The Hetero Ring Contains Chalcogen Patents (Class 540/467)
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Patent number: 7964721Abstract: A mercury selective fluorescent chemosensor for detecting mercury ions by a compound represented by formula 1 and a novel fluorescent sensitive compound prepared by introducing two aminopyrene functions as a fluorescent sensitive moiety into a binding site of the compound of formula 1 is used for selectively detecting mercury ions are provided. The mercury selective fluorescent sensitive chemosensor is a switch type chemosensor having ON-OFF-type Hg2+-selective fluorescence quenching behavior and is not affected by other coexistent metal ions. Changes in fluorescence of the compounds of formula 1 were analyzed by ratiometric approach using monomer and excimer emissions of the pyrene fluorophore to selectively signal the concentration of mercury ions. The chemosensor can detect mercury ions in a micromolar unit even in a solution including an excess of water. Accordingly, the mercury selective fluorescent chemosensor for detecting mercury ions can be used effectively in environmental and medical applications.Type: GrantFiled: October 9, 2007Date of Patent: June 21, 2011Assignee: Chung-Ang University Industry-Academy Cooperation FoundationInventors: Suk-Kyu Chang, Jun Soo Kim, Myung Gil Choi, Ki Cheol Song, Sangdoo Ahn, Kyoung Tai No
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Publication number: 20110118330Abstract: Compounds that inhibit proteolytic enzymes of Human Immunodeficiency Virus (HIV) are described. Preparation of the inhibitors, pharmaceutical compositions containing them, and uses of the compounds or compositions for the treatment of HIV infections are also described.Type: ApplicationFiled: July 8, 2009Publication date: May 19, 2011Applicant: PURDUE RESEARCH FOUNDATIONInventor: Arun K. Ghosh
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Publication number: 20110059959Abstract: The present invention is directed to novel multicyclic molecules that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of PARP, VEGFR2, and MLK3 enzymes, including, for example, neurodegenerative diseases, inflammation, ischemia, and cancer.Type: ApplicationFiled: November 18, 2010Publication date: March 10, 2011Applicant: CEPHALON, INC.Inventors: Sankar Chatterjee, James L. Diebold, Derek Dunn, Robert L. Hudkins, Reddeppareddy Dandu, Gregory J. Wells, Allison L. Zulli
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Publication number: 20110039815Abstract: In one embodiment the present invention relates to a method of treating cancerous cells in a mammal comprising the steps of administering to the cancerous cells an effective amount of a cyclic amine wherein the cyclic amine contains sulfur or nitrogen and the structure includes an interchealted metal ion.Type: ApplicationFiled: June 14, 2006Publication date: February 17, 2011Inventors: Wiley J. Youngs, Claire A. Tessier, Doug A. Medvetz, Michael J. Taschner
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Patent number: 7858383Abstract: The invention relates to methods of determining sodium ions in a sample, wherein the ions are contacted with a compound having chromophoric moiety and an ionophoric moiety, where the ionophoric moiety interacts with the sodium ions present in the sample, resulting in the chromophoric moiety changing its radiation absorption properties in the ultraviolet and visible regions of the spectrum. For example, a change in an intensity of an absorption maximum is measured and the ion concentration is determined accordingly.Type: GrantFiled: May 2, 2007Date of Patent: December 28, 2010Assignee: Opti Medical SystemsInventors: Huarui He, Chao Lin, Neeta Raje, Chusheng Liu
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Patent number: 7851496Abstract: Disclosed relates to an ionic liquid type crown ether derivative, expressed by Chemical Formula 1 below, for isolating metal ions, a method for preparing the same and a method for isolating selectively the metal ions using the cycle size of the same. The present invention can provide the ionic liquid type crown ether and isolate metal ions including radioactive isotopes efficiently using the same. Furthermore, the prevent invention provides crown ether valuably used as a recyclable and environment-friendly isolating medium by preparing crown ether of ionic liquid type. wherein m, n, X? and R are identical with those in the description.Type: GrantFiled: June 23, 2006Date of Patent: December 14, 2010Assignee: Korea Atomic Energy Research InstituteInventors: Sang Hyun Park, Seung Ho Jang, Hui Jeong Gwon, Myung Woo Byun
