CPC Scheme Between 2015.05 and 2015.07
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Synthesis of 1,2,4 Oxadiazol-5-Imine, 1,2,4-Triazol-3-Imine and Derivatives: a Substituted Cyanamide-Based Strategy for Heterocycle Synthesis
Synthesis of 1,2,4 oxadiazol-5-imine, 1,2,4-triazol-3-imine and derivatives: A Substituted Cyanamide-based Strategy for Heterocycle Synthesis Shreesha V. Bhat A thesis submitted in partial fulfilment of the requirements of the University of Lincoln for the degree of Doctor of Philosophy June 2017 Statement of Originality “I, Shreesha V. Bhat, hereby declare that this submission is my own work and to the best of my knowledge it contains no materials previously published or written by another person, or substantial proportions of material which have been published or accepted for the award of any other degree or diploma at University of Lincoln or any other educational institution, except where references have been made in the thesis. Any contribution made to the research by others, with whom I have worked at the University of Lincoln or elsewhere, is explicitly acknowledged in the thesis. I also declare that the intellectual content of this thesis is the product of my own work, except to the extent that assistance from others in the project's design and conception or in style, presentation and linguistic expression is acknowledged.” (Shreesha V. Bhat) ii | P a g e Abstract Considering the importance of nitrogen-rich heterocycles in drug discovery, a novel strategy towards heterocycle synthesis was envisioned using cyanamide chemistry. Synthesis which involve mild conditions, avoids multi-step sequence and non-toxic reagents are desirable for generation of large combinatorial libraries of drug molecules. We envisaged that the NCN linkage of the cyanamide as well as the concomitant use of the nucleo-and electrophilic centres of the cyanamide could provide a novel synthetic route towards nitrogen heterocycles. -
Annual Conference Abstracts
ANNUAL CONFERENCE 14-17 April 2014 Arena and Convention Centre, Liverpool ABSTRACTS SGM ANNUAL CONFERENCE APRIL 2014 ABSTRACTS (LI00Mo1210) – SGM Prize Medal Lecture (LI00Tu1210) – Marjory Stephenson Climate Change, Oceans, and Infectious Disease Prize Lecture Dr. Rita R. Colwell Understanding the basis of antibiotic resistance University of Maryland, College Park, MD, USA as a platform for early drug discovery During the mid-1980s, satellite sensors were developed to monitor Laura JV Piddock land and oceans for purposes of understanding climate, weather, School of Immunity & Infection and Institute of Microbiology and and vegetation distribution and seasonal variations. Subsequently Infection, University of Birmingham, UK inter-relationships of the environment and infectious diseases Antibiotic resistant bacteria are one of the greatest threats to human were investigated, both qualitatively and quantitatively, with health. Resistance can be mediated by numerous mechanisms documentation of the seasonality of diseases, notably malaria including mutations conferring changes to the genes encoding the and cholera by epidemiologists. The new research revealed a very target proteins as well as RND efflux pumps, which confer innate close interaction of the environment and many other infectious multi-drug resistance (MDR) to bacteria. The production of efflux diseases. With satellite sensors, these relationships were pumps can be increased, usually due to mutations in regulatory quantified and comparatively analyzed. More recent studies of genes, and this confers resistance to antibiotics that are often used epidemic diseases have provided models, both retrospective and to treat infections by Gram negative bacteria. RND MDR efflux prospective, for understanding and predicting disease epidemics, systems not only confer antibiotic resistance, but altered expression notably vector borne diseases. -
Part One Amino Acids As Building Blocks
