Polycyclo Ring System Containing Anthracene Configured Ring System Having At Least One Double Bond Between Ring Members And Having Oxygen Single Bonded Or Any Atom Double Bonded Directly At The 9- Or 10- Positions (e.g., Anthrone, Anthraquinone, Etc.) Patents (Class 548/356.5)
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Publication number: 20150045358Abstract: A pharmaceutical composition for treating disorders associated with insulin resistance is disclosed, and the composition comprises at least one inhibitor which is an effective agent to suppress endothelin-1-stimulated resistin gene expression through decreasing the endothelin-1-stimulated phosphorylation of proteins downstream of endothelin type A receptor, wherein the downstream signaling molecules comprise ERK1/2, JNKs, AKT, and STAT3 proteins, and wherein the inhibitor is selected from at least one antagonist of the endothelin type A receptor or downstream signaling proteins.Type: ApplicationFiled: May 21, 2013Publication date: February 12, 2015Inventors: Yung-hsi KAO, Ya-chu Tang, Hsin-huei Chang, Hui-chen Ku
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Patent number: 8940911Abstract: A library of unnatural squarylated homoserine lactones (SHLs) and squarylated lactones that bear potential to modulate biofilm formation in Gram negative bacteria. At low concentrations (˜200 ?M), these small molecules inhibit biofilm formation of E. coli. Moreover, these compounds are not toxic up to 300 ?M and do not significantly attenuate E. coli growth. The SHLs have potential to disperse established biofilm and demonstrate an enhanced reduction (˜50%) of the maximum biofilm thickness by use of SHLs during biofilm growth.Type: GrantFiled: August 1, 2013Date of Patent: January 27, 2015Assignee: Syracuse UniversityInventors: Yan-Yeung Luk, Sri Kamesh Narasimhan, Eric Falcone
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Patent number: 8846745Abstract: A method of treating insulin resistance, obesity and metabolic syndrome by administering an indazolemethoxyalkanoic acid as described herein.Type: GrantFiled: May 8, 2012Date of Patent: September 30, 2014Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Angelo Guglielmotti, Giuseppe Biondi
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Publication number: 20140221357Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 25, 2012Publication date: August 7, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Publication number: 20140066466Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.Type: ApplicationFiled: March 12, 2012Publication date: March 6, 2014Applicant: President and Fellows of Harvard CollegeInventor: Junying Yuan
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Publication number: 20140039195Abstract: A library of unnatural squarylated homoserine lactones (SHLs) and squarylated lactones that bear potential to modulate biofilm formation in Gram negative bacteria. At low concentrations (˜200 ?M), these small molecules inhibit biofilm formation of E. coli. Moreover, these compounds are not toxic up to 300 ?M and do not significantly attenuate E. coli growth. The SHLs have potential to disperse established biofilm and demonstrate an enhanced reduction (˜50%) of the maximum biofilm thickness by use of SHLs during biofilm growth.Type: ApplicationFiled: August 1, 2013Publication date: February 6, 2014Applicant: SYRACUSE UNIVERSITYInventors: Yan-Yeung Luk, Sri Kamesh Narasimhan, Eric Falcone
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Patent number: 8536157Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.Type: GrantFiled: April 14, 2008Date of Patent: September 17, 2013Assignee: The University of MelbourneInventors: Alastair Stewart, Martin Banwell, Brenda Leung, Anu Augustine, Jacki Kitching, Thomasz Bilski
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Publication number: 20130203786Abstract: The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: May 16, 2011Publication date: August 8, 2013Inventors: Jacqueline D. Hicks, Tesfaye Biftu, Ping Chen, Xiaoxia Qian, Robert R. Wilkening
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Patent number: 8344016Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: GrantFiled: September 9, 2010Date of Patent: January 1, 2013Assignee: AstraZeneca ABInventors: Martin John Packer, James Stewart Scott, Andrew Stocker, Paul Robert Owen Whittamore
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Publication number: 20120214847Abstract: The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 26, 2010Publication date: August 23, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Christopher James Bungard, James J. Perkins, Jesse J. Manikowski, Pablo de Leon, Robert S. Meissner
