The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 549/454)
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Publication number: 20100273968Abstract: The invention pertains to a process for preparing compounds of formula (I-A) or (I-B) here below: by reaction of perfluoroallylfluorosulfate (FAFS) of formula (II): with at least one hypofluorite of formula (II-A) or (II-B): wherein: RF in formulae (I-A) and (II-A) is a monovalent fluorocarbon C1-C20 group, optionally comprising oxygen catenary atoms, optionally comprising functional groups comprising heteroatoms (e.g. —SO2F groups); R?F in formulae (I-B) and (II-B) is a divalent fluorocarbon C1-C6 group, preferably a group of formula wherein X1 and X2, equal to or different from each other, are independently a fluorine atom or a C1-C3 fluorocarbon group. The FAFS-hypofluorite adducts of formulae (I-A) and (I-B) can be produced with high selectivity so as to access useful intermediates which can further be reacted taking advantage of the un-modified fluorosulfate group chemistry.Type: ApplicationFiled: December 17, 2008Publication date: October 28, 2010Applicant: SOLVAY SOLEXIS S.P.A.Inventors: Giuseppe Marchionni, Vito Tortelli
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Publication number: 20100222603Abstract: Glyceryl ether compounds prepared by the reaction of glycerol and olefin epoxides are disclosed. The compounds are renewable biomass-based surfactants useful as detergents and emulsifiers in formulations for cleaning, laundry, personal care, cosmetics, and industrial uses.Type: ApplicationFiled: November 22, 2006Publication date: September 2, 2010Inventor: Sergey Selifonov
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Publication number: 20100222286Abstract: The present invention provides therapeutically active compounds and compositions as NMDA and MC receptor antagonists, which are useful in preventing and treating central nervous system disorders by inhibiting over-activation of NMDA and/or MC receptors. In one aspect, the present invention provides methods of treating and/or preventing neurodegenerative diseases and neuropathological disorders, methods of providing neuroprotection under stress conditions such as a stroke, methods of enhancing the brain's cognitive functions and methods of treating depression, anxiety and cachexia induced by a chronic disease in mammals and humans.Type: ApplicationFiled: November 10, 2009Publication date: September 2, 2010Applicant: The Hong Kong University of Science & TechnologyInventors: Nancy Yuk-Yu Ip, Fanny Chui-Fun Ip, Yueqing Hu, Wen Cai Ye
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Patent number: 7763743Abstract: This invention is directed to compounds useful as intermediates in the synthesis of lipoxin A4 analogs of the following formulas (I) and (II): wherein R1, R2, R3, R4 and R5 are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.Type: GrantFiled: November 3, 2006Date of Patent: July 27, 2010Assignee: Bayer Schering Pharma AGInventors: Danja Grossbach, William Guilford, Michael Sander
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Publication number: 20100152457Abstract: A method whereby a compound having HCV replication inhibitory activity and desired optical activity can be synthesized selectively and at high yield in a small number of steps by using a compound having a specific chiral auxiliary as a starting compound is provided. A compound represented by the formula (1-8): wherein Y represents a group represented by the following formula: Q represents a protected carbonyl group; D represents —(CH2)m—R?, etc.; and n represents an integer of 0 to 10.Type: ApplicationFiled: February 4, 2010Publication date: June 17, 2010Inventors: Tatsuya Kato, Nobuaki Kimura, Akemi Mizutani, Toshihiko Makino, Kenichi Kawasaki, Hiroshi Fukuda, Susumu Komiyama, Takuo Tsukuda
