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DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai)
, INDIA
36Yrs Exp. in the feld of Organic Chemistry,Working for AFRICURE PHARMA as ADVISOR earlier with GLENMARK PHARMA at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google,
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USV Limited , WO 2014167577 Synthesis of dabigatran….NEW PATENT FEATURE ON NEWDRUGAPPROVALS
USV Limited
16-Oct-2014 pub date
WO-2014167577-A2
PATENT FEATURE ON THIS BLOG
Title of the invention: “”SYNTHESIS OF DABIGATRAN”.”
Applicants: USV LIMITED (IN).
Inventors: Laxmikant Narhari Patkar (IN), Harish Kashinath Mondkar (IN), Sachin Shivaji Patil (IN), Tanaji Shamrao Jadhav (IN), Nitin Nivrutti Hagavane (IN), Rajesh Ganpat Bopalkar (IN) and Nitin Dnyaneshwar Arote (MY).
The present invention relates to a process for preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof. The present invention relates to novel compounds, in particular Ethyl-3-{[(2-formyl-l-methyl-lH-benzimidazole-5-yl) carbonyl] -(2-pyridinyl) amino} propanoate and Ethyl-3-{[(2-dichloromethyl-l-methyl -lH-benzimidazole-5-yl)carbonyl]- (2-pyridinyl) amino}propanoate and process for preparation thereof. The present invention further relates to the use of these novel compounds in the preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof.
Dabigatran is used to prevent strokes in those with atrial fibrillation due to non heart valve causes
Process for preparing dabigatran etexilate mesylate, useful for treating thrombosis, stroke and embolism. Also claims novel intermediates of dabigatran and their synthesis. Represents the first patenting from USV on this API, which was originally developed and launched, by Boehringer Ingelheim for treating conditions such as stroke, thrombosis and atrial fibrillation.
Dabigatran (Pradaxa in Australia, Europe and USA, Pradax in Canada, Prazaxa in Japan) is an oral anticoagulant from the class of the direct thrombin inhibitors. It is being studied for various clinical indications and in some cases it offers an alternative to warfarin as the preferred orally administered anticoagulant (“blood thinner”) since it does not require frequent blood tests for international normalized ratio (INR) monitoring while offering similar results in terms of efficacy. There is no specific way to reverse the anticoagulant effect of dabigatran in the event of a major bleeding event, unlike warfarin, although a potential dabigatran antidote (pINN: idarucizumab) is undergoing clinical studies. It was developed by the pharmaceutical company Boehringer Ingelheim.
Family members of its product case, WO9837075, have SPC protection in most EU states until February 2023, and expiry dates in the US until July 2020. The FDA Orange Book lists US7932273 (product derivative) and US7866474 (describing film blister-card containers for pradaxa®), which expire in September 2025 and August 2027 respectively, for dabigatran.
The drug also has New Chemical Entity exclusivity expiring on October 19, 2015. As of October 2014, Newport Premium™ reports that USV has dabigatran under development.
SEE
Настоящее изобретение относится к способу приготовления дабигатран этексилата или его фармацевтически приемлемой соли.
Настоящее изобретение относится к новым соединениям, в частности этил-3 – {[(2-формил-L-метил-LH-бензимидазол-5-ил) карбонил] – (2-пиридинил) амино} пропаноата и этил-3-{ [(2-дихлорметил-L-метил-бензимидазола-5-ил) карбонил] – (2-пиридинил) амино} пропаноат и процесс его подготовки.
Настоящее изобретение дополнительно относится к применению этих новых соединений в подготовке дабигатран этексилата или его фармацевтически приемлемой соли.
요약서 WO2014167577
본 발명은 다비가 트란 이텍 실 레이트, 또는 이들의 약학 적으로 허용 가능한 염의 제조 방법에 관한 것이다.
{[(2 – 포르 밀-L-LH-메틸 벤즈 이미 다졸 -5 – 일) 카르 보닐] – – (2 – 피리 디닐) 아미노} 프로판 산 에틸 3 – {} 본 발명은 특히 에틸 3에서, 신규 화합물에 관한 것이다 [(2 – 디클로로 메틸-L–LH 벤즈 이미 다졸 -5 – 일) 카르 보닐] – 이들의 제조 (2 – 피리 디닐) 아미노} 프로판 산 및 방법.
또한, 본 발명은 다비가 트란 이텍 실 레이트, 또는 이들의 약학 적으로 허용 가능한 염의 제조에서 이러한 신규 한 화합물의 용도에 관한 것이다.
要約書 WO2014167577
本発明は、ダビガトランまたは薬学的に許容される塩の製造方法に関する。
{[（2 – ホルミル-L-メチル – イソキノリン-ベンゾイミダゾール-5 – イル）カルボニル] – – （2 – ピリジニル）アミノ}プロパノエート及びエチル3 – {本発明は、特定のエチル3に、新規化合物に関する[（2-ジクロロ-1-メチル-1H-ベンゾイミダゾール-5 – イル）カルボニル] – その製造（2 – ピリジニル）アミノ}プロパノエートおよびプロセス。
さらに、本発明は、ダビガトランまたは薬学的に許容される塩の調製におけるこれらの新規化合物の使用に関する。
摘要 WO2014167577
本发明涉及一种用于制备达比加群酯或其药学上可接受的盐的方法。
本 发明涉及新的化合物，特别是乙基-3 – {[（2 – 甲酰基-L-甲基-LH-苯并咪唑-5 – 基）羰基] – （2 – 吡啶基）氨基}丙酸乙酯和乙基3 – { [（2 – 二氯甲基-L-甲基-1H-苯并咪唑-5 – 基）羰基] – （2 – 吡啶基）氨基}丙酸乙酯和方法，及其制备方法。
本发明还涉及在达比加群酯或其药学上可接受的盐的制备中使用这些新化合物的。
Advanced Intermediate Flow Studies: Nevirapine
After looking through a number of flow articles that describe and illustrate processes toward the production of drug final products and advanced intermediates, I thought an article from Florida State — Tyler McQuade (open source Beilstein JOC 2013) was informative and storytelling. He was able to show some of the challenges that go into designing a flow methodology around process that have already been worked out in batch mode, and had been looked at in a number of labs already.
Before talking about the chemistry, Professor McQuade talks about a number of concerns in transferring technology from batch to flow: DOE, solvent exchange (precipitation and moving from one reaction to another), Cost of Goods Analysis – reaction concentrations, solvent costs, process time, by-product formation and purification. There certainly is a lot that goes into the strategy. To give you the framework: this group was looking to make a continuous process…
View original post 247 more words
System Suitability for USP Chromatographic Methods
System Suitability for USP Chromatographic Methods
How should system suitability tests (SSTs) be structured for USP monographs? More about USP experts group’s recommendations on the parameters and acceptance criteria for SSTs and the essential aspects of this new approach can be found in this News.
read
An interesting article from the USP experts group “Small Molecules” has been published in the Pharmacopoeial Forum 39(5). It deals with USP’s future requirements regarding system suitability tests (SST).
SSTs are performed each time an analytical method is used. Together with instruments qualification and methods validation, the SST ensures the quality of analytical test results. The SST shows that a procedure and an instrumental system are performing as they did when the procedure was validated and that the method is thus “fit for purpose” for the intended use.
General requirements can be found in the USP Chapter <621> Chromatography which also contains provisions and acceptance…
View original post 116 more words
The U.S. Food and Drug Administration approved Ofev (nintedanib) for the treatment of idiopathic pulmonary fibrosis (IPF).
Nintedanib
FDA approves Ofev to treat idiopathic pulmonary fibrosis
10/15/2014
The U.S. Food and Drug Administration today approved Ofev (nintedanib) for the treatment of idiopathic pulmonary fibrosis (IPF).
read at
see synthesis
https://newdrugapprovals.org/2014/05/21/in-battle-of-ipf-drugs-bis-nintedanib-impresses/
FDA approves Esbriet (pirfenidone ピルフェニドン 吡非尼酮) to treat idiopathic pulmonary fibrosis
The U.S. Food and Drug Administration today approved Esbriet (pirfenidone)
ピルフェニドン 吡非尼酮
for the treatment of idiopathic pulmonary fibrosis (IPF).
read at
SYNTHESIS
Click for synthesis
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US priority review for Eisai cancer drug lenvatinib
US priority review for Eisai cancer drug lenvatinib
Eisai has been boosted by news that regulators in the USA have agreed to a quicker review of its anticancer agent lenvatinib.
The US Food and Drug Administration has granted a priority review to Eisai’s New Drug Application for lenvatinib as a treatment for progressive radioiodine-refractory differentiated thyroid cancer. This means that the agency has assigned a Prescription Drug User Fee Act action date of April 14 next year, eight months after the NDA was submitted.
Read more at: http://www.pharmatimes.com/Article/14-10-15/US_priority_review_for_Eisai_cancer_drug_lenvatinib.aspx#ixzz3GH3iXiDU
SEE SYNTHESIS
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Final Concept Paper ICH Q12: Technical and Regulatory Considerations for Pharmaceutical Product Lifecycle
Final Concept Paper ICH Q12: Technical and Regulatory Considerations for Pharmaceutical Product Lifecycle
Currently, there are no harmonised approaches to technical and regulatory considerations for the lifecycle management of pharmaceutical products. Therefore, ICH has just published a Final Concept Paper for a new ICH Q12 Guideline: Technical and Regulatory Considerations for Pharmaceutical Product Lifecycle. The proposed ICH Guideline is intended to fill this gap. read
ICH has just published a Final Concept Paper for a new ICH Q12 guideline: Technical and Regulatory Considerations for Pharmaceutical Product Lifecycle.
Currently, there is a lack of a harmonised approach to technical and regulatory considerations for the lifecycle management of pharmaceutical products. Although there are concepts in ICH Q8, Q9, Q10 and Q11 for a more science and risk-based approach for assessing changes across the lifecycle, several gaps exist which hinder a full realization of the benefits intended. The original aim of ‘operational flexibility’…
View original post 305 more words
DR ANTHONY MELVIN CRASTO
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