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Patent number: 8198310Abstract: Use of a compound of formula (I) in which R, R? and R? have the meanings given in the description, optionally in the form of a salt thereof with a pharmaceutically acceptable organic or mineral base, to prepare a pharmaceutical composition for reducing the blood triglyceride, cholesterol and glucose levels.Type: GrantFiled: November 13, 2007Date of Patent: June 12, 2012Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F.S.p.A.Inventors: Angelo Guglielmotti, Giuseppe Biondi
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Publication number: 20120046255Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 14, 2008Publication date: February 23, 2012Applicant: THE UNIVERSITY OF MELBOURNE of ROYAL PARADE PARKVILLEInventors: Alastair Stewart, Martin Banwell, Brenda Leung, Anu Augustine, Jacki Kitching, Tomasz Bilski
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Publication number: 20110237628Abstract: This invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of the formula I wherein A and R1 to R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. The invention relates also to compositions including these compounds and methods of using the compounds.Type: ApplicationFiled: March 17, 2011Publication date: September 29, 2011Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Bernd Kuhn, Hans Richter, Sven Taylor
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Publication number: 20110178075Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, 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 (indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: March 7, 2011Publication date: July 21, 2011Inventors: Wenge XIE, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
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Publication number: 20110144121Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: June 16, 2010Publication date: June 16, 2011Applicant: CARA THERAPEUTICS, INC.Inventor: Robert Zhiyong Luo
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Publication number: 20110124878Abstract: A compound of Formula II and salts thereof are useful in the preparation of a compound of Formula I and pharmaceutically acceptable salts and prodrugs thereof.Type: ApplicationFiled: February 3, 2011Publication date: May 26, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Robert Groneberg, Laurence E. Burges, Darren Harvey, Ellen Laird, Mark C. Munson, James P. Rizzi, Martha Rodriguez, Charles Todd Eary, Daniel John Watson
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Publication number: 20110118236Abstract: An object of the present invention is to provide a novel AMPA receptor potentiator. A compound represented by the following formula (I) or a salt thereof: wherein in formula (I) R1 represents (1) a halogen atom, or (2) cyano group, or the like; Ra and Rb each independently represent a hydrogen atom or C1-4 alkyl; L represents a bond, or a spacer in which the number of atoms in the main chain is 1 to 8; Ring A represents (1) a non-aromatic carbon ring of 4-8 carbon atoms, or (2) a 4- to 8-membered non-aromatic heterocycle either of which is optionally substituted with 1 or more substituents selected from (a) halogen atoms, and (b) cyano group; and Ar represents a substituted phenyl group, or optionally substituted 5- or 6-membered aromatic heterocyclic group.Type: ApplicationFiled: March 25, 2009Publication date: May 19, 2011Inventors: Michiyo Mochizuki, Shotaro Miura
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Publication number: 20110053883Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect c-Jun NH2-terminal kinase; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a c-Jun NH2-terminal kinase in a reaction system in which the c-Jun NH2-terminal kinase contacts with a test substance, and the like.Type: ApplicationFiled: June 23, 2006Publication date: March 3, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yasutaka Shimokawatoko, Mar Van De Craen, Irene Nooren, Sandra Turconi, Annelies Roobrouck, Wendy Maddelein
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Publication number: 20100305120Abstract: Compounds of formula (I): wherein X, L1, R1, L2, R2, R3, and R4 are as defined herein, are useful in the treatment or prophylaxis of Duchenne muscular dystrophy, Becker muscular dystrophy, or cachexia.Type: ApplicationFiled: April 3, 2009Publication date: December 2, 2010Inventors: Graham Michael Wynne, Stephen Paul Wren, Renate Maria Van Well, Daniel Robert Chancellor, Frank Schroer, Francis Xavier Wilson
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Patent number: 7816391Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: GrantFiled: October 28, 2008Date of Patent: October 19, 2010Assignee: AstraZeneca ABInventors: Martin John Packer, James Stewart Scott, Andrew Stocker, Paul Robert Owen Whittamore