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Patent number: 7829563Abstract: The present invention relates to compounds of formula I wherein Ar1, Ar2, Ar3, n, and R1 to R8 are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved, like sleep disorders.Type: GrantFiled: February 27, 2008Date of Patent: November 9, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Henner Knust, Parichehr Malherbe, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20100086482Abstract: The present invention describes a process for preparing new looped dendrimer and dendron compounds by controlling the molar amount of branch cell reagent monomer that is combined with various cores bearing core-XR functionalities (e.g., primary, or secondary amines, thiol, or epoxy functionalities). These looped, macrocyclic structures are more robust to various conditions, with greater resistance to acid/base hydrolysis. Alternatively, the looped, macrocyclic structure may offer new orientations that would qualify it as a better chelation ligand for metals, and other similar uses.Type: ApplicationFiled: December 28, 2007Publication date: April 8, 2010Applicant: Dendritic Nanotechnologies, Inc.Inventors: Donald A. Tomalia, Douglas R. Swanson, Baohua Huang, Veera Reddy Pulgam
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Publication number: 20100069354Abstract: The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and the use in medicine and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them.Type: ApplicationFiled: August 5, 2009Publication date: March 18, 2010Applicant: Eisai R&D Management Co., Ltd.Inventors: Piotr Pawel GRACZYK, Paschalis DIMOPOULOS, Afzal KHAN, Gurpreet Singh BHATIA, Christopher Neil FARTHING
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Patent number: 7678778Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.Type: GrantFiled: October 25, 2005Date of Patent: March 16, 2010Assignee: DEKK-TEC, Inc.Inventor: Lee Roy Morgan
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Patent number: 7662977Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: December 21, 2007Date of Patent: February 16, 2010Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Patent number: 7659263Abstract: The present invention relates to a thienopyrrole compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound as an active ingredient. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: GrantFiled: November 10, 2005Date of Patent: February 9, 2010Assignee: Japan Tobacco Inc.Inventors: Ryo Mizojiri, Takahiro Oka, Kenta Aoki, Satoru Noji, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yasushi Niwa
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Publication number: 20090306044Abstract: The present invention relates to the use of quinazolines of formula (I), wherein the groups Ra to Rd have the meanings given in the claims and specification, in cancer therapy.Type: ApplicationFiled: November 9, 2006Publication date: December 10, 2009Inventors: Flavio Solca, Andree Amelsberg, Gerd Stehle, Jacobus C.A. Van Meel, Anke Baum
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Publication number: 20090221697Abstract: The present invention relates to macrolide conjugates of pyrrolizine and indolizine derivatives with macrocyclic antibiotics and derivatives thereof. The macrolide conjugates are potent inhibitors of 5-lipoxygenase and cyclooxygenase and are therefore suitable to treat disorders of the rheumatic type and to prevent allergically induced diseases. The macrolide conjugates have significantly enhanced potency and efficacy.Type: ApplicationFiled: July 26, 2006Publication date: September 3, 2009Applicant: MERCKLE GMBHInventors: Stefan Laufer, Wolfgang Albrecht, Michael Burnet, Hans-Jürgen Gutke
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Patent number: 7582280Abstract: The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.Type: GrantFiled: July 8, 2008Date of Patent: September 1, 2009Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Helen Fan, Michael F. Tweedle, Rolf E. Swenson
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Patent number: 7579334Abstract: The present invention relates to new compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure II: L represents the chain of the substructure III: —X1—(CH2)m-Q-(CH2)n—X2—??III D represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity; The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to process and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.Type: GrantFiled: April 22, 2004Date of Patent: August 25, 2009Assignee: GlaxoSmithKline Istrazivacki Centar ZagrebInventors: Mladen Mercep, Milan Mesic, Linda Tomaskovic
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Publication number: 20090202521Abstract: A bifunctional polyazamacrocyclic chelating agent of the formula (I): wherein: and the variables A, L, Q, Q1, X, Y, Z, Z1, m, n and r are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a metal ion, such as an ion of 90Y, 111Li or 177Lu; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate. A method of therapeutic treatment of a mammal involving administration of the pharmaceutical composition is also described.Type: ApplicationFiled: March 6, 2007Publication date: August 13, 2009Applicant: MDS (Canada) Inc.Inventors: Zoltan Kovaks, Garry E. Kiefer, Corinne Bensimon, A. Dean Sherry, Gyula Tircso
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Publication number: 20090105301Abstract: The present invention relates to novel 9a-substituted azalides having antimalarial activity. More particularly, the invention relates to 9a-substituted 9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A, 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-5-O-dedesosaminyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds having antimalarial activity, to the method of preparation, to the method of use, and to pharmaceutically acceptable derivatives thereof having antimalarial activity.Type: ApplicationFiled: May 1, 2007Publication date: April 23, 2009Inventors: Sulejman Alihodzic, Andrea Fajdetic, Anton Hutinec, Zrinka Ivezic, Nedjeljko Kujundzic, Renata Rupcic
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Publication number: 20090048221Abstract: Compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure VIII: L represents the chain of the substructure IX or XIII: —X1—(CH2)m-Q-(CH2)n—X2—??IX —X1—(CH2)m—V—(CH2)p-Q-(CH2)n—X2—??XIII and Z represents a steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity are disclosed. Pharmaceutically acceptable salts and solvates of such compounds, processes and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals are also disclosed.Type: ApplicationFiled: October 27, 2005Publication date: February 19, 2009Inventors: Mladen Mercep, Milan Mesic, Linda Tomaskovic, Stribor Markovic, Visnja Poljak, Gordana Sijan, Selvira Selmani
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Patent number: 7470469Abstract: A medical device comprising a substrate having a plasma polymerized functionality bonded to at least a portion of the substrate. A superoxide dismutase mimic agent having a complimentary functional group to the plasma polymerized functionality is bonded to the portion of the substrate by bonding to the plasma polymerized functionality. The functionalities can be carboxylate, amine, or sulfate groups and/or polyethylene glycol and can optionally include crosslinking groups.Type: GrantFiled: July 5, 2007Date of Patent: December 30, 2008Assignee: Advanced Cardiovascular Systems Inc.Inventors: Eugene T. Michal, Murthy Simhambhatla, Charles D. Claude
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Patent number: 7468434Abstract: This invention provides a method for treating an eye disease in a patient comprising: providing a photosensitive prodrug that releases upon exposure to light an active ingredient to treat the eye disease; administering the prodrug in a pharmaceutically accepted vehicle to the subject, and exposing the eye of the subject to an external light source to cause the prodrug to release the active ingredient. This invention also provides a composition for the treatment of glaucoma, comprising a compound containing a lithium ion-chelated in a crown ether- or aza-crown ether-containing chromene or diazene derivative and a pharmaceutically acceptable carrier.Type: GrantFiled: December 21, 2005Date of Patent: December 23, 2008Assignee: The University of Hong KongInventors: Paul Michel Georges Vanhoutte, Chi-Ming Che, Kwok-Fai So, Iona Hiu Tung Sham
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Publication number: 20080255346Abstract: A mercury selective fluorescent chemosensor for detecting mercury ions (Hg2+) by a compound represented by formula 1 is provided. A novel fluorescent sensitive compound prepared by introducing two aminopyrene functions as a fluorescent sensitive moiety into a binding site of the compound represented by the formula 1, is used for selectively detecting mercury ions (Hg2+) is also provided. The mercury selective fluorescent sensitive chemosensor is a switch type chemosensor having ON-OFF-type Hg2+-selective fluorescence quenching behavior and is not affected by other coexistent metal ions. The changes in fluorescence of the compounds represented by formula 1 were analyzed by ratiometric approach using monomer and excimer emissions of the pyrene fluorophore to selectively signal the concentration of mercury ions (Hg2+). The chemosensor can detect mercury ions in a micromolar unit even in a solution including an excess of water.Type: ApplicationFiled: October 9, 2007Publication date: October 16, 2008Applicant: Chung-Ang University Industry-Academy Cooperation FoundationInventors: Suk-Kyu Chang, Jun Soo Kim, Myung Gil Choi, Ki Cheol Song, Sangdoo Ahn
