Additional Hetero Ring Which Is Unsaturated Patents (Class 544/300)
  • Publication number: 20100210762
    Abstract: A compound represented by formula (I-1): wherein R21, R22, R23 and R24 each independently represent a hydrogen atom or a monovalent substituent, with the proviso that compounds, in which R21, R22, R23 and R24 each are an alkylthio group, are excluded; R21 and R22 and/or R23 and R24 each may bond to each other to form a ring, with the proviso that compounds, in which the formed ring is a dithiol ring or a dithiolane ring, are excluded; R25 and R26 each independently represent a hydrogen atom or a monovalent substituent; X21, X22, X23 and X24 each independently represent a hetero atom; compounds, wherein R21, R22, R23 and R24 each represent a cyan group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group or a hydrogen atom, are excluded; and compounds, wherein R21 and R23 each represent a hydrogen atom; R22 and R24 each represent an arylcarbonyl group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group, are e
    Type: Application
    Filed: August 15, 2008
    Publication date: August 19, 2010
    Applicant: FUJIFILM CORPORATION
    Inventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
  • Patent number: 7767670
    Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: August 3, 2010
    Assignee: Ambit Biosciences Corporation
    Inventors: Shamal A. Mehta, Robert M. Grotzfeld, Zdravko V. Milanov, Andiliy G. Lai, Hitesh K. Patel, David J. Lockhart
  • Publication number: 20100113444
    Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I), (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
    Type: Application
    Filed: June 22, 2007
    Publication date: May 6, 2010
    Inventors: Kevin J. Duffy, Duke M. Fitch, Jian Jin, Ronggang Liu, Antony N. Shaw, Kenneth Wiggall
  • Patent number: 7691870
    Abstract: The present invention relates to benzimidazole carboxamides of formula I, the use of the compounds of formula I of as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of pharmaceutical compositions and methods of treatment, comprising administering said pharmaceutical compositions to a patients.
    Type: Grant
    Filed: June 11, 2004
    Date of Patent: April 6, 2010
    Assignee: Merck Patent GmbH
    Inventors: Hans-Peter Buchstaller, Matthias Wiesner, Frank Zenke, Christiane Amendt, Matthias Grell, Christian Sirrenberg
  • Publication number: 20100081678
    Abstract: Indole derivatives that are useful in the treatment of cancer as a chemotherapeutic agent or radiosensitizing agent.
    Type: Application
    Filed: September 30, 2009
    Publication date: April 1, 2010
    Inventors: Peter A. Crooks, Thirupathi R. Yerramreddy, Narsimha R. Penthala, Michael L. Freeman, Sekhar R. Konjeti
  • Publication number: 20100003612
    Abstract: Isoindoline pigments of the general formula I in which the variables are defined as follows: R1 is C1-C4-alkyl; R2 is hydrogen or C1-C4-alkyl, whose value expressing ease of dispersion in LDPE is ?10 and which require a reduction ratio of ?5 to obtain ? of standard depth of shade.
    Type: Application
    Filed: July 11, 2007
    Publication date: January 7, 2010
    Applicant: BASF SE
    Inventors: Johannes Loebel, Andreas Stohr, Peter Boettcher
  • Patent number: 7642303
    Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: January 5, 2010
    Inventors: Thomas L. Shakely, James John Krutak
  • Publication number: 20090312352
    Abstract: The invention generally relates to compositions and methods for treatment of disease caused by Yersinia spp. infection. More specifically, the invention relates to protein tyrosine phosphatase inhibitors and derivatives and analogs thereof, pharmaceutical compositions containing the protein tyrosine phosphatase inhibitors and analogs, methods of making the protein tyrosine phosphatase inhibitors and analogs and methods of use thereof.
