Nitrogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 549/63)
  • Publication number: 20150023889
    Abstract: Disclosed are compounds, compositions, and methods relating to fluoride aptamers, fluoride-responsive riboswitches, fluoride-regulated expression constructs, fluoride transporters, nucleic acids encoding fluoride transporters, expression constructs encoding fluoride transporters, and cells containing or including any combination of these.
    Type: Application
    Filed: September 17, 2012
    Publication date: January 22, 2015
    Inventors: Ronald Breaker, Jenny Baker, Narasimhan Sudarsan, Zasha Weinberg, Adam Roth, Tyler Ames, James Nelson
  • Patent number: 8916183
    Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Lindsey G. Fischer, Gary D. Crouse, Thomas C. Sparks, Erich W. Baum
  • Publication number: 20140336137
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
  • Publication number: 20140275232
    Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
    Type: Application
    Filed: May 28, 2014
    Publication date: September 18, 2014
    Applicant: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
  • Publication number: 20140234365
    Abstract: The present invention relates to novel 2-hydroxyhippuric acid analogs, and methods for their synthesis and use. Such analogs are designed to provide a protected or functional moiety such as a free thiol (—SH) group or a protected thiol group, thereby providing a convenient linkage chemistry for coupling under mild conditions to a suitable group on a target protein, polypeptide, solid phase or detectable label.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Applicant: ALERE SAN DIEGO, INC.
    Inventor: Mariusz Banaszczyk
  • Patent number: 8772331
    Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: July 8, 2014
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
  • Publication number: 20140142156
    Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.
    Type: Application
    Filed: December 12, 2013
    Publication date: May 22, 2014
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Helen E. BLACKWELL, Christine E. McINNIS
  • Patent number: 8703811
    Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.
    Type: Grant
    Filed: May 7, 2009
    Date of Patent: April 22, 2014
    Assignees: Genzyme Corporation, Massachusetts Institute of Technology, President and Fellows of Harvard College
    Inventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
  • Patent number: 8680139
    Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: March 25, 2014
    Assignee: Progenra
    Inventors: Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
  • Patent number: 8674118
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: March 18, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
  • Patent number: 8546444
    Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.
    Type: Grant
    Filed: May 28, 2012
    Date of Patent: October 1, 2013
    Assignee: Magnachem International Laboratories, Inc.
    Inventors: Federico M. Gomez, C. Federico Gomez Garcia-Godoy
  • Patent number: 8357718
    Abstract: Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.
    Type: Grant
    Filed: February 4, 2008
    Date of Patent: January 22, 2013
    Assignee: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Nghe Nguyen-Ba, Liliane Halab, Bettina Hamelin, Oswy Z. Pereira, Carl Poisson, Melanie Proulx, Thumkunta Jagadeeswar Reddy, Zhang Ming-Qiang
  • Patent number: 8350061
    Abstract: Bacterial quorum-sensing molecule analogs having the following structures: and methods of reducing bacterial pathogenicity, comprising providing a biological system comprising pathogenic bacteria which produce natural quorum-sensing molecule; providing a synthetic bacterial quorum-sensing molecule having the above structures and introducing the synthetic quorum-sensing molecule into the biological system comprising pathogenic bacteria. Further is provided a method of targeted delivery of an antibiotic, comprising providing a synthetic quorum-sensing molecule; chemically linking the synthetic quorum-sensing molecule to an antibiotic to produce a quorum-sensing molecule-antibiotic conjugate; and introducing the conjugate into a biological system comprising pathogenic bacteria susceptible to the antibiotic.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: January 8, 2013
    Assignee: Los Alamos National Security, LLC
    Inventors: Rashi S. Iyer, Kumkum Ganguly, Louis A. Silks
  • Patent number: 8329924
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
    Type: Grant
    Filed: April 7, 2011
    Date of Patent: December 11, 2012
    Assignee: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
  • Publication number: 20120258965
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: June 22, 2012
    Publication date: October 11, 2012
    Applicants: The Johns Hopkins University, Cardioxyl Pharmaceuticals
    Inventors: John P. TOSCANO, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Patent number: 8269022
    Abstract: The present invention provides novel crystalline polymorphs of enantiopure Erdosteine, referred to as Form I and Form II, and processes for the preparation thereof.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: September 18, 2012
    Assignee: Edmond Pharma S.R.L
    Inventors: Pier Andrea Gatti, Matteo Zacche′, Massimo Nicola
  • Patent number: 8247443
    Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: August 21, 2012
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
  • Patent number: 8188145
    Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.
