Bicyclo Ring System Patents (Class 568/819)
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Publication number: 20150125892Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.Type: ApplicationFiled: October 10, 2014Publication date: May 7, 2015Applicant: SynAffix B.V.Inventors: Floris Louis VAN DELFT, Floris Petrus Johannes Theodorus Rutjes, Frederik Jan Dommerholt
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Patent number: 8993809Abstract: A process for isolating at least one target compound, such as manool, geranyl linalool, ethyl guaiacol, eugenol, veratraldehyde, squalene, terpin, cholesterol, beta-sitosterol, campesterol, stigmasterol, stigmastenol and dehydroabietic acid, from biomass, the process including steps of: obtaining a condensate from a recovery evaporator, a reverse osmosis retentate of a condensate of a pulp and paper mill, or both, the condensate, retentate or both being substantially free of higher molecular weight (approximately >1000 Da) cellulose and/or lignin and/or lignin-derived material; optionally pH adjusting and filtering the condensate to collect insoluble material; extracting the condensate, the collected insoluble material, or both, with solid phase extraction (SPE), liquid-liquid extraction or solid-liquid extraction to produce an extract containing the at least one target compound; and optionally purifying the extract containing the at least one target compound by thermal fractionation, chromatographic separType: GrantFiled: April 7, 2011Date of Patent: March 31, 2015Assignee: Her Majesty the Queen in Right of Canada, as Represented by the Minister of EnvironmentInventors: Craig Brennan Milestone, Deborah L. MacLatchy, L. Mark Hewitt
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Publication number: 20150017227Abstract: Disclosed are methods and compositions for treating skin diseases or conditions with a composition containing a lipid component as an active ingredient.Type: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Inventors: Byung Eui Kim, Donald Y.M. Leung
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Patent number: 8927594Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.Type: GrantFiled: March 15, 2011Date of Patent: January 6, 2015Assignees: National Sun Yat-Sen University, National Museum of Marine Biology & AquariumInventors: Jyh-Horng Sheu, Wei-Hsien Wang, Zhi-Hong Wen, Bo-Wei Chen, Ping-Jyun Sung
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Patent number: 8883468Abstract: (3S,5R)-3,8-dimethyl-5-(prop-1-en-2-yl)-octahydroazulen-1-ols, their use as flavor or fragrance ingredient, and a process of their production by oxidation in the presence of laccase.Type: GrantFiled: June 28, 2011Date of Patent: November 11, 2014Assignee: Givaudan S.A.Inventors: Boris Schilling, Thierry Granier, Esther Locher
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Publication number: 20140309300Abstract: The present invention relates to bicyclic labdane diterpenes for use in the treatment of a disease associated with activation of transient receptor potential cation channel 6 (TRPC6), preferably a pulmonary or a renal disease. In one aspect the invention relates to the use of a bicyclic labdane diterpene for blocking calcium transport via TRPC6. Another aspect of the invention is a bicyclic labdane diterpene according to formula (1) for use as a medicament wherein R1 is selected from hydrogen and C1 to C4 acyl, wherein the bicyclic labdane diterpene optionally comprises at least one double bond between the carbon atoms at positions 1 and 2, 2 and 3, 5 and 6, 6 and 7 and/or 14 and 15, wherein the carbon atoms at positions 1, 2, 3, 7, 11, 12, 13, 14, 15, 16, 17, 18, 19 or 20 are connected to hydrogen atoms or comprise at least one substitution.Type: ApplicationFiled: August 10, 2012Publication date: October 16, 2014Applicant: UNIVERSITAET LEIPZIGInventors: Michael Schaefer, Nicole Urban, Wolfgang Kuebler
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Patent number: 8859629Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.Type: GrantFiled: April 26, 2011Date of Patent: October 14, 2014Assignee: Synaffix B.V.Inventors: Floris Louis van Delft, Floris Petrus Johannes Theodorus Rutjes, Frederik Jan Dommerholt
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Publication number: 20140256782Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic is visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.Type: ApplicationFiled: October 19, 2012Publication date: September 11, 2014Applicant: Bikam Pharmaceuticals, Inc.Inventors: David S. Garvey, Gregory J. Larosa, Jeremy R. Greenwood, Leah L. Frye, Tan Quach, Jamie B. Cote, Judd Berman
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Publication number: 20140171498Abstract: This invention relates to diterpenes of general formula (1) belonging to labdane class, isolated from Leucas stelligera, being useful for prevention, treatment, inhibition or controlling growth and proliferation of mycobacterial activity in mammals. The invention further discloses process for isolation of the fractions containing the same.Type: ApplicationFiled: August 6, 2012Publication date: June 19, 2014Applicant: Council of Scientific & Indusrtial ReasearchInventors: Swati Joshi, Roshan Rajan Kulkarni, Ketaki Dilip Shurpali, Sampa Sarkar, Dhiman Sarkar
