NCBI Name Molecular Formula Monoisotopic Mass Of
Total Page：16
File Type：pdf, Size：1020Kb
Load more
Recommended publications
-
(12) United States Patent (10) Patent No.: US 9,498,481 B2 Rao Et Al
USOO9498481 B2 (12) United States Patent (10) Patent No.: US 9,498,481 B2 Rao et al. (45) Date of Patent: *Nov. 22, 2016 (54) CYCLOPROPYL MODULATORS OF P2Y12 WO WO95/26325 10, 1995 RECEPTOR WO WO99/O5142 2, 1999 WO WOOO/34283 6, 2000 WO WO O1/92262 12/2001 (71) Applicant: Apharaceuticals. Inc., La WO WO O1/922.63 12/2001 olla, CA (US) WO WO 2011/O17108 2, 2011 (72) Inventors: Tadimeti Rao, San Diego, CA (US); Chengzhi Zhang, San Diego, CA (US) OTHER PUBLICATIONS Drugs of the Future 32(10), 845-853 (2007).* (73) Assignee: Auspex Pharmaceuticals, Inc., LaJolla, Tantry et al. in Expert Opin. Invest. Drugs (2007) 16(2):225-229.* CA (US) Wallentin et al. in the New England Journal of Medicine, 361 (11), 1045-1057 (2009).* (*) Notice: Subject to any disclaimer, the term of this Husted et al. in The European Heart Journal 27, 1038-1047 (2006).* patent is extended or adjusted under 35 Auspex in www.businesswire.com/news/home/20081023005201/ U.S.C. 154(b) by Od en/Auspex-Pharmaceuticals-Announces-Positive-Results-Clinical M YW- (b) by ayS. Study (published: Oct. 23, 2008).* This patent is Subject to a terminal dis- Concert In www.concertpharma. com/news/ claimer ConcertPresentsPreclinicalResultsNAMS.htm (published: Sep. 25. 2008).* Concert2 in Expert Rev. Anti Infect. Ther. 6(6), 782 (2008).* (21) Appl. No.: 14/977,056 Springthorpe et al. in Bioorganic & Medicinal Chemistry Letters 17. 6013-6018 (2007).* (22) Filed: Dec. 21, 2015 Leis et al. in Current Organic Chemistry 2, 131-144 (1998).* Angiolillo et al., Pharmacology of emerging novel platelet inhibi (65) Prior Publication Data tors, American Heart Journal, 2008, 156(2) Supp. -
Zebrafish Behavioral Profiling Links Drugs to Biological Targets and Rest/Wake Regulation
www.sciencemag.org/cgi/content/full/327/5963/348/DC1 Supporting Online Material for Zebrafish Behavioral Profiling Links Drugs to Biological Targets and Rest/Wake Regulation Jason Rihel,* David A. Prober, Anthony Arvanites, Kelvin Lam, Steven Zimmerman, Sumin Jang, Stephen J. Haggarty, David Kokel, Lee L. Rubin, Randall T. Peterson, Alexander F. Schier* *To whom correspondence should be addressed. E-mail: [email protected] (A.F.S.); [email protected] (J.R.) Published 15 January 2010, Science 327, 348 (2010) DOI: 10.1126/science.1183090 This PDF file includes: Materials and Methods SOM Text Figs. S1 to S18 Table S1 References Supporting Online Material Table of Contents Materials and Methods, pages 2-4 Supplemental Text 1-7, pages 5-10 Text 1. Psychotropic Drug Discovery, page 5 Text 2. Dose, pages 5-6 Text 3. Therapeutic Classes of Drugs Induce Correlated Behaviors, page 6 Text 4. Polypharmacology, pages 6-7 Text 5. Pharmacological Conservation, pages 7-9 Text 6. Non-overlapping Regulation of Rest/Wake States, page 9 Text 7. High Throughput Behavioral Screening in Practice, page 10 Supplemental Figure Legends, pages 11-14 Figure S1. Expanded hierarchical clustering analysis, pages 15-18 Figure S2. Hierarchical and k-means clustering yield similar cluster architectures, page 19 Figure S3. Expanded k-means clustergram, pages 20-23 Figure S4. Behavioral fingerprints are stable across a range of doses, page 24 Figure S5. Compounds that share biological targets have highly correlated behavioral fingerprints, page 25 Figure S6. Examples of compounds that share biological targets and/or structural similarity that give similar behavioral profiles, page 26 Figure S7. -
Food and Drug Administration, HHS § 310.201
Food and Drug Administration, HHS § 310.201 (d) Prescription legend not allowed on (v) The preparation is labeled with exempted drugs. The use of the prescrip- adequate directions for use in minor tion caution statement quoted in sec- conditions as a simple analgesic. tion 503(b) (4) of the act, in the labeling (vi) The dosages of N-acetyl-p-amino- of a drug exempted under the provi- phenol recommended or suggested in sions of this section, constitutes mis- the labeling do not exceed: For adults, branding. Any other statement or sug- 0.65 gram (10 grains) per dose or 2.6 gestion in the labeling of a drug ex- grams (40 grains) per 24-hour period: for empted under this section, that such children 6 to 12 years of age, one-half of drug is limited to prescription use, the maximum adult dose or dosage; for may constitute misbranding. children 3 to 6 years of age, one-fifth of (e) Prescription-exemption procedure of the maximum adult dose or dosage. OTC drug review. A drug limited to pre- (vii) The labeling bears, in juxtaposi- scription use under section 503(b)(1)(B) tion with the dosage recommendations, of the act may also be exempted from a clear warning statement against ad- prescription-dispensing requirements ministration of the drug to children by the procedure set forth in § 330.13 of under 3 years of age and against use of this chapter. the drug for more than 10 days, unless such uses are directed by a physician. [39 FR 11680, Mar. -
Author Index Page Numbers in Italics Refer to Bibliography
Author Index Page Numbers in italics refer to bibliography Aaron,T.H., Criep,L.H. 180. Adams,M.R., see Litchfield,J. Albert,A., Serjeant,E.P. 176, 207 T., Jr. 386, 409, 432, 441, 207 Aaron, T. H., see Criep, L. H. 465,496 Albert,J.R., see Lish,P.M. 398,427 Adamson,D.W., Barrett,P.A., 449, 465, 466, 495 Aarsen,P.N., Zeegers,A. 15, Billinghurst, J. W., Green, A. Albert, U., see Giertz, H. 444, 30 F .. Jones,T.S.G. 190,192, 489 Abbozzo, G., Genazzani, E., 207 Alberty,J. 387,425, 442, Donatelli, L. 562,570 Adamson, D. W., Barrett, P. A., 452--455,480 Abdel-Galil, A. A. M., Marshall, Billinghurst,J. W., Jones, T. Alberty, J., Huurrekorpi, L. P. B. 114, 122 S.G. 190,207 399, 425, 455, 480 Aborg, e.-H .. Novotny,J., Adamson, D. W., Billinghurst, Alberty,J., Schiede,M. 399, Uvniis,B. 86.90 J.W. 189,194,207 425,455,480 Aborg,e. H., Uvniis,B. 87, 90 Adashek, D., Grossman, M. I. Alberty, J., Takkunen, R. 467, Aborg, C.-H., see Uvniis,B. 58. 46,47,55 480 74. 75, 82, 84-87. 92 Adlerova, E., see Protiva, M. Albinus,M., Sewing.K.F. 2, Abram, L. E., see Cohen, M. B. 201, 212 3, 6, 8, 11, 21, 30, 264, 287, 421,427 Ado,A.D., Abrossimow,W.N. 463,480 Abrams,G., see Lear,E. 566, 453.480 Albrecht, I., see Cort, J. H. 579, 571 Ado, A. D., Ishimova, L. M., 597 Abramson, D. -
Quasi-Experimental Health Policy Research: Evaluation of Universal Health Insurance and Methods for Comparative Effectiveness Research
Quasi-Experimental Health Policy Research: Evaluation of Universal Health Insurance and Methods for Comparative Effectiveness Research The Harvard community has made this article openly available. Please share how this access benefits you. Your story matters Citation Garabedian, Laura Faden. 2013. Quasi-Experimental Health Policy Research: Evaluation of Universal Health Insurance and Methods for Comparative Effectiveness Research. Doctoral dissertation, Harvard University. Citable link http://nrs.harvard.edu/urn-3:HUL.InstRepos:11156786 Terms of Use This article was downloaded from Harvard University’s DASH repository, and is made available under the terms and conditions applicable to Other Posted Material, as set forth at http:// nrs.harvard.edu/urn-3:HUL.InstRepos:dash.current.terms-of- use#LAA Quasi-Experimental Health Policy Research: Evaluation of Universal Health Insurance and Methods for Comparative Effectiveness Research A dissertation presented by Laura Faden Garabedian to The Committee on Higher Degrees in Health Policy in partial fulfillment of the requirements for the degree of Doctor of Philosophy in the subject of Health Policy Harvard University Cambridge, Massachusetts March 2013 © 2013 – Laura Faden Garabedian All rights reserved. Professor Stephen Soumerai Laura Faden Garabedian Quasi-Experimental Health Policy Research: Evaluation of Universal Health Insurance and Methods for Comparative Effectiveness Research Abstract This dissertation consists of two empirical papers and one methods paper. The first two papers use quasi-experimental methods to evaluate the impact of universal health insurance reform in Massachusetts (MA) and Thailand and the third paper evaluates the validity of a quasi- experimental method used in comparative effectiveness research (CER). My first paper uses interrupted time series with data from IMS Health to evaluate the impact of Thailand’s universal health insurance and physician payment reform on utilization of medicines for three non-communicable diseases: cancer, cardiovascular disease and diabetes. -
(12) Patent Application Publication (10) Pub. No.: US 2010/0081713 A1 Sharma Et Al
US 20100081713A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0081713 A1 Sharma et al. (43) Pub. Date: Apr. 1, 2010 (54) COMPOSITIONS AND METHODS FOR (22) Filed: Mar. 18, 2009 TREATINGVIRAL INFECTIONS Related U.S. Application Data (75) Inventors: Geeta Sharma, Singapore (SG); (60) Provisional application No. 61/069,917, filed on Mar. Ralf Altmeyer, Singapore (SG); 19, 2008. Vishal Pendharker, Singapore (SG); Yu Chen, Singapore (SG); Publication Classification Michael Foley, Chestnut Hill, MA (51) Int. Cl. (US) A63L/35 (2006.01) A6II 3L/25 (2006.01) Correspondence Address: A63L/35 (2006.01) Gearhart Law LLC A6II 3/13 (2006.01) 4 Femdale Avenue A6IP3L/2 (2006.01) Chatham, NJ 07928 (US) (52) U.S. Cl. .......... 514/459; 514/529; 514/647: 514/662 (73) Assignee: CombinatoRx, (Singapore) Pte. (57) ABSTRACT Ltd. The present invention provides compositions, methods, and kits for treating or preventing a viral infection (e.g., an infec (21) Appl. No.: 12/406,716 tion caused by an influenza virus). Patent Application Publication Apr. 1, 2010 Sheet 1 of 2 US 2010/0081713 A1 ------ 80 r -0. Vehicle 0.5% HPMC g - - Sertraline-30mg/kg/day - £ 60 “A Sertraline-100mg/kg/day/kg/day i -v. Oseltamivir-30mg/kg/day ...i -0. Oseltamivir-100mg/kg/day -0. (Sertraline 30mg/kg+ . 40 Prednisolone 0.1 mg/Kg) Figure 1 Patent Application Publication Apr. 1, 2010 Sheet 2 of 2 US 2010/0081713 A1 100 468OOO 2 O Wehicle Sentraline 10 mg/kg Sentraline 30mg/kg Setraline 100mg/kg Figure 2 US 2010/008 1713 A1 Apr. -
| Hao Ha Ta Maria Tai Mai Multe Detalian Mature