Part One Amino Acids as Building Blocks Amino Acids, Peptides and Proteins in Organic Chemistry. Vol.3 – Building Blocks, Catalysis and Coupling Chemistry. Edited by Andrew B. Hughes Copyright Ó 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim ISBN: 978-3-527-32102-5 j3 1 Amino Acid Biosynthesis Emily J. Parker and Andrew J. Pratt 1.1 Introduction The ribosomal synthesis of proteins utilizes a family of 20 a-amino acids that are universally coded by the translation machinery; in addition, two further a-amino acids, selenocysteine and pyrrolysine, are now believed to be incorporated into proteins via ribosomal synthesis in some organisms. More than 300 other amino acid residues have been identified in proteins, but most are of restricted distribution and produced via post-translational modification of the ubiquitous protein amino acids [1]. The ribosomally encoded a-amino acids described here ultimately derive from a-keto acids by a process corresponding to reductive amination. The most important biosynthetic distinction relates to whether appropriate carbon skeletons are pre-existing in basic metabolism or whether they have to be synthesized de novo and this division underpins the structure of this chapter. There are a small number of a-keto acids ubiquitously found in core metabolism, notably pyruvate (and a related 3-phosphoglycerate derivative from glycolysis), together with two components of the tricarboxylic acid cycle (TCA), oxaloacetate and a-ketoglutarate (a-KG). These building blocks ultimately provide the carbon skeletons for unbranched a-amino acids of three, four, and five carbons, respectively. a-Amino acids with shorter (glycine) or longer (lysine and pyrrolysine) straight chains are made by alternative pathways depending on the available raw materials. -
2016 Joint Meeting Program
April 15 – 17, 2016 Fairmont Chicago Millennium Park • Chicago, Illinois The AAP/ASCI/APSA conference is jointly provided by Boston University School of Medicine and AAP/ASCI/APSA. Meeting Program and Abstracts www.jointmeeting.org www.jointmeeting.org Special Events at the 2016 AAP/ASCI/APSA Joint Meeting Friday, April 15 Saturday, April 16 ASCI President’s Reception ASCI Food and Science Evening 6:15 – 7:15 p.m. 6:30 – 9:00 p.m. Gold Room The Mid-America Club, Aon Center ASCI Dinner & New Member AAP Member Banquet Induction Ceremony (Ticketed guests only) (Ticketed guests only) 7:00 – 10:00 p.m. 7:30 – 9:45 p.m. Imperial Ballroom, Level B2 Rouge, Lobby Level How to Solve a Scientific Puzzle: Speaker: Clara D. Bloomfield, MD Clues from Stockholm and Broadway The Ohio State University Comprehensive Cancer Center Speaker: Joe Goldstein, MD APSA Welcome Reception & University of Texas Southwestern Medical Center at Dallas Presidential Address APSA Dinner (Ticketed guests only) 9:00 p.m. – Midnight Signature Room, 360 Chicago, 7:30 – 9:00 p.m. John Hancock Center (off-site) Rouge, Lobby Level Speaker: Daniel DelloStritto, APSA President Finding One’s Scientific Niche: Musings from a Clinical Neuroscientist Speaker: Helen Mayberg, MD, Emory University Dessert Reception (open to all attendees) 10:00 p.m. – Midnight Imperial Foyer, Level B2 Sunday, April 17 APSA Future of Medicine and www.jointmeeting.org Residency Luncheon Noon – 2:00 p.m. Rouge, Lobby Level 2 www.jointmeeting.org Program Contents General Program Information 4 Continuing Medical Education Information 5 Faculty and Speaker Disclosures 7 Scientific Program Schedule 9 Speaker Biographies 16 Call for Nominations: 2017 Harrington Prize for Innovation in Medicine 26 AAP/ASCI/APSA Joint Meeting Faculty 27 Award Recipients 29 Call for Nominations: 2017 Harrington Scholar-Innovator Award 31 Call for Nominations: George M. -
Mild Reductive Functionalization of Amides Into N‐Sulfonylformamidines
http://www.diva-portal.org This is the published version of a paper published in ChemistryOpen. Citation for the original published paper (version of record): Trillo, P., Slagbrand, T., Tinnis, F., Adolfsson, H. (2017) Mild Reductive Functionalization of Amides into N-Sulfonylformamidines. ChemistryOpen, 6(4): 484-487 https://doi.org/10.1002/open.201700087 Access to the published version may require subscription. N.B. When citing this work, cite the original published paper. Permanent link to this version: http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-138585 DOI:10.1002/open.201700087 Mild Reductive Functionalization of Amides into N- Sulfonylformamidines Paz Trillo,[a] Tove Slagbrand,[a] Fredrik Tinnis,*[a] and Hans Adolfsson*[a, b] The development of aprotocolfor the reductivefunctionaliza- tion of amides into N-sulfonylformamidines is reported. The one-pot procedure is based on amild catalytic reduction of tertiaryamides into the corresponding enamines by the use of Mo(CO)6 (molybdenum hexacarbonyl) and TMDS (1,1,3,3-tetra- methyldisiloxane). The formed enamines were allowed to react with sulfonyl azidestogive the target compounds in moderate to good yields. The amidine functional group is frequently found in biological- ly activecompounds possessing anti-inflammatory,antibacteri- al, antiviral, antibiotic, and anestheticproperties.[1] They are also employed as intermediates and precursors in organic syn- thesis of importantheterocyclic compounds such as imida- zoles, quinazolines,isoquinolines, and pyrimidines.[2] Further- more, amidines are employed as ligandsinmetal complexes and as protecting groups for primary amines.[3] Scheme1.Preparation of amidines through a–c) electrophilic amide activa- The stability of amides makes this functional group valuable tion and d) reductive functionalization of amides. -
George Michael Humphrey Birchenough
GEORGE MICHAEL HUMPHREY BIRCHENOUGH Analysis of intestinal factors contributing to the age- dependency of systemic neuropathogenic Escherichia coli K1 infection in the neonatal rat Thesis submitted in accordance with the requirements of the UCL School of Pharmacy for the degree of Doctor of Philosophy Microbiology Group, Department of Pharmaceutics, UCL School of Pharmacy July 2012 PLAGIARISM STATEMENT This thesis describes research conducted in the UCL School of Pharmacy between October 2008 and July 2012 under the supervision of Professor Peter W. Taylor. I certify that the research described is original and that any parts of the work that have been conducted by collaboration are clearly indicated. I also certify that I have written all the text herein and have clearly indicated by suitable citation any part of the dissertation that has already appeared in publication. Signature: Date: Acknowledgements Firstly I wish to thank my supervisor, Professor Peter Taylor, for giving me the opportunity to work on such an interesting and rewarding project. Your continued support and enthusiasm has been a constant source of encouragement and I greatly appreciate all the advice and help (both scientific and general!) that you have provided over the last four years. I owe you a lot of beer. I also wish to thank my amazing parents for all their love and support over the eight years of my higher education. Without your enthusiasm and belief I would not have been able to follow this path. I sincerely promise I will now get a job! Furthermore, I wish to thank colleagues at the London School of Hygiene & Tropical Medicine, Dr. -
United States Patent Office Patented Jan
3,017,356 United States Patent Office Patented Jan. 16, 1962 1. 2 rated aliphatic radical, a cycloaliphatic radical, an aryl 3,017,356 radical, an aralkyl radical, an alkaryl radical, an alkoxy WillianPROCESS B. Hughes, OF andINHIBITING Verner L. Stronberg,CORROSION Webster alkyl radical, an aryloxyalkyl radical, and the like; and Groves, Mo., assignor's to Petroite Corporation, Wii A is an alkylene group; for example, ethylene and propyl mington, Del, a corporation of Delaware ene radicals, such as No Drawing. Original application Mar. 3, 1958, Ser. No. 718,391 Divided and this application Nov. 23, 1959, Ser. No. 854,553 -CH2CH2CH 15 Claims. (C. 252-8.55) CH-CH2 O B This application is a division of Serial No. 718,391, CHs filed March 3, 1958. This invention relates to esters of cyclic amidines of -CH-CH-CH,- the formula gh, CHis O 15 -bH-bH In general, the amidine esters are prepared by reacts o-o-c- ing a hydroxyaliphatic cyclic amidine ()-ROH with less where (A) and (B) are cyclic amidine-containing radicals, than a stoichiometric amount of a polycarboxylic acid to for example, imidazoline and tetrahydropyrimidine radi form a half ester cals (hereafter referred to as “amidine esters'). More 20 particularly, this invention relates to esters wherein. A contains one type of cyclic amidine ring and B contains (a)-R-O C-Z-COH the same or another type not selected in A. This inven which is subsequently reacted with an amidine forming tion also relates to a process of preparing these com polyamine to form the amidine ester pounds which comprises reacting a hydroxy-containing 25 O cyclic amidine with less than a stoichiometric amount of a polycarboxylic acid to form a partial ester and then re Q-R-O-)-2- acting this partial ester with a polyamine capable of form More specifically, the corrosion inhibiting aspect of this ing a second amidine ring of the same or different type. -
Poly(Vinylammonium Formate) and Process for Making Amidine
Europaisches Patentamt (19) European Patent Office Office europeenpeen des brevets EP0617 054B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) intci.e: C08F 8/12, C08F 8/44 of the grant of the patent: 04.12.1996 Bulletin 1996/49 (21) Application number: 94104538.7 (22) Date of filing: 22.03.1994 (54) Poly(vinylammonium formate) and process for making amidine-containing polymers Poly(Vinylammoniumformiat) und Verfahren zur Herstellung von Amidinegruppen enthaltender Polymeren Poly(formiate vinylique d'ammonium) et procede de preparation de polymeres contenant de groupes amidine (84) Designated Contracting States: (72) Inventor: Ford, Michael Edward BE DE FR GB NL Coopersburg, PA 18036 (US) (30) Priority: 25.03.1993 US 36757 (74) Representative: Kador & Partner Corneliusstrasse 15 (43) Date of publication of application: 80469 Miinchen (DE) 28.09.1994 Bulletin 1994/39 (56) References cited: (73) Proprietor: AIR PRODUCTS AND CHEMICALS, EP-A- 0 374 646 EP-A- 0 528 409 INC. DE-A-3 715 824 US-A- 4 393 174 Allentown, PA 18195-1501 (US) US-A- 4 943 676 DO ^> o Is- CO Note: Within nine months from the publication of the mention of the grant of the European patent, any person may give notice the Patent Office of the Notice of shall be filed in o to European opposition to European patent granted. opposition a written reasoned statement. It shall not be deemed to have been filed until the opposition fee has been paid. (Art. a. 99(1) European Patent Convention). LU Printed by Jouve, 75001 PARIS (FR) EP 0 617 054 B1 Description FIELD OF THE INVENTION 5 This invention relates to poly(vinylammonium formate) and to a process for its manufacture. -
European Patent Office U.S. Patent and Trademark Office
EUROPEAN PATENT OFFICE U.S. PATENT AND TRADEMARK OFFICE CPC NOTICE OF CHANGES 89 DATE: JULY 1, 2015 PROJECT RP0098 The following classification changes will be effected by this Notice of Changes: Action Subclass Group(s) Symbols deleted: C12Y 101/01063 C12Y 101/01128 C12Y 101/01161 C12Y 102/0104 C12Y 102/03011 C12Y 103/01004 C12Y 103/0103 C12Y 103/01052 C12Y 103/99007 C12Y 103/9901 C12Y 103/99013 C12Y 103/99021 C12Y 105/99001 C12Y 105/99002 C12Y 113/11013 C12Y 113/12012 C12Y 114/15002 C12Y 114/99028 C12Y 204/01119 C12Y 402/01052 C12Y 402/01058 C12Y 402/0106 C12Y 402/01061 C12Y 601/01025 C12Y 603/02027 Symbols newly created: C12Y 101/01318 C12Y 101/01319 C12Y 101/0132 C12Y 101/01321 C12Y 101/01322 C12Y 101/01323 C12Y 101/01324 C12Y 101/01325 C12Y 101/01326 C12Y 101/01327 C12Y 101/01328 C12Y 101/01329 C12Y 101/0133 C12Y 101/01331 C12Y 101/01332 C12Y 101/01333 CPC Form – v.4 CPC NOTICE OF CHANGES 89 DATE: JULY 1, 2015 PROJECT RP0098 Action Subclass Group(s) C12Y 101/01334 C12Y 101/01335 C12Y 101/01336 C12Y 101/01337 C12Y 101/01338 C12Y 101/01339 C12Y 101/0134 C12Y 101/01341 C12Y 101/01342 C12Y 101/03043 C12Y 101/03044 C12Y 101/98003 C12Y 101/99038 C12Y 102/01083 C12Y 102/01084 C12Y 102/01085 C12Y 102/01086 C12Y 103/01092 C12Y 103/01093 C12Y 103/01094 C12Y 103/01095 C12Y 103/01096 C12Y 103/01097 C12Y 103/0701 C12Y 103/08003 C12Y 103/08004 C12Y 103/08005 C12Y 103/08006 C12Y 103/08007 C12Y 103/08008 C12Y 103/08009 C12Y 103/99032 C12Y 104/01023 C12Y 104/01024 C12Y 104/03024 C12Y 105/01043 C12Y 105/01044 C12Y 105/01045 C12Y 105/03019 C12Y 105/0302 -
CHEM 330 Topics Discussed on Sept 28 Heterocycles Such As Pyrazole
