Silicon Containing Patents (Class 549/214)
  • Publication number: 20100137244
    Abstract: Chemical syntheses and medical uses of novel modulators of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and diastereomeric mixtures of isomers, individual diastereomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of hypercholesterolemia, dyslipidemia, coronary artery disease, atherosclerosis, metabolic syndrome, a hyperproliferative disease such as colorectal cancer, prostate cancer, and melanoma, a neurodegenerative disease such as cerebral ischemia, Alzheimer's disease, and Parkinson's disease are described.
    Type: Application
    Filed: July 12, 2007
    Publication date: June 3, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20100123123
    Abstract: A thin-film transistor comprises a semiconducting layer comprising a semiconducting material selected from Formula (I) or (II): wherein X, R1, R2, R3, R4, R5 a, b, and n are as described herein. Semiconducting compositions of Formula (I) or (II) are also described.
    Type: Application
    Filed: November 19, 2008
    Publication date: May 20, 2010
    Applicant: Xerox Corporation
    Inventors: Yuning Li, Yiliang Wu, Ping Liu, Paul F. Smith
  • Publication number: 20100099875
    Abstract: The invention relates to novel organo phosphorus P-chiral optically active compounds of formula (I) having a hydroxyl, mercapto, amino, carboxyl, sulfonyl group on aryl near a phosphorus atom, to the preparation and the use thereof in then asymmetrical catalysis of unsaturated compounds. Novel acylphosphine optically pure ligands embodied in the form of transition metal complexes exhibit an increased activity and enantloselectivity, in particular in asymmetrical hydrogenation, in comparison with the same type Uganda such as DiPAMP.
    Type: Application
    Filed: June 20, 2006
    Publication date: April 22, 2010
    Applicants: PHOSPHOENIX SARL, NATIONAL INSTITUTE OF CHEMISTRY
    Inventors: Michel Stephan, Barbara Mohar
  • Patent number: 7678926
    Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: September 20, 2007
    Date of Patent: March 16, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
  • Publication number: 20100048887
    Abstract: 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: Application
    Filed: April 20, 2009
    Publication date: February 25, 2010
    Inventors: Eric Anderson, Gary L. Bolton, Deborah A. Ferguson, Xin Jiang, Robert M. Kral, JR., Patrick M. O'Brien, Melean Visnick
  • Publication number: 20100048917
    Abstract: The present invention provides (i) a process for preparing a 2-deoxy-2-fluoro-2-methyl-D-ribonolactone derivative, (ii) conversion of the lactone to nucleosides with potent anti-HCV activity, and their analogues, and (iii) a method to prepare the anti-HCV nucleosides containing the 2-deoxy-2-fluoro-2-C-methyl-?-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.
    Type: Application
    Filed: September 3, 2009
    Publication date: February 25, 2010
    Applicant: Pharmassett, Inc.
    Inventors: Peiyuan Wang, Wojciech Stec, Byoung-Kwon Chun, Junxing Shi, Jinfa Du
  • Publication number: 20100035839
    Abstract: Disclosed are merocyanine derivatives which correspond to the formula (I), wherein L1, L2 and L3 independently of each other are hydrogen; or L1 and L3 may be linked together to form a carbocyclic ring; R3 and R4 independently of each other are CN; —COR5; —COOR5; —CONR5R6; C1-C22alkyl; C2-C22alkenyl; C2-C22alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C20aralkyl; C1-C20heteroalkyl; C3-C12cycloheteroalkyl; C3-C18heteroaralkyl; C6-C20 aryl; C1-C12alkylcarbonylamino-C6-C20aryl; C2-C12heteroaryl; or —X2—Sil2; n is a number from 1 to 4; the meaning of R1 and R2 depends on the definition of n. The compounds are useful as UV absorbers for cosmetic applications.
    Type: Application
    Filed: October 5, 2007
    Publication date: February 11, 2010
    Applicant: CIBA CORPORATION
    Inventor: Barbara Wagner
  • Publication number: 20100029953
    Abstract: Alkoxy-substituted phenyltetraene nonlinear optically active compounds, films and devices that include the compounds, and methods for making and using the compounds, films, and devices.