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Publication number: 20100249123Abstract: The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1n are defined as in formula I; invention compounds are modulators of follicle-stimulating hormone—(“FSH”) which are useful for male and female contraception as well as other disorders modulated by FSH receptor.Type: ApplicationFiled: March 19, 2008Publication date: September 30, 2010Applicant: ADDEX PHARMA SAInventors: Beatrice Bonnet, Brice Campo, Luca Raveglia, Mauro Riccaboni
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Publication number: 20100113762Abstract: Methods and apparatus for facilitating the synthesis of compounds in a batch device are presented. Application of the batch type microfluidic devices to the synthesis of radiolabeled compounds is described. These methods and apparatus enable the selective introduction of multiple reagents via an enhanced rotary flow distribution valve through a single inlet port of the synthetic device. The sequential introduction of multiple reagents through a single inlet port allows an optimal delivery of highly concentrated reagents into the reactor and facilitates the synthesis of the desired products with a minimal loss of materials during transfers, which is critical to the synthesis of radiolabeled biomarkers.Type: ApplicationFiled: November 4, 2009Publication date: May 6, 2010Applicant: Siemens Medical Solutions USA, Inc.Inventors: Carroll Edward Ball, Arkadij M. Elizarov, Hartmuth C. Kolb, Reza Miraghaie, Jianzhong Zhang
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Publication number: 20100087467Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein A, B, Q, R1, and R2 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT or PDK1 kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds, and methods of utilizing those compositions in the treatment of various disorders.Type: ApplicationFiled: December 9, 2009Publication date: April 8, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Hayley Binch, Simon Everitt, Francesca Mazzei, Daniel Robinson
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Publication number: 20100062429Abstract: Provided are compounds, methods and kits for identifying in cells of interest organelles including nuclei and a wide variety of organelles other than nuclei (non-nuclear organelles), as well as cell regions or cell domains. These compounds and methods can be used with other conventional detection reagents for identifying the location or position or quantity of organelles and even for distinguishing between organelles in cells of interest.Type: ApplicationFiled: September 8, 2008Publication date: March 11, 2010Inventors: Wayne Forrest Patton, Praveen Pande, Yuejun Xiang, Zaiguo Li, James J. Donegan, Elazar Rabbani
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Publication number: 20100056596Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.Type: ApplicationFiled: March 20, 2009Publication date: March 4, 2010Applicant: Sequoia PharmaceuticalsInventors: Michael Eissenstat, Andrey Topin, Greg Delahanty, Gnana Ravi Rajendran
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Patent number: 7662821Abstract: The invention relates to tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents.Type: GrantFiled: October 12, 2004Date of Patent: February 16, 2010Assignee: Bayer Schering Pharma AGInventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
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Patent number: 7659297Abstract: The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) process for their production and their use as antiinflammatory agents.Type: GrantFiled: October 8, 2004Date of Patent: February 9, 2010Assignee: Bayer Schering Pharma, AGInventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
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Publication number: 20090143422Abstract: This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.Type: ApplicationFiled: February 2, 2009Publication date: June 4, 2009Applicant: ARRAY BIOPHARMA INC.Inventors: Mark Munson, David A. Mareska, Youngboo Kim, Robert D. Groneberg, James Rizzi, Martha Rodriguez, Ganghyeok Kim, Guy Vigers, Chang Rao, Devan Balachari, Darren Harvey
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Publication number: 20090137655Abstract: The invention provides non-steroidal ligands for the glucocorticoid receptor, methods for making non-steroidal ligands of the glucocorticoid receptor, compositions of non-steroidal ligands of the glucocorticoid receptor and methods of using non-steroidal ligands and compositions of non-steroidal ligands of the glucocorticoid receptor for treating or preventing diseases (e.g., obesity, diabetes, depression, neurodegeneration or an inflammatory disease) associated with glucocorticoid binding to the glucocorticoid receptor.Type: ApplicationFiled: February 3, 2009Publication date: May 28, 2009Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Thomas S. Scanlan, Nilesh Shah