    Type: Application
    Filed: October 19, 2005
    Publication date: December 17, 2009
    Inventors: Tomas Mikael Mustelin, Maurizio Pellecchia, Lutz Tautz
  • Publication number: 20090229670
    Abstract: An organic photoelectric conversion material for a photoelectric conversion element is provided, the organic photoelectric conversion material represented by formula 1 and having a molecular weight of 250 or greater but not greater than 800: wherein, A represents an electron withdrawing atomic group; R1, R2 and R3 each independently represents a hydrogen atom or a substituent; L represents a divalent TC conjugated substituent; D represents an electron donating aromatic substituent; and X represents O, S, or N—Ra in which Ra represents a hydrogen atom or a substituent.
    Type: Application
    Filed: March 11, 2009
    Publication date: September 17, 2009
    Applicant: FUJIFILM Corporation
    Inventors: Tetsu KITAMURA, Kimiatsu Nomura, Tetsuro Mitsui
  • Publication number: 20090186913
    Abstract: Methods for inhibiting a neoplasm in a subject and methods of inhibiting undesired angiogenesis that include administering to a subject a therapeutically effective amount of at least one novel tetrahalogenated compound, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 10, 2008
    Publication date: July 23, 2009
    Inventors: William D. Figg, Erin Gardner, Michael Gutschow, Agnieszka Ambrozak
  • Publication number: 20090087376
    Abstract: The present invention relates to the identification of compounds that are suitable for imaging amyloid deposits in living patients. The invention relates, in part, to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease. The present invention also relates to therapeutic uses for such compounds, as exemplified by compounds of the formula (1) in which Y is independently S, O, or N and m is 1, 2, or 3.
    Type: Application
    Filed: July 15, 2005
    Publication date: April 2, 2009
    Applicants: The General Hospital Corporation, Massachusetts Institute of Technology, University of Pittsburg of the Commonwealth System of Higher Education
    Inventors: Brian Bacskai, Bradley T. Hyman, William E. Klunk, Chester A. Mathis, Timothy Swager, Evgueni Nesterov, Ivory Hills
  • Publication number: 20090044857
    Abstract: Disclosed is a photoelectric conversion device wherein a methine dye represented by the formula (1) below is supported by a thin film of oxide semiconductor particles arranged on a substrate. Also disclosed is a solar cell manufactured by using such a photoelectric conversion device. (In the formula (1), n represents an integer of 0-5; m represents an integer of 0-5; R1-R4 independently represent a hydrogen atom, an optionally substituted aromatic residue, an optionally substituted aliphatic hydrocarbon residue or the like; X and Y independently represent a hydrogen atom; an optionally substituted aromatic residue, an optionally substituted aliphatic hydrocarbon residue or the like; Z represents an oxygen atom, a sulfur atom or the like; A1, A2, A3, A4 and A5 independently represent a hydrogen atom, an optionally substituted aromatic residue, an optionally substituted aliphatic hydrocarbon residue or the like; and rings a, b and c may be substituted.
    Type: Application
    Filed: March 1, 2007
    Publication date: February 19, 2009
    Inventors: Koichiro Shigaki, Masayoshi Kaneko, Takayuki Hoshi, Teruhisa Inoue
  • Publication number: 20090044863
    Abstract: Briefly described, embodiments of this disclosure include coronene charge-transport materials, methods of forming coronene charge-transport materials, and methods of using the coronene charge-transport materials.
    Type: Application
    Filed: February 28, 2006
    Publication date: February 19, 2009
    Inventors: Seth Marder, Zesheng An, Jungsheng Yu, Bernard Kippelen
  • Publication number: 20080300407
    Abstract: The invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II; R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.
    Type: Application
    Filed: July 22, 2008
    Publication date: December 4, 2008
    Applicant: Eli Lilly and Company
    Inventors: Michael Philip Cohen, Daniel Timothy Kohlman, Sidney Xi Liang, Vincent Mancuso, Frantz Victor, Yao-Chang Xu, Bai-Ping Ying, DeAnna Piatt Zacherl, Deyi Zhang
  • Patent number: 7452901
    Abstract: The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: April 26, 2004
    Date of Patent: November 18, 2008
    Assignee: Gilead Sciences, Inc.
    Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Steven Krawczyk, Christopher P. Lee, Kuei-Ying Lin, Richard L. Mackman, David Y. Markevitch, Peter H. Nelson, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Sundaramoorthi Swaminathan, William J. Watkins, Jennifer R. Zhang, Lijun Zhang
  • Patent number: 7442486
    Abstract: Radiation-sensitive element comprising: (a) one or more types of monomers each comprising at least one ethylenically unsaturated group accessible to a free-radical polymerization, (b) at least one sensitizer, (c) at least one coinitiator capable of forming free radicals together with the sensitizer (b) and selected from the following classes of compounds: metallocenes; 1,3,5-triazine derivatives with one to three CX3 groups, wherein X represents chlorine or bromine; peroxides; hexaarylbiimidazoles; oxime ethers; oxime esters; N-aryl glycines and derivatives thereof; thiol compounds; N-aryl, S-aryl and O-aryl polycarboxylic acids with at least 2 carboxyl groups of which at least one is bonded to the N, S or O atom of the aryl unit; alkyltriarylborates; benzoin ethers; benzoin esters; trihalogenomethylarylsulfones; amines; N,N-dialkylaminobenzoic acid esters; aromatic sulfonyl halides; trihalogenomethylsulfones; imides; diazosulfonates; 9,10-dihydroanthracene derivatives; a-hydroxy and a-amino acetophenones; an
    Type: Grant
    Filed: February 20, 2004
    Date of Patent: October 28, 2008
    Assignee: Eastman Kodak Company
    Inventors: Harald Baumann, Udo Dwars, Detlef Pietsch, Michael Flugel
  • Publication number: 20080142759
    Abstract: The present invention relates to the use of pyridine N-oxide based azo dyes and their metal complexes in optical layers for optical data recording, preferably for optical data recording using a blue laser with a wavelength up to 450 nm or a red laser with a wavelength up to 650 nm. The invention further relates to a write only read many (WORM) type optical recording medium capable of recording and reproducing information with radiation of a blue or red laser, which employs a pyridine N-oxide based azo dye or a respective metal complex in the optical layer.
    Type: Application
    Filed: December 7, 2005
    Publication date: June 19, 2008
    Inventor: Christophe Pays
  • Patent number: 7351829
    Abstract: The invention relates to compounds based on merocyanines with the general formulas I and/or II, where n=0 or an integer from 1 to 3, X=O or S and the residues R1 to R12 are the same or different and signify in particular hydrogen or various organic residues, without or with functional groups, and R2 incorporates an amine function. The compounds in accordance with the invention are suitable as fluorescent dyes (fluorophores) for used in optical determination and demonstration methods, in particular those employing fluorescence, for example in medicine, pharmacology and the biological, materials and environmental sciences. They are characterized by high photostability and long storage life, and exhibit a high fluorescence quantum yield. Excitation causing them to emit light can be achieved in a simple manner, by white-light sources or by laser irradiation in the UV, visible or NIR spectral region.
    Type: Grant
    Filed: July 3, 2002
    Date of Patent: April 1, 2008
    Assignee: Dyomics GmbH
    Inventors: Peter Czerney, Wilhelm Frank, Matthias Wenzel, Frank Lehmann
  • Patent number: 7291642
    Abstract: The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically acceptable salts with organic or inorganic acids or bases having useful properties, their preparation, medicaments comprising the pharmacologically effective compounds, their preparation and their use.
    Type: Grant
    Filed: October 21, 2005
    Date of Patent: November 6, 2007
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Iris Kauffmann-Hefner, Norbert Hauel, Henri Doods, Angelo Ceci, Stefan Peters
  • Patent number: 7205307
    Abstract: The present invention provides a genus of pyrimidine amides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: April 17, 2007
    Assignee: Icagen, Inc.
