DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Fasoracetam
- Molecular FormulaC10H16N2O2
- Average mass196.246 Da
Fasoracetam is a research chemical of the racetam family.[3] It is a putative nootropic that failed to show sufficient efficacy in clinical trials for vascular dementia. It is currently being studied for its potential use for attention deficit hyperactivity disorder.[2][4]
Fasoracetam appears to agonize all three groups of metabotropic glutamate receptors and has improved cognitive function in rodent studies.[5] It is orally bioavailable and is excreted mostly unchanged via the urine.[6]
Fasoracetam was discovered by scientists at the Japanese pharmaceutical company Nippon Shinyaku, which brought it through Phase 3 clinical trials for vascular dementia, and abandoned it due to lack of efficacy.[5][7]
Scientists at Children’s Hospital of Philadelphia led by Hakon Hakonarson have studied fasoracetam’s potential use in attention deficit hyperactivity disorder.[5] Hakonarson started a company called neuroFix Therapeutics to try to bring the drug to market for this use; neuroFix acquired Nippon Shinyaku’s clinical data as part of its efforts.[7][8] neuroFix was acquired by Medgenics in 2015.[8] Medgenics changed its name to Aevi Genomic Medicine in 2016.[9] Clinical trials in adolescents with ADHD who also have mGluR mutations started in 2016.[8]
SYN
Chemistry – A European Journal, 24(27), 7033-7043; 2018
PAPER
Chemistry – A European Journal (2018), 24, (27), 7033-7043
https://onlinelibrary.wiley.com/doi/full/10.1002/chem.201800372
Amidation of unprotected amino acids has been investigated using a variety of ‘classical“ coupling reagents, stoichiometric or catalytic group(IV) metal salts, and boron Lewis acids. The scope of the reaction was explored through the attempted synthesis of amides derived from twenty natural, and several unnatural, amino acids, as well as a wide selection of primary and secondary amines. The study also examines the synthesis of medicinally relevant compounds, and the scalability of this direct amidation approach. Finally, we provide insight into the chemoselectivity observed in these reactions.
Patent
WO-2019143829
Novel crystalline forms of fasoracetam , processes for their preparation and compositions comprising them are claimed.
PATENT
WO2019143824
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2019143824&_cid=P10-JYNTH3-69052-1
Novel crystalline and cocrystal forms of fasoracetam (R-fasoracetam) and a co-former, processes for their preparation and compositions comprising them are claimed. Also claims are novel crystalline forms of fasoracetam and 4-aminobenzoic acid or trimesic acid or R- ibuprofen or phloroglucinol or methyl-3,4-5-trihydroxybenzoate or ethyl gallate or phthalic acid or 6-hydroxy-2-napthoic acid or 4-nitrobenzoic acid or 2-indole-3-acetic acid or urea and their monohydrate and dihydrate (designated as Form B).
PATENT
WO2018195184
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2018195184&_cid=P10-JYNTI8-69210-1
claiming methods for diagnosing and treating ADHD in biomarker positive subjects, assigned to Aevi Genomics Medicine, Inc and The Childrens Hospital of Philadelphia , naming different teams.
PAPER
https://advances.sciencemag.org/content/3/9/e1701028
References
- ^ FDA/NIH Substance registration system. Page accessed March 21, 2016
- ^ Jump up to:a b “Drug Profile Fasoracetam”.
- ^ “5-oxo-D-prolinepiperidinamide monohydrate – Compound Summary”. Retrieved 21 July 2013.
- ^ “Recommended INN List 40” (PDF). WHO Drug Information. 12 (2). 1998.
- ^ Jump up to:a b c Connolly, J; Glessner, J; Kao, C; Elia, J; Hakonarson, H. “ADHD & Pharmacotherapy: Past, Present and Future: A Review of the Changing Landscape of Drug Therapy for Attention Deficit Hyperactivity Disorder”. Ther Innov Regul Sci. 49 (5): 632–642. doi:10.1177/2168479015599811. PMC 4564067. PMID 26366330.
- ^ Malykh, AG; Sadaie, MR (12 February 2010). “Piracetam and piracetam-like drugs: from basic science to novel clinical applications to CNS disorders”. Drugs. 70 (3): 287–312. doi:10.2165/11319230-000000000-00000. PMID 20166767.
- ^ Jump up to:a b Moskowitz, D. H. (2017). Finding the Genetic Cause and Therapy for ADHD, Autism and 22q. BookBaby (self published). ISBN 9781483590981.
- ^ Jump up to:a b c Sharma, B. “Medgenics: NFC-1 Could Be A Key Future Revenue Driver”.
- ^ “Press Release: Medgenics, Inc. Announces Name Change to Aevi Genomic Medicine, Inc”. Aevi via MarketWired. 16 December 2016.
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| IUPAC name
(5R)-5-(Piperidine-1-carbonyl)pyrrolidin-2-one
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| Properties | |||
| C10H16N2O2 | |||
| Molar mass | 196.250 g·mol−1 | ||
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Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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/////////Fasoracetam, attention deficit hyperactivity disorder, NS 105, Phase 3, vascular dementia
C1CCN(CC1)C(=O)[C@H]2CCC(=O)N2
New Drug Approvals 