Halogen Attached Directly Or Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/303)
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Publication number: 20150133301Abstract: 3-alkoxy, thioalkyl and amino-4-amino-6-(substituted)picolinic acids having a halogen, alkyl or mono-, di-tri- and tetra-substituted aryl substituents in the 6-position, and their acid derivatives, are herbicides demonstrating a broad spectrum of weed control.Type: ApplicationFiled: April 29, 2014Publication date: May 14, 2015Applicant: DOW AGROSCIENCES LLCInventors: Jeffrey B. Epp, Christian T. Lowe, James M. Renga, Paul R. Schmitzer, Joseph D. Eckelbarger, Katherine A. Guenthenspberger, Thomas L. Siddall, Carla N. Yerkes, Lindsey G. Fischer, Natalie C. Giampietro, Jeremy Kister, Joshua Roth
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Publication number: 20150111885Abstract: The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Michael John Bennett, Juan Manuel Betancort, Amogh Boloor, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
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Patent number: 9012494Abstract: The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo,Type: GrantFiled: April 29, 2005Date of Patent: April 21, 2015Assignee: Janssen Pharmaceutica N.V.Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Christophe Francis Robert Nestor Buyck, Louis Jozef Elisabeth Van Der Veken, Vladimir Dimtchev Dimitrov, Theo Teofanov Nikiforov
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Patent number: 8952025Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.Type: GrantFiled: April 2, 2013Date of Patent: February 10, 2015Assignee: Arizona Board of Regents, A Body Corporate of the State of Arizona Acting for and on Behalf of Arizona State UniversityInventors: Sidney Hecht, Omar Khdour, Jun Lu, Pablo Arce
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Publication number: 20140301999Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: June 23, 2014Publication date: October 9, 2014Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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Publication number: 20140228310Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one 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 at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.Type: ApplicationFiled: April 28, 2014Publication date: August 14, 2014Applicant: InterMune, Inc.Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid D. Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
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Patent number: 8748462Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I?A or I?B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: GrantFiled: October 13, 2009Date of Patent: June 10, 2014Assignee: Amgen Inc.Inventors: Sean P. Brown, Paul Dransfield, Xiaohui Du, Zice Fu, Jonathan Houze, XianYun Jiao, Sujen Lai, An-Rong Li, Jiwen Liu, Zhihua Ma, Julio C. Medina, Vatee Pattaropong, Wang Shen, Marc Vimolratana, Yingcai Wang, Zhongyu Wang, Ming Yu, Liusheng Zhu
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Patent number: 8716487Abstract: The present invention relates to a process for preparing 4-hydroxypyridines of formula I wherein R1, R2, R3 and R4 have the meanings defined in the description.Type: GrantFiled: June 20, 2011Date of Patent: May 6, 2014Assignee: BASF SEInventors: Volker Maywald, Frederik Menges, Uwe Josef Vogelbacher, Michael Rack, Michael Keil, Wassilios Grammenos, Marianna Vrettou-Schultes, Jan Klaas Lohmann, Bernd Mueller, Thorsten Jabs
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Patent number: 8513222Abstract: This invention relates to use of inhibitors of the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4) in treating, preventing, or reducing fibrosis, cancer, and vascular injuries.Type: GrantFiled: June 24, 2011Date of Patent: August 20, 2013Assignee: EWHA University—Industry Collaboration FoundationInventors: Dae-Kee Kim, Yhun Yhong Sheen, Chenghua Jin, Chul-Yong Park, Domalapally Sreenu, Kota Sudhakar Rao, Maddeboina Krishnaiah, Vura Bala Subrahmanyam
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Publication number: 20130096312Abstract: The present invention relates to a process for preparing 4-hydroxypyridines of formula I wherein R1, R2, R3 and R4 have the meanings defined in the description.Type: ApplicationFiled: June 20, 2011Publication date: April 18, 2013Applicant: BASF SEInventors: Volker Maywald, Frederik Menges, Uwe Josef Vogelbacher, Michael Rack, Michael Keil, Wassilios Grammenos, Marianna Vrettou-Schultes, Jan Klaas Lohmann, Bernd Mueller, Thorsten Jabs
