Chalcogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 549/33)
  • Patent number: 9796728
    Abstract: Disclosed are a cyclic carbonate monomer containing a double-sulfur five-membered ring functional group, and preparation method thereof. The cyclic carbonate monomer can be simply and efficiently synthesized without protection and deprotection processes. The cyclic carbonate monomer of the present invention can be utilized to obtain polycarbonate having a controllable molecular weight and molecular weight distribution via ring opening polymerization, and has biodegradability and reduction-sensitive reversible crosslinking properties. The present invention can be used in a carrier having controllably released drug, a biological tissue scaffold or a biochip.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: October 24, 2017
    Assignee: Brightgene Bio-Medical Technology Co., Ltd.
    Inventors: Fenghua Meng, Yan Zou, Zhiyuan Zhong, Jiandong Yuan
  • Publication number: 20150037734
    Abstract: A resist composition containing a compound represented by general formula (m0), wherein R1 and R2 each independently represents an aryl group which may have a substituent, an alkyl group which may have a substituent, or an alkenyl group which may have a substituent, provided that R1 and R2 may be mutually bonded to form a ring with the sulfur atom; R3 represents an aromatic hydrocarbon group which may have a substituent, an alkenyl group which may have a substituent, or an alkynyl group which may have a substituent; V1 represents a single bond or an alkylene group, provided that, when R3 is an aromatic hydrocarbon group which may have a substituent, V1 is an alkylene group; and X0? represents a monovalent organic anion.
    Type: Application
    Filed: July 23, 2014
    Publication date: February 5, 2015
    Inventors: Takashi Nagamine, Yoshitaka Komuro, Masatoshi Arai, Yoshiyuki Utsumi
  • Patent number: 8946450
    Abstract: The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency.
    Type: Grant
    Filed: January 7, 2013
    Date of Patent: February 3, 2015
    Assignee: Duquesne University of the Holy Ghost
    Inventors: Partha Basu, Igor Pimkov
  • Patent number: 8933108
    Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
    Type: Grant
    Filed: September 5, 2012
    Date of Patent: January 13, 2015
    Assignee: Novartis AG
    Inventors: Jun Cao, Bernhard Erb, Robin Alec Fairhurst, Arnaud Grandeury, Shinji Hatakeyama, Magdalena Koziczak-Holbro, Xinzhong Lai, Philipp Lustenberger, Bernd Riebesehl, Nicola Tufilli, Thomas Ullrich, Xiang Wu, Jianguang Zhou
  • Patent number: 8722900
    Abstract: The present invention relates to processes for making cabazitaxel, cabazitaxel analogues and intermediates thereof. The invention provides novel compounds useful in the synthesis of cabazitaxel.
    Type: Grant
    Filed: October 30, 2012
    Date of Patent: May 13, 2014
    Assignee: ScinoPharm Taiwan, Ltd.
    Inventors: TsungYu Hsiao, Julian Paul Henschke, HsinChang Tseng
  • Publication number: 20140100242
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Application
    Filed: September 17, 2013
    Publication date: April 10, 2014
    Applicant: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie Bassler, Lee Swem
  • Patent number: 8618312
    Abstract: Production of a bicyclo[3.1.0]hexane derivative, useful as a metabotropic glutamate receptor modulator, becomes possible by a production method that includes converting a compound represented by Formula (II) into a compound represented by Formula (III) by reaction with an acyl group donor in the presence of a microorganism-derived enzyme, without using an expensive optically active trans hydroxy ester as a starting material and without employing a fluorination reaction requiring an ultralow temperature reaction. Furthermore, since asymmetric synthesis can be carried out in a stage closer to the final product, the production method is useful as a production method that can mass produce a bicyclo[3.1.0]hexane derivative.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: December 31, 2013
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Mitsuaki Hirotsuka, Joji Sasaki, Hiroaki Kamiyama, Motoko Oshida, Takaaki Ishii
  • Patent number: 8558012
    Abstract: A 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethyl group introduction agent that is effective as an intermediate in pharmaceutical and agrochemical synthesis, a production method thereof, and a production method of a monofluoromethyl group-containing compound using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative are provided. The 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative represented by the following general formula (1) (wherein R1, R2, R3, and R4 each independently represent a hydrogen atom, a straight-chain or branched alkyl group having 1 to 4 carbon atoms, a straight-chain or branched alkyloxy group having 1 to 4 carbon atoms, a halogen atom, a nitro group, or a cyano group), the production method thereof, and various monofluoromethyl group-containing compounds are manufactured using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethylating agent.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: October 15, 2013
    Assignees: Nagoya Institute of Technology, Tosoh P-Tech, Inc.
    Inventor: Norio Shibata
  • Patent number: 8486606
    Abstract: An acrylate derivative represented by the following general formula (1): (in the formula, R1 represents a hydrogen atom, a methyl group or a trifluoromethyl group; each of R2, R3, R5, R7, R8, R9 and R10 independently represents a hydrogen atom, an alkyl group, a cycloalkyl group or an alkoxy group; each of R4 and R6 independently represents a hydrogen atom, an alkyl group, a cycloalkyl group or an alkoxy group, or R4 and R6 are bonded to each other to represent an alkylene group, —O— or —S—; n represents 0, 1 or 2; and W represents an alkylene group or a cycloalkylene group); an intermediate thereof; a method for producing the same; a polymer compound which is obtainable from polymerization of a raw material containing the foregoing acrylate derivative and which is excellent in solubility in an organic solvent used for the preparation of a photoresist composition; and a photoresist composition containing the polymer compound, an organic solvent and a photo acid generator and having excellent adhesion to s
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: July 16, 2013
    Assignee: Kuraray Co., Ltd.
    Inventors: Junko Sato, Osamu Nakayama, Takashi Fukumoto
  • Patent number: 8481243
    Abstract: The present invention provides a resin comprising a structural unit represented by the formula (aa): wherein R1 represents a C1-C6 alkyl group optionally having one or more halogen atoms, a hydrogen atom or a halogen atom, T1 represents a C4-C34 sultone ring group optionally having one or more substituents, Z1 represents a C1-C6 alkanediyl group optionally having one or more substituents, or a group represented by the formula (a-1): -A10X10-A11sX11-A12-??(a-1) wherein X10 and X11 each independently represents —O—, —NH—, —CO—, —CO—O—, —O—CO—, —CO—NH— or —NH—CO—, A10, A11 and A12 each independently represent a C1-C5 divalent aliphatic hydrocarbon group optionally having one or more substituents, and s represents 0 or 1, and Z2 represents a single bond or —CO—.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: July 9, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hyungjoo Kim, Akira Kamabuchi, Koji Ichikawa
  • Patent number: 8471008
    Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex, which comprises a compound having a specific heterocyclic structure, is described. Also described is an organic electroluminescence device having an anode, a cathode and an organic thin film layer having one or more layers. The organic thin film layer is interposed between the anode and cathode and has a light emitting layer containing a host material in combination with at least one phosphorescent metal complex. At least one layer of the organic thin film layer contains the material for organic electroluminescence devices. The material for organic electroluminescence devices provides an organic electroluminescence device which has a high emitting efficiency, causes little pixel defects, is excellent in heat resistance, and show a long lifetime.
    Type: Grant
    Filed: November 25, 2011
    Date of Patent: June 25, 2013
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
  • Patent number: 8440639
    Abstract: Provided herein is a pharmaceutical composition or a kit comprising a combination of a carbonic anhydrase inhibitor analog and an adenosine A1 receptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of dorzolamide marketed under the brand Trusopt™ and Compound A.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: May 14, 2013
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley
  • Publication number: 20130116444
    Abstract: The present invention relates to processes for making cabazitaxel, cabazitaxel analogues and intermediates thereof. The invention provides novel compounds useful in the synthesis of cabazitaxel.
    Type: Application
    Filed: October 30, 2012
    Publication date: May 9, 2013
    Applicant: Scinopharm Taiwan, LTD.
    Inventor: Scinopharm Taiwan, LTD.
  • Patent number: 8420831
    Abstract: The present invention relates to a process for preparing 1-O-acyl-2-deoxy-2-fluoro-4-thio-?-D-arabinofuranoses having formula I and intermediates thereof: wherein R1 represents —C(O)—C1-C6-alkyl or —C(O)-aryl; and R2 represents C1-C6-alkyl, C1-C4-perfluoroalkyl or aryl.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: April 16, 2013
    Assignee: LIBRAMEDICINA, Inc.
    Inventors: David Voigtländer, Michael Sander, Michael Harre
  • Publication number: 20130078233
    Abstract: Compounds having one or more phenol moieties, derivatives thereof, compositions containing same and uses thereof for the treatment of amyloid-associated diseases are provided.
    Type: Application
    Filed: November 27, 2012
    Publication date: March 28, 2013
    Applicant: Tel Aviv University Future Technology Development L.P.
    Inventor: Tel Aviv University Future Technology Development
  • Patent number: 8378123
    Abstract: The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency.
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: February 19, 2013
    Assignee: Duquesne University of the Holy Ghost
    Inventors: Partha Basu, Igor Pimkov
  • Patent number: 8372880
    Abstract: Compounds having one or more phenol moieties, derivatives thereof, compositions containing same and uses thereof for the treatment of amyloid-associated diseases are provided.
    Type: Grant
    Filed: March 23, 2006
    Date of Patent: February 12, 2013
    Assignee: Tel Aviv University Future Technology Development L.P.
    Inventors: Ehud Gazit, Yair Porat
  • Patent number: 8367849
    Abstract: There is provided a means to produce industrially a highly pure 2-hydroxy-4-oxa-5-thiatricyclo[4.2.1.03,7]nonane 5,5-dioxide derivative in high yield from highly pure and industrially available raw materials. The production method for a sultone derivative of the present invention comprises a step (A) to obtain a sulfonic acid derivative by hydrolyzing a sulfonyl halide derivative represented by the following chemical formula 1: or an enantiomer thereof and a step (B) to obtain a corresponding sultone derivative represented by the following chemical formula 2: or an enantiomer thereof by treating the sulfonic acid derivative with a oxidizing agent.
    Type: Grant
    Filed: September 2, 2009
    Date of Patent: February 5, 2013
    Assignee: Kuraray Co., Ltd.
    Inventors: Osamu Nakayama, Takashi Fukumoto, Jyunko Sato, Toshiki Endo, Hideki Matsuda
  • Publication number: 20130005991
    Abstract: The present invention relates to a process for preparing 1-O-acyl-2-deoxy-2-fluoro-4-thio-?-D-arabinofuranoses having formula I and intermediates thereof: wherein R1 represents —C(O)—C1-C6-alkyl or —C(O)-aryl; and R2 represents C1-C6-alkyl, C1-C4-perfluoroalkyl or aryl.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 3, 2013
    Applicant: LibraMedicina, Inc.
    Inventors: David VOIGTLÄNDER, Michael SANDER, Michael HARRE
  • Publication number: 20120245168
    Abstract: The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency.
    Type: Application
    Filed: March 25, 2011
    Publication date: September 27, 2012
    Applicant: DUQUESNE UNIVERSITY OF THE HOLY GHOST
    Inventors: Partha Basu, Igor Pimkov
  • Patent number: 8197722
    Abstract: Compositions capable of simultaneous two-photon absorption and higher order absorptivities are provided. Compounds having a donor-pi-donor or acceptor-pi-acceptor structure are of particular interest, where the donor is an electron donating group, acceptor is an electron accepting group, and pi is a pi bridge linking the donor and/or acceptor groups. The pi bridge may additionally be substituted with electron donating or withdrawing groups to alter the absorptive wavelength of the structure. Also disclosed are methods of generating an excited state of such compounds through optical stimulation with light using simultaneous absorption of photons of energies individually insufficient to achieve an excited state of the compound, but capable of doing so upon simultaneous absorption of two or more such photons. Applications employing such methods are also provided, including controlled polymerization achieved through focusing of the light source(s) used.
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: June 12, 2012
    Assignee: The California Institute of Technology
    Inventors: Seth Marder, Joseph Perry
  • Publication number: 20120122849
    Abstract: Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.
    Type: Application
    Filed: November 4, 2011
    Publication date: May 17, 2012
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Publication number: 20110319637
    Abstract: A 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethyl group introduction agent that is effective as an intermediate in pharmaceutical and agrochemical synthesis, a production method thereof, and a production method of a monofluoromethyl group-containing compound using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative are provided. The 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative represented by the following general formula (1) (wherein R1, R2, R3, and R4 each independently represent a hydrogen atom, a straight-chain or branched alkyl group having 1 to 4 carbon atoms, a straight-chain or branched alkyloxy group having 1 to 4 carbon atoms, a halogen atom, a nitro group, or a cyano group), the production method thereof, and various monofluoromethyl group-containing compounds are manufactured using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethylating agent.
    Type: Application
    Filed: February 12, 2010
    Publication date: December 29, 2011
    Inventor: Norio Shibata
  • Patent number: 8080658
    Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex contains a compound represented by formula 1: wherein R1 to R10 are each independently hydrogen atom, halogen atom, alkyl group having 1 to 40 carbon atoms, cycloalkyl group having 3 to 15 carbon atoms, heterocyclic group having 3 to 20 carbon atoms which is optionally substituted, alkoxy group having 1 to 40 carbon atoms, non-condensed aryl group having 6 to 40 carbon atoms, condensed aryl group having 10 to 18 carbon atoms, aryloxy group having 6 to 20 carbon atoms, aralkyl group having 7 to 20 carbon atoms, arylamino group having 6 to 40 carbon atoms, alkylamino group having 1 to 40 carbon atoms, aralkylamino group having 7 to 60 carbon atoms, arylcarbonyl group having 7 to 40 carbon atoms, alkyl halide group having 1 to 40 carbon atoms, or cyano group, R8 and R9 being optionally bonded to each other to form a ring structure and each of R1 to R10 being optionally
    Type: Grant
    Filed: July 10, 2007
    Date of Patent: December 20, 2011
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
  • Publication number: 20110160465
    Abstract: There is provided a means to produce industrially a highly pure 2-hydroxy-4-oxa-5-thiatricyclo[4.2.1.03,7]nonane 5,5-dioxide derivative in high yield from highly pure and industrially available raw materials. The production method for a sultone derivative of the present invention comprises a step (A) to obtain a sulfonic acid derivative by hydrolyzing a sulfonyl halide derivative represented by the following chemical formula 1: or an enantiomer thereof and a step (B) to obtain a corresponding sultone derivative represented by the following chemical formula 2: or an enantiomer thereof by treating the sulfonic acid derivative with a oxidizing agent.
    Type: Application
    Filed: September 2, 2009
    Publication date: June 30, 2011
    Applicant: KURARAY CO., LTD
    Inventors: Osamu Nakayama, Takashi Fukumoto, Jyunko Sato, Toshiki Endo, Hideki Matsuda
  • Patent number: 7955816
    Abstract: The present invention relates to the synthesis and characterization of biotinylated analogue of N-arachidonoylethanolamine (AEA) and its use as a tool to study AEA transport and trafficking through biochemical and morphological techniques. In particular biotinylated AEA (b-AEA, for which we propose the common name MM22) is suitable to design highly sensitive and simple methods for the non-radioactive detection and quantitation of AEA from complex samples, which would offer a useful alternative approach to the routinely used radiometric assays. The invention also relates to the use of b-AEA as a potential therapeutic and diagnostic agent.
    Type: Grant
    Filed: May 2, 2006
    Date of Patent: June 7, 2011
    Assignees: Universita Degli Studi Di Roma “Tor Vergata”, Universita Degli Studi Di Teramo
    Inventors: Mauro Maccarrone, Sergio Oddi, Filomena Fezza, Alessandro Finazzi Agro′
  • Publication number: 20110039819
    Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: April 9, 2009
    Publication date: February 17, 2011
    Inventors: Marion Hitchcock, Ingo Hartung
  • Publication number: 20100160411
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of R1, R2, R3, R4, y, n, m, p, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
    Type: Application
    Filed: October 24, 2007
    Publication date: June 24, 2010
    Applicant: Wyeth
    Inventors: Gary Paul Stack, Ivana Bianchi, Stefania Vallese, Giovanna Luoni
  • Publication number: 20090218039
    Abstract: An dye compound of the following formula (1): wherein D represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group; L represents ?CR2—, ?N—, or ?N—NH—; R1 represents a monovalent substituent; R2 represents a hydrogen atom or a cyano group; n indicates an integer of from 0 to 4; when n is 2 or more, then plural R1's may be the same or different.
    Type: Application
    Filed: February 27, 2009
    Publication date: September 3, 2009
    Applicant: FUJIFILM Corporation
    Inventors: Yoshihiko FUJIE, Tetsuya WATANABE, Hisashi MIKOSHIBA
  • Patent number: 7211592
    Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydro-benzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.
    Type: Grant
    Filed: September 13, 2004
    Date of Patent: May 1, 2007
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Stefan Petry, Karl-Heinz Baringhaus, Swen Hoelder, Guenter Mueller
  • Patent number: 7176317
    Abstract: Compounds of the formula wherein R1, R2, R3, R4, R5, R6, R7, a, b, c, d, Y, Q, Q—, A, and CA are as defined herein.
    Type: Grant
    Filed: June 26, 2003
    Date of Patent: February 13, 2007
    Assignee: Xerox Corporation
    Inventors: Jeffery H. Banning, Bo Wu, James M. Duff, Wolfgang G. Wedler, Donald R. Titterington
  • Patent number: 6958358
    Abstract: Compounds of general formula (I): wherein R1, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.
    Type: Grant
    Filed: January 17, 2002
    Date of Patent: October 25, 2005
    Assignee: Amura Therapeutics Limited
    Inventors: Martin Quibell, Manoj Kumar Ramjee
  • Publication number: 20030191161
    Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydrobenzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.
    Type: Application
    Filed: March 31, 2003
    Publication date: October 9, 2003
    Inventors: Stefan Petry, Karl-Heinz Baringhaus, Swen Hoelder, Guenter Mueller
  • Patent number: 6605632
    Abstract: The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: August 12, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Daniel Lesieur, Frédérique Klupsch, Gérald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Patent number: 6420130
    Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.
    Type: Grant
    Filed: April 28, 1999
    Date of Patent: July 16, 2002
    Assignee: Aurora Biosciences Corporation
    Inventors: Lewis R. Makings, Gregor Zlokarnik
  • Publication number: 20020055523
    Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydro-benzo [c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.
    Type: Application
    Filed: August 9, 2001
    Publication date: May 9, 2002
    Inventors: Stefan Petry, Karl-Heinz Baringhaus, Swen Hoelder, Guenter Mueller
  • Patent number: 6380235
    Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstitut
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: April 30, 2002
    Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.
    Inventors: Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Patent number: 6130101
    Abstract: The present invention describes xanthene dyes, including rhodamines, rhodols and fluoresceins that are substituted one or more times by a sulfonic acid or a salt of a sulfonic acid. The dyes of the invention, including chemically reactive dyes and dye-conjugates are useful as fluorescent probes, particularly in biological samples.
    Type: Grant
    Filed: September 23, 1997
    Date of Patent: October 10, 2000
    Assignee: Molecular Probes, Inc.
    Inventors: Fei Mao, Wai-Yee Leung, Richard P. Haugland
  • Patent number: 5932731
    Abstract: The present invention provides a process for preparing an aromatic or heteroaromatic thiol represented by the formula (2), the process comprising hydrolyzing an aromatic or heteroaromatic halogenated methyl sulfide represented by the formula (1)Ar.paren open-st.SCH.sub.3-m X.sub.m).sub.n (1)Ar.paren open-st.SH).sub.n (2)wherein Ar is an aromatic or heteroaromatic ring which has no substituent or which has an optional substituent or substituents, X is a halogen atom, m is an integer of 1 to 3 and n is 1 or 2.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: August 3, 1999
    Assignee: Sumitomo Seika Chemicals Co., Ltd.
    Inventors: Hiroshi Goda, Mikio Yamamoto, Jun-ichi Sakamoto, Hitoshi Karino
  • Patent number: 5925759
    Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive intermediates.
    Type: Grant
    Filed: September 5, 1997
    Date of Patent: July 20, 1999
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Srinivasan Babu, Bennett C. Borer, Travis P. Remarchuk, Robert J. Szendroi, Kathleen R. Whitten, Juliette K. Busse, Kim F. Albizati
  • Patent number: 5817639
    Abstract: The present invention provides a novel purine 4'-thioarabinonucleoside represented by the following formula ?1!: ##STR1## wherein B represents a purine base other than adenine. Also disclosed are a method for preparing the purine 4'-thioarabinonucleoside and pharmaceutical compositions containing the purine 4'-thioarabinonucleoside.
    Type: Grant
    Filed: July 12, 1996
    Date of Patent: October 6, 1998
    Assignee: Yamasa Corporation
    Inventors: Mikari Watanabe, Yuichi Yoshimura, Shinji Sakata, Noriyuki Ashida, Haruhiko Machida
  • Patent number: 5763483
    Abstract: Novel carbocyclic compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
    Type: Grant
    Filed: December 27, 1996
    Date of Patent: June 9, 1998
    Assignee: Gilead Sciences, Inc.
    Inventors: Norbert W. Bischofberger, Choung U. Kim, Willard Lew, Hongtao Liu, Matthew A. Williams
  • Patent number: 5728696
    Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: March 17, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
  • Patent number: 5723486
    Abstract: Disclosed are 1,3-dithiolo(4,5-d)-1,3-dithiino-2-thione compounds corresponding to one of the formulae: ##STR1## wherein R.sup.1 represents --Br, --Cl, --F, --CN or --CH(CH.sub.2).sub.n CH.sub.3 and n is an integer of from 0 to 10.These compounds as well as the unsubstituted compound have been found to exhibit antimicrobial and marine antifouling activity in industrial and commercial applications and compositions containing these compounds are so employed.
    Type: Grant
    Filed: July 10, 1996
    Date of Patent: March 3, 1998
    Assignee: The Dow Chemical Company
    Inventors: Weishi W. Wu, Duane R. Romer, Ravi B. Shankar, R. Garth Pews
  • Patent number: 5716624
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: February 10, 1998
    Assignee: C.I.R.D. Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5693460
    Abstract: This invention provides a silver halide photographic element comprising a silver halide emulsion in reactive association with a dioxide compound represented by the following formula: ##STR1## wherein b is C(O), C(S), C(Se), CH2 or (CH2)2; and R.sup.1 and R.sup.2 are independently H, or aliphatic, aromatic or heterocyclic groups, or R.sup.1 and R.sup.2 together represent the atoms necessary to form a five or six-membered ring or a multiple ring system. This invention further provides a method of making silver halide emulsions containing the dioxide compounds.
    Type: Grant
    Filed: June 24, 1996
    Date of Patent: December 2, 1997
    Assignee: Eastman Kodak Company
    Inventor: Roger Lok
  • Patent number: 5684152
    Abstract: Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. This invention relates to a process of making the carboxy-peptidyl compounds of formula I.
    Type: Grant
    Filed: September 19, 1996
    Date of Patent: November 4, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Mitree M. Ponpipom, William K. Hagmann
  • Patent number: 5672620
    Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is hydrogen or straight, branched or cyclic alkyl, aryl, hydroxy or alkoxy; and(f) R.sub.1 and R.sub.2 are independently hydrogen or straight, branched or cyclic alkyl having from one to 10 carbon atoms, aryl, heterocyclyl, heteroaryl, hydroxy, or alkoxy; or R.sub.1 and R.sub.2 are bonded together to form a ring having from from 3 to about 7 atoms wherein one to three atoms may be heteroatoms.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.
    Type: Grant
    Filed: February 1, 1996
    Date of Patent: September 30, 1997
    Assignee: The Procter & Gamble Company
    Inventors: Michael Wiard Scherz, Laurence Ichih Wu
  • Patent number: 5605924
    Abstract: The present invention relates to compounds of the formula ##STR1## where X is a bond or --CH2--;R.sup.2 is pyrrolidino;R is OH, --OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3 or ##STR2## R.sup.1 is hydrogen, OH, fluoro, chloro, --OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3 or ##STR3## each R.sup.3 is independently C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, unsubstituted or substituted phenyl where the substituent is fluoro, chloro, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy;each n is independently 3, 4 or 5; and pharmaceutically acceptable salts and solvates thereof; provided that at least one of R and R.sup.1 is ##STR4## The invention also relates to methods of use of the compounds of formula I and pharmaceutical compositions which comprise compounds of formula I.
    Type: Grant
    Filed: January 17, 1996
    Date of Patent: February 25, 1997
    Assignee: Eli Lilly and Company
    Inventors: Larry J. Black, Henry U. Bryant, George J. Cullinan
  • Patent number: 5591722
    Abstract: 2'-Deoxy-4'-thio-ribonucleosides, intermediates in their production, and their use as antiviral and anticancer agents are disclosed.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: January 7, 1997
    Assignee: Southern Research Institute
    Inventors: John A. Montgomery, John A. Secrist, III