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Publication number: 20100152456Abstract: A method whereby a compound having HCV replication inhibitory activity and desired optical activity can be synthesized selectively and at high yield in a small number of steps by using a compound having a specific chiral auxiliary as a starting compound is provided. A compound represented by the formula (1-8): wherein Y represents a group represented by the following formula: Q represents a protected carbonyl group; D represents —(CH2)m—R?, etc.; and n represents an integer of 0 to 10.Type: ApplicationFiled: February 4, 2010Publication date: June 17, 2010Inventors: Tatsuya Kato, Nobuaki Kimura, Akemi Mizutani, Toshihiko Makino, Kenichi Kawasaki, Hiroshi Fukuda, Susumu Komiyama, Takuo Tsukuda
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Publication number: 20100111888Abstract: Disclosed are compounds having the ability to modulate, namely to improve, enhance and or modify fragrance compositions due to their ability to inhibit cytochrome P450 enzymes, e.g. CYP2A13 and CYP2B6.Type: ApplicationFiled: March 20, 2008Publication date: May 6, 2010Applicant: GIVAUDAN SAInventors: Boris Schilling, Thierry Granier, Georg Frater, Andreas Hanhart
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Publication number: 20100113460Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.Type: ApplicationFiled: March 20, 2008Publication date: May 6, 2010Applicant: Givaudan SAInventors: Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart
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Patent number: 7709665Abstract: A fluorosulfonyl group-containing compound having a high polymerization reactivity, a process for its production, a sulfonyl group-containing polymerizable monomer led from the sulfonyl group-containing compound, and a polymer obtainable by polymerizing the sulfonyl group-containing polymerizable monomer, are provided. A compound (3) is fluorinated to form a compound (4), and then, the compound (4) is subjected to a decomposition reaction to produce a compound (5). A preferred compound (5-1) of the compound (5) is thermally decomposed to produce a compound (7-1) having a high polymerization reactivity. wherein RA is a bivalent organic group such as a fluoroalkylene group, RAF is a group having RA fluorinated, or the same group as RA, each of RB to RD which are independent of one another, is a hydrogen atom, etc., each of RBF to RDF is a fluorine atom, etc.Type: GrantFiled: July 27, 2007Date of Patent: May 4, 2010Assignee: Asahi Glass Company, LimitedInventors: Takashi Okazoe, Atsushi Watakabe, Masahiro Ito, Kunio Watanabe, Takeshi Eriguchi, Kimiaki Kashiwagi, Shu-zhong Wang
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Publication number: 20100048887Abstract: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: ApplicationFiled: April 20, 2009Publication date: February 25, 2010Inventors: Eric Anderson, Gary L. Bolton, Deborah A. Ferguson, Xin Jiang, Robert M. Kral, JR., Patrick M. O'Brien, Melean Visnick
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Patent number: 7655649Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 5, 2005Date of Patent: February 2, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
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Publication number: 20090311403Abstract: A method of using organic compounds and providing slow release flavoring in or for food products wherein flavor precursors are added to flavor compositions and/or food products and release flavor compounds upon consumption of the food products, and novel flavor precursor compounds. The flavor precursors can be prepared from monoglycerides and flavor compounds which comprise one or more carbonyl groups.Type: ApplicationFiled: July 24, 2007Publication date: December 17, 2009Applicant: Givaudan SAInventor: Willi Grab
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Publication number: 20090221811Abstract: The present invention provides processes for preparing intermediates useful in the preparation of gemcitabine and other nucleosides, and processes for preparing gemcitabine therewith. Exemplary intermediates include mixtures of D-erythro and D-threo isomers of 3-(hydroxy)-2,2-difluoro-3-(2,2-dimethyldioxolan-4-yl)-propionic acid salts. Also provided is a process for selectively isolating the D-erythro and D-threo isomers of D-erythro and D-threo isomers of 3-(hydroxy)-2,2-difluoro-3-(2,2-dimethyldioxolan-4-yl)-propionic acid salts, and processes for using such isomers in the preparation of nucleoside analogs such as, e.g., gemcitabine, intermediates thereof, and analogs thereof.Type: ApplicationFiled: April 27, 2009Publication date: September 3, 2009Applicant: CHEMAGIS LTD.Inventors: Vladimir NADDAKA, Eyal KLOPFER, Shady SAEED, Dionne MONTVILISKY, Oded ARAD, Joseph KASPI
