The 1,3-diazole Ring Is Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/274.1)
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Publication number: 20120202787Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I; as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: October 12, 2010Publication date: August 9, 2012Inventors: Christopher William am Ende, Douglas Scott Johnson, Martin Youngjin Pettersson, Chakrapani Subramanyam, Christopher John O'Donnell
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Publication number: 20120202834Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: February 7, 2012Publication date: August 9, 2012Applicant: PFIZER INC.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20120149675Abstract: The present invention is concerned with novel 1,2,3-triazole-imidazole compounds of formula (I) wherein X, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention provides a method for the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutic agents.Type: ApplicationFiled: December 2, 2011Publication date: June 14, 2012Inventor: Andrew Thomas
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Publication number: 20120122885Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: October 6, 2011Publication date: May 17, 2012Inventors: Francesco G. Salituro, Jeffrey O. Saunders
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Publication number: 20120115870Abstract: An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.Type: ApplicationFiled: January 11, 2012Publication date: May 10, 2012Applicant: ALCON RESEARCH, LTD.Inventors: Debra L. Fleenor, Iok-Hou Pang, Allan R. Shepard, Mark R. Hellberg, Peter G. Klimko, Abbot F. Clark
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Publication number: 20120110701Abstract: This document discloses molecules having the following formula (Formula One) and processes related thereto.Type: ApplicationFiled: October 31, 2011Publication date: May 3, 2012Applicant: Dow AgroSciences LLCInventors: Negar Garizi, Maurice C. H. Yap, Tony K. Trullinger, CaSandra L. McLeod, Paul R. LePlae, JR., Timothy C. Johnson, Ricky Hunter, John F. Daeuble, SR., Ann M. Buysse
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Publication number: 20120108635Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.Type: ApplicationFiled: May 18, 2010Publication date: May 3, 2012Applicant: Bayer CropScience AGInventors: Tetsuya Murata, Yasushi Yoneta, Hidetoshi Kishikawa, Jun Mihara, Daiei Yamazaki, Mamoru Hatazawa, Norio Sasaki, Kei Domon, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Masashi Ataka, Ulrich Görgens
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Publication number: 20120094837Abstract: The present invention relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which include arthropods and especially insects.Type: ApplicationFiled: July 15, 2011Publication date: April 19, 2012Applicant: Bayer Crop Science AGInventors: Friedrich August MÜHLTHAU, Thomas BRETSCHNEIDER, Reiner FISCHER, Martin FÜßLEIN, Markus HEIL, Achim HENSE, Joachim KLUTH, Adeline KÖHLER, Eva-Maria FRANKEN, Olga MALSAM, Arnd VOERSTE, Peter JESCHKE, Angela BECKER, Peter LÖSEL, Yoshitaka SATO
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Publication number: 20120040977Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: February 22, 2010Publication date: February 16, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Patent number: 8097349Abstract: A novel derivative of heterocyclic compound having nitrogen atom with a structure made by bonding special groups to benzimidazole, a material for an organic electroluminescence (EL) device comprising the derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising at least one organic compound layer containing a light emitting layer sandwiched between a pair of electrodes, wherein the device contains the derivative of heterocyclic compound having nitrogen atom. An organic EL device achieving elevation of luminance and of efficiency in light emission even under low driving voltage is obtainable by an employment of the derivative of heterocyclic compound having nitrogen atom for at least one layer composing organic compound layers of the EL device.Type: GrantFiled: April 7, 2010Date of Patent: January 17, 2012Assignee: Idemitsu Kosan Co., Ltd.Inventors: Hiroshi Yamamoto, Masahide Matsuura, Mineyuki Kubota, Masahiro Kawamura
