Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Imides, Etc.) Patents (Class 548/513)
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Patent number: 10981898Abstract: The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.Type: GrantFiled: August 8, 2019Date of Patent: April 20, 2021Assignees: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Gianni Chessari, Steven Howard, Ildiko Maria Buck, Benjamin David Cons, Christopher Norbert Johnson, Rhian Sara Holvey, David Charles Rees, Jeffrey David St. Denis, Emiliano Tamanini, Bernard Thomas Golding, Ian Robert Hardcastle, Celine Florence Cano, Duncan Charles Miller, Martin Edward Mäntylä Noble, Roger John Griffin, James Daniel Osborne, Joanne Peach, Arwel Lewis, Kim Louise Hirst, Benjamin Paul Whittaker, David Wyn Watson, Dale Robert Mitchell
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Patent number: 10544132Abstract: The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.Type: GrantFiled: September 29, 2016Date of Patent: January 28, 2020Assignees: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Gianni Chessari, Steven Howard, Ildiko Maria Buck, Benjamin David Cons, Christopher Norbert Johnson, Rhian Sara Holvey, David Charles Rees, Jeffrey David St. Denis, Emiliano Tamanini, Bernard Thomas Golding, Ian Robert Hardcastle, Celine Florence Cano, Duncan Charles Miller, Martin Edward Mäntylä Noble, Roger John Griffin, James Daniel Osborne, Joanne Peach, Arwel Lewis, Kim Louise Hirst, Benjamin Paul Whittaker, David Wyn Watson, Dale Robert Mitchell
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Patent number: 10457778Abstract: A method of manufacture of a polyetherimide composition includes contacting a substituted phthalic anhydride and an organic diamine in the presence of diphenyl sulfone, sulfolane, or a combination comprising at least one of the foregoing solvents at a temperature of greater than 130° C. to provide a bis(phthalimide) composition comprising diphenyl sulfone, sulfolane, or a combination comprising at least one of the foregoing solvents and a bis(phthalimide); and polymerizing the bis(phthalimide) and an alkali metal salt of a dihydroxy aromatic compound in the presence of diphenyl sulfone, sulfolane, or a combination comprising at least one of the foregoing to form a polyetherimide. The method does not require any catalyst either for the imidization or the polymerization.Type: GrantFiled: May 15, 2018Date of Patent: October 29, 2019Assignee: SABIC GLOBAL TECHNOLOGIES B.V.Inventors: Mani Raj Chaulagain, Thomas Link Guggenheim, Roy Ray Odle
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Patent number: 8993584Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as procymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.Type: GrantFiled: July 21, 2011Date of Patent: March 31, 2015Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Koji Sugimoto, Hiroyuki Hayashi
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Publication number: 20140288106Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.Type: ApplicationFiled: June 3, 2014Publication date: September 25, 2014Applicant: SanofiInventors: Imre BATA, Peter BUZDER-LANTOS, Attila VASAS, Veronika BARTANE BODOR, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Sandor BATORI, Martin SMRCINA, Marcel PATEK, Aleksandra WEICHSEL, David Squire Thorpe
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Publication number: 20140275048Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Alkermes Pharma Ireland LimitedInventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
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Publication number: 20140235533Abstract: The present invention provides compounds of formula I wherein Q is Q1 or Q2; A1, A2, A3 and A4 are independently of each other C—H, C—R7, or nitrogen; R1 is C1-C8haloalkyl; R2 is aryl or aryl substituted by one to five R11, or heteroaryl or heteroaryl substituted by one to five R11; and R3, R4, R5, R6 and R7 are as defined in the claims. The invention also provides methods of controlling insects, acarines, nematodes or molluscs which methods comprise applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I).Type: ApplicationFiled: August 10, 2012Publication date: August 21, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Tomas Smejkai, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere
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Publication number: 20140142322Abstract: The present application provides methods and catalysts for activation of carboxylic acids for organic reactions.Type: ApplicationFiled: February 14, 2012Publication date: May 22, 2014Inventors: Dennis Hall, Nicolas Gernigon, Raed Al-Zoubi, Paul D. Thornton