CHEM 330 Topics Discussed on Sept 28 Heterocycles such as pyrazole, pyrimidine, etc., as common subunits of pharmaceuticals O O Celebrex (Pfizer) S Pyrimethamine H2N N H2N anti-inflammatory antimalarial N N N CF3 Cl R1 N NH N N R1 R3 R2 R4 R2 R3 pyrazole pyrimidine Imine– and enamine-type linkages in nitrogen heterocycles R1 H imine- N N enamine- imine- N N enamine- type type 1 3 type type R R R2 R4 R2 R3 pyrazole pyrimidine Principle: the construction of heterocyclic systems often involves the formation of imines (=Schiff bases) and / or enamines. These are produced upon the condensation of carbonyl compounds with appropriate amines (see CHEM 203 & CHEM 213 notes): 2 + 2 R cat. H R3 R2 ± H+ R3 R 3 R –NH2 + O N N 1 1 H 1 R – H2O R R primary enamine: amine ketone imine (= Schiff base): generally favored generally disfavored tautomer tautomer 4 2 + R4 2 4 R R cat. H R – H+ R R2 NH + O N N 1 3 1 R3 R – H2O R R R3 R1 secondary ketone iminium amine enamine ion Approach to the synthesis of pyrazoles by reaction of 1,3-dicarbonyls with hydrazine: lecture of Sept 28 p. 2 H H N imine-type N N enamine-type 2 imagine the imagine O NH linkage functionality releasing imino or the R1 R3 R1 R3 iminium R2 the imine ... R2 tautomer ... pyrazole: an aromatic compound H2N NH2 hydrazine H2N imagine O N (NH ) releasing O O "type A" 1 3 R1 R3 the imine R R 1,3-di-O functionality! (or iminum).. -
12) United States Patent (10
US007635572B2 (12) UnitedO States Patent (10) Patent No.: US 7,635,572 B2 Zhou et al. (45) Date of Patent: Dec. 22, 2009 (54) METHODS FOR CONDUCTING ASSAYS FOR 5,506,121 A 4/1996 Skerra et al. ENZYME ACTIVITY ON PROTEIN 5,510,270 A 4/1996 Fodor et al. MICROARRAYS 5,512,492 A 4/1996 Herron et al. 5,516,635 A 5/1996 Ekins et al. (75) Inventors: Fang X. Zhou, New Haven, CT (US); 5,532,128 A 7/1996 Eggers Barry Schweitzer, Cheshire, CT (US) 5,538,897 A 7/1996 Yates, III et al. s s 5,541,070 A 7/1996 Kauvar (73) Assignee: Life Technologies Corporation, .. S.E. al Carlsbad, CA (US) 5,585,069 A 12/1996 Zanzucchi et al. 5,585,639 A 12/1996 Dorsel et al. (*) Notice: Subject to any disclaimer, the term of this 5,593,838 A 1/1997 Zanzucchi et al. patent is extended or adjusted under 35 5,605,662 A 2f1997 Heller et al. U.S.C. 154(b) by 0 days. 5,620,850 A 4/1997 Bamdad et al. 5,624,711 A 4/1997 Sundberg et al. (21) Appl. No.: 10/865,431 5,627,369 A 5/1997 Vestal et al. 5,629,213 A 5/1997 Kornguth et al. (22) Filed: Jun. 9, 2004 (Continued) (65) Prior Publication Data FOREIGN PATENT DOCUMENTS US 2005/O118665 A1 Jun. 2, 2005 EP 596421 10, 1993 EP 0619321 12/1994 (51) Int. Cl. EP O664452 7, 1995 CI2O 1/50 (2006.01) EP O818467 1, 1998 (52) U.S. -
Conceptualizing Multiple Drug Use in Patients with Comorbidity and Multimorbidity: Proposal for Standard Definitions Beyond the Term Polypharmacy Umesh T
Journal of Clinical Epidemiology 106 (2019) 98e107 ORIGINAL ARTICLE Conceptualizing multiple drug use in patients with comorbidity and multimorbidity: proposal for standard definitions beyond the term polypharmacy Umesh T. Kadama,d,*, Isobel Robertsb, Simon Whitec, Ruth Bednallb, Kamlesh Khuntid, Peter M. Nilssone, Claire A. Lawsond aDepartment of Health Sciences, University of Leicester, Leicester LE1 7RH, UK bPharmacy Directorate, University Hospitals of North Staffordshire, Stoke-on-Trent ST4 6QG, UK cSchool of Pharmacy, Keele University, Keele ST5 5BG, UK dDiabetes Research Centre, University of Leicester, Leicester LE5 4PW, UK eDepartment of Clinical Sciences, Lund University, Malmo€ S-205 02, Sweden Accepted 24 October 2018; Published online 29 October 2018 Abstract With older and aging populations, patients experience multiple chronic diseases at the same time. Individual chronic disease guidelines often recommend pharmacological therapies as a key intervention, resulting in patients being prescribed multiple regular medications for their different diseases. Although the term ‘‘polypharmacy’’ has been applied to the use of multiple medications, there is no consistent definition, and this term is now being used all inclusively. To improve both scientific rigor and optimal patient care, it is crucial that a stan- dard terminology is used, which reclassifies the term ‘‘polypharmacy’’ into distinct phenotypes relating to the index chronic disease, addi- tional conditions to the index (comorbidity), or the experience of multiple chronic