The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Of Diverse Chalcogens Patents (Class 546/341)
  • Patent number: 10214516
    Abstract: Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: February 26, 2019
    Assignee: VIIV HEALTHCARE UK (NO.5) LIMITED
    Inventors: John F. Kadow, B. Narasimhulu Naidu, Tao Wang, Zhiwei Yin, Zhongxing Zhang
  • Publication number: 20150018515
    Abstract: A method of producing an epoxy compound, which comprises reacting hydrogen peroxide with a compound having a carbon-carbon double bond, in the presence of at least one of a tungsten compound and a molybdenum compound; and an onium salt comprising 20 or more carbon atoms and one or more of substituents convertible to a functional group containing an active hydrogen or a salt thereof.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 15, 2015
    Applicant: MITSUBISHI CHEMICAL CORPORATION
    Inventors: Akemi HOSOKAWA, Haruhiko KUSAKA
  • Publication number: 20140364586
    Abstract: Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.
    Type: Application
    Filed: June 26, 2014
    Publication date: December 11, 2014
    Inventors: Andrew Graham WATTS, Terrence Kantner, Amanda Barbara MacKenzie
  • Publication number: 20140343284
    Abstract: A compound of Formula 2 is disclosed wherein R1, MA and MB are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 1 wherein RI and X are as defined in the disclosure comprising contacting a compound of Formula 2 with a halogenating agent. Also disclosed is a method for preparing a compound of Formula 4 wherein R1, R3 and R4 are as defined in the disclosure, comprising reacting a compound of Formula 5 wherein R3 and R4 are as defined in the disclosure with a compound of Formula 1, with a compound of Formula 1, the process of preparing the compound of Formula 4 includes the step of preparing the compound of Formula 1 from the compound of Formula 2 by the method disclosed above. Also disclosed is compound that is methyl 3,5-dichlorobenzeneethanimidate methyl 3,5-dichlorobenzeneethanimidate or ethyl 3,5-dichlorobenzeneethanimidate or salts thereof.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 20, 2014
    Inventor: Wenming Zhang
  • Patent number: 8835409
    Abstract: 3-Alkenyl-6-halo-4-aminopicolinic acids and their derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: September 16, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Paul R. Schmitzer, Thomas L. Siddall
  • Publication number: 20140221330
    Abstract: An objective of the present invention is to provide a novel NDM (New Delhi metallo-?-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of ?-lactam antibiotics that have been inactivated as a result of decomposition by NDM.
    Type: Application
    Filed: July 26, 2012
    Publication date: August 7, 2014
    Inventors: Akihiro Morinaka, Kazunori Maebashi, Takashi Ida, Muneo Hikida, Mototsugu Yamada, Takao Abe
  • Patent number: 8585930
    Abstract: A quaternary nitrogen-containing corrosion inhibitor of formula wherein is an aromatic, nitrogen-containing ring of 5 to 14 ring atoms, optionally containing an additional N, O or S ring atom and optionally substituted with one or more alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, amino, aminoalkyl, alkoxy, hydroxylalkyl, or cyano groups, or a mixture thereof; Y is a group of formula —OC(O)R1 or —C(O)R1; L is C1-C10 alkyl, C2-C10 alkenyl or a group of formula —CH2CH(OR2)CH2—; R1 is C8-C20 alkyl or C8-C20 alkenyl; R2 is H or —C(O)R1; R3 and R4 are independently selected from H, alkyl, alkenyl, amino, alkoxy, hydroxylalkyl and cyano; and X is Br, Cl or I is particularly useful for inhibiting corrosion in oil and gas field applications.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: November 19, 2013
    Assignee: Nalco Company
    Inventor: Laxmikant Tiwari
  • Patent number: 8338441
    Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: December 25, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Christiane Yoakim, Murray Bailey, Francois Bilodeau, Rebekah Carson, Lee Fader, Stephen Kawai, Sebastien Morin, Carl Thibeault, Bruno Simoneau, Simon Surprenant, Youla Tsantrizos, Steven Laplante
  • Publication number: 20120322769
    Abstract: A method of reducing virulence in a bacterium comprising at least one of a GacS/GacA-type system, a HrpX/HrpY-type system, a T3SS-type system, and a Rsm-type system, the method comprising contacting the bacterium with an effective amount of a compound described herein.