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Patent number: 8629084Abstract: The invention relates to novel iodophenyl-substituted cyclic ketenols of the formula (I) in which CKE, J, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly iodophenyl-substituted cyclic ketonols of the formula (I) and secondly at least one crop plant compatibility-improving compound.Type: GrantFiled: September 13, 2005Date of Patent: January 14, 2014Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Kerstin Ilg, Stefan Lehr, Dieter Feucht, Olga Malsam, Udo Reckmann, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Waltraud Hempel, Erich Sanwald
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Patent number: 8592587Abstract: The disclosure relates to a method for the synthesis of a compound of the following formula (I) in which: R1 and R2 are independently an N-protective group; R3 is a hydrogen atom, a C1-C6 alkyl group, a C1-C6 arylalkyl group, a C2-C6 alkenyl group, or a alkoxycarbonylalkyl group; Y is a —C(HR4)- group in which R4 is a hydrogen atom, a C1-C6 alkyl group, an aryl group, a C1-C6 arylalkyl group, or a C2-C6 alkenyl group; or an orthophenylene group.Type: GrantFiled: March 21, 2008Date of Patent: November 26, 2013Assignees: Centre National de la Recherche Scientifique (CNRS), Universite de Montpellier IInventors: Jean Martinez, Georges Dewynter, Daniel Farran
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Publication number: 20130123287Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.Type: ApplicationFiled: July 21, 2011Publication date: May 16, 2013Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Koji Sugimoto, Hiroyuki Hayashi
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Patent number: 8334300Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: March 24, 2011Date of Patent: December 18, 2012Assignee: Bayer AktiengesellshaftInventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christophe Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Publication number: 20120094232Abstract: There is provided a simple production method of a polyhydroxyimide. A production method of a polyhydroxyimide, characterized by comprising adding to a polyhydroxyimide precursor containing a repeating structure of Formula (1): in which X is a tetravalent aliphatic group or aromatic group, Y is an organic group containing an aromatic group substituted with at least one OH group, and n is an integer of 1 or more, at least a compound of Formula (2) or Formula (3): in which R1 to R4 or R5 to R8 are independently a hydrogen atom or a monovalent organic group, and m is a natural number, and heating the resultant reaction mixture at a temperature of 50° C. or more to obtain a polyimide having a weight average molecular weight measured by gel permeation chromatography (GPC) in terms of polystyrene of 5,000 to 100,000.Type: ApplicationFiled: April 22, 2010Publication date: April 19, 2012Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventor: Kazuya Ebara
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Publication number: 20120015807Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.Type: ApplicationFiled: October 13, 2007Publication date: January 19, 2012Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
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Publication number: 20110224274Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.Type: ApplicationFiled: June 25, 2009Publication date: September 15, 2011Inventors: Bernard Thomas Golding, Christiane Riedinger, Roger John Griffin, Ian Robert Hardcasctle, Eric Valeur, Anna Frances Watson, Martin Noble
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Patent number: 7947704Abstract: The invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I), in which CKE, W, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly the 2,4,6-phenyl-substituted cyclic ketoenols and secondly at least one compound which improves crop plant tolerance.Type: GrantFiled: March 11, 2005Date of Patent: May 24, 2011Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Oliver Gaertzen, Klaus Kunz, Stefan Lehr, Dieter Feucht, Peter Lösel, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Rosinger
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Publication number: 20110117015Abstract: The invention relates to aryl-sulphonamido compounds endowed with affinity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, G and n have the meanings reported in the specification, properly labelled with diagnostic imaging moieties or even radiotherapeutic moieties. The invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as diagnostic imaging agents or radiotherapeutic agents.Type: ApplicationFiled: July 21, 2009Publication date: May 19, 2011Applicant: BRACCO IMAGING S.P.A.Inventors: Armando Rossello, Elisa Nuti, Stanislava Ivanova Avramova, Fulvio Uggeri, Alessandro Maiocchi