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Publication number: 20130005574Abstract: 3-alkoxy, thioalkyl and amino-4-amino-6-(substituted)picolinic acids having a halogen, alkyl or mono-, di- tri- and tetra-substituted aryl substituents in the 6-position, and their acid derivatives, are herbicides demonstrating a broad spectrum of weed control.Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Inventors: Jeffrey B. Epp, Christian T. Lowe, James M. Renga, Paul R. Schmitzer, Joseph D. Eckelbarger, Katherine A. Guenthenspberger, Thomas L. Siddall, Carla N. Yerkes, Lindsey G. Fischer, Natalie C. Giampietro, Jeremy Kister, Joshua Roth
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Publication number: 20120258924Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one 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 at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.Type: ApplicationFiled: June 20, 2012Publication date: October 11, 2012Applicant: INTERMUNE, INC.Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
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Patent number: 8273773Abstract: Compounds having the formula I wherein R1, R2, R3, R4a, R4b, R4c, R5, R6, R9 and n 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: GrantFiled: July 22, 2009Date of Patent: September 25, 2012Assignee: Roche Palo Alto LLCInventors: Kenneth Albert Brameld, David Scott Carter, Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Eric Brian Sjogren, Francisco Xavier Talamas
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Publication number: 20120208809Abstract: The invention relates to novel 9H-pyrrolo[2,3-b:5,4-c?]dipyridine azacarbolines of formula (I), where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH alkyl, CONH cycloalkyl; CONH heterocycloalkyl; CON(alkyl)2; CON(alkyl)(heterocycloalkyl); CONHN(alkyl)2; C(O)heterocycloalkyl; Rs is H; Hal, OH; O-alkyl(C1-C10); NH2; N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NHC(O)R3a; N(alkyl(C1-C10)C(O)R3a; NHS(O2)R3a; N(alkyl)(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; Ra and Rs optionally form a cycle; R3a is selected from among Hal, CF3, C1-C10 alkyl; C3-C7 cycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; OH; O-alkyl(C1-C10); (C3-C7); heterocycloalkyl (C3-C7); NH2; NH-(alkyl(C1-C10) or cycloalkyl(C3-C7)); N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NH-(alkyl(C1-C10) or heterocycloalkyl(C3-C7)); N(alkyl(C1-C10) or heterocycloalkyl(C3-C7))2, as well as to the isomers anType: ApplicationFiled: November 30, 2009Publication date: August 16, 2012Applicant: SANOFIInventors: Didier Babin, Olivier Bedel, Thierry Gouyon, Serge Mignani, David Papin
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Publication number: 20120183522Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: March 26, 2012Publication date: July 19, 2012Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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Patent number: 8222281Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.Type: GrantFiled: September 29, 2010Date of Patent: July 17, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Narihiro Toda, Masao Yoshida, Rieko Takano, Masahiro Inoue, Takeshi Honda, Koji Matsumoto, Ryutaro Nakashima
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Publication number: 20120022115Abstract: Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.Type: ApplicationFiled: October 7, 2011Publication date: January 26, 2012Applicant: BIOTHERYX INC.Inventors: Frank Mercurio, Kyle W.H. Chan
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Publication number: 20110263845Abstract: It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I): the method including reacting a compound represented by the following formula (III): and a compound represented by the following formula (II): in a solvent and in the presence of a palladium catalyst and a base, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group that may be protected with a protective group, etc.; one of X and Y represents a nitrogen atom and the other represents a nitrogen atom or an oxygen atom; Q represents a leaving group; the ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, etc.Type: ApplicationFiled: December 25, 2008Publication date: October 27, 2011Applicant: Eisai R&D Management Co., Ltd.Inventors: Jun Niijima, Kazuhiro Yoshizawa, Yuki Kosaka, Shinya Abe
