Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/244)
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Patent number: 11453645Abstract: A process for producing a compound of the formula (I) involves at least reacting a compound of the formula (II) with hydrogen and water in the presence of at least one homogeneous transition metal catalyst TMC 1.Type: GrantFiled: October 29, 2019Date of Patent: September 27, 2022Assignee: BASF SEInventors: Thomas Schaub, Martin Ernst, Pilar Calleja, A. Stephen K. Hashmi
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Patent number: 10844014Abstract: A new intermediate for synthesizing 1-substituted-4-[phenyl(propanoyl)amino]piperidine-4-carbonitrile derivatives is laid open. Specifically set out is a method for use of this intermediate in the preparation of remifentanil. The enclosed shorter process offers a greater yield of products with higher purity as compared to methods reported in the prior art.Type: GrantFiled: October 25, 2019Date of Patent: November 24, 2020Assignee: HAMELN PHARMA GMBHInventors: Pavol Valachovic, Janka Králová, L'ubo{hacek over (s)} Slí{hacek over (z)}ik, Norbert Varga
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Patent number: 10577384Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor. The compounds have the general Formula I: or pharmaceutically acceptable salts thereof.Type: GrantFiled: February 6, 2018Date of Patent: March 3, 2020Assignee: Helsinn Healthcare SAInventors: Claudio Giuliano, Silvina Garcia Rubio, Antoine Daina, Angelo Guainazzi, Claudio Pietra
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Patent number: 10287305Abstract: Provided is a substituted piperidine compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as a prophylactic or therapeutic agent for narcolepsy.Type: GrantFiled: February 1, 2017Date of Patent: May 14, 2019Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tatsuhiko Fujimoto, Kentaro Rikimaru, Hiromichi Sugimoto, Takahiro Matsumoto
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Patent number: 9096523Abstract: A cyclic amine compound having a prescribed configuration can be efficiently prepared by reducing an imine derivative in the presence of a sulfonic acid. Specifically, a cyclic amine compound which is substituted with an amino group and a carboxyl group in which both groups are arranged in the trans configuration can be prepared efficiently.Type: GrantFiled: March 28, 2012Date of Patent: August 4, 2015Assignee: KANEKA CORPORATIONInventors: Yoshinori Hirai, Akira Nishiyama
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Patent number: 9035062Abstract: A process for preparing the compound of the following formula (E): wherein Bn represents a benzyl group, and tBu represents a tert-butyl group, the process including: (a) subjecting the following compound (B) to trifluoroacetylation, wherein tBu represents a tert-butyl group to produce the following compound (C): wherein tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; (b) reacting the compound (C) with benzyloxyamine in the presence of a hydroxyl group activating agent to produce the following compound (D): wherein Bn represents a benzyl group, tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; and (c) subjecting the compound (D) to detrifluoroacetylation.Type: GrantFiled: May 27, 2014Date of Patent: May 19, 2015Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Takao Abe, Masayuki Okue, Yoshiaki Sakamaki
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Patent number: 9034903Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases. In some embodiments, the present invention provides a method for monitoring the activity of a soluble epoxide hydrolase, the method including contacting the soluble epoxide hydrolase with an amount of a compound of the present invention sufficient to produce a detectable change in the fluorescence of the soluble epoxide hydrolase by interacting with one or more tryptophan residues present in the catalytic site of said sEH.Type: GrantFiled: February 1, 2013Date of Patent: May 19, 2015Assignee: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Kin Sing Lee, Christophe Morisseau
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Publication number: 20150087823Abstract: The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.Type: ApplicationFiled: April 26, 2013Publication date: March 26, 2015Inventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Kunihiko Higashiura
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Publication number: 20150079035Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.Type: ApplicationFiled: April 2, 2013Publication date: March 19, 2015Inventors: Brent R. Stockwell, Scott J. Dixon, Rachid Skouta
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Publication number: 20150065718Abstract: A method for preparing 1-adamantyltrimethylammonium methylcarbonate or N,N-dimethyl-3,5-dimethylpiperidinium methylcarbonate is disclosed. The method comprises reacting dimethyl carbonate and 3,5-dimethylpiperidine or a 1-adamantylamine compound and in the presence of water in a sealed vessel at a temperature of from 80 to 200° C. The 1-adamantylamine compound is 1-adamantylamine, 1-adamantylmethylamine, or mixtures thereof.Type: ApplicationFiled: August 28, 2014Publication date: March 5, 2015Inventor: RICHARD CHARLES BRYAN
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Publication number: 20150011586Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases. In some embodiments, the present invention provides a method for monitoring the activity of a soluble epoxide hydrolase, the method including contacting the soluble epoxide hydrolase with an amount of a compound of the present invention sufficient to produce a detectable change in the fluorescence of the soluble epoxide hydrolase by interacting with one or more tryptophan residues present in the catalytic site of said sEH.Type: ApplicationFiled: February 1, 2013Publication date: January 8, 2015Inventors: Bruce D. Hammock, Kin Sing Lee, Christophe Morisseau
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Publication number: 20140303375Abstract: A process for preparing the compound of the following formula (E): wherein Bn represents a benzyl group, and tBu represents a tert-butyl group, the process including: (a) subjecting the following compound (B) to trifluoroacetylation, wherein tBu represents a tert-butyl group to produce the following compound (C): wherein tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; (b) reacting the compound (C) with benzyloxyamine in the presence of a hydroxyl group activating agent to produce the following compound (D): wherein Bn represents a benzyl group, tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; and (c) subjecting the compound (D) to detrifluoroacetylation.Type: ApplicationFiled: May 27, 2014Publication date: October 9, 2014Applicant: Meiji Seika Pharma. Co., Ltd.Inventors: Takao ABE, Masayuki OKUE, Yoshiaki SAKAMAKI
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Publication number: 20140296526Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.Type: ApplicationFiled: May 10, 2014Publication date: October 2, 2014Applicant: WOCKHARDT LIMITEDInventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
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Publication number: 20140275126Abstract: Disclosed is a process for the preparation of the following compounds: where R1, R1a and R2a have the definitions in the description, as well as a process to prepare other intermediates that may be useful to synthesise downstream products, especially compounds that are useful as medicaments, for instance Bruton's tyrosine kinase (Btk) inhibitors such as ibrutinib. Also disclosed are other processes, other intermediates and compounds per se.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Inventors: Philip PYE, Cyril BEN HAIM, Matteo CONZA, Ioannis Nicolaos HOUPIS
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Patent number: 8829191Abstract: The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).Type: GrantFiled: June 15, 2012Date of Patent: September 9, 2014Inventors: Melanie Simone Ronsheim, Saibaba Racha, Graham Richard Lawton, Shao Hong Zhou, Yuriy B. Kalyan, Michael Golden, David Milne, Alexander Telford, Janette Cherryman, Alistair Boyd, Andrew John Phillips, Mahendra G. Dedhiya
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Publication number: 20140235636Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.Type: ApplicationFiled: April 25, 2014Publication date: August 21, 2014Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins UniversityInventors: John P. Toscano, Art Sutton, Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
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Publication number: 20140221428Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: April 22, 2014Publication date: August 7, 2014Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei LY, Garrett Thomas POTTER, Jared Andrew FORRESTER
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Patent number: 8791264Abstract: The invention relates to piperidinyl and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: April 13, 2007Date of Patent: July 29, 2014Assignee: Purdue Pharma L.P.Inventors: Zhengming Chen, Bin Shao, Jiangchao Yao, Xiaoming Zhou
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Publication number: 20140203226Abstract: A photochromic curable composition that contains a (meth)acrylate compound represented by the following formula (1-X1); (wherein Y is an oxygen atom or a divalent group represented by —NH—, R1 and R2 are hydrogen atoms or methyl groups, R3 is an alkylene group having 1 to 6 carbon atoms, R4 is an alkylene group having 1 to 6 carbon atoms, a cycloalkylene group having 3 to 8 carbon atoms and which may include a double bond, or an arylene group having 6 to 10 carbon atoms, and a is a positive number of 1 to 20), other radically polymerizable monomers and a photochromic compound. The invention provides a lens that features excellent durability and high photochromic property free of the problems of turbidity in the surfaces of the lens caused by bleed out or the peeling in the step of production.Type: ApplicationFiled: October 15, 2012Publication date: July 24, 2014Applicant: Tokuyama CorporationInventors: Junji Takenaka, Junji Momoda
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Patent number: 8778628Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 17, 2013Date of Patent: July 15, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Patent number: 8748617Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.Type: GrantFiled: August 6, 2012Date of Patent: June 10, 2014Assignees: University of Tokyo, Otsuka Chemical Co., Ltd.Inventors: Hiroaki Suga, Jun Igarashi
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Patent number: 8741894Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: March 17, 2011Date of Patent: June 3, 2014Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Garrett Thomas Potter, Jared Andrew Forrester