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Patent number: 7915282Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: March 21, 2001Date of Patent: March 29, 2011Assignee: Bayer AktiengesellschaftInventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Publication number: 20100256393Abstract: The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (1R, 2S, 5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid (“D-DTTA”) salt or a (1S, 2R, 5R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt (“L-DTTA”) in a high enantiomeric excess. This invention also provides for a process for preparing a (1R, 2S, 5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (“D-DBTA”) salt or a (1S, 2R, 5R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (“L-DBTA”) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.Type: ApplicationFiled: April 9, 2010Publication date: October 7, 2010Applicant: Schering CorporationInventors: George Wu, Frank X. Chen, Paitoon Rashatasakhon, Jeffrey M. Eckert, George S.K. Wong, Hong-Chang Lee, Nolan C. Erickson, Jennifer Ann Vance, Peter C. Nirchio, Juergen Weber, David Jieh-Shyh Tsai, Nanfei Zou
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Publication number: 20100099874Abstract: The disclosure relates to a method for the synthesis of a compound of the following formula (I) in which: R1 and R2 are independently an N-protective group; R3 is a hydrogen atom, a C1-C6 alkyl group, a C1-C6 arylalkyl group, a C2-C6 alkenyl group, or a alkoxycarbonylalkyl group; Y is a —C(HR4)- group in which R4 is a hydrogen atom, a C1-C6 alkyl group, an aryl group, a C1-C6 arylalkyl group, or a C2-C6 alkenyl group; or an orthophenylene group.Type: ApplicationFiled: March 21, 2008Publication date: April 22, 2010Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRSInventors: Jean Martinez, Georges Dewynter, Daniel Farran
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Publication number: 20100009850Abstract: The invention relates to novel iodophenyl-substituted cyclic ketenols of the formula (I) in which CKE, J, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly iodophenyl-substituted cyclic ketonols of the formula (I) and secondly at least one crop plant compatibility-improving compound.Type: ApplicationFiled: September 13, 2005Publication date: January 14, 2010Inventors: Reiner Fischer, Thomas Bretschneider, Kerstin Ilg, Stefan Lehr, Dieter Feucht, Olga Malsam, Udo Rechkmann, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Waltraud Hempel, Erich Sanwald
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Publication number: 20090240063Abstract: The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid (“D-DTTA”) salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt (“L-DTTA”) in a high enantiomeric excess. This invention also provides for a process for preparing a (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (“D-DBTA”) salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (“L-DBTA”) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.Type: ApplicationFiled: December 20, 2006Publication date: September 24, 2009Inventors: George Wu, Frank X. Chen, Paitoon Rashatasakhon, Jeffrey M. Eckert, George S.K. Wong, Hong-Chang Lee, Nolan C. Erickson, Jennifer Ann Vance, Peter C. Nirchio, Juergen Weber, David Jieh-Shyh Tsai, Nanfei Zou
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Patent number: 7459585Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: March 24, 2005Date of Patent: December 2, 2008Assignee: Ajinomoto Co., Inc.Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
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Publication number: 20080176917Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is C1-4alkyl; R3 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; p is 0, 1, 2, 3 or 4; and R4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy and C1-4alkanoyl; n is 0 or 1; wherein when R4 is chlorine and p is 1, such R4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R3 comprises at least one SF5 group as a substituent; processes for their preparation, intermediates used in these processes, pharmaceutical compositions contaiType: ApplicationFiled: April 12, 2006Publication date: July 24, 2008Inventors: Daniele Andreotti, Anna Checchia, Dieter Hamprecht, Fabrizio Micheli
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Patent number: 7388027Abstract: The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R2? R5, G, n and W are defined herein.Type: GrantFiled: March 2, 2005Date of Patent: June 17, 2008Assignee: Bristol-Myers Squibb CompanyInventors: James J. Li, Lawrence Hamann, David Augeri, Yingzhi Bi
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Publication number: 20080119660Abstract: The present invention provides a method for preparing relatively insoluble bisimides under conditions which afford high imidization reaction rates and which permit the monitoring and adjustment of reactant stoichiometry at any stage of the reaction. The bisimides provided by the present invention are prepared either by reaction of a diamine such as 4,4?-diaminodiphenylsulfone (DDS) with an anhydride, for example 3-chlorophthalic anhydride (3-ClPA) in the presence of a solvent at a pressure greater than one atmosphere and at a temperature above the normal boiling point of the solvent, or by reaction of a monoamine with a dianhydride under the same conditions. In one embodiment, the relatively insoluble product bisimides provided by the present invention have a solubility in ortho-dichlorobenzene of less than about 10 percent by weight at a temperature of about 180° C.Type: ApplicationFiled: November 16, 2006Publication date: May 22, 2008Applicant: General Electric CompanyInventors: Farid Fouad Khouri, Albert Santo Stella