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Publication number: 20110201816Abstract: The present inventors succeeded in isolating GWT1 (PfGWT1), which is one of the enzymes involved in GPI biosynthesis in the malaria parasite P. falciparum. In addition, the inventors revealed that degenerate mutant DNAs, with a lower AT content than the DNA encoding the PfGWT1 protein, can complement the phenotype of GWT1-deficient yeast. Based on the findings, the present invention provides the GWT1 protein of malaria parasites and the use of the protein in methods of screening for antimalarial drugs. The present invention also provides degenerate mutant DNAs encoding proteins involved in GPI biosynthesis, and which have a lower AT content than the original DNAs. The present invention also provides methods of screening for antimalarial drugs which use the degenerate mutant DNAs.Type: ApplicationFiled: March 4, 2011Publication date: August 18, 2011Applicant: EISAI R&D MANAGEMENT CO., LTDInventors: Katsura Hata, Kaoru Ogawa, Itaru Tsukada, Kazutaka Nakamoto, Koji Sagane, Keigo Tanaka, Kappei Tsukahara, Toshihiro Horii
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Patent number: 7960554Abstract: Ambient-temperature molten salts of formula (I): wherein Y+ is a cation selected from the group consisting of an ammonium ion, a sulfonium ion, a pyridinium ion, a(n) (iso)thiazolium ion, and a(n) (iso)oxazolium ion that may be optionally substituted with C1-10 alkyl and/or C1-10 alkyl having ether linkage, provided that the above cation has at least one substituent of —CH2Rf1 or —OCH2Rf1 (wherein Rf1 is C1-10 perfluoroalkyl); Rf2 and Rf3 are independently C1-10 perfluoroalkyl or may together form C1-4 perfluoroalkylene; and X is —SO2— or —CO—.Type: GrantFiled: April 16, 2007Date of Patent: June 14, 2011Assignee: Toyota Jidosha Kabushiki KaishaInventor: Teruo Umemoto
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Patent number: 7785678Abstract: The present invention relates to liquid-crystalline mixtures and to novel compounds therefor, and to the use thereof in nematic liquid-crystal displays having positive dielectric anisotropy, such as, for example, STN or IPS displays, which are characterised in that they comprise one or more compounds of the formula (I) in which R1, A1, A2, Z1, Z2, n are as defined in claim (1).Type: GrantFiled: March 21, 2007Date of Patent: August 31, 2010Assignee: Merck Patent GmbHInventors: Michael Junge, Ursula Patwal, Volker Reiffenrath
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Patent number: 7638514Abstract: There are described compounds of formula (I) wherein X1 and X2 are each independently of the other fluorine, chlorine or bromine; A1 and A2 are, for example, a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge; R1 and R2 are, for example, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkyl-carbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C3-C6alkynyl; R,3 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R4 and R5 are, for example, H, halogen, cyano, nitro, C1-C6alkyl or C1-C3haloalkyl; m is 1 or 2; Y is, for example, O, S, SO or SO2; Q is, for example, O, S, SO or SO2; W is, for example, a bond, O, S, SO, S02, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; and E is aryl unsubstituted or substituted from one to five times or heterocyclyl unsubstituted or, depending upon the possibilities of substitution on the ring, substituted from one to four times; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtType: GrantFiled: August 25, 2004Date of Patent: December 29, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Werner Zambach, Stephan Trah, Roger Graham Hall, William Lutz
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Publication number: 20090306115Abstract: In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.Type: ApplicationFiled: April 18, 2006Publication date: December 10, 2009Inventors: Nicholas D. Cosford, Thomas J. Seiders
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Patent number: 7585883Abstract: The present invention is directed to substituted pyridines, methods for their preparation and methods for their use in the treatment and/or prevention of mast cell related conditions.Type: GrantFiled: October 31, 2005Date of Patent: September 8, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Ankush Argade, David Carroll, Alexander B. Rossi
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Patent number: 7528255Abstract: The invention relates to the use of a group of aryl ureas in treating raf mediated diseases and pharmaceutical compositions for use in such therapy of the formula wherein, Y is NHR Hal is chlorine or bromine, R is H, CH3 or CH2OH, and X1 to X7 are each, independently, H, OH or —OC(O)C1-C4 alkyl, or a salt purified stereoisomer thereof, wherein at least one of X1 to X7 is OH or —OC(O)C1-C4 alkyl.Type: GrantFiled: February 11, 2002Date of Patent: May 5, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy Lowinger, William Scott, Roger Smith, Jill Wood