|HAO HA TA MARIAUS009730892B2 TAI MAI MULTE DETALIAN MATURE (12 ) United States Patent ( 10 ) Patent No. : US 9 , 730 ,892 B2 Schutt et al. ( 45 ) Date of Patent : Aug . 15 , 2017 (54 ) METHOD FOR FORMULATING LARGE ( 56 ) References Cited DIAMETER SYNTHETIC MEMBRANE VESICLES U . S . PATENT DOCUMENTS 2 ,044 , 296 A 6 /1936 Hardgrove ( 71 ) Applicant : Pacira Pharmaceuticals , Inc ., San 2 ,824 ,807 A 2 / 1958 Laster et al . Diego , CA (US ) ( Continued ) (72 ) Inventors : Ernest George Schutt , San Diego , CA (US ) ; Ronald Warren McGuire , FOREIGN PATENT DOCUMENTS Murrieta , CA (US ) ; Peter Andrew AU 2002301268 B2 2 /2003 Walters, San Diego , CA (US ) ; AU 2006200044 Al 2 / 2006 Kathleen D . A . Los, San Diego , CA CA 933796 9 / 1973 ?? 960811 1 / 1975 (US ) CA 2 564 120 A1 8 / 1998 CA 2464668 5 / 2003 (73 ) Assignee : Pacira Pharmaceuticals , Inc ., San CH 519936 7 / 1971 Diego , CA (US ) CH 587023 7 / 1974 CN 101396345 5 / 2009 DE 1199191 8 / 1965 ( * ) Notice : Subject to any disclaimer, the term of this DE 51254 10 / 1966 patent is extended or adjusted under 35 DE 56223 5 / 1967 U . S . C . 154 ( b ) by 0 days . ( Continued ) ( 21 ) Appl . No . : 15 / 249 , 195 OTHER PUBLICATIONS Aug . 26 , 2016 (22 ) Filed : Atiemo -Obeng et al. “ Rotor - Stator Mixing Devices ” , Handbook of (65 ) Prior Publication Data Industrial Mixing Science and Practice , 2004 , 479 - 505 , Eds. Paul , US 2016 /0361260 A1 Dec . 15 , 2016 et al. , Hoboken , NJ: John Wiley and Sons , Inc. Related U . S . Application Data (Continued ) (63 ) Continuation of application No. 13 / 786 ,378 , filed on Primary Examiner — Monzer R Chorbaji Mar . -
The Organic Chemistry of Drug Synthesis
THE ORGANIC CHEMISTRY OF DRUG SYNTHESIS VOLUME 3 DANIEL LEDNICER Analytical Bio-Chemistry Laboratories, Inc. Columbia, Missouri LESTER A. MITSCHER The University of Kansas School of Pharmacy Department of Medicinal Chemistry Lawrence, Kansas A WILEY-INTERSCIENCE PUBLICATION JOHN WILEY AND SONS New York • Chlchester • Brisbane * Toronto • Singapore Copyright © 1984 by John Wiley & Sons, Inc. All rights reserved. Published simultaneously in Canada. Reproduction or translation of any part of this work beyond that permitted by Section 107 or 108 of the 1976 United States Copyright Act without the permission of the copyright owner is unlawful. Requests for permission or further information should be addressed to the Permissions Department, John Wiley & Sons, Inc. Library of Congress Cataloging In Publication Data: (Revised for volume 3) Lednicer, Daniel, 1929- The organic chemistry of drug synthesis. "A Wiley-lnterscience publication." Includes bibliographical references and index. 1. Chemistry, Pharmaceutical. 2. Drugs. 3. Chemistry, Organic—Synthesis. I. Mitscher, Lester A., joint author. II. Title. [DNLM 1. Chemistry, Organic. 2. Chemistry, Pharmaceutical. 3. Drugs—Chemical synthesis. QV 744 L473o 1977] RS403.L38 615M9 76-28387 ISBN 0-471-09250-9 (v. 3) Printed in the United States of America 10 907654321 With great pleasure we dedicate this book, too, to our wives, Beryle and Betty. The great tragedy of Science is the slaying of a beautiful hypothesis by an ugly fact. Thomas H. Huxley, "Biogenesis and Abiogenisis" Preface Ihe first volume in this series represented the launching of a trial balloon on the part of the authors. In the first place, wo were not entirely convinced that contemporary medicinal (hemistry could in fact be organized coherently on the basis of organic chemistry. -
(12) United States Patent (10) Patent No.: US 9,393,221 B2 W (45) Date of Patent: Jul.19, 2016
USOO9393221B2 (12) United States Patent (10) Patent No.: US 9,393,221 B2 W (45) Date of Patent: Jul.19, 2016 (54) METHODS AND COMPOUNDS FOR FOREIGN PATENT DOCUMENTS REDUCING INTRACELLULAR LIPID STORAGE WO WO2007096,251 8, 2007 OTHER PUBLICATIONS (75) Inventor: Sean Wu, Brookline, MA (US) Onyesom and Agho, Asian J. Sci. Res., Oct. 2010, vol. 4, No. 1, p. (73) Assignee: THE GENERAL, HOSPITAL 78-83. CORPORATION, Boston, MA (US) Davis et al., Br J Clin Pharmacol., 1996, vol. 4, p. 415-421.* Schweiger et al., Am J Physiol Endocrinol Metab, 2009, vol. 279, E289-E296. (*) Notice: Subject to any disclaimer, the term of this Maryam Ahmadian et al., Desnutrin/ATGL is regulated by AMPK patent is extended or adjusted under 35 and is required for a brown adipose phenotype, Cell Metabolism, vol. U.S.C. 154(b) by 748 days. 13, pp. 739-748, 2011. Mohammadreza Bozorgmanesh et al., Diabetes prediction, lipid (21) Appl. No.: 13/552,975 accumulation product, and adiposity measures; 6-year follow-up: Tehran lipid and glucose study, Lipids in Health and Disease, vol. 9, (22) Filed: Jul.19, 2012 pp. 1-9, 2010. Judith Fischer et al., The gene encoding adipose triglyceride lipase (65) Prior Publication Data (PNPLA2) is mutated in neutral lipid storage disease with myopathy, Nature Genetics, vol.39, pp. 28-30, 2007. US 2013/OO23488A1 Jan. 24, 2013 Astrid Gruber et al., The N-terminal region of comparative gene identification-58 (CGI-58) is important for lipid droplet binding and activation of adipose triglyceride lipase, vol. 285, pp. 12289-12298, Related U.S. -
Modes of Action of Herbal Medicines and Plant Secondary Metabolites
Medicines 2015, 2, 251-286; doi:10.3390/medicines2030251 OPEN ACCESS medicines ISSN 2305-6320 www.mdpi.com/journal/medicines Review Modes of Action of Herbal Medicines and Plant Secondary Metabolites Michael Wink Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, INF 364, Heidelberg D-69120, Germany; E-Mail: [email protected]; Tel.: +49-6221-544-881; Fax: +49-6221-544-884 Academic Editor: Shufeng Zhou Received: 13 August 2015 / Accepted: 31 August 2015 / Published: 8 September 2015 Abstract: Plants produce a wide diversity of secondary metabolites (SM) which serve them as defense compounds against herbivores, and other plants and microbes, but also as signal compounds. In general, SM exhibit a wide array of biological and pharmacological properties. Because of this, some plants or products isolated from them have been and are still used to treat infections, health disorders or diseases. This review provides evidence that many SM have a broad spectrum of bioactivities. They often interact with the main targets in cells, such as proteins, biomembranes or nucleic acids. Whereas some SM appear to have been optimized on a few molecular targets, such as alkaloids on receptors of neurotransmitters, others (such as phenolics and terpenoids) are less specific and attack a multitude of proteins by building hydrogen, hydrophobic and ionic bonds, thus modulating their 3D structures and in consequence their bioactivities. The main modes of action are described for the major groups of common plant secondary metabolites. The multitarget activities of many SM can explain the medical application of complex extracts from medicinal plants for more health disorders which involve several targets. -
Structural Investigation of Heteroyohimbine Alkaloid Synthesis Reveals Active Site Elements That Control Stereoselectivity
