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Probable GSK 2245035

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Figure imgf000047_0002 GSK 2245035 PROBABLE

8H-​Purin-​8-​one, 6-​amino-​2-​butoxy-​7,​9-​dihydro-​9-​[[1-​(2-​hydroxyethyl)​-​4-​piperidinyl]​methyl]​-

CAS NO 1264370-20-8

GSK 2245035

PHASE 2, Allergic asthma; Allergic rhinitis

Toll-like receptor 7 agonist

Immunomodulators; Interferon alfa 2a stimulants; Toll-like receptor 7 agonists

  • 01 Aug 2014 GlaxoSmithKline completes a phase II trial in Allergic asthma and allergic rhinitis in Canada (NCT01788813)
  • 31 Jul 2013 GlaxoSmithKline completes a phase II trial in Allergic asthma and allergic rhinitis in Canada (NCT01607372)
  • 29 Mar 2013 GlaxoSmithKline initiates enrolment in a phase II trial for Allergic asthma and allergic rhinitis in Canada (NCT01788813)

WP_000297

Patent

WO2011098451

 https://www.google.com/patents/WO2011098451A1?cl=en

Example 2: 6-Amino-2-(butyloxy)-9-([1 -(2-hvdroxyethyl)-3-piperidinyllmethyl|-7,9-dihydro-8/-/-purin-8- one

2-(Butyloxy)-8-(methyloxy)-9-(-piperidinylmethyl)-9/-/-purin-6-amine (for example, as prepared for Intermediate 14) (33.4 mg, 0.1 mmol) was suspended in DMF (0.3 mL) was added to 2- bromoethanol (commercially available, for example, from Aldrich) (0.0071 mL, 0.100 mmol). DIPEA (0.040 mL, 0.23 mmol) was added. The reaction was shaken in a stoppered vial at ambient temperature overnight. The reaction mixture was diluted with DMSO (0.4 mL) and the resultant solution purified by MDAP (Method A). Appropriate fractions were combined and evaporated in vacuo. The residues was dissolved in 4M HCI in dioxane (0.4 mL) and allowed to stand at room temperature overnight. The solvent was dried under a stream of nitrogen in the Radleys blowdown apparatus. The residue was redissolved in methanol (0.5 mL) and applied to the top of a 0.5 g aminopropyl SPE (preconditioned with methanol, 2 CV). The cartridge was washed with methanol (2 mL). The solvent was dried under a stream of nitrogen in the Radleys blowdown apparatus to give the title compound (0.022 g).

LCMS (System A): tRET = 0.57min; MH+ 365

 

REF

pdf (892 KB), English, Pages 211

hrcak.srce.hr/file/138695
by K BENDELJA – ‎2012 – ‎Related articles

titis B vaccine both manufactured by GlaxoSmithKline. MPL is a nontoxic derivate … GSK2245035 compound that is a highly selective TLR7 agonist. Intranasal …

Study ID Status Title Patient Level Data
116392 Completed A randomised, double blind, placebo-controlled study to investigate the safety, pharmacodynamics and efficacy against allergic reactivity of repeat intranasal administration of the TLR7 agonist GSK2245035 in subjects with respiratory allergies
116958 Completed A randomized, double blind, placebo-controlled study to investigate the safety, pharmacodynamics and effect on allergic reactivity of repeat intranasal administration of the TLR7

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DR ANTHONY CRASTO

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 29 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 29 year tenure till date Aug 2016, Around 30 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 25 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 13 lakh plus views on New Drug Approvals Blog in 212 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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