    Type: Application
    Filed: May 28, 2009
    Publication date: February 4, 2010
    Applicant: WASHINGTON, UNIVERSITY OF
    Inventors: Kwan-Yue Jen, Jingdong Luo, Su Huang, Yen-Ju Cheng, Tae-Dong Kim, Zhengwei Shi, Xing-Hua Zhou, Brent M. Polishak, Yanqing Tian
  • Patent number: 7638256
    Abstract: Silicon compounds having fluorinated hemiacetal structure are provided. Silicone resins having the same structure have an appropriate acidity to enable formation of a finer pattern by minimizing the pattern collapse by swelling, exhibit improved resistance to the etching used in the pattern transfer to an organic film, and are thus suited for use in resist compositions for the bilayer process.
    Type: Grant
    Filed: July 6, 2006
    Date of Patent: December 29, 2009
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Takeshi Kinsho, Takeru Watanabe, Mutsuo Nakashima, Yoshitaka Hamada
  • Publication number: 20090318481
    Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.
    Type: Application
    Filed: August 28, 2009
    Publication date: December 24, 2009
    Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Michael GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
  • Publication number: 20090259085
    Abstract: The invention relates to a process for producing a complex for use in olefin polymerization and oligomerization of the general formula (III): wherein Mt is a group 3 to 12 element in a +2 to +6 oxidation state with between 1 to 4 additional ligands (anionic and/or neutral) coordinated, wherein R1 and R2 are hydrogen, halogen, alkoxy, or a hydrocarbon group containing between 1 to 12 carbon atoms; E is a group 16 element, preferably O; Z is a direct bond between carbon atoms of the adjacent aromatic rings or a —CR3R4— or —SiR3R4— bridge between those carbon atoms, where R3 and R4 are hydrogen or a hydrocarbon groups with 1 to 10 carbons, R5, R6, R7 and R8 are hydrogen, halogen, alkoxy, or a hydrocarbon group containing between 1 to 10 carbon atoms and J1 and J2 are —NR9R10 or —PR9R10, where R9 is H or SiMe3 group and R10 is selected from a group consisting of alkyl, aryl, substituted aryl, heteroalkyl, and heteroaryl containing between 1 to 30 non-hydrogen atoms through a route involving novel precursors s
    Type: Application
    Filed: April 15, 2008
    Publication date: October 15, 2009
    Inventor: John R. Hagadorn
  • Publication number: 20090224658
    Abstract: An organic electroluminescence device comprising a compound having a specific structure having a heteroatom and an organic electroluminescence device which comprises a cathode, an anode and an organic thin film layer which comprises at least one layer comprising at least a light emitting layer and is disposed between the cathode and the anode, wherein at least one layer in the organic thin film layer comprises the above compound. The device provides excellent efficiency of light emission, forms no defects in pixels, exhibits excellent heat resistance and has a long life.
    Type: Application
    Filed: May 29, 2007
    Publication date: September 10, 2009
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Toshihiro Iwakuma, Masahide Matsuura, Yuki Nakano, Hidetsugu Ikeda
  • Patent number: 7576142
    Abstract: The object of the present invention is to provide a polyorganosiloxane that has a specific structure and is superior to curability and a curable composition which is high in workability during curing, which leads to a cured product excellent in ultraviolet-ray transparency and heat resistance, and further wherein toughness thereof and occurrence of a crack by cyclic heat-cool are improved. The present polyorganosiloxane is one obtained by conducting hydrolysis and condensation of a silicon-containing organic compound represented by the general formula (1) below in the presence of an organic polyol compound having two or more hydroxyl groups and has an oxetanyl group.
    Type: Grant
    Filed: August 2, 2005
    Date of Patent: August 18, 2009
    Assignee: Toagosei Co., Ltd.
    Inventors: Kunikazu Tauchi, Hiroshi Suzuki
  • Publication number: 20090187031
    Abstract: Synthetic methods and intermediates useful in the preparation of lactone containing compounds such as discodermolide and compounds which mimic the chemical or biological activity of discodermolide are provided.
