The Polycyclo Ring Systems Are Bonded To The Same Acyclic Carbon Atom Or To The Same Acyclic Carbon Chain (e.g., Di-[2-benzimidazolyl)-methane; Di-[benzimidazyl-(2)]-monohydroxyethylene, Etc.) Patents (Class 548/305.7)
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Patent number: 12098119Abstract: Disclosed by the present invention are an SIRT6 small-molecule allosteric activator and the application thereof and provided is an SIRT6 small-molecule allosteric activator that contains a derivative as shown in formula (1) or a pharmacologically acceptable salt thereof as the active ingredient. The SIRT6 small-molecule allosteric activator designed and synthesized in the present invention has high efficacy and low toxicity, may significantly activate SIRT6 activity during in vitro experiments, and has great importance in the development of pharmaceuticals for relevant diseases.Type: GrantFiled: May 14, 2018Date of Patent: September 24, 2024Assignee: Nutshell BioTech (Shanghai) Co., Ltd.Inventors: Jian Zhang, Yinyi Chen, Cong Ruan, Xiuyan Yang, Chengxiang Wang, Qiufen Zhang, Jialin Shang, Xinyuan Xu
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Patent number: 9199965Abstract: Disclosed herein are novel benzoimidazole derivatives functioning as antagonists to vanilloid receptor-1, and a pharmaceutical composition comprising the same. They are useful in preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraines, arthralgia, neuropathy, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, strokes, bladder hypersensitivity, irritable bowel syndrome, respiratory disorders such as asthma, chronic obstructive pulmonary disease, etc., burns, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.Type: GrantFiled: January 27, 2006Date of Patent: December 1, 2015Assignee: Daewoong Co., Ltd.Inventors: Ji Duck Kim, Hong Chul Yoon, In Woo Kim, Hyae Jung Hyun
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Patent number: 8952177Abstract: The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein X1, X1?, X1?, R1, R2 and R3 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: GrantFiled: March 13, 2014Date of Patent: February 10, 2015Assignee: Janssen Pharmaceutica NVInventors: Wenying Chai, Curt A. Dvorak, Wendy Eccles, James P. Edwards, Steven D. Goldberg, Paul J. Krawczuk, Alec D. Lebsack, Jing Liu, Daniel J. Pippel, Zachary S. Sales, Virginia M. Tanis, Mark S. Tichenor, John J. M. Wiener
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Publication number: 20140343286Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.Type: ApplicationFiled: December 15, 2011Publication date: November 20, 2014Inventors: Allan C. Krueger, Warren M. Kati, Clarence J. Maring, Rolf Wagner, Charles W. Hutchins
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Patent number: 8884029Abstract: A photoelectric conversion device capable of improving conversion efficiency is provided. The photoelectric conversion device includes a work electrode, an opposed electrode, and an electrolyte-containing layer. In the work electrode, a metal oxide semiconductor layer supporting a dye is provided. The dye contains a cyanine compound that has a methine chain, an indolenine skeleton bonded with both ends of the methine chain, and anchor groups introduced to a nitrogen atom included in the indolenine skeleton. Electron injection efficiency to the metal oxide semiconductor layer is improved, and the dye is hardly exfoliated from the metal oxide semiconductor layer.Type: GrantFiled: September 9, 2009Date of Patent: November 11, 2014Assignee: Adeka CorporationInventors: Junji Tanabe, Atsushi Monden, Masahiro Shinkai, Mitsuhiro Okada, Toru Yano, Yohei Aoyama, Yusuke Kubota
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Patent number: 8748433Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.Type: GrantFiled: April 25, 2011Date of Patent: June 10, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
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Publication number: 20140155382Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: November 22, 2013Publication date: June 5, 2014Applicant: ABBVIE INC.Inventors: David A. DEGOEY, Allan C. KRUEGER, Charles W. HUTCHINS, Warren M. KATI, William A. CARROLL
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Patent number: 8680274Abstract: Stable, bent allenes, organometallic complexes of bent allenes are provided along with methods of conducting chemical processes such as olefin metathesis, comprising contacting an olefin substrate with an organometallic complex as described herein, under suitable conditions.Type: GrantFiled: January 9, 2009Date of Patent: March 25, 2014Assignee: The Regents of the University of CaliforniaInventors: Guy Bertrand, Vincent Lavallo, Adam C. Dyker
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Publication number: 20130172570Abstract: This present invention provides a method of making benzazoles comprising a process of making aryl or alkyl benzazoles from corresponding aryl acid chlorides or alkyl acid chlorides without applying hazard condensing agent. The benzazole compounds described in this invention have following formula I: Wherein: n is an integer of from 3 to 8; Z is O, NR or S; and R and R? are individually hydrogen; alkyl of from 1 to 24 carbon atoms, for example, propyl, t-butyl, heptyl, and the like; aryl or hetero-atom substituted aryl of from 5 to 20 carbon atoms, for example, phenyl and naphthyl, furyl, thienyl, pyridyl, quinolinyl and other heterocyclic systems; or halo such as chloro, fluoro, bromo, cyano; or atoms necessary to complete a fused aromatic ring; and B is a linkage unit consisting of alkyl, aryl, substituted alkyl, or substituted aryl which conjugately or unconjugately connects the multiple benzazoles together.Type: ApplicationFiled: February 15, 2012Publication date: July 4, 2013Applicant: US Government as Represented by the Secretary of the ARMYInventors: Jianmin Shi, Eric W. Forsythe, David C. Morton
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Publication number: 20130172389Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.Type: ApplicationFiled: December 27, 2012Publication date: July 4, 2013Applicant: Allegan, Inc.Inventor: Allergan, Inc.
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Patent number: 8461351Abstract: A sterically bulky stabilizer that includes an alkylated-benzimidazolone compound, where the sterically bulky stabilizer is associated non-covalently with a benzimidazolone pigment, and the presence of the sterically bulky stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.Type: GrantFiled: July 28, 2011Date of Patent: June 11, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Rina Carlini, Darren Andrew Makeiff
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Patent number: 8410283Abstract: An electrolyte additive is selected from N-alkyl benzimidazole derivatives and is applicable to dye-sensitized solar cells. Accordingly, the electrolyte additive can be added to electrolyte at low concentration, and loss of function due to crystallization after long-term use can be prevented; in addition, short circuit photocurrent density and solar energy-to-electricity conversion efficiency of solar cells incorporating the electrolyte additive can be increased.Type: GrantFiled: July 15, 2010Date of Patent: April 2, 2013Assignee: National Taipei University of TechnologyInventors: Sheng-Tung Huang, Chung-Kuang Yang
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Publication number: 20130053403Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.Type: ApplicationFiled: April 25, 2011Publication date: February 28, 2013Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
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Publication number: 20120215005Abstract: The present invention relates to diionic liquid salts of dicationic or dianionic molecules, as well as solvents comprising diionic liquids and the use of diionic liquids as the stationary phase in a gas chromatographic column.Type: ApplicationFiled: April 19, 2012Publication date: August 23, 2012Applicant: SIGMA-ALDRICH CO. LLCInventors: Daniel W. Armstrong, Jared Anderson
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Publication number: 20120146012Abstract: The present invention relates to heterocyclic radicals or diradicals, the dimers, oligomers, polymers, dispiro compounds and polycycles thereof, to the use thereof, to organic semiconductive materials and to electronic and optoelectronic components.Type: ApplicationFiled: February 16, 2012Publication date: June 14, 2012Applicant: NOVALED AGInventors: Michael Limmert, Olaf Zeika, Martin Amman, Horst Hartmann, Ansgar Werner
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Publication number: 20110312996Abstract: The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: May 16, 2011Publication date: December 22, 2011Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
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Publication number: 20110257235Abstract: The present disclosure relates to certain new and known triazolium and/or imidazolium salts and to their therapeutic use, for example in methods of treating or preventing an infection by a Plasmodium or Babesia parasite in a subject in need thereof. The triazolium and imidazolium salts are compounds of the Formula (I) or (II): wherein R1-R4, R1?-R3?, R8-R11, X, X?, X?, Y, Y? and Y? are as defined in the disclosure.Type: ApplicationFiled: September 4, 2009Publication date: October 20, 2011Inventors: Ian E. Crandall, Walter A. Szarek, Jason Z. Vlahakis
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Patent number: 7888515Abstract: The present invention relates to an improved process for preparing N,N?-carbonyldiazoles by reacting azoles with phosgene.Type: GrantFiled: December 7, 2004Date of Patent: February 15, 2011Assignee: Saltigo GmbHInventors: Andreas Job, Bernd Griehsel, Johannes Scherer
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Publication number: 20110021775Abstract: Stable, bent allenes, organometallic complexes of bent allenes are provided along with methods of conducting chemical processes such as olefin metathesis, comprising contacting an olefin substrate with an organometallic complex as described herein, under suitable conditions.Type: ApplicationFiled: January 9, 2009Publication date: January 27, 2011Inventors: Guy Bertrand, Vincent Lavallo, Adam C. Dyker
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Publication number: 20100292465Abstract: Novel N-heterocyclic carbene ligand precursors, N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are provided. Metal-carbene complexes comprising N-heterocyclic carbene ligands can be chiral, which are useful for catalyzing enantioselective synthesis. Methods for the preparation of the N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are given.Type: ApplicationFiled: February 15, 2008Publication date: November 18, 2010Applicant: University of Florida Research Foundation, Inc.Inventors: Adam Steven Veige, Mathew S. Jeletic, Roxy J. Lowry, Khalil A. Abboud
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Publication number: 20100221214Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 9, 2010Publication date: September 2, 2010Inventors: Yat Sun Or, Ce Wang, Xiaowen Peng, Lu Ying, Yao-Ling Qiu
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Publication number: 20100160402Abstract: The present invention relates to antimalarial agents. In particular, the present invention relates to the use of bisbenzimidazoles of Formula I for the prevention and/or treatment of malaria, wherein n is an integer selected from 0 to 10, and R1 and R2 are each independently selected from hydrogen, halogen, hydroxyl, alkyl, alkoxy, amino, alkylamino, alkylcarbonylamino, alkylcarbonyloxy, formyl, alkylcarbonyl, alkyloxycarbonyl, halocarbonyl, haloalkyl, haloalkoxy, carbamoyl, cyano, nitro, sulfo, or a carboxyl group.Type: ApplicationFiled: June 10, 2009Publication date: June 24, 2010Inventors: Tien Huang, Jean Jacques Vanden Eynde, Aurelie Pietka, Annie Mayence
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Publication number: 20100068176Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 5, 2009Publication date: March 18, 2010Inventors: Makonen Belema, Andrew C. Good, Jason Goodrich, Ramesh Kakarla, Guo Li, Omar D. Lopez, Van N. Nguyen, Jayne Kapur, Yuping Qiu, Jeffrey Lee Romine, Denis R. St. Laurent, Michael Serrano-Wu, Lawrence B. Snyder, Fukang Yang
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Publication number: 20090131401Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: February 12, 2008Publication date: May 21, 2009Applicant: Paratek Pharmaceuticals, Inc.Inventors: Stuart B. Levy, Michael N. Alekshun, Brent L. Podlogar, Kwasi Ohemeng, Atul K. Verma, Tadeusz Warchol, Beena Bhatia, Todd Bowser, Mark Grier
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Patent number: 7102012Abstract: A process is provided for preparing N,N?-carbonyldiazoles by reacting azoles with phosgene in halogenated aliphatic hydrocarbon solvents, the entirety of the azole for reaction being introduced in the solvent, followed by the addition of phosgene.Type: GrantFiled: May 11, 2005Date of Patent: September 5, 2006Assignee: LANXESS Deutschland GmbHInventors: Andreas Job, Bernd Griehsel
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Patent number: 7030150Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.Type: GrantFiled: May 9, 2002Date of Patent: April 18, 2006Assignee: Trimeris, Inc.Inventors: John William Lackey, Daniel S Kinder, Nicolai A Tvermoes
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Patent number: 6919331Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: GrantFiled: December 4, 2002Date of Patent: July 19, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Kuo-Long Yu, Xiangdong Wang, Yaxiong Sun, Christopher Cianci, Jan Willem Thuring, Keith Combrink, Nicholas Meanwell, Yi Zhang, Rita L. Civiello
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Patent number: 6844342Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: GrantFiled: August 19, 2003Date of Patent: January 18, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Kuo-Long Yu, Rita L. Civiello, Keith D. Combrink, Hatice Belgin Gulgeze, Ny Sin, Xiangdong Wang, Nicholas Meanwell, Brian Lee Venables, Yi Zhang, Bradley C. Pearc, Zhiwei Yin, Jan Willem Thuring
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Publication number: 20040186278Abstract: Disclosed are cyanine dyes having meso-substituents in the polymethine chain linking the heterocyclic ring systems.Type: ApplicationFiled: March 21, 2003Publication date: September 23, 2004Inventors: Chung-Yuan Chen, Shiv Kumar
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Patent number: 6784231Abstract: A pigment having weak dispersion force to be readily dispersed in a medium to be colored from which an excellent yellow image having superior transparency can be produced. The pigment includes a compound having the same chemical formula as C.I. Pigment Yellow 180. The BET specific surface area based on the nitrogen absorption process of the pigment is 20-100 m2/g, and the ratio of the absolute strength of X-ray diffraction at Bragg angle 2&thgr;=17.5°±0.2° to the absolute strength of X-ray diffraction at Bragg angle 2&thgr;=18.2°±0.2° of the pigment in a powder X-ray diffraction diagram using a CuK&agr; characteristic X-ray is less than 1.8/1.0. The present invention also provides a dispersion including the pigment and a thermoplastic resin having excellent transparency and color strength.Type: GrantFiled: March 19, 2002Date of Patent: August 31, 2004Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Katsunori Shimada, Junko Sunouchi
