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

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HEARD OF F-SOFOSBUVIR...CN103848877A

F SOFOSBUVIR

1613739-48-2
L-​Alanine, N-​[[P(S)​,​2'R]​-​2'-​deoxy-​2',​5-​difluoro-​2'-​methyl-​P-​phenyl-​5'-​uridylyl]​-​, 1-​methylethyl ester
C₂₂ H₂₈ F₂ N₃ O₉ P, 547.44

http://www.google.com/patents/CN103848877A?cl=en


Preparation of Comparative Example II of the compound of formula I
The present invention with reference to US20110251152A1 (Example 1) Preparation of the technical contents disclosed to give a compound of formula II.

 δ (1HNMR, DMS0_d6): 1.25 (d, J = 22.4Hz, 3H), 3.64 (m, 1H), 3.83 (m, 3H), 5.27 (m, 1H), 5.64 (m, 1H), 5.66 (m, 1H), 5.97 (d, J = 18.8Hz, 1H), 9.96 (d, J = 8.0Hz, 1H), 11.45 (s, lH) ppm; δ (19FNMR, DMS0-d6): - 159.9 (s) ppm; MS: 261 (MH +) o
 The preparation of the usual 2Sofosbuvir
The present invention with reference to US20110251152A1 (Example 10_7) Preparation of the technical contents disclosed in the Sofosbuvir.

 δ (1HMlR, DMS0_d6): 1.15 (d, J = 6.0Hz, 6H), 1.22 (d, J = 6.4Hz, 3H), 1.25 (d, J = 22.3Hz, 3H), 3.80-4.00 ( m, 3H), 4.11 (m, 1H), 4.42 (m, 1H), 4.52 (m, 1H), 5.00 (m, 1H), 5.30 (d, J = 8.0Hz, 1H), 6.20 (m, 1H ), 7.10-7.30 (m, 3H), 7.30-7.35 (m, 2H), 7.46 (d, J = 8.2Hz, 1H), 11.45 (s, 1H) ppm; δ (19MMR, DMS0_d6): - 161.68 ( s) ppm; δ (31PNMR, DMS0-d6): 3.35 (s) ppm; MS: 530 (MH +) o
Preparation of Comparative Example 3 Compound of Formula III
The present invention with reference to Chinese Patent Application CN201310098009.6 (Example 4) Preparation of the technical contents disclosed to give a compound of formula III.

δ (1HNMR, DMS0_d6): 1.35 (d, J = 22.4Hz, 3H), 3.71 (m, 1H), 3.98 (m, 1H), 4.13 (m, 1H), 4.93 (m, 1H), 5.72 (m, 1H), 6.05 (d, J = 20.4Hz, 1H), 7.76 (d, J = 6.8Hz, 1H), 11.88 (s, lH) ppm; δ (19FNMR, DMS0-d6): - 168.06 (s), -176.03 (s) ppm; MS: 279 (MH +) o
 The preparation of the usual 4F_Sofosbuvir
The present invention with reference to Chinese Patent Application CN201310098009.6 (Example 5) was prepared technical contents disclosed to Ij F-Sofosbuvir0

δ (1HMlR, DMS0-d6): 1.13 (d, J = 6.0Hz, 6H), 1.22 (d, J = 6.4Hz, 3H), 1.25 (d, J = 22.3Hz, 3H), 3.80- 4.00 (m, 3H), 4.11 (m, 1H), 4.42 (m, 1H), 4.52 (m, 1H), 5.00 (m, 1H), 6.20 (m, 1H), 7.10-7.30 (m, 3H) , 7.30-7.35 (m, 2H), 7.46 (d, J = 8.1Hz, 1H), 11.50 (s, lH) ppm; δ (19FNMR, DMS0-d6): - 161.68 (s), -167.58 (s) ppm; δ (31PNMR, DMS0_d6): 3.35 (s) ppm; MS: 548 (MH +).





http://www.google.com/patents/CN103848876A?cl=en
A compound of the structure shown in formula I,

Wherein, X is selected from F, Cl, Br, I of any one.

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Kawran Bazar

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Dry fish sellers at the Karwan Dry Fish Market (Bazar), Dhaka, Bangladesh.

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Cadila reports Stable amorphous form of vortioxetine hydrobromide...WO 2015044963

Vortioxetine
O N Sept. 30, 2013 — The U.S. Food and Drug Administration today approved Brintellix (vortioxetine) to treat adults with major depressive disorder. Major depressive disorder (MDD),

Commonly referred to as depression, is a mental disorder characterized by mood changes and other symptoms that interfere with a person’s ability to work, sleep, study, eat and enjoy once-pleasurable activities. Episodes of depression often recur throughout a person’s lifetime, although some may experience a single occurrence.

 READ ALL AT http://www.drugs.com/newdrugs/fda-approves-brintellix-major-depressive-disorder-3918.html


 SYNTHESIS........http://newdrugapprovals.org/2013/10/01/vortioxetine-fda-approves-brintellix-to-treat-major-depressive-disorder/

     

NEW PATENT WO 2015044963 An amorphous vortioxetine and salts thereof Cadila Healthcare Ltd Singh, Kumar Kamlesh; Gajera, Jitendra Maganbhai; Raikwar, Dinesh Kumar; Khera, Brij; Dwivedi, Shri Prakash Dhar

The present invention relates to an amorphous vortioxetine and salts thereof. In particular, the invention relates to a process for the preparation of an amorphous vortioxetine hydrobromide. Further, the invention also relates to a process for preparation of amorphous vortioxetine free base. The invention also relates topharmaceutical compositions comprising an amorphous vortioxetine or hydrobromide salt thereof for oral administration for treatment of major depressive disorder (MDD) and generalized anxiety disorder (GAD).

Stable amorphous form of vortioxetine hydrobromide, useful for treating depression, major depressive disorder (MDD) and generalized anxiety disorder. Also claims a process for preparing the amorphous form and solid dispersions comprising the same.

This API, which was originally developed and launched by Lundbeck and Takeda for treating MDD. A phase IV trial (NCT02357797) for schizophrenia was scheduled to begin in March 2015.
Family members of the product case, WO03029232, hold SPC protection in the EP until 2027 and one of its Orange Book listed filings, US7144884, expire in the US in 2023 with US154 extension.

The US FDA Orange Book also lists patents describing crystalline forms of vortioxetine/Brintellix, US8722684 and US8969355, that are due to expire in 2030 and 2027 respectively. The drug also has NCE exclusivity expiring in September 2018.




Cadila is potentially interested in vortioxetine hydrobromide.    

P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent.

P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent.

P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent.

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