    Type: Application
    Filed: February 28, 2008
    Publication date: July 23, 2009
    Applicant: The Trustees of The University of Pennsylvania
    Inventors: Amos B. Smith, III, Thomas J. Beauchamp, Matthew J. LaMarche, Yuping Qiu, Michael D. Kaufman, Hirokazu Arimoto, David R. Jones, Kaoru Kobayashi
  • Publication number: 20090163596
    Abstract: The invention provides a novel polymorphic form I of crystalline bimatoprost, method for preparation thereof and new crystalline intermediates in the preparation. This form I of crystalline bimatoprost is used in purification of crude bimatoprost and in storage of bimatoprost as active pharmaceutical intermediate. Use of the physical form of bimatoprost in the manufacture of a medicament is also disclosed.
    Type: Application
    Filed: August 29, 2007
    Publication date: June 25, 2009
    Inventors: Arie Gutman, Igor Rukhman, Boris Tishin, Lev Yudovich, Alexander Vilensky, Boris Pertsikov, Gennady Nisnevich
  • Publication number: 20090163724
    Abstract: A process for the carbonylation of ethylenically unsaturated compounds including vinyl esters and a process for the production of 3-hydroxy propanoate esters or acids. The process comprises reacting said compound with carbon monoxide in the presence of a source of hydroxyl groups and of a catalyst system. The catalyst system is obtainable by combining: (a) a metal of Group 8, 9 or 10 or a compound thereof: and (b) a bidentate ligand of general formula (I): X1(X2)-Q2-A-R—B-Q1-X3(X4).
    Type: Application
    Filed: November 8, 2006
    Publication date: June 25, 2009
    Applicant: Lucite International Uk Limited
    Inventors: Graham Ronald Eastham, Mark Waugh, Philip Ian Richards
  • Patent number: 7550608
    Abstract: The present invention provides processes for the production of docetaxel. Docetaxel is produced by protecting the C(7) and the C(10) hydroxy groups of 10-DAB with a bridging silicon-based protecting group. The resulting 7,10-protected 10-DAB derivative is then derivatized and deprotected to form docetaxel.
    Type: Grant
    Filed: June 8, 2006
    Date of Patent: June 23, 2009
    Assignee: Florida State University Research Foundation, Inc.
    Inventors: Phong Vu, Robert A. Holton
  • Publication number: 20090156753
    Abstract: The present invention relates to a silphenylene compound represented by the following formula (1): in which R1 to R4 each independently represents a hydrogen atom or a monovalent hydrocarbon group having 1 to 6 carbon atoms, and R5 and R6 each independently represents a divalent hydrocarbon group having 2 to 8 carbon atoms. The silphenylene compound of the present invention is useful as a flexible printed wiring board material, a passivation film for IC chips, and a panel material for liquid crystals.
    Type: Application
    Filed: December 11, 2008
    Publication date: June 18, 2009
    Inventors: Michihiro Sugo, Takahiro Goi, Tomoyuki Goto, Shohei Tagami
  • Publication number: 20090118521
    Abstract: Nonlinear optically active compounds having film-forming properties, films including the compounds, methods for making the compounds and films, and electro-optic devices including the films and compounds.
    Type: Application
    Filed: August 3, 2006
    Publication date: May 7, 2009
    Applicant: WASHINGTON, UNIVERSITY OF
    Inventors: Kwan-Yue Jen, Jingdong Luo, Tae-Dong Kim, Baoquan Chen, Jae-Wook Kang
  • Publication number: 20090043101
    Abstract: To provide an industrially advantageous process for producing 5-chloro-2,4-dihydroxypyridine, which is an inhibitor acting on a biodegradation enzyme that biodegrades an anti-malignant-tumor agent 5-fluorouracil. The process is carried out under mild conditions with a small number of steps and produces less industrial waste. The process employs a 5-chloro-1,3-dioxin-4-one derivative (2) as a starting substance to thereby form a pyrone derivative (4) represented by formula (4): (wherein R3 and R4, which are identical to or different from each other, each represent a C1 to C6 linear-chain or branched-chain alkyl group, or a silyl group having a C1 to C6 linear-chain or branched-chain alkyl group), and subsequently, 5-chloro-2,4-dihydroxypyridine (1) is produced from the pyron derivative.
    Type: Application
    Filed: January 25, 2006
    Publication date: February 12, 2009
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Nagasawa, Katsuyuki Higurashi, Etsuji Yamanaka
  • Publication number: 20090005557
    Abstract: The present invention provides a ?-electron-conjugated organice silane compound that give an organic thin film superior in peeling restance, orientation, crystallinity and eletroconductive properties, and a production method thereof. A ?-electron-conjugated organice silane compound represented by General Formula: R1-SiX1X2X3 (R1 represents an organic group having a particular monocyclic heterocyclic unit; and X1 to X3 are a group giving a hydroxyl group by hydrolysis). A method of producing the organic silane compound, comprising allowing a compound represented by General Formula: R1-Li (R1 is the same as above) or a compound represented by General Formula: R1-MgX5 (R1 is the same as above; and X5 represents a halogen atom) with a compound represented by General Formula: X4-SiX1X2X3 (X1 to X3 are the same as above; and X4 represents a hydrogen or halogen atom or a lower alkoxy group).
    Type: Application
    Filed: July 4, 2005
    Publication date: January 1, 2009
    Inventors: Masatoshi Nakagawa, Hiroyuki Hanato, Toshihiro Tamura
  • Publication number: 20080311514
    Abstract: In a mixture of silsesquioxane compounds comprising silsesquioxane units having a side chain including a direct bond between a silicon atom and a norbornane skeleton and having a degree of condensation of substantially 100%, a dimethylene chain of the norbornane skeleton remote from the silicon bonded side is substituted with at least one substituent group other than hydrogen, and an isomer having a bulkier substituent group on the dimethylene chain at an exo position is present in a higher proportion.
    Type: Application
    Filed: September 25, 2007
    Publication date: December 18, 2008
    Applicant: SHIN-ETSU CHEMICAL CO., LTD.
    Inventors: Mutsuo NAKASHIMA, Yoshitaka HAMADA, Katsuya TAKEMURA, Kazumi NODA
  • Publication number: 20080293875
    Abstract: An object of the present invention is to provide a curable composition which: is excellent in reactivity, in particular, cationic polymerizability with respect to light and heat; and has good heat resistance. The object is carried out by an oxetane compound producible by a reaction between a silane compound having an epoxy group and an alkoxysilyl group, and a compound having an oxetane ring and an active hydrogen group.
    Type: Application
    Filed: December 19, 2005
    Publication date: November 27, 2008
    Applicant: The Yokohama Rubber Co., Ltd.
    Inventor: Kazuhiro Hatanaka
  • Patent number: 7456298
    Abstract: The present invention is related to cis-diols and biological methods of producing cis-diols. The present invention further relates to processes for subsequently converting such silane cis-diols to the more stable acetonide derivatives, as well as a process for converting silane cis-diols to the corresponding catechols and the compounds produced thereby. The present invention also provides chemical methods for the conversion of said silane cis-diols and acetonide compounds to epoxy, saturated and otherwise modified derivatives. It is emphasized that this abstract is provided to comply with the rules requiring an abstract which will allow a searcher or other reader to quickly ascertain the subject matter of the technical disclosure. It is submitted with the understanding that is will not be used to interpret or limit the scope or meaning of the claims.
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: November 25, 2008
    Assignee: Genencor International, Inc.
    Inventors: Joseph C. McAuliffe, Gregory M. Whited, Wyatt Charles Smith
  • Publication number: 20080249306
    Abstract: The present invention relates to a process for the production of statins, which are known as HMG-CoA reductase inhibitors. A few of the intermediate compounds for use in the process in accordance with the invention are novel compounds and the invention also relates to these novel intermediate compounds.