    Inventors: Grant A. McNaughton-Smith, George S. Amato, Paul C. Fritch
  • Patent number: 7160893
    Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, R2, R3, and R4 are as defined in the specification. The invention also provides related pharmaceutical compositions, methods of use, and combinations.
    Type: Grant
    Filed: August 5, 2003
    Date of Patent: January 9, 2007
    Assignee: Warner-Lambert Company
    Inventors: James Lester Hicks, William Howard Roark
  • Patent number: 7119201
    Abstract: The present invention relates to triaryl-oxy-aryloxy-pyrimidine-2,4,6-trione; metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, W, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: April 28, 2003
    Date of Patent: October 10, 2006
    Assignee: Pfizer Inc
    Inventors: Lawrence Alan Reiter, Kevin Daniel Freeman-Cook
  • Patent number: 7119102
    Abstract: Disclosed are compounds of formula (I): wherein the variables R1, R2, R3 and Z are described herein, which are useful as inhibitors of the kinase activity of the I?B kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.
    Type: Grant
    Filed: December 2, 2004
    Date of Patent: October 10, 2006
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Zhidong Chen, Pier Francesco Cirillo, Darren DiSalvo, Weimin Liu, Daniel Richard Marshall, Lifen Wu, Erick Richard Roush Young
  • Patent number: 6995262
    Abstract: The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae (a) to (n) given in the claims. The polymethine dyes according to the invention are suitable for use as dyes and/or labels, in particular for staining or labeling biomolecules.
    Type: Grant
    Filed: July 24, 2000
    Date of Patent: February 7, 2006
    Assignee: Bayer CropScience AG
    Inventors: Geert Deroover, Michael Missfeldt, Lydia Simon
  • Patent number: 6979695
    Abstract: The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.
    Type: Grant
    Filed: October 2, 2002
    Date of Patent: December 27, 2005
    Assignee: Targacept, Inc.
    Inventors: William S. Caldwell, Gary M. Dull, Balwinder S. Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared M. Wagner, Peter A. Crooks, Patrick M. Lippiello, Merouane Bencherif
  • Patent number: 6919332
    Abstract: The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: April 28, 2003
    Date of Patent: July 19, 2005
    Assignee: Pfizer Inc.
    Inventors: Mark C. Noe, Lilli Ann Wolf-Gouveia
  • Patent number: 6914160
    Abstract: This invention relates to compounds of formula (I)
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: July 5, 2005
    Assignee: Pfizer Inc
    Inventors: Duncan Robert Armour, Andrew Simon Bell, Paul John Edwards, David Ellis, David Hepworth, Mark Llewellyn Lewis, Christopher Ronald Smith
  • Patent number: 6849622
    Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: February 1, 2005
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
  • Patent number: 6841671
    Abstract: The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said “A” is a 5-7 membered heterocyclic ring as defined in the specification and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: October 23, 2001
    Date of Patent: January 11, 2005
    Assignee: Pfizer Inc.
    Inventors: Mark C. Noe, Martin J. Wythes, Brian S. Bronk
  • Patent number: 6833372
    Abstract: Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated.
    Type: Grant
    Filed: February 11, 2003
    Date of Patent: December 21, 2004
    Assignee: Pfizer, Inc.
    Inventors: Lance C. Christie, Mark B. Anderson, Jun Feng, Yufeng Hong, Ved P. Pathak, Ranjan J. Rajapakse, Eileen V. Tompkins, Haresh Vazir, Haitao Li
  • Patent number: 6833378
    Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.
