Plural 1,4-oxazine Rings Are Cyclos In The Polycyclo Ring System Patents (Class 544/74)
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Patent number: 11543404Abstract: The present invention provides a nerve cell device in which early observation of nerve activity (spikes, bursts, and the like) is made possible and the measured electric strength is increased by cultivating neurons upon a cell scaffold. By using this nerve cell device, imaging of intracellular signaling is also possible.Type: GrantFiled: November 15, 2018Date of Patent: January 3, 2023Assignee: STEM CELL & DEVICE LABORATORY, INC.Inventors: Kazuhiro Aiba, Norie Tooi, Kosuke Hori, Masaki Sudo
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Patent number: 10107493Abstract: The present invention provides a safer all-around radiation heating assembly than similar traditional heaters. As typical with traditional heaters, a shroud is used to surroundably cover a portable liquid propane tank. To replace the portable liquid propane tank, the shroud must be continuously raised to a predetermined height while a service person accesses the propane tank. There is a danger that if and when the shroud drops, a spark could be created resulting in igniting highly flammable escaped propane gas. The present invention overcomes dangers associated with the traditional heaters by eliminating the spark creation danger and by introducing a ventilation system to allow any leaked propane gas to escape away from the heater.Type: GrantFiled: March 28, 2016Date of Patent: October 23, 2018Assignee: CHANGZHOU GARDENSUN FURNACE CO., LTD.Inventor: Jianping Wang
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Patent number: 9890951Abstract: The present invention provides a safer all-around radiation heating assembly than similar traditional heaters. As typical with traditional heaters, a shroud is used to surroundably cover a portable liquid propane tank. To replace the portable liquid propane tank, the shroud must be continuously raised to a predetermined height while a service person accesses the propane tank. There is a danger that if and when the shroud drops, a spark could be created resulting in igniting highly flammable escaped propane gas. The present invention overcomes dangers associated with the traditional heaters by eliminating the spark creation danger and by introducing a ventilation system to allow any leaked propane gas to escape away from the heater.Type: GrantFiled: March 28, 2016Date of Patent: February 13, 2018Assignee: CHANGZHOU GARDENSUN FURNACE CO.Inventor: Jianping Wang
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Patent number: 9540514Abstract: The present disclosure provides carbazole-dioxazine pigment of Formula I; wherein, R is C1-C8 alkyl group, preferably R is an ethyl group, R1 is a chloro group, and R2 is a —NHC(?O)Ph group. The pigment is synthesized from 3-nitro-N-ethylcarbazole. The first step is nitration of 3-nitro-N-ethylcarbazole to form 3,6-dinitro-N-ethylcarbazole which is reduced to form 3-amino-6-nitro-N-ethylcarbazole. This amino compound is benzoylated to form 3-benzamido-6-nitro-N-ethylcarbazole which is then hydrogenated to form 6-amino-3-benzamido-N-ethylcarbazole. Condensation of 6-amino-3-benzamido-N-ethylcarbazole with chloranil provides an intermediate. Cyclization of the intermediate in the presence of a cyclization reagent provides the compound of Formula-I. The pigment has wavelength of maximum absorption (?max) at 571 nm in dimethylformamide as a solvent.Type: GrantFiled: June 11, 2014Date of Patent: January 10, 2017Inventor: Keki Hormusji Gharda
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Patent number: 9533998Abstract: The present disclosure relates to a benzoyl substituted carbazole-dioxazine pigment and its preparation. The process involves benzoylation of 3-nitro-N-ethylcarbazole in monochlorobenzene using benzoylchloride and ferric chloride to yield 3-nitro-6-benzoyl-N-ethyl carbazole, which on catalytic hydrogenation and subsequent condensation with chloranil and cyclization yields benzoyl substituted carbazole-dioxazine pigment.Type: GrantFiled: April 25, 2014Date of Patent: January 3, 2017Inventor: Keki Hormusji Gharda
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Publication number: 20150099737Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R1, R2y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: December 12, 2014Publication date: April 9, 2015Applicant: NOVARTIS AGInventors: Christopher Thomas BRAIN, Young Shin CHO, John William GIRALDES, Bharat LAGU, Julian Roy LEVELL, Michael Joseph LUZZIO, Lawrence Blas PEREZ, Yaping WANG, Fan YANG
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Publication number: 20150079081Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.Type: ApplicationFiled: October 27, 2014Publication date: March 19, 2015Applicant: Genentech, Inc.Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQuing Wei