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Publication number: 20090137420Abstract: This invention is directed to methods for screening and identification of compounds capable of selectively eliminating cancer cells with specific loss-of-function alterations, including but not limited to mutations, deletions, hypermethylations, and other types of gene silencing. This invention is also directed to novel compounds that selectively eliminate cancer cells with specific loss-of-function alterations. Furthermore, this invention is directed to methods for production and therapeutic use of compounds that selectively eliminate cancer cells with specific loss-of-function alterations.Type: ApplicationFiled: April 14, 2006Publication date: May 28, 2009Inventors: Daniel D. Von Hoff, Haiyong Han, Hong Wang, Gary A. Flynn
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Publication number: 20090082346Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.Type: ApplicationFiled: July 29, 2008Publication date: March 26, 2009Applicant: Pfizer Italia S.r.l.Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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Publication number: 20090048250Abstract: The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.Type: ApplicationFiled: August 20, 2007Publication date: February 19, 2009Inventors: Alex Aronov, David J. Lauffer, Huan Qiu Li, Ronald Charles Tomlinson, Pan Li
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Patent number: 7442794Abstract: The invention relates to the compounds of formula I, a process for their production and their use as anti-inflammatory agents.Type: GrantFiled: October 8, 2004Date of Patent: October 28, 2008Assignee: Schering AGInventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
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Publication number: 20080214641Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicamentsType: ApplicationFiled: December 20, 2007Publication date: September 4, 2008Inventors: Markus Berger, Jan Dahmen, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepisto, Darren McKerrecher, Magnus Munck af Rosenschold, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
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Publication number: 20080207721Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: November 21, 2007Publication date: August 28, 2008Inventors: Markus Berger, Lena Bergstrom, Jan Dahmen, Anders Eriksson, Balint Gabos, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepisto, Stinabritt Nilsson, Camilla Taflin, Darren McKerrecher, Hartmut Rehwinkel
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Publication number: 20080036373Abstract: A platinum complex represented by the general formula (1) below, useful as a phosphorescence emission material, a tetradentate ligand useful for synthesizing the platinum complex, and a light-emitting device containing at least one of the platinum complex. wherein ring B represents a nitrogen-containing aromatic heterocyclic ring; rings A, C and D each independently represent an aromatic or aromatic heterocyclic ring, while either of the rings C and D represents five-membered ring, the other represents a five- or six-membered ring; RA, RB, RC, and RD respectively represent substituents on the rings A, B, C, and D; two of XA, XB, XC, and XD represent a nitrogen atom that may be bound with the platinum atom by a coordinate bond, the others each independently represent a carbon atom or nitrogen atom that may be bound with the platinum atom by a covalent bond; Q represents a bivalent atom or atomic group bridging the rings B and C; and YC and YD each independently represent a carbon atom or nitrogen atom.Type: ApplicationFiled: August 8, 2007Publication date: February 14, 2008Inventors: Hisanori Itoh, Takeshi Iwata, Yoshimasa Matsushima
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Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Patent number: 6358980Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: January 27, 2000Date of Patent: March 19, 2002Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
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Patent number: RE39198Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amounts of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 15, 2000Date of Patent: July 18, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Yulin Chiang, Kenneth J. Bordeau, Edward J. Glamkowski
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Patent number: RE40183Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula wherein R, X, R5 and R6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.Type: GrantFiled: June 3, 2005Date of Patent: March 25, 2008Assignee: Wyeth Holdings CorporationInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross