Annexure-1 Patents Granted for Drugs (Products and Processes)
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List of New Drugs Approved in India from 1991 to 2000
LIST OF NEW DRUGS APPROVED IN INDIA FROM 1991 TO 2000 S. No Name of Drug Pharmacological action/ Date of Indication Approval 1 Ciprofloxacin 0.3% w/v Eye Indicated in the treatment of February-1991 Drops/Eye Ointment/Ear Drop external ocular infection of the eye. 2 Diclofenac Sodium 1gm Gel March-1991 3 i)Cefaclor Monohydrate Antibiotic- In respiratory April-1991 250mg/500mg Capsule. infections, ENT infection, UT ii)Cefaclor Monohydrate infections, Skin and skin 125mg/5ml & 250mg/5ml structure infections. Suspension. iii)Cefaclor Monohydrate 100mg/ml Drops. iv)Cefaclor 187mg/5ml Suspension (For paediatric use). 4 Sheep Pox Vaccine (For April-1991 Veterinary) 5 Omeprazole 10mg/20mg Short term treatment of April-1991 Enteric Coated Granules duodenal ulcer, gastric ulcer, Capsule reflux oesophagitis, management of Zollinger- Ellison syndrome. 6 i)Nefopam Hydrochloride Non narcotic analgesic- Acute April-1991 30mg Tablet. and chronic pain, including ii)Nefopam Hydrochloride post-operative pain, dental 20mg/ml Injection. pain, musculo-skeletal pain, acute traumatic pain and cancer pain. 7 Buparvaquone 5% w/v Indicated in the treatment of April-1991 Solution for Injection (For bovine theileriosis. Veterinary) 8 i)Kitotifen Fumerate 1mg Anti asthmatic drug- Indicated May-1991 Tablet in prophylactic treatment of ii)Kitotifen Fumerate Syrup bronchial asthma, symptomatic iii)Ketotifen Fumerate Nasal improvement of allergic Drops conditions including rhinitis and conjunctivitis. 9 i)Pefloxacin Mesylate Antibacterial- In the treatment May-1991 Dihydrate 400mg Film Coated of severe infection in adults Tablet caused by sensitive ii)Pefloxacin Mesylate microorganism (gram -ve Dihydrate 400mg/5ml Injection pathogens and staphylococci). iii)Pefloxacin Mesylate Dihydrate 400mg I.V Bottles of 100ml/200ml 10 Ofloxacin 100mg/50ml & Indicated in RTI, UTI, May-1991 200mg/100ml vial Infusion gynaecological infection, skin/soft lesion infection. -
Product List March 2019 - Page 1 of 53
Wessex has been sourcing and supplying active substances to medicine manufacturers since its incorporation in 1994. We supply from known, trusted partners working to full cGMP and with full regulatory support. Please contact us for details of the following products. Product CAS No. ( R)-2-Methyl-CBS-oxazaborolidine 112022-83-0 (-) (1R) Menthyl Chloroformate 14602-86-9 (+)-Sotalol Hydrochloride 959-24-0 (2R)-2-[(4-Ethyl-2, 3-dioxopiperazinyl) carbonylamino]-2-phenylacetic 63422-71-9 acid (2R)-2-[(4-Ethyl-2-3-dioxopiperazinyl) carbonylamino]-2-(4- 62893-24-7 hydroxyphenyl) acetic acid (r)-(+)-α-Lipoic Acid 1200-22-2 (S)-1-(2-Chloroacetyl) pyrrolidine-2-carbonitrile 207557-35-5 1,1'-Carbonyl diimidazole 530-62-1 1,3-Cyclohexanedione 504-02-9 1-[2-amino-1-(4-methoxyphenyl) ethyl] cyclohexanol acetate 839705-03-2 1-[2-Amino-1-(4-methoxyphenyl) ethyl] cyclohexanol Hydrochloride 130198-05-9 1-[Cyano-(4-methoxyphenyl) methyl] cyclohexanol 93413-76-4 1-Chloroethyl-4-nitrophenyl carbonate 101623-69-2 2-(2-Aminothiazol-4-yl) acetic acid Hydrochloride 66659-20-9 2-(4-Nitrophenyl)ethanamine Hydrochloride 29968-78-3 2,4 Dichlorobenzyl Alcohol (2,4 DCBA) 1777-82-8 2,6-Dichlorophenol 87-65-0 2.6 Diamino Pyridine 136-40-3 2-Aminoheptane Sulfate 6411-75-2 2-Ethylhexanoyl Chloride 760-67-8 2-Ethylhexyl Chloroformate 24468-13-1 2-Isopropyl-4-(N-methylaminomethyl) thiazole Hydrochloride 908591-25-3 4,4,4-Trifluoro-1-(4-methylphenyl)-1,3-butane dione 720-94-5 4,5,6,7-Tetrahydrothieno[3,2,c] pyridine Hydrochloride 28783-41-7 4-Chloro-N-methyl-piperidine 5570-77-4 -
United States Patent Office
Patented Feb. 11, 1947 2,415,786 UNITED STATES PATENT OFFICE UNSYMMETRICALLY SUBSTITUTED PPERAZINES Johannes S. Buck, East Greenbush, and Richard Baltzly, New York, N. Y., assignors to Bur roughs Welcome & Co. (U. S. A.) Inc., New York, N.Y., a corporation of New York No Drawing. Application January 6, 1944, serial No. 517,224 9 Claims. (C. 260-268) 2 This invention relates to N-monosubstituted According to the present invention, these diffi and N-N'-unsymmetrically disubstituted piper culties are overcome by treating piperazine with azines and has for an object to provide new com a halide of benzyl or of a substituted benzyl to positions of the above type and a novel and im form a reaction mixture containing, in addition proved method of making the same. to unreacted piperazine and di-N-N'- Substituted Another object is to provide a method of mak piperazine, a substantial amount of N-mono sub ing and isolating the above substances which is stituted piperazine separating the mono-N-sub Suitable for commercial Operation. stituted piperazine from the unreacted piperazine In our copending application Serial No. 476,914, and the disubstituted piperazine, introducing the filed February 24, 1943, of which the present ap O desired substituent on to the second N' nitrogen plication is a continuation in part and in our atom of the mono-N-substituted piperazine, then Copending application Serial No. 517,225, filed removing the benzyl or substituted benzyl group January 6, 1944, which is also a continuation in by catalytic hydrogenation. part, We have described certain methods for mak As catalysts for this hydrogenation, platinum, ing and isolating substituted piperazines of the palladium and nickel are all suitable, but We pre type fer in general to use palladium since, while CEI-CI equally or perhaps more effective in removing a benzyl group, it is practically devoid of any N /N-R tendency to reduce aromatic rings. -
Recent Progress Toward the Asymmetric Synthesis of Carbon-Substituted Piperazine Pharmacophores and Oxidative Related Heterocycles RSC Medicinal Chemistry
Volume 11 Number 7 July 2020 RSC Pages 735–850 Medicinal Chemistry rsc.li/medchem ISSN 2632-8682 REVIEW ARTICLE Plato A. Magriotis Recent progress toward the asymmetric synthesis of carbon-substituted piperazine pharmacophores and oxidative related heterocycles RSC Medicinal Chemistry View Article Online REVIEW View Journal | View Issue Recent progress toward the asymmetric synthesis Cite this: RSC Med. Chem.,2020,11, of carbon-substituted piperazine pharmacophores 745 and oxidative related heterocycles Plato A. Magriotis † The important requirement for approval of a new drug, in case it happens to be chiral, is that both enantiomers of the drug should be studied in detail, which has led synthetic organic and medicinal chemists to focus their attention on the development of new methods for asymmetric synthesis especially of relevant saturated N-heterocycles. On the other hand, the piperazine ring, besides defining a major class of saturated N-heterocycles, has been classified as a privileged structure in medicinal chemistry, since it is more than frequently found in biologically active compounds including several marketed blockbuster drugs such as Glivec (imatinib) and Viagra (sildenafil). Indeed, 13 of the 200 best-selling small molecule drugs in 2012 contained a piperazine ring. Nevertheless, analysis of the piperazine substitution pattern reveals a lack Creative Commons Attribution 3.0 Unported Licence. of structural diversity, with almost every single drug in this category (83%) containing a substituent at both Received 16th February 2020, the N1- and N4-positions compared to a few drugs having a substituent at any other position (C2, C3, C5, Accepted 27th April 2020 and C6). Significant chemical space that is closely related to that known to be biologically relevant, therefore, remains unexplored. -
Synthesis of Condensed 1,2,4-Triazolo-Heterocycles
Chemistry SYNTHESIS OF CONDENSED 1,2,4-TRIAZOLO-HETEROCYCLES MOHAMMED A. E. SHABAN ADEL Z. NASR MAMDOUH A. M. TAHA SUMMARY: Cyclization of 2-hydrazino-1, 3-benzothiazole, 2-hydrozinoquioline, 2-hydrazinolepidine, and 2-hydrazino-pyridine with one-carbon cyclizing agents such as triethyl orthoformate, ethyl chlorofor- mate, urea, phenylthiourea, and carbon disulfide gave 3-substituted-1,2,4-triazolo (3,4, -b) 1, 3-benzothia- zoles, 3-substituted-1,2,4-triazolo (4,3-a) quinolines, 3-substituted-1,2,4-triazolo (4,3-a) quinolines, 3-substituted-1,2,4-triazolo (4,3-a) lepidines and 3-substituted-1,2,4-triazolo (4,3-a) pyridines respectively. Reactions with acetic acid and acetic anhydride gave the corresponding acetyl hydrazines which were cyclized to the 3-methyl 1,2,4-triazolo-heterocyles. Ring closure with phenyl isocyanate and phenyl isothio- cyanate, gave the intermediate 4-phenylsemicarbazides and 4-phenylthiosemicarbazides which, upon fusion, afforded the corresponding 3-oxo- and 3-thioxo-1,2,4-triazolo-heterocyles. The 3-oxo-compounds were also obtained when 2-chloroquinoloni or 2-chlorolepidine was fused with semicarbazide hydrochloride. Key Words: Synthesis, amidrazones, triazolo-heterocycles. INTRODUCTION The synthesis and biological activities of condensed In an attempt to prepare 3-methyl-1,2,4-triazolo (3,4-b) 1,2,4-triazolo (3,4-z) heterocyles have recently been 1,3-benzothiazole (5a) by heating 2-hydrazino-1, 3- reviewed (14). Several condendes 1,2,4-triazolo-hetero- benzothiazole (1a) with an excess of acetic acid or acetic cyles exhibit various biological activities such as fungicidal anhydride, 1,1,2-triacetyl-2-(1,3-benzothiazol-2-yl) hyd- (1,9) bactericidal (1,9) analgesic (4,7,10) anxiolytic (8) razine (3a) was obtained. -
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Synthesis of [1,3,2]Dithiazolo[4,5-B][1,2,5]Oxadiazolo[3,4-E]Pyrazines
General Papers ARKIVOC 2011 (xi) 69-81 Synthesis of [1,3,2]dithiazolo[4,5-b][1,2,5]oxadiazolo[3,4-e]pyrazines Lidia S. Konstantinova,a Vadim V. Popov,a Natalia V. Obruchnikova,a Konstantin A. Lyssenko,b Ivan V. Ananyev,b and Oleg A. Rakitina* aN. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Leninsky Prospect, 47, 119991 Moscow, Russia bA. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Vavilov Str., 28, 119991 Moscow, Russia E-mail: [email protected] Abstract The reaction temperature has a strong impact on the results of chlorination of 5,6-bis(tert- butylthio)[1,2,5]oxadiazolo[3,4-b]pyrazine that is readily prepared from 5,6- dichloro[1,2,5]oxadiazolo[3,4-b]pyrazine and sodium tert-butylsulfide. Mono- and bis(sulfenylchlorides) were selectively obtained in high yield and their structure was confirmed by the reaction with morpholine. Treatment of [1,2,5]oxadiazolo[3,4-b]pyrazine-5,6-disulfenyl dichloride with primary aliphatic amines and benzylamine afforded N-substituted [1,3,2]dithiazolo[4,5-b][1,2,5]oxadiazolo[3,4-e]pyrazines in moderate yields. Novel pentacyclic [1,2,5]oxadiazolo[3'',4'':5',6']pyrazino[2',3':5,6][1,2,4]thiadiazino[3,4-b][1,3]benzothiazole, whose structure was confirmed by X-ray diffraction, was obtained by the reaction of this disulfenyl dichloride with 2-aminobenzothiazole. Keywords: Fused 1,3,2-dithiazoles, [1,2,5]oxadiazolo[3,4-b]pyrazines, disulfenyl dichlorides, primary amines, bis(tert-butylthio) derivatives, chlorination Introduction Amongst five-membered -
Drug–Drug Salt Forms of Ciprofloxacin with Diflunisal and Indoprofen
CrystEngComm View Article Online COMMUNICATION View Journal | View Issue Drug–drug salt forms of ciprofloxacin with diflunisal and indoprofen† Cite this: CrystEngComm,2014,16, 7393 Partha Pratim Bag, Soumyajit Ghosh, Hamza Khan, Ramesh Devarapalli * Received 27th March 2014, and C. Malla Reddy Accepted 12th June 2014 DOI: 10.1039/c4ce00631c www.rsc.org/crystengcomm Two salt forms of a fluoroquinolone antibacterial drug, Crystal engineering approach has been effectively ciprofloxacin (CIP), with non-steroidal anti-inflammatory drugs, utilized in recent times in the synthesis of new forms particu- diflunisal (CIP/DIF) and indoprofen (CIP/INDP/H2O), were synthe- larly by exploiting supramolecular synthons. Hence the sized and characterized by PXRD, FTIR, DSC, TGA and HSM. Crystal identification of synthons that can be transferred across Creative Commons Attribution-NonCommercial 3.0 Unported Licence. structure determination allowed us to study the drug–drug different systems is important. For example, synthon trans- interactions and the piperazine-based synthon (protonated ferability in cytosine and lamivudine salts was recently dem- piperazinecarboxylate) in the two forms, which is potentially useful onstrated by Desiraju and co-workers by IR spectroscopy for the crystal engineering of new salt forms of many piperazine- studies.20a Aakeröy and co-workers successfully estab- based drugs. lished the role of synthon transferability (intermolecular amide⋯amide synthons) in the assembly and organization of Multicomponent pharmaceutical forms consisting of an bidentate acetylacetonate (acac) and acetate “paddlewheel” active pharmaceutical ingredient (API) and an inactive 20b complexes of a variety of metal(II)ions. Recently Das et al. co-former,whichisideallyagenerally recognized as safe – have reported the gelation behaviour in various diprimary This article is licensed under a 1 3 (GRAS) substance, have been well explored in recent times. -
A Comparative Evaluation of Lafutidine and 2 Rabeprazole in The
1 *Original research paper 2 A comparative evaluation of Lafutidine and 3 Rabeprazole in the treatment of gastritis and 4 peptic ulcer: A double-blind, randomized study 5 in Indian patients. 6 Dr. Sanjay Kumar 1, Dr. Bhupesh Dewan 2*, Deepashri Shah 2 7 8 1Global Liver and Gastroenterology Centre, Bhopal, India 2 9 Medical Department, Zuventus Healthcare Ltd., Mumbai, India 10 11 . 12 ABSTRACT 13 Aims: To assess the efficacy of lafutidine therapy versus rabeprazole in Indian patients with endoscopically and histologically proven gastritis and peptic ulcer. Study design: A double blind, double dummy, randomized, comparative study. Place and Duration of Study: Global Liver and Gastroenterology Centre, Bhopal, India, between March 2010 and October 2010. Methodology: A total of 100 patients were enrolled, including 50 with endoscopically and histologically proven gastritis and other 50 with peptic ulcer (over 5 mm in diameter). Each group was randomized to receive either lafutidine or rabeprazole tablet and their corresponding competitor placebo dummy tablet, for a period of 4 weeks. Gastritis/ulcer cure rates confirmed by endoscopic histology, symptom response and Helicobacter pylori (H. Pylori) eradication were compared among the two drugs Results: Complete cure of gastritis was observed in all the patients (100%) treated with lafutidine and 95.24% [20/21; 95% CI: 76.18 to 99.88%] patients treated with rabeprazole. Complete cure of ulcer was observed in 72.0% (18/25, 95% CI = 50.61 to 87.93%) and 79.16% (19/24, 95% CI = 57.85 to 92.87%) patients treated with lafutidine and rabeprazole respectively. There was no significant difference in gastritis/ulcer cure rate and symptom response rate between the two treatment groups at the end of the study. -
Pharmacologyonline 2: 971-1020 (2009) Newsletter Gabriella Galizia
Pharmacologyonline 2: 971-1020 (2009) Newsletter Gabriella Galizia THE TREATMENT OF THE SCHIZOPHRENIA: AN OVERVIEW Gabriella Galizia School of Pharmacy,University of Salerno, Italy e-mail: [email protected] Summary The schizophrenia is a kind of psychiatric disease, characterized by a course longer than six months (usually chronic or relapsing), by the persistence of symptoms of alteration of mind, behaviour and emotion, with such a seriousness to limitate the normal activity of a person. The terms antipsychotic and neuroleptic define a group of medicine principally used to treat schizophrenia, but they are also efficacious for other psychosis and in states of psychic agitation. The antipsychotics are divided into two classes: classic or typical and atypical. The paliperidone, the major metabolite of risperidone, shares with the native drug the characteristics of receptoral bond and of antagonism of serotonin (5HT2A) and dopamine (D2). It's available in a prolonged release formulation and it allows the administration once daily. Besides, the paliperidone has a pharmacological action independent of CYT P450 and in such way a lot of due pharmacological interactions would be avoided to interference with the activity of the CYP2D6, that is known to have involved in the metabolism of the 25% of the drugs of commune therapeutic employment. Introduction The schizophrenia has been a very hard disease to investigate by the research. This is not surprising because it involves the most mysterious aspects of human mind, as emotions and cognitive processes. According to scientific conventions, the schizophrenia is a kind of psychiatric disease, characterized by a course longer than six months (usually chronic or relapsing), by the persistence of symptoms of alteration of mind, behaviour and emotion, with such a seriousness to limitate the normal activity of a person. -
Tall Man Lettering List REPORT DECEMBER 2013 1
Tall Man Lettering List REPORT DECEMBER 2013 1 TALL MAN LETTERING LIST REPORT WWW.HQSC.GOVT.NZ Published in December 2013 by the Health Quality & Safety Commission. This document is available on the Health Quality & Safety Commission website, www.hqsc.govt.nz ISBN: 978-0-478-38555-7 (online) Citation: Health Quality & Safety Commission. 2013. Tall Man Lettering List Report. Wellington: Health Quality & Safety Commission. Crown copyright ©. This copyright work is licensed under the Creative Commons Attribution-No Derivative Works 3.0 New Zealand licence. In essence, you are free to copy and distribute the work (including other media and formats), as long as you attribute the work to the Health Quality & Safety Commission. The work must not be adapted and other licence terms must be abided. To view a copy of this licence, visit http://creativecommons.org/licenses/by-nd/3.0/nz/ Copyright enquiries If you are in doubt as to whether a proposed use is covered by this licence, please contact: National Medication Safety Programme Team Health Quality & Safety Commission PO Box 25496 Wellington 6146 ACKNOWLEDGEMENTS The Health Quality & Safety Commission acknowledges the following for their assistance in producing the New Zealand Tall Man lettering list: • The Australian Commission on Safety and Quality in Health Care for advice and support in allowing its original work to be either reproduced in whole or altered in part for New Zealand as per its copyright1 • The Medication Safety and Quality Program of Clinical Excellence Commission, New South -
(12) United States Patent (10) Patent N0.: US 6,967,201 B1 Briner Et Al
US006967201B1 (12) United States Patent (10) Patent N0.: US 6,967,201 B1 Briner et al. (45) Date of Patent: *Nov. 22, 2005 (54) BENZOFURYLPIPERAZINES AND (56) References Cited BENZOFURYLHOMOPIPERAZINES: SEROTONIN AGONISTS U.S. PATENT DOCUMENTS 5,698,766 A 12/1997 Julius et 211. (75) Inventors: Karin Briner, Indianapolis, IN (US); 6,638,936 B1 * 10/2003 Briner et a1. Joseph Paul Burkhart, Plain?eld, IN (US); Timothy Paul Burkholder, FOREIGN PATENT DOCUMENTS Carmel, IN (US); Brian Eugene EP 0 006 524 A 1/1980 Cunningham, Martinsville, IN (US); EP 0 189 612 A 8/1986 Matthew Joseph Fisher, Mooresville, W0 W0 95 11243 A 4/1995 IN (US); William Harlan Gritton, W0 W0 97 08167 A 3/1997 Zionsville, IN (US); Shawn W0 W0 97 36893 A 10/1997 Christopher Miller, Noblesville, IN (US); J e?'rey Thomas Mullaney, OTHER PUBLICATIONS Indianapolis, IN (US); Matthew Robert Kuipers W. et al: “N4-unsubstituted 1-6 nl-arylpiperaZines Reinhard, Indianapolis, IN (US); as high-affinity 5 -HT1A recept r ligands” Journal of Medici Dennis Charles Thompson, nal Chemistry., vol. 38, No. 11, May 26, 1995, pp. 1942 Indianapolis, IN (US); Leonard Larry 1954, XP002153536 American Chemical Society. Washing Winneroski, Greenwood, IN (US); ton., US ISSN: 0022-2623. Yanping Xu, Fishers, IN (US) * cited by examiner (73) Assignee: Eli Lilly and Company, Indianapolis, Primary Examiner—Emily Bernhardt IN (US) (74) Attorney, Agent, or Firm—R. Craig Tucker (57) ABSTRACT (*) Notice: Subject to any disclaimer, the term of this patent is extended or adjusted under 35 U.S.C. 154(b) by 0 days. -
Package Leaflet: Information for the User Hydroxyzine Bluefish 25 Mg
Package leaflet: Information for the user Hydroxyzine Bluefish 25 mg film-coated tablets hydroxyzine hydrochloride Read all of this leaflet carefully before you start using this medicine because it contains important information for you. - Keep this leaflet. You may need to read it again. - If you have any further questions, ask your doctor or pharmacist. - This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours. - If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. See section 4. What is in this leaflet 1. What Hydroxyzine Bluefish is and what it is used for 2. What you need to know before you use Hydroxyzine Bluefish 3. How to use Hydroxyzine Bluefish 4. Possible side effects 5. How to store Hydroxyzine Bluefish 6. Contents of the pack and other information 1. What Hydroxyzine Bluefish is and what it is used for Hydroxyzine Bluefish blocks histamine, a substance found in body tissues. It is effective against anxiety, itching and urticaria. Hydroxyzine Bluefish is used to treat anxiety in adults itching (pruritus) associated with hives (urticaria) in adults adolescents and children of 5 years and above 2. What you need to know before you take Hydroxyzine Bluefish Do not take Hydroxyzine Bluefish - if you are allergic to hydroxyzine hydrochloride or any of the other ingredients of this medicine (listed in section 6) - if you are allergic (hypersensitive) to cetirizine, aminophylline, ethylenediamine or piperazine derivatives (closely related active substances of other medicines).