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Patent number: 8716456Abstract: The present invention relates to per-substituted pentalene compounds, including permethylpentalene and precursors thereof. In particular, the invention provides substituted pentalene compounds and methods of preparing substituted pentalene compounds; complexes of metals with substituted pentalene compounds and methods for their production; and the use of complexes of metals with substituted pentalene compounds in catalysis.Type: GrantFiled: March 10, 2008Date of Patent: May 6, 2014Assignee: Isis Innovation LimitedInventors: Dermot Michael O'Hare, Andrew Edward Ashley
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Patent number: 8664206Abstract: Compounds of formula I are provided where X1, X2, and X3 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.Type: GrantFiled: January 6, 2012Date of Patent: March 4, 2014Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Agnieszka Flores, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame, James B. Thoden, Hazel M. Holden
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Patent number: 8614345Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of specific ruthenium catalysts, or pre-catalysts, in hydrogenation processes for the reduction of ketones and/or aldehydes into the corresponding alcohol respectively. Said catalysts are ruthenium complexes comprising a tetradentate ligand (L4) coordinating the ruthenium with: —two nitrogen atoms, each in the form of a primary or secondary amine (i.e. a NH2 or NH group) or N-alkyl imine functional groups (i.e. a C?N group), and —two sulfur atoms, each in the form of thioether functional groups.Type: GrantFiled: December 19, 2011Date of Patent: December 24, 2013Assignee: Firmenich SAInventors: Francesco Santoro, Lionel Saudan, Michel Alfred Joseph Saudan, Sylvia Joyeuse Adélaïde Ada Saudan
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Publication number: 20130331459Abstract: Disclosed are 19-nor-vitamin D compounds, and specifically seco-A-2,19-dinor-1,25-dihydroxyvitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high activity in vivo, specifically in intestinal tissues, but relatively low VDR binding activity, cell differentiation activity and gene transcription activity. There is thus potential for these compounds to have strong cell selectivity for use as therapeutic agents against some cancers, such as colon cancer or polyps, as well as hyperplastic intestinal disorders, such as Crohn's disease, ulcerative colitis and celiac disease. These compounds also have relatively high intestinal calcium transport activity evidencing potential in the treatment of bone diseases.Type: ApplicationFiled: March 14, 2013Publication date: December 12, 2013Applicant: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Agnieszka Glebocka
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Publication number: 20130324752Abstract: Disclosed are methods of purifying the compound (20R,22R)-2-methylene-19-nor-22-methyl-1?,25-dihydroxyvitamin D3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals. Certain diol precursors formed during the synthesis of the compound and its diasteromers also may be obtained in crystalline form using ethyl acetate as a solvent.Type: ApplicationFiled: March 14, 2013Publication date: December 5, 2013Inventors: Hector F. DeLuca, Pawel Grzywacz, Lori A. Plum, Agnieszka Flores, James B. Thoden, Hazel M. Holden
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Publication number: 20130274487Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of specific ruthenium catalysts, or pre-catalysts, in hydrogenation processes for the reduction of ketones and/or aldehydes into the corresponding alcohol respectively. Said catalysts are ruthenium complexes comprising a tetradentate ligand (L4) coordinating the ruthenium with: two nitrogen atoms, each in the form of a primary or secondary amine (i.e. a NH2 or NH group) or N-alkyl imine functional groups (i.e. a C?N group), and two sulfur atoms, each in the form of thioether functional groups.Type: ApplicationFiled: December 19, 2011Publication date: October 17, 2013Applicant: FIRMENICH SAInventors: Sylvia Joyeuse Adélaïde Ada Saudan, Michel Alfred Joseph Saudan
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Publication number: 20130210904Abstract: Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.Type: ApplicationFiled: August 15, 2012Publication date: August 15, 2013Inventors: Jeremy E. Wulff, Michael G. Brant, Jeremy W. Mason, Caleb M. Bromba, Martin J. Boulanger
