Chalcogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 548/213)
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Publication number: 20090005353Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 9, 2006Publication date: January 1, 2009Applicant: AstraZeneca ABInventors: Anders Broo, Robert Judkins, Lanna Li, Eva-Lotte Lindstedt-Alstermark, Pernilla Sandberg, Marianne Swanson, Lars Weidolf, Kay Brickmann, Patrik Holm
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Publication number: 20080300249Abstract: The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.Type: ApplicationFiled: July 29, 2008Publication date: December 4, 2008Applicants: PFIZER, INC., OSI PHARMACEUTICALS, INC.Inventors: Eric R. Larson, Mark C. Noe, Thomas G. Gant
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Patent number: 7442240Abstract: An alkoxylpropyl isothiazolinone of formula: C6H6Cl2NO2SR, in which R is CH3, CH2CH3, CH(CH3)2, CH2CH2CH2CH3, CH2CH2OCH3 or CH2CH2OC6H5Cl. A method for preparing the isothiazolinone by reacting sodium polysulphide with methyl acrylate to obtain dimethyl dithiodipropionate, followed by aminolysis with alkoxyl propylamine to obtain N,N?-dialkoxylpropyldithio-dipropionamide, which is then reacted with sulfuric chloride. The alkoxylpropyl-isothiazolinone of the invention can be used for preparing marine antifouling paint coating as antifoulant, and also used as bactericide.Type: GrantFiled: September 30, 2005Date of Patent: October 28, 2008Assignee: Ocean University of ChinaInventors: Liangmin Yu, Xiaohui Jiang, Zhiming Zhang, Huanzhi Xu, Changcheng Li
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Publication number: 20080255122Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 9, 2006Publication date: October 16, 2008Applicant: ASTRAZENECA ABInventors: Jonas Bostrom, Kay Brickmann, Anders Broo, Robert Judkins, Lanna Li, Pernilla Sandberg, Marianne Swanson, Christer Westerlund, Patrik Holm
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Patent number: 7429667Abstract: The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones.Type: GrantFiled: January 20, 2006Date of Patent: September 30, 2008Assignee: Ardea Biosciences, Inc.Inventors: Hassan Abdellaoui, Robert Tam, Huanming Chen, Varaprasad Chamakura, Dinesh Barawkar, Andreas Maderna, Zhi Hong, Stanley Lang
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Publication number: 20080227986Abstract: Provided is a process for the preparation of an N-substituted isothiazolinone derivative having the general formula (I), comprising reacting N-substituted 3-mercaptopropionamides of formula (II) or N,N?-bis-substituted 3,3?-dithiodipropionamides of formula (III) with sulfuryl chloride in the absence of solvents. Also provided is a process for the preparation of a compound having the general formula (III), comprising reacting a methyl ester of formula (IV) with an amine of formula (V) in a solvent of methanol. As no addition solvent is used in the process of the invention, the cost of manufacturing and pollution to the environment can be reduced.Type: ApplicationFiled: April 3, 2006Publication date: September 18, 2008Applicant: Beijing Tianqing Chemicals Co. Ltd.Inventor: Yuechun Jin
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Patent number: 7405218Abstract: The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.Type: GrantFiled: February 3, 2003Date of Patent: July 29, 2008Assignees: Pfizer, Inc., OSI Pharmaceuticals, Inc.Inventors: Eric R. Larson, Mark C. Noe, Thomas G. Gant
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Patent number: 7402678Abstract: Multifunctional compounds having acylsulfonamide amine-reactive groups are described that can be used for the capture of amine containing materials.Type: GrantFiled: December 17, 2004Date of Patent: July 22, 2008Assignee: 3M Innovative Properties CompanyInventors: Karl E. Benson, Cary A. Kipke, Brinda B. Lakshmi, Charles M. Leir, George G. I. Moore, Rahul Shah
