Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/408)
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Patent number: 7910747Abstract: Pyrazoloamides are provided which are phosphonate and phosphinate glucokinase activators that are useful in treating diabetes and related diseases and have the structure wherein is a pyrazoyl ring; R4 is —(CH2)n—Z—(CH2)m—PO(OR7)(OR8), —(CH2)nZ—(CH2)m—PO(OR7)R9, or —(CH2)nZ—(CH2)m—PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R3(CH2)s, wherein R3 is aryl , s is 0, X is a bond; and n, Z, m, R4, R5, R6, and R7 are as defined herein; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 28, 2007Date of Patent: March 22, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Denis E. Ryono, Peter T. W. Cheng, Scott A. Bolton, Sean Chen, Yan Shi, Wei Meng, Joseph A. Tino
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Publication number: 20110053950Abstract: The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or heteroaryl; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.Type: ApplicationFiled: April 9, 2009Publication date: March 3, 2011Inventors: Marvin Jay Meyers, Matthew James Peic, Barbara Ann Schweitzer, Atli Thorarensen
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Publication number: 20110046159Abstract: The present invention relates to arylpyrazinone derivatives of formula (I), wherein R1, R2, R3 and A are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.Type: ApplicationFiled: March 31, 2009Publication date: February 24, 2011Applicant: Merck Patent GesellschaftInventors: Gérard Botton, Eric Valeur, Christine Charon, Micheline Kergoat, Samer Elbawab
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Publication number: 20110040092Abstract: The invention relates to a process for making HOF.RCN and using it to oxidise organic substrates in a quick and safe way. The process comprises passing diluted fluorine through a conduit and RCN in water through another conduit into a microreactor to form HOF.RCN and reacting this with an organic substrates.Type: ApplicationFiled: September 5, 2008Publication date: February 17, 2011Applicant: THE SECRETARY OF STATE FOR DEFENSEInventors: Christopher Murray, Graham Sandford
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Publication number: 20110021533Abstract: The present invention provides cysteine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.Type: ApplicationFiled: October 4, 2010Publication date: January 27, 2011Applicants: Marquette University, University of Wisconsin- MilwaukeeInventors: James M. Cook, David A. Baker, Edward Merle Johnson, III, Wenyuan Yin
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Publication number: 20110015210Abstract: The present invention relates to pyrazinone derivatives of formula (I), wherein n, R1, R2, R3 and R4 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.Type: ApplicationFiled: January 15, 2009Publication date: January 20, 2011Applicant: MERCK PAATENT GESELLSCHAFTInventors: Gérard Botton, Micheline Kergoat, Christine Charon, Samer Elbawab
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Patent number: 7872009Abstract: 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, 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: GrantFiled: November 14, 2006Date of Patent: January 18, 2011Assignee: Amgen Inc.Inventors: Brian K. Albrecht, Denise Lyn Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Stephen Hitchcock, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Wenge Zhong
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20110003759Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.Type: ApplicationFiled: September 14, 2010Publication date: January 6, 2011Inventors: Philip D. Stein, Sharon N. Bisaha, Saleen Ahmad, Khehyong Ngu, William N. Washburn
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Publication number: 20110003787Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: ApplicationFiled: July 26, 2010Publication date: January 6, 2011Inventors: Akihiro Furukawa, Takehiro Fukuzaki, Yukari Onishi, Hideki Kobayashi, Takeshi Honda, Yumi Matsui, Masahiro Konishi, Kenjiro Ueda, Tetsuyoshi Matsufuji
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Publication number: 20100328600Abstract: The invention provides a liquid crystal compound having stability to heat, light and so forth, a wide temperature range of a nematic phase, a small viscosity, a suitable optical anisotropy, a suitable elastic constant K33, a suitable and negative dielectric anisotropy, and an excellent compatibility with other liquid crystal compounds. The invention provides a liquid crystal composition containing the compound described above and having stability to heat, light and so forth, a small viscosity, a suitable optical anisotropy, a suitable and negative dielectric anisotropy, a suitable elastic constant K33, a low threshold voltage, a high maximum temperature of a nematic phase, and a low minimum temperature of the nematic phase. The invention also provides a liquid crystal display device having a short response time, a small power consumption, a low driving voltage, and a large contrast, and containing the composition described above which can be used in a large temperature range.Type: ApplicationFiled: September 1, 2008Publication date: December 30, 2010Applicants: CHISSO CORPORATION, CHISSO PETROCHEMICAL CORPORATIONInventors: Teru Shimada, Masahide Kobayashi
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Publication number: 20100331234Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.Type: ApplicationFiled: March 3, 2010Publication date: December 30, 2010Applicant: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher Gerard Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel G. Anderson
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Publication number: 20100331328Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc.Type: ApplicationFiled: February 19, 2009Publication date: December 30, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Charles Reader, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Michael Cherry
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Publication number: 20100324061Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.Type: ApplicationFiled: September 1, 2010Publication date: December 23, 2010Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
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Publication number: 20100297077Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: ApplicationFiled: October 3, 2008Publication date: November 25, 2010Applicant: BIONOMICS LIMITEDInventors: Bernard Luke Flynn, Jonathan Bayldon Baell, Jason Hugh Chaplin, Girmit Singh Gill, Damian Wojciech Grobelny, Andrew John Harvey, Jorgen Alvar Mould, Dharam Paul
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Publication number: 20100286394Abstract: Disclosed is an organic amine salt of 6-fluoro-3-hydroxy-2-pyrazinecarbonitrile, which is excellent in crystallinity and useful as a production intermediate for 6-fluoro-3-hydroxy-2-pyrazinecarboxamide.Type: ApplicationFiled: September 25, 2008Publication date: November 11, 2010Applicant: Toyama Chemical Co., Ltd.Inventors: Tamotsu Takamatsu, Kenji Yonezawa
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Publication number: 20100272677Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5a, R5b, R5c and R6 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: April 23, 2010Publication date: October 28, 2010Inventors: Eun Kyung Lee, Ryan Craig Schoenfeld, Francisco Xavier Talamas
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Publication number: 20100266539Abstract: The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.Type: ApplicationFiled: March 25, 2010Publication date: October 21, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Hiroshi Ochiai, Natsuko Tokuda, Shiro Shibayama, Noriki Watanabe, Takaki Komiya, Kazuhiko Takeda
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Publication number: 20100261673Abstract: Embodiments of the present invention provide novel antibacterials that target penicillin-binding proteins or other important cellular targets. Methods for inhibiting growth (reproduction, etc.) of bacteria using compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, such as certain strains of Entercoccus and Staphylococcus aureus.Type: ApplicationFiled: December 21, 2007Publication date: October 14, 2010Applicant: UNIVERSITY OF NOTRE DAME DU LACInventors: Shahriar Mobashery, Peter I. O'Daniel, Mayland Chang
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Publication number: 20100249101Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: January 7, 2010Publication date: September 30, 2010Applicant: SANOFI-AVENTISInventors: Henning STEINHAGEN, Hauke SZILLAT, Markus FOLLMANN, Reinhard KIRSCH, Volkmar WEHNER, Hans MATTER, Martin LORENZ, Kent W. Neuenschwander, Anthony C. SCOTESE
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Publication number: 20100249405Abstract: The present invention relates to novel IAP inhibitor compounds of formula I:Type: ApplicationFiled: December 7, 2007Publication date: September 30, 2010Inventors: Zhuoliang Chen, Run-Ming David Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
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Publication number: 20100249117Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: May 11, 2010Publication date: September 30, 2010Inventors: Yonghong SONG, Zhaozhong J. JIA, Anjali PANDEY, Robert M. SCARBOROUGH, Carroll SCARBOROUGH
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Patent number: 7803802Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.Type: GrantFiled: July 20, 2005Date of Patent: September 28, 2010Assignee: Schering CorporationInventors: Ying Huang, Guoqing Li, Andrew W Stamford
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Publication number: 20100216816Abstract: The present invention is directed to pyrazinyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: ApplicationFiled: October 23, 2008Publication date: August 26, 2010Inventors: James C. Barrow, Zhi-Qiang Yang
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Patent number: 7781437Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.Type: GrantFiled: October 10, 2006Date of Patent: August 24, 2010Assignee: Schering CorporationInventors: Seong Heon Kim, Bandarpalle B. Shankar, Joseph A. Kozlowski, Stuart B. Rosenblum, Neng-Yang Shih
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Publication number: 20100193774Abstract: The invention relates to quinoid compounds and their use in semiconductive matrix materials, electronic and optoelectronic structural elements.Type: ApplicationFiled: July 2, 2008Publication date: August 5, 2010Applicant: NOVALED AGInventors: Olaf Zeika, Ina Faltin, Andrea Lux, Steffen Willmann
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Publication number: 20100197696Abstract: The invention relates to compounds of formula wherein Het, A1, A2, A3, A4, D, W, T, Q, Y, X1, X2, R1, R2, R3, R4, k and m are as defined hereinabove, and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, to a process for the preparation of and to the use of those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, to pesticidal compositions in which the active ingredient has been selected from those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in agrochemically usable salt form, to a process for the preparation of and to the use of those compositions, to plant propagation material treated with those compositions, to a method of controlling pests, to intermediates and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, for the preparation of those compounds, E/Z isomers, mType: ApplicationFiled: April 8, 2010Publication date: August 5, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Roger Graham Hall, Stephan Trah, Werner Zambach, Juraj Tuleja
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Publication number: 20100160292Abstract: Methods of inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, methods of treating patients by inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, chemical entities that bind to BTK and inhibited complexes are provided.Type: ApplicationFiled: September 11, 2007Publication date: June 24, 2010Applicant: CGI PHARMACEUTICALS, INCInventors: James A. Whitney, Julie Di Paolo, Mark Velleca, David R. Brittelli, Kevin S. Currie, James W. Darrow, Jeffrey E. Krope, Seung H. Lee, Steven L. Gallion, Scott A. Mitchell, Doughlas A.I. Pippen, Peter A. Blomgren, Doughlas Gregory Stafford
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Publication number: 20100158860Abstract: Compounds having the formula I wherein A, R1, R2, R3, R4a, R4b, R4c, R5, R6, R7a, R7b, Ar1, Rc, Rd, Re, Rf, X, n and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: December 14, 2009Publication date: June 24, 2010Inventors: Sandra Steiner, Jim Li, Ryan Craig Schoenfeld, Francisco Xavier Talamas
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Patent number: 7737151Abstract: The present invention relates to compounds useful as inhibitors of protein kinases of the following formula: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: August 17, 2006Date of Patent: June 15, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Julian M. C. Golec
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Publication number: 20100137583Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: ApplicationFiled: September 8, 2008Publication date: June 3, 2010Inventors: Robert Edward Babine, Shu-Hui Chen, Jason Eric Lamar, Nancy June Snyder, Xicheng Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Ivan Collado, Cristina Garcia-Paredes, Raymond Samuel Parker, III, Ling Jin, Deqi Guo, John Irvin Glass
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Publication number: 20100137595Abstract: Use vaginal odorant compounds for controlling motile cell chemotaxis.Type: ApplicationFiled: June 27, 2008Publication date: June 3, 2010Applicant: Fraunhofer-Gesellshcaft zur Forderung der angewandten Forschung e.V.Inventor: Andrea Büttner
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Publication number: 20100130739Abstract: Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, an amino group or the like; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, —CO— or the like; and Q is a hydrogen atom or a phenyl group.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Applicant: ASUBIO PHARMA CO., LTD.Inventors: Naohiro Takemoto, Kenji Murata, Norihito Murayama, Chikaomi Yamada
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Patent number: 7723362Abstract: The invention relates to compounds of formula wherein Het, A1, A2, A3, A4, D, W, T, Q, Y, X1, X2, R1, R2, R3, R4, k and m are as defined hereinabove, and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, to a process for the preparation of and to the use of those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, to pesticidal compositions in which the active ingredient has been selected from those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in agrochemically usable salt form, to a process for the preparation of and to the use of those compositions, to plant propagation material treated with those compositions, to a method of controlling pests, to intermediates and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, for the preparation of those compounds, E/Z isomers, mType: GrantFiled: January 7, 2005Date of Patent: May 25, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Roger Graham Hall, Stephan Trah, Werner Zambach, Juraj Tuleja
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Publication number: 20100105694Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in claim 1, having selective 2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.Type: ApplicationFiled: October 10, 2007Publication date: April 29, 2010Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Lourdes Linares De La Morena, Sonia Martinez Gonzalez, Julen Oyarzabal Santamarina, Joaquin Pastor-Fernández, Juan Antonio Vega-Ramiro, Francisca Delgado-Jiménez, Wilhelmus Helena Ignatius Maria Drinkenburg
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Publication number: 20100075924Abstract: Deoxyuridine derivatives of the formula where A is O, S or CH2; B is O, S or CHR3; R1 is H, or various substituents; R2 is H, F; R3 is H, F, OH, NH2; or R2 and R3 together form a chemical bond; D is —NHCO—, —CONH—, —O—, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, or a stable monocyclic, bicyclic or tricyclic ring system have utility in the prophylaxis o treatment of parasitic diseases such as malariaType: ApplicationFiled: August 28, 2009Publication date: March 25, 2010Applicant: Medivir ABInventors: Ian Gilbert, Corinne Nguyen, Gian Filippo Ruda, Alessandro Schhipani, Ganasan Kasinathan, Nils-Gunnar Johansson, Dolores Gonzales Pacanowska
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Patent number: 7652010Abstract: Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile, the compounds may be used for the treatment of various diseases or disorders, including those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: October 14, 2005Date of Patent: January 26, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen
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Publication number: 20100010000Abstract: An amino alcohol derivative useful as an excellent immunosuppressive agent is provided. As a result of intensive research to create a highly safe compound which has an excellent immunosuppressive activity, it was discovered that an amino alcohol derivative represented by the general formula (1), has excellent immunosuppressive activity.Type: ApplicationFiled: August 7, 2007Publication date: January 14, 2010Inventors: Yasushi Kohno, Kiyoshi Fujii, Tatsuhiro Saito, Kazuhiko Kuriyama, Tokutarou Yasue
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Publication number: 20090318455Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.Type: ApplicationFiled: June 3, 2009Publication date: December 24, 2009Applicant: INTERMUNE, INC.Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid Beigelman, Luca F. Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
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Publication number: 20090318684Abstract: The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are compounds that inhibit Rho-protein associated kinase function. Compounds of the invention include piperazinyl pyridines, piperazinylmethyl pyridines, piperazinyl ureas and carbamates, piperazinyl pyridines and quinoilines (including isoquinliones) as well as piperazinyl (including piperazinylmethyl) pyridines and quinolines (including isoquinolines). Compounds of the invention disrupt Rho-kinase activation and function and significantly inhibit tumor cell growth and induce tumor cell death.Type: ApplicationFiled: June 22, 2009Publication date: December 24, 2009Applicants: UNIVERSITY OF SOUTH FLORIDA, YALE UNIVERSITYInventors: Said M. Sebti, Andrew D. Hamilton
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Publication number: 20090306052Abstract: The present invention relates to novel indenyl derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.Type: ApplicationFiled: December 5, 2005Publication date: December 10, 2009Inventor: David Matthew Wilson
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Publication number: 20090299067Abstract: A method for the synthesis of 2,6-Diamino-3,5-dinitropyrazine-1-oxide including nitration of 2,6-diaminopyrazine-1-oxide. The step of nitration may use nitrating agents 20% Oleum/100% HNO3, 100% HNO3 and conc. H2504/100% HNO3 or nitronium tetrfluoraoborate. The synthesis of 2,6-diaminopyrazine-1-oxide may involve both the oxidation of 2,6-diaminopyrazine, the amination of a precursor 2,6-disubstitutedpyrazine-1-oxide or direct formation of the 2,6-diaminopyrazine-l-oxide from the precursor, 2-amino-6-hydroxamino-pyrazine-1-oxide.Type: ApplicationFiled: May 30, 2008Publication date: December 3, 2009Inventors: Philip F. Pagoria, Alexander R. Mitchell, Kason Bala
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Publication number: 20090291936Abstract: The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 20, 2008Publication date: November 26, 2009Inventors: Kazutoshi Sugawara, Tetsuji Matsudaira, Hiroshi Sugama, Masao Nawano, Rikiya Ohashi
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Publication number: 20090281109Abstract: The present invention provides cysteine and cystine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.Type: ApplicationFiled: February 9, 2009Publication date: November 12, 2009Inventors: James M. Cook, David A. Baker, Wenyuan Yin, Edward Merle Johnson, II
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Patent number: 7615635Abstract: Novel N-formyl hydroxylamine compounds and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed.Type: GrantFiled: May 22, 2006Date of Patent: November 10, 2009Assignees: Novartis AG, Vicuron Pharmaceuticals, Inc.Inventors: Kathryn Rene Bracken, Simon Bushell, Karl Dean, Charles Francavilla, Rakesh K. Jain, Kwangho Lee, Mohindra Seepersaud, Lei Shu, Arathi Sundaram, Zhengyu Yuan
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Patent number: 7608618Abstract: Compounds of the formula wherein: Y? is O or S, W? is optionally substituted, Z? is selected from the group consisting of wherein Q? is OR7 and R7 is C1-3alkyleneC3-8heterocycloalkyl useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.Type: GrantFiled: April 27, 2005Date of Patent: October 27, 2009Assignee: Icos CorporationInventors: Edward A. Kesicki, John Joseph Gaudino, Adam Wade Cook, Scott Douglas Cowen, Laurence Edward Burgess
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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: 20090227601Abstract: The invention encompasses novel compounds and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for treatment of diseases mediated by B1 bradykinin receptor.Type: ApplicationFiled: December 6, 2006Publication date: September 10, 2009Applicant: Amgen Inc.Inventors: Jiawang Zhu, Jian Jeffrey Chen, Jason B. Human, Wenyuan Qian
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Patent number: 7560462Abstract: Substituted urea compounds useful in the treatment of diseases and C1-3alkyleneOR3 conditions related to DNA damage or lesions in DNA replication are disclosed formula (I), wherein X1 is null, —O—, —S—, —CH2—, or —N(R1)—; X2 is —O—, . -£>. -, or —N(R1)—,—. . Y xs 0 or S; or =y represents two hydrogen atoms attached to a common carbon atom, —W is selected from the group consisting of heteroaryl, aryl, heterocycloalkyl, cycloalkyl, and C1-6alkyl substituted with a heteroaryl. or aryl group; R6 is —C?C—R7 or heteroaryl; R8, R9, and R10, independently, are selected from the group consisting of halo, optionally substituted C1-6alkyl, C2-6alkenyl, C2-6alkynyl, OCP3, CF3, NO2, CN, NC, N(R3)2, OR3, CO2R3, C(O)N (R3)2, C(O)R3, N(R1)COR3, N(R1)C(O)OR3, N(R8)C(O)OR3, N(R1)C(O)C1-3alkyleneC(O)R3, N(R1)C(O)C1 -3alkyleneC(O)OR3, N(R1)C(O)C1-3alkyleneOR3, N(R1)C(O)C1-3alkyleneNHC(O)OR3, N(R1)C(O)C1-3alkyleneSO2.Type: GrantFiled: July 1, 2005Date of Patent: July 14, 2009Assignee: ICOS CorporationInventors: John Joseph Gaudino, Adam Wade Cook
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Patent number: 7553972Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: February 9, 2007Date of Patent: June 30, 2009Assignee: Pfizer, Inc.Inventors: Mark A. Dombrowski, Allen J. Duplantier, Chakrapani Subramanyam