    Type: Grant
    Filed: April 18, 2005
    Date of Patent: May 29, 2012
    Assignee: Magnachem International Laboratories, Inc.
    Inventors: Federico M. Gomez, C. Federico Gomez Garcia-Godoy
  • Publication number: 20120114765
    Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.
    Type: Application
    Filed: March 31, 2010
    Publication date: May 10, 2012
    Inventors: Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
  • Publication number: 20110262492
    Abstract: A method of synthesizing a biocompatible hydrogel by covalently cross-linking an effective amount of a first macromonomer including a cyclic thioester group with an effective amount of a second macromonomer including a terminal cysteine group is disclosed. In addition, the synthesis and use of the following specific cyclic thioester macromonomer that can be used in the method, as well as specific hydrogels made using this macromonomer are disclosed. The disclosed method produces a biocompatible hydrogel, while producing substantially no toxic free thiol by-product. Accordingly, the method can be used in making biomedical products, such as sutures and tissue replacement biomaterials, and for encapsulating therapeutic cells and pharmaceuticals.
    Type: Application
    Filed: April 20, 2011
    Publication date: October 27, 2011
    Applicant: NORTHWESTERN UNIVERSITY
    Inventors: Phillip B. Messersmith, Jing Su, Bi-Huang Hu
  • Patent number: 8022079
    Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: September 20, 2011
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
  • Publication number: 20110178102
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Application
    Filed: June 30, 2004
    Publication date: July 21, 2011
    Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Vern L Schramm, Anthony A. Suave
  • Patent number: 7968560
    Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: June 28, 2011
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
  • Publication number: 20110152318
    Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.
    Type: Application
    Filed: July 2, 2009
    Publication date: June 23, 2011
    Applicant: Amorepacific Corporation
    Inventors: Byoung Young Woo, Sun-Young Kim, Yeonjoon Kim, Song Seok Shin, Jin Kwan Kim, Ki-Wha Lee, Dong Hyun Kim, Kyung Min Lim, Joo-Hyun Moh, Yeon Su Jeong, Jin Kyu Choi, Hyun Ju Koh, Jeongho Lee, Hyuk Kim, Jeong Hoon Yoon, Funan Li, Jee-Suk Kim, Young-Ger Suh
  • Publication number: 20110053890
    Abstract: Bacterial quorum-sensing molecule analogs having the following structures: and methods of reducing bacterial pathogenicity, comprising providing a biological system comprising pathogenic bacteria which produce natural quorum-sensing molecule; providing a synthetic bacterial quorum-sensing molecule having the above structures and introducing the synthetic quorum-sensing molecule into the biological system comprising pathogenic bacteria. Further is provided a method of targeted delivery of an antibiotic, comprising providing a synthetic quorum-sensing molecule; chemically linking the synthetic quorum-sensing molecule to an antibiotic to produce a quorum-sensing molecule-antibiotic conjugate; and introducing the conjugate into a biological system comprising pathogenic bacteria susceptible to the antibiotic.
    Type: Application
    Filed: September 1, 2009
    Publication date: March 3, 2011
    Applicant: Los Alamos National Security, LLC.
    Inventors: Rashi Iyer, Kumkum Ganguly, Louis A. Silks
  • Publication number: 20110046195
    Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.
    Type: Application
    Filed: June 24, 2010
    Publication date: February 24, 2011
    Inventors: Helen E. BLACKWELL, Christine E. McInnis
  • Patent number: 7833693
    Abstract: The present application relates to a compound of formula A-X—B, where (i) A-X—B form an ionic compound Ai Xi Bi where Ai and Bi are each individually an organic onium cation; and Xi is anion of the formula Q-R500—SO3? or (ii) A-X—B form a non-ionic compound Ac-Xc-Bc, where Ai, Bi, Q, R500, Ac, Bc, and Xc are defined herein. The compounds are useful as photoactive materials.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: November 16, 2010
    Inventors: M. Dalil Rahman, Francis M. Houlihan, Munirathna Padmanaban, SangHo Lee, Ralph R. Dammel, David Rentkiewicz, Clement Anyadiegwu
  • Publication number: 20100249435
    Abstract: The present invention provides novel crystalline polymorphs of enantiopure Erdosteine, referred to as Form I and Form II, and processes for the preparation thereof.