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Publication number: 20080149175Abstract: Disclosed are an organic dye having a specific structure, a photoelectric conversion material containing the dye, a semiconductor electrode formed of a substrate having an electrically conductive surface, a semiconductor layer coated on the electrically conductive surface and the above dye adsorbed on the surface, and a photoelectric conversion device to which the above dye is applied. The present invention uses the above dye and can therefore provide a photoelectric conversion device excellent in photoelectric conversion efficiency, and the photoelectric conversion device is suitable for use in a solar cell or the like.Type: ApplicationFiled: November 14, 2007Publication date: June 26, 2008Inventors: Tamotsu Horiuchi, Hidetoshi Miura, Tatsuya Kodera
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Publication number: 20080139616Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 9, 2006Publication date: June 12, 2008Applicant: ASTRAZENECA ABInventors: Lanna Li, Marianne Swanson, Kay Brickmann
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Publication number: 20080125396Abstract: The present invention relates to certain novel compounds of formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 9, 2006Publication date: May 29, 2008Applicant: AtraZeneca ABInventors: Marianne Swanson, Kay Brickmann, Lanna Li
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Patent number: 7365196Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.Type: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
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Publication number: 20070265321Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 7, 2007Publication date: November 15, 2007Inventors: Robert M. Burk, David W. Old, Todd Gac
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Patent number: 7276602Abstract: The invention relates to compounds of the formula 1 or pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof, wherein wherein X, R1, and R2 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.Type: GrantFiled: July 24, 2003Date of Patent: October 2, 2007Assignee: Pfizer IncInventors: Blaise Lippa, Tricia Ann Kwan, Joel Morris, Susan D. LaGreca, Matthew David Wessel
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Patent number: 7253198Abstract: The present invention relates to novel hydroxyethylamine compounds having Asp2 (?-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.Type: GrantFiled: December 3, 2003Date of Patent: August 7, 2007Assignee: Glaxo Group LimitedInventors: Emmanuel H Demont, Andrew Faller, David Timothy MacPherson, Peter Henry Milner, Alan Naylor, Sally Redshaw, Steven James Stanway, David R Vesey, Daryl S Walter
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Patent number: 7169933Abstract: Compounds having two reactive functional groups are described that can be used to provide a connector group between a substrate and an amine-containing material. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonylaminocarbonyl group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a carbonylimino-containing connector group. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.Type: GrantFiled: November 14, 2003Date of Patent: January 30, 2007Assignee: 3M Innovative Properties CompanyInventors: Karl E. Benson, Moses M. David, Cary A. Kipke, Brinda B. Lakshmi, Charles M. Leir, George G. Moore, Rahul Shah
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 6989451Abstract: Substituted isothiazole compounds and compositions are provided, wherein particularly preferred compositions and methods are directed towards inhibition of various protein kinases (especially MEK and/or ERK). Consequently, particularly preferred methods include treatment of diseases associated with abnormality in MEK and/or ERK function.Type: GrantFiled: June 4, 2003Date of Patent: January 24, 2006Assignee: Valeant Research & DevelopmentInventors: Weijian Zhang, William Ricketts, Haoyun An, Zhi Hong
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Patent number: 6927216Abstract: The present application describes novel cyclic sulfonyl derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.Type: GrantFiled: September 17, 2001Date of Patent: August 9, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Robert J. Cherney, Bryan W. King
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Patent number: 6852716Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: February 10, 2003Date of Patent: February 8, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Jason K. Myers, Vincent E. Groppi, Jr.
