Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 544/250)
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Publication number: 20130143896Abstract: The present invention relates to substituted isoxazolo-quinazolines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular human MPS1 and PERK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: July 20, 2011Publication date: June 6, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Italo Beria, Nicoletta Colombo, Claudia Piutti, Matteo Salsa, Gabriella Traquandi
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Publication number: 20130129677Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: December 7, 2012Publication date: May 23, 2013Applicant: Siga Technologies, Inc.Inventor: Siga Technologies, Inc.
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Patent number: 8445482Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: April 25, 2012Date of Patent: May 21, 2013Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20130123286Abstract: Certain novel fused quinazoline derivatives of formula (I) as c-Met inhibitors, their synthesis and their uses for treating a c-Met mediated disorder. Methods for treating a c-Met-mediated disorder are also disclosed in the invention.Type: ApplicationFiled: July 14, 2011Publication date: May 16, 2013Inventors: Shaojing Hu, Fei Wang, Wei Long, Xiaoyan Shen, Fenlai Tan, Yinxiang Wang
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Publication number: 20130123105Abstract: The invention relates to isoxazolo[5,4-b]pyridine compounds of formula I, to the agriculturally useful salts of isoxazolo[5,4-b]pyridine compounds of formula I, and to their use as herbicides.Type: ApplicationFiled: July 20, 2011Publication date: May 16, 2013Applicant: BASF SEInventors: Anna Aleksandra Michrowska-Pianowska, Julia Major, Johannes Hutzler, Trevor William Newton, Richard Roger Evans, Klaus Kreuz, Klaus Grossmann, Dschun Song, Anja Simon, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Helmut Kraus, Thomas Seitz, Andree Van der Kloet, Ruediger Reingruber
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Publication number: 20130119360Abstract: Disclosed is an organic electroluminescence element comprising an anode, a cathode and a plurality of organic compound layers between the anode and the cathode, provided that one of the organic compound layers is a light emitting layer containing a phosphorescence emitting compound, wherein at least one of the organic compound layers contains a compound represented by Formula (1), wherein, X represents O or S; Y1 to Y3 each represents a hydrogen atom, a substituent or a group represented by Formula (A) disclosed un the specification, provided that at least two of Y1 to Y3 are groups represented by Formula (A), not all of Y1 to Y3 are the same group, and at least one of the groups represented by Formula (A) has Ar of a carbazolyl group, or an azacarbazolyl group containing 2 to 5 nitrogen atoms.Type: ApplicationFiled: December 13, 2012Publication date: May 16, 2013Inventors: Rie KATAKURA, Shuichi SUGITA, Eisaku KATOH, Motoaki SUGINO, Rie FUJISAWA
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Patent number: 8440654Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: April 25, 2012Date of Patent: May 14, 2013Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20130102623Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: ApplicationFiled: October 10, 2012Publication date: April 25, 2013Inventor: Aleem Gangjee
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Publication number: 20130096146Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: ApplicationFiled: October 9, 2012Publication date: April 18, 2013Inventor: Aleem Gangjee
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Publication number: 20130079323Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.Type: ApplicationFiled: September 10, 2010Publication date: March 28, 2013Applicant: TRIUS THERAPEUTICS, INC.Inventors: Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
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Publication number: 20130065842Abstract: Heterocyclic compounds, and pharmaceutical compositions thereof, are disclosed as ROR?t modulators that have a formula represented by the following: and wherein n1, n2, R1, R2, R3, and R4 are as described herein. These compounds may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.Type: ApplicationFiled: March 11, 2011Publication date: March 14, 2013Inventors: Dan Littman, Jun R. Huh, Wenwei Huang, Ruili Huang
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Patent number: 8383638Abstract: The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: December 13, 2010Date of Patent: February 26, 2013Assignee: Merck Sharp & DohmeInventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng DiMarco, Thomas J. Greshock