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Publication number: 20110311649Abstract: The present invention relates to novel imidazole derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is halogen, C1-C4alkyl or C1-C4haloalkyl; R2 is an optionally substituted aryl or heteroaryl; R3 is halogen; R4 is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, hydroxyl, C1-C4alkoxy, OR6, C1-C4haloalkoxy or cyano; R5 is halogen; R6 is hydrogen, C3-C7 cycloalkyl, C3-C10 alkylcycloalkyl, C1-C6 haloalkyl, C2-C6 alkenyl, C2-C6 haloalkenyl, C3-C7 cycloalkenyl, C2-C6 alkynyl, C2-C6 haloalkynyl or C2-C6 alkyloxyalkyl; X is N or C(R); and R is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or cyano; or an agrochemically usable salt form thereof; provided that when X is C(R), R2 cannot be an optionally substituted aryl.Type: ApplicationFiled: October 24, 2008Publication date: December 22, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Raphael Dumeunier, Clemens Lamberth, Stephan Trah, Sebastian Volker Wendeborn
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Publication number: 20110306615Abstract: According to the present invention, a compound represented by formula (I): wherein Q is: A is a hydrogen atom, a halogen atom, —ORa or a C1-4 alkyl group which may be substituted by one or more halogen atoms; E is independently selected from a C1-6 alkyl group; m is selected from integers from 0 to 3; R2 and R3 are independently selected from a C1-6 alkyl group; X1 and X2 are independently selected from O and S; Y is selected from an arylene group and a divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group, wherein the arylene group and the heterocyclic group may be substituted by 1 to 3 substituents independently selected from E1; E1 is independently selected from a hydroxyl group, a halogen atom, a C1-4 alkyl group, a cyano group, a C1-4 alkoky group, a carbamoyl group, a C1-4 alkylcarbamoyl group, a di(C1-4 alkyl)carbamoyl group, an amino group, a C1-4 alkylamino group, a di(C1-4 alkylamino group, a sulfamoyl group, a C1-4 alkylsulfamoyl group and a di(C1-4 alkyl)suType: ApplicationFiled: September 9, 2005Publication date: December 15, 2011Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Kazutaka Tachibana, Haruhiko Sato, Masateru Ohta, Mitsuaki Nakamura, Takuya Shiraishi, Hitoshi Yoshino, Takashi Emura, Akie Honma, Etsuro Onuma, Hiromitsu Kawata, Kenji Taniguchi
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Publication number: 20110294854Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein a, R1, R2, R3, and R4 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Applicant: ABBOTT LABORATORIESInventors: Xenia B. Searle, Ming C. Yeung, Michael R. Schrimpf
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Publication number: 20110294840Abstract: There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitrogen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.Type: ApplicationFiled: February 5, 2010Publication date: December 1, 2011Inventors: Hideki Ihara, Koji Kumamoto
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Publication number: 20110269769Abstract: The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: June 4, 2009Publication date: November 3, 2011Inventors: Linus S. Lin, Marc D. Chioda, Ping Liu, Ravi P. Nargund
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Publication number: 20110245506Abstract: A process for manufacturing a 2,3-disubstituted-5-methoxymethylpyridine of formula (I), where Z is H or halogen; Z1 is H, halogen, CN or NO2; Y2 is OM, and M is an alkali metal or an alkaline earth metal, comprises the step of: (i) reacting a compound of formula (II) where Q is a tertiary aliphatic or cyclic, saturated, partially unsaturated or aromatic amine; Z is H or halogen; Z1 is H, halogen, CN or NO2; Y1 and Y2 are each independently OR1, NR1R2, or when taken together Y1Y2 is —O—, —S— or —NR3—; R1 and R2 are each independently H, C1-C4 alkyl optionally substituted with C1-C1 alkoxy or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms, or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms; R3 is H or C1-C4 alkyl, in a methanol/H2O mixture, comprising at least 20% by weight H2O (based on the sum of water and bromide (II)), with a base comprising MOCH3 and/or MOH, where M is alkali metal or alkalineType: ApplicationFiled: December 7, 2009Publication date: October 6, 2011Applicant: Basf SEInventor: David Cortes
