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Real World Efficacy and Tolerability of Acotiamide, in Relieving Meal
testinal & in D o i tr g s e Journal of Gastrointestinal & a s t G i v f e o Narayanan et al., J Gastrointest Dig Syst 2018, 8:1 S l y a s n r ISSN: 2161-069Xt Digestive System DOI: 10.4172/2161-069X.1000553 e u m o J Research Article Open Access Real World Efficacy and Tolerability of Acotiamide, in Relieving Meal- related Symptoms of Functional Dyspepsia Varsha Narayanan*, Amit Bhargava and Shailesh Pallewar 1Department of Medical Services and Research, Lupin Ltd., India *Corresponding author: Narayanan V, Department of Medical Services and Research, Lupin Ltd., Mumbai, India, Tel: +912266402222; E-mail: [email protected] Received date: February 09, 2018; Accepted date: February 21, 2018; Published date: February 27, 2018 Copyright: © 2018 Narayanan V, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Abstract Background: Functional Dyspepsia (FD) is a highly prevalent clinical condition that imposes negative economic burden on health-care system as well as greatly impairs quality of life. Treatment of non-specific and bothersome meal-related FD symptoms like post-prandial fullness, upper abdominal bloating and early satiety, is a therapeutic challenge for the clinicians as poorly-defined and ill-understood pathogenesis has hampered efforts to develop effective treatments. Acotiamide is first-in-class drug that exerts its gastro-kinetic effect by enhancing acetylcholine release. Though evidence of its efficacy and tolerance are available through randomized clinical trials, real world data from its regular in-clinic use is lacking. -
UC San Francisco Electronic Theses and Dissertations
UCSF UC San Francisco Electronic Theses and Dissertations Title Machine Learning for Medical Image Analysis and Compound-Target Interactions Permalink https://escholarship.org/uc/item/8c54b5m7 Author Gaskins, Garrett Publication Date 2020 Peer reviewed|Thesis/dissertation eScholarship.org Powered by the California Digital Library University of California Machine Learning for Medical Image Analysis and Compound-Target Interactions by Garrett Gaskins DISSERTATION Submitted in partial satisfaction of the requirements for degree of DOCTOR OF PHILOSOPHY in Biological and Medical Informatics in the GRADUATE DIVISION of the UNIVERSITY OF CALIFORNIA, SAN FRANCISCO Approved: ______________________________________________________________________________Michael J Keiser Chair ______________________________________________________________________________Jason Gestwicki ______________________________________________________________________________Sourav Bandyopadhyay ______________________________________________________________________________ ______________________________________________________________________________ Committee Members Copyright 2020 by Garrett Gaskins ii ACKNOWLEDGEMENTS The graduate process is quite an experience. There is a subtle difficulty in describing it, as a peculiar quality of its existence is defined by the uniqueness of it all. Everyone I’ve known to be a part of or to have gone through graduate school has described a truly different journey. Perhaps this is integral to what makes the whole thing work. At the least, -
PN0496-Acotiamide.Pdf
Acotiamide hydrochloride hydrate (Acofide®) 盐酸阿考替胺 Z-338 in Zeria; YM-443 in Astellas Tablet, oral, EQ 100 mg acotiamide Acotiamide is a peripheral acetylcholinesterase inhibitor, indicated for the treatment of functional dyspepsia (FD), which was first-in-class drug to treat FD in the world and approved in 2013 by Japan PMDA. It was originally discovered by Zeria, and co-developed with Astellas. The drug is co-marketing in Japan with a single brand name. The human recommended starting dose is 100 mg at a time, and 3 times a day before meals. Worldwide Key Approvals Global Sales ($Million) Key Substance Patent Expiration 2016-May (US5981557A) 2016-May (EP0870765B1) 2013-Mar (JP) Not available 2021-May (JP3181919B2) 2016-May (CN1063442C) Mechanism of Action Acotiamide hydrochloride hydrate is an acetylcholinesterase (AChE) inhibitor and enhanced the acetylcholine (ACh)-induced contraction and motility of the gastric antrum and the gastric body. Target Binding Selectivity In vitro Efficacy In vivo Efficacy Mixed pattern: Ki1= 0.61 µM Effect dose of contraction in gastric sample: Significantly improved the gastrointestinal motility: Ki2= 2.7 µM ACh-induced: at 1 µM In normal and gastric hypomotility dogs: at 10 mg/kg. Inhibition: IC50= 3 µM Electrical-induced: at 0.3 µM In gastric hypomotility rats: at 100 mg/kg. Pharmacokinetics Parameters Rats Dogs Healthy Humans 3 10 3 10 50 mg 100 mg 200 mg 400 mg 800 mg Dose (mg/kg) (i.v.) (p.o.) (i.v.) (p.o.) (p.o.) (p.o.) (p.o.) (p.o.) (p.o.) Tmax (hr) - 0.08 - 0.5 2.75 2.42 2.08 2.25 2.13 Cmax -
(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. -
Nitrate Prodrugs Able to Release Nitric Oxide in a Controlled and Selective
Europäisches Patentamt *EP001336602A1* (19) European Patent Office Office européen des brevets (11) EP 1 336 602 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.7: C07C 205/00, A61K 31/00 20.08.2003 Bulletin 2003/34 (21) Application number: 02425075.5 (22) Date of filing: 13.02.2002 (84) Designated Contracting States: (71) Applicant: Scaramuzzino, Giovanni AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU 20052 Monza (Milano) (IT) MC NL PT SE TR Designated Extension States: (72) Inventor: Scaramuzzino, Giovanni AL LT LV MK RO SI 20052 Monza (Milano) (IT) (54) Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases (57) New pharmaceutical compounds of general effects and for this reason they are useful for the prep- formula (I): F-(X)q where q is an integer from 1 to 5, pref- aration of medicines for prevention and treatment of in- erably 1; -F is chosen among drugs described in the text, flammatory, ischemic, degenerative and proliferative -X is chosen among 4 groups -M, -T, -V and -Y as de- diseases of musculoskeletal, tegumental, respiratory, scribed in the text. gastrointestinal, genito-urinary and central nervous sys- The compounds of general formula (I) are nitrate tems. prodrugs which can release nitric oxide in vivo in a con- trolled and selective way and without hypotensive side EP 1 336 602 A1 Printed by Jouve, 75001 PARIS (FR) EP 1 336 602 A1 Description [0001] The present invention relates to new nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without the side effects typical of nitrate vasodilators drugs. -
IIIHIIIUSOO5304377A Unitedo States Patent 19 (11) Patent Number: 5,304,377 Yamada Et Al
IIIHIIIUSOO5304377A UnitedO States Patent 19 (11) Patent Number: 5,304,377 Yamada et al. (45) Date of Patent: Apr. 19, 1994 54 PROLONGED RELEASE PREPARATION 4,954,298 9/1990 Yamamoto et al. ................. 264/4.6 AND POLYMERS THEREOF 4,962,091 10/1990 Eppstein et al. ........................ 514/2 75) Inventors: Minoru Yamada; Seiko Ishiguro, both 5,061,492 10/1991 Okada et al. ........................ 424/423 Otokuni, all of Japan 0052510 11/1981 European Pat. Off. 73) Assignee: Sherical4. industries, Ltd., O256726O190833 7/19871/1986 European Pat. Off. a, Japan 0263490 10/1987 European Pat. Off. (21) Appl. No.: 986,299 0281482 3/1988 European Pat. Off. 035.0246 7/1989 European Pat. Off. 22 Filed: Dec. 7, 1992 2-212436 8/1990 Japan. Related U.S. Application Data OTHER PUBLICATIONS 63) continuation of ser. No. 777,170, oct. 16, 1991, aban- Chemical Abstracts, vol. 114/No. 6 (Feb. 11, 1991); doned. Columbus, Ohio; Abstract No. 49615R. 30 Foreign Application Priority Data Primary Ent, S. Sir Mueller & Oct. 16, 1990 (JP) Japan .................................. 2-278037 story Agent, or Firm-Wegner, Cantor, Mueller Aug. 28, 1991 JP Japan .................................. 3.217045 51 Int, Cl. ......................... A61K 9/22; A61K 9/52; ' ABSTRACT A61K 31/74 A polymer for a prolonged release preparation which 52 U.S. Cl. ................................. 424/426; 424/78.08; comprises 424/78.37; 424/434; 424/457; 424/468; (A) a polylactic acid and 424/486; 424/497; 525/450, 514/2 (B) a copolymer of glycolic acid and a hydroxycar 58) Field of Search .................. 424/426, 78.08, 78.37, boxylic acid of general formula 424/434, 457, 468, 486, 497; 525/450; 514/2 (56) References Cited R U.S. -
1-(4-Amino-Cyclohexyl)
(19) & (11) EP 1 598 339 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07D 211/04 (2006.01) C07D 211/06 (2006.01) 24.06.2009 Bulletin 2009/26 C07D 235/24 (2006.01) C07D 413/04 (2006.01) C07D 235/26 (2006.01) C07D 401/04 (2006.01) (2006.01) (2006.01) (21) Application number: 05014116.7 C07D 401/06 C07D 403/04 C07D 403/06 (2006.01) A61K 31/44 (2006.01) A61K 31/48 (2006.01) A61K 31/415 (2006.01) (22) Date of filing: 18.04.2002 A61K 31/445 (2006.01) A61P 25/04 (2006.01) (54) 1-(4-AMINO-CYCLOHEXYL)-1,3-DIHYDRO-2H-BENZIMIDAZOLE-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS NOCICEPTIN ANALOGS AND ORL1 LIGANDS FOR THE TREATMENT OF PAIN 1-(4-AMINO-CYCLOHEXYL)-1,3-DIHYDRO-2H-BENZIMIDAZOLE-2-ON DERIVATE UND VERWANDTE VERBINDUNGEN ALS NOCICEPTIN ANALOGE UND ORL1 LIGANDEN ZUR BEHANDLUNG VON SCHMERZ DERIVÉS DE LA 1-(4-AMINO-CYCLOHEXYL)-1,3-DIHYDRO-2H-BENZIMIDAZOLE-2-ONE ET COMPOSÉS SIMILAIRES POUR L’UTILISATION COMME ANALOGUES DU NOCICEPTIN ET LIGANDES DU ORL1 POUR LE TRAITEMENT DE LA DOULEUR (84) Designated Contracting States: • Victory, Sam AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU Oak Ridge, NC 27310 (US) MC NL PT SE TR • Whitehead, John Designated Extension States: Newtown, PA 18940 (US) AL LT LV MK RO SI (74) Representative: Maiwald, Walter (30) Priority: 18.04.2001 US 284666 P Maiwald Patentanwalts GmbH 18.04.2001 US 284667 P Elisenhof 18.04.2001 US 284668 P Elisenstrasse 3 18.04.2001 US 284669 P 80335 München (DE) (43) Date of publication of application: (56) References cited: 23.11.2005 Bulletin 2005/47 EP-A- 0 636 614 EP-A- 0 990 653 EP-A- 1 142 587 WO-A-00/06545 (62) Document number(s) of the earlier application(s) in WO-A-00/08013 WO-A-01/05770 accordance with Art. -
(19) United States (12) Patent Application Publication (10) Pub
US 20130289061A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0289061 A1 Bhide et al. (43) Pub. Date: Oct. 31, 2013 (54) METHODS AND COMPOSITIONS TO Publication Classi?cation PREVENT ADDICTION (51) Int. Cl. (71) Applicant: The General Hospital Corporation, A61K 31/485 (2006-01) Boston’ MA (Us) A61K 31/4458 (2006.01) (52) U.S. Cl. (72) Inventors: Pradeep G. Bhide; Peabody, MA (US); CPC """"" " A61K31/485 (201301); ‘4161223011? Jmm‘“ Zhu’ Ansm’ MA. (Us); USPC ......... .. 514/282; 514/317; 514/654; 514/618; Thomas J. Spencer; Carhsle; MA (US); 514/279 Joseph Biederman; Brookline; MA (Us) (57) ABSTRACT Disclosed herein is a method of reducing or preventing the development of aversion to a CNS stimulant in a subject (21) App1_ NO_; 13/924,815 comprising; administering a therapeutic amount of the neu rological stimulant and administering an antagonist of the kappa opioid receptor; to thereby reduce or prevent the devel - . opment of aversion to the CNS stimulant in the subject. Also (22) Flled' Jun‘ 24’ 2013 disclosed is a method of reducing or preventing the develop ment of addiction to a CNS stimulant in a subj ect; comprising; _ _ administering the CNS stimulant and administering a mu Related U‘s‘ Apphcatlon Data opioid receptor antagonist to thereby reduce or prevent the (63) Continuation of application NO 13/389,959, ?led on development of addiction to the CNS stimulant in the subject. Apt 27’ 2012’ ?led as application NO_ PCT/US2010/ Also disclosed are pharmaceutical compositions comprising 045486 on Aug' 13 2010' a central nervous system stimulant and an opioid receptor ’ antagonist. -
)&F1y3x PHARMACEUTICAL APPENDIX to THE
)&f1y3X PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE )&f1y3X PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 3 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. Product CAS No. Product CAS No. ABAMECTIN 65195-55-3 ACTODIGIN 36983-69-4 ABANOQUIL 90402-40-7 ADAFENOXATE 82168-26-1 ABCIXIMAB 143653-53-6 ADAMEXINE 54785-02-3 ABECARNIL 111841-85-1 ADAPALENE 106685-40-9 ABITESARTAN 137882-98-5 ADAPROLOL 101479-70-3 ABLUKAST 96566-25-5 ADATANSERIN 127266-56-2 ABUNIDAZOLE 91017-58-2 ADEFOVIR 106941-25-7 ACADESINE 2627-69-2 ADELMIDROL 1675-66-7 ACAMPROSATE 77337-76-9 ADEMETIONINE 17176-17-9 ACAPRAZINE 55485-20-6 ADENOSINE PHOSPHATE 61-19-8 ACARBOSE 56180-94-0 ADIBENDAN 100510-33-6 ACEBROCHOL 514-50-1 ADICILLIN 525-94-0 ACEBURIC ACID 26976-72-7 ADIMOLOL 78459-19-5 ACEBUTOLOL 37517-30-9 ADINAZOLAM 37115-32-5 ACECAINIDE 32795-44-1 ADIPHENINE 64-95-9 ACECARBROMAL 77-66-7 ADIPIODONE 606-17-7 ACECLIDINE 827-61-2 ADITEREN 56066-19-4 ACECLOFENAC 89796-99-6 ADITOPRIM 56066-63-8 ACEDAPSONE 77-46-3 ADOSOPINE 88124-26-9 ACEDIASULFONE SODIUM 127-60-6 ADOZELESIN 110314-48-2 ACEDOBEN 556-08-1 ADRAFINIL 63547-13-7 ACEFLURANOL 80595-73-9 ADRENALONE -
Pharmacological Agents Currently in Clinical Trials for Disorders in Neurogastroenterology
Pharmacological agents currently in clinical trials for disorders in neurogastroenterology Michael Camilleri J Clin Invest. 2013;123(10):4111-4120. https://doi.org/10.1172/JCI70837. Clinical Review Esophageal, gastrointestinal, and colonic diseases resulting from disorders of the motor and sensory functions represent almost half the patients presenting to gastroenterologists. There have been significant advances in understanding the mechanisms of these disorders, through basic and translational research, and in targeting the receptors or mediators involved, through clinical trials involving biomarkers and patient responses. These advances have led to relief of patients’ symptoms and improved quality of life, although there are still significant unmet needs. This article reviews the pipeline of medications in development for esophageal sensorimotor disorders, gastroparesis, chronic diarrhea, chronic constipation (including opioid-induced constipation), and visceral pain. Find the latest version: https://jci.me/70837/pdf Review Pharmacological agents currently in clinical trials for disorders in neurogastroenterology Michael Camilleri Clinical Enteric Neuroscience Translational and Epidemiological Research (CENTER), Mayo Clinic, Rochester, Minnesota, USA. Esophageal, gastrointestinal, and colonic diseases resulting from disorders of the motor and sensory functions represent almost half the patients presenting to gastroenterologists. There have been significant advances in under- standing the mechanisms of these disorders, through basic and translational research, and in targeting the recep- tors or mediators involved, through clinical trials involving biomarkers and patient responses. These advances have led to relief of patients’ symptoms and improved quality of life, although there are still significant unmet needs. This article reviews the pipeline of medications in development for esophageal sensorimotor disorders, gastropa- resis, chronic diarrhea, chronic constipation (including opioid-induced constipation), and visceral pain. -
Amfepramone (Diethylpropion) Elisa Kit Instructions Product #182119, 182116 & 182113 Forensic Use Only
Neogen Corporation 944 Nandino Blvd., Lexington KY 40511 USA 800/477-8201 USA/Canada | 859/254-1221 Fax: 859/255-5532 | E-mail: [email protected] | Web: www.neogen.com/Toxicology AMFEPRAMONE (DIETHYLPROPION) ELISA KIT INSTRUCTIONS PRODUCT #182119, 182116 & 182113 FORENSIC USE ONLY INTENDED USE: For the determination of trace quantities of Amfepramone (Diethylpropion) and/or other metabolites in human samples. DESCRIPTION Neogen Corporation’s Amfepramone (Diethylpropion) ELISA (Enzyme-Linked Immunosorbent Assay) test kit is a qualitative one-step kit designed for use as a screening device for the detection of drugs and/or their metabolites. The kit was designed for screening purposes and is intended for forensic use only. It is recommended that all suspect samples be confirmed by a quantitative method such as gas chromatography/mass spectrometry (GC/MS). ASSAY PRINCIPLE The Neogen forensic drug detection ELISA is a solid phase immunoassay designed to detect drugs of abuse for forensic application. The test is performed in microwells coated with a high affinity capture antibody. A control or sample is added to the wells followed by an enzyme conjugate. During the following incubation period, the enzyme conjugate competes with the drug in the sample for binding sites on the antibody coated well. After a wash step to remove any unbound material, substrate is added for the color development process. Acid stop solution is added to discontinue the enzyme-substrate reaction. The color intensity is inversely proportional to the amount of drug present in the sample. Therefore, those samples which contain the drug will inhibit binding of the enzyme conjugate to the capture antibody resulting in less color than the negative control. -
1 Liste Des 3000 Ingrédients Controversés Évités Par
LISTE DES 3000 INGRÉDIENTS CONTROVERSÉS ÉVITÉS PAR MODERE 1 SOINS PERSONNELS Conformément au paradigme des ingrédients de MODERE, la compagnie exclu une liste de plus de 3000 ingrédients controversés différents à éviter dans les formulations de ses produits. Chaque année, les chercheurs publient de nouvelles informations sur les ingrédients des produits. Modere convoque régulièrement son Scientific Advisory Board (Conseil Consultatif Scientifique) afin de : - réexaminer la science qui se cache derrière certains ingrédients et - donner des recommandations sur l'utilisation que Modere fait de ces ingrédients. Cependant, quand de nouveaux ingrédients sont ajoutés à sa liste, il est possible que certains éléments faisant partie de la large gamme de produits MODERE contiennent ces nouveaux ingrédients controversés. Ainsi, Modere doit entamer le processus de reformulation qui prend un certain temps à développer et à implémenter. Malheureusement, en raison de ces processus continus de découvertes, d'évaluations et de reformulations, MODERE ne sera respectera peut être pas toujours sa liste d'ingrédients controversés à 100%. Nous sommes cependant fiers de la position de leader que Modere occupe dans cette industrie, et nous sommes confiants que les produits Modere garantissent de manière jusqu'à présent inégalée la sécurité de nos consommateurs. Modere évite les formulations dans ses soins personnels avec des ingrédients tels que : (2-Isopropylpent.4-Enoyl) 2,2,6-Trimethyl-4-piperidyl 2-Methyl-m- urée (apronalide) benzoate (benzamine) phenylenediamine