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Publication number: 20130045229Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.Type: ApplicationFiled: April 20, 2011Publication date: February 21, 2013Applicant: KINETA, INC.Inventors: Shawn P. Iadonato, Kristin Bedard
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Publication number: 20130023538Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: September 26, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Patent number: 8357707Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase.Type: GrantFiled: July 2, 2010Date of Patent: January 22, 2013Assignee: Novartis AGInventors: Robin Alec Fairhurst, Marc Gerspacher, Robert Mah
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Publication number: 20130018051Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
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Publication number: 20130018057Abstract: A series of quinoline and quinoxaline derivatives, substituted by a fused bicyclic pyridine or pyrimidine moiety attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: November 11, 2010Publication date: January 17, 2013Applicant: UCB PHARMA S.A.Inventors: Roland Bürli, Alan Findlay Haughan, Mîzio Matteucci, Andrew Pate Owens, Gilles Raphy, Andrew Sharpe
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Patent number: 8354418Abstract: The present invention relates to compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.Type: GrantFiled: January 9, 2009Date of Patent: January 15, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Trixi Brandl, Udo Maier, Christoph Hoenke, Anne T. Joergensen, Alexander Pautsch, Steffen Breitfelder, Matthias Grauert, Matthias Hoffmann, Stefan Scheuerer, Klaus Erb, Michael Pieper, Ingo Pragst
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Patent number: 8334378Abstract: Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing these compounds and their use as pharmaceutical compositions.Type: GrantFiled: February 17, 2010Date of Patent: December 18, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Trixi Brandl, Udo Maier, Matthias Hoffmann, Stefan Scheuerer, Anne T. Joergensen, Alexander Pautsch, Steffen Breitfelder, Matthias Grauert, Christoph Hoenke, Klaus Erb, Michael Pieper, Ingo Pragst
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Publication number: 20120316184Abstract: Compounds of formula (I) wherein G1 represents together with the two ring atoms of the pyrimidine ring to which it is attached, a 5- to 6-membered aromatic heterocyclic ring system which contains one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the other substituents are as defined in claim 1, are suitable for use as micro-biocides.Type: ApplicationFiled: February 18, 2011Publication date: December 13, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Martin Pouliot, David Guillaume Claude Francois Lefranc, Laura Quaranta, Clemens Lamberth, Nityakalyani Srinivas
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Patent number: 8329898Abstract: The present invention relates to pyrido[3,2-h]quinazolines and/or 5,6-dihydro derivatives thereof, methods for their production and doped organic semiconductor material which use such quinazolines.Type: GrantFiled: October 27, 2011Date of Patent: December 11, 2012Assignee: Novaled AGInventors: Josef Salbeck, Manfred Kussler, Andrea Lux
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Patent number: 8324227Abstract: The present invention discloses novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.Type: GrantFiled: September 5, 2008Date of Patent: December 4, 2012Assignee: FDC LimitedInventors: Hanumant Bapurao Borate, Suleman Riyajsaheb Maujan, Sangmesher Prabhakar Sawargave, Sheerang Vidhyadhar Joshi, Sharangi Vaiude, Mohan Anand Chandavarkar
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Publication number: 20120302434Abstract: The present invention provides a catalyst complex or ligand, and compositions thereof, for use in a variety of organic reactions having high reactivity and enantioselectivity. The catalyst is a N-heterocyclic carbene having three fused rings with first and second rings being six-membered rings and the third being a five-membered ring. The first ring is fused to the second and has four substituents. The second ring has two nitrogens flanking a carbene atom with one nitrogen bound to a substituent. The carbene atom may optionally be bonded to a metal. The third ring is fused to the second ring and contains two nitrogens. The third ring of the catalyst has a double bond and two substituents on adjacent non-fused carbons. A non-fused nitrogen of the third ring is partially bonded to another substituent. Methods for the synthesis and use of the catalyst embodiments of the present invention are also provided.Type: ApplicationFiled: May 22, 2012Publication date: November 29, 2012Applicant: FLORIDA STATE UNIVERSITY RESEARCH FOUNDATIONInventors: D. TYLER MCQUADE, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