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Publication number: 20090216009Abstract: An industrially easily realizable and economical process comprising only few steps, and built on new intermediates for the production of 1-(4-3(R)-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) according to the reaction scheme described herein.Type: ApplicationFiled: December 18, 2006Publication date: August 27, 2009Inventors: Jozsef Bodi, Janos Eles, Katalin Szoke, Krisztina Vukics, Tamas Gati, Krisztina Temesvari, Dorottya Kiss-Bartos
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Publication number: 20090163576Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, compound of the formula (I): wherein n is 1 or 2; m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; R3 and R4 together are alkyl having two or three carbon atoms; or R3 and R4 are the same as each other and each is methyl or ethyl; R5 is hydrogen or alkyl having from one to six carbon atoms.Type: ApplicationFiled: May 11, 2007Publication date: June 25, 2009Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, Reid W. von Borstel
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Publication number: 20090137393Abstract: The invention relates to novel 2,4,6-trialkylphenyl-substituted cyclopentane-1,3-diones of the formula (I) in which X, Y, A, B, Q1, Q2 and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the 2,4,6-trialkylphenyl-substituted cyclopentane-1,3-diones of the formula (I) and, secondly, at least one crop plant compatibility-improving compound.Type: ApplicationFiled: January 3, 2007Publication date: May 28, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Ulrich Gorgens, Olga Malsam, Alfred Angermann, Guido Bojack, Alan Graff, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Hein Kehne, Christopher Hugh Rosinger, Jan Dittgen
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Patent number: 7498451Abstract: The invention relates to a process for obtaining a pure aliphatic dialdehyde monoacetal by reaction of the corresponding aliphatic dialdehyde or a precursor of the corresponding aliphatic dialdehyde with one or more aliphatic mono- or polyhydric alcohols while distillatively removing water to obtain a reaction mixture which is separated distillatively, which comprises carrying out the distillative separation continuously in a dividing wall column to obtain pure aliphatic dialdehyde monoacetal as a sidestream from the dividing wall column, or in two distillation columns to obtain crude aliphatic dialdehyde monoacetal as a sidestream in the first distillation column, feed the crude aliphatic dialdehyde monoacetal to the second distillation column and obtain pure aliphatic dialdehyde monoacetal as the sidestream from the second distillation column.Type: GrantFiled: November 27, 2003Date of Patent: March 3, 2009Assignee: BASF AktiengesellschaftInventors: Gerd Haderlein, Hans-Georg Göbbel, Wolfgang Siegel
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Publication number: 20090048424Abstract: To provide a fluorosulfonyl group-containing monomer having a high polymerization reactivity and plural fluorosulfonyl groups. Further, to provide a fluorosulfonyl group-containing polymer and a sulfonic acid group-containing polymer, obtained by using the monomer. A perfluoro(2-methylene-1,3-dioxolane) derivative which is represented by the following formula (3) and which has two fluorosulfonyl groups, and its production process and its synthetic intermediate. A fluorosulfonyl group-containing polymer having monomer units represented by the following formula (3U) obtained by polymerizing the compound (3) by itself or with a comonomer, and a sulfonic acid group-containing polymer having the following units (5U) obtained by hydrolyzing a fluorosulfonyl group of the polymer. In the following formulae, each of Rf1 and Rf2 which are independent of each other, is a C1-8 perfluoroalkylene group which may have an etheric oxygen atom between carbon atoms.Type: ApplicationFiled: August 6, 2008Publication date: February 19, 2009Applicant: ASAHI GLASS COMPANY LIMITEDInventors: Atsushi WATAKABE, Hiromasa YAMAMOTO, Masao IWAYA, Susumu SAITO
