One Double Bond Between The Ring Members Of The Oxazole Ring Patents (Class 548/237)
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Patent number: 11993592Abstract: The present disclosure provides compounds which are useful for a number of catalytic transformations of organic molecules, non-limiting examples including dehydrogenation of alkanes. The present disclosure further relates to methods of preparing the compounds of the present disclosure.Type: GrantFiled: September 7, 2022Date of Patent: May 28, 2024Assignee: Rutgers, The State University of New JerseyInventors: Alan S. Goldman, Thomas R. Dugan
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Patent number: 11465996Abstract: The present disclosure provides compounds which are useful for a number of catalytic transformations of organic molecules, non-limiting examples including dehydrogenation of alkanes. The present disclosure further relates to methods of preparing the compounds of the present disclosure.Type: GrantFiled: March 23, 2021Date of Patent: October 11, 2022Assignee: Rutgers, The State University of New JerseyInventors: Alan S. Goldman, Thomas R. Dugan
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Publication number: 20150057269Abstract: The present invention regards compositions and methods for the modulation of amidases capable of hydrolysing N-acylethanolamines useable in the therapy of inflammatory diseases. In particular, the present invention regards a compound of general formula (I): enantiomers, diastereoisomers, racemes and mixtures, polymorphs, salts, solvates thereof, wherein: (a) R is a linear alkyl radical having 13 to 19 carbon atoms or alkenyl radical having 13 to 19 carbon atoms carrying a double bond; (b) X is 0 or S; (c) Y is a 2 or 3 carbon atom alkylene residue, optionally substituted with one or two groups equal or different from each other and selected from among the group consisting of: —CH3, —CH2OH, —COOCH3, —COOH. Y may preferably be: —CH2—CH2—, —CH2—CH2—CH2—, CH(CH3)—CH2—, —CH2—CH(CH3)—, —CH2—C(CH3)2—, —CH2—CH(CH2OH)—, —CH2—C((CH2OH)2)—, —CH?CH—, —CH2—CH(COOCH3)—, —CH2—CH(COOH)—, for use as a medicine.Type: ApplicationFiled: February 17, 2012Publication date: February 26, 2015Applicant: Epitech Group S.r.l.Inventors: Francesco Della Valle, Maria Federica Della Valle, Gabriele Marcolongo, Vincenzo Di Marzo, Salvatore Cuzzocrea
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Publication number: 20140364618Abstract: The present invention relates to a method of making indeno-fused naphthol materials, that involves, with some embodiments, forming an indanone acid intermediate, represented by the following general Formula V, With Formula V, m is from 0 to 4, and R1 for each m, Rg and Rh can each be independently selected from, for example, hydrogen and hydrocarbyl.Type: ApplicationFiled: May 13, 2014Publication date: December 11, 2014Applicant: Transitions Opticals, Inc.Inventors: Anu Chopra, Barry Van Gemert, Wenjing Xiao, Huayun Yu
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Patent number: 8883797Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 20, 2012Date of Patent: November 11, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger
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Publication number: 20140287011Abstract: Disclosed is an arthropod pest control composition comprising 2-(2,6-difluorophenyl)-4-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydrooxazole and an inert carrier, wherein the volume median diameter of 2-(2,6-difluorophenyl)-4-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydrooxazole is from 1.5 to 5.Type: ApplicationFiled: November 2, 2012Publication date: September 25, 2014Inventors: Katsuya Natsuhara, Yusuke Kimura, Mamoru Takiuchi
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Patent number: 8809402Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: GrantFiled: December 8, 2011Date of Patent: August 19, 2014Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
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Patent number: 8754236Abstract: The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.Type: GrantFiled: July 22, 2013Date of Patent: June 17, 2014Assignee: Eisai R&D Management Co., Ltd.Inventors: Francis G. Fang, James E. Foy, Lynn Hawkins, Charles Lemelin, Andre LesCarbeau, Xiang Niu, Kuo-Ming Wu