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Patent number: 7514564Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: May 2, 2006Date of Patent: April 7, 2009Assignee: Amgen Inc.Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
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Patent number: 7488828Abstract: 4-Trifluoromethyl-2(1H)-pyridinone is prepared by reaction of 4-alkoxy-1,1,1-trifluorobut-3-en-2-one or 4,4-dialkoxy-1,1,1-trifluorobutan-2-one with a trialkyl phosphonoacetate followed by cyclization.Type: GrantFiled: June 24, 2005Date of Patent: February 10, 2009Assignee: Dow AgroSciences LLCInventors: Christopher Thomas Hamilton, Michael Frederick Gullo, Michael Allen Gonzalez, Gary Alan Roth, David Bruce Gorman, Joachim Gebhardt, Norbert Götz, Hagen Jaedicke, Guido Mayer, Michael Rack
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Patent number: 7446117Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.Type: GrantFiled: September 12, 2003Date of Patent: November 4, 2008Assignee: Glaxo Group LimitedInventors: Paul Beswick, Neil Pegg, Martin Swarbrick, John Skidmore, Sandeep Modi
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Publication number: 20080242705Abstract: The invention relates to a novel use of fluridone—compound known per se and used as an aquatic erbicide—in the medical field, in particular as an active compound for preparing a medicament having anti-inflammatory activity. Pharmaceutical compositions comprising fluridone as an active compound and pharmaceutically acceptable carriers and/or diluents are also disclosed. Finally, there is disclosed the pro-inflammatory activity of abscisic acid (ABA), a plant hormone which is also found in mammal serum and against which fluridone acts an inhibitor.Type: ApplicationFiled: October 6, 2006Publication date: October 2, 2008Inventors: Elena Zocchi, Lucrezia Guida, Santina Bruzzone, Sonia Scarfi, Mirko Magnone, Giovanna Basile, Umberto Benatti, Antonio De Flora, Illana Moreschi, Luisa Franco, Annalisa Salis
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Publication number: 20080214621Abstract: The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention compositions containing these compounds for the treatment of metabolic syndrome, diabetes, hyperglycemia obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula I wherein G1 is methylene or ethylene; L is —(C1-C4)alkylene-, —S—, —CH(OH)—, or —O—; R0 is Formula II or Formula III and the other substituents are as defined in the claims.Type: ApplicationFiled: December 16, 2005Publication date: September 4, 2008Inventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Cassandra A. Gauthier, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace, Alexei Pavlovych Krasutsky, John Gordon Allen
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Publication number: 20080139625Abstract: Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogType: ApplicationFiled: April 29, 2005Publication date: June 12, 2008Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Christophe Francis Robert Nestor Buyck, Louis Jozef Elizabeth Van Der Veken, Vladimir Dimichev Dimitrov, Theo Teofanov Nikiforov
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Patent number: 7342115Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Patent number: 7314873Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammationType: GrantFiled: June 6, 2003Date of Patent: January 1, 2008Assignee: Merck & Co., Inc.Inventors: James B. Doherty, Swaminathan R. Natarajan, John E. Stelmach
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Patent number: 7186839Abstract: A process for extracting from aqueous solution the alkali metal or calcium salt of a halo or haloalkyl substituted 2-hydroxypyridine, or a 2-hydroxyquinoline or 2-hydroxybenzothiazole which comprises contacting an aqueous alkaline or neutral solution of the alkali metal or calcium salt, in which is dissolved an alkali metal fluoride, chloride, bromide, hydroxide, sulphate, sulphite, cyanate, cyanide, thiocyanate, thiosulphate, sulphide, phosphate, hydrogen phosphate, carbonate, bicarbonate, borate, chlorate, hypochlorite, perchlorate, nitrite, chromate, dichromate or permanganate or calcium chloride, bromide, nitrate, nitrite, chlorate, hypochlorite, perchlorate, thiocyanate, thiosulphate, chromate, dichtromate or permanganate, with a partially water-miscible organic solvent so as to transfer aqueous solution of the alkali metal or calcium salt of the 2-hydroxypyridine, 2-hydroxyquinoline or 2-hydroxybenzothiasole into the solvent whilst retaining separate aqueous and solvent phases, and thereafter separatingType: GrantFiled: June 14, 2001Date of Patent: March 6, 2007Assignee: Syngenta LimitedInventors: Raymond Vincent Heavon Jones, Joanne Emma Murray, Jennifer Ann White, Alastair Iain Currie Stewart, Susan Thomson Hamilton, Alan John Whitton, Julie Forrester