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Publication number: 20080312317Abstract: There provided a 12-membered-ring macrolactam derivative having antitumor activity: A compound represented by Formula (1) or a salt thereof. In this Formula, R1 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group or a C6-14 arylcarbonyl group; R2 is a hydrogen atom or a C1-6 alkyl group; R3 is a hydrogen atom or a hydroxyl group; R4 is a hydrogen atom or a hydroxyl group; R5 is a hydrogen atom or a C1-6 alkyl group; R6 is a hydrogen atom or a hydroxyl group; and R7 is an acetyl group or the like.Type: ApplicationFiled: April 10, 2008Publication date: December 18, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Masayuki Miyano, Daisuke Ito, Norio Murai
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Publication number: 20080287694Abstract: A fluorosulfonyl group-containing compound having a high polymerization reactivity, a process for its production, a sulfonyl group-containing polymerizable monomer led from the sulfonyl group-containing compound, and a polymer obtainable by polymerizing the sulfonyl group-containing polymerizable monomer, are provided. A compound (3) is fluorinated to form a compound (4), and then, the compound (4) is subjected to a decomposition reaction to produce a compound (5). A preferred compound (5-1) of the compound (5) is thermally decomposed to produce a compound (7-1) having a high polymerization reactivity. wherein RA is a bivalent organic group such as a fluoroalkylene group, RAF is a group having RA fluorinated, or the same group as RA, each of RB to RD which are independent of one another, is a hydrogen atom, etc., each of RBF to RDF is a fluorine atom, etc.Type: ApplicationFiled: July 27, 2007Publication date: November 20, 2008Applicant: ASAHI GLASS COMPANY LIMITEDInventors: Takashi OKAZOE, Atsushi Watakabe, Masahiro Ito, Kunio Watanabe, Takeshi Eriguchi, Kimiaki Kashiwagi, Shu-zhong Wang
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Publication number: 20080242721Abstract: The present disclosure relates to the preparation of ketal compounds from glycerol and levulinic acid and esters, and uses thereof.Type: ApplicationFiled: May 31, 2007Publication date: October 2, 2008Applicant: AROMAGEN CORPORATIONInventor: Sergey Selifonov
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Publication number: 20080103191Abstract: Pharmaceutical composition comprising one or more entacapone derivatives and one or more pharmaceutically acceptable carriers, a process for producing the pharmaceutical composition, specific entacapone derivatives, a process for the preparation of entacapone derivatives, and the use of the entacapone derivatives for the preparation of a medicament.Type: ApplicationFiled: June 14, 2007Publication date: May 1, 2008Inventors: Klaus Hansen, Robert Kraemer, Thomas Lauterbach, Dirk Schmidt, Fritz Paar, Petra Pfeiffer, Detlef Geffken, Wolfgang Thimann, Katharina Wehner
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Publication number: 20080033036Abstract: The present invention provides a method and composition for promoting hair growth in a mammal which comprises a prostaglandin compound having two hetero atoms at the 15 position as an active ingredient thereof.Type: ApplicationFiled: August 12, 2004Publication date: February 7, 2008Inventors: Ryuji Ueno, Tsuyoshi Habe, Takashi Sekida
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Patent number: 7192968Abstract: The invention relates a compound represented by the formula (1): Q1-Q2-C(?O)—N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.Type: GrantFiled: April 5, 2001Date of Patent: March 20, 2007Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Toshiharu Yoshino, Tsutomu Nagata, Noriyasu Haginoya, Kenji Yoshikawa, Hideyuki Kanno, Masatoshi Nagamochi