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Patent number: 8669257Abstract: The present invention provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein each of W, Q, R1, R2, R3, R4, R5, m, and n is as defined herein, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: March 22, 2010Date of Patent: March 11, 2014Assignee: The Johns Hopkins UniversityInventors: Jun O. Liu, Yunzhao Ren, Fan Pan, Curtis R. Chong, Reinhold Penner, Jonathan R. Behr
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Publication number: 20140018317Abstract: A compound having a structure of:Type: ApplicationFiled: February 17, 2012Publication date: January 16, 2014Applicant: University of Pittsburgh-Of the Commonwealth System of Higher EducationInventors: Peter Wipf, Marie-Celine Frantz
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Patent number: 8624022Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.Type: GrantFiled: October 7, 2011Date of Patent: January 7, 2014Assignee: UCB Pharma, S.A.Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
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Patent number: 8623887Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2, R4, Rg, X, m, n and p are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: May 11, 2007Date of Patent: January 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Stephan Karl Zahn, Bojan Bister, Guido Boehmelt, Ulrich Guertler, Andreas Mantoulidis, Ulrich Reiser, Andreas Schoop, Flavio Solca, Ulrike Tontsch-Grunt, Matthias Treu
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Patent number: 8603947Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.Type: GrantFiled: July 20, 2011Date of Patent: December 10, 2013Assignee: Bayer Cropscience AGInventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
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Publication number: 20130281702Abstract: A method and an intermediate are provided for preparing fentanyl. Aniline and 1-phenylethyl-4-piperidone are reacted with a borane complex, in a lower C1-C4 alcoholic solvent, in the presence of an alkanoic acid. The reaction mixture is then treated with a hydrohalic acid to precipitate 4-anilino-N-phenethyl-4-piperidine (ANPP) as the bis-hydrohalide salt in high yield and purity. This ANPP salt may be directly treated with propionyl halide to produce fentanyl, or the ANPP salt may be converted to the free base of ANPP and similarly treated with propionyl halide to produce fentanyl.Type: ApplicationFiled: April 23, 2013Publication date: October 24, 2013Inventors: Jonathan P. Pease, Anthony J. LePine, Catherine M. Smith
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Publication number: 20130274475Abstract: Substituted bicyclic beta-lactams of Formula I: are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.Type: ApplicationFiled: June 6, 2013Publication date: October 17, 2013Inventors: Ian MANGION, Nelo Rivera, Rebecca T. Ruck, Michael Shelvin
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Patent number: 8519188Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.Type: GrantFiled: June 15, 2009Date of Patent: August 27, 2013Assignee: Marc-Henry PittyInventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
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Patent number: 8492111Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 7, 2010Date of Patent: July 23, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
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Publication number: 20130158050Abstract: The present invention relates to a compound of formula I wherein R1, R2, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.Type: ApplicationFiled: February 14, 2013Publication date: June 20, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8466238Abstract: The invention aims to provide latent curing agents which exert high low-temperature curing properties when used together with ionically polymerizable compounds and which exhibit high storage stability at room temperature. Latent curing agents for ionically polymerizable compounds which agents each contain a hydroxyl-free amine imide compound having an N—N bond energy of 100 to 210 kJ/mol as determined by B3LYP functional theory method.Type: GrantFiled: December 26, 2008Date of Patent: June 18, 2013Assignee: Mitsui Chemicals, Inc.Inventors: Hiroaki Tamatani, Mitsuaki Chida, Yugo Yamamoto, Yuichi Ito, Takashi Nakano, Naritoshi Yoshimura
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Publication number: 20130116216Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.Type: ApplicationFiled: November 12, 2010Publication date: May 9, 2013Inventors: Celia Dominguez, John Wityak, Michael Prime, Stephen Martin Courtney, Christopher Yarnold, Frederick Brookfield, Richard Marston, Douglas Macdonald
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Patent number: 8399486Abstract: The invention relates to pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, Z and m are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: April 8, 2008Date of Patent: March 19, 2013Assignee: Purdue Pharma L.P.Inventors: Donald J. Kyle, Jiangchao Yao
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Publication number: 20130065756Abstract: Compounds of the formula I wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: November 22, 2010Publication date: March 14, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Publication number: 20130012712Abstract: The disclosure relates to a method for preparing a compound of formula (I), wherein P1 and P2 are groups protecting the carboxylic acid and oxyamine functions, starting from pyroglutamic acid (S). The disclosure also relates to novel intermediates.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventors: Alain Priour, Alain Bonnet, Gilles Oddon, Alain Mazurie
