Chalcogen Or The Nitrogen Attached Directly To Diazole Ring Nitrogen By Nonionic Bonding Patents (Class 548/331.1)
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Patent number: 9084423Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: GrantFiled: January 8, 2014Date of Patent: July 21, 2015Assignee: North Carolina State UniversityInventors: Christian Melander, John Cavanagh, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards
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Patent number: 8653124Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: GrantFiled: February 2, 2011Date of Patent: February 18, 2014Assignee: North Carolina State UniversityInventors: Christian Melander, John Cavanagh, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards
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Publication number: 20140023691Abstract: Disclosure is provided for imidazole derivative compounds useful to inhibit the formation of biofilms and/or inhibit microbial growth, compositions including these compounds, devices including these compounds, and methods of using the same.Type: ApplicationFiled: September 24, 2013Publication date: January 23, 2014Applicant: North Carolina State UniversityInventors: Christian Melander, W. Steve McCall, Zhaoming Su, Roberta Worthington
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Publication number: 20130225587Abstract: The compound of Formula (I), pharmaceutically acceptable salts thereof, solvates thereof, chelates thereof, non-covalent complexes thereof or produgs of compounds mentioned above or the mixture of any form above mentioned are provided. The use of the compounds in manufacturing a medicament for the treatment and/or prevention of diabetes, obesity and related disorders.Type: ApplicationFiled: November 9, 2011Publication date: August 29, 2013Applicants: Zhejiang Beta Pharma Incorporation, Fujian Haixi Pharmaceuticals, Inc.Inventors: Xinshan Kang, Wei Long, Cunbo Ma, Yanping Wang, Xiaoyan Shen, Yunyan Hu, Fenlai Tan, Yinxiang Wang
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Patent number: 8466182Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.Type: GrantFiled: November 2, 2011Date of Patent: June 18, 2013Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University of Maryland, BaltimoreInventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
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Publication number: 20120283303Abstract: The present invention relates to the use of N-aminoimidazole or N-aminoimidazole thione derivatives as cytoprotective compounds in vitro and in vivo and for the treatment or prevention of cell death mediated disorders and/or GSK-3 mediated disorders or processes.Type: ApplicationFiled: April 30, 2012Publication date: November 8, 2012Applicant: K.U.LEUVEN RESEARCH AND DEVELOPMENTInventors: Christophe Pannecouque, Wim Robberecht, Miguel Stevens
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Patent number: 8071609Abstract: This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: August 11, 2006Date of Patent: December 6, 2011Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
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Patent number: 8053435Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.Type: GrantFiled: November 1, 2007Date of Patent: November 8, 2011Assignees: Korea Research Institute of Chemical Technology, Crystalgenomics, Inc.Inventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee, Dongkyu Shin
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Patent number: 7906544Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: GrantFiled: January 25, 2008Date of Patent: March 15, 2011Assignee: North Carolina State UniversityInventors: Christian Melander, John Cavanagh, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards
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Patent number: 7745458Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.Type: GrantFiled: August 18, 2006Date of Patent: June 29, 2010Assignee: Glaxo Group LimitedInventors: Luca Arista, Anna Checchia, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli
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Patent number: 7479357Abstract: An organophotoreceptor that includes: (a) a charge transport material having the formula wherein A is selected from heterocyclic groups, naphthyl group, alkylsulfonylphenyl, stilbenyl or the group X, wherein X is represented by the formula B is selected from hydrogen, alkyl group, and an aryl group, with the proviso that when A is naphthyl, B is naphthyl; or where R1 is selected from the group consisting of N-pyrrolyl, N-pyrazolyl, N-tetrazolyl, N-indolyl, N-carbazolyl, N-triazolyl, N-imidazolyl, N-benzimidazolyl, N-indazolyl, and N-benzotriazolyl group, and R3 is a 9-fluorenone group. (b) a charge generating compound; and (c) an electrically conductive substrate.Type: GrantFiled: September 13, 2002Date of Patent: January 20, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katritzky, Ritu Jain, Rexiat Maimait, Anatoliy V. Vakulenko
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Patent number: 7304083Abstract: A 2-iminoimidazole derivative represented by the formula: {wherein R1, R2 and R3 represent hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10–R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.}or salt thereof.Type: GrantFiled: April 19, 2002Date of Patent: December 4, 2007Assignee: Eisai R&D Management Co., Ltd.Inventors: Shuichi Suzuki, Makoto Kotake, Mitsuaki Miyamoto, Tetsuya Kawahara, Akiharu Kajiwara, Ieharu Hishinuma, Kazuo Okano, Syuhei Miyazawa, Richard Clark, Fumihiro Ozaki, Nobuaki Sato, Masanobu Shinoda, Atsushi Kamada, Itaru Tsukada, Fumiyoshi Matsuura, Yoshimitsu Naoe, Taro Terauchi, Yoshiaki Oohashi, Osamu Ito, Hiroshi Tanaka, Takashi Musha, Motoji Kogushi, Tsutomu Kawata, Toshiyuki Matsuoka, Hiroko Kobayashi, Ken-ichi Chiba, Akifumi Kimura, Naoto Ono
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Publication number: 20070197569Abstract: The present invention relates to a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, X, A, and n are as defined in the specification and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms thereof.Type: ApplicationFiled: January 19, 2007Publication date: August 23, 2007Inventors: Marius Hoener, Sabine Kolczewski, Henri Stalder
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Patent number: 7186742Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1–R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: May 12, 2004Date of Patent: March 6, 2007Assignee: Pfizer IncInventors: Mark A Dombroski, Allen J. Duplantier, Chakrapani Subramanyam
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Patent number: 7109227Abstract: The invention relates to novel imidazolamino compounds. Also disclosed are methods of treating cancer by using one of these compounds and pharmaceutical compositions containing one of these compounds.Type: GrantFiled: August 26, 2003Date of Patent: September 19, 2006Assignee: National Health Research InstitutesInventors: Chiung-Tong Chen, Wen-Tai Li, Der-Ren Hwang, Chu-Chung Lin
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Patent number: 7049332Abstract: An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R1 is selected from hydrogen, methyl or ethyl, R2 is selected from hydrogen, SH or —SR0 wherein R0 is methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl.Type: GrantFiled: February 23, 2001Date of Patent: May 23, 2006Assignee: K. U. Leuven Research & DevelopmentInventors: Erik De Clercq, Arthur Van Aerschot, Piet Herdewijn, Irene Lagoja, Christophe Pannecoucque
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Patent number: 6891068Abstract: Disclosed is a one step method for preparing a ?-substituted sulfide by treating a ?-halosulfide with a nucleophile in water.Type: GrantFiled: March 19, 2003Date of Patent: May 10, 2005Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Hartmuth C. Kolb, Zhi-Cai Shi, Zhi-Min Wang
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Patent number: 6846838Abstract: Compounds having the formula (I), or pharmaceutically-acceptable salts, hydrates or prodrugs thereof, are effective as inhibitors of Factor VIIa.Type: GrantFiled: June 17, 2003Date of Patent: January 25, 2005Assignee: Bristol-Myers Squibb CompanyInventors: William A. Slusarchyk, Scott A. Bolton, Timothy Herpin, Gregory S. Bisacchi, Zulan Pi, E. Scott Priestley
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Publication number: 20040248958Abstract: The present invention relates to novel heterocyclic amide derivatives of the formula 1Type: ApplicationFiled: June 10, 2004Publication date: December 9, 2004Inventors: Graham Holmwood, Klaus-Gunther Tietjen, Michael Schindler, Christoph Erdelen, Angelika Lubos-Erdelen, Ulrike Wachendorff-Neumann, Andreas Turberg, Olaf Hansen
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Publication number: 20040242662Abstract: Novel azinylsulfonylimidazoles of the formula 1Type: ApplicationFiled: October 7, 2003Publication date: December 2, 2004Inventors: Stefan Hillebrand, Lutz Assmann, Ulrike Wachendorff-Neumann
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Patent number: 6797828Abstract: The invention provides novel processes for preparing efficiently compounds of general formula (1) (wherein R1 and R2 are each independently hydrogen, optionally substituted C1-C10 alkyl, C3-C14 hydrocarbyl bearing alicyclic skeleton, or the like) and initermediates thereof. Compounds of general formula (I) can be prepared by subjecting compounds of general formula (II) and/or salts thereof to cyclization hydrolysis in an aqueous basic solution. Further, compounds of general formula (II) can be prepared from industrially easily available diaminomaleonitrile in a high yield.Type: GrantFiled: March 15, 2002Date of Patent: September 28, 2004Assignee: Nippon Soda Co. Ltd.Inventors: Hiroaki Shibasaki, Fumihiko Nagasaki, Mitsuru Takase, Satoru Yamazaki, Yutaka Ishii, Kimihiko Oohata
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Patent number: 6737433Abstract: Imidazole derivatives of the formula: in which R1 and R2 are each independently hydrogen, (C1-C6)alkyl or (C3-C8)cycloalkyl; n is 0, 1 or 2; R3, R4, R5 and R6 are each independently hydrogen or a (C1-C6)alkyl, halogen, cyano, (C1-C6)alkoxy, trifluoromethyl, (C1-C6)alkylthio, (C1-C6)alkylsulfonyl, sulfonamido, acyl, (C1-C6)alkoxycarbonyl, or carboxamido group; R3 and R6 together with the phenyl ring bearing them can also form a benzofurane, or a N-methylbenzotriazole. The invention also relates to pharmaceutical compositions containing these derivatives, and to the uses thereof.Type: GrantFiled: December 16, 2002Date of Patent: May 18, 2004Assignee: Laboratoire TheramexInventors: Nathalie Adje, Paule Bonnet, Denis Carniato, Remi Delansorne, Jean Lafay, Jean-Claude Pascal
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Publication number: 20040014745Abstract: This invention relates to new amide compounds having the potentiation of the cholinergic activity, etc., and represented by general formula [I].Type: ApplicationFiled: July 15, 2003Publication date: January 22, 2004Applicant: Fujisawa Pharmaceutical Co. Ltd.Inventors: Akira Yamada, Satoshi Aoki
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Patent number: 6677353Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6620963Abstract: Compounds of the formula where the variables have the meaning defined in the specification, which bind specifically or selectively to to RAR&agr; retinoid receptors.Type: GrantFiled: September 19, 2002Date of Patent: September 16, 2003Assignee: Allergan, Inc.Inventors: Tien T. Duong, Richard Beard, Roshantha A. Chandraratna
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Patent number: 6566387Abstract: The invention relates to the use of guanidine compounds in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: November 8, 2001Date of Patent: May 20, 2003Assignee: SmithKline Beecham CorporationInventors: Michael R. Palovich, Katherine L. Widdowson
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Publication number: 20030040630Abstract: Sulphonyl-imidazole derivatives of the formula 1Type: ApplicationFiled: August 2, 2002Publication date: February 27, 2003Inventors: Holger Weintritt, Reinhard Lantzsch, Thorsten Muh
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Patent number: 6479531Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently ═N—, —N(R5)—═CH—, —S— or —O—.Type: GrantFiled: August 2, 2001Date of Patent: November 12, 2002Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Ildiko Maria Buck, Ian Duncan Linney, Paul Trevor Wright, Iain Mair McDonald, Katherine Isobel Mary Steel, Robert Antony David Hull, Sonia Patricia Roberts, John David Gaffen, Jeremy Gilbert Vinter, Martin Keith Walker, James Whyte Black, Gillian Fairfull Watt, Elaine Anne Harper, Nigel Paul Shankley, Matthew John Tozer, David John Dunstone, Michael John Pether, Elliot James Lilley, David Andrew Sykes, Caroline Minli Rachel Low, Eric Peter Griffin, Laurence Wright
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Patent number: 6458803Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: November 23, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6448286Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 28, 1998Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Publication number: 20020095055Abstract: The present invention provides a process for the preparation of high quality amine oxide by reacting a tertiary or secondary amine with hydrogen peroxide as an oxidant in presence of a recyclable heterogeneous layered double hydroxide exchanged with one of the anions of transition metal oxides as a catalyst in a solvent selected from the group consisting of water, water containing dodecylbenzenesulfonic acid sodium salt as additive, and a water miscible organic solvent.Type: ApplicationFiled: September 27, 2001Publication date: July 18, 2002Inventors: Boyapati M. Choudary, Balagam Bharathi, Mannepalli L. Kantam, Chinta R.V. Reddy, Kondapuram V. Raghavan
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Patent number: 6291499Abstract: Novel 4-substituted cyclohexanes substituted in the 1-position with 2-benzimidazoles, 2-imidazopyridines, or 4-imidazoles either directly or through a C1-C4alkyl, cycloalkyl, hydroxyalkyl, alkoxy or aminoalkyl chain are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: October 25, 2000Date of Patent: September 18, 2001Assignee: Merck & Co., Inc.Inventors: Wayne Thompson, David A. Claremon, Peter M. Munson, John A. McCauley