    Type: Application
    Filed: February 16, 2011
    Publication date: December 20, 2012
    Applicants: DUKE UNIVERSITY, UWM RESEARCH FOUNDATION
    Inventors: Ching-Hong Yang, Xin Chen, Eric J. Toone
  • Publication number: 20120289403
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Application
    Filed: November 11, 2010
    Publication date: November 15, 2012
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Patent number: 8293899
    Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: October 23, 2012
    Assignee: Lanxess Deutschland GmbH
    Inventors: Boris Bosch, Markus Eckert, Hans-Christian Militzer, Claus Dreisbach
  • Publication number: 20120102826
    Abstract: A diesel fuel additive composition, a fuel containing the fuel additive, a method for improving diesel engine performance using the additive. The diesel fuel additive includes a reaction product of (a) a hydrocarbyl-substituted acylating agent and (b) a reactant selected from the group consisting of a nitrogen-containing compound, a hydroxyl-containing compound, and water that provides a reaction product selected from the group consisting (1) a mono-amide/mono-acid or metal free mono-acid salt thereof, (2) a diacid or metal free diacid salt thereof, and (3) mono-ester/mono-acid or metal free mono-acid salt thereof. The reaction product includes at least about 10 molar percent acid groups based on total moles of the reaction product.
    Type: Application
    Filed: November 3, 2010
    Publication date: May 3, 2012
    Applicant: AFTON CHEMICAL CORPORATION
    Inventor: Xinggao FANG
  • Patent number: 8168734
    Abstract: The invention relates to compounds represented by Formula (1): wherein Ra is independently halogen, cyano, —CF3, —CF2H, —CFH2, —OCF3, —OCF2H, —N?C?O, —N?C?S or alkyl having a carbon number of approximately 1 to approximately 20; in the alkyl, optional —CH2— may be substituted with —O—, —S—, —SO2—, —CO—, —COO—, —OCO—, —CH?CH—, —CF?CF— or —C?C—, and optional hydrogen may be substituted with halogen; Rb is fluorine or —CF3; A is independently 1,4-cyclohexylene, 1,4-cyclohexenylene, 1,4-phenylene, naphthalene-2,6-diyl, tetrahydronaphthalene-2,6-diyl, fluorene-2,7-diyl or bicyclo[2.2.
    Type: Grant
    Filed: February 23, 2011
    Date of Patent: May 1, 2012
    Assignees: JNC Corporation, Chisso Petrochemical Corporation
    Inventor: Takashi Kato
  • Patent number: 8158021
    Abstract: A polymerizable liquid crystal compound shown by the following formula (I), a polymerizable liquid crystal composition that includes the polymerizable liquid crystal compound and a chiral compound polymerizable with the polymerizable liquid crystal compound, a liquid crystalline polymer obtained by polymerizing the polymerizable liquid crystal compound or the polymerizable liquid crystal composition, and an optical anisotropic article that includes the liquid crystalline polymer. The polymerizable liquid crystal compound shows a liquid crystal phase over a wider temperature range, is chemically stable, can be inexpensively produced, and has a wide selective reflection wavelength band ?? (i.e., a large value ?n).
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: April 17, 2012
    Assignee: Zeon Corporation
    Inventors: Kei Sakamoto, Naoto Kogoshi, Yoshihide Yachi
  • Publication number: 20120088784
    Abstract: The present invention relates to substituted aromatic compounds of Formula I and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds in the prevention and/or treatment of various diseases and conditions in subjects, including the prevention or treatment of (i) blood disorders, (ii) renal disorders, a nephropathies, or renal disorder complications; (iii) inflammatory-related diseases; and/or (iv) oxidative stress related disorders.
    Type: Application
    Filed: November 4, 2011
    Publication date: April 12, 2012
    Inventors: Boulos Zacharie, Christopher Penney, Lyne Gagnon, Jean-François Bienvenu, Valérie Perron, Brigitte Grouix
  • Publication number: 20120071457
    Abstract: A new metallo-?-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of ?-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-?-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of ?-lactam antibiotics against metallo-?-lactamase producing bacteria by combining the compound of the general formula (I) with ?-lactam antibiotics.
    Type: Application
    Filed: November 29, 2011
    Publication date: March 22, 2012
    Inventors: Ken Chikauchi, Mizuyo Ida, Takao Abe, Yukiko Hiraiwa, Akihiro Morinaka, Toshiaki Kudo
  • Patent number: 8026239
    Abstract: A method of treating a malignant tumor selected from the group consisting of leukemia, colorectal cancer, ovarian cancer, oral cancer, lung carcinoma, breast carcinoma, prostate carcinoma, and melanoma by administering to a patient in need thereof an effective amount of at least one compound represented by formula (1) wherein A, X, Q, R1-3, and n are defined herein.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: September 27, 2011
    Assignee: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
  • Publication number: 20110165087
    Abstract: The present invention relates to nitroxide imaging probes that are isotopically modified or unmodified. Such nitroxide imaging probes may be included in liposomes that encapsulate self-quenching concentrations thereof, wherein the liposomes optionally comprise a targeting ligand specific to and having affinity for targeted tissue.
    Type: Application
    Filed: December 22, 2010
    Publication date: July 7, 2011
    Inventors: JOSEPH P.Y. KAO, SCOTT R. BURKS, GERALD R. ROSEN
  • Patent number: 7923446
    Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: April 12, 2011
    Assignee: Wyeth LLC
    Inventors: Jason Shaoyun Xiang, Steve Yikkai Tam, Yonghan Hu, Phaik-Eng Sum, David Brian How, Darrin William Hopper, Matthew Douglas Vera, Joshua James Sabatini, Thomas Saltmarsh Rush, III, Elisabeth Ann Morris, Katy Evangelia Georgiadis
  • Patent number: 7919648
    Abstract: The invention relates to compounds represented by Formula (1): wherein Ra is alkyl or the like; Rb is fluorine or —CF3; A is 1,4-cyclohexylene, 1,4-phenylene or the like; Z is a single bond, alkylene or the like; Y is a single bond, alkylene or the like; and m and n are an integer of approximately 0 to approximately 5.
    Type: Grant
    Filed: December 7, 2006
    Date of Patent: April 5, 2011
    Assignees: Chisso Corporation, Chisso Petrochemical Corporation
    Inventor: Takashi Kato
  • Patent number: 7816367
    Abstract: The present invention provides compounds useful, for example, for modulating insulin levels in a subject and that have the general formula Q-L1-P-L2-M-X-L3-A wherein the definitions of the variables Q, L1, P, L2, M, X, L3 and A are provided herein. The present invention also provides compositions and methods for use of the compounds, for instance, for treatment of type II diabetes.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: October 19, 2010
    Assignee: Amgen Inc.
    Inventors: Michelle Akerman, Jonathan Houze, Daniel C. H. Lin, Jiwen Liu, Jian Luo, Julio C. Medina, Wei Qiu, Jeffrey D. Reagan, Rajiv Sharma, Stephen J. Shuttleworth, Ying Sun, Jian Zhang, Liusheng Zhu, Jinqian Liu, Zhihua Ma, Yingcai Wang, Michael J. Schmitt
  • Publication number: 20090312355
    Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.
    Type: Application
    Filed: August 1, 2007
    Publication date: December 17, 2009
    Applicant: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-Sen Lai
  • Publication number: 20090312354
    Abstract: The present invention relates to a docosahexaenoic acid ester with an alcohol chosen among the group-B vitamins or provitamins, advantageously comprised by: nicotinyl alcohol of the following formula (I), panthenol of the following formula (II), and inositol of the following formula (III) or with isosorbide of the following formula (IV) or isosorbide mononitrate of the following formula (V). It also relates to a method of preparation of same, a pharmaceutical composition comprising same and the use of same in the treatment or prevention of cardiovascular disease, in particular auricular fibrillation.
    Type: Application
    Filed: June 22, 2007
    Publication date: December 17, 2009
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Frédérique Brune, André Delhon, Jean Gardette, Jean François Patoiseau, Alain Marty, Etienne Severac
  • Publication number: 20090241221
    Abstract: Methods and compositions reduce growth of Geminiviruses employing a compound with the following structure: or a pharmaceutical salt. The invention inactivates viruses by attacking the zinc finger domain in plants through Picolinic Acid (PA) and then ejecting the Zn2+ from the zinc finger proteins (ZFPs). The PA and derivatives control viruses containing essential ZFPs. A Tandem Repeated Sequence (TRS) technology, denoted the Cassette TRS construct method, produces syngenic plants with increased virus resistance. This technology incorporates into the plant genome tandem repeated stable DNA coding for enzymes that produce PA or derivatives. The increased production of PA, induced by a TRS viral protein promoter present in the Cassette TRS construct, disrupts the viral ZFPs for replication. The syngenic plants with the cassette TRS construct are genetically stable, flower and seed producing, and capable of producing new TRS syngenic plants.
    Type: Application
    Filed: March 19, 2008
    Publication date: September 24, 2009
    Inventors: Jose Alberto Fernandez-Pol, Sebastian Fernandez-Pol
  • Patent number: 7459415
    Abstract: Embodiments relate to lubricants disposed over magnetic storage media, such as rotatable thin film magnetic discs. One embodiment comprises a lubricant compound of a fluoropolyether chain having one or more carbonyl-imide pairs. For example, the carbonyl-imide pair may be located at one end, both ends, and/or in the middle of the fluoropolyether chain.
    Type: Grant
    Filed: October 13, 2004
    Date of Patent: December 2, 2008
    Assignee: Seagate Technology LLC
    Inventors: Jianwei Liu, Michael Joseph Stirniman, Jing Gui
  • Publication number: 20080221333
    Abstract: The present invention relates to a process for preparing a beta-keto ester compound of formula (1), which is an intermediate for the synthesis of quinolone antibiotics. Particularly, the present invention is characterized by the reaction of an organo nitrile compound with a salt of mono-alkyl malonate in the presence of metal salt, and so the reaction is easy to control due to its endothermic nature, and is devoid of lachrymatory reagents with excellent reproducibility. Subsequent in situ hydrolysis in the presence of aqueous acid solution provided the compound of formula (1).
    Type: Application
    Filed: September 15, 2006
    Publication date: September 11, 2008
    Inventors: Hyun Ik Shin, Bo Seung Choi, Jae Hoon Lee
  • Patent number: 7321044
    Abstract: The invention relates to intermediate products and a new process for the production of benzocycloheptene C. The process for the production of its new intermediate products according to the invention starts from economical starting materials, provides the intermediate stages in high yields and high purity, without chromatographic purification steps, and allows production on an industrial scale.
    Type: Grant
    Filed: October 15, 2002
    Date of Patent: January 22, 2008
    Assignee: Schering Aktiengesellschaft
    Inventors: Johannes Platzek, Wolfgang Beckmann, Jens Geisler, Holger Kirstein, Ulrich Niedballa, Eckhard Ottow, Sigmar Radau, Claudia Schulz, Thomas Wessa
  • Patent number: 7268135
    Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
    Type: Grant
    Filed: December 1, 2004
    Date of Patent: September 11, 2007
    Assignee: Wyeth
    Inventors: Jason Shaoyun Xiang, Steve Yikkai Tam, Yonghan Hu, Phaik-Eng Sum, David Brian How, Darrin William Hopper, Matthew Douglas Vera, Joshua James Sabatini, Thomas Saltmarsh Rush, III
  • Patent number: 7247732
    Abstract: The present invention provides a method for producing an optically active ?-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.
    Type: Grant
    Filed: June 12, 2006
    Date of Patent: July 24, 2007
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Toru Yamano, Naohiro Taya, Akio Ojida
  • Patent number: 7157458
    Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.
    Type: Grant
    Filed: January 31, 2002
    Date of Patent: January 2, 2007
    Assignee: Cryolife, Inc.
    Inventors: Carl W. Gilbert, Eleanor B. McGowan, Kirby S. Black, T. Gregory P. Harper
  • Patent number: 7071175
    Abstract: The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds: to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.
    Type: Grant
    Filed: May 3, 2000
    Date of Patent: July 4, 2006
    Assignee: Astrazeneca AB
    Inventors: Marcel Linschoten, Magnus Polla
  • Patent number: 7067501
    Abstract: The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.
    Type: Grant
    Filed: May 20, 2004
    Date of Patent: June 27, 2006
    Assignee: H. Lundbeck A/S
    Inventors: Garrick P. Smith, Gitte Mikkelsen, Kim Andersen, Daniel Greve, Thomas Ruhland, Stephen P. Wren
  • Patent number: 7037914
    Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.
    Type: Grant
    Filed: September 23, 2002
    Date of Patent: May 2, 2006
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
  • Patent number: 6969768
    Abstract: A process for preparing 4-haloalkylnicotinic esters of the formula (I), where RF is (C1-C4)-haloalkyl and R is (C1-C6)-alkyl; which comprises a) reacting an aminoketone of the formula (II), RF—C(O)—CH?CH—NH2 ??(II) ?in a condensation reaction under reduced pressure with a compound of the formulae (III) to (V), (R1Z)CH?CH—COOR??(III), (R1Z)2CH—CH2—COOR??(IV), HC?C—COOR??(V), where R1 is (C1-C6)-alkyl and Z is O, S, NR1 or C(O)O, ?to give a compound of the formulae (VI) and/or (VII), RF—C(O)—CH?CH—NH—CH?CH—COOR??(VI) RF—C(O)—CH?CH—NH—CH(ZR1)—CH2—COOR??(VII) b) and subjecting the reaction product to a ring closure reaction.
    Type: Grant
    Filed: September 9, 2002
    Date of Patent: November 29, 2005
    Assignee: Bayer CropScience GmbH
    Inventor: Sergiy Pazenok
  • Publication number: 20040249154
    Abstract: A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt.
    Type: Application
    Filed: July 14, 2004
    Publication date: December 9, 2004
    Inventors: Guang-Pei Chen, Prasad Koteswara Kapa, Eric M. Loeser, Ulrich Beutler, Werner Zaugg, Michael J. Girgis
  • Publication number: 20040248919
    Abstract: The present invention relates to a method of modulating retinoid X receptor activity in a mammal, novel compounds and pharmaceutical compositions for modulating retinoid X receptor activity in a mammal, and methods of making compounds that modulate retinoid X receptor activity in a mammal. The compounds are represented by Structural Formula 1: The compounds of Structural Formual 1 are efficacious insulin sensitizers and do not have the undesirable side effects of increasing triglycerides or suppressing the thyroid hormone axis.
    Type: Application
    Filed: April 15, 2004
    Publication date: December 9, 2004
    Inventors: Michael Gregory Bell, Timothy Alan Grese, Douglas Linn Gernett, Nathan P. Yumibe, Marcus F. Boehm, Pierre-Yves Michellys, Robert J. Ardecky, Christopher M Mapes, Jyun-Hung Chen, John S. Tyhonas, Lawrence G. Hamann
  • Publication number: 20040214827
    Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Application
    Filed: June 5, 2003
    Publication date: October 28, 2004
    Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
  • Publication number: 20040204594
    Abstract: This invention relates to preparation of enantio-enriched compounds, and more particularly to enantio-enriched kavalactone compounds and derivatives thereof. The methods provide compounds that are useful as reagents, or building blocks, in the construction of other enantio-enriched compounds.
    Type: Application
    Filed: January 12, 2004
    Publication date: October 14, 2004
    Inventors: Shoujun Chen, Lijun Sun, Joel McCleary
  • Patent number: 6780997
    Abstract: Pharmaceutical compositions including an effective amount of the compound of formula IV in which R1 is hydrogen or alkyl; R2 is —CHO, —CH2OH, —CH3 or —CO2R5 in which R5 is hydrogen, alkyl, or aryl; or R2 is —CH2O-alkyl- in which alkyl is covalently bonded to the oxygen at the 3-position instead of R1; R3 and R3′ are independently hydrogen or halo; or R3 and R3′ taken together constitute a second covalent bond between the carbons to which they are substituent; and R4 is hydrogen; or a pharmaceutically acceptable acid addition salt thereof, are taught. Also taught are methods of using the compositions, including for the treatment of myocardial infarctions, ischemia, congestive heart failure, arrhythmia, blood clots, hypertrophy, diabetes, insulin resistance, diabetes related damage, and obesity.
    Type: Grant
    Filed: October 28, 2002
    Date of Patent: August 24, 2004
    Assignee: Medicure International Inc.
    Inventor: Wasimul Haque
  • Publication number: 20040127717
    Abstract: Compounds having therapeutic utility are of formula (I)
    Type: Application
    Filed: December 15, 2003
    Publication date: July 1, 2004
    Inventors: John Gary Montana, Andrew Douglas Baxter, David Alan Owen, Robert John Watson
  • Patent number: 6749988
    Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.
    Type: Grant
    Filed: November 28, 2001
    Date of Patent: June 15, 2004
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
  • Publication number: 20040087792
    Abstract: Compounds of the formula I, wherein M, A1, A2, K1 and K2 have the meanings as indicated in the description are novel effective tryptase inhibitors.
    Type: Application
    Filed: September 4, 2003
    Publication date: May 6, 2004
    Inventors: Thomas Martin, Wolf-Rudiger Ulrich
  • Publication number: 20040087791
    Abstract: Compounds of the formula I, in which M, A1, A2, K1 and K2 have the meanings given in the description are novel effective tryptase inhibitors.
    Type: Application
    Filed: August 6, 2003
    Publication date: May 6, 2004
    Inventor: Thomas Martin
  • Publication number: 20040063961
    Abstract: Crystalline forms of Cerivastatin sodium were found, referred to hereinafter as polymorphic Forms X, A1, A2, B, C, D1, D3, D4, E and F. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and pharmaceutical compositions comprising the crystalline forms.
    Type: Application
    Filed: June 19, 2003
    Publication date: April 1, 2004
    Inventors: Paul Adriaan Van Der Schaaf, Fritz Blatter, Martin Szelagiewicz, Nicole End
  • Publication number: 20040049072
    Abstract: The present invention provides a novel class of RXR modulator compounds that exhibit an improved pharmacologic profile relative to the profile of previously studied RXR modulators, including those that share common structural features with the presently claimed modulators. The present invention also provides synthetic methods for preparing these compounds as well as pharmaceutical compositions incorporating these novel compounds and methods for the therapeutic use of such compounds and pharmaceutical compositions.
    Type: Application
    Filed: May 9, 2003
    Publication date: March 11, 2004
    Inventors: Robert J. Ardecky, Marcus F. Boehm, Amy L. Faulkner, Lawrence G. Hamann, Todd K. Jones, Christopher M. Mapes, Pierre-Yves Michellys, John S. Tyhonas
  • Patent number: 6703509
    Abstract: The invention relates to a process for the preparation of 5-arylnicotinaldehydes by reduction of the corresponding 5-arylnicotinic acids by catalytic hydrogenation in the presence of carboxylic anhydrides in which the catalyst used is a palladium/ligand complex, characterized in that the molar ratio between palladium and ligand is from 1:5 to 1:15 in the case of monodentate ligands and from 1:2.5 to 1:7.5 in the case of bidentate ligands.
    Type: Grant
    Filed: August 6, 2002
    Date of Patent: March 9, 2004
    Assignee: Merck Patent GmbH
    Inventors: Andreas Bathe, Heinz Bokel, Thomas Keil, Ralf Knieriemen, Christoph Murmann
  • Publication number: 20040019037
    Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.
    Type: Application
    Filed: July 10, 2003
    Publication date: January 29, 2004
    Inventors: Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
  • Publication number: 20030236416
    Abstract: Compounds having therapeutic utility are of formula (I)
    Type: Application
    Filed: February 6, 2001
    Publication date: December 25, 2003
    Inventors: John Gary Montana, Andrew Douglas Baxter, David Alan Owen, Robert John Watson
  • Patent number: RE40703
    Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.
    Type: Grant
    Filed: October 3, 2006
    Date of Patent: April 28, 2009
    Assignee: Schering Aktiengesellschaft
    Inventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
  • Patent number: RE41008
    Abstract: The invention relates to a process for the preparation of 5-arylnicotinaldehydes by reduction of the corresponding 5-arylnicotinic acids by catalytic hydrogenation in the presence of carboxylic anhydrides in which the catalyst used is a palladium/ligand complex, characterized in that the molar ratio between palladium and ligand is from 1:5 to 1:15 in the case of monodentate ligands and from 1:2.5 to 1:7.5 in the case of bidentate ligands.
    Type: Grant
    Filed: January 5, 2001
    Date of Patent: November 24, 2009
    Assignee: Merck Patent GmbH
    Inventors: Andreas Bathe, Heinz Bokel, Ralf Knieriemen, Christoph Muermann, Thomas Keil