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Patent
NeRRe Therapeutics | Date: 2016-12-27

This invention relates to the new use of the compound 2-(R)-(4-Fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide (orvepitant) or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing it for the treatment of chronic cough, including chronic refractory cough and to combinations for such a use.


Patent
NeRRe Therapeutics | Date: 2017-02-07

This invention relates to the new use of the compound (I) or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing it for the treatment of pruritus and to combinations for such a use.


Trower M.K.,NeRRe Therapeutics | Fisher A.,Transpharmation Ltd | Upton N.,Transpharmation Ltd | Ratti E.,NeRRe Therapeutics | Ratti E.,Takeda Pharmaceutical
Experimental Dermatology | Year: 2014

Data suggest that substance P could play an important role in pruritus, and therefore, blockade of the neurokinin (NK)-1 receptor might be antipruritic. Thus, we explored in the Mongolian gerbil the effect on scratching behaviour, induced by intra-dermal injection of the NK-1 receptor-specific agonist GR73632, of oral administration of the NK-1 receptor antagonist orvepitant. Orvepitant at all doses tested (0.1-10 mg/kg p.o.) produced a profound inhibition of GR73632 (30 nmol i.d.) induced hindlimb scratching; the minimum effective dose of orvepitant in this model was identified as ≤0.1 mg/kg. The data generated supported the proposition that the antipruritic potential of orvepitant should be evaluated in clinical trials. © 2014 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.


Ridler K.,Imanova Ltd. | Gunn R.N.,Imperial College London | Searle G.E.,Imanova Ltd. | Barletta J.,Imanova Ltd. | And 11 more authors.
Journal of Psychopharmacology | Year: 2014

GSK1144814 is a potent, insurmountable antagonist at human NK1 and NK3 receptors. Understanding the relationship between plasma pharmacokinetics and receptor occupancy in the human brain, was crucial for dose selection in future clinical studies. GSK1144814 occupancy data were acquired in parallel with the first-time-in-human safety and tolerability study. [11C]GR-205171 a selective NK1 receptor PET ligand was used to estimate NK1 occupancy at several time-points following single dose administration of GSK1144814. The time-plasma concentration-occupancy relationship post-single dose administration was assessed, and used to predict the plasma concentration-occupancy relationship following repeat dose administration. Repeat dose predictions were tested in a subsequent cohort of subjects examined following approximately 7 and 14 days dosing with GSK1144814. GSK1144814 was shown to demonstrate a dose-dependent occupancy of the NK1 receptor with an estimated in vivo EC50 ∼0.9 ng/mL in the human brain. A direct relationship was seen between the GSK1144814 plasma concentration and its occupancy of the brain NK1 receptor, indicating that in future clinical trials the occupancy of brain receptors can be accurately inferred from the measured plasma concentration. Our data provided support for the further progression of this compound and have optimised the likely therapeutic dose range. © 2014 The Author(s).


News Article | November 30, 2016
Site: www.newsmaker.com.au

The report provides comprehensive information on the therapeutics under development for Cough, complete with analysis by stage of development, drug target, mechanism of action (MoA), route of administration (RoA) and molecule type. The report also covers the descriptive pharmacological action of the therapeutics, its complete research and development history and latest news and press releases. Additionally, the report provides an overview of key players involved in therapeutic development for Cough   and features dormant and discontinued projects. The report helps in identifying and tracking emerging players in the market and their portfolios, enhances decision making capabilities and helps to create effective counter strategies to gain competitive advantage. Complete report on Cough - Pipeline Review, H2 2016 addition with 38 market data tables and 12 figures, spread across 96 pages is available at http://www.reportsnreports.com/reports/703640-cough-pipeline-review-h2-2016.html This report features investigational drugs from across globe covering over 20 therapy areas and nearly 3,000 indications. The report is built using data and information sourced from Global Markets Directs proprietary databases, company/university websites, clinical trial registries, conferences, SEC filings, Investor presentations and featured press releases from company/university sites and industry-specific third party sources. Drug profiles featured in the report undergoes periodic review following a stringent set of processes to ensure that all the profiles are updated with the latest set of information. Additionally, various dynamic tracking processes ensure that the most recent developments are captured on a real time basis Ax-8, benzonatate, CCP-05, CCP-06, CCP-07, CCP-08, CLAT-313, codeine + guaifenesin, cromolyn sodium,         DWJ-1340, GRC-17536, GSK-2339345, guaifenesin + hydrocodone, guaifenesin ER , JNJ-39729209, lesogaberan, levodropropizine CR, MD-990, MK-7264, NEO-5937, orvepitant maleate, S-1226, Small Molecule to Antagonize TRPA-1 for Pain And Respiratory Disorders, Small Molecules to Agonize CB1 and CB2 for Chronic Cough and Inflammatory Skin Diseases, ST-015, XEND-0501, Afferent Pharmaceuticals, Alitair Pharmaceuticals, Alveonix AG, AstraZeneca Plc, AusBio Ltd, Charleston Laboratories, Conrig Pharma ApS, Daewoong Pharmaceutical Co., GlaxoSmithKline Plc, Glenmark Pharmaceuticals Ltd., GW Pharmaceuticals Plc, Hyundai Pharmaceutical Co., Johnson & Johnson, NeRRe Therapeutics Ltd, Orbis Biosciences Inc, Inquire before buying http://www.reportsnreports.com/contacts/inquirybeforebuy.aspx?name=703640premium report price at US$2000 for a single user PDF license).


Trist D.G.,Analytical Pharmacologist | Ratti E.,NeRRe Therapeutics | Bye A.,Alan Bye and Company Ltd
Journal of Receptors and Signal Transduction | Year: 2013

The difference in location between the receptor occupancy curve of an agonist and its functional response has been described as receptor reserve. This "reserve" for a specific receptor has been found to differ from tissue to tissue and between agonists acting on the same tissue. Recently, two structurally different neurokinin 1 (NK1) receptor antagonists were taken into human and both were tested as antidepressants and for insomnia. Vestipitant and Casopitant both have high affinity for the human NK1 receptor (pKi=9.4 and 10.2, respectively). In human, at the chosen clinical doses, receptor occupancy was measured in the frontal cortex, at 24 hours post administration, as ∼90% for vestipitant (15mg) and ∼100% for casopitant (30mg). In patients with moderate to severe major depression, vestipitant given at 15mg for 8 weeks showed no statistical significant benefit as measured by change in baseline in HAM-D total score; whereas casopitant at 80mg achieved statistically significant improvement versus placebo at week 8 (LOCF HAMD17=-2.7, p=0.023). A lower dose of 30mg showed a clear but not significant separation from placebo. However, in acute studies in insomnia, both vestipitant and casopitant at 15mg and 30mg, respectively, significantly reduced latency to persistent sleep, wakenings after sleep onset and increased total sleep time by similar amounts. These clinical results suggest that for major depression the receptor occupancy of an NK1 antagonist needs to be very high (almost 100%), whereas, for insomnia a lower occupation is sufficient to give clinical effect. © 2013 Informa Healthcare USA, Inc.


Patent
NeRRe Therapeutics | Date: 2013-10-09

This invention relates to the new use of the compound (I) or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing it for the treatment of pruritus and to combinations for such a use.


The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C_(1-4 )alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.


Patent
NeRRe Therapeutics | Date: 2016-05-18

This invention relates to new use of dual NK-1/NK-3 receptor antagonists or a pharmaceutically acceptable salt thereof in the treatment of sex-hormone dependent diseases.


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