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Patent number: 8309561Abstract: Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: December 21, 2007Date of Patent: November 13, 2012Assignee: Ajinomoto Co., Inc.Inventors: Kazuyuki Sagi, Tatsuya Okuzumi, Tatsuhiro Yamada, Shunsuke Kageyama, Yoichiro Shima, Tadakiyo Nakagawa, Munetaka Tokumasu, Masayuki Sugiki, Hajime Ito, Itsuya Tanabe, Tamotsu Suzuki, Akira Nakayama, Kazuyuki Ubukata, Kenji Shinkai, Yasuhiro Tanaka, Misato Noguchi, Ayatoshi Andou, Yoriko Yamamoto, Noriyasu Kataoka, Koichi Fujita
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Publication number: 20120283238Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: January 10, 2012Publication date: November 8, 2012Applicant: NIMBUS IRIS, INC.Inventors: Donna L. Romero, Matthew David Wessel, Shaughnessy Robinson, Jeremy Robert Greenwood, Karl Shawn Watts, Leah Lynn Frye, Geraldine C. Harriman, Alan Franklin Corin, Craig E. Masse
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Publication number: 20120270855Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: ApplicationFiled: April 25, 2012Publication date: October 25, 2012Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20120264761Abstract: The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: December 13, 2010Publication date: October 18, 2012Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng DiMarco, Thomas J. Greshock
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Publication number: 20120264768Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.Type: ApplicationFiled: February 2, 2012Publication date: October 18, 2012Inventor: Aleem Gangjee
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Patent number: 8288376Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: GrantFiled: January 24, 2012Date of Patent: October 16, 2012Assignee: SanofiInventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
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Patent number: 8288400Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: August 8, 2011Date of Patent: October 16, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
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Publication number: 20120252828Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: December 9, 2010Publication date: October 4, 2012Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
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Patent number: 8273758Abstract: Compounds of formula (I): wherein: Z, R1, R2, R3, n, and m are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.Type: GrantFiled: December 15, 2010Date of Patent: September 25, 2012Assignees: Sanofi, Mitsubishi Tanabe Pharma CorporationInventors: Antonio Almario Garcia, Alistair Lochead, Mourad Saady, Philippe Yaiche
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Publication number: 20120238544Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: ApplicationFiled: April 25, 2012Publication date: September 20, 2012Inventors: James P. Edwards, Daneile K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20120238751Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.Type: ApplicationFiled: March 14, 2012Publication date: September 20, 2012Applicant: TRIUS THERAPEUTICS, INC.Inventors: Daniel Bensen, Zhiyong Chen, John Finn, Thanh To Lam, Suk Joong Lee, Xiaoming Li, Douglas W. Phillipson, Leslie William Tari, Michael Trzoss, Junhu Zhang, Felice C. Lightstone, Toan B. Nguyen, Sergio E. Wong, Paul Aristoff, Michael Jung
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Patent number: 8268846Abstract: Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein.Type: GrantFiled: July 10, 2009Date of Patent: September 18, 2012Assignee: Abbott LaboratoriesInventors: Brian D. Wakefield, Robert J. Altenbach, Lawrence A. Black, Marlon D. Cowart, Irene Drizin, Huaqing Liu
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Publication number: 20120232086Abstract: The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.Type: ApplicationFiled: November 12, 2010Publication date: September 13, 2012Applicant: MERCK SHARP & DOHME CORP.Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew W. Stampford
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Publication number: 20120220588Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, and methods of making and using the same.Type: ApplicationFiled: November 1, 2010Publication date: August 30, 2012Inventors: Lara S. Kallander, Brian Griffin Lawhorn, Joanne Philp
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Publication number: 20120220566Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.Type: ApplicationFiled: October 15, 2010Publication date: August 30, 2012Applicant: Rib-X Pharmaceuticals, Inc.Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Zoltan F. Kanyo, Jacek G. Martinow, Ik-Hyeon Paik, Matthew H. Scheideman, Sandra Sinishtaj, Brian T. Wimberly, Yusheng Wu