    Type: Application
    Filed: November 10, 2008
    Publication date: September 30, 2010
    Applicant: Edmond Pharma S.R.L
    Inventors: Pier Andrea Gatti, Matteo Zacche', Massimo Nicola
  • Publication number: 20100160423
    Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
    Type: Application
    Filed: December 21, 2009
    Publication date: June 24, 2010
    Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
  • Patent number: 7625914
    Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.
    Type: Grant
    Filed: December 20, 2005
    Date of Patent: December 1, 2009
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
  • Patent number: 7572826
    Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: January 13, 2004
    Date of Patent: August 11, 2009
    Assignee: AstraZeneca AB
    Inventors: Alan Wellington Faull, Craig Johnstone, Andrew David Morley, Jeffrey Philip Poyser
  • Publication number: 20090181320
    Abstract: Fluorine-free photoacid generators and photoresist compositions containing fluorine-free photoacid generators are enabled as alternatives to PFOS/PFAS photoacid generator-containing photoresists. The photoacid generators are characterized by the presence of a fluorine-free heteroaromatic sulfonate anionic component. The photoacid generators preferably contain an onium cationic component, more preferably a sulfonium cationic component. The photoresist compositions preferably contain an acid sensitive imaging polymer. The compositions are especially useful for forming material patterns using 193 nm (ArF) imaging radiation.
    Type: Application
    Filed: January 16, 2008
    Publication date: July 16, 2009
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Patent number: 7553868
    Abstract: The invention relates to thiophene carboxamides of formula (I) wherein Ar, R1, R2, R3, R4, R5, m and n are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: January 13, 2004
    Date of Patent: June 30, 2009
    Assignee: AstraZeneca AB
    Inventors: Andrew David Morley, Jeffrey Philip Poyser
  • Patent number: 7510657
    Abstract: The present invention is a method of preparing affinity ligands, which method comprises to provide a cyclic scaffold comprising a thiol group, a carbonyl group and an amine group; to derivatize the amine group of said scaffold with an electrophile that carries either a functionality capable of affinity interaction or a functionality capable of a second interaction with a target molecule; and to open up the derivatized scaffold and add an amine that carries either a functionality capable of a second interaction or a functionality capable of affinity interaction with a target molecule. The method provides provide affinity ligands, which are capable of affinity interaction as well as a second kind of interaction.
    Type: Grant
    Filed: March 5, 2004
    Date of Patent: March 31, 2009
    Assignee: GE Healthcare Bio-Sciences AB
    Inventors: Jean-Luc Maloisel, Nicolas Thevenin
  • Patent number: 7402608
    Abstract: Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.
    Type: Grant
    Filed: December 9, 2003
    Date of Patent: July 22, 2008
    Assignee: ViroChem Pharma Inc.
    Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Nghe Nguyen-Ba, Liliane Halab, Oswy Z. Pereira, Carl Poisson, Melanie Proulx, Thumkunta Jagadeeswar Reddy, Zhang Ming-Qiang
  • Patent number: 7393868
    Abstract: The present invention relates to AMPA receptor potentiators of Formula I: formulations comprising them, methods for their use, and intermediates useful for their preparation.
    Type: Grant
    Filed: June 5, 2006
    Date of Patent: July 1, 2008
    Assignee: Eli Lilly and Company
    Inventors: Ana Maria Castano Mansanet, Frederic Laurent Cordier, Esteban Dominguez-Manzanares, Jian Eric Hong, William Joseph Hornback, Delu Jiang
  • Patent number: 7375131
    Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.
    Type: Grant
    Filed: May 29, 2003
    Date of Patent: May 20, 2008
    Assignee: SmithKlineBeecham Corp.
