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ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 29 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 29 year tenure till date Aug 2016, Around 30 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 25 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 13 lakh plus views on New Drug Approvals Blog in 212 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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Sreeni Labs Private Limited, Hyderabad, India ready to deliver New, Economical, Scalable Routes to your advanced intermediates & API’s in early Clinical Drug Development Stages


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Sreeni Labs Private Limited, Hyderabad, India is ready to take up challenging synthesis projects from your preclinical and clinical development and supply from few grams to multi-kilo quantities. Sreeni Labs has proven route scouting ability  to  design and develop innovative, cost effective, scalable routes by using readily available and inexpensive starting materials. The selected route will be further developed into a robust process and demonstrate on kilo gram scale and produce 100’s of kilos of in a relatively short time.

Accelerate your early development at competitive price by taking your route selection, process development and material supply challenges (gram scale to kilogram scale) to Sreeni Labs…………

INTRODUCTION

Sreeni Labs based in Hyderabad, India is working with various global customers and solving variety of challenging synthesis problems. Their customer base ranges from USA, Canada, India and Europe. Sreeni labs Managing Director, Dr. Sreenivasa Reddy Mundla has worked at Procter & Gamble Pharmaceuticals and Eli Lilly based in USA.

The main strength of Sreeni Labs is in the design, development of innovative and highly economical synthetic routes and development of a selected route into a robust process followed by production of quality product from 100 grams to 100s of kg scale. Sreeni Labs main motto is adding value in everything they do.

They have helped number of customers from virtual biotech, big pharma, specialty chemicals, catalog companies, and academic researchers and drug developers, solar energy researchers at universities and institutions by successfully developing highly economical and simple chemistry routes to number of products that were made either by very lengthy synthetic routes or  by using highly dangerous reagents and Suzuki coupling steps. They are able to supply materials from gram scale to multi kilo scale in a relatively short time by developing very short and efficient synthetic routes to a number of advanced intermediates, specialty chemicals, APIs and reference compounds. They also helped customers by drastically reducing number of steps, telescoping few steps into a single pot. For some projects, Sreeni Labs was able to develop simple chemistry and avoided use of palladium & expensive ligands. They always begin the project with end in the mind and design simple chemistry and also use readily available or easy to prepare starting materials in their design of synthetic routes

Over the years, Sreeni labs has successfully made a variety of products ranging from few mg to several kilogram scale. Sreeni labs has plenty of experience in making small select libraries of compounds, carbocyclic compounds like complex terpenoids, retinal derivatives, alkaloids, and heterocyclic compounds like multi substituted beta carbolines, pyridines, quinolines, quinolones, imidazoles, aminoimidazoles, quinoxalines, indoles, benzimidazoles, thiazoles, oxazoles, isoxazoles, carbazoles, benzothiazoles, azapines, benzazpines, natural and unnatural aminoacids, tetrapeptides, substituted oligomers of thiophenes and fused thiophenes, RAFT reagents, isocyanates, variety of ligands,  heteroaryl, biaryl, triaryl compounds, process impurities and metabolites.

Sreeni Labs is Looking for any potential opportunities where people need development of cost effective scalable routes followed by quick scale up to produce quality products in the pharmaceutical & specialty chemicals area. They can also take up custom synthesis and scale up of medchem analogues and building blocks.  They have flexible business model that will be in sink with customers. One can test their abilities & capabilities by giving couple of PO based (fee for service) projects.

Some of the compounds prepared by Sreeni labs;

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See presentation below

LINK ON SLIDESHARE

Sreeni Labs Profile from Sreenivasa Reddy

Managing Director at Sreeni Labs Private Limited\

 

Few Case Studies : Source SEEENI LABS

QUOTE………….

One virtual biotech company customer from USA, through a common friend approached Sreeni Labs and told that they are buying a tetrapeptide from Bachem on mg scale at a very high price and requested us to see if we can make 5g. We accepted the challenge and developed solution phase chemistry and delivered 6g and also the process procedures in 10 weeks time. The customer told that they are using same procedures with very minor modifications and produced the tetrapeptide ip to 100kg scale as the molecule is in Phase III.

 

One East coast customer in our first meeting told that they are working with 4 CROs of which two are in India and two are in China and politely asked why they should work with Sreeni Labs. We told that give us a project where your CROs failed to deliver and we will give a quote and work on it. You pay us only if we deliver and you satisfy with the data. They immediately gave us a project to make 1.5g and we delivered 2g product in 9 weeks. After receiving product and the data, the customer was extremely happy as their previous CRO couldn’t deliver even a milligram in four months with 3 FTEs.

 

One Midwest biotech company was struggling to remove palladium from final API as they were doing a Suzuki coupling with a very expensive aryl pinacol borane and bromo pyridine derivative with an expensive ligand and relatively large amount of palldium acetate. The cost of final step catalyst, ligand and the palladium scavenging resin were making the project not viable even though the product is generating excellent data in the clinic. At this point we signed an FTE agreement with them and in four months time, we were able to design and develop a non suzuki route based on acid base chemistry and made 15g of API and compared the analytical data and purity with the Suzuki route API. This solved all three problems and the customer was very pleased with the outcome.

 

One big pharma customer from east coast, wrote a structure of chemical intermediate on a paper napkin in our first meeting and asked us to see if we can make it. We told that we can make it and in less than 3 weeks time we made a gram sample and shared the analytical data. The customer was very pleased and asked us to make 500g. We delivered in 4 weeks and in the next three months we supplied 25kg of the same product.

 

Through a common friend reference, a European customer from a an academic institute, sent us an email requesting us to quote for 20mg of a compound with compound number mentioned in J. med. chem. paper. It is a polycyclic compound with four contiguous stereogenic centers.  We gave a quote and delivered 35 mg of product with full analytical data which was more pure than the published in literature. Later on we made 8g and 6g of the same product.

 

One West coast customer approached us through a common friend’s reference and told that they need to improve the chemistry of an advanced intermediate for their next campaign. At that time they are planning to make 15kg of that intermediate and purchased 50kg of starting raw material for $250,000. They also put five FTEs at a CRO  for 5 months to optimize the remaining 5 steps wherein they are using LAH, Sodium azide,  palladium catalyst and a column chromatography. We requested the customer not to purchase the 50kg raw material, and offered that we will make the 15kg for the price of raw material through a new route  in less than three months time. You pay us only after we deliver 15 kg material. The customer didn’t want to take a chance with their timeline as they didn’t work with us before but requested us to develop the chemistry. In 7 weeks time, we developed a very simple four step route for their advanced intermediate and made 50g. We used very inexpensive and readily available starting material. Our route gave three solid intermediates and completely eliminated chromatographic purifications.

 

One of my former colleague introduced an academic group in midwest and brought us a medchem project requiring synthesis of 65 challenging polyene compounds on 100mg scale. We designed synthetic routes and successfully prepared 60 compounds in a 15 month time.  

UNQUOTE…………

 

The man behind Seeni labs is Dr. Sreenivasa Reddy Mundla 

Sreenivasa Reddy

Dr. Sreenivasa Reddy Mundla.

Managing Director at Sreeni Labs Private Limited

Sreeni Labs Private Limited

Road No:12, Plot No:24,25,26

  • IDA, Nacharam
    Hyderabad, 500076
    Telangana State, India

Links

LINKEDIN https://in.linkedin.com/in/sreenivasa-reddy-10b5876

FACEBOOK https://www.facebook.com/sreenivasa.mundla

RESEARCHGATE https://www.researchgate.net/profile/Sreenivasa_Mundla/info

EMAIL mundlasr@hotmail.com,  Info@sreenilabs.com, Sreeni@sreenilabs.com

Dr. Sreenivasa  Reddy Mundla

Dr. M. Sreenivasa Reddy obtained Ph.D from University of Hyderabad under the direction Prof Professor Goverdhan Mehta in 1992. From 1992-1994, he was a post doctoral fellow at University of Wisconsin in Professor Jame Cook’s lab. From 1994 to 2000,  worked at Chemical process R&D at Procter & Gamble Pharmaceuticals (P&G). From 2001 to 2007 worked at Global Chemical Process R&D at Eli Lilly and Company in Indianapolis. 

In 2007  resigned to his  job and founded Sreeni Labs based in Hyderabad, Telangana, India  and started working with various global customers and solving various challenging synthesis problems. 
The main strength of Sreeni Labs is in the design, development of a novel chemical route and its development into a robust process followed by production of quality product from 100 grams to 100’s of kg scale.
 

They have helped number of customers by successfully developing highly economical simple chemistry routes to number of products that were made by Suzuki coupling. they are able to shorten the route by drastically reducing number of steps, avoiding use of palladium & expensive ligands. they always use readily available or easy to prepare starting materials in their design of synthetic routes.

Sreeni Labs is Looking for any potential opportunities where people need development of cost effective scalable routes followed by quick scale up to produce quality products in the pharmaceutical & specialty chemicals area. They have flexible business model that will be in sink with customers. One can test their abilities & capabilities by giving PO based projects

Experience

Founder & Managing Director

Sreeni Labs Private Limited

August 2007 – Present (8 years 11 months)

Sreeni Labs Profile

Sreeni Labs Profile

View On SlideShare

Principal Research Scientist

Eli Lilly and Company

March 2001 – August 2007 (6 years 6 months)

Senior Research Scientist

Procter & Gamble

July 1994 – February 2001 (6 years 8 months)

Education

University of Hyderabad

Doctor of Philosophy (Ph.D.), 
1986 – 1992

 

PUBLICATIONS

Article: Expansion of First-in-Class Drug Candidates That Sequester Toxic All-Trans-Retinal and Prevent Light-Induced Retinal Degeneration

Jianye Zhang · Zhiqian Dong · Sreenivasa Reddy Mundla · X Eric Hu · William Seibel ·Ruben Papoian · Krzysztof Palczewski · Marcin Golczak

Article: ChemInform Abstract: Regioselective Synthesis of 4Halo ortho-Dinitrobenzene Derivative

Sreenivasa Mundla

Aug 2010 · ChemInform

Article: Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-β Receptor Type I Inhibitor as Antitumor Agent

Hong-yu Li · William T. McMillen · Charles R. Heap · Denis J. McCann · Lei Yan · Robert M. Campbell · Sreenivasa R. Mundla · Chi-Hsin R. King · Elizabeth A. Dierks · Bryan D. Anderson · Karen S. Britt · Karen L. Huss

Apr 2008 · Journal of Medicinal Chemistry

Article: ChemInform Abstract: A Concise Synthesis of Quinazolinone TGF-β RI Inhibitor Through One-Pot Three-Component Suzuki—Miyaura/Etherification and Imidate—Amide Rearrangement Reactions

Hong-yu Li · Yan Wang · William T. McMillen · Arindam Chatterjee · John E. Toth ·Sreenivasa R. Mundla · Matthew Voss · Robert D. Boyer · J. Scott Sawyer

Feb 2008 · ChemInform

Article: ChemInform Abstract: A Concise Synthesis of Quinazolinone TGF-β RI Inhibitor Through One-Pot Three-Component Suzuki—Miyaura/Etherification and Imidate—Amide Rearrangement Reactions

Hong-yu Li · Yan Wang · William T. McMillen · Arindam Chatterjee · John E. Toth ·Sreenivasa R. Mundla · Matthew Voss · Robert D. Boyer · J. Scott Sawyer

Nov 2007 · Tetrahedron

Article: Dihydropyrrolopyrazole Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: A Novel Benzimidazole Series with Selectivity versus Transforming Growth Factor-β Type II Receptor Kinase and Mixed Lineage Kinase-7

Hong-yu Li · Yan Wang · Charles R Heap · Chi-Hsin R King · Sreenivasa R Mundla · Matthew Voss · David K Clawson · Lei Yan · Robert M Campbell · Bryan D Anderson · Jill R Wagner ·Karen Britt · Ku X Lu · William T McMillen · Jonathan M Yingling

Apr 2006 · Journal of Medicinal Chemistry

Read full-textSource

Article: Studies on the Rh and Ir mediated tandem Pauson–Khand reaction. A new entry into the dicyclopenta[ a, d]cyclooctene ring system