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Publication number: 20150041784Abstract: A compound represented by the general formula (1) is useful as a light-emitting material. In the general formula (1), Ar1 to Ar3 represent an aryl group, provided that at least one thereof represents an aryl group substituted by a group represented by the general formula (2). In the general formula (2), R1 to R8 represent a hydrogen atom or a substituent; Z represents O, S, O?C or Ar4—N; and Ar4 represents an aryl group.Type: ApplicationFiled: May 10, 2013Publication date: February 12, 2015Inventors: Katsuyuki Shizu, Hiroyuki Tanaka, Hajime Nakanotani, Chihaya Adachi
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Publication number: 20150011752Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.Type: ApplicationFiled: September 4, 2014Publication date: January 8, 2015Inventors: Aranapakam Mudumbai VENKATESAN, Zecheng CHEN, Christoph Martin DEHNHARDT, Osvaldo DOS SANTOS, Efren Guillermo DELOS SANTOS, Arie ZASK, Jeroen Cunera VERHEIJEN, Joshua Aaron KAPLAN, David James RICHARD, Semiramis AYRAL-KALOUSTIAN, Tarek Suhayl MANSOUR, Ariamala GOPALSAMY, Kevin Joseph CURRAN, Mengxiao SHI
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Publication number: 20140326164Abstract: A method for preparing a surface modified organic pigment includes the steps of a) reacting the organic pigment in an aromatic hydrocarbon solvent with a surface modifying reagent to form a surface modified organic pigment; and b) washing and drying the surface modified organic pigment; wherein the surface modifying reagent is represented by Formula (I): wherein, X is selected from the group consisting of O, S and N—R3; Y is selected from the group consisting of —O and NR4; R1 to R4 are each independently selected from the group consisting of hydrogen, an alkyl group, an alkenyl group, an alkynyl group, a -aralkyl group, an alkaryl group, and an aryl group and s heteroaryl group; with the proviso that when Y—R1 is different from OH that at least one of R2 to R4 is substituted by at least one functional group having a pKa between 2.5 and 9.Type: ApplicationFiled: November 21, 2012Publication date: November 6, 2014Applicant: AGFA GRAPHICS NVInventors: Johan Loccufier, Nicolas Vriamont, Paul Callant
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Publication number: 20140231715Abstract: The present invention relates to a compound of the formula (I), to the use of this compound in an electronic device, and to an electronic device comprising one or more compounds of the formula (I). The invention furthermore relates to the preparation of the compound of the formula (I) and to a formulation comprising one or more compounds of the formula (I).Type: ApplicationFiled: March 23, 2012Publication date: August 21, 2014Applicant: Merck Patent GmbH Patents & Scientific InformationInventors: Philipp Stoessel, Arne Buesing, Frank Voges, Christof Pflumm, Amir Hossain Parham, Thomas Eberle, Teresa Mujica-Fernaud
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Patent number: 8796256Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: May 24, 2011Date of Patent: August 5, 2014Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20130338142Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided.Type: ApplicationFiled: June 14, 2013Publication date: December 19, 2013Inventors: Peter A. BLOMGREN, Kevin S. CURRIE, Randall HALCOMB, Jeffrey E. KROPF, Seung H. LEE, Jiayao LI, Jennifer R. LO, Scott A. MITCHELL, Aaron SCHMITT, Qiaoyin WU, Jin-Min XIONG, Jianjun XU, Zhongdong ZHAO, Jayaraman CHANDRASEKHAR, Eric LANSDON
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Patent number: 8263591Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors.Type: GrantFiled: August 8, 2008Date of Patent: September 11, 2012Assignee: Cortex Pharmaceuticals, Inc.Inventors: Rudolf Mueller, Leslie Street
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Publication number: 20120171199Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.Type: ApplicationFiled: December 15, 2011Publication date: July 5, 2012Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQing Wei
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Publication number: 20120134959Abstract: The invention relates to pyrimidine compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.Type: ApplicationFiled: April 15, 2010Publication date: May 31, 2012Applicant: Wyeth LLCInventors: Kevin Joseph Curran, Joshua Aaron Kaplan, David James Richard, Jeroen Cunera Verheijen, Arie Zask
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Publication number: 20120122804Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.Type: ApplicationFiled: March 30, 2007Publication date: May 17, 2012Applicant: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terrance Moran
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Patent number: 8119632Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors.Type: GrantFiled: January 29, 2010Date of Patent: February 21, 2012Assignee: Cortex Pharmaceuticals, Inc.Inventors: Rudolf Mueller, Leslie J. Street