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Patent number: 6844375Abstract: The invention relates to: 4-methylene-1,3-dioxolanes of the general formula (I) wherein R1 denotes hydrogen, C5-C6-cycloalkyl or C1-C4-alkyl; m and n, which may be the same or different, denote 0 or 1, whereby m?n, o denotes 2, 3 or 4 depending on the valency of the group X; and X denotes a C—C single bond, straight-chain or branched C1-C18-alkylene, C5-C6-cycloalkylene, C8-C18-arylalkylene, —CH2(OCH2CH2)pOCH2—, —CH2(OCH(CH3)CH2)pOCH2—, wherein p is an integer from 0 to 100; a process for their production; and intermediate products used. Moreover, compositions capable of emission-free, photocationic cross-linking, which comprise 4-methylene-1,3-dioxolanes of the general formula (I) and their use for the production of solvent-resistant and transparent films.Type: GrantFiled: August 23, 2001Date of Patent: January 18, 2005Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Helmut Hartl, Rainer B. Frings, Gerwald F. Grahe
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Patent number: 6803488Abstract: The present invention provides a process whereby fluorinated ketones of various structures can be produced by short process steps and which is useful as an industrial production process.Type: GrantFiled: February 26, 2003Date of Patent: October 12, 2004Assignee: Asahi Glass Company, LimitedInventors: Takashi Okazoe, Kunio Watanabe, Masahiro Ito, Daisuke Shirakawa, Shin Tatematsu, Hirokazu Takagi
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Patent number: 6753127Abstract: Disclosed is an norbornene-based copolymer for photoresist, a preparation method thereof, and a photoresist composition comprising the same. The copolymer of the present invention exhibits high transparency to light of 193 nm wavelength and an excellent etching resistance, excellent resolution due to the remarkable difference between light-exposed part and light-unexposed part in the dissolving rate and excellent adhesion to the substrate due to very hydrophilic diketone group of its own. As a result, the copolymer of the present invention is very useful as ArF exposure photoresist material in the fabrication of semiconductor devices.Type: GrantFiled: September 19, 2002Date of Patent: June 22, 2004Assignee: Samsung Electronics Co., Ltd.Inventors: Eun Sil Han, Bong Seok Moon, Jung Han Shin, Ouck Han
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Patent number: 6624177Abstract: The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix melatoproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: March 2, 1999Date of Patent: September 23, 2003Assignee: Warner-Lambert CompanyInventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic, Andrew David White
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Patent number: 6610892Abstract: The invention relates to a process for preparing 2,7-dimethyl-2,4,6-octatrienal monoacetals of the general formula I which comprises a) condensing an ester phosphonium salt of the general formula II or an ester phosphonate of the general formula III with an aldehyde of the formula IV in a Wittig or Wittig-Horner reaction to give an acetal ester of the general formula V b) reducing the ester of the formula V to give an acetal alcohol of the general formula VI and c) oxidizing the alcohol to 2,7-dimethyl-2,4,6-octatrienal monoacetals of the general formula I, where the substituents have the meaning defined in the description.Type: GrantFiled: March 12, 2002Date of Patent: August 26, 2003Assignee: BASF AktiengesellschaftInventors: Hansgeorg Ernst, Klaus Henrich
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Publication number: 20030118933Abstract: Disclosed is an norbornene-based copolymer for photoresist, a preparation method thereof, and a photoresist composition comprising the same. The copolymer of the present invention exhibits high transparency to light of 193 nm wavelength and an excellent etching resistance, excellent resolution due to the remarkable difference between light-exposed part and light-unexposed part in the dissolving rate and excellent adhesion to the substrate due to very hydrophilic diketone group of its own. As a result, the copolymer of the present invention is very useful as ArF exposure photoresist material in the fabrication of semiconductor devices.Type: ApplicationFiled: September 19, 2002Publication date: June 26, 2003Inventors: Eun Sil Han, Bong Seok Moon, Jung Han Shin, Ouck Han