    Type: Grant
    Filed: January 17, 2001
    Date of Patent: December 21, 2004
    Assignee: Pfizer Inc
    Inventor: Yuhpyng L. Chen
  • Patent number: 6800590
    Abstract: This invention relates to new 2-pyrimidinyloxy-N-aryl-benzylamine derivatives, their preparation processes and uses as chemical herbicides in agriculture. The compound has the following structure: wherein, D or E is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl or C1-C4 haloalkoxy; R1 is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy; R2 is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 carbamyl, C1-C4 alkoxycarbonyl, C1-C4 haloalkyl, cyano, nitro, carboxy or its alkali metal, alkali earth metal and organoammonium salts, C1-C4 alkylamido, C1-C4 haloalkylamido, heterocyclic amido, benzamido or substituted benzamido, benzo or substituted benzo compounds; R3 is hydrogen, C1-C4 alkanoyl, C1-C4 haloalkanoyl, benzoyl or C1-C4 alkoxyacetyl; X is CH or N; n=1-3.
    Type: Grant
    Filed: April 9, 2003
    Date of Patent: October 5, 2004
    Assignees: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Zheijiang Chemical Industry Research Institute
    Inventors: Long Lü, Jie Chen, Jun Wu, Wen Ling, Lisheng Mao, Mingzhi Li, Xian Cai, Weili Peng, Yong Wu, Shenggan Wu, Hongjun Wang, Guochao Wang, Hu Cui, Shidong Han, Weilian Qiu, Yonghua Wang
  • Patent number: 6780868
    Abstract: Compounds of formula (I): wherein: V represents a single bond or a linear or branched (C1-C6)alkylene chain, M represents a single bond or a linear or branched (C1-C6)alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i): X represents carbonyl, G1 represents a linear C3 alkylene chain optionally containing a double bond and/or being optionally substituted by a hydroxyl group, their isomers, their hydrates, their solvates, and additional salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.
    Type: Grant
    Filed: February 20, 2003
    Date of Patent: August 24, 2004
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
  • Patent number: 6765009
    Abstract: Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
    Type: Grant
    Filed: April 10, 2002
    Date of Patent: July 20, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, Kristen Mueller, John Robinson Regan
  • Patent number: 6716845
    Abstract: The present invention pertains to derivatives of 5,5-disubstituted pyrimidine-2,4,6,-trianones having the formula: wherein R1, R2, R3, and R4 are described herein. These compounds have antitumor and antimetastatic activity.
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: April 6, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Dagmar Geppert, Frank Grams, Hans-Willi Krell, Herbert Leinert, Ernesto Menta, Gerd Zimmermann
  • Patent number: 6713486
    Abstract: 2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R1 is a C6-10 aryl or C3-10 heteroaryl group optionally having one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkyl substituted with one or more halogen atoms, C3-4 cycloalkyl, cyano, nitro, hydroxy, thiohydroxy, azido, C1-6 alkoxy, oximino, C1-3 alkyloximino, O—(C1-6 alkyl)-substituted oximino, C—1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethlyl, C1-6 alkoxymethyl, C1-6 acyloxynethyl, carbamoyloxymethyl, anminomethyl, N—(C1-3 alkyl)aminomethyl, N,N-di(C1-3 alkyl)aminomethyl, carboxy, C1-6 alkoxycarbonyl, aziridine, amino, hydroxyethylamino, cyclopropylamino, C1-6 alkylamino, di(C1-6 alkyl)amino, trifluoroacetamido, C1-6 acylamido, carbamoyl, hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl)carbamoyl, aminocarbamoyl, dimethylamin
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: March 30, 2004
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jong-Chan Son, Seun-Shil Shin, Shin-Keol Kim, Chong-Kyo Lee, Hae-Soo Kim
  • Patent number: 6706723
    Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, A, B and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: October 25, 2001
    Date of Patent: March 16, 2004
    Assignee: Pfizer, Inc.
