搜索此博客

2017年3月10日星期五

Olodaterol HCl

Name: Olodaterol HCl
CAS#: 869477-96-3
Chemical Formula: C21H26N2O5
Exact Mass: 386.18417
Molecular Weight: 386.44
Elemental Analysis:
 
 
EOS Med Chem produce Olodaterol HCl 869477-96-3  in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Olodaterol HCl 869477-96-3  Intermediates, EOS Med Chem have 8; Olodaterol HCl 869477-96-3  Impurity we have 10, all from GMP, FDA plant.
Now Olodaterol HCl 869477-96-3  DMF document is preparing.
Until 2016, Aug, Olodaterol HCl 869477-96-3  more than produced 25kg API, 120kg Intermediates
 
olodaterol BI-1744;Striverdi 868049-49-4(free base)
olodaterol BI-1744;Striverdi 869477-96-3(HCl)
olodaterol Intermediates 1-(5-(benzyloxy)-2-hydroxyphenyl)ethanone 30992-63-3
olodaterol Intermediates 1-(5-(benzyloxy)-2-hydroxy-3-nitrophenyl)ethanone 861841-94-3
olodaterol Intermediates 1-(3-amino-5-(benzyloxy)-2-hydroxyphenyl)ethanone 861841-90-9
olodaterol Intermediates 8-acetyl-6-(benzyloxy)-2H-benzo[b][1,4]oxazin-3(4H)-one 869478-09-1
olodaterol Intermediates 6-(benzyloxy)-8-(2-bromoacetyl)-2H-benzo[b][1,4]oxazin-3(4H)-one 926319-53-1
olodaterol Intermediates (R)-6-(benzyloxy)-8-(oxiran-2-yl)-2H-benzo[b][1,4]oxazin-3(4H)-one 869478-12-6
olodaterol Intermediates 6-benzyloxy-8-((R)-2-chloro-1-hydroxy-ethyl)-4H-benzo[1,4]-oxazin-3-one 869478-11-5
 
 
Description: Olodaterol (trade name Striverdi) is a long acting beta-adrenoceptor agonist used as an inhalation for treating patients with chronic obstructive pulmonary disease (COPD), manufactured by Boehringer-Ingelheim. Olodaterol was approved by FDA in 2014 for the treatment of chronic obstructive pulmonary disease.
Synonym: Olodaterol; Striverdi
IUPAC/Chemical Name: (R)-6-hydroxy-8-(1-hydroxy-2-((1-(4-methoxyphenyl)-2-methylpropan-2-yl)amino)ethyl)-2H-benzo[b][1,4]oxazin-3(4H)-one
SMILES Code: O=C1COC2=C([C@@H](O)CNC(C)(C)CC3=CC=C(OC)C=C3)C=C(O)C=C2N1
 
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO.
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
 
 
1: Hussar DA, Wetty DR. New Drugs: Dulaglutide, olodaterol hydrochloride, and vorapaxar sulfate. J Am Pharm Assoc (2003). 2015 Jan 1;55(1):106-11. doi: 10.1331/JAPhA.2015.15504. PubMed PMID: 25575154.
2: Buhl R, Maltais F, Abrahams R, Bjermer L, Derom E, Ferguson G, Fležar M, Hébert J, McGarvey L, Pizzichini E, Reid J, Veale A, Grönke L, Hamilton A, Korducki L, Tetzlaff K, Waitere-Wijker S, Watz H, Bateman E. Tiotropium and olodaterol fixed-dose combination versus mono-components in COPD (GOLD 2-4). Eur Respir J. 2015 Jan 8. pii: ERJ-01360-2014. [Epub ahead of print] PubMed PMID: 25573406.
3: Olodaterol (Striverdi Respimat) for COPD. Med Lett Drugs Ther. 2015 Jan 5;57(1459):1-3. PubMed PMID: 25555071.
4: Donohue JF. Systematic review comparing LABA, olodaterol, and indacaterol: limitations. Int J Chron Obstruct Pulmon Dis. 2014 Dec 5;9:1331-5. doi: 10.2147/COPD.S74766. eCollection 2014. PubMed PMID: 25525350; PubMed Central PMCID: PMC4266268.
5: ZuWallack R, Allen L, Hernandez G, Ting N, Abrahams R. Efficacy and safety of combining olodaterol Respimat(®) and tiotropium HandiHaler(®) in patients with COPD: results of two randomized, double-blind, active-controlled studies. Int J Chron Obstruct Pulmon Dis. 2014 Oct 14;9:1133-44. doi: 10.2147/COPD.S72482. eCollection 2014. PubMed PMID: 25342898; PubMed Central PMCID: PMC4206204.
6: Feldman GJ, Bernstein JA, Hamilton A, Nivens MC, Korducki L, LaForce C. The 24-h FEV1 time profile of olodaterol once daily via Respimat® and formoterol twice daily via Aerolizer® in patients with GOLD 2-4 COPD: results from two 6-week crossover studies. Springerplus. 2014 Aug 9;3:419. doi: 10.1186/2193-1801-3-419. eCollection 2014. PubMed PMID: 25187881; PubMed Central PMCID: PMC4152473.
7: Roskell NS, Anzueto A, Hamilton A, Disse B, Becker K. Once-daily long-acting beta-agonists for chronic obstructive pulmonary disease: an indirect comparison of olodaterol and indacaterol. Int J Chron Obstruct Pulmon Dis. 2014 Jul 31;9:813-24. doi: 10.2147/COPD.S59673. eCollection 2014. PubMed PMID: 25114521; PubMed Central PMCID: PMC4124050.
8: Koch A, Pizzichini E, Hamilton A, Hart L, Korducki L, De Salvo MC, Paggiaro P. Lung function efficacy and symptomatic benefit of olodaterol once daily delivered via Respimat® versus placebo and formoterol twice daily in patients with GOLD 2-4 COPD: results from two replicate 48-week studies. Int J Chron Obstruct Pulmon Dis. 2014 Jul 5;9:697-714. doi: 10.2147/COPD.S62502. eCollection 2014. PubMed PMID: 25045258; PubMed Central PMCID: PMC4094569.
9: Ferguson GT, Feldman GJ, Hofbauer P, Hamilton A, Allen L, Korducki L, Sachs P. Efficacy and safety of olodaterol once daily delivered via Respimat® in patients with GOLD 2-4 COPD: results from two replicate 48-week studies. Int J Chron Obstruct Pulmon Dis. 2014 Jun 16;9:629-45. doi: 10.2147/COPD.S61717. eCollection 2014. PubMed PMID: 24966672; PubMed Central PMCID: PMC4064950.
10: Smit M, Zuidhof AB, Bos SI, Maarsingh H, Gosens R, Zaagsma J, Meurs H. Bronchoprotection by olodaterol is synergistically enhanced by tiotropium in a guinea pig model of allergic asthma. J Pharmacol Exp Ther. 2014 Feb;348(2):303-10. doi: 10.1124/jpet.113.208439. Epub 2013 Dec 4. PubMed PMID: 24307202.