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Patent number: 8658735Abstract: The graft copolymer comprises a polymerizable monomer (A1) represented by general formula (III) and a polymerizable monomer (B1) containing a pyridyl group, and a ligand can be bonded via the functional group at the terminus of R3a. In the formula, R1a represents a polymerizable group, R2a represents an alkylene group having a carbon number of 2-5, R3a represents an organic group having at a terminus a functional group selected from among an azide group, a phenyl azide group, a carboxyl group, a primary to quaternary amino group, an acetal group, an aldehyde group, a thiol group, a disulfide group, an active ester group, a trialkoxysilyl group, and a polymerizable group, and n represents any integer from 5 to 20,000.Type: GrantFiled: August 28, 2009Date of Patent: February 25, 2014Assignee: Tokyo University of Science Educational Foundation Administrative OrganizationInventors: Hidenori Otsuka, Masayuki Fukaishi, Takashi Ishiduka
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Publication number: 20140012010Abstract: Provided is a process for producing an optically active compound represented by Formula (3): (wherein R1 is an alkyl group, an alkynyl group, an alkenyl group, an aliphatic heterocyclic group, a cycloalkyl group, an aryl group, an aralkyl group, or an aromatic heterocyclic group, and any hydrogen atom of R1 may be replaced with a substituent; R2 is a hydrogen atom or a group which is not reactive in the reaction below; and * represents a chiral center) or a salt thereof by subjecting a compound represented by Formula (1): (wherein R1 and R2 have the same meanings as defined in Formula (3)) to a ring closure reaction in the presence of a chiral ligand having 1 or more coordination sites, a Lewis acid represented by Formula (2): MmZn??(2) (wherein M is a metal ion, Z is a counter anion of M, and m and n are integers of 1 to 4), and a sulfonyl halide having an optionally substituted alkyl or phenyl groupType: ApplicationFiled: January 31, 2012Publication date: January 9, 2014Inventors: Osamu Onomura, Yutaro Tsuda, Masami Kuriyama, Toshiharu Yanagi, Kazuya Kodama
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Patent number: 8487114Abstract: Disclosed are compounds having one of the following formulae (11), (12), wherein X is an aromatic nucleophilic substitution leaving group; R1 is hydrogen, an alkyl group, or an aryl group; and Q1 is a carboxyl protecting group or an aldehyde protecting group. Also disclosed are fused thiophenes that can be prepared using these compounds, as well as stannylthio-containing thiophene, thienothiophene, and dithienothiophene compounds that can be used to prepare fused thiophenes. Methods for making and using the aforementioned compounds, fused thiophenes, and stannylthio-containing thiophene, thienothiophene, and dithienothiophene compounds are also disclosed.Type: GrantFiled: March 30, 2009Date of Patent: July 16, 2013Assignee: Corning IncorporatedInventors: Mingqian He, Thomas Mark Leslie, Feixia Zhang
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Patent number: 8460447Abstract: Substituted oxazoline compounds and/or substituted oxazoline derivatives having amorphous, semi-crystalline, or crystalline properties and methods for producing such compounds and derivatives are presented. The substituted oxazoline compounds and/or substituted oxazoline derivatives are useful for various applications. For example, the substituted oxazoline compounds and/or substituted oxazoline derivatives may function as phase-change agents, a binder resins, rheology modifiers or plasticizers for ink compositions.Type: GrantFiled: April 27, 2011Date of Patent: June 11, 2013Assignee: Xerox CorporationInventors: Rina Carlini, Guerino G. Sacripante, Stephan V. Drappel, Bo Wu
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Patent number: 8399675Abstract: This invention relates to novel compounds and a process for preparation of montelukast sodium.Type: GrantFiled: February 22, 2010Date of Patent: March 19, 2013Assignee: Formosa Laboratories, Inc.Inventors: Jui-Te Hung, Ching-Peng Wei
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Publication number: 20130053387Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.Type: ApplicationFiled: May 4, 2011Publication date: February 28, 2013Applicant: FerroKin BioScience, Inc.Inventor: James W. Malecha
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Publication number: 20130012719Abstract: Azolines are oxidized in the presence of a copper-containing catalyst to azoles in the presence of molecular oxygen. A synthetic scheme converting azolines azoles is also provided.Type: ApplicationFiled: July 6, 2012Publication date: January 10, 2013Applicant: University of Southern CaliforniaInventors: Travis J. Williams, Anna C. Dawsey, Vincent Li, Kimberly C. Hamilton, Jianmei Wang
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Publication number: 20120272859Abstract: Substituted oxazoline compounds and/or substituted oxazoline derivatives having amorphous, semi-crystalline, or crystalline properties and methods for producing such compounds and derivatives are presented. The substituted oxazoline compounds and/or substituted oxazoline derivatives are useful for various applications. For example, the substituted oxazoline compounds and/or substituted oxazoline derivatives may function as phase-change agents, a binder resins, rheology modifiers or plasticizers for ink compositions.Type: ApplicationFiled: April 27, 2011Publication date: November 1, 2012Applicant: XEROX CORPORATIONInventors: Rina CARLINI, Guerino G. SACRIPANTE, Stephan V. DRAPPEL, Bo WU
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Patent number: 8143418Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: GrantFiled: February 7, 2011Date of Patent: March 27, 2012Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
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Patent number: 8093275Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: GrantFiled: June 22, 2010Date of Patent: January 10, 2012Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
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Publication number: 20110275636Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.Type: ApplicationFiled: May 4, 2011Publication date: November 10, 2011Applicant: FerroKin BioSciences, Inc.Inventor: James Malecha
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Publication number: 20110098478Abstract: Disclosed are compounds having one of the following formulae (11), (12), wherein X is an aromatic nucleophilic substitution leaving group; R1 is hydrogen, an alkyl group, or an aryl group; and Q1 is a carboxyl protecting group or an aldehyde protecting group. Also disclosed are fused thiophenes that can be prepared using these compounds, as well as stannylthio-containing thiophene, thienothiophene, and dithienothiophene compounds that can be used to prepare fused thiophenes. Methods for making and using the aforementioned compounds, fused thiophenes, and stannylthio-containing thiophene, thienothiophene, and dithienothiophene compounds are also disclosed.Type: ApplicationFiled: March 30, 2009Publication date: April 28, 2011Inventors: Mingqian He, Thomas Mark Leslie, Feixia Zhang
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Publication number: 20110098479Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2 ??(1) wherein RType: ApplicationFiled: December 29, 2010Publication date: April 28, 2011Inventors: KAZUSHI MASHIMA, Takashi Ohshima, Takanori Iwasaki, Hironori Maeda, Kenya Ishida
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Publication number: 20110091508Abstract: The invention features oligofluorinated cross-linked polymers and their use in the manufacture of articles and coating surfaces.Type: ApplicationFiled: October 2, 2008Publication date: April 21, 2011Applicant: Interface Biologics ,Inc.Inventors: Roseita Esfand, J. Paul Santerre, Mark J. Ernsting, H. Hung Pham, Vivian Z. Wang, Meilin Yang
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Patent number: 7888513Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2??(1) wherein R1Type: GrantFiled: December 4, 2006Date of Patent: February 15, 2011Assignee: Takasago International CorporationInventors: Kazushi Mashima, Takashi Ohshima, Takanori Iwasaki, Hironori Maeda, Kenya Ishida
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Publication number: 20110034700Abstract: The present invention describes a heterogeneous chiral catalyst comprising a heterogeneous chiral catalyst precursor complexed with a metal species. The precursor comprises a chiral bisoxazoline group coupled to an inorganic substrate. The heterogeneous chiral catalyst may be capable of catalysing a chemical reaction, for example cyclopropanation, and the chemical reaction may be capable of generating a chiral product.Type: ApplicationFiled: March 8, 2005Publication date: February 10, 2011Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCHInventors: Jackie Y. Ying, Su Seong Lee, Sukandar Hadinoto
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Patent number: 7884211Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: GrantFiled: July 24, 2009Date of Patent: February 8, 2011Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
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Publication number: 20110003787Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: ApplicationFiled: July 26, 2010Publication date: January 6, 2011Inventors: Akihiro Furukawa, Takehiro Fukuzaki, Yukari Onishi, Hideki Kobayashi, Takeshi Honda, Yumi Matsui, Masahiro Konishi, Kenjiro Ueda, Tetsuyoshi Matsufuji
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Publication number: 20100324025Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: ApplicationFiled: September 21, 2009Publication date: December 23, 2010Applicant: University of WashingtonInventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
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Patent number: 7842839Abstract: It is provided to an optically active cycloalkylidenebisamidoalcohol compound represented by the formula (3): wherein R1 represents a C1-6 alkyl group, an optionally substituted phenyl group, an optionally substituted aralkyl group or a hydrogen atom, or two R1s, which are bonded to the same carbon atom, are bonded to form a ring together with the carbon atom to which they are bonded, R2 represents a C1-6 alkyl group, an optionally substituted aralkyl group or an optionally substituted phenyl group and * represents an asymmetric center, a method for producing it and a method for producing an optically active cycloalkylidenebisoxazoline compound represented by the formula (4): wherein R1, R2 and * are as defined above, using thereof.Type: GrantFiled: December 21, 2004Date of Patent: November 30, 2010Assignee: Sumitomo Chemical Company, LimitedInventor: Makoto Itagaki
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Patent number: 7834190Abstract: An objective of the present application is to provide an industrially practicable method for producing an optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof from an inexpensive easily-available starting material. The derivative or salt thereof is useful as an intermediate for a medicine. It is also intended by the present application to provide a useful intermediate of the derivative. The objective is attained by the following method. First, an easily-available 2-halo-3-oxopropionic acid derivative is asymmetrically reduced, and then epoxidated to produce an optically-active epoxycarboxylic acid derivative. Next, the derivative is converted into an optically-active epoxyamide derivative by reaction with cyclopropylamine, and then reacted with a nitrile to obtain an optically-active oxazolinamide derivative. Subsequently, selective acid solvolysis of the oxazoline skeleton gives the optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof.Type: GrantFiled: May 22, 2007Date of Patent: November 16, 2010Assignee: Kaneka CorporationInventors: Kohei Mori, Akira Nishiyama, Naoaki Taoka, Daisuke Moriyama, Nobuo Nagashima
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Patent number: 7816538Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: GrantFiled: July 24, 2009Date of Patent: October 19, 2010Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
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Publication number: 20100217008Abstract: The present invention relates to a new method for the production of valsartan, a valine derivative having the chemical N name is (S)—N-(1-carboxy-2-methylprop-1-yl)-N-pentanoyl-N-[2?-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]amine, and pharmacologically acceptable salts thereof. Furthermore the invention relates to new intermediate compounds which are suitable for the production of valsartan and new methods for the production of intermediate compounds which are suitable for the production of valsartan.Type: ApplicationFiled: December 11, 2007Publication date: August 26, 2010Applicant: ratiopharm GmbHInventors: Jiri Stohandl, Pavel Bobal, Jaroslav Frantisek
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Patent number: 7767667Abstract: It has now been found that certain novel heterocyclic derivitives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)?C(R7)N(R8)—, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)?C(R12)C(R13)?C(R14) 1 12, -, where R,R,R6, R7, R8, RI1, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound with at least one insecticidally compatable carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: August 22, 2008Date of Patent: August 3, 2010Assignee: FMC CorporationInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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Patent number: 7767825Abstract: The present invention relates to a method for preparing 2,2?,6,6?-tetraoxazolinyl biphenyl ligand in chemical industry field. In the present invention, compound (III) is reacted with an activator that can activate the hydroxyl group selected from the group consisting of alkyl halosulfonium compound, aryl halosulfonium compound, phosphoryl chloride, phosphorus pentachloride, thionyl chloride and triphenyl phosphine, in the presence of alkali(s), to give the target product (IV), 2,2?,6,6?-tetraoxazolinyl biphenyl ligand. The ligand of the present invention can be used in various asymmetric reactions catalyzed by metals, with high reactivity and stereoselectivity, and thus represents a good application outlook.Type: GrantFiled: December 29, 2006Date of Patent: August 3, 2010Assignee: Shanghai Jiaotong UniversityInventors: Wanbin Zhang, Yongjian Zhang, Feijun Wang
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Patent number: 7754891Abstract: The present invention relates to a 5,5?-position linked 1,1?-biphenyl axis chiral ligand in chemical industry field. The present invention incorporates both the central chirality of oxazoline and the axial chirality of diphenyls. Such ligand can be used in various asymmetric reactions catalyzed by metal with high reactivity and stereoselectivity, and thus represents a good application outlook. The ligand of the present invention has the formula of: wherein: n=5, 6, 7, 8, 9, 10, 11 or 12; R1=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R2=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R3=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R4=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl.Type: GrantFiled: December 29, 2006Date of Patent: July 13, 2010Assignee: Shanghai Jiaotong UniversityInventors: Wanbin Zhang, Yongjian Zhang, Feijun Wang
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Publication number: 20100152453Abstract: This invention relates to novel compounds and a process for preparation of montelukast sodium.Type: ApplicationFiled: February 22, 2010Publication date: June 17, 2010Applicant: FORMOSA LABORATORIES, INC.Inventors: Jui-Te Hung, Ching-Peng Wei
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Publication number: 20100069367Abstract: Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R00, R200, R400, R500, J11, J21, G1, G21, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: December 7, 2007Publication date: March 18, 2010Applicant: EXELIXIS, INC.Inventors: Brant Clayton Boren, Brett B. Busch, Xiao-Hui Gu, Vasu Jammalamadaka, Shao Po Lu, Richard Martin, Raju Mohan, Edwin Schweiger, William C. Stevens, Tie-Lin Wang, Yinong Xie, Wei Xu
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Patent number: 7659296Abstract: The present invention relates to novel, non-secosteroidal, phenyl-benzoxazole compounds of Formula (I) wherein the variables R, R?, RP, RP3, LP1, LP2, ZP, RB, RB?, LXB and ZXB are as hereinafter defined, their preparation, pharmaceutical compositions, and methods of use.Type: GrantFiled: December 19, 2005Date of Patent: February 9, 2010Assignee: Eli Lilly and CompanyInventors: Quanrong Shen, Alan M. Warshawsky, Ying Kwong Yee
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Patent number: 7626035Abstract: The present invention relates to new optically active heteroaromatic ?-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.Type: GrantFiled: January 3, 2005Date of Patent: December 1, 2009Assignee: Bayer Schering Pharma AGInventors: Johannes Platzek, Ludwig Zorn, Bernd Buchmann, Werner Skuballa, Orlin Petrov
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Publication number: 20090281155Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: ApplicationFiled: July 24, 2009Publication date: November 12, 2009Inventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
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Patent number: 7579478Abstract: The present invention provides processes for the purification of substituted benzoxazole compounds, and in particular 2-(3-fluoro-4-hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol. The processes include recrystallizing the compound from a solution comprising acetone and acetonitrile; treating the crude purified product with a clarifying agent in a solution comprising ethyl acetate, and precipitating or triturating the compound from a mixed solvent system.Type: GrantFiled: March 6, 2006Date of Patent: August 25, 2009Assignee: WyethInventor: Silvio Iera
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Publication number: 20090198070Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2??(1) whereinType: ApplicationFiled: December 4, 2006Publication date: August 6, 2009Applicants: OSAKA UNIVERSITY, TAKASAGO INTERNATIONAL CORPORATIONInventors: Kazushi Mashima, Takashi Ohshima, Takanori Iwasaki, Hironori Maeda, Kenya Ishida
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Patent number: 7560570Abstract: Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having Ki's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an ?-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other ?-unsaturation corresponding to the arachidonyl ?8,9/?11,12 and/or oleyl ?9,10 positions. A preferred ?-keto heterocylic head group is ?-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).Type: GrantFiled: March 28, 2005Date of Patent: July 14, 2009Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20090156829Abstract: The present invention relates to a 5,5?-position linked 1,1?-biphenyl axis chiral ligand in chemical industry field. The present invention incorporates both the central chirality of oxazoline and the axial chirality of diphenyls. Such ligand can be used in various asymmetric reactions catalyzed by metal with high reactivity and stereoselectivity, and thus represents a good application outlook. The ligand of the present invention has the formula of: wherein: n=5, 6, 7, 8, 9, 10, 11 or 12; R1=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R2=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R3=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R4=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl.Type: ApplicationFiled: December 29, 2006Publication date: June 18, 2009Applicant: SHANGHAI JIAOTONG UNIVERSITYInventors: Wanbin Zhang, Yongjian Zhang, Feijun Wang
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Patent number: 7538228Abstract: A chiral ligand represented by the formula and its enantiomer: wherein A, X, Y and Z are as defined in the specification is provided. Also provided is a process of making the chiral ligands and catalysts prepared from these ligands and a transition metal, a salt thereof or a complex thereof. In addition, a method of preparing an asymmetric compound by a transition metal catalyzed asymmetric reaction, such as, hydrogenation, hydride transfer reaction, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, allylic alkylation, epoxidation, cyclopropanation, Diels-Alder reaction, Aldol reaction, ene reaction, Heck reaction and Michael addition is provided.Type: GrantFiled: December 17, 2004Date of Patent: May 26, 2009Assignee: The Penn State Research FoundationInventors: Xumu Zhang, Duan Liu
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Publication number: 20090043104Abstract: The present invention relates to a method for preparing 2,2?,6,6?-tetraoxazolinyl biphenyl ligand in chemical industry field. In the present invention, compound (III) is reacted with an activator that can activate the hydroxyl group selected from the group consisting of alkyl halosulfonium compound, aryl halosulfonium compound, phosphoryl chloride, phosphorus pentachloride, thionyl chloride and triphenyl phosphine, in the presence of alkali(s), to give the target product (IV), 2,2?,6,6?-tetraoxazolinyl biphenyl ligand. The ligand of the present invention can be used in various asymmetric reactions catalyzed by metals, with high reactivity and stereoselectivity, and thus represents a good application outlook.Type: ApplicationFiled: December 29, 2006Publication date: February 12, 2009Applicant: SHANGHAI JIAOTONG UNIVERSITYInventors: Wanbin Zhang, Yongjian Zhang, Feijun Wang
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Publication number: 20090012070Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)=C(R7)N(R8)-, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)=C(R12)C(R13)=C(R14) 112, -, where R, R, R6, R7, R8, R11, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: August 22, 2008Publication date: January 8, 2009Applicant: Bayer Cropscience AGInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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PROCESS FOR PREPARING OXAZOLINE-PROTECTED AMINODIOL COMPOUNDS USEFUL AS INTERMEDIATES TO FLORFENICOL
Publication number: 20080319200Abstract: A method of preparing oxazoline-protected aminodiol compounds is disclosed. These compounds are useful intermediates in processes for preparing Florfenicol and related compounds.Type: ApplicationFiled: May 28, 2008Publication date: December 25, 2008Inventor: JAMES C. TOWSON -
Publication number: 20080207913Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.Type: ApplicationFiled: April 27, 2007Publication date: August 28, 2008Applicant: Intezyne TechnologiesInventors: Kurt Breitenkamp, Kevin N. Sill, Habib Skaff
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Publication number: 20080194782Abstract: A solid, hydrocarbon-insoluble, catalyst component useful in polymerizing olefins containing magnesium, titanium, and halogen further contains an internal electron donor comprising a compound containing electron donating substituents with a structure: wherein D1 and D2 are selected individually from and R, R2, R3, R4, R5, R6, and R7 individually are hydrocarbon or substituted hydrocarbon groups containing 1 to 20 carbon atoms and R2, R3, R4, R6, and R7 may be hydrogen; R4 may be —NR2; and wherein groups R1 and R2, R2 and R3, R3 and R4, R3 and R5, and groups R6 and R7 may be joined to form a cyclic structure.Type: ApplicationFiled: April 1, 2008Publication date: August 14, 2008Inventors: Roger Uhrhammer, John P. Lalka
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Patent number: RE46129Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: GrantFiled: January 10, 2014Date of Patent: August 30, 2016Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G Harran, Xiaodong Wang, Jef K. DeBrabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki