Brexpiprazole ブレクスピプラゾール...NEW PATENT WO-2015054976

Brexpiprazole

ブレクスピプラゾール

OPC-34712, UNII-2J3YBM1K8C, OPC34712,

CAS 913611-97-9,

Molecular Formula:C₂₅H₂₇N₃O₂S

Molecular Weight:433.56578 g/mol

7-[4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy]-1H-quinolin-2-one

7-[4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy]quinolin-2(1H)-one

2(1H)​-​Quinolinone, 7-​[4-​(4-​benzo[b]​thien-​4-​yl-​1-​piperazinyl)​butoxy]​-

7- [ 4- ( 4-benzo[b]thiophen-4- yl-piperazin-l-yl)butoxy] -lH-quinolin-2-one

7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one

UNII-2J3YBM1K8C

Otsuka Pharma Co Ltd,

OTSUKA ...............INNOVATOR

NDA is considered filed as of September 9, 2014 (60 days after submission). The PDUFA date is July 11, 2015.

 SEE AT http://newdrugapprovals.org/2015/03/23/brexpiprazole/
WO-2015054976  SEE THIS PATENT
AT NEW DRUG APPROVALS BLOG

SUZHOU VIGONVITA LIFE SCIENCES CO., LTD.














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GSK WO2011025799

http://www.google.com/patents/WO2011025799A1?cl=en


Example 72
7V-[(3S)-l-(3-cyano-4'-fluoro-4-biphenylyl)-3-pyrrolidinyl]-L-prolinami(ie
hydrochloride

A solution of 1,1-dimethylethyl (25)-2-({[(35)-l-(3-cyano-4'-fluoro-4-biphenylyl)- 3-pyrrolidinyl]amino}carbonyl)-l-pyrrolidinecarboxylate (72 mg, 0.150 mmol) in HCl (4 M solution in 1,4-dioxane, 0.50 mL, 2.00 mmol) was stirred at RT for 1 h 25 min. The reaction mixture was diluted with Et₂O (2 mL), and the resultant precipitate was filtered through a plug of cotton and washed with Et₂O (1 mL). The solid was dissolved in MeOH and concentrated under a stream of nitrogen at 50 ⁰C. Water (2 mL) was added and the mixture was lyophilized with a Genevac^® HT-4X to afford the title compound (48 mg, 77%). LC-MS m/z 379 (M+H)⁺, 0.95 min (ret time).














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