miller, Neil David Pearson, Israil Pendrak
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Publication number: 20100063066Abstract: Compounds of Formulas (I), (IIA) and (IIIA) are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formulas (I), (IIA) and (IIIA) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: August 31, 2007Publication date: March 11, 2010Applicant: Array Biopharma, Inc.Inventors: Alexandre J. Buckmelter, Joseph P. Lyssikatos, Greg Miknia, Li Ren, Steven Mark Wenglowsky, Bryson Rast
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Patent number: 7674907Abstract: The present invention relates to furanopyridine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof.Type: GrantFiled: July 18, 2005Date of Patent: March 9, 2010Assignee: Amgen Inc.Inventors: Joseph J. Nunes, Matthew W. Martin, Ryan White, David McGowan, Jean E. Bemis, Frank Kayser, Jiasheng Fu, Jinqian Liu, XianYun Jiao
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Publication number: 20100048537Abstract: The present invention relates to a compound represented by formula [1] or a pharmaceutically acceptable salt thereof: In formula [1], one of X and Y is CH and the other is oxygen or sulfur; R is hydrogen, etc.; Z is hydrogen, etc.; Ar is phenyl, etc.; and n is 1 or 2 and or m is 1 or 2, excluding compounds where n is 2 and m is 2 simultaneously. Also provided is a pharmaceutical composition comprising a compound of formula [1] or a pharmaceutically acceptable salt thereof as an active ingredient. The composition is usable as an agent for the prevention or treatment of depression, panic disorder, anxiety, obsessive-compulsive disorder, chronic pain, fibromyalgia, obesity, stress urinary incontinence, and overactive bladder.Type: ApplicationFiled: March 28, 2008Publication date: February 25, 2010Applicant: Nippon Shinyaku Co., Ltd.Inventors: Masato Matsuoka, Tatsuya Oyama
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Publication number: 20100048610Abstract: [Object] 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 carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.Type: ApplicationFiled: May 29, 2009Publication date: February 25, 2010Applicant: KOWA COMPANY, LTD.Inventors: Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Takayuki Matsuda, Ayumu Okuda, Hisashi Sumida, Yuuichirou Watanabe, Takashi Enomoto, Kimiyuki Shibuya
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Patent number: 7659399Abstract: The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, A8, R2, R3, R5, R6, R7, and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: GrantFiled: January 5, 2006Date of Patent: February 9, 2010Assignee: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Jason Allan Wiles
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Patent number: 7648994Abstract: The present invention relates to steroidal alkaloids that can be used in the treatment of hedgehog pathway related disorders, particularly cancer.Type: GrantFiled: March 7, 2008Date of Patent: January 19, 2010Assignee: Infinity Discovery, Inc.Inventors: Alfredo C. Castro, Michael J. Grogan, Martin Tremblay
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Publication number: 20100009992Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.Type: ApplicationFiled: February 4, 2009Publication date: January 14, 2010Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
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Patent number: 7645753Abstract: This invention is concerned with compounds of the formula wherein A, B1, B2, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: March 2, 2006Date of Patent: January 12, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Andreas Dominik Christ, Luke Gideon Granville Green, Wolfgang Guba, Hans-Peter Maerki, Rainer Eugen Martin, Peter Mohr
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Patent number: 7638530Abstract: The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 20, 2004Date of Patent: December 29, 2009Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Zhicai Wu
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Publication number: 20090318436Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: October 14, 2008Publication date: December 24, 2009Applicant: Amgen Inc.Inventors: Brian K. Albrecht, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michelle Potashman, Aaron C. Siegmund, Stephanie K. Springer, Markian Stec, Ning Xi, Kevin Yang
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Patent number: 7625923Abstract: The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X, Y and n are defined herein.Type: GrantFiled: March 2, 2005Date of Patent: December 1, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Alexandra Nirschl, James C. Sutton, Lawrence Hamann, Tammy Wang, Yan Zou, Chongqing Sun
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Patent number: 7625924Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: GrantFiled: December 21, 2005Date of Patent: December 1, 2009Assignee: Memory Pharmaceuticals CorporationInventors: Truc Minh Nguyen, Wenge Xie, Richard Schumacher, Brian Herbert, Ashok Tehim
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Patent number: 7625922Abstract: The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc.Type: GrantFiled: October 21, 2005Date of Patent: December 1, 2009Assignees: Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer Hospital, Astex Therapeutics LimitedInventors: Dan Niculescu-Duvaz, Caroline Joy Springer, Adrian Liam Gill, Richard David Taylor, Richard Malcol Marais, Harmen Dijkstra, Catherine Gaulon, Delphine Menard, Esteban Roman Vela
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Patent number: 7622479Abstract: The present invention provides a heterocyclic compound having potent tyrosine kinase-inhibiting activity represented by formula: (wherein, R1b is a C6-10 aryl group which has substituent(s), and the like; Ta is a single bond, a C1-6 alkyl group, —CH2O—, and the like; X and Y are the same or different, and each is a nitrogen atom which may have substituent(s), and the like; the broken line is a single bond or a double bond; Za is a nitrogen atom or CH; W is a single bond, an oxygen atom, and the like; Q is a C6-10 aryl group which may have substituent(s) or an aromatic heterocyclic group which may have substituent(s)); or a salt thereof and a pharmaceutical composition comprising thereof.Type: GrantFiled: November 25, 2002Date of Patent: November 24, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Oda, Takashi Imada, Kenichiro Naito, Toshiya Tamura, Shuichi Furuya
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Publication number: 20090281138Abstract: 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: November 12, 2009Applicant: AstraZeneca ABInventors: Johan Bylund, Marie E. Ek, Annika Kers, Gunnar Nordvall, Liselotte Ohberg, Jenny Viklund, Stefan Von Berg, Jorg Holenz, Katja Narhi, Daniel Sohn, Martin H. Johansson
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Publication number: 20090275558Abstract: Substituted sulfonamide compounds corresponding to formula I processes for the preparation thereof, pharmaceutical compositions containing such compounds, and the use of such compounds for treating and/or inhibiting pain or other conditions at least partly mediated by the bradykinin 1 receptor.Type: ApplicationFiled: April 9, 2009Publication date: November 5, 2009Applicant: GRUENENTHAL GmbHInventors: Melanie Reich, Ellen Klegraf, Stefan Oberboersch, Stefan Schunk, Ruth Jostock, Sabine Hees, Tieno Germann, Michael Engels
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Publication number: 20090270374Abstract: Bicyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: July 18, 2007Publication date: October 29, 2009Inventors: Llius Ballell, David Barros, Gerald Brooks, Julia Castro Pichel, Steven Dabbs, Robert A. Daines, David Thomas Davies, Jose Maria Fiandor Roman, Israil Pendrak, Modesto J. Remuinan Blanco, Jason Anthony Rossi, Ilaria Giordano, Alan Joseph Hennessy, James B. Hoffman, Graham Elgin Jones, Timothy James Miles, Neil David Pearson, Lihua(lily) Zhang
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Publication number: 20090264653Abstract: Indoles that have activity as inhibitors of FAAH are described as are indoles and indole derivatives that have activity as inhibitors of DAO.Type: ApplicationFiled: December 18, 2006Publication date: October 22, 2009Inventors: Wilmin Bartolini, Brian M Cali, Barbara Chen, Yueh-Tyng Chien, Mark G. Currie, G. Todd Milne, James Philip Pearson, John Jeffrey Talley, Jane Yang, Craig Zimmerman, Charles Kim, Kevin Sprott, Timothy Barden, Regina Lundigran, Ara Mermerian
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Publication number: 20090264405Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: October 30, 2006Publication date: October 22, 2009Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
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Patent number: 7605156Abstract: This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.Type: GrantFiled: May 27, 2005Date of Patent: October 20, 2009Assignee: WyethInventors: John C. McKew, Steve Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark L. Behnke, Baihua Hu, James D. Clark, Wei Li, Valerie Clerin, Suzana Marusic, Kevin Pong
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Publication number: 20090253691Abstract: The present invention relates to 3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.Type: ApplicationFiled: April 19, 2007Publication date: October 8, 2009Applicants: JANSSEN PHARMACEUTICA N.V., BIOFOCUS DPI LIMITEDInventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Anne Simone Josephine Lesage, Wei Zhuang, Marcel Frans Leopold De Bruyn, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck, Theodorus Dinklo
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Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20090239866Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: July 28, 2006Publication date: September 24, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jeffrey Michael Axten, Jesus R. Medina