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Patent number: 6833370Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3 I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: April 26, 2000Date of Patent: December 21, 2004Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jerome F. Daanen, Keith Brian Ryther, Jianguo Ji
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Patent number: 6831091Abstract: The invention relates to hydrochloride, hydrobromide, hemi-citrate, acetate, p-tosylate, L-tartrate, hemi-succinate, and mesylate salt forms of 3-(4-bromo-2,6-difluoro-benzyloxy)-5-[3-(4-pyrrolidin-1-yl-butyl)-ureido]-isothiazole-4-carboxylic acid amide having the following formula: The invention also relates to pharmaceutical compositions containing the hydrochloride, hydrobromide, hemi-citrate, acetate, p-tosylate, L-tartrate, hemi-succinate, and mesylate salts of formula I. The invention further relates to methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above salts and to methods of preparing the crystal forms of the above salts.Type: GrantFiled: November 27, 2001Date of Patent: December 14, 2004Assignee: Pfizer Inc.Inventors: Thomas George Gant, Glenn R. Williams
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Patent number: 6828276Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C1, C2, C3 are cyclic radicals, X1 is a hetero atom, X2 is a chain of carbon atoms, L is a chain-like element, R1, R2, R3, R4, R5 are various radicals, and Y and Z are monoatomic bridge elements.Type: GrantFiled: August 30, 2001Date of Patent: December 7, 2004Assignee: Aventis CropScience GmbHInventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Hermann Bieringer, Thomas Auler, Hubert Menne
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Patent number: 6809107Abstract: This invention provides compounds having the following general structures: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.Type: GrantFiled: June 14, 2000Date of Patent: October 26, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ramesh M. Kanojia, Alfonzo D. Jordan, Allen B. Reitz, Mark J. Macielag, Boyu Zhao
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Patent number: 6806369Abstract: PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: November 5, 2002Date of Patent: October 19, 2004Assignee: SmithKline Beecham CorporationInventors: Kelly M. Aubart, Siegfried B. Christensen, IV, Jacques Briand, Maxwell David Cummings
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Publication number: 20040186152Abstract: Chlorinating agent is reacted with a compound represented by formula (I) 1Type: ApplicationFiled: March 26, 2004Publication date: September 23, 2004Applicant: Chemicrea Inc.Inventors: Masayuki Morita, Guo-bin Liu, Noriko Yoneta
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Publication number: 20040147574Abstract: Novel isothiazole compounds, including derivatives thereof, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, hyperproliferative disorders and fibrotic diseases.Type: ApplicationFiled: January 26, 2004Publication date: July 29, 2004Applicant: Pfizer IncInventor: Michael J. Munchhof
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Patent number: 6759423Abstract: The present invention relates to the use of 4-hydroxyisothiazole compounds as antimicrobially active substances, certain new 4-hydroxyisothiazole compounds and a process for their preparation.Type: GrantFiled: October 3, 2001Date of Patent: July 6, 2004Assignee: Ciba Specialty Chemicals CorporationInventors: Werner Hölzl, Wolfgang Haap, Dietmar Ochs, Karin Puchtler, Marcel Schnyder, Dinesh Narendra Rele, Sitaram Pal, Asawari Bhikaji Mahtre, Surendra Umesh Kulkarni, Arakali Srinivasarao Radhakrishna
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Patent number: 6750346Abstract: The disclosure is directed to so-called laser-compatible NIR marker dyes based on polymethines for use in optical, in particular, fluorescence optical determination and detection methods, for example, in the fields of medicine, pharmaceutics and in the areas of life science, materials science and environmental science. The disclosure further discusses the aim of the invention which was to create NIR marker dyes based on polymethine which have a high degree of photostability and stability in storage as well as a high fluorescent yield and which can be excited to fluorescence in the easiest possible manner by means of laser radiation in the visible or NIR spectral range, particularly with light of an argon, helium/neon, or diode laser. Dyes based on polymethine of general formula (I) are used.Type: GrantFiled: January 22, 2002Date of Patent: June 15, 2004Assignee: Carl Zeiss Jena GmbHInventors: Peter Czerney, Frank Lehmann, Bernd Schweder, Matthias Wenzel