ARTICLE Received 30 Dec 2015 | Accepted 31 May 2016 | Published 15 Jul 2016 DOI: 10.1038/ncomms12116 OPEN Structural investigation of heteroyohimbine alkaloid synthesis reveals active site elements that control stereoselectivity Anna Stavrinides1,*, Evangelos C. Tatsis1,*, Lorenzo Caputi1, Emilien Foureau2, Clare E.M Stevenson1, David M. Lawson1, Vincent Courdavault2 & Sarah E. O’Connor1 Plants produce an enormous array of biologically active metabolites, often with stereo- chemical variations on the same molecular scaffold. These changes in stereochemistry dramatically impact biological activity. Notably, the stereoisomers of the heteroyohimbine alkaloids show diverse pharmacological activities. We reported a medium chain dehydrogenase/reductase (MDR) from Catharanthus roseus that catalyses formation of a heteroyohimbine isomer. Here we report the discovery of additional heteroyohimbine synthases (HYSs), one of which produces a mixture of diastereomers. The crystal structures for three HYSs have been solved, providing insight into the mechanism of reactivity and stereoselectivity, with mutation of one loop transforming product specificity. Localization and gene silencing experiments provide a basis for understanding the function of these enzymes in vivo. This work sets the stage to explore how MDRs evolved to generate structural and biological diversity in specialized plant metabolism and opens the possibility for metabolic engineering of new compounds based on this scaffold. 1 The John Innes Centre, Department of Biological Chemistry, Norwich NR4 7UH, UK. 2 Universite´ Franc¸ois-Rabelais de Tours, EA2106 ‘Biomole´cules et Biotechnologies Ve´ge´tales’, Tours 37200, France. * These authors contributed equally to this work. Correspondence and requests for materials should be addressed to V.C. (email: [email protected]) or to S.E.O’C. -
In-Silico Approaches
molecules Review Recent Developments in New Therapeutic Agents against Alzheimer and Parkinson Diseases: In-Silico Approaches Pedro Cruz-Vicente 1,2 , Luís A. Passarinha 1,2,3,* , Samuel Silvestre 1,3,4,* and Eugenia Gallardo 1,3,* 1 CICS-UBI, Health Sciences Research Centre, University of Beira Interior, 6201-001 Covilhã, Portugal; [email protected] 2 UCIBIO—Applied Molecular Biosciences Unit, Department of Chemistry, Faculty of Sciences and Technology, NOVA University Lisbon, 2829-516 Caparica, Portugal 3 Laboratory of Pharmaco-Toxicology—UBIMedical, University of Beira Interior, 6200-001 Covilhã, Portugal 4 CNC—Center for Neuroscience and Cell Biology, University of Coimbra, 3004-504 Coimbra, Portugal * Correspondence: [email protected] (L.A.P.); [email protected] (S.S.); [email protected] (E.G.); Tel.: +351-275-329-002/3 (L.A.P. & S.S. & E.G.) Abstract: Neurodegenerative diseases (ND), including Alzheimer’s (AD) and Parkinson’s Disease (PD), are becoming increasingly more common and are recognized as a social problem in modern societies. These disorders are characterized by a progressive neurodegeneration and are considered one of the main causes of disability and mortality worldwide. Currently, there is no existing cure for AD nor PD and the clinically used drugs aim only at symptomatic relief, and are not capable Citation: Cruz-Vicente, P.; of stopping neurodegeneration. Over the last years, several drug candidates reached clinical trials Passarinha, L.A.; Silvestre, S.; phases, but they were suspended, mainly because of the unsatisfactory pharmacological benefits. Gallardo, E. Recent Developments in Recently, the number of compounds developed using in silico approaches has been increasing at New Therapeutic Agents against a promising rate, mainly evaluating the affinity for several macromolecular targets and applying Alzheimer and Parkinson Diseases: filters to exclude compounds with potentially unfavorable pharmacokinetics.