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Publication number: 20040067949Abstract: The present invention relates to novel indole derivatives, to their preparation and to their use, as inhibitors of the enzyme poly(ADP-ribose)polymerase or PARP (EC 2.4.2.30), for producing drugs.Type: ApplicationFiled: October 6, 2003Publication date: April 8, 2004Inventors: Roland Grandel, Wilfried Lubisch, Michael Kock, Thomas Hoger, Reinhold Muller, Sabine Schult, Uta Holzenkamp
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Publication number: 20040053981Abstract: Abstract Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.Type: ApplicationFiled: September 2, 2003Publication date: March 18, 2004Inventors: W. David Wilson, David W. Boykin, Richard R. Tidwell
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Publication number: 20030191320Abstract: The present invention provides a process for the preparation of a compound of formula (I) wherein Y represents —O—, —S— or —N(R2)—, R2 being hydrogen, C1-C10alkyl or aralkyl; Z represents a 2,5-furanyl, 2,5-thiophenyl, 4,4′-stilbenyl or a 1,2-ethyleny residue and R1 represents hydrogen, halogen, C1-C10alkoxyl, cyano, COOM or SO3M, M being hydrogen or an alkaline or alkaline earth metal, characterized by reacting a compound of formula (II) with a dicarboxylic acid of formula (III): HOOC-Z-COOH, or an ester thererof, Y, Z and R1 being as previously defined, in N-methylpyrrolidone or N,N-dimethylacetamide, in the presence of an acidic catalyst and, optionally, in the presence of a secondary solvent capable of removing water from the reaction mixture, which are useful as optical whitening agents for natural and synthetic materials.Type: ApplicationFiled: April 16, 2003Publication date: October 9, 2003Inventors: Victor Paul Eliu, Julia Hauser
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Patent number: 6562854Abstract: Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.Type: GrantFiled: June 4, 2001Date of Patent: May 13, 2003Assignee: Axys Pharmaceuticals, Inc.Inventors: Timothy J. Church, Neil Scott Cutshall, Anthony R. Gangloff, Thomas E. Jenkins, Martin S. Linsell, Joane Litvak, Kenneth D. Rice, Jeffrey R. Spencer, Vivian R. Wang
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Patent number: 6541486Abstract: Compounds, pharmaceutical compositions, and methods of use are described which are effective in inhibiting cell death, particularly apoptotic cell death. The compositions may be used for prevention and treatment of injuries associated with cell death, including ischemia, such as results from stroke or myocardial infarction, trauma, neurodegeneration, and inflammation.Type: GrantFiled: June 2, 2000Date of Patent: April 1, 2003Assignee: Elan Pharma International Ltd.Inventors: Catherine M. Bitler, Paul L. Wood, Duran T. Anstine, Anke Meyer-Franke, Qi Zhao, Mohamed A. Khan
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Publication number: 20020111497Abstract: This invention relates to the preparation of N,N′-carbonyldiazoles in a particularly advantageous manner by reacting corresponding azolide salts with phosgene in an aromatic compound or an ether as solvent. The azolide salts are preferably prepared by a novel process from an azole that is reacted with a compound of the formula M′R7 or MgR8Z′ in the presence of a solvent.Type: ApplicationFiled: July 17, 2001Publication date: August 15, 2002Inventors: Johannes Scherer, Alexander Klausener, Robert Sollner
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Patent number: 6403807Abstract: Bridged fluorescent dyes of the cyanine and squaraine families are disclosed. The dyes are useful as markers in assay techniques and offer advantages of undergoing excitation at a common wavelength but emitting at structure dependent different wavelengths.Type: GrantFiled: July 6, 2000Date of Patent: June 11, 2002Assignee: SurroMed, Inc.Inventors: Rajendra Singh, Gregory Gorski, Gary Frenzel
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Publication number: 20020049246Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.Type: ApplicationFiled: December 29, 2000Publication date: April 25, 2002Applicant: NeuroSearch A/SInventors: Bo Skaaning Jensen, Soren Peter Olesen, Lene Teuber, Dan Peters, Dorte Strobaek
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Patent number: 6194447Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.Type: GrantFiled: July 2, 1999Date of Patent: February 27, 2001Assignee: Neurosearch A/SInventors: Bo Skaaning Jensen, Søren Peter Olesen, Lene Teuber, Dan Peters, Dorte Strøbæk