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Patent number: 6746989Abstract: The invention relates to novel substituted benzoylpyrazoles of the general formula (I), in which n represents the numbers 0, 1, 2 or 3, A represents a single bond or represents alkanediyl(alkylene), R1 represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkoxycarbonyl or cycloalkyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl, Y represents hydrogen or represents in each case optionally substitutedType: GrantFiled: September 26, 2001Date of Patent: June 8, 2004Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Hans-Georg Schwarz, Heinz-Jürgen Wroblowsky, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
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Patent number: 6740759Abstract: Chlorinating agent is reacted with a compound represented by formula (I) (wherein R represents C1 to C8 alkyl groups or aralkyl groups) or a compound represented by formula (II) in a solvent in which hydrogen chloride is insoluble or has low solubility.Type: GrantFiled: September 20, 2000Date of Patent: May 25, 2004Assignee: Chemicrea, Inc.Inventors: Masayuki Morita, Guo-bin Liu, Noriko Yoneta
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Patent number: 6696475Abstract: The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.Type: GrantFiled: August 8, 2001Date of Patent: February 24, 2004Assignee: NeuroSearch A/SInventors: Bjarne H. Dahl, Palle Christophersen
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Publication number: 20040006096Abstract: Imido and Amido substituted alkanohydroxamic acids reduce the levels of TNFa and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.Type: ApplicationFiled: June 16, 2003Publication date: January 8, 2004Inventors: George W. Muller, Hon-Wah Man
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Patent number: 6670385Abstract: The present invention relates to novel aryl-substituted S(O)m cycles of the formula (I) in which F1, F2, G, V, W, X, Y, Z and m are each as defined in the description, to processes for their preparation and to their use in agriculture, for example as crop protection agents (fungicides, herbicides and insecticides).Type: GrantFiled: November 26, 2001Date of Patent: December 30, 2003Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Oliver Kretschik, Thomas Schenke, Ralf-Ingo Schenkel, Jürgen Wiedemann, Christoph Erdelen, Peter Lösel, Mark Wilhelm Drewes, Dieter Feucht, Wolfram Andersch
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Publication number: 20030220339Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.Type: ApplicationFiled: January 29, 2003Publication date: November 27, 2003Applicant: Tularik Inc.Inventors: Xian Yun Jiao, Frank Kayser, David J. Kopecky, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Publication number: 20030216396Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.Type: ApplicationFiled: February 11, 2003Publication date: November 20, 2003Applicant: BAYER CORPORATIONInventors: Jacques Dumas, William J. Scott, Bernd Riedl
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Publication number: 20030212116Abstract: A heterocyclic imino compound of the formula (1) and an agrochemically acceptable salt thereof; and an agricultural chemical, fungicide and insecticide containing at least one member selected from the group of such compounds as an active ingredient: 1Type: ApplicationFiled: June 25, 2002Publication date: November 13, 2003Inventors: Toshio Niki, Takashi Mizukoshi, Hiroaki Takahashi, Jun Satow, Tomoyuki Ogura, Kazuhiro Yamagishi, Hiroyuki Suzuki, Fumio Hayasaka
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Publication number: 20030203889Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.Type: ApplicationFiled: April 1, 2003Publication date: October 30, 2003Applicant: Merck & Co., Inc.Inventors: Peter Blurton, Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher, Angus Murray MacLeod, Daniel Spinks, Monique Bodil Van Niel
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Publication number: 20030190566Abstract: A silver halide photosensitive material contains a compound of the following general formula (I): 1Type: ApplicationFiled: September 24, 2002Publication date: October 9, 2003Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Tadashi Inaba, Masaru Takasaki, Atsushi Matsunaga, Mamoru Sakurazawa, Shinichi Ichikawa
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Publication number: 20030149048Abstract: The present invention relates to compounds of the formula 1 1Type: ApplicationFiled: February 3, 2003Publication date: August 7, 2003Applicant: Pfizer Inc.Inventors: Eric R. Larson, Mark C. Noe, Thomas G. Gant
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Patent number: 6593349Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by opening potassium channels associated with the onset or recurrence of the indicated conditions.Type: GrantFiled: March 11, 2002Date of Patent: July 15, 2003Assignee: ICAgen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato
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Publication number: 20030125364Abstract: A novel antirheumatic agent comprising as an active ingredient a compound of formula I: 1Type: ApplicationFiled: December 4, 2002Publication date: July 3, 2003Inventors: Saichi Matsumoto, Hirokuni Jyoyama, Shinji Kakudo, Kohji Hanasaki, Kenzo Koizumi, Tsuneaki Sakata, Ryuji Suzuki
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Patent number: 6583291Abstract: A safe and economical process for obtaining salts of 4-carboxy-3-hydroxy-5-mercapto-isothiazole. This process comprises refluxing a disodium or dipotassium salt of 3-hydroxy-5-mercapto-4-isothiazole carbonitrile in an aqueous solution of sodium or potassium hydroxide to produce the desired salt. The desired salt may be precipitated out of solution by adjusting the pH downward to a minimum value of about pH 8. Compounds produced by this process may be used for producing semi-synthetic cephalosporins.Type: GrantFiled: April 17, 2002Date of Patent: June 24, 2003Assignee: ACS Dobfar S.p.A.Inventors: Maurizio Zenoni, Alessandro Donadelli, Marco Silvagni
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Patent number: 6566382Abstract: The present invention relates to isothiazolone-containing compositions comprising a) 3-isothiazolone compounds; b) a metal nitrate; c) magnesium chloride; d) at least one compound selected from the group consisting of iodic acid, periodic acid, an iodate salt, and a periodate salt; e) chlorite salts; and f) solvents. The invention further provides a method for stabilizing isothiazolone-containing compositions by inhibiting precipitation of by-products formed during production and precipitation of the compounds formed during storage. The compositions of the invention are useful for suppressing the growth of microorganisms.Type: GrantFiled: November 27, 2001Date of Patent: May 20, 2003Assignees: Lonza Inc., SK Chemicals Co., Ltd.Inventors: Miron Gerard Still, Wan Pyo Hong, Jin Man Kim, Ki Seung Choi, Jung Ho Park, Jae Min Ha, Hi Weon Jung, Soon Jong Hahn
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Patent number: 6548526Abstract: The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.Type: GrantFiled: March 9, 2001Date of Patent: April 15, 2003Assignee: Pfizer IncInventors: Eric R. Larson, Mark C. Noe, Thomas G. Gant
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Publication number: 20030065192Abstract: Novel antimicrobial compounds based on 5-substituted 3-isothiazolones, where the 5-substituent is an aryl or heterocyclic ether/thioether group, are disclosed. These 5-substituted 3-isothiazolones provide enhanced antimicrobial activity over that of related 3-isothiazolones, particularly when the 5-substituent is a substituted pyridinyl thioether group.Type: ApplicationFiled: December 12, 2001Publication date: April 3, 2003Inventors: Tirthankar Ghosh, Barry Clifford Lange, Eileen Fleck Warwick
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Patent number: 6534076Abstract: The present invention relates to stabilized isothiazolone compositions and methods of stabilization of isothiazolone, more particularly, to stabilized isothiazolone solutions comprising (a) an isothiazolone composition, (b) sulfuric acid, and (c) solvent.Type: GrantFiled: June 5, 2000Date of Patent: March 18, 2003Assignee: SK ChemicalsInventors: Soon-Jong Hahn, Jin-Man Kim, Ki-Seung Choi, Seung-Hwan Kim, Jung-Ho Park, Jae-Min Ha, Gi-Bae Kim
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Patent number: 6531604Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.Type: GrantFiled: January 11, 2002Date of Patent: March 11, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Patent number: 6511673Abstract: Microbicidal compositions containing selected ratios of a non-halogenated 2-alkyl-3-isothiazolone and one or more (C1-C7) esters of para-hydroxybenzoic acid are disclosed as improved formulations for controlling microbial growth. In particular the combination of 2-methyl-3-isothiazolone with a mixture of methyl para-hydroxybenzoate and propyl para-hydroxybenzoate is especially effective as a microbicidal component in personal care compositions.Type: GrantFiled: April 12, 2001Date of Patent: January 28, 2003Assignee: Rohm and Haas CompanyInventors: Li Liang Chia, Megan Anne Diehl, Christine Mary Schultz, Dolores Ann Shaw, Eileen Fleck Warwick, Terry Michael Williams