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Publication number: 20120018687Abstract: The surface of a base pigment is modified so as to have a specific functional group such as sulfonic acid or its derivative, in order to increase rheological and colouristic properties and flocculation stability of dioxazine pigments (e.g., Pigment Violet 23). By modifying a pigment surface and further kneading it, dispersibility and the efficiency (brightness) of a color filter are improved without any other adverse effects.Type: ApplicationFiled: March 26, 2010Publication date: January 26, 2012Applicant: SOLVAY SAInventors: Kisuck Jung, Sangmin Han, Dongyoon Kim, Hyunsuk Jeong, Hyunsu Lee
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Publication number: 20110294780Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20110257168Abstract: The present invention relates to compounds of formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).Type: ApplicationFiled: July 1, 2009Publication date: October 20, 2011Applicant: Targacept, Inc.Inventors: Srinivasa R. Akireddy, Scott R. Breining, Nikolai Fedorov, David Kombo, Anatoly A. Mazurov, Lan Miao, Srinivasa V. Murthy, Todd Showalter, Yunde Xiao, Daniel Yohannes
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Patent number: 7947802Abstract: Benzoxazine monomers comprising at least one pendant group are described. (Co)Polymers comprising at least one benzoxazine monomer having at least one pendant group are also described. In a preferred embodiment, the pendant group is located in a side chain of the benzoxazine monomer or polymer. Methods for preparing the benzoxazine monomers and polymers are described. Compositions comprising the benzoxazine monomers and polymers have numerous uses including optical materials, and in electronic materials as electrically insulating materials, and as fireproof materials.Type: GrantFiled: September 6, 2007Date of Patent: May 24, 2011Assignee: Case Western Reserve UniversityInventors: Hatsuo Ishida, Pedro Velez-Herrera
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Publication number: 20110098466Abstract: The invention relates to a process for the preparation of compounds of the general formula (I) where X are halogen atoms, the rings labeled A are linearly or angularly fused in position 1,2; 2,3 or 3,4, and in position 8,9; 9,10 or 10,11, to a 5- or 6-membered heterocyclic ring containing in the ring one nitrogen atom and one oxygen atom, or containing in the ring two nitrogen atoms, comprising an oxidation of a 3,6-bisarylamino-2,5-dihalobenzoquinone of the formula (II) in an aprotic-polar organic solvent in the presence of an organic sulfonic acid.Type: ApplicationFiled: June 12, 2006Publication date: April 28, 2011Applicant: CLARIANT FINANCE (BVI) LIMITEDInventors: Peter Kempter, Wilhelm Streck
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Publication number: 20110065687Abstract: This application relates to certain novel polycyclic compounds that interact with quadruplex-forming regions of polynucleotides and thereby inhibit translation of genetic information into polypeptides. These compounds can thus provide anticancer and antibacterial and antiviral effects. The invention includes novel compounds and pharmaceutical compositions, and methods of using them to treat cancer and other conditions.Type: ApplicationFiled: April 17, 2008Publication date: March 17, 2011Inventors: Michael Schwaebe, Johnny Yasuo Nagasawa, Mustapha Haddach
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Publication number: 20100222335Abstract: There is provided a process for the preparation of a sulfonic acid salt of formula I, or a solvate thereof, which process comprises hydrogenating a sulfonic acid salt of formula II, or a solvate thereof; in the presence of a solvent system consisting essentially of water, a C3-5 secondary alkyl alcohol and no more than 15% v/v of another organic solvent, wherein the sulfonic acid salt of formula I is optionally, without isolation, converted to a compound of formula IX, or a pharmaceutically-acceptable derivative thereof, wherein R1, R2, R3, R6, R7, R8, A, B and D have meanings given in the description.Type: ApplicationFiled: June 12, 2006Publication date: September 2, 2010Applicant: ASTRAZENECA ABInventors: David Cladingboel, Gareth Ensor
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Publication number: 20100173902Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors.Type: ApplicationFiled: January 29, 2010Publication date: July 8, 2010Applicant: CORTEX PHARMACEUTICAL, INC.Inventors: Rudolf Mueller, Leslie J. Street
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Publication number: 20100160626Abstract: There is provided processes for the preparation of various compounds, including compounds of formulae I, IV and VII, or salts and/or solvates thereof, which compounds are useful intermediates in the synthesis of certain oxabispidines having antiarrhythmic activity, such as compounds of formula XI wherein R1?, R15?, R16?, R18? and D have meanings given in the description.Type: ApplicationFiled: June 12, 2006Publication date: June 24, 2010Applicant: ASTRAZENECA ABInventors: Emma Anderson, David Cladingboel, Gareth Ensor, David Holmes, Mark Purdie
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Publication number: 20100113773Abstract: The present invention relates to a compound represented by formula (I): wherein R1 represents a C1-3 alkyl group, R2 represents a hydrogen atom or a C1-3 alkyl group, Ar represents a phenyl group or the like which may be substituted with 1 to 3 substituents, X represents an oxygen atom or the like, n and m are the same or different and integers of 0 to 2, or a pharmacologically acceptable salt, and use thereof as a medicament.Type: ApplicationFiled: February 27, 2008Publication date: May 6, 2010Inventors: Teiji Kimura, Koki Kawano, Eriko Doi, Noritaka Kitazawa, Mamoru Takaishi, Koichi Ito, Toshihiko Kaneko, Takeo Sasaki, Nobuaki Sato, Takehiko Miyagawa, Hiroaki Hagiwara
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Patent number: 7691197Abstract: The present invention relates to a method of preparing a yellow pigment comprising an asymmetric quinolonoquinolone in an amount greater than 50% by weight of the yellow pigment. Also disclosed are modified yellow pigments comprising this yellow pigment having attached at least one organic group as well as inkjet ink compositions comprising the yellow pigments or the modified yellow pigments.Type: GrantFiled: October 20, 2006Date of Patent: April 6, 2010Assignee: Cabot CorporationInventor: Alexander I. Shakhnovich
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Patent number: 7648985Abstract: There is provided compounds of formula (I), wherein R1, R2, R3, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: GrantFiled: June 13, 2005Date of Patent: January 19, 2010Assignee: AstraZeneca ABInventors: Annika Bjore, Ulrik Gran, Peter Bonn, Johan Kajanus, Christina Olsson, Fritiof Ponten
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Publication number: 20090326221Abstract: There is provided compounds of formula I, wherein R1, R2, R3, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: ApplicationFiled: September 1, 2009Publication date: December 31, 2009Applicant: AstraZeneca AB,Inventors: Annika Bjore, Magnus Bjorsne, David Cladingboel, Kurt-Jurgen Hoffman, John Pavey, Fritiof Ponten, Gert Strandlund, Peder Svensson, Colin Thomson, Michael Wilsterman
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Publication number: 20090270383Abstract: There is provided compounds of formula (I), wherein R1, R2, R3, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: ApplicationFiled: July 6, 2009Publication date: October 29, 2009Applicant: AstraZeneca ABInventors: Annika Bjore, Peter Bonn, Ulrik Gran, Johan Kajanus, Christina Olsson, Fritiof Ponten
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Publication number: 20090240051Abstract: There is provided a process for the preparation of a compound of formula I, or a pharmaceutically acceptable derivative thereof, wherein A, B, G, R1, R2, R3, R4 and R41 to R46 have meanings given in the description, which process comprises the dehydrative cyclisation of a compound of formula II,Type: ApplicationFiled: March 6, 2009Publication date: September 24, 2009Applicant: AstraZeneca ABInventor: John Pavey
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Publication number: 20090062532Abstract: An acid addition salt of a compound of Formula I, wherein R2 represents C1-6 alkyl (optionally substituted and/or terminated by one or more substituents selected from —OH, halo, cyano, nitro and aryl) or aryl, wherein each aryl and aryloxy group, unless otherwise specified, is optionally substituted.Type: ApplicationFiled: November 19, 2007Publication date: March 5, 2009Applicant: ASTRAZENECA ABInventor: David Cladingboel
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Publication number: 20090054422Abstract: There is provided compounds of formula I, wherein R1, R2, R3, R41 to R46, X, Y and Z have meanings given in the description, which compounds are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: ApplicationFiled: June 12, 2006Publication date: February 26, 2009Applicant: ASTRAZENECA ABInventors: Annika Bjore, David Cladingboel, Gareth Ensor, Adam Herring, Johan Kajanus, Robert Lundqvist, Christina Olsson, Carl-Gustav Sigfridsson, Gert Strandlund
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Publication number: 20090005558Abstract: There is provided compounds of formula (I), wherein R1, R2, R3, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: ApplicationFiled: June 13, 2005Publication date: January 1, 2009Applicant: ASTRAZENECA ABInventors: Annika Bjore, Peter Bonn, Ulrik Gran, Johan Kajanus, Christina Olsson, Fritiof Ponten