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6703379Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: March 12, 2001Date of Patent: March 9, 2004Assignee: Ajinomoto Co., Inc.Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
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Patent number: 6417178Abstract: Amyloid binding compounds which are derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing Chrysamine G and derivatives thereof and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: November 6, 1997Date of Patent: July 9, 2002Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
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Patent number: 6395907Abstract: The present invention is directed to new polycyclicaromatic-ethynyl terminated materials that possesses excellent mechanical and chemical properties for high-performance composite application that can be cured at lower temperatures than phenyl-ethynyl terminated imide materials.Type: GrantFiled: November 17, 2000Date of Patent: May 28, 2002Assignee: Virginia Commonwealth UniversityInventors: Michel E. Wright, Derek Schorzman
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Patent number: 6255479Abstract: A method for preparing an &agr;-oxolactam comprising, reacting a corresponding &agr;-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding &agr;-oxolactam.Type: GrantFiled: December 29, 1998Date of Patent: July 3, 2001Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Akireddy Srinivasa Rao
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Patent number: 6204222Abstract: Substituted cyclohexene-1,2-dicarboxylic acid derivatives I (R1 and R2 are each H, unsubstituted or substituted C1-C6-alkyl, C3-C6-alkenyl or C3-C6-alkynyl, C3-C8-cycloalkyl, unsubstituted or substituted phenyl or heterocyclyl and, if R1 is H or C1-C6-alkyl, R2 is additionally OH, C1-C6-alkoxy, C3-C6-alkenyloxy, C3-C6-alkynyloxy, C3-C6-cycloalkoxy, C5-C7-cycloalkenyloxy, C1-C6-haloalkoxy, C3-C6-haloalkenyloxy, C3-C7-cycloalkyl-C1-C6-alkoxy, C1-C6-alkyl-carbonyloxy, C1-C6-cyanoalkoxy, hydroxy-C1-C6-alkoxy, C1-C6-alkoxy-C1-C6-alkoxy, C1-C6-alkoxycarbonyl-C1-C6-alkoxy, C1-C6-alkoxy-C1-C6-alkoxy, C1-C6-alkylamino-C1-C6-alkoxy, C1-C6-dialkylamino-C1-C6-alkoxy, unsubstituted or substituted phenyl-C1-C6-alkoxy, phenyl-C3-C6-alkenyloxy or phenyl-C3-C7-alkynyloxy or unsubstituted or substituted amino, or R1 and R2, together with the nitrogen atom to which they are bonded, form an unsubstituted or substituted 3-membered to 8-membered heterocyclic structure, R3 is H or C1-C6-alkyl, R4 is H or halogenType: GrantFiled: May 29, 1998Date of Patent: March 20, 2001Assignee: BASF AktiengesellschaftInventors: Ralf Klintz, Elisabeth Heistracher, Peter Schaefer, Gerhard Hamprecht, Peter Plath, Uwe Kardorff, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 6168776Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: April 18, 1997Date of Patent: January 2, 2001Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
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Patent number: 6130241Abstract: The invention provides an insect- or acarid-repellent formulation comprising a compound of formula (I), wherein R represents straight or branched chain C.sub.2-10 alkyl, straight or branched chain C.sub.2-10 alkenyl, or straight or branched chain C.sub.2-10 alkynyl, which groups are optionally substituted by one or more groups selected from halogen, C.sub.4-8 cycloalkyl and C.sub.4-8 cycloalkenyl; and a suitable adjuvant, diluent or carrier.Type: GrantFiled: March 10, 1999Date of Patent: October 10, 2000Assignee: Pfizer Inc.Inventor: Darren John Schulz
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Patent number: 6013606Abstract: Substituted cinnamic oxime derivatives I and cinnamic hydroxamide derivatives II ##STR1## (R.sup.1= halogen, NO.sub.2, CN, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3= H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, hydroxy-C.sub.1 -C.sub.6 -alkyl;R.sup.4= H, halogen, CN, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl orR.sup.3 +R.sup.4 =chemical bond;Y=--O--, --S--, --O--CO--, --O--SO.sub.2 -- or chemical bond;Y'=--O-- or --S--;R.sup.5= unsubst. or subst. C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -haloalkyl; C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, unsubst. or subst. phenyl or phenyl-C.sub.1 -C.sub.6 -alkyl, or, if Y is --O--, --S-- or a chemical bond, is (C.sub.1 -C.sub.6 -alkyl)carbonyl or (C.sub.1 -C.sub.6 -alkoxy)carbonyl; or, if Y is a chemical bond, is hydrogen or halogen;R.sup.5 '=R.sup.5, H or (C.sub.1 -C.sub.6 -haloalkyl)carbonyl;R.sup.6= H, C.sub.1 -C.Type: GrantFiled: June 30, 1997Date of Patent: January 11, 2000Assignee: BASF AkteingesellschaftInventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Christoph-Sweder von dem Bussche-Hunnefeld, Peter Munster, Reinhard Kirstgen, Albrecht Harreus, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5994143Abstract: Fluorescent conjugates suitable for use in flow cytometry and other biological applications. The fluorescent conjugates comprise an antibody having a polymeric dye bound thereto. The polymeric dye is preferably enhanced by a hydrophobic and conformationally restrictive moiety either bound thereto or in close association therewith. The hydrophobic and conformationally restrictive moiety is preferably derived from a cyclodextrin. The polymeric dye comprises a polymeric entity having signal-generating groups, such as aminostyryl pyridinium dye residues attached thereto. The fluorescent conjugates exhibit exceptional stability characteristics and avoid many of the problems of energy transfer, bio-conjugability, and solubility.Type: GrantFiled: February 1, 1996Date of Patent: November 30, 1999Assignee: Abbott LaboratoriesInventors: Christopher Bieniarz, Jeffrey B. Huff, Michael J. Cornwell, Seshagiri R. Tata Venkata
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Patent number: 5962695Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.Type: GrantFiled: August 7, 1998Date of Patent: October 5, 1999Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
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Patent number: 5942535Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 24, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5916847Abstract: Arylheterocycles having the general formula (I): ##STR1## and process for preparing them. The arylheterocycles having the general formula (I) display high herbicidal activity.Type: GrantFiled: March 17, 1997Date of Patent: June 29, 1999Assignee: Isagro Ricerca S.r.l.Inventors: Franco Bettarini, Piero La Porta, Giovanni Meazza, Giampaolo Zanardi, Ernesto Signorini, Domenico Portoso
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Patent number: 5858925Abstract: The invention relates to new heterocyclylbenzonitriles of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Het have the meanings given in the description, new processes and new intermediate products for their preparation and their use as herbicides.Type: GrantFiled: October 21, 1996Date of Patent: January 12, 1999Assignee: Bayer AktiengesellschaftInventors: Mark-Wilhelm Drewes, Roland Andree, Kurt Findeisen, Wilhelm Haas, Andreas Lender, Karl-Heinz Linker, Otto Schallner, Markus Dollinger, Hans-Joachim Santel
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Patent number: 5847158Abstract: A process for preparing a compound of formula (I): ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or benzyl, and wherein the phenyl moiety of said benzyl group is optionally substituted with one or two substituents each independently selected from halo, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino and trifluoromethyl, which comprises treating a solution of a compound of formula (II): ##STR2## wherein R is as defined for formula (I), and a halonitromethane in a first organic solvent, with a quaternary ammonium fluoride of formula (III):R.sup.1 R.sup.2 R.sup.3 F.sup.4 N.sup.+ F.sup.- (III)wherein R.sup.1,R.sup.2,R.sup.3 and R.sup.4 are each independently selected from C.sub.1 -C.sub.8 alkyl and benzyl, optionally in solution in a second organic solvent.Type: GrantFiled: June 19, 1997Date of Patent: December 8, 1998Assignee: Pfizer Inc.Inventor: Nicholas John Lawson
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Patent number: 5821373Abstract: Solid solutions consisting of 3,6-bis(biphenyl-4-yl)- 2,5-dihydropyrrolo?3,4-c!pyrrole-1,4-dione and either a) a second 1,4-diketopyrrolopyrrole or b) a quinacridone, which are further defined herein, are outstandingly suited to pigmenting high molecular weight organic material.Type: GrantFiled: September 12, 1996Date of Patent: October 13, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, Olof Wallquist
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Patent number: 5756746Abstract: The present invention relates to a solid solution consisting of 60-90 mol-% of an asymmetric 2,5-dihydro-1,4-diketopyrrolo?3,4-c!pyrrole of the formula (I) ##STR1## in which G.sub.1 and G.sub.2 independently of one another are different substituted or unsubstituted aromatic radicals or pyridyl, but the volume of all substituents on G.sub.1 and G.sub.2 is greater than that of two methyl groups;and 40-10 mol-% of a 2,5-dihydro-1,4-diketopyrrolo?3,4-c!pyrrole of the formula (IIa) ##STR2## in which G.sub.3 and G.sub.4 independently of one another are different substituted or unsubstituted aromatic radicals or pyridyl, but the volume of all substituents on G.sub.3 and G.sub.4 is less than that of two butoxy groups;or 40-10 mol-% of a quinacridone of the formula (IIb) ##STR3## in which R.sub.9 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy;which is a single-phase solid solution having the crystal structure of the asymmetric 2,5-dihydro-1,4-diketopyrrolo?3,4-c!pyrrole of the formula (I).Type: GrantFiled: September 23, 1996Date of Patent: May 26, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, Abul Iqbal
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Patent number: 5734063Abstract: The present invention provides a method for preparation of a compound of the formula (I) useful as a fog restrainer for a silver halide light-sensitive material, especially for a heat-developing light-sensitive material and a synthetic intermediate for the fog restrainer. The method makes it possible to obtain the fog restrainer in good yield and in short steps. ##STR1## wherein, R.sup.1 is alkyl, cycloalkyl, or aryl, R.sup.2 and R.sup.3 are hydrogen atom or alkyl, R.sup.4 is hydrogen atom or acyl, and R.sup.1 and R.sup.4 may be bonded together to form 5- or 6-membered ring.Type: GrantFiled: October 24, 1996Date of Patent: March 31, 1998Assignee: Fuji Photo Film Co.,Ltd.Inventors: Katsuyoshi Yamakawa, Tadahisa Sato
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Patent number: 5731441Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.Type: GrantFiled: October 29, 1996Date of Patent: March 24, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
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Patent number: 5719104Abstract: Bicyclic imides of formulae (I) and (II) and their agriculturally-suitable salts, are disclosed which are useful for controlling undesirable vegatation, wherein G is O or S; n and m are each independently 0; 1; 2; or 3; provided that m+n is 2 or 3; q is 1 or 2; X is CH.sub.2 ; CH(halogen); CF.sub.2 ; CHOCH.sub.2 F; CHOCF.sub.3 ; CHOCH.sub.2 CF.sub.3 ; O; S(O).sub.0-2 ; NH; N(C.sub.1 -C.sub.4 alkyl); or N(C.sub.1 -C.sub.4 haloalkyl); and R.sup.1. R.sup.2, and Q are as defined in the disclosure. Also disclosed are compositions containing the bicyclic imides of formulae (I) and (II) and a method for controlling growth of undesired vegetation comprising applying to the locus to be protected an effective amount, of the bicyclic imides formulae (I) and (II).Type: GrantFiled: October 3, 1996Date of Patent: February 17, 1998Assignee: E. I. du Pont de Nemours and CompanyInventors: John J. Kilama, Karlheinz Drauz, Wonpyo Hong, Matthias Schafer
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Patent number: 5709947Abstract: A method for the preparation of a diaminobisimide compound of the formula (I) substantially free of oligomers: ##STR1## wherein Ar.sup.1 is an optionally substituted aromatic residue which provides for good conjugation between the nitrogen containing groups; andAr is an optionally substituted aromatic residue characterized in that at least two molar proportions of an aromatic diamine of the formula (II)H.sub.2 N--Ar.sup.1 --NH.sub.2 (II)wherein Ar.sup.1 is as defined above,are heated with one molar proportion of an aromatic tetracarboxylic acid of the formula (III) or the corresponding dianhydride,(HOOC).sub.2 Ar(COOH).sub.2 (III)wherein Ar is as defined above,optionally in the presence of a polar solvent and optionally including 0.1 to 2 molar proportions of a tertiary amine.The compounds of formula (I) are useful curing agents in epoxy resin formulations.Type: GrantFiled: June 2, 1995Date of Patent: January 20, 1998Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Jonathan Howard Hodgkin, Mervyn Benjamin Jackson, John West Loder
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Patent number: 5710281Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.Type: GrantFiled: February 23, 1996Date of Patent: January 20, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
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Patent number: 5693797Abstract: A process for the preparation of brominated phthalimides that involves mixing tetrabromophthalic anhydride, an organic acid, and an organic dispersing agent in water at approximately 110.degree. C. under 1 bar pressure is disclosed. An amine is added and the reaction mixture is stirred for six hours under approximately 5 bar pressure and heated at least to 120.degree. C. The reactant mass is washed in water and then methanol. The process decreases production time, increases whiteness and purity, and decreases yellowness and particle size of the resulting product.Type: GrantFiled: February 14, 1997Date of Patent: December 2, 1997Assignee: Unitex Chemical CorporationInventor: James F. Day
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Patent number: 5693663Abstract: The invention relates to substituted bicyclic 3-aryl-pyrrilidine-2,4-dione derivatives of the formula ##STR1## wherein Q and A form a substituted 4- to 6-membered ring. These compounds have utility as pesticides.Type: GrantFiled: August 20, 1996Date of Patent: December 2, 1997Assignee: Bayer AktiengesellschaftInventors: Hans Joachim Santel, Robert R. Schmidt, Ulrike Wachendorff-Neumann, Christoph Erdelen, Thomas Bretschneider, Reiner Fischer, Hermann Hagemann, Bernd-Wieland Kruger, Klaus Lurssen