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Patent number: 7015320Abstract: The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) process, comprising: contacting a compound of formula (II): with hydrogen under a suitable pressure in the presence of an iridium complex of the formula (R2)IrL+X? wherein L is a chelating diene, X is a non coordinating anion, and R2 is selected fromType: GrantFiled: March 18, 2003Date of Patent: March 21, 2006Assignee: Bristol-Myers Squibb CompanyInventors: William A. Nugent, Tai Yue
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Patent number: 6916933Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: September 24, 2003Date of Patent: July 12, 2005Assignee: Hoffman-La Roche Inc.Inventors: Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
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Patent number: 6858742Abstract: The present invention relates to DNA labeling reagents comprising a furocoumarin derivative and a detectable group with or without bound via a binding enhancer, and acridinium-9-carboxamide derivatives for use as chemiluminescent labels. The present invention also relates to a process of preparing DNA labeling compound.Type: GrantFiled: October 22, 2003Date of Patent: February 22, 2005Assignee: AsiaGEN CorporationInventors: George Chin-Sheng Chou, Yu-Cheng Wu, Po-Ya Hsu
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Patent number: 6844032Abstract: The compound (1) having 2,3-bis(trifluoromethyl)-1,4-phenylene is stable chemically and has excellent miscibility with other liquid crystal compounds, large and negative dielectric anisotropy and proper optical anisotropy. A liquid crystal composition comprising the compound has large specific resistance and a large voltage holding ratio, and that the composition is useful for a liquid crystal display element.Type: GrantFiled: March 29, 2002Date of Patent: January 18, 2005Assignees: Chisso Corporation, Chisso Petrochemical CorporationInventors: Kazutoshi Miyazawa, Takashi Kato, Yasuhiro Kubo, Kanetsugu Terashima
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Patent number: 6828466Abstract: A process to synthesize substituted phenols such as those of the general formula RR′R″Ar(OH) wherein R, R′, and R″ are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed C—H activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.Type: GrantFiled: July 15, 2003Date of Patent: December 7, 2004Assignee: Board of Trustees of Michigan State UniversityInventors: Robert E. Maleczka, Jr., Milton R. Smith, III, Daniel Holmes, Feng Shi
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Patent number: 6765095Abstract: A compound of the formula (I) wherein A is O, S, CHR1 or NR2, R1 and R2 are H, lower alkyl, X1 and X2 are H, halogen, nitro, cyano, etc., Y1 is H, lower alkyl, Z1 and Z2 are H, halogen, cyano, hydroxy, lower alkyl, etc., and n is an integer of 2 to 4, a pharmaceutically acceptable salt thereof, a process for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and an intermediate therefor. The compounds (I) of the present invention show a potent PDE IV inhibitory activity as well as an excellent bronchodilating activity, and hence, they are widely useful as a PDE IV inhibitor in the treatment or prophylaxis of allergic inflammatory diseases or organ inflammatory diseases, especially in the treatment or prophylaxis of pulmonary diseases accompanied by airway obstruction such as asthma.Type: GrantFiled: March 10, 2003Date of Patent: July 20, 2004Assignee: Dainippon Pharmaceutical Company, LimitedInventors: Motoji Kawasaki, Tomohiro Nigo
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Patent number: 6710045Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which m represents integers from 3 to 10, n represents 0, 1 or 2 and Het represents the following, in each case optionally substituted, groupings: to processes for their preparation and to their use as pesticides.Type: GrantFiled: May 12, 2003Date of Patent: March 23, 2004Assignee: Bayer CropScience AGInventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
