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)
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Patent number: 10214516Abstract: 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: GrantFiled: August 10, 2016Date of Patent: February 26, 2019Assignee: VIIV HEALTHCARE UK (NO.5) LIMITEDInventors: John F. Kadow, B. Narasimhulu Naidu, Tao Wang, Zhiwei Yin, Zhongxing Zhang
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Publication number: 20150018515Abstract: 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: ApplicationFiled: September 30, 2014Publication date: January 15, 2015Applicant: MITSUBISHI CHEMICAL CORPORATIONInventors: Akemi HOSOKAWA, Haruhiko KUSAKA
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Publication number: 20140364586Abstract: 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: ApplicationFiled: June 26, 2014Publication date: December 11, 2014Inventors: Andrew Graham WATTS, Terrence Kantner, Amanda Barbara MacKenzie
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Publication number: 20140343284Abstract: 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: ApplicationFiled: December 13, 2012Publication date: November 20, 2014Inventor: Wenming Zhang
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Patent number: 8835409Abstract: 3-Alkenyl-6-halo-4-aminopicolinic acids and their derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: January 24, 2012Date of Patent: September 16, 2014Assignee: Dow AgroSciences, LLC.Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Paul R. Schmitzer, Thomas L. Siddall
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Publication number: 20140221330Abstract: 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: ApplicationFiled: July 26, 2012Publication date: August 7, 2014Inventors: Akihiro Morinaka, Kazunori Maebashi, Takashi Ida, Muneo Hikida, Mototsugu Yamada, Takao Abe
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Patent number: 8585930Abstract: 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: GrantFiled: September 15, 2010Date of Patent: November 19, 2013Assignee: Nalco CompanyInventor: Laxmikant Tiwari
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Patent number: 8338441Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.Type: GrantFiled: May 11, 2010Date of Patent: December 25, 2012Assignee: 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
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Publication number: 20120322769Abstract: 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: ApplicationFiled: February 16, 2011Publication date: December 20, 2012Applicants: DUKE UNIVERSITY, UWM RESEARCH FOUNDATIONInventors: Ching-Hong Yang, Xin Chen, Eric J. Toone
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Publication number: 20120289403Abstract: 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: ApplicationFiled: November 11, 2010Publication date: November 15, 2012Inventors: 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
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Patent number: 8293899Abstract: 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: GrantFiled: February 27, 2003Date of Patent: October 23, 2012Assignee: Lanxess Deutschland GmbHInventors: Boris Bosch, Markus Eckert, Hans-Christian Militzer, Claus Dreisbach
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Publication number: 20120102826Abstract: 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: ApplicationFiled: November 3, 2010Publication date: May 3, 2012Applicant: AFTON CHEMICAL CORPORATIONInventor: Xinggao FANG
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Patent number: 8168734Abstract: 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: GrantFiled: February 23, 2011Date of Patent: May 1, 2012Assignees: JNC Corporation, Chisso Petrochemical CorporationInventor: Takashi Kato
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Patent number: 8158021Abstract: 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: GrantFiled: April 24, 2008Date of Patent: April 17, 2012Assignee: Zeon CorporationInventors: Kei Sakamoto, Naoto Kogoshi, Yoshihide Yachi
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Publication number: 20120088784Abstract: 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: ApplicationFiled: November 4, 2011Publication date: April 12, 2012Inventors: Boulos Zacharie, Christopher Penney, Lyne Gagnon, Jean-François Bienvenu, Valérie Perron, Brigitte Grouix
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Publication number: 20120071457Abstract: 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: ApplicationFiled: November 29, 2011Publication date: March 22, 2012Inventors: Ken Chikauchi, Mizuyo Ida, Takao Abe, Yukiko Hiraiwa, Akihiro Morinaka, Toshiaki Kudo
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Patent number: 8026239Abstract: 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: GrantFiled: March 11, 2010Date of Patent: September 27, 2011Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
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Publication number: 20110165087Abstract: 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: ApplicationFiled: December 22, 2010Publication date: July 7, 2011Inventors: JOSEPH P.Y. KAO, SCOTT R. BURKS, GERALD R. ROSEN
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Patent number: 7923446Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: GrantFiled: May 31, 2007Date of Patent: April 12, 2011Assignee: Wyeth LLCInventors: 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
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Patent number: 7919648Abstract: 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: GrantFiled: December 7, 2006Date of Patent: April 5, 2011Assignees: Chisso Corporation, Chisso Petrochemical CorporationInventor: Takashi Kato
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Patent number: 7816367Abstract: 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: GrantFiled: February 24, 2005Date of Patent: October 19, 2010Assignee: 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
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Publication number: 20090312355Abstract: 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: ApplicationFiled: August 1, 2007Publication date: December 17, 2009Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-Sen Lai
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Publication number: 20090312354Abstract: 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: ApplicationFiled: June 22, 2007Publication date: December 17, 2009Applicant: PIERRE FABRE MEDICAMENTInventors: Frédérique Brune, André Delhon, Jean Gardette, Jean François Patoiseau, Alain Marty, Etienne Severac
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Publication number: 20090241221Abstract: 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: ApplicationFiled: March 19, 2008Publication date: September 24, 2009Inventors: Jose Alberto Fernandez-Pol, Sebastian Fernandez-Pol
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Patent number: 7459415Abstract: 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: GrantFiled: October 13, 2004Date of Patent: December 2, 2008Assignee: Seagate Technology LLCInventors: Jianwei Liu, Michael Joseph Stirniman, Jing Gui
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Publication number: 20080221333Abstract: 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: ApplicationFiled: September 15, 2006Publication date: September 11, 2008Inventors: Hyun Ik Shin, Bo Seung Choi, Jae Hoon Lee
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Patent number: 7321044Abstract: 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: GrantFiled: October 15, 2002Date of Patent: January 22, 2008Assignee: Schering AktiengesellschaftInventors: Johannes Platzek, Wolfgang Beckmann, Jens Geisler, Holger Kirstein, Ulrich Niedballa, Eckhard Ottow, Sigmar Radau, Claudia Schulz, Thomas Wessa
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Patent number: 7268135Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: GrantFiled: December 1, 2004Date of Patent: September 11, 2007Assignee: WyethInventors: 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
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Patent number: 7247732Abstract: 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: GrantFiled: June 12, 2006Date of Patent: July 24, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Toru Yamano, Naohiro Taya, Akio Ojida
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Patent number: 7157458Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.Type: GrantFiled: January 31, 2002Date of Patent: January 2, 2007Assignee: Cryolife, Inc.Inventors: Carl W. Gilbert, Eleanor B. McGowan, Kirby S. Black, T. Gregory P. Harper
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Patent number: 7071175Abstract: 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: GrantFiled: May 3, 2000Date of Patent: July 4, 2006Assignee: Astrazeneca ABInventors: Marcel Linschoten, Magnus Polla
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Patent number: 7067501Abstract: The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.Type: GrantFiled: May 20, 2004Date of Patent: June 27, 2006Assignee: H. Lundbeck A/SInventors: Garrick P. Smith, Gitte Mikkelsen, Kim Andersen, Daniel Greve, Thomas Ruhland, Stephen P. Wren
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Patent number: 7037914Abstract: 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: GrantFiled: September 23, 2002Date of Patent: May 2, 2006Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
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Patent number: 6969768Abstract: 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: GrantFiled: September 9, 2002Date of Patent: November 29, 2005Assignee: Bayer CropScience GmbHInventor: Sergiy Pazenok
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Publication number: 20040248919Abstract: 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: ApplicationFiled: April 15, 2004Publication date: December 9, 2004Inventors: 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
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Publication number: 20040249154Abstract: 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: ApplicationFiled: July 14, 2004Publication date: December 9, 2004Inventors: Guang-Pei Chen, Prasad Koteswara Kapa, Eric M. Loeser, Ulrich Beutler, Werner Zaugg, Michael J. Girgis
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Publication number: 20040214827Abstract: 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: ApplicationFiled: June 5, 2003Publication date: October 28, 2004Inventors: 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
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Publication number: 20040204594Abstract: 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: ApplicationFiled: January 12, 2004Publication date: October 14, 2004Inventors: Shoujun Chen, Lijun Sun, Joel McCleary
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Patent number: 6780997Abstract: 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: GrantFiled: October 28, 2002Date of Patent: August 24, 2004Assignee: Medicure International Inc.Inventor: Wasimul Haque
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Publication number: 20040127717Abstract: Compounds having therapeutic utility are of formula (I)Type: ApplicationFiled: December 15, 2003Publication date: July 1, 2004Inventors: John Gary Montana, Andrew Douglas Baxter, David Alan Owen, Robert John Watson
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Patent number: 6749988Abstract: 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: GrantFiled: November 28, 2001Date of Patent: June 15, 2004Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
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Publication number: 20040087792Abstract: 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: ApplicationFiled: September 4, 2003Publication date: May 6, 2004Inventors: Thomas Martin, Wolf-Rudiger Ulrich
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Publication number: 20040087791Abstract: 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: ApplicationFiled: August 6, 2003Publication date: May 6, 2004Inventor: Thomas Martin
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Publication number: 20040063961Abstract: 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: ApplicationFiled: June 19, 2003Publication date: April 1, 2004Inventors: Paul Adriaan Van Der Schaaf, Fritz Blatter, Martin Szelagiewicz, Nicole End
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Publication number: 20040049072Abstract: 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: ApplicationFiled: May 9, 2003Publication date: March 11, 2004Inventors: Robert J. Ardecky, Marcus F. Boehm, Amy L. Faulkner, Lawrence G. Hamann, Todd K. Jones, Christopher M. Mapes, Pierre-Yves Michellys, John S. Tyhonas
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Patent number: 6703509Abstract: 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: GrantFiled: August 6, 2002Date of Patent: March 9, 2004Assignee: Merck Patent GmbHInventors: Andreas Bathe, Heinz Bokel, Thomas Keil, Ralf Knieriemen, Christoph Murmann
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Publication number: 20040019037Abstract: 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: ApplicationFiled: July 10, 2003Publication date: January 29, 2004Inventors: Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
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Publication number: 20030236416Abstract: Compounds having therapeutic utility are of formula (I)Type: ApplicationFiled: February 6, 2001Publication date: December 25, 2003Inventors: John Gary Montana, Andrew Douglas Baxter, David Alan Owen, Robert John Watson
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Patent number: RE40703Abstract: 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: GrantFiled: October 3, 2006Date of Patent: April 28, 2009Assignee: Schering AktiengesellschaftInventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
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Patent number: RE41008Abstract: 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: GrantFiled: January 5, 2001Date of Patent: November 24, 2009Assignee: Merck Patent GmbHInventors: Andreas Bathe, Heinz Bokel, Ralf Knieriemen, Christoph Muermann, Thomas Keil