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Patent number: 7432371Abstract: Nanofilms useful for filtration are prepared from oriented amphiphilic molecules and oriented macrocyclic modules. The amphiphilic species may be oriented on an interface or surface. The nanofilm may be prepared by depositing or attaching an oriented layer to a substrate. A nanofilm may also be prepared by coupling the oriented macrocyclic modules to provide a membrane.Type: GrantFiled: February 7, 2003Date of Patent: October 7, 2008Assignee: Covalent Partners, LLCInventors: Joshua W. Kriesel, Timothy B. Karpishin, Donald B. Bivin, Grant Merrill, Martin S. Edelstein, Thomas H. Smith, Jeffery A. Whiteford, Robert T. Jonas, Mark Micklatcher, Serena Joshi
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Publication number: 20080221158Abstract: The present invention relates to 15-membered macrolides substituted at the 4? position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.Type: ApplicationFiled: May 11, 2004Publication date: September 11, 2008Inventors: Sulejman Alihodzic, Andrea Berdik, Richard Lewis Jarvest, Gorjana Lazarevski
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Publication number: 20080161554Abstract: Disclosed are a macrocyclic carbodiimide (MC-CDI) and a process for synthesizing the same through condensation of a molecule with multiple-isocyanate terminal functional groups under high dilution in the presence of a phospholene catalyst such as phospholene or arsenic catalyst. Also disclosed are MC-CDI derivatives, such as MC-urea (MC-U), MC-acylurea (MC-ACU), acid functionalized MC-ACU, and anhydride functionalized MC-ACU, processes for synthesizing the same, and the applications of such derivatives as hydrolysis stabilizers in organic polymeric materials, such as polyurethane (PU) and polyesters, as well as the applications in the syntheses of the amide- and imide-modified polyurethane by ring-opening reaction of the MC-ACU.Type: ApplicationFiled: December 28, 2006Publication date: July 3, 2008Applicant: GREAT EASTERN RESINS INDUSTRIAL CO., LTD.Inventors: Shenghong A. Dai, Chih-Chia Cheng, Chien-Wen Chen, Chih-Hung Chen
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Publication number: 20080139806Abstract: Methods and compounds are provided for the formation of carbon-nitrogen or carbon-carbon bonds comprising reacting an amine or an aryl boronic acid with an aryl halide in the presence of a palladium catalyst, a base, and a compound of formula II:Type: ApplicationFiled: January 24, 2008Publication date: June 12, 2008Inventors: John G. Verkade, Sameer Urgaonkar, JuHua Xu
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Patent number: 7311970Abstract: A medical device comprising a substrate having a plasma polymerized functionality bonded to at least a portion of the substrate. A superoxide dismutase mimic agent having a complimentary functional group to the plasma polymerized functionality is bonded to the portion of the substrate by bonding to the plasma polymerized functionality.Type: GrantFiled: September 17, 2004Date of Patent: December 25, 2007Assignee: Abbott Cardiovascular Systems Inc.Inventors: Eugene T. Michal, Murthy Simhambhatla, Charles D. Claude
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Patent number: 7309567Abstract: The invention relates to a process for reducing the fluorescence quenching caused by the measuring medium, in a fluorescence assay for an analyte using at least one fluorescent label, characterized in that a fluorescent conjugate comprising an oligonucleotide bonded to a rare-earth metal cryptate is introduced into the measuring medium.Type: GrantFiled: March 14, 2000Date of Patent: December 18, 2007Assignee: CIS Bio InternationalInventors: Gerard Mathis, Herve Bazin, Eric Trinquet
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Patent number: 7279491Abstract: Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: October 23, 2003Date of Patent: October 9, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Richard L. Apodaca, Curt A. Dvorak, Chandravadan R. Shah, Wei Xiao
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Patent number: 7271154Abstract: This invention features a compound of the following formula: wherein T is a transportophore, L is a bond or linker, and C is an antibiotic therapeutic agent, the transportophore is covalently bonded to the antibiotic therapeutic agent via the bond or the linker, and the transportophore is an azithromycin derivative or crown ether derivative.Type: GrantFiled: February 14, 2003Date of Patent: September 18, 2007Assignee: Merckle GmbHInventors: Michael Burnet, Jan-Hinrich Guse, Gene Kim