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Publication number: 20110245505Abstract: A process for manufacturing a 5-formyl-pyridine-2,3-dicarboxylic acid ester (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro and R1, R2 are independently C1-C10-alkyl, comprising the steps of (i) reacting a compound of formula (II), wherein the symbols are as in formula (I), with a nitrosation agent (III) R3—O—N?O (III) wherein R3 is C1-C8-alkyl, in the presence of an alkali metal or alkaline earth metal alcoholates or carbonates in a polar aprotic solvent at a temperature of from ?45 to 40° C., to obtain an oxime compound (IV) where Z, Z1, R1 and R2 are as in formula (I), and (ii) reacting oxime compound (IV) with an aliphatic C1-C10-aldehyde in the presence of a Lewis acid at a temperature in the range of from 0 to 100° C. The compounds of formula (I) are useful intermediates in the synthesis of herbicidal imidazolinones, like imazamox.Type: ApplicationFiled: December 7, 2009Publication date: October 6, 2011Applicant: BASF SEInventors: Michael Rack, Joachim Gebhardt, Frederik Menges, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schröder
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Publication number: 20110224252Abstract: The present invention relates to novel imidazole derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is halogen, C1-C4alkyl or C1-C4haloalkyl; R2 is an optionally substituted aryl or heteroaryl; R3 is halogen; R4 is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or cyano; R5 is halogen; X is N or C(R); and R is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or cyano; or an agrochemically usable salt form thereof; provided that when X is C(R), R2 cannot be an optionally substituted aryl.Type: ApplicationFiled: October 24, 2008Publication date: September 15, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Raphael Dumeunier, Clemens Lamberth, Stephan Trah, Sebastian Wendeborn
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Publication number: 20110218340Abstract: 2-[(1-cyanopropyl)carbamoyl]-5-chloromethyl nicotinic acids of formula (I) where Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; R1 is C1-C4 alkyl; R2 is C1-C4 alkyl, C3-C6 cycloalkyl or R1 and R2, when taken together with the atom to which they are attached, represent a C3-C6 cycloalkyl group optionally substituted with methyl, and R3 is hydrogen or a cation preferably selected from the group consisting of alkali metals, alkaline earth metals, manganese, copper, iron, zinc, cobalt, lead, silver, nickel, ammonium and organic ammonium; are useful intermediates for the synthesis of herbicidal imidazolinones.Type: ApplicationFiled: November 3, 2009Publication date: September 8, 2011Applicant: BASF SEInventors: Frederik Menges, Joachim Gebhardt, Michael Rack, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schröder
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Publication number: 20110172427Abstract: This invention relates to a new synthesis, intermediates and precursors leading to a mixture of the compounds 11 and 12 as shown below. It also relates to the resolution of the stereoisomeric mixture to provide in substantial stereochemical purity compound 12. The synthesis of the invention involves preparation of compound 7 and compound 10 as shown below and their reaction to prepare a mixture of compound 11 and compound 12.Type: ApplicationFiled: August 26, 2009Publication date: July 14, 2011Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Taiju Nakamura, Masaaki Matsuda, Yongbo Hu, Daiju Hasegawa, Yorihisa Hoshino, Kazato Inanaga, Minetaka Isomura, Nobuaki Sato, Kazuhiro Yoshizawa, George A. Moniz, Gordon D. Wilkie, Francis G. Fang, Yoshihiro Nishikawa