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Patent number: 6569810Abstract: The present invention relates to novel bicyclic cyclopentane-1,3-dione derivatives of the formula (I) to a process for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: September 17, 2002Date of Patent: May 27, 2003Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Michael Ruther, Alan Graff, Arno Widdig, Jacques Dumas, Christoph Erdelen, Peter Dahmen, Markus Dollinger, Ulrike Wachendorff-Neumann
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Patent number: 6515150Abstract: Cyclic acetal compounds of formula (1) wherein k=0 or 1 and n is an integer of 0 to 6 are novel. Using the cyclic acetal compounds as a monomer, polymers are obtained. A resist composition comprising the polymer as a base resin is sensitive to high-energy radiation and has excellent sensitivity, resolution, and etching resistance.Type: GrantFiled: October 2, 2001Date of Patent: February 4, 2003Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Mutsuo Nakashima, Seiichiro Tachibana, Takeru Watanabe, Takeshi Kinsho, Koji Hasegawa, Tsunehiro Nishi, Jun Hatakeyama
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Patent number: 6486331Abstract: Substituted alkylketo compounds of the formula can be converted to the corresponding amino acid by a stereoselective enzymatic process. The resulting amino acid compounds can be employed as starting materials for pharmaceutically active compounds. This invention is directed to the substituted alkylketo compounds and their method of preparation.Type: GrantFiled: May 3, 2001Date of Patent: November 26, 2002Assignee: Bristol-Myers Squibb Co.Inventors: Ronald L. Hanson, Paul A. Jass, Wen-Sen Li, Ramesh Patel, Keith Ramig, John J. Venit
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Patent number: 6462076Abstract: The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.Type: GrantFiled: June 1, 2001Date of Patent: October 8, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Tobias Gabriel, Michael Pech, Rosa Maria Rodriguez Sarmiento
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Publication number: 20020128519Abstract: The invention relates to a process for preparing 2,7-dimethyl-2,4,6-octatrienal monoacetals of the general formula I 1Type: ApplicationFiled: March 12, 2002Publication date: September 12, 2002Inventors: Hansgeorg Ernst, Klaus Henrich
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Patent number: 6395911Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (−)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.Type: GrantFiled: October 9, 2001Date of Patent: May 28, 2002Assignee: Pfizer Inc.Inventor: Charles K. F. Chiu
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Patent number: 6388104Abstract: Novel 4-methylene-1,3-dioxolanes of the general formula I in which R1 denotes hydrogen or alkyl, X denotes a single bond, C1-C18 alkylene, cycloalkylene, arylalkylene, —CH2(OCH2CH2)n— or —CH2(OCH(CH3)CH2)n—, in which n is an integer from 1 to 100, and Z means a functional group selected from among —OH, —COOR′ or —OCOR′, in which R′ denotes hydrogen or C1-C8 alkyl, are described, as are a process for the production thereof and the intermediates used in this process.Type: GrantFiled: October 5, 2000Date of Patent: May 14, 2002Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Helmut Hartl, Rainer B. Frings, Gerwald F. Grahe
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Publication number: 20020049342Abstract: Substituted alkylketo compounds of the formula 1Type: ApplicationFiled: May 3, 2001Publication date: April 25, 2002Inventors: Ronald L. Hanson, Paul A. Jass, Wen-Sen Li, Ramesh Patel, Keith Ramig, John J. Venit
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Patent number: 6376683Abstract: The present invention relates to an improved, efficient and enantio-selective process for the synthesis of (4R, 6S)-4-hydroxy-6-hydroxymethyl tetrahydropyran-2-one, employing the Sharpless asymmetric dihydroxylation and regiospecific nucleophilic hydride opening of the cyclic sulfite/sulfate as the key steps. The invention also resides in the intermediates used in the process.Type: GrantFiled: June 1, 2001Date of Patent: April 23, 2002Assignee: Council of Scientific & Industrial ResearchInventors: Pradeep Kumar, Rodney Agustinho Fernandes
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Publication number: 20020045769Abstract: The present invention relates to a novel acyclic chiral derivatives of Hibiscus acid of formula I, 1Type: ApplicationFiled: September 5, 2001Publication date: April 18, 2002Inventors: Ibrahim Ibnu Saud, Rani Rajasekharan Nair
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Publication number: 20020042528Abstract: The present invention relates to a novel acyclic chiral compound of Garcinia acid of formula I, 1Type: ApplicationFiled: September 5, 2001Publication date: April 11, 2002Inventors: Ibrahim Ibnu Saud, Tom Thomas Puthiyaparampil
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Patent number: 6355812Abstract: The invention relates to improved methods of producing aryl dioxoalkanoic acid compounds and derivatives useful as intermediates for diarylpyrrole therapeutic agents by the alcoholysis of benzoylcyclohexanone ketal compounds.Type: GrantFiled: May 5, 2000Date of Patent: March 12, 2002Assignee: Orth-McNeil Pharmaceutical, Inc.Inventors: Michael P. Ferro, Kathleen A. McCoy
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Patent number: 6251937Abstract: The invention relates to cleavable surfactants of formula: in which R′ and R, which may be identical or different, represent a hydrogen atom or a linear or branched, saturated or unsaturated alkyl radical, the sum of the carbon atoms of R′ and R being between 5 and 42. The invention also relates to the corresponding derivatives obtained by alkaline hydrolysis or amidation. The invention furthermore relates to the preparation of these surfactants from glucono-1(5)-lactone and a compound of formula R—CO—R′ in the presence of an acid catalyst, R and R′ having the meaning given above. The surfactants are used in particular in emulsion polymerization and in the field of cosmetics.Type: GrantFiled: April 13, 1998Date of Patent: June 26, 2001Assignee: CECA S.A.Inventors: Serge Petit, Stephane Fouquay
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Patent number: 6214859Abstract: Ethylamine derivatives of the formula (I): (wherein R1 is hydrogen, hydroxyl, lower alkoxy or halogen; R2 is alkyl having 2 to 5 carbon atoms; R3 is hydrogen, alkyl having 2 to 5 carbon atoms, alkylcarbonyl having 2 to 5 carbon atoms, aryl having 6 to 10 carbon atoms or arylalkyl having 7 to 11 carbon atoms; the ring is a bicyclic compound which consists of at least one benzene ring and may comprise a saturated or unsaturated five- or six-membered ring which may or may not have heteroatoms, providing that when the ring is indole or 1,3-benzodioxole, R2 and R3 do not constitute, at the same time, two carbon atoms members, and when R3 is hydrogen, the ring is a bicyclic compound which is not indole, benzothiophene or benzodioxole and R2 is alkyl having 3 to 5 carbon atoms and pharmaceutically acceptable acid addition salts thereof. These compounds are promising as psychotropic drugs, antidepressants, drugs for Parkinson's disease and/or drugs for Alzeimer's disease.Type: GrantFiled: July 12, 1999Date of Patent: April 10, 2001Assignee: Fujimoto Brothers Co., Ltd.Inventors: Fumio Yoneda, Joseph Knoll, Hironori Ode, Masatoshi Sakae, Masanori Katurada, Toshiaki Moto, Takashi Ando, Seiichiro Shimazu, Kazue Takahata, Michitaro Fujimoto