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Patent number: 6673745Abstract: The invention relates to novel compounds of formula I: wherein R, A, B and X have the meaning given in claim 1; and the agronomically acceptable salts or N-oxides thereof, and to herbicidal compositions containing such compounds as active ingredients.Type: GrantFiled: January 12, 2001Date of Patent: January 6, 2004Assignee: BASF AktiengesellschaftInventors: Thomas Maier, Stefan Scheiblich, Helmut S. Baltruschat
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Patent number: 6670380Abstract: Compounds are provided having the formula: wherein A, Q, and X are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such compounds alone or in combination with other antidiabetic agents such as metformin, glyburide, troglitazone and/or insulin.Type: GrantFiled: November 20, 2001Date of Patent: December 30, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Richard Sulsky, Jeffrey A. Robl
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Patent number: 6632823Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.Type: GrantFiled: December 22, 1997Date of Patent: October 14, 2003Assignee: Merck & Co., Inc.Inventors: Jean-Michel Vernier, Nicholas D. P. Cosford, Ian A. McDonald
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Patent number: 6509471Abstract: The present invention relates to 3-substituted and 2,3-disubstituted pyridine compounds which are useful as intermediates in the synthesis of pyridylsulfonylurea herbicides. The invention also relates to arylation of alcohols using a pyridinediazonium salt. More particularly the arylation process of the instant invention relates to the synthesis of 2,3-disubstituted pyridine compounds via anhydrous diazotization of 3-aminopyridines to form a diazonium salt intermediate that is then reacted with the appropriate alcohol to produce the desired product. The invention additionally relates to pyridine-3-diazonium salt intermediates.Type: GrantFiled: January 22, 2001Date of Patent: January 21, 2003Assignee: Syngenta Participations AGInventor: Dean Kent Hoglen
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Patent number: 6472348Abstract: The present invention relates to pyridone derivatives and herbicidal compositions containing the pyridone derivatives as active ingredients.Type: GrantFiled: May 10, 2001Date of Patent: October 29, 2002Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Mikio Yamaguchi, Yoshihiro Ito, Atsushi Shibayama, Yoshihiro Yamaji, Ryo Hanai, Sota Uotsu, Hideo Sadohara
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Patent number: 6441007Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines, including pyridyloxylalkylamines and phenoxyalkylamines, such as (3-(3-pyridyloxy)propyl)methylamine and (3-(5-bromo(3-pyridyloxy))propyl)methylamine.Type: GrantFiled: July 31, 2000Date of Patent: August 27, 2002Assignee: Targacept, Inc.Inventors: Gary Maurice Dull, Grayland Page Dobson, Jared Miller Wagner
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Patent number: 6437139Abstract: A process is provided for the preparation of compounds of formula I, useful in the preparation of compounds such as Omeprazole, Lansoprazole and Pantoprazole, wherein R1=H or CH3, R2=H or CH3, R3=Alkoxy (1-4C), OCH2CF3, Cyano, Hydrogen, Halogen, Acetoxy or Aryloxy, any electron withdrawing group or salts (organic or inorganic) of electron donating groups, R=Alkoxy, Hydroxy, Halogen, Activated ester, Tosylate, Mesylate, Thiol or Xanthyl, wherein the process for the preparation of compound of formula I employs a free radical reaction to functionalize the 2-position.Type: GrantFiled: June 23, 2000Date of Patent: August 20, 2002Assignee: PDi-Research Laboratories, Inc.Inventors: Michel Zoghbi, Liquin Chen
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Patent number: 6420565Abstract: 2-lithio-5-halopyridine is formed as a predominant component of a reaction mixture by reacting BuLi with 2,5-dihalopyridine in a non-coordinating solvent.Type: GrantFiled: February 27, 2001Date of Patent: July 16, 2002Assignees: Merck & Co., Inc., Merck Frosst Canada & CoInventors: Paul O'Shea, Xin Wang, Richard Tillyer
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Patent number: 6420564Abstract: The present invention provides a process for preparing a tribromomethylsulfonylpyridine, which comprises reacting a methylthiopyridine and a hypobromite in the presence of a base and water in a heterogeneous system. According to the present invention, it is possible to prepare a tribromomethylsulfonylpyridine industrially advantageously, and with high yield and high purity.Type: GrantFiled: October 17, 2001Date of Patent: July 16, 2002Assignee: Sumitomo Seika Chemicals Co., Ltd.Inventors: Eiji Fujisawa, Hiroyuki Hata