    Inventors: James F. Callahan, Yue Hu Li
  • Patent number: 7358376
    Abstract: The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: February 7, 2001
    Date of Patent: April 15, 2008
    Assignee: AstraZeneca AB
    Inventors: Andrew Baxter, Stephen Brough, Alan Faull, Craig Johnstone, Thomas McInally
  • Patent number: 7238815
    Abstract: Process for the industrial synthesis of the compound of formula (I): Application to the synthesis of bivalent salts of ranelic acid and more especially strontium ranelate and its hydrates.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: July 3, 2007
    Assignee: Les Laboratoires Servier
    Inventors: Lucile Vaysse-Ludot, Jean-Pierre Lecouve, Pascal Langlois
  • Patent number: 7125907
    Abstract: This invention provides new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, inhibiting angiogenesis, effecting a TGF-? activity or a neuronal activity, and treating a glutamate abnormality, a compulsive disorder, neuropathy, pain, a prostate disease, cancer, Huntington's disease, diabetes, a retinal disorder or glaucoma.
    Type: Grant
    Filed: March 3, 2004
    Date of Patent: October 24, 2006
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Barbara S. Slusher, Takashi Tsukamoto
  • Patent number: 7098240
    Abstract: The invention relates to thiophene carboxamides of formula (I), wherein R1, R2, R3, A, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy
    Type: Grant
    Filed: July 19, 2002
    Date of Patent: August 29, 2006
    Assignee: AstraZeneca AB
    Inventors: David Griffiths, Craig Johnstone
  • Patent number: 7071215
    Abstract: Novel anthelmintic compositions containing thiophene derivatives as active ingredients are disclosed.
    Type: Grant
    Filed: October 16, 2003
    Date of Patent: July 4, 2006
    Assignee: Pharmacia & Upjohn Company LLC
    Inventor: Byung Hyun Lee
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 7014796
    Abstract: Nonlinear optically active compounds, methods for making nonlinear optically active compounds, compounds useful for making nonlinear optically active compounds, methods for making compounds useful for making nonlinear optically active compounds, macrostructures that include nonlinear optically active components, and devices including the nonlinear optically active compounds and the macrostructures.
    Type: Grant
    Filed: January 15, 2003
    Date of Patent: March 21, 2006
    Assignee: University of Washington
    Inventors: Kwan-Yue Jen, Hong Ma, Sen Liu, Larry R. Dalton
  • Patent number: 6972292
    Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: December 6, 2005
    Assignee: Novartis AG
    Inventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
  • Patent number: 6927298
    Abstract: A 3,4-alkylenedioxythiophenedioxide compound represented by formula (I): in which: A represents a C1-5-alkylene bridge; R represents an optionally substituted C1-24-alkyl, C3-18-cycloalkyl, C1-18-alkoxy or polyethylene oxide group (optionally with at least one substituent selected from the group consisting of an alcohol, amide, ether, ester or sulphonate group) or an optionally substituted aryl group; a polymer comprising monomeric units represented by formula (I); an aqueous dispersion of a polymer comprising monomeric units corresponding to at least one compound according to formula (I) and a polyanion; a chemical polymerization process for preparing the aqueous dispersion comprising the steps of: (i) providing a solution of a polyanion; (ii) adding a compound according to formula (I) and a thiophene or pyrrole compound to the solution provided in step (i); and (iii) adding an oxidizing or reducing system to the mixture provided in step (ii); a printable paste containing the aqueous dispersion; an elect
    Type: Grant
    Filed: August 27, 2003
    Date of Patent: August 9, 2005
    Assignee: Agfa-Gevaert
    Inventors: Bert Groenendaal, Frank Louwet, Hieronymus Andriessen
  • Patent number: 6919369
    Abstract: Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
    Type: Grant
    Filed: August 19, 2002
    Date of Patent: July 19, 2005
    Assignee: Genentech, Inc.
    Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
  • Patent number: 6881741
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
    Type: Grant
    Filed: June 11, 2002
    Date of Patent: April 19, 2005
    Assignee: ViroChem Pharma Inc.
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constanin Yannopoulos
  • Patent number: 6849660
    Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.
    Type: Grant
    Filed: August 1, 2000
    Date of Patent: February 1, 2005
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventors: Elizabeth Jefferson, Eric Swayze
  • Patent number: 6849733
    Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.
    Type: Grant
    Filed: August 22, 1997
    Date of Patent: February 1, 2005
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Yufeng Hong, Vlad Edward Gregor, Anthony Lai Ling, Eileen Valenzuela Tompkins