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Patent number: 6184376Abstract: Methods and novel intermediates of the formula: wherein R6 and R7 are lower alkyl or benzyl or R6 and R7 taken together are —CH2CH2—, —CH2CH2CH2— or —CH2CH2CH2CH2CH2—, R8 is C1-C21 alkyl or a C2-C21 monounsaturated alkenyl, which may optionally be substituted with substitution substituents independently selected from the group consisting of hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy C1-C6 alkyl, C1-C6 alkanoyl, amino, halo, cyano, azido, oxo, mercapto and nitro, and R9 is an alcohol protecting group. The intermediates are useful for the preparation of acyclic nucleoside derivatives of the formula: where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a —C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl and R3 is OH or H; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 6, 1998Date of Patent: February 6, 2001Assignee: Mediver ABInventors: M. Robert Leanna, Steven M. Hannick, Michael Rasmussen, Jien-Heh J. Tien, Lakshmi Bhagavatula, Pulla Reddy Singam, Bradley D. Gates, Lawrence Kolaczkowski, Ramesh R. Patel, Greg Wayne, Greg Lannoye, Weijiang Zhang, Zhenping Tian, Kirill A. Lukin, Bikshandarkoil A. Narayanan, David A. Riley, Howard Morton, Sou-Jen Chang, Cynthia B. Curty, Daniel Plata, John Bellettini, Bhadra Shelat, Tiffany Spitz, Cheng-Xi Yang
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Patent number: 6051711Abstract: A method for synthesizing swainsonine salts and intermediates thereof comprising subjecting a compound of the formula I ##STR1## wherein R.sup.2 and R.sup.2' are the same or different and represent alkyl, halogen, alkenyl, alkoxy, cycloalkyl or aryl which may be substituted, to acid hydrolysis in the presence of a C.sub.1-4 alkanol to obtain a crystalline salt of swainsonine; and optionally, recrystallizing the swainsonine salt from a C.sub.1-4 alkanol. The reaction may be used in combination with one or more additional reaction steps.Type: GrantFiled: October 23, 1998Date of Patent: April 18, 2000Assignee: GLYCODesign Inc.Inventors: Francois Tropper, Rajan N. Shah, Pradeep Sharma
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Patent number: 6001535Abstract: Monomers with cyclic carbonate groups of the formula I are suitable for the production of photosensitive recording materials, for example for the production of offset printing plates ##STR1## in which A means an (n+m)-valent hydrocarbon residue with 3 to 30 C atoms, which may be OH-substituted and may contain up to 8 ether bridges,R means H or methyl;n means an integer from 1 to 5;m means an integer from 1 to 3, providing that n+m is at least 3.Type: GrantFiled: October 1, 1997Date of Patent: December 14, 1999Assignee: Agfa Gevaert AGInventors: Wolfgang Podszun, Ludger Heiliger, Michael Muller, Carl Casser, Friedrich Bruder
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Patent number: 6001994Abstract: An improved process to make gemcitabine hydrocrhloride, the improvement consisting essentially of making the lactone intermediate, 2-deoxy-2,2-difluoro-D-erythro-pentafuranose-1 ulose-3,5-dibenzoate: ##STR1## from D-erythro-2-Deoxy-2,2-difluoro 4,5-O-(1-ethylpropyl)-idene) pentoic acid tert Butyl ester wherein, the D-erythro-2-deoxy-2,2 difluoro-4,5-O-(1-ethylproyl)-ideno) pentoic acid tert-Butyl ester is prepared by the process of reacting S-tert-butyl difluoroethane thioate with 2,3-O (1-ethylpropylidene)-D-glyceraldehyde, in a solvent and in the presence of a strong base; with the proviso that the process is conducted in the absence of a catalyst and in the absence of a silyl containing compound.Type: GrantFiled: December 10, 1998Date of Patent: December 14, 1999Assignee: Eli Lilly and CompanyInventor: John A. Weigel
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Patent number: 5998633Abstract: The invention is an improved process for the preparation of a compound of formula I wherein R and R.sup.1 are each independently alkyl of from 1 to 3 carbon atoms; and R.sup.2 is alkyl of from 1 to 8 carbon atoms.Type: GrantFiled: January 27, 1999Date of Patent: December 7, 1999Assignee: Warner-Lambert CompanyInventors: Thomas E. Jacks, Donald E. Butler
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Patent number: 5994379Abstract: The present invention relates to inhibitors of COX-2, compositions which contain such compounds and methods of use. The compounds are represented by formula I: ##STR1## and include pharmaceutically acceptable salts and esters thereof.Type: GrantFiled: February 9, 1999Date of Patent: November 30, 1999Assignee: Merck Frosst Canada, Inc.Inventors: Christopher I. Bayly, Cameron Black, Nathalie Ouimet, David Percival, Serge Leger, Marc Ouellet