Hui Cao · Sreenivasa R. Mundla · James M. Cook

Aug 2003 · Tetrahedron Letters

Article: ChemInform Abstract: A New Method for the Synthesis of 2,6-Dinitro and 2Halo6-nitrostyrenes

Sreenivasa R. Mundla

Nov 2000 · ChemInform

Article: ChemInform Abstract: A Novel Method for the Efficient Synthesis of 2-Arylamino-2-imidazolines

Read at

[LINK]

Patents by Inventor Dr.Sreenivasa Reddy Mundla

  • Patent number: 7872020

    Abstract: The present invention provides crystalline 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl)-5,6-dihydro -4H-pyrrolo[1,2-b]pyrazole monohydrate.

    Type: Grant

    Filed: June 29, 2006

    Date of Patent: January 18, 2011

    Assignee: Eli Lilly and Company

    Inventor: Sreenivasa Reddy Mundla

  • Publication number: 20100120854

    Abstract: The present invention provides crystalline 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole monohydrate.

    Type: Application

    Filed: June 29, 2006

    Publication date: May 13, 2010

    Applicant: ELI LILLY AND COMPANY

    Inventor: Sreenivasa Reddy Mundla

  • Patent number: 6066740

    Abstract: The present invention provides a process for making 2-amino-2-imidazoline, guanidine, and 2-amino-3,4,5,6-tetrahydroyrimidine derivatives by preparing the corresponding activated 2-thio-subsituted-2-derivative in a two-step, one-pot procedure and by further reacting yields this isolated derivative with the appropriate amine or its salts in the presence of a proton source. The present process allows for the preparation of 2-amino-2-imidazolines, quanidines, and 2-amino-3,4,5,6-tetrahydropyrimidines under reaction conditions that eliminate the need for lengthy, costly, or multiple low yielding steps, and highly toxic reactants. This process allows for improved yields and product purity and provides additional synthetic flexibility.

    Type: Grant

    Filed: November 25, 1997

    Date of Patent: May 23, 2000

    Assignee: The Procter & Gamble Company

    Inventors: Michael Selden Godlewski, Sean Rees Klopfenstein, Sreenivasa Reddy Mundla, William Lee Seibel, Randy Stuart Muth

TGF-β inhibitors

US 7872020 B2

Sreenivasa Reddy Mundla

The present invention provides 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl) -5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole monohydrate, i.e., Formula I.

Figure US07872020-20110118-C00002

EXAMPLE 1 Preparation of 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl-5,6-dihydro-4H -pyrrolo[1,2-b]pyrazole monohydrate

Figure US07872020-20110118-C00008

Galunisertib

1H NMR (CDCl3): δ=9.0 ppm (d, 4.4 Hz, 1H); 8.23-8.19 ppm (m, 2H); 8.315 ppm (dd, 1.9 Hz, 8.9 Hz, 1H); 7.455 ppm (d, 4.4 Hz, 1H); 7.364 ppm (t, 7.7 Hz, 1H); 7.086 ppm (d, 8.0 Hz, 1H); 6.969 ppm (d, 7.7 Hz, 1H); 6.022 ppm (m, 1H); 5.497 ppm (m, 1H); 4.419 ppm (t, 7.3 Hz, 2H); 2.999 ppm (m, 2H); 2.770 ppm (p, 7.2 Hz, 7.4 Hz, 2H); 2.306 ppm (s, 3H); 1.817 ppm (m, 2H). MS ES+: 370.2; Exact: 369.16

ABOVE MOLECULE IS

https://newdrugapprovals.org/2016/05/04/galunisertib/

Galunisertib

Phase III

LY-2157299

CAS No.700874-72-2

 

 

READ MY PRESENTATION ON

Accelerating Generic Approvals, see how you can accelerate your drug development programme

Accelerating Generic Approvals by Dr Anthony Crasto

KEYWORDS   Sreenivasa Mundla Reddy, Managing Director, Sreeni Labs Private Limited, Hyderabad, Telangana, India,  new, economical, scalable routes, early clinical drug development stages, Custom synthesis, custom manufacturing, drug discovery, PHASE 1, PHASE 2, PHASE 3,  API, drugs, medicines

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Kiran Mazumdar Shaw Conferred with ‘The Global Leadership in Engineering 2016’ Award by USC


KMS-ON-USC-VITERBI-AWARD.png.

 

http://societyofwomenengineers.swe.org/awards/individual-awards/4153-global-leadership

Society of Women Engineers

The Global Leadership Award honors a person with at least fifteen (15) years professional experience who has worked in and led an internationally based engineering, scientific or technology-based business or organization, and in doing so, serves as a role model to women engineers and technologists worldwide. A maximum of three (3) awards may be presented annually.

 

 

Biocon

“This award is a recognition of Biocon’s significant role in harnessing the potential of Biotechnology to provide affordable access to highly complex bio-pharmaceuticals like Insulins and monoclonal antibodies for the benefit of patients the world over.” – Kiran Mazumdar-Shaw

Kiran Mazumdar-Shaw

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

//////Kiran Mazumdar Shaw,  ‘The Global Leadership in Engineering 2016’ , Award by USC

I (Anthony Crasto) am Editorial Board member for our Journal of Analytical & Pharmaceutical Research


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Dear Readers
I am on  editorial board ……… Editorial Board member for our Journal of Analytical & Pharmaceutical Research………http://medcraveonline.com/JAPLR/editorial-board

This is possible with your cooperation and support

SOME PAPERS

read…….http://medcraveonline.com/JAPLR/JAPLR-02-00010.pdf
http://medcraveonline.com/JAPLR/JAPLR-02-00011.pdf

Tackling the Challenges with Poorly Soluble Drugs
http://medcraveonline.com/JAPLR/JAPLR-01-00001.pdf

New Drug Approvals Blog has 2 lakh plus viewers in USA alone


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New Drug Approvals Blog has 2 lakh plus viewers in USA alone

that is 200 thousand viewers

A record 1170135 views (11 lakh plus)all over the world in 211 countries

that is 1100 thousand plus views on this blog

I suffered a paralytic stroke in dec 2007 and bound to a wheelchair, this seems to have injected feul in me to help chemists around the world, I am more active than before and  pushing boundaries, I have 2,5 lakh connections on all networking sites, I am available to all, contact me on +91 9323115463, amcrasto@gmail.com, Twitter @amcrasto

 

 

 

My son lionel was only in first standard in school when I was hit by a deadly one in a million spine stroke called acute transverse mylitis, it made me 90% paralysed and bound to a wheel chair, He cried bitterly and we had never seen him so depressed

Now I keep Lionel as my source of inspiration and helping millions, thanks to millions of my readers who keep me going and help me to keep my son and family happy.

success

 

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Zydus Cadila’s, Lipaglyn (Saroglitazar) won a lot of support at the 75th Anniversary Conference of the American Diabetes Association


Lipaglyn (Saroglitazar) won a lot of support at the 75th Anniversary Conference of the American Diabetes Association. Lipaglyn is currently under Phase III clinical development for treatment of Non Alcoholic SteatoHepatitis (NASH), a serious liver disease and an unmet healthcare need, globally. There is currently no drug approved for treating NASH. Lipaglyn is already approved in India for the treatment of diabetic dyslipidemia

Zydus Group

20160215_115547.jpg

Speaking on the development, Mr. Pankaj R. Patel, Chairman and Managing Director, Zydus Cadila said, “These new robust scientific data on the safety and efficacy of Lipaglyn
(Saroglitazar) being presented at the 75th Annual Scientific Sessions of the American Diabetes Association (ADA) reflect our continued commitment to millions of patients living with Diabetes, Dyslipidemia, Non-alcoholic fatty liver disease (NAFLD) and Non-alcoholic steatohepatitis (NASH).”

Zydus Cadila, a leading global healthcare provider, today announced that new scientific and clinical data on Saroglitazar will be presented at the 75th Annual Scientific Sessions of the American Diabetes Association (ADA) in Boston, Massachusetts, USA from 5thto 9th June, 2015. Several analyses of real-world patient data of Saroglitazar will also be presented. The abstracts are available on theADA website.

Lipaglyn – The world’s first drug for treating Diabetic Dyslipidemia combines lipid and glucose lowering effects in one single molecule.

Pankaj Patel, chairman and MD, Cadila Healthcare Ltd

 

 

 

Zydus is an innovation-led global healthcare provider that discovers, manufactures and markets a broad range of healthcare therapies. The group employs over 19,000 people worldwide including over 1200 scientists engaged in research and is dedicated to creating healthier communities globally.

With a strong research pipeline of NCEs, biologics and vaccines, the group became India’s first pharmaceutical company to launch its own indigenously researched therapy Lipaglyn which is also the world’s first approved therapy for diabetic dyslipidaemia. Exemptia, the world’s first biosimilar of Adalimumab is also a product of Zydus innovation. Zydus also collaborates with partners to support and make therapies affordable and accessible to communities across the world.

As a leading healthcare provider, it aims to become a global research-based pharmaceutical company by 2020.

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Zydus Group

 

Pankaj R. Patel (left), Chairman & Managing Director, Zybus Cadila,

Ganesh Nayak, Chief Operating Officer and Executive Director, Zydus Cadila

 

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Zydus Cadila has announced a breakthrough in the anti-diabetic drug Lipaglyn. Lipaglyn – The world’s first drug for treating Diabetic Dyslipidemia combines lipid and glucose lowering effects in one single molecule.

The Zydus Group announced a breakthrough in its research efforts with Lipaglyn (Saroglilazar), a novel drug targeted at bridging an unmet healthcare need for treating Diabetic Dyslipidemia or Hypertriglyeeridemia in Type II diabetes, not controlled by statins alone. The drug has been approved for launch in India by the Drug Controller General of India (DCGI). With a novel action that offers lipid and glucose lowering effects in one molecule, Lipaglyn is the first Glitazar to be approved anywhere in the world.
“Lipaglyn provides patients suffering from diabetic dyslipidemia the option of a once-daily oral therapy that has a beneficial effect on both lipid parameters as well as glycemic control,” said Pankaj R. Fatel, Chairman and Managing Director, Zydus Cadila. “It has always been our dream to take a molecule right from the concept stage up to its launch. Today, we have realized this dream. It is an important breakthrough and I would like to dedicate this to all the Indian research scientists in the Held of drug discovery,” Patel added,
Diabetic Dyslipidemia is a condition where a person is diabetic and has elevated levels of the total cholesterol, the “bad” low-density lipoprotein (LDL) cholesterol and the triglycerides and a decrease in the “good” high-density lipoprotein (HDL) cholesterol concentration in the blood. Optimal LDL cholesterol levels ibr adults with diabetes are less than 100 mg/dh, optimal HDL cholesterol levels are equal to or greater than 40 mg/dL, and desirable triglycerides levels are less than 150 mg/dLT LipaglynrM, a non-thiazoKdinedione, is the first therapy to be approved for this condition,
World over, it is estimated that 30% of all deaths occur due lo cardiovascular diseases (CVD). In India, one out of every five persons is at serious risk of developing CVD, Research has shown that diabetes is one of the major risk factors of CVD. India has a population of nearly 65 million diabetics and 77 million prc-diabctics, 85 – 97% of the diabetes patients suffer from dyslipidemia or lipid abnormalities. Hence, addressing the problem of diabetes and dyslipidemia is crucial in tackling the health risk posed by CVD.
Discovered by the Zydus Research Centre, the dedicated NCE research arm of the Zydus group, LipaglynrM is a best-in-class innovation, designed to have a unique cellular mechanism of action following an extensive structure-activity relationship study initiated in the year 2000, Lipaglyn1M has a predominant affinity to PPAR alpha isoform and moderate affinity to PPAR gamma isoform of PPAR nuclear receptor subfamily. The molecule has shown beneficial effects on lipids and glyeemic control without side effects. This molecule underwent extensive pre-clinical characterisation and the I.ND was submitted in the year 2004,
As a part of the clinical development programme, extensive Phase-I, Phase-II and Phase-Ill clinical trials were conducted to evaluate the phamacokinetics, pharmacodynamics, efficacy and safety of Lipaglyn. The new drug application for Lipaglyn1 was based on a comprehensive clinical development programme spanning eight years.
Results from the first Phase III programme with Pioglitazone as a comparator drug in diabetes patients showed that the 4 mg dose of Lipaglyn led to a reduction of triglycerides and LDL (bad) cholesterol, and an increase in HDL (good) cholesterol and also showed a reduction in Fasting Plasma Glucose and glycosylated haemoglobin (HbAlc) thereby confirming its beneficial effects of both lipid and glyeemic control in diabetic patients,
In the second Phase III study, Lipaglyn was studied in diabetic dyslipidemic patients insufficiently controlled with statin therapy. The results from this study confirmed that Lipaglyn had a pronounced beneficial effect on both the lipid and glyeemic parameters in these subjects.
In both the studies, Lipaglyn was well tolerated and had a better safety profile than the comparators. Importantly Lipaglyn1 M has a non-renal route of elimination, and did not show adverse events like edema, weight gain, myopathies or derangement of liver and/or kidney functions, thus making it sale and efficacious. LipaglynIM is recommended for once daily administration as 4 mg tablets.
Zydus will offer a dedicated LipaglynIM support programme to patients and earegivers, The programme shall provide important support and information regarding access, adherence, education and thereby help patients to start and appropriately manage their disease and therapy over time.