    Inventors: Mark C. Noe, Lawrence A. Reiter, Martin J. Wythes
  • Publication number: 20040006057
    Abstract: The present invention relates to triaryl-oxy-aryloxy-pyrimidine-2,4,6-trione; metalloproteinase inhibitors of the formula 1
    Type: Application
    Filed: April 28, 2003
    Publication date: January 8, 2004
    Inventors: Lawrence Alan Reiter, Kevin Daniel Freeman-Cook
  • Patent number: 6673925
    Abstract: Method of producing thiobarbituric acid derivatives of formula I wherein R1 is SH, S−M+ or CH3S—, and M+ is an alkali metal ion, by hydrogenolysis of a compound of formula II wherein R2 is chlorine or CH3O—, with a) a hydrogenolysis agent in the presence of an inert solvent and by a direct reaction of the hydrogenolysis product with an alkali metal methylate in methanol, or b) with a hydrogenolysis agent in the presence of an inert solvent and in the presence of a methylation reagent, and subsequently with an alkali metal methylate in methanol, as well as the use of these compound of formula I in the production of 7-[(4,6-dimethoxy-pyrimidin-2-yl)thio]-3-methylphthalide.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: January 6, 2004
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Bernhard Urwyler, Thomas Rapold, Marco Passafaro
  • Patent number: 6656911
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: December 2, 2003
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W Spruce
  • Patent number: 6656910
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: December 2, 2003
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Publication number: 20030220198
    Abstract: This invention relates to new 2-pyrimidinyloxy-N-aryl-benzylamine derivatives, their preparation processes and uses as chemical herbicides in agriculture.
    Type: Application
    Filed: April 9, 2003
    Publication date: November 27, 2003
    Inventors: Long L, Jie Chen, Jun Wu, Wen Ling, Lisheng Mao, Mingzhi Li, Xian Cai, Weili Peng, Yong Wu, Shenggan Wu, Hongjun Wang, Guochao Wang, Hu Cui, Shidong Han, Weilian Qiu, Yonghua Wang
  • Patent number: 6646149
    Abstract: Novel “bispolyamine” inhibitor compounds of polyamine transport are disclosed. These compounds are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. These compounds display desirable activities both for diagnostic and research assays and therapy.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: November 11, 2003
    Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
  • Patent number: 6613773
    Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocyclyl group.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: September 2, 2003
    Assignee: Syngenta Limited
    Inventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
  • Patent number: 6579982
    Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: June 17, 2003
    Assignee: Pfizer Inc.
    Inventor: Julian Blagg
  • Publication number: 20030085388
    Abstract: Novel compositions and synthetic methods for forming nonlinear optic polymers, which may be incorporated into multiple light-based devices, are disclosed. These compositions include chromophoric monomer units that incorporate nonlinear optic chromophores, linking monomers that may be used to link chromophoric monomers, and polymers made from chromophoric monomers or chromophoric monomers in combination with linking monomers. The polymers can exhibit high thermal stability, which is believed to arise from their covalently bonded chromophore structures. In addition to their covalently bonded chromophore structures, in one aspect, nonlinear optic polymers are disclosed that may be crosslinked to further increase the thermal and dipole stability of the polymers.
    Type: Application
    Filed: July 15, 2002
    Publication date: May 8, 2003
    Inventor: Luping Yu
  • Patent number: 6548512
    Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: April 15, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
  • Patent number: 6545006
    Abstract: The invention relates to a process for obtaining L-dihydroorotic acid by chromatography on an anionic exchange material in a base water mixture under a pressure from about 1.1 MPa to about 40 MPa. The process can be used to investigate the in vitro and in vivo activity of N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide, N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrontonamide and similar compounds.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: April 8, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Ulrike Milbert, Robert Bartlett, Eric Ruuth, Claude Fudali
  • Publication number: 20030045717
    Abstract: The invention relates to compounds based on merocyanines with the general formulas I and/or II, 1
    Type: Application
    Filed: July 3, 2002
    Publication date: March 6, 2003
    Applicant: Dyomics GmbH
    Inventors: Peter Czerney, Matthias Wenzel, Wilhelm Frank, Frank Lehmann
  • Patent number: 6518425
    Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.
    Type: Grant
    Filed: May 15, 2000
    Date of Patent: February 11, 2003
    Assignees: Emory University, Triangle Pharmaceuticals, Inc.
    Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman