Chalcogen Attached Directly To Diazole Ring Nitrogen By Nonionic Bonding Patents (Class 548/307.7)
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Patent number: 10927083Abstract: The present invention provides inhibitors of TAK1 having formula (II), affinity resins, and fluorescent dyes and methods of using such compounds to treat various diseases or in protein isolation or purification.Type: GrantFiled: February 12, 2019Date of Patent: February 23, 2021Assignee: Duke UniversityInventors: Emily Derbyshire, Timothy A. J. Haystead, Philip F. Hughes
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Patent number: 9018393Abstract: A method for preparing 2-(N-substituted)-amino-benzimidazole derivatives is provided, which comprises the following steps: (1) reacting a compound of 2-(N-protecting group)-O-aryl diamine with a compound of N-phenoxycarbonyl monosubstituted amine to obtain a compound of 2-(N-protecting group)-amino aryl urea; (2) in a suitable organic solvent, performing dehydrating cyclization reaction of the compound of 2-(N-protecting group)-amino aryl urea in the presence of an organic base and dichloro triphenylphosphine prepared by triphenylphosphine oxide with oxalyl chloride or diphosgene or triphosgene, or dibromo triphenylphosphine prepared by triphenylphosphine oxide with bromine, to produce a compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole; (3) deprotecting the resulting compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole to obtain the compound 2-(N-substituted)-amino-benzimidazole.Type: GrantFiled: January 26, 2011Date of Patent: April 28, 2015Assignee: ABA Chemicals CorporationInventors: Yueheng Jiang, Tong Cai, Limin Que, Zhigang Lin
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Patent number: 8476435Abstract: A fluorine-containing polyether carboxylic acid amide represented by the general formula: CnF2n+1O(C3F6O)mRfCONHAr, wherein Rf is a fluorocarbon group having 1 to 2 carbon atoms, Ar is a nitrogen-containing heterocyclic group, n is an integer of 1 to 3, and m is an integer of 10 to 30, is produced by reacting a fluorine-containing polyether carboxylic acid fluoride represented by the general formula: CnF2n+1(C3F6O)mRfCOF, wherein Rf, n, and m are as defined above, with a nitrogen-containing heterocyclic amine compound represented by the general formula: ArNH2, wherein Ar is as defined above; wherein the reaction is carried out while a reaction temperature is first increased to 80 to 100° C., and then increased at a temperature increase rate that produces a temperature difference of 3 to 5° C. after 48 hours.Type: GrantFiled: April 16, 2010Date of Patent: July 2, 2013Assignee: Unimatec Co., Ltd.Inventors: Keisuke Kokin, Seiichiro Murata, Hideki Abe, Yusuke Takahashi
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Publication number: 20120041201Abstract: A fluorine-containing polyether carboxylic acid amide represented by the general formula: CnF2n+1O(C3F6O)mRfCONHAr, wherein Rf is a fluorocarbon group having 1 to 2 carbon atoms, Ar is a nitrogen-containing heterocyclic group, n is an integer of 1 to 3, and m is an integer of 10 to 30, is produced by reacting a fluorine-containing polyether carboxylic acid fluoride represented by the general formula: CnF2n+1(C3F6O)mRfCOF, wherein Rf, n, and m are as defined above, with a nitrogen-containing heterocyclic amine compound represented by the general formula: ArNH2, wherein Ar is as defined above; wherein the reaction is carried out while a reaction temperature is first increased to 80 to 100° C., and then increased at a temperature increase rate that produces a temperature difference of 3 to 5° C. after 48 hours.Type: ApplicationFiled: April 16, 2010Publication date: February 16, 2012Applicant: UNIMATEC CO., LTD.Inventors: Keisuke Kokin, Seiichiro Murata, Hideki Abe, Yusuke Takahashi
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Patent number: 7482466Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: November 14, 2007Date of Patent: January 27, 2009Assignee: Pharmacyclics, Inc.Inventors: Erik J. Verner, Hon C. Hui
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Patent number: 7176312Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.Type: GrantFiled: October 12, 2002Date of Patent: February 13, 2007Assignees: The Scripps Research Institute, IRM LLCInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
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Publication number: 20040063584Abstract: Cyclohexenone derivatives of benzazolones of the formula I 1Type: ApplicationFiled: May 29, 2003Publication date: April 1, 2004Inventors: Guido Mayer, Ulf Miblitz, Ernst Baumann, Wolfgang von Deyn, Steffen Kudis, Michel Hofmann, Thorsten Volk, Matthias Witschel, Cyrill Zagar, Andreas Landes, Klaus Langemann
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Patent number: 6613743Abstract: The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity. The sulfonamides of formula I have the structure: wherein A, B, D, D′, E, G and R7 are as defined above.Type: GrantFiled: December 6, 2000Date of Patent: September 2, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Robin Hale, Clarence Webster Andrews, III, Eric Steven Furfine, Ronald George Sherrill, Andrew Spaltenstein, Gregory Thomas Lowen
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Publication number: 20010047020Abstract: Benzimidazole derivatives of the formula (I): 1Type: ApplicationFiled: March 27, 2001Publication date: November 29, 2001Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Patent number: 6187928Abstract: Novel imidazolium compounds of the formula wherein A represents the atomic group necessary to form a heteroaromatic ring, which may be optionally substituted by one or more R substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substitutents; B is an optional substituent which represents the atomic group necessary to form a heteroaromatic ring or a double or triple carbon-nitrogen bond, which may optionally be substituted by one or more R′ substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substitutents; C is an optional substituent which represents the atomic group necessary to form an aromatic or heteroaromatic ring, which may optionally be substituted by one or more R″″ substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substituents; R″ and R′″ are each independently a lower alkType: GrantFiled: March 7, 2000Date of Patent: February 13, 2001Assignee: The Rockefeller UniversityInventors: Robert J. Donovan, Robert J. Morgan