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Publication number: 20080249086Abstract: There is provided compounds of formula I, wherein R1, R2, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: ApplicationFiled: February 11, 2008Publication date: October 9, 2008Applicant: ASTRAZENECA ABInventors: Annika Bjore, Ulrik Gran, Gert Strandlund
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Publication number: 20080207900Abstract: The present invention relates to a compound represented by formula (I): wherein R1 represents a C1-3 alkyl group, R2 represents a hydrogen atom or a C1-3 alkyl group, Ar represents a phenyl group or the like which may be substituted with 1 to 3 substituents, X represents an oxygen atom or the like, n and m are the same or different and integers of 0 to 2, or a pharmacologically acceptable salt, and use thereof as a medicament.Type: ApplicationFiled: February 26, 2008Publication date: August 28, 2008Inventors: Teiji KIMURA, Koki Kawano, Eriko Doi, Noritaka Kitazawa, Mamoru Takaishi, Koichi Ito, Toshihiko Kaneko, Takeo Sasaki, Nobuaki Sato, Takehiko Miyagawa, Hiroaki Hagiwara
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Publication number: 20080207899Abstract: There is provided compounds of formula I, wherein R1, R2, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: ApplicationFiled: February 12, 2008Publication date: August 28, 2008Applicant: ASTRAZENECA ABInventors: Annika Bjore, Ulrik Gran, Gert Strandlund
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Publication number: 20080200673Abstract: There is provided a process for the isolation of a sulfonic acid salt of formula I, or a solvate thereof, from a mixture comprising: (i) the corresponding free base; and (ii) a compound of formula III. or a salt and/or solvate thereof, which process comprises providing an aqueous dispersion of the compounds of formulae II and III and a source of R3SO3? anions and then, if necessary, adjusting the pH of the aqueous dispersion to any value from 3 to 8. There are further provided processes wherein the mixture of compounds of formulae II and III is provided by incomplete reaction, for example in the presence of base and an aqueous phase, between a compound of formula III and a compound of formula IV In such processes, the RSO3? anions of the resulting salt of formula I may be derived from the compound of formula IV. Also for all of these processes, D, R1, R2 and R3 have meanings given in the description.Type: ApplicationFiled: June 12, 2006Publication date: August 21, 2008Applicant: AstraZeneca ABInventors: Lal Cheema, David Cladingboel
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Patent number: 7375104Abstract: A compound of formula 1? wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1? are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1? together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2?, R2?, and R?? are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, orType: GrantFiled: November 15, 2006Date of Patent: May 20, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Thierry Bouyssou, Ingo Konetzki, Philipp Lustenberger, Juergen Mack, Andreas Schnapp, Dieter Wiedenmayer, Christoph Hoenke, Klaus Rudolf
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Patent number: 7351821Abstract: There is provided compounds of formula I, wherein R1, R2, R3, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: GrantFiled: December 18, 2006Date of Patent: April 1, 2008Assignee: AstraZeneca ABInventors: Annika Björe, Magnus Björsne, David Cladingboel, Kurt-Jürgen Hoffmann, John Pavey, Fritiof Pontén, Gert Strandlund, Peder Svensson, Colin Thomson, Michael Wilsterman
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Patent number: 7314931Abstract: Compounds of Formula I, wherein R2 represents C1-6 alkyl (optionally substituted by one or more substituents selected from —OH, halo, cyano, nitro and aryl) or aryl, wherein each aryl and aryloxy group, unless otherwise specified, is optionally substituted, and methods of preparation thereof are disclosedType: GrantFiled: October 13, 2003Date of Patent: January 1, 2008Assignee: AstraZeneca ABInventor: David Cladingboel
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Patent number: 7217708Abstract: There is provided substantially crystalline forms of 4-({3-[7-(3,3-dimethyl-2-oxobutyl) -9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]propyl}amino)benzo-nitrile; tert-butyl 2 -{7-[3-(4-cyanoanilino)propyl]-9-oxa-3,7-diazabicyclo-[3.3.1]non-3-yl}ethylcarbamate; tert-butyl 2-{7-[4-(4-cyanophenyl)butyl]-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl}ethylcarbamate; or tert-butyl 2-{7-[2S)-3-(4-cyanophenoxy)-2-hydroxypropyl]-9-oxa-3,7-diazabicyclo-[3.3.1]non-3-yl}ethylcarbamate and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of cardiac arhythmias.Type: GrantFiled: April 12, 2002Date of Patent: May 15, 2007Assignee: Astrazeneca ABInventors: Neil Barnwell, Annika Björe, Lal Cheema, David Cladingboel, Adam Herring, Karin Lövqvist
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Patent number: 7169921Abstract: There is provided a process for the preparation of a compound of formula (I): which process comprises reaction of a compound of formula (II): with either a compound of formula (III): or acrylamide, followed, in the latter case, by reaction of the resulting intermediate of formula (IV): with an alcohol of formula R2—OH and an agent that promotes, or agents that in combination promote, rearrangement and oxidation of the compound of formula IV to an intermediate isocyanate, which may then react with the alcohol of formula R2—OH, and wherein R1, R2 and R16 have meanings given in the descriptionType: GrantFiled: April 12, 2002Date of Patent: January 30, 2007Assignee: Astrazeneca ABInventors: Lal Cheema, David Cladingboel, Rhona Sinclair
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Patent number: 6949539Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2001Date of Patent: September 27, 2005Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber
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Patent number: 6762299Abstract: A mixed crystal of two or more different benzimidazolonedioxazine compounds of the formula (1) where X and X′ are identical or different and are hydrogen or halogen, R1, R1′, R2 and R2′ are identical or different and are hydrogen, C1-C18 alkyl, trifluoromethyl, C1-C18 alkylcarbonyl, C5-C6 cycloalkyl or phenyl which may be unsubstituted or substituted by one or more halogen atoms, nitro groups, trifluoromethyl, C1-C18 alkyl, C1-C18 alkoxy, C1-C18 alkylcarbonyl and/or C1-C18 alkoxycarbonyl groups. The mixed crystals are of low solubility and feature good fastness properties and red to blue colorations. The mixed crystals are suitable for pigmenting paints, plastics, printing inks, aqueous or solvent-based pigment preparations, electrophotographic toners and developers, powder coating materials, inks, preferably inkjet inks, color filters, and for coloring seed and cosmetics.Type: GrantFiled: October 24, 2001Date of Patent: July 13, 2004Assignee: Clariant GmbHInventors: Martin U. Schmidt, Peter Kempter, Carsten Plueg, Roland Born
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Publication number: 20040133000Abstract: There is provided a process for the preparation of a benzenesulfonic acid salt of a compound of formula (1) which process comprises reaction of a compound of formula (II) with a compound of formula (III) wherein R1, R2, A and B have meanings given in the description.Type: ApplicationFiled: October 10, 2003Publication date: July 8, 2004Inventors: Lal Cheema, David Cladingboel
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Patent number: 6620931Abstract: Process for phase conversion of a methyl-substituted, benzimidazolone-fused dioxazine pigment of composition C22H12Cl2N6O4 having the formula (1) or of an isomer or tautomer thereof, which comprises treating the pigment of formula (1) with certain organic solvents. In the course of this phase conversion, 4 novel crystal polymorphs are formed which are called phases II, IV, V and VI and are characterized by means of their X-ray powder diagrams. The novel polymorphs are of low solubility and feature good fastness properties and violet colorations. The novel crystal polymorphs are suitable for pigmenting coating materials, plastics, printing inks, aqueous or solvent-based pigment preparations, electrophotographic toners and developers, powder coating materials, inks, preferably inkjet inks, and color filters, and for coloring seed.Type: GrantFiled: October 22, 2001Date of Patent: September 16, 2003Assignee: Clariant GmbHInventors: Martin U. Schmidt, Peter Kempter, Roland Born
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Patent number: 6617453Abstract: The triphendioxazine compounds of the general formula (I) in which the rings labeled A in positions 1,2-, 2,3- or 3,4- and 8,9-, 9,10- or 10,11- carry a linearly or angularly fused heterocyclic ring containing at least one nitrogen atom which is substituted or unsubstituted, with the proviso that compounds with only unsubstituted nitrogen atoms and symmetrically disubstituted compounds with C1-2alkyl and unsubstituted phenyl substituents are excluded, are outstanding pigments and are notable over the closest comparable pigments in particular for better migration, light and solvent fastnesses, better heat stability and enhanced colouring power and also better dispersibility and capability to be brought into pigment form. The invention also relates to a process for preparing these triphendioxazine compounds which is characterized by a cyclization step conducted in the presence of manganese dioxide and concentrated sulphuric acid.Type: GrantFiled: November 22, 2000Date of Patent: September 9, 2003Assignee: Clariant Finance (BVI) LimitedInventors: Bansi Lal Kaul, Patrick Boeglin, Peter Kempter