About Lipaglyn

Lipaglyn[TM] (Saroglitazar) was launched in September 2013 in India, for treating Hypertriglyceridemia and Diabetic Dyslipidemia in Patients with Type 2 Diabetes not controlled by statins. Since then, more than 80,000 patients are availing this drug with a prescriber base over 3500 diabetologists, cardiologists and physicians. Lipaglyn[TM] helps in a reduction of triglycerides and LDL (bad) cholesterol, and an increase in HDL (good) cholesterol and has also shown a reduction in Fasting Plasma Glucose and glycosylated haemoglobin (HbA1c), thereby confirming its beneficial effects on both lipid and glycemic control in diabetic patients. Lipaglyn[TM] is a prescription medicine, and can be taken only under the advice and guidance of a registered medical practitioner.

About Zydus

Zydus Cadila is an innovative, global pharmaceutical company that discovers, manufactures and markets a broad range of healthcare therapies, including small molecule drugs, biologic therapeutics and vaccines. The group employs over 16,500 people worldwide including over 1200 scientists engaged in R & D and is dedicated to creating healthier communities globally. As a leading healthcare provider, it aims to become a global research based pharmaceutical company by 2020.

References

Zydus to present new scientific data on Lipaglyn in the US

New Delhi, Jun 8 (UNI) Healthcare services provider, Zydus Cadila today said the new scientific and clinical data on Lipaglyn (Saroglitazar) will be presented at the 75th annual scientific sessions of the American Diabetes Association (ADA) in Boston, Massachusetts, US from 5th to 9th June,2015.
Read more at http://www.uniindia.com/news/business-economy/zydus-to-present-new-scientific-data-on-lipaglyn-in-the-us/84440.html

READ …..https://newdrugapprovals.org/2013/06/07/cadila-banks-on-diabetes-druglipaglynsaroglitazar/

SEE…..https://newdrugapprovals.org/2015/03/09/saroglitazar-magnesium-new-patent-wo-2015029066-cadila-healthcare-ltd/

http://lipaglyn.com/downloads/Lipaglyn_Product_Monograph.pdf

http://www.ijpcs.net/sites/default/files/IJPCS_3_1_02_0.pdf

http://zyduscadila.com/wp-content/uploads/2015/08/Saroglitazar-in-Diabetic-Dyslipidemia-1-Year-Data.pdf

http://onlinelibrary.wiley.com/doi/10.1002/prp2.136/pdf

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Mr. Glenn Saldanha Chairman & and Managing Director, Glenmark Pharmaceuticals Limited, conferred ‘India Pharma Leader Award’ by the Government of India


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Mr. Glenn Saldanha Chairman & and Managing Director, Glenmark Pharmaceuticals Limited, conferred ‘India Pharma Leader Award’ by the Government of India

Indian Ministry for Chemicals and Fertilizers on Thursday conferred 1st India Pharma awards to 12 Indian drug companies under various categories to motivate Indian Pharma and medical devices industries.

As per reports, Union Minister for Chemicals and Fertilizers Ananth Kumar conferred 1st India Pharma awards in Bengaluru on Thursday evening.

Speaking on the occasion, Ananth Kumar said that the Pharma Industry in the country is growing at a higher rate than GDP and needs to be complimented for this.
“Indian government would like domestic Pharma industry to be global leaders,” he said, adding that the government and the Pharma entrepreneurs will work together as team Pharma India, with the aim of serving millions of ailing people. He also assured full support to the industry.

The awards constituted by Department of Pharmaceuticals were given to outstanding Pharma Industries to motivate Indian Pharma and medical devices industries. The winner of the awards are:

CATEGORY OF AWARD NAME OF THE COMPANY
OVERALL INDIA PHARMA EXCELLENCE AWARD CADILA HEALTHCARE LIMITED

INDIA PHARMA LEADER AWARD GLENN SALDANA, CHAIRMAN & MANAGING DIRECTOR, GLENMARK PHARMACEUTICALS LIMITED

INDIA PHARMA COMPANY OF THE YEAR AWARD LUPIN LIMITED

INDIA PHARMA BULK DRUG COMPANY OF THE YEAR AWARD SMS PHARMACEUTICALS LTD

INDIA PHARMA INNOVATION OF THE YEAR AWARD CADILA HEATHCARE LIMITED

INDIA PHARMA RESEARCH AND DEVELOPMENT ACHIEVEMENT AWARD SUN PHARMACEUTICALS INDUSTRIES LTD

INDIA PHARMA CORPORATE SOCIAL RESPONSIBILITY PROGRAMME OF THE YEAR AWARD ABBOTT INDIA LIMTED

INDIA PHARMA MEDICAL DEVICES COMPANY OF THE YEAR AWARD HARSORIA HEALTHCARE PVT LTD

INDIA PHARMA EXPORT COMPANY OF THE YEAR AWARD CAMUS PHARMA PVT LTD

INDIA PHARMA BULK DRUG EXPORT COMPANY OF THE YEAR SMS PHARMACEUTICALS LTD

INDIA PHARMA MEDICAL DEVICES EXPORT COMPANY OF THE YEAR AWARD SCOPE MEDICAL DEVICES PVT LTD

SPECIAL AWARD: PHARMA PSU COMPANY OF THE YEAR AWARD KARNATAKA ANTIBIOTICS AND PHARMACEUTICALS LIMITED, A PSU UNDER DEPARTMENT OF PHARMACEUTICALS

CLIP

India Pharma Awards given by Minister of Chemicals and …

pib.nic.in/newsite/PrintRelease.aspx?relid=134291

Jan 8, 2016 – OVERALL INDIA PHARMA EXCELLENCE AWARD. CADILA HEALTHCARE LIMITED. INDIA PHARMA LEADER AWARD. SHRI GLENN …

Press Information Bureau
Government of India
Ministry of Chemicals and Fertilizers
08-January-2016 12:49 IST

India Pharma Awards given by Minister of Chemicals and Fertilizers

The Union Minister for Chemicals and Fertilizers, Shri Ananth Kumar gave away the 1st India Pharma awards in Bengaluru on Thursday evening. The awards constituted by Department of Pharmaceuticals were given to outstanding Pharma Industries to motivate Indian Pharma and medical devices industries. The winner of the awards are:

CATEGORY OF AWARD NAME OF THE COMPANY
OVERALL INDIA PHARMA EXCELLENCE AWARD CADILA HEALTHCARE LIMITED
INDIA PHARMA LEADER AWARD SHRI GLENN SALDANA, CHAIRMAN & MANAGING DIRECTOR, GLENMARK PHARMACEUTICALS LIMITED
INDIA PHARMA COMPANY OF THE YEAR AWARD LUPIN LIMITED
INDIA PHARMA BULK DRUG COMPANY OF THE YEAR AWARD SMS PHARMACEUTICALS LTD
INDIA PHARMA INNOVATION OF THE YEAR AWARD CADILA HEATHCARE LIMITED
INDIA PHARMA RESEARCH AND DEVELOPMENT ACHIEVEMENT AWARD SUN PHARