Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Azide Group Patents (Class 552/6)
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Publication number: 20120264901Abstract: The present invention relates to a compound with the following formula (I) where: R1 is particularly a straight or branched alkyl group, a is a single or double bond; R2 is particularly a hydrogen atom; R3 and R5 are a hydrogen atom when a is a single bond, and absent when a is a double bond; R4 is a hydrogen atom or an ORb group, where Rb is a hydrogen atom or an alkyl group including 1 to 12 atoms of carbon, and A1 is a divalent alkylene radical.Type: ApplicationFiled: October 15, 2010Publication date: October 18, 2012Applicant: Centre National De La Recherche Scientifique (C.N.R.S.)Inventors: Henri Cramail, Aurelie Boyer, Dnyaneshwar Palaskar, Eric Cloutet, Carine Alfos
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Publication number: 20120238767Abstract: Disclosed herein are novel oleanolic acid derivatives. Methods of preparing these compounds are also disclosed. The oleanolic acid derivatives of this invention may be used for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.Type: ApplicationFiled: November 11, 2011Publication date: September 20, 2012Inventors: Xin Jiang, Jack Greiner, Lester L. Maravetz, Stephen S. Szucs, Melean Visnick
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Publication number: 20120130097Abstract: The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.Type: ApplicationFiled: January 30, 2012Publication date: May 24, 2012Applicant: AstraZeneca ABInventors: Adrian Clark, Elfyn Jones, Ulf Larsson, Anna Minidis
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Patent number: 8003771Abstract: The present invention relates to compositions useful as probes and in other applications and methods of their use. In some embodiments, nucleotides are prepared and functionalized with dyes. In some embodiments a first molecule is functionalized with an alkynyl group, a second molecule is functionalized with an azide group, and said first and second molecules are mixed under conditions to form a conjugate with a 1,2,3-triazol group. In further embodiments, a nucleotide is functionalized with an alkynyl group, a dye is functionalized with an azide group, and mixing the nucleotide and the dye forms a conjugate capable of emitting light.Type: GrantFiled: March 1, 2010Date of Patent: August 23, 2011Assignee: Third Wave Technologies, Inc.Inventors: Zbigniew Skrzypczynski, Sarah R Wayland
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Publication number: 20110190520Abstract: The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.Type: ApplicationFiled: February 8, 2011Publication date: August 4, 2011Applicant: AstraZeneca ABInventors: Adrian Clark, Elfyn Jones, Ulf Larsson, Anna Minidis
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Publication number: 20110178316Abstract: Fullerene compounds represented by the formulae Cm[C(R)CON3]n, Cm[C(R)NCO]n, Cm[C(R)NHCORd]n, and Cm[C(R)NH2]n, wherein Cm represents a fullerene moiety having m carbon atoms, m represents an even integer from about 60 to about 200, n represents an integer of about 1 or more, R represents an electron-withdrawing group, and Rd represents an alkoxy or alkylamino group. In addition, processes for preparing these fullerene compounds involving reacting an acyl azide with a fullerene in the presence of a base.Type: ApplicationFiled: July 28, 2009Publication date: July 21, 2011Applicant: Luna Innovations IncorporatedInventor: Jing Zhang
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Publication number: 20110082302Abstract: Disclosed are a process suited to large scale synthesis with high yield for producing oseltamivir phosphate, in which a preparation of oseltamivir phosphate which is highly safe as a pharmaceutical product can be produced, and an intermediate compound for producing oseltamivir phosphate. In this production process, an intermediate compound represented by general formula (V) is synthesized by employing Michael reaction/Michael reaction/Horner-Wadsworth-Emmons reaction, and oseltamivir phosphate is produced by converting the substituent groups in this intermediate compound.Type: ApplicationFiled: May 28, 2009Publication date: April 7, 2011Inventors: Yujiro Hayashi, Hayato Ishikawa
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Patent number: 7906662Abstract: The compounds trans-(1R,2R)-2-(3,4-difluorophenyl)cyclopropanecarbonyl azide and trans-(1R,2S)-2-(3,4-difluorophenyl)cyclopropanaminium (2R)-2-hydroxy-2-phenylethanoate.Type: GrantFiled: July 17, 2006Date of Patent: March 15, 2011Assignee: Astrazeneca ABInventors: Adrian Clark, Elfyn Jones, Ulf Larsson, Anna Minidis
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Patent number: 7674924Abstract: The present invention relates to compositions useful as probes and in other applications and methods of their use. In some embodiments, nucleotides are prepared and functionalized with dyes. In some embodiments a first molecule is functionalized with an alkynyl group, a second molecule is functionalized with an azide group, and said first and second molecules are mixed under conditions to form a conjugate with a 1,2,3-triazol group. In further embodiments, a nucleotide is functionalized with an alkynyl group, a dye is functionalized with an azide group, and mixing the nucleotide and the dye forms a conjugate capable of emitting light.Type: GrantFiled: May 22, 2007Date of Patent: March 9, 2010Assignee: Third Wave Technologies, Inc.Inventors: Zbigniev Skrzypczynski, Sarah R. Wayland
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Patent number: 7605191Abstract: The invention provides a photosensitive resin which can readily form, through photo-crosslinking, a surface coating which has hydrophilicity and high bioadaptability; a photosensitive composition containing the photosensitive resin; and a photo-crosslinked structure obtained from the photosensitive composition.Type: GrantFiled: March 31, 2006Date of Patent: October 20, 2009Assignee: Toyo Gosei Co., Ltd.Inventors: Takeshi Ikeya, Toru Shibuya, Kana Miyazaki
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Publication number: 20090069448Abstract: In one embodiment of the present invention, a degradable polymer having a peroxide bond therein is disclosed. The degradable polymer can be utilized in the fields of medicals or medical materials, can be applied to a DDS or gene delivery system, and can be used as a novel polymeric material or environmentally-friendly material. A polyperoxide, which is an alternating copolymer, has in a side chain thereof, a functional group (which is a substituent comprising a therapeutic molecule), a water-soluble substituent, or a biodegradable substituent.Type: ApplicationFiled: May 8, 2006Publication date: March 12, 2009Inventor: Akikazu Matsumoto
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Publication number: 20080306292Abstract: Provided are syntheses of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin via a chiral intermediate of the following formula 4 wherein Ar is a C6-10 aromatic group, R is a straight or branched C1-4 alkyl, ester, or carboxylic acid, and R1 is a straight or branched C1-5 alkyl, aralkyl, or substituted aralkyl.Type: ApplicationFiled: March 24, 2008Publication date: December 11, 2008Inventors: Vinod Kumar Kansal, Brijnath P. Chaurasia, Anand Prakash Tiwari, Shivaji Haribhau Shelke
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Patent number: 7335792Abstract: The invention relates to novel diazoketone derivatives. The invention also relates to processes for homologation of these diazoketone derivatives. The processes are useful for preparing compounds that are caspase inhibitors.Type: GrantFiled: October 9, 2002Date of Patent: February 26, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Oliver Philps, John Studley
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Patent number: 6861456Abstract: The present invention provides a novel photosensitive compound having an azido group suitable for exposure to light of a short wavelength; a photosensitive resin containing the photosensitive compound; and a photosensitive composition containing the photosensitive compound or photosensitive resin. The photosensitive compound containing a photosensitive unit represented by formula (1): wherein R is selected from among the following groups, R: X is selected from among the following groups, X: and each of Y and Z represents a hydrogen atom, an alkyl group, an acetal-group-containing alkyl group, an aryl group, an aralkyl group, or a substituent containing a base-forming nitrogen atom, wherein at least one of R and X contains an azido group.Type: GrantFiled: March 27, 2003Date of Patent: March 1, 2005Assignee: Toyo Gosei Kogyo Co., Ltd.Inventors: Toru Shibuya, Masanori Kurihara, Mineko Takeda, Kazuo Yamada
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Patent number: 6846946Abstract: A method for preparing organic products from aqueous solutions, such as waste or byproduct liquid streams and waste or byproduct gas or vapor streams, uses phase transfer catalysis to transfer a chemical species in low concentration from the aqueous solution to the organic phase or the aqueous-organic interface. The system has little or no organic solvent, and the organic phase contains an electrophile which participates in the reaction. In one embodiment, the aqueous solution is contacted with the electrophile and a phase transfer catalyst and, optionally, a pH adjusting agent in the event that the chemical species in the aqueous solution is not sufficiently ionized to react with the electrophile, and optionally an organic solvent. A method for continuously converting a chemical species involves this contacting step, separating the phases, then dividing the organic phase into the product, the phase transfer catalyst, and the optional organic solvent.Type: GrantFiled: September 6, 2002Date of Patent: January 25, 2005Assignee: Value Recovery, Inc.Inventors: Peter J. Joyce, Roman Bielski, Marc Halpern
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Publication number: 20040127697Abstract: Novel arylisothiocyanate compounds are described that are useful for activating alcohol-containing macromolecules, for example polyethyleneglycols and cellulose, for covalent linkage to amino-groups of biomolecules, for example polypeptides such as antibodies, enzymes, and proteins.Type: ApplicationFiled: December 19, 2003Publication date: July 1, 2004Inventor: Paul K. Smith
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Patent number: 6737524Abstract: Novel arylisothiocyanate compounds are described that are useful for activating alcohol-containing macromomolecules, for example polyethyleneglycols and cellulose, for covalent linkage to amino-groups of biomolecules, for example polypeptides such as antibodies, enzymes, and proteins.Type: GrantFiled: March 25, 2002Date of Patent: May 18, 2004Inventor: Paul K. Smith
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Publication number: 20030187248Abstract: Novel arylisothiocyanate compounds are described that are useful for activating alcohol-containing macromolecules, for example polyethyleneglycols and cellulose, for covalent linkage to amino-groups of biomolecules, for example polypeptides such as antibodies, enzymes, and proteins.Type: ApplicationFiled: March 25, 2002Publication date: October 2, 2003Inventor: Paul K. Smith
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Publication number: 20030045725Abstract: A method for the production of substituted aromatic aldehydes or ketones and optionally substituted heteroaromatic aldehydes or ketones of formula (I) by reacting a compound of formula (II) in a suitable solvent in the presence of a carbonyl compound of formula (III), optionally in the presence of oxygen at a normal pressure or high temperature and at temperatures of 5-200° C.Type: ApplicationFiled: September 20, 2002Publication date: March 6, 2003Inventors: Wolfram Hendel, Ferdinand Heu, Peter Poechlauer, Berthold Winkler
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Patent number: 5132432Abstract: The invention relates to novel fluorescent dyes based on the following pyrenyloxy sulfonic acid structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is --OCH.sub.2 C(O)OCH.sub.3, --OCH.sub.2 CON(O)H, --OCH.sub.2 CON.sub.3, --OCH.sub.2 CONHNH.sub.2, ##STR2## or --CH.sub.2 CONH(CH.sub.2).sub.n NH.sub.2 where n is an integer from 1 to 10; at least one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is sulfonic acid or alkali salts of sulfonic acid; and all other of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydrogen or a hydroxyl group. The new reagents contain functional groups typically found in biomolecules or polymers. The spectral properties of the fluorescent dyes are sufficiently different in wavelengths and intensity from fluorescein as to permit simultaneous use of both dyes with minimum interference.Type: GrantFiled: September 22, 1989Date of Patent: July 21, 1992Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, James E. Whitaker
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Patent number: 5021602Abstract: Novel compounds have at least one perfluorocyclobutane ring and at least two functional groups suitable for forming condensation polymers. Preferably the compounds have a structures represented by Formula II: ##STR1## wherein R and R' independently represent optionally inertly substituted groups; X and X' represent any molecular structures which link R and R' with the perfluorocyclobutane ring; n and n' are the number of G and G' groups, respectively; and G and G' independently represent any reactive functional groups or any groups convertible into reactive functional groups. The compound are preferably prepared by a process of thermally dimerizing trifluorovinyl compound to form a compounds of Formula IG.sub.n --R--X--CF.dbd.CF.sub.2wherein G represents G or G' in Formula II; X represents X or X' of Formual II; and n represents n or n' of Formula II, to form a compound having a perfluorocyclobutane group.Type: GrantFiled: June 9, 1989Date of Patent: June 4, 1991Assignee: The Dow Chemical CompanyInventors: Katherine S. Clement, David A. Babb, Bobby R. Ezzell
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Patent number: 4857660Abstract: 1-Phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.Type: GrantFiled: April 22, 1988Date of Patent: August 15, 1989Assignee: Ciba-Geigy CorporationInventors: Alex Alder, Jaroslav Stanek, Daniel Bellus