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Patent number: 8481013Abstract: Sandalwood perfuming ingredients that are 2-[perhydro-trialkyl-2-naphthalenylidene]-1-propanol or propanal derivatives of the formula wherein one dotted line represents a carbon-carbon single bond and the other a carbon-carbon single bond or double bond; X represents a CH2OH group or a CHO group; each R1 represents a hydrogen atom or a methyl group; and the R2, taken separately, represent each a hydrogen atom or the two R2 groups, taken together, represent a CH2 group or a carbon-carbon double bond; and said compound is in the form of any one of its stereoisomers or a mixture thereof, along with the use of such compound(s) in perfuming compositions or articles in the perfumery industry.Type: GrantFiled: November 18, 2009Date of Patent: July 9, 2013Assignee: Firmenich SAInventor: Christian Chapuis
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Publication number: 20130137763Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.Type: ApplicationFiled: April 26, 2011Publication date: May 30, 2013Inventors: Floris Louis van Delft, Floris Petrus Johannes Theodorus Rutjes, Frederik Jan Dommerholt
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Patent number: 8450533Abstract: A method for the preparation of cyclopropyl carbinols by cyclopropanation of unsaturated alcoholates, utilizing a reagent system selected from (A) magnesium metal and dibromomethane, and (B) dibromomethane and a tertiary Grignard reagent, the reaction being carried out in the presence of an ether solvent. The process is useful, for example, for the preparation of ingredients for the flavor and fragrance industry.Type: GrantFiled: August 19, 2008Date of Patent: May 28, 2013Assignee: Givaudan SAInventor: Fridtjof Schroder
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Publication number: 20130089904Abstract: (3S,5R)-3,8-dimethyl-5-(prop-1-en-2-yl)-octahydroazulen-1-ols, their use as flavour or fragrance ingredient, and a process of their production by oxidation in the presence of laccase.Type: ApplicationFiled: June 28, 2011Publication date: April 11, 2013Applicant: GIVAUDAN S.A.Inventors: Boris Schilling, Thierry Granier, Esther Locher
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Publication number: 20130072724Abstract: A process for isolating at least one target compound, such as manool, geranyl linalool, ethyl guaiacol, eugenol, veratraldehyde, squalene, terpin, cholesterol, beta-sitosterol, campesterol, stigmasterol, stigmastenol and dehydroabietic acid, from biomass, the process including steps of: obtaining a condensate from a recovery evaporator, a reverse osmosis retentate of a condensate of a pulp and paper mill, or both, the condensate, retentate or both being substantially free of higher molecular weight (approximately >1000 Da) cellulose and/or lignin and/or lignin-derived material; optionally pH adjusting and filtering the condensate to collect insoluble material; extracting the condensate, the collected insoluble material, or both, with solid phase extraction (SPE), liquid-liquid extraction or solid-liquid extraction to produce an extract containing the at least one target compound; and optionally purifying the extract containing the at least one target compound by thermal fractionation, chromatographic separType: ApplicationFiled: April 7, 2011Publication date: March 21, 2013Applicant: Her Majesty The Queen in the Right of Canada, as Represented by the Minister of EnvironmentInventors: Craig Brennan Milestone, Deborah L. MacLatchy, L. Mark Hewitt
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Patent number: 8309511Abstract: The present invention is directed to novel fragrance compounds and their unexpected advantageous use in enhancing, improving or modifying a fragrance formulation through the addition of an olfactory acceptable amount of the compounds, wherein the compounds are represented by the following formula: wherein a methyl group is bonded to the 5-membered ring at position 2 or 3, or a mixture thereof.Type: GrantFiled: May 22, 2012Date of Patent: November 13, 2012Assignee: International Flavors & Fragrances Inc.Inventors: Richard A. Weiss, Anubhav P. S. Narula, James Anthony Lasome, Richard M. Boden
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Publication number: 20120270901Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: December 8, 2011Publication date: October 25, 2012Applicant: Aquinox Pharmaceuticals Inc.Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
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Patent number: 8269048Abstract: The present invention refers to a method for allylic catalytic oxidation to obtain ?,?-unsaturated ketones and alcohols from bicyclic compounds reacted with oxygen and catalysts comprising metal-organic compounds and gold nanoparticles. The present invention also relates to a method for the preparation of fragrances using the above methods or products of the above method.Type: GrantFiled: September 23, 2010Date of Patent: September 18, 2012Assignee: International Flavors & Fragrances Inc.Inventors: Onofre Casanova Navarro, Avelino Corma Canós, Sara Iborra Jornet
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Patent number: 8227629Abstract: The present invention concerns a process for the preparation of a compound of formula (I), wherein the dotted line is a single bond and n is 1 or the dotted line is a double bond and n is 0, and wherein the relative configuration is as shown, in the form of any one of its diastereoisomers or enantiomers or mixtures thereof.Type: GrantFiled: October 20, 2008Date of Patent: July 24, 2012Assignee: Firmenich SAInventor: Charles Fehr
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Patent number: 8227630Abstract: The present invention concerns a process for the preparation of a compound of formula (I) wherein the dotted line is a single bond and n is 1 or the dotted line is a double bond and n is 0, and wherein the relative configuration is as shown, in the form of any one of its diastereoisomers or enantiomers or mixtures thereof.Type: GrantFiled: October 20, 2008Date of Patent: July 24, 2012Assignee: Firmenich SAInventor: Charles Fehr
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Publication number: 20120165300Abstract: Compounds of formula I are provided where X1, X2, and X3 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.Type: ApplicationFiled: January 6, 2012Publication date: June 28, 2012Inventors: Hector F. DeLUCA, Agnieszka FLORES, Pawel GRZYWACZ, Lori A. PLUM, Margaret CLAGETT-DAME, James B. THODEN, Hazel M. HOLDEN
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Publication number: 20120130133Abstract: Processes for preparing vitamin D2 derivatives and intermediates to vitamin D2 derivatives are disclosed. An improved photolysis process for the preparation of cis intermediate (I) from the trans starting material (II) are disclosed. Also disclosed is an improved process for the formation of a trans double bond at C22-C23 of the vitamin D2 derivative, which provides high selectivity of the desired trans double bond of compound (III) over the undesired cis double bond of compound (IIIA).Type: ApplicationFiled: November 25, 2009Publication date: May 24, 2012Applicant: CYTOCHROMA INC.Inventor: Uttam Saha
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Patent number: 8173824Abstract: There are provided a novel process for producing [{(5Z,7E)-(1S,3R,20S)-1,3-dihydroxy-9,10-secopregna-5,7,10(19),16-tetraen-20-yl}oxy]-N-(2,2,3,3,3-pentafluoropropyl)acetamide, which process is shown in the following reaction scheme: an intermediate useful for carrying out the process, and a process for producing the intermediate.Type: GrantFiled: December 4, 2006Date of Patent: May 8, 2012Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Kunio Ogasawara, Takashi Emura, Akira Kawase, Koji Takano, Keisuke Yamamoto, Yoshiaki Kato
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Publication number: 20120077992Abstract: The present invention relates to a device for treatment of material transported through the device comprising at least one porous element consisting of solid, for example metallic, structure which allows cross-flow of the material through the porous element. The invention also relates to various types of uses of the device. A device in accordance with the invention is particularly useful to carry out chemical reactions under homogenous and heterogeneous conditions. Such a device hereinafter also referred as reactor may comprises a tube (1) having a cylindrical wall (2) with one inlet end (3) and one outlet end (4). Arranged in the tube (1) is at least one cylindrical porous element (5) consisting of solid metal structure, wherein said porous element (5) comprises a plurality of hollow spaces that are connected to each other and form an interconnected cavity network and wherein the at least one porous element (5) and the cylindrical wall (2) are made in one piece.Type: ApplicationFiled: June 14, 2010Publication date: March 29, 2012Inventors: Cédric Hutter, Francesco Mascarello, Philipp Von Rohr, David Ruppen
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Publication number: 20120058977Abstract: A pharmaceutical composition for the treatment of a disease caused by a bacterium that belongs to the group of nocardioform actinomycetes, said composition comprising an effective amount of a compound selected from compound I, (+)-compound II, (?)-compound II, compound III, or mixtures thereof.Type: ApplicationFiled: February 23, 2010Publication date: March 8, 2012Applicant: Rijksuniversiteit GroningenInventors: Robert Van Der Geize, Lubbert Dijkhuizen, Martin Ostendorf, Peter Van Der Meijden
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Publication number: 20120028957Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.Type: ApplicationFiled: August 1, 2010Publication date: February 2, 2012Inventors: William F. DeGrado, Jun Wang
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Publication number: 20110311469Abstract: The present invention relates to certain derivatives of 2-ethyl-4-(2?,2?-dimethyl-3?-alkyl-3?-cyclopenten-1?-yl)-4-penten-1-ol. These compounds possess very interesting perfuming ingredients due to their unusual combination of sandalwood and floral notes. The present invention also concerns the use of such compounds in the perfumery industry as well as the compositions or articles containing such compounds.Type: ApplicationFiled: March 19, 2010Publication date: December 22, 2011Inventors: Hervé Pamingle, Christian Chapuis, Peter Fankhauser, Piero Fantini
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Publication number: 20110294764Abstract: Compounds of formula I are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.Type: ApplicationFiled: November 29, 2010Publication date: December 1, 2011Inventors: Hector F. DeLuca, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20110218347Abstract: The present invention concerns a process for the preparation of a compound of formula (I) wherein the dotted line is a single bond and n is 1 or the dotted line is a double bond and n is 0, and wherein the relative configuration is as shown, in the form of any one of its diastereoisomers or enantiomers or mixtures thereof.Type: ApplicationFiled: October 20, 2008Publication date: September 8, 2011Inventor: Charles Fehr
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Patent number: 8013176Abstract: Paricalcitol, a synthetic vitamin D analog, is purified to a purity greater than 99.7% by crystallization from solution in isopropyl acetate solvent, followed by filtration and vacuum drying. Isopropyl acetate appears to be unique among commonly available and pharmaceutically acceptable solvents in its ability to precipitate paricalcitol in this high purity, essentially free of isomers thereof. In addition, paricalcitol of purity of at least 99.9% has been shown to have exceptional storage stability.Type: GrantFiled: August 19, 2009Date of Patent: September 6, 2011Assignee: Alphora Research Inc.Inventors: Fabio Eduardo Silva e Souza, Ming Pan, Kathleen Da Silva Turcot
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Publication number: 20110195038Abstract: Sandalwood perfuming ingredients that are 2-[perhydro-trialkyl-2-naphthalenylidene]-1-propanol or propanal derivatives of the formula wherein one dotted line represents a carbon-carbon single bond and the other a carbon-carbon single bond or double bond; X represents a CH2OH group or a CHO group; each R1 represents a hydrogen atom or a methyl group; and the R2, taken separately, represent each a hydrogen atom or the two R2 groups, taken together, represent a CH2 group or a carbon-carbon double bond; and said compound is in the form of any one of its stereoisomers or a mixture thereof, along with the use of such compound(s) in perfuming compositions or articles in the perfumery industry.Type: ApplicationFiled: November 18, 2009Publication date: August 11, 2011Inventor: Christian Chapuis
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Patent number: 7973200Abstract: The invention relates to the use as perfuming ingredients of 8a-alkyl-perhydro-naphthalenol derivatives, to impart odor notes of the woody-earthy type.Type: GrantFiled: October 29, 2008Date of Patent: July 5, 2011Assignee: Firmenich SAInventors: Robert Moretti, Olivier Etter
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Publication number: 20110124924Abstract: A method for the preparation of cyclopropyl carbinols by cyclopropanation of unsaturated alcoholates, utilising a reagent system selected from (A) magnesium metal and dibromomethane, and (B) dibromomethane and a tertiary Grignard reagent, the reaction being carried out in the presence of an ether solvent. The process is useful, for example, for the preparation of ingredients for the flavour and fragrance industry.Type: ApplicationFiled: August 19, 2008Publication date: May 26, 2011Applicant: GIVAUDAN SAInventor: Fridtjof Schroder
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Publication number: 20110098350Abstract: Novel substituted cyclohexylidene-ethylidene-octahydro-indene compounds and compositions comprising the same are described. The compounds exhibit profound anti-proliferative effects, in comparison to other compounds known for their anti-cancer and anti-hyperproliferative ability. Methods of use of such compounds and compositions are described for treating a variety of cancers, inflammatory and other hyperproliferative diseases and disorders.Type: ApplicationFiled: June 16, 2009Publication date: April 28, 2011Inventors: Shimon Ben Shabat, Amnou Sintov
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Publication number: 20110086824Abstract: This invention discloses (20S,22E)-2-methylene-19-nor-22-ene-1?,25-dihydroxyvitamin D3 analogs, and specifically(20S,22E)-2-methylene-19-nor-22-ene-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits significant vitamin D receptor binding activity and transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent, especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.Type: ApplicationFiled: September 30, 2010Publication date: April 14, 2011Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Pawel Grzywacz, Lori A. Plum, Margaret Clagett-Dame
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Publication number: 20110082121Abstract: This invention discloses 1-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-1-desoxy-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Katarzyna M. Barycka, Izabela Sibilska, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki, Rafal R. Sicinski, Katarzyna Plonska-Ocypa
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Publication number: 20110082123Abstract: This invention discloses 6-methylvitamin D3 analogs, and specifically 1?,25-dihydroxy-6-methylvitamin D3, and pharmaceutical uses therefor. This compound exhibits vitamin D receptor binding activity and transcription activity as well as activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent, especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. This compound also exhibits low in vivo calcemic activity, but because it binds the receptor with the same affinity as the native hormone calcitriol, it may act as an antagonist to inhibit development of hypercalcemia.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Katarzyna Sokolowska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Antonio Mouriño
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Publication number: 20110082122Abstract: 19-nor-vitamin D analogs having an additional cyclopentene ring connecting carbon 1 and carbon 2, or connecting carbon 3 and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro activities, making them therapeutic agents for the treatment or prophylaxis of some types of cancers, particularly leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Agnieszka Glebocka, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski
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Publication number: 20110071320Abstract: The present invention refers to a method for allylic catalytic oxidation to obtain ?,?-unsaturated ketones and alcohols from bicyclic compounds reacted with oxygen and catalysts comprising metal-organic compounds and gold nanoparticles. The present invention also relates to a method for the preparation of fragrances using the above methods or products of the above method.Type: ApplicationFiled: September 23, 2010Publication date: March 24, 2011Inventors: Onofre Casanova Navarro, Avelino Corma Canós, Sara Iborra Jornet
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Patent number: 7902142Abstract: Provided is a fragrance composition containing 8- drimanol represented by the formula (Ia): and containing none of 7-acetyl-1,2,3,4,5,6,7,8-octahydro- 1,1,6,7-tetramethylnaphthalene, 1,2,3,4,4a,5,6,7-octahydro- 2,5,5-trimethyl-2-naphthalenol, 1,2,3,4,4a,7,8,8a- octahydro-2,4a,5,8a-tetramethyl-l-naphthylformate, 3a-ethyldodecahydro-6, 6,9a-trimethylnaphtho[2,1-b]furan, and racemic and optically-active substance of dodecahydro- 3a,6,6,9a-tetramethylnaphtho[2,1-b]furan; and personal care products, household products and environmental hygiene products containing the composition. The fragrance composition of the present invention contains 8-drimanol (Ia) so that it can produce various novel odors and emit a odor with softness and warmth typical to natural ambergris.Type: GrantFiled: July 24, 2006Date of Patent: March 8, 2011Assignee: Kao CorporationInventors: Kazuyuki Fukuda, Naotoshi Toki
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Publication number: 20110052707Abstract: We disclose compositions comprising Vitamin D (cholecalciferol and/or ergocalciferol) and 25-OH D3 (calcifediol), and use of those compositions to affect at least concentration, bioavailability, metabolism, or efficacy of vitamin D in a human. Forms and dosages of the composition, as well as processes for manufacturing a spray-dried formulation, are also disclosed.Type: ApplicationFiled: February 12, 2008Publication date: March 3, 2011Inventors: Neil Robert Buck, Wouter Claerhout, Bruno H. Leuenberger, Elisabeth Stoecklin, Kai Urban, Swen Wolfram
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Publication number: 20110009439Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: February 23, 2010Publication date: January 13, 2011Applicant: AQUINOX PHARMACEUTICALS INC.Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
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Publication number: 20100311990Abstract: The present invention concerns a process for the preparation of a compound of formula (I), wherein the dotted line is a single bond and n is 1 or the dotted line is a double bond and n is 0, and wherein the relative configuration is as shown, in the form of any one of its diastereoisomers or enantiomers or mixtures thereof.Type: ApplicationFiled: October 20, 2008Publication date: December 9, 2010Applicant: FIRMENICH SAInventor: Charles Fehr
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Patent number: 7834222Abstract: A process for the preparation of a the formula (I): which process comprises the intramolecular cyclopropanation of an epoxide of me formula (II); in the presence of 0.05 to 0.75 equivalents of a secondary amine base and at least one equivalent of an alkyl lithium base, wherein R R1, R2 and R3 are each hydrogen or C1-4 alkyl or R1 and R2 are linked to form- a C3-7 cycloaUcyl or C3-7 cycloalkenyl ring.Type: GrantFiled: August 1, 2006Date of Patent: November 16, 2010Assignee: Merck Sharp & Dohme Ltd.Inventors: Matthew Bio, Karel Marie Joseph Brands, Edward Cleator