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Patent number: 7091196Abstract: The invention provides a family of compounds useful as anti-infective agents and/or anti-proliferative agents, for example, chemotherapeutic agents, anti-fungal agents, anti-bacterial agents, anti-parasitic agents, anti-viral agents, and/or anti-inflammatory agents, and/or prokinetic (gastrointestinal modulatory) agents, having the formula: or pharmaceutically acceptable salts, esters, or prodrugs thereof.Type: GrantFiled: September 25, 2003Date of Patent: August 15, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Deping Wang, Joyce A. Sutcliffe, Adegboyega K. Oyelere, Timothy S. McConnell, Joseph A. Ippolito, John N. Abelson, Dane M. Springer, Joseph M. Salvino, Rongliang Lou, Joel A. Goldberg, Jay J. Farmer, Erin M. Duffy, Ashoke Bhattacharjee
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Patent number: 7067508Abstract: The present invention relates to a novel diaminedithiol derivative or a pharmaceutically acceptable salt thereof; radiorhenium or radiotechneticum complex thereof; a composition for treating liver cancer comprising the radiorhenium complex and lipiodol; and, a preparative kit of the composition for treating liver cancer. In the composition according to the invention, the diaminedithiol derivative is a novel compound in which long chain alkyl groups were introduced to diaminedithiol, capable of forming a radiorhenium or radiotechnetium complex thereof with an ease and leading to stronger van der Waals bonds with lipiodol. As a result, the complex becomes more stable in a medium, lipiodol, whereby the composition of the invention exhibits a high accumulation rate in liver cancer tissue when injected via hepatic artery, thereby capable of achieving an efficient treatment of liver cancer.Type: GrantFiled: March 8, 2002Date of Patent: June 27, 2006Assignee: Seoul National University Industry FoundationInventors: Jae Min Jeong, Young Ju Kim, Yun-Sang Lee, Dong Soo Lee, June-Key Chung, Myung Chul Lee
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Patent number: 7022717Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV- or FIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.Type: GrantFiled: November 7, 2003Date of Patent: April 4, 2006Assignee: AnorMED, Inc.Inventors: Gary James Bridger, Eva Maria Boehringer, Zhongren Wang, Dominique Schols, Renato Tony Skerlj, David Earl Bogucki
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Patent number: 6949537Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: April 5, 2004Date of Patent: September 27, 2005Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Patent number: 6936700Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.Type: GrantFiled: January 17, 2003Date of Patent: August 30, 2005Assignee: NeoRx CorporationInventor: Sudhakar Kasina
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Patent number: 6887994Abstract: A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. In another case, the C-nitroso compound contains the moiety —C—N(O)X— where X is S, O or NR. One embodiment is directed to COX-2 inhibitors where a tertiary carbon atom and/or an oxygen atom and/or a sulfur atom is nitrosylated.Type: GrantFiled: January 17, 2003Date of Patent: May 3, 2005Assignee: Duke UniversityInventors: Jonathan S. Stamler, Eric J. Toone
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Patent number: 6869589Abstract: The present invention relates to cryptate compounds useful as chelating agents. In particular, the present invention relates to functionalized derivatives of certain cryptate compounds. These functionalized derivatives are suitable for use in radiolabelling and similar applications. The present invention also relates to a method for diagnosis or therapy of a disease utilizing functionalized derivatives of cryptase compounds.Type: GrantFiled: January 5, 2000Date of Patent: March 22, 2005Assignees: Australian Nuclear Science & Technology Organization, The Australian National UniversityInventors: Suzanne V. Smith, John M. Harrowfield, Nadine M. Di Bartolo, Alan McLeod Sargeson
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Patent number: 6849203Abstract: The invention relates to photoisomerizable compounds of formula I wherein A, Z, L, R, R1, k, m and r are defined herein.Type: GrantFiled: April 5, 2002Date of Patent: February 1, 2005Assignee: Merck Patent Gesellschaft Mit Beschraenkter HaftungInventors: Louise Diane Farrand, Christopher Worrall, Owain Llyr Parri
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Patent number: 6787522Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, anType: GrantFiled: April 30, 2002Date of Patent: September 7, 2004Assignee: British Biotech PharmaceuticalsInventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
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Patent number: 6764996Abstract: Compounds of formula (I) formula (II) formula (III) and formula (IV) or pharmaceutically acceptable salts or prodrugs thereof, are antibacterial agents. Compositions containing the compounds, processes for making the compounds, synthetic intermediates employed in the processes, and methods for treatment and prevention of bacterial infections are disclosed.Type: GrantFiled: July 25, 2000Date of Patent: July 20, 2004Assignee: Abbott LaboratoriesInventors: Yat Sun Or, Robert F. Keyes, Zhenkun Ma
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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: 20040087567Abstract: The present invention relates to a novel diaminedithiol derivative or a pharmaceutically acceptable salt thereof; radiorhenium or radiotechneticum complex thereof; a composition for treating liver cancer comprising the radiorhenium complex and lipiodol; and, a preparative kit of the composition for treating liver cancer.Type: ApplicationFiled: August 25, 2003Publication date: May 6, 2004Inventors: Jae Min Jeong, Young Ju Kim, Yun-Sang Lee, Dong Soo Lee, June-Key Chung, Myung Chul Lee
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Patent number: 6667320Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV- or FIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.Type: GrantFiled: December 15, 2000Date of Patent: December 23, 2003Assignee: AnormedInventors: Gary James Bridger, Eva Maria Boehringer, Zhongren Wang, Dominique Schols, Renato Tony Skerlj, David Earl Bogucki
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Publication number: 20030199688Abstract: Macrocyclic module compositions are made from cyclic synthons. The macrocyclic module structures are prepared by stepwise or concerted schemes which couple synthons in a closed ring. The macrocyclic module structures may have a pore of nanometer dimensions.Type: ApplicationFiled: August 23, 2002Publication date: October 23, 2003Inventors: Josh Kriesel, Timothy B. Karpishin, Donald B. Bivin, Grant Merrill, Martin Stuart Edelstein, Thomas H. Smith, Jeffery A. Whiteford, Robert Thomas Jonas
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Patent number: 6635637Abstract: Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R1, R3-R6, R21-R26, L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formulae I and II. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: August 2, 2001Date of Patent: October 21, 2003Assignee: Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Tianbao Lu, Bruce Edward Tomczuk, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Publication number: 20030191306Abstract: The invention relates to substituted N-Aliphatic-N-Aromatic tertiary-Heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis, dyslipidemia, and other coronary artery disease.Type: ApplicationFiled: December 16, 2002Publication date: October 9, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Deborah A. Mischke, Emily J. Reinhard, Barry L. Parnas, Melvin L. Rueppel
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Patent number: 6610697Abstract: This invention relates to a series of imidazopyrimidines of Formula I, and pharmaceutical compositions containing them. The compounds of the invention inhibit the production of a number of inflammatory cytokines and are useful in the treatment and prevention of diseases associated with the overproduction thereof.Type: GrantFiled: October 27, 2000Date of Patent: August 26, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John H. Dodd, James R. Henry, Kenneth C. Rupert
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Patent number: 6608048Abstract: This invention provides compounds of Formula (I), where A″, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.Type: GrantFiled: March 28, 2001Date of Patent: August 19, 2003Assignee: Wyeth HoldingsInventors: Hwei-Ru Tsou, Elsebe Geraldine Overbeek-Klumpers, Allan Wissner
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Patent number: 6548509Abstract: This invention encompasses compounds of the formula wherein Ar represents a mono-, di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; and R1 represents lower alkyl; R2 is hydrogen or lower alkyl; and R3 and R4 independently represent organic and inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.Type: GrantFiled: March 23, 2001Date of Patent: April 15, 2003Assignee: Neurogen CorporationInventor: Jun Yuan
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Patent number: 6545038Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: November 6, 2000Date of Patent: April 8, 2003Assignee: The Procter & Gamble CompanyInventors: Biswanath De, Stanislaw Pikul, Menyan Cheng, Neil Gregory Almstead, Randall Stryker Matthews, Michael George Natchus, Yetunde Olabisi Taiwo