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Publication number: 20110160210Abstract: An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.Type: ApplicationFiled: March 8, 2011Publication date: June 30, 2011Applicant: ALCON, INC.Inventors: Debra L. Fleenor, Iok-Hou Pang, Allan R. Shapard, Mark R. Hellberg, Abbot F. Clark, Peter G. Klimko
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Publication number: 20110144110Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: August 14, 2009Publication date: June 16, 2011Applicant: N30 PHARMACEUTICALS, LLCInventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Patent number: 7956066Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: GrantFiled: February 8, 2007Date of Patent: June 7, 2011Assignee: Janssen Pharmaceutica NVInventors: Daniel J. Buzard, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20110112097Abstract: The invention relates to compounds of formula (I) wherein the groups R and R?, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.Type: ApplicationFiled: August 6, 2010Publication date: May 12, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Jaehne, Peter Below, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Irvin Winkler
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Publication number: 20110105436Abstract: Provided herein are novel heteroaryl compounds, compositions comprising the compounds, and methods of treatment or prevention comprising administration of the compounds. The compounds are effective in the targeting of cells defective in the von Hippel-Lindau gene and in inducing autophagic cell death. The methods are directed to treating or preventing diseases such as cancer, and in particular cancers resulting from von Hippel-Lindau disease. The compounds of the invention may be administered in combination with another therapeutic agent.Type: ApplicationFiled: March 10, 2009Publication date: May 5, 2011Applicants: AUCKLAND UNISERVICES LIMITED, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Sandra Turcotte, Denise A. Chan, Patrick D. Sutphin, Amato J. Giaccia, Michael P. Hay, William A. Denny, Muriel Marie Bonnet
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Publication number: 20110082155Abstract: The invention provides compounds of formula wherein R1, R3, R4, R5, R6, R7, L, X and Y are as defined in the specification; together with processes and intermediates for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: AstraZeneca ABInventors: Andiappan Murugan, Lena Kristina Bergstrom, Anna Kristoffersson, Martin Lindsjö, Peter Olof Sjö, Mark David Ashton, Jon Meigh
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Publication number: 20110077399Abstract: This invention provides azoles which may be useful as inhibitors of protein tyrosine phosphatases (PTPases). The present invention provides compounds of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds and their use in treating human or animal disorders. The compounds of the invention may be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes, Type II diabetes.Type: ApplicationFiled: December 1, 2010Publication date: March 31, 2011Applicant: TRANSTECH PHARMA, INC.Inventors: Adnan M. M. Mjalli, Robert C. Andrews, Ravindra R. Yarragunta, Rongyuan Xie, Govindan Subramanian, James C. Quada, JR., Murty N. Arimilli, Dharma R. Polisetti
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Publication number: 20110076230Abstract: The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted indole derivatives, compositions, and therapeutic uses and processes for making such compounds.Type: ApplicationFiled: May 28, 2009Publication date: March 31, 2011Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Scott Wolkenberg
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Patent number: 7910743Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: May 20, 2009Date of Patent: March 22, 2011Assignee: Cytokinetics, Inc.Inventors: Bradley P. Morgan, Alex Muci, Erica Kraynack, Pu-Ping Lu, Todd Tochimoto, David J. Morgans, Jr.
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Publication number: 20110053947Abstract: The invention relates to compounds of formula (I) wherein the groups R and R?, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.Type: ApplicationFiled: August 6, 2010Publication date: March 3, 2011Applicant: SANOFI-AVENTISInventors: Gerhard JAEHNE, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER
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Publication number: 20110046378Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's DiseaseType: ApplicationFiled: February 17, 2009Publication date: February 24, 2011Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Qianwa Liang, Brian A. Duclos, Wei Zhang, Peter J.H. Scott, Kai Chen, Zhiyong Gao, Tieming Zhao, Vani P. Mocharla, Dhanalakshmi Kasi, Gang Chen, Eric Wang, Anjana Sinha, Chunfang Xia, Henry Clifton Padgett, Farhad Karimi
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Patent number: 7893076Abstract: The invention relates to the F-crystal form, G-crystal form, H-crystal form, I-crystal form and K-crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, certain processes for their preparation, pharmaceutical compositions containing these crystal forms, their use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, especially humans.Type: GrantFiled: November 23, 2006Date of Patent: February 22, 2011Assignees: Novartis AG, Novartis Pharma GmbHInventor: Michael Mutz
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Publication number: 20110040078Abstract: The present invention relates to a process for the preparation of erythromysin derivatives, in particular telithromycin of formula (I) and its pharmaceutically acceptable salts, providing the isolated intermediates in crystalline form of superior stability and purity.Type: ApplicationFiled: October 10, 2008Publication date: February 17, 2011Applicants: SANDOZ AGInventors: Ingolf Macher, Dominic de Souza
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Publication number: 20110034495Abstract: A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-1-yl or related moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.Type: ApplicationFiled: November 22, 2006Publication date: February 10, 2011Applicant: INTERMUNE, INC.Inventors: Scott D. Seiwert, Karl Kossen, Vladimir Serebryany
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Publication number: 20110015202Abstract: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3, and R4 are as defined in the specification and to pharmaceutically acceptable salts thereof. Compounds of formula I are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.Type: ApplicationFiled: July 9, 2010Publication date: January 20, 2011Inventors: Georg Jaeschke, Lothar Lindemann, Eric Vieira, Juergen Wichmann
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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: 20110009619Abstract: Disclosed is a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, which is effective as a therapeutic or prophylactic agent for a disease induced by A?, wherein Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group, or the like; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group, or the like; X1 represents a double bond, or the like; and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, or the like.Type: ApplicationFiled: August 28, 2008Publication date: January 13, 2011Applicant: Eisai R&D Management Co., Ltd.Inventors: Teiji Kimura, Noritaka Kitazawa, Toshihiko Kaneko, Nobuaki Sato, Koki Kawano, Koichi Ito, Mamoru Takaishi, Takeo Sasaki, Yu Yoshida, Toshiyuki Uemura, Takashi Doko, Daisuke Shinmyo, Daiju Hasegawa, Takehiko Miyagawa, Hiroaki Hagiwara
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Publication number: 20100331326Abstract: The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.Type: ApplicationFiled: June 28, 2010Publication date: December 30, 2010Inventors: Mark G. BOCK, Christoph GAUL, Venkateshwar Rao GUMMADI, Saumitra SENGUPTA
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Patent number: 7851071Abstract: A novel derivative of heterocyclic compound having nitrogen atom with a structure made by bonding special groups to benzimidazole, a material for an organic electroluminescence (EL) device comprising the derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising at least one organic compound layer containing a light emitting layer sandwiched between a pair of electrodes, wherein the device contains the derivative of heterocyclic compound having nitrogen atom. An organic EL device achieving elevation of luminance and of efficiency in light emission even under low driving voltage is obtainable by an employment of the derivative of heterocyclic compound having nitrogen atom for at least one layer composing organic compound layers of the EL device.Type: GrantFiled: January 27, 2004Date of Patent: December 14, 2010Assignee: Idemitsu Kosan Co., Ltd.Inventors: Hiroshi Yamamoto, Masahide Matsuura, Mineyuki Kubota, Masahiro Kawamura
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Patent number: 7846933Abstract: The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 may be the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, —NR3R4, —OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 13, 2008Date of Patent: December 7, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Akira Kubo, Ritsuo Imashiro, Hiroaki Sakurai, Hidetaka Miyoshi, Akihito Ogasawara, Hajime Hiramatsu, Tatsuo Nakajima, Tetsu Nakane
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Publication number: 20100298301Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: May 9, 2008Publication date: November 25, 2010Applicant: SAREUM LIMITEDInventors: John Charles Reader, John Mark Ellard, Helen Boffey, Susanne Taylor, Andrew David Carr, Michael Cherry, Michelle Wilson, Richard Boakye Owoare
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Publication number: 20100273833Abstract: The invention relates to 2-sulfinyl- or 2-sulfonyl-substituted imidazole derivatives of the formula (I) in which the radicals R1, R2, R3 and R4 have the meaning indicated in the description. The compounds of the invention have an immunomodulating and/or cytokine release-inhibiting effect and are therefore suitable for the treatment of disorders associated with an impairment of the immune system.Type: ApplicationFiled: February 27, 2006Publication date: October 28, 2010Inventors: Wolfgang Albrecht, Cornelia Greim, Hans-Gunter Striegel, Karola Tollmann, Philipp Merkle, Stefan Laufer
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Publication number: 20100256165Abstract: A large conductance calcium-activated K channel opener comprising as an active ingredient a nitrogen-containing 5-membered heterocyclic compound represented by the following formula (I): wherein X represents N—R4, O or S, R1 and R2 each independently represent hydrogen, halogen, carboxyl, amino, lower alkyl, lower alkoxycarbonyl, lower alkenyl, cyclo-lower alkyl, carbamoyl, aryl, heterocyclic or heterocyclic-substituted carbonyl group, R3 represents aryl, heterocyclic or lower alkyl group, and R4 represents hydrogen or lower alkyl group, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 7, 2010Publication date: October 7, 2010Inventors: Mitsuya Hongu, Toshihiro Hosaka, Toshihiko Kashiwagi, Rikako Kono, Hiroyuki Kobayashi
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Patent number: 7803819Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: July 17, 2007Date of Patent: September 28, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Markus Boehringer, Daniel Hunziker, Holger Kuehne, Bernd Michael Loeffler, Ramakanth Sarabu, Hans Peter Wessel
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Publication number: 20100233120Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: May 25, 2010Publication date: September 16, 2010Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Patent number: 7795439Abstract: A method for the in-situ treatment of a pyridine-2,3-dicarboxylic acid ester with an oxidizing agent, such as hydrogen peroxide, to improve product quality is provided. The method for the in-situ removal of impurities from a saponified solution of pyridine-2,3-dicarboxylic acid ester comprises the steps of providing a solution of pyridine-2,3-dicarboxylic acid ester, saponifying the solution with a base to form the corresponding pyridine-2,3-dicarboxylic acid salt, reacting the solution with an oxidizing agent in an amount effective to remove impurities, acidifying the solution with an acid to convert the pyridine-2,3-dicarboxylic acid into the corresponding pyridine-2,3-dicarboxylic acid, and collecting a purified solution comprising pyridine-2,3-dicarboxylic acid. Further provided is a method for the preparation of herbicidal 2-(2-imidazolin-2-yl)nicotinic acids, esters, and salts by using a pyridine-2,3-dicarboxylic acid salt prepared by the above method as an intermediate.Type: GrantFiled: June 25, 2004Date of Patent: September 14, 2010Assignee: BASF AktiengesellschaftInventor: Michael A. Levy
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Publication number: 20100216818Abstract: The present invention provides compounds, pharmaceutical compositions, and methods for treating or inhibiting development of AGE- and/or ALE-associated complications in subjects in need thereof.Type: ApplicationFiled: May 7, 2010Publication date: August 26, 2010Inventor: Raja Khalifah
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Publication number: 20100210665Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: ApplicationFiled: February 18, 2010Publication date: August 19, 2010Applicant: The Regents of the University of CaliforniaInventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Derek Welsbie, Chris Tran, John Wongvipat
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Publication number: 20100204260Abstract: A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-?B as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 ?m/mL.Type: ApplicationFiled: January 26, 2010Publication date: August 12, 2010Inventors: Jetze J. Tepe, Satyamaheshwar Peddibhotla
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Patent number: 7759366Abstract: This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R?, R1 to R10, A, D, E, G, L and p are as defined herein. The invention also relates to processes for preparing them, pharmaceutical compositions comprising them and their therapeutic use. The compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.Type: GrantFiled: February 5, 2009Date of Patent: July 20, 2010Assignee: Sanofi-AventisInventors: Gerhard Jaehne, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Irvin Winkler