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Publication number: 20120214792Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: ApplicationFiled: April 25, 2012Publication date: August 23, 2012Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20120208793Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: ApplicationFiled: April 25, 2012Publication date: August 16, 2012Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20120208828Abstract: The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.Type: ApplicationFiled: June 7, 2010Publication date: August 16, 2012Applicant: OSLO UNIVERSITY HOSPITAL HFInventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss
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Patent number: 8236950Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.Type: GrantFiled: December 19, 2007Date of Patent: August 7, 2012Assignee: Abbott LaboratoriesInventors: David A. Betebenner, Clarence J. Maring, Todd W. Rockway, Curt S. Cooper, David D. Anderson, Rolf Wagner, Rong Zhang, Akhteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie V L. Masse, Robert J. Carrick, Wenping He, Liangjun Lu
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Patent number: 8236802Abstract: The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.Type: GrantFiled: October 2, 2008Date of Patent: August 7, 2012Assignee: Eisai Inc.Inventors: Weizheng Xu, Greg Delahanty, Ling Wei, Jie Zhang
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Publication number: 20120196301Abstract: The present invention relates to the use of binding partners for 5-HT5 receptors for the treatment of neuropathological, in particular neurodegenerative and/or neuropsychiatric, disorders, which can occur, in particular, in cerebral ischemia, stroke, epilepsy and seizures in general, chronic schizophrenia, other psychotic disorders, dementia, in particular Alzheimer's dementia, demyelinizing disorders, in particular multiple sclerosis, and brain tumors. The invention also relates to processes for the identification and characterization of such binding partners, in particular in the form of screening processes.Type: ApplicationFiled: November 15, 2011Publication date: August 2, 2012Inventors: Francisco Javier Garcia-Ladona, Laszlo Szabo, Gerd Steiner, Hans-Peter Hofmann
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Publication number: 20120190654Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: July 28, 2010Publication date: July 26, 2012Applicant: MERCK PATENT GMBHInventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
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Publication number: 20120184734Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: June 14, 2010Publication date: July 19, 2012Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
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Publication number: 20120183577Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: August 8, 2011Publication date: July 19, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
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Patent number: 8222265Abstract: The present invention provides a catalyst complex or ligand, and compositions thereof, for use in a variety of organic reactions having high reactivity and enantioselectivity. The catalyst is a N-heterocyclic carbene having three fused rings with first and second rings being six-membered rings and the third being a five-membered ring. The first ring is fused to the second and has four substituents. The second ring has two nitrogens flanking a carbene atom with one nitrogen bound to a substituent. The carbene atom may optionally be bonded to a metal. The third ring is fused to the second ring and contains two nitrogens. The third ring of the catalyst has a double bond and two substituents on adjacent non-fused carbons. A non-fused nitrogen of the third ring is partially bonded to another substituent. Methods for the synthesis and use of the catalyst embodiments of the present invention are also provided.Type: GrantFiled: August 30, 2010Date of Patent: July 17, 2012Assignee: Florida State University Research FoundationInventors: D. Tyler McQuade, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
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Publication number: 20120178769Abstract: The present invention discloses novel compounds for inhibiting eEF2 kinase and methods of use thereof.Type: ApplicationFiled: July 15, 2010Publication date: July 12, 2012Applicant: The University of Medicine and DentistryInventor: Alexey G. Ryazanov
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Patent number: 8211898Abstract: This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.Type: GrantFiled: July 16, 2009Date of Patent: July 3, 2012Assignee: Ardea Biosciences, Inc.Inventors: Jean-Luc Girardet, Zhi Hong, Stephanie Shaw, Yung-hyo Koh