    Type: Application
    Filed: April 28, 2006
    Publication date: October 9, 2008
    Inventors: Vitali Tararov, Armin Boerner, Gerd Koenig, Andrei Korostylev
  • Patent number: 7432381
    Abstract: The present invention relates to 1,3-oxathiolane-2-thione compounds of the general formula (I): wherein R1 and R2 are the same or different, each of which denotes a straight-chain or branched alkoxy residue with 1 to 6 carbon atoms or an aryloxy or aralkyloxy residue, R3 is different or the same as R1 or R2 or an aliphatic residue, an amino residue, a halogen residue, an aromatic or heteroaromatic residue, or an araliphatic or heteroaraliphatic residue, R4 is a bridging group selected from the groups consisting of aliphatic, heteroaliphatic, araliphatic, heteroaraliphatic, aromatic and heteroaromatic groups and R5 is hydrogen, an aliphatic, heteroaliphatic, araliphatic, heteroaraliphatic, aromatic, heteroaromatic, cycloaliphatic or heterocycloaliphatic group or R4 and R5 form a cycloaliphatic, cycloheteroaliphatic, aromatic or heteroaromatic residue, which is optionally substituted with an aliphatic, heteroaliphatic residue serving as a bridging group to the silicon atom and X and Y are different and sele
    Type: Grant
    Filed: February 15, 2006
    Date of Patent: October 7, 2008
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Kazuya Uenishi, Atsushi Sudo, Hiroshi Morikawa, Takeshi Endo, Olaf Lammerschop, Thomas Huver, Pavel Gentschev
  • Patent number: 7425283
    Abstract: A siloxane modified with a cyclic carbonate of the formula: is combined with a non-aqueous solvent and an electrolyte salt to form a non-aqueous electrolytic solution, which is used to construct a secondary battery having improved temperature and cycle characteristics.
    Type: Grant
    Filed: September 13, 2006
    Date of Patent: September 16, 2008
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Tetsuo Nakanishi, Meguru Kashida, Satoru Miyawaki
  • Publication number: 20080194521
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Application
    Filed: August 13, 2007
    Publication date: August 14, 2008
    Inventors: Robert Eugene Hormann, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
  • Publication number: 20080167389
    Abstract: The present invention provides for a composition comprising a silane having the formula: (R1)(R2)(R3)Si—R4—Si(R5)(R6)(R7) wherein R1, R2, R3, R5, and R6 are each independently selected from the group consisting of 1 to 6 monovalent hydrocarbon radicals, aryl, and a hydrocarbon group of 7 to 10 carbons containing an aryl group; R4 is a hydrocarbon group of 1 to 3 carbons; R7 comprises an anionic, cationic or zwitterionic substituent. The silanes of the present invention exhibit resistance to hydrolysis over a wide pH range.
    Type: Application
    Filed: December 10, 2007
    Publication date: July 10, 2008
    Applicant: MOMENTIVE PERFORMANCE MATERIALS INC.
    Inventors: Mark D. Leatherman, George A. Policello, Wenqing Peng, Liping Zheng, Roland Wagner, Suresh K. Rajaraman, Zijun Xia
  • Publication number: 20080146820
    Abstract: This invention relates to surfactant compositions comprising a phosphate fluorosurfactant and a siloxane surfactant wherein the surfactant composition's ability to lower equilibrium surface tension exceeds that of either the phosphate fluorosurfactant or the siloxane surfactant. Because of the synergistic interaction of the phosphate fluorosurfactant and the siloxane surfactant, it is possible to use only small amounts of the more expensive fluorosurfactant in the surfactant composition of the present invention while preserving or improving the ability to lower the equilibrium surface tension of a liquid, such as water.
    Type: Application
    Filed: November 13, 2007
    Publication date: June 19, 2008
    Inventors: Axel Hans-Joachim Herzog, Shaun Raymond Rinehimer
  • Publication number: 20080139505
    Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.
    Type: Application
    Filed: November 15, 2005
    Publication date: June 12, 2008
    Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
  • Patent number: 7385221
    Abstract: Novel silylethynylated heteroacenes and electronic devices made with those compounds are disclosed.