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Patent number: 8350042Abstract: Disclosed are compounds and methods of synthesis of Formula I for the development of antiviral drugs for the treatment of HCV infection.Type: GrantFiled: January 29, 2009Date of Patent: January 8, 2013Assignee: The Regents of the University of CaliforniaInventors: Thomas C. Hermann, Maia Carnevali
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Patent number: 8338439Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same. In some embodiments, the present invention provides a compound of formula I-a or I-b: wherein each of Ring A, Ring B, W1, W2, Ry, Rv, Rx, m, p, and R1 is described herein.Type: GrantFiled: December 29, 2009Date of Patent: December 25, 2012Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Publication number: 20120323010Abstract: The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).Type: ApplicationFiled: June 15, 2012Publication date: December 20, 2012Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventors: Melanie Simone Ronsheim, Saibaba Racha, Graham Richard Lawton, Shao Hong Zhou, Yuriy B. Kalyan, Michael Golden, David Milne, Alexander Telford, Janette Cherryman, Alistair Boyd, Andrew John Phillips, Mahendra G. Dedhiya
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Publication number: 20120296094Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.Type: ApplicationFiled: August 6, 2012Publication date: November 22, 2012Applicants: OTSUKA CHEMICAL CO., LTD., UNIVERSITY OF TOKYOInventors: Hiroaki SUGA, Jun Igarashi
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Publication number: 20120289548Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.Type: ApplicationFiled: June 29, 2012Publication date: November 15, 2012Applicant: Nektar TherapeuticsInventors: Jennifer RIGGS-SAUTHIER, Bo-Liang Deng, Timothy A. Riley
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Patent number: 8304403Abstract: Compounds of formula Ia and Ib and wherein A, B, C and R1 are described herein.Type: GrantFiled: June 10, 2010Date of Patent: November 6, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
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Publication number: 20120277250Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: July 11, 2012Publication date: November 1, 2012Applicant: THERAVANCE, INC.Inventors: YuHua Ji, Craig HUSFELD, YongQi MU, Cameron Smith
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Patent number: 8288553Abstract: The disclosure relates to a method for preparing a compound of formula (I), wherein P1 and P2 are groups protecting the carboxylic acid and oxyamine functions, starting from pyroglutamic acid (S). The disclosure also relates to novel intermediates.Type: GrantFiled: September 12, 2008Date of Patent: October 16, 2012Inventors: Alain Priour, Alain Bonnet, Gilles Oddon, Alain Mazurie
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Publication number: 20120245026Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.Type: ApplicationFiled: November 30, 2010Publication date: September 27, 2012Applicant: Syngenta Crop Protection LLCInventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Publication number: 20120238452Abstract: Compounds of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: November 29, 2010Publication date: September 20, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Patent number: 8258307Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.Type: GrantFiled: November 6, 2007Date of Patent: September 4, 2012Assignees: University of Tokyo, Otsuka Chemical Co., Ltd.Inventors: Hiroaki Suga, Jun Igarashi
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Patent number: 8252934Abstract: 4-amino-2,2,6,6-tetramethylpiperidine is prepared by reacting 2,2,6,6-tetramethylpiperidine-4-one with ammonia and hydrogen in the presence of nickel and/or cobalt catalyst and water. The main reaction is carried out at a pressure of at most 50 bar and a temperature of at most 120° C. up to a conversion of the 2,2,6,6-tetramethylpiperidine-4-one of at least 80%. Then, an after-reaction takes place at a higher temperature and at a higher pressure compared to the pressure and temperature of the main reaction.Type: GrantFiled: January 29, 2009Date of Patent: August 28, 2012Assignee: Evonik Degussa GmbHInventors: Volker Brehme, Daniel Dembkowski
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Publication number: 20120136073Abstract: There are provided for herein novel amine-containing transfection compounds and methods for making and using same. The compounds are generally obtained by reacting a primary amine with an unsaturated compound. Transfection complexes made using the amine-containing transfection compounds in combination with additional compounds to encapsulate biologically active agents such as nucleic acids are also provided for herein. Methods of using the transfection complexes for the in vivo or in vitro delivery of biologically active agents are also described. The transfection complexes of the present invention are highly potent, thereby allowing effective modulation of a biological activity at relatively low doses compared to analogous transfection compounds known in the art.Type: ApplicationFiled: November 15, 2011Publication date: May 31, 2012Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Zhiwei Yang, Parul Angrish, Xavier de Mollerat du Jeu, Kristin Wiederholt