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: June 10, 2008
    Assignee: University of Kentucky Research Foundation
    Inventors: John E. Anthony, Marcia M. Payne, Susan A. Odom, Sean Richard Parkin
  • Patent number: 7381349
    Abstract: A process to produce a polymer liquid crystalline composition having temperature dependency of desired circular polarization selective reflection wave length property by only mixing two or more kinds of starting materials having different weight-average molecular weight comprising, mixing two or more kinds of rigid rodlike helical polymers with chiral side chains having different weight-average molecular weight synthesized from same molecules and having same repeating unit whose molecular weight distribution defined by the ratio of weight average molecular weight/number average molecular weight is from 1.00 to 1.25, and controlling weight average molecular weight, number average molecular weight and molecular weight distribution by mixing ratio.
    Type: Grant
    Filed: April 14, 2003
    Date of Patent: June 3, 2008
    Assignee: Japan Science and Technology Agency
    Inventors: Michiya Fujiki, Junji Watanabe, Kento Okoshi
  • Patent number: 7365213
    Abstract: [Problems] To provide a novel alkoxysilane having a diol protected, an organosilicon resin which has a diol and the composition of which can be easily regulated, and to processes for producing these. [Means for solving problems] The alkoxysilane is an organosilicon compound represented by the following formula (1). The organosilicon resin having a diol is one obtained by hydrolyzing-condensing this compound with a multifunctional alkoxysilane. (In the formula, each of R1, R2 and R3 is an alkyl group or an alkoxy group each having carbon number from 1 to 6. R4 is an alkylene group having carbon number from 2 to 6. Z is an alkylene group having carbon number from 1 to 3.) The alkoxysilane of the present invention can be produced by a hydrosilylation reaction of a compound represented by the following formula (4) and a silane compound R1R2R3SiH. (In the formula, Z is an alkylene group having carbon number from 1 to 3 and R5 has a carbon-carbon double bond at the terminal.
    Type: Grant
    Filed: February 9, 2005
    Date of Patent: April 29, 2008
    Assignee: Toagosei Co., Ltd.
    Inventors: Katsuhiko Komuro, Hiroshi Suzuki
  • Patent number: 7329654
    Abstract: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: February 12, 2008
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ramesh M. Kanojia, Nareshkumar F. Jain, Raymond Ng, Zhihua Sui, Jiayi Xu
  • Patent number: 7312203
    Abstract: The present invention relates to 1-aza-dibenzoazulene derivatives, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.
    Type: Grant
    Filed: May 20, 2003
    Date of Patent: December 25, 2007
    Assignee: GlaxoSmithKline istraziva{hacek over (c)}ki Centar Zagreb d.o.o.
    Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic
  • Publication number: 20070293687
    Abstract: A novel semisynthetic route has been provided in the preparation of docetaxel and paclitaxel. This new process involves the conversion of 9-dihydro-13-acetylbaccatinIII to docetaxel and paclitaxel by the step of converting 9-dihydro-13-acetylbaccatin III into 7-O-triethylsilyl-9,10-diketobaccatin III, and adding docetaxel and paclitaxel side chain precursors, respectively, to form a new class of taxane intermediates, such as 7-O-triethylsilyl-9,10-diketodocetaxel and 7-O-triethylsilyl-9,10-diketopaclitaxeltaxel. These new intermediates then by a series reduction, acetylation of the 10-hydroxyl position for paclitaxel and finally deprotection to yield docetaxel and paclitaxel, the most important anti-cancer drugs.
    Type: Application
    Filed: June 19, 2006
    Publication date: December 20, 2007
    Inventor: Jian LIU
  • Publication number: 20070278461
    Abstract: Various non-limiting embodiments of the present invention relate to photochromic materials which include a haloalkyl group. More particularly, various non-limiting embodiments disclosed herein provide photochromic materials including an indeno-fused naphthopyran, such as, an indeno[2?,3?:3,4]naphtho[1,2-b] pyran, and a haloalkyl group bonded at the 13-position thereof, wherein the haloalkyl group is a perhalogenated group or a group represented by —O(CH2)a(CX2)bCT3, wherein T is a halogen, each X is independently hydrogen or halogen, a is an integer ranging from 1 to 10, and b is an integer ranging from 1 to 10. Other non-limiting embodiments disclosed herein provide photochromic composition and photochromic articles, such as, but not limited to ophthalmic lens, which include the disclosed photochromic materials and methods of making the same.
    Type: Application
    Filed: April 2, 2007
    Publication date: December 6, 2007
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Olga G. Petrovskaia, Anu Chopra, Patrick M. Brown
  • Patent number: 7304161
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Grant
    Filed: February 9, 2004
    Date of Patent: December 4, 2007
    Assignee: Intrexon Corporation
    Inventors: Robert Eugene Hormann, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
  • Patent number: 7230123
    Abstract: The invention relates to ureido or carbamate derivatives of crown ethers and of silicon of formula: These derivatives can be grafted to silica gel for the purpose of obtaining supports for the chromatographic separation of cations or of molecules comprising amine functional groups, such as amino acids.
    Type: Grant
    Filed: January 20, 2003
    Date of Patent: June 12, 2007
    Assignee: Commissariat a l'Energir Atomique
    Inventors: Yves Barre, Marc Simon, Roger Neige, Raphaël Duval
  • Patent number: 7193092
    Abstract: The present invention relates to chiral diphosphorus compounds and their transition metal complexes, to a process for preparing chiral diphosphorus compounds and their transition metal complexes and also to their use in asymmetric syntheses.
    Type: Grant
    Filed: August 19, 2003
    Date of Patent: March 20, 2007
    Assignee: Lanxess Deutschland GmbH
    Inventors: Benjamin Meseguer, Hans-Christian Militzer, Sergio Castillon, Carmen Claver, Yolanda Diaz, Mohamed Aghmiz, Ester Guiu, Ali Aghmiz, Anna Masdeu
  • Patent number: 7166583
    Abstract: The present invention relates to 1,3-diaza-dibenzoazulene derivatives, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumor necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.
    Type: Grant
    Filed: May 20, 2003
    Date of Patent: January 23, 2007
    Assignee: Pliva-Istrazivacki Institut d.o.o.
    Inventors: Mladen Mercep, Milan Mesic, Renata Rupcic, Dijana Pesic
  • Patent number: 7115651
    Abstract: The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof) wherein R0–R4, Z, X, A—B, D—E, G—J, and K—L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.
    Type: Grant
    Filed: August 24, 2001
    Date of Patent: October 3, 2006
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Robert M. Garbaccio, Daniel K. Baeschlin, Shawn J. Stachel, David Solit, Neal Rosen
  • Patent number: 7109281
    Abstract: This invention relates to the reversible protection of hydroxy-silane functional groups by acid cleavable protecting groups. The development of reversible protecting groups greatly enhances the current utility of silanes while introducing further novel applications. For instance, reversibly protected silanes are of particular value in applications where room temperature cure and/or adhesion is of value, such as coatings, high resolution imaging, caulks, adhesives, sealants, gaskets, and silicones. Reversibly protected silanes can also be beneficially used in reticulating agents, and in sizing agents, tires, and release coatings. The incorporation of reversibly protected silanes into coating resins is of particular value. The reversibly protected silane can be incorporated into the coating resin by polymerizing a monomer containing the reversibly protected silane into the resin or by post-addition into the coating formulation.
    Type: Grant
    Filed: November 6, 2003
    Date of Patent: September 19, 2006
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Daniel Edward Bowen, III, Eric Sean Castner
  • Patent number: 7102018
    Abstract: Intermediate compounds, including 2-(t-butyldimethylsilyloxymethyl)-3,4-[(dimethylmethylene)dioxy]-5-hydroxy-tricyclo[5.2.1.02,6]dec-8-ene, which are useful for the synthesis of neplanocin A having strong antitumor activity. Improved processes for the preparation of neplanocin A, starting from optically active 2-hydroxymethyl-5-hydroxy-tricyclo[5.2.1.02,6]deca-3,8-diene and via a key step comprising a retro-Diels-Alder reaction of the above intermediate.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: September 5, 2006
    Assignee: Chisso Corporation
    Inventors: Naoyuki Yoshida, Kunio Ogasawara
  • Patent number: 7084289
    Abstract: This invention relates to the reversible protection of hydroxy-silane functional groups by acid cleavable protecting groups. The development of reversible protecting groups greatly enhances the current utility of silanes while introducing further novel applications. For instance, reversibly protected silanes are of particular value in applications where room temperature cure and/or adhesion is of value, such as coatings, high resolution imaging, caulks, adhesives, sealents, gaskets, and silicones. Reversibly protected silanes can also be beneficially used in reticulating agents, and in sizing agents, tires, and release coatings. The incorporation of reversibly protected silanes into coating resins is of particular value. The reversibly protected silane can be incorporated into the coating resin by polymerizing a monomer containing the reversibly protected silane into the resin or by post-addition into the coating formulation.
    Type: Grant
    Filed: December 1, 2003
    Date of Patent: August 1, 2006
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Daniel Edward Bowen, III, Eric Sean Castner
  • Patent number: 7078549
    Abstract: This invention relates to the reversible protection of hydroxy-silane functional groups by acid cleavable protecting groups. The development of reversible protecting groups greatly enhances the current utility of silanes while introducing further novel applications. For instance, reversibly protected silanes are of particular value in applications where room temperature cure and/or adhesion is of value, such as coatings, high resolution imaging, caulks, adhesives, sealents, gaskets, and silicones. Reversibly protected silanes can also be beneficially used in reticulating agents, and in sizing agents, tires, and release coatings. The incorporation of reversibly protected silanes into coating resins is of particular value. The reversibly protected silane can be incorporated into the coating resin by polymerizing a monomer containing the reversibly protected silane into the resin or by post-addition into the coating formulation.
    Type: Grant
    Filed: November 4, 2003
    Date of Patent: July 18, 2006
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Daniel Edward Bowen, III, Eric Sean Castner
  • Patent number: 7078538
    Abstract: A process for the preparation of 14 beta-hydroxy-1,4-carbonate-deacetylbaccatin III and intermediates useful for the preparation of novel taxan derivatives with antitumor activity are disclosed.
    Type: Grant
    Filed: October 26, 2004
    Date of Patent: July 18, 2006
    Assignee: INDENA S.p.A.
    Inventors: Alessandro Pontiroli, Ezio Bombardelli
  • Patent number: 7074866
    Abstract: This invention relates to the reversible protection of hydroxy-silane functional groups by acid cleavable protecting groups. The development of reversible protecting groups greatly enhances the current utility of silanes while introducing further novel applications. For instance, reversibly protected silanes are of particular value in applications where room temperature cure and/or adhesion is of value, such as coatings, high resolution imaging, caulks, adhesives, sealents, gaskets, and silicones. Reversibly protected silanes can also be beneficially used in reticulating agents, and in sizing agents, tires, and release coatings. The incorporation of reversibly protected silanes into coating resins is of particular value. The reversibly protected silane can be incorporated into the coating resin by polymerizing a monomer containing the reversibly protected silane into the resin or by post-addition into the coating formulation.
    Type: Grant
    Filed: November 6, 2003
    Date of Patent: July 11, 2006
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Daniel Edward Bowen, III, Eric Sean Castner
  • Patent number: 7067600
    Abstract: This invention relates to the reversible protection of hydroxy-silane functional groups by acid cleavable protecting groups. The development of reversible protecting groups greatly enhances the current utility of silanes while introducing further novel applications. For instance, reversibly protected silanes are of particular value in applications where room temperature cure and/or adhesion is of value, such as coatings, high resolution imaging, caulks, adhesives, sealents, gaskets, and silicones. Reversibly protected silanes can also be beneficially used in reticulating agents, and in sizing agents, tires, and release coatings. The incorporation of reversibly protected silanes into coating resins is of particular value. The reversibly protected silane can be incorporated into the coating resin by polymerizing a monomer containing the reversibly protected silane into the resin or by post-addition into the coating formulation.
    Type: Grant
    Filed: August 16, 2002
    Date of Patent: June 27, 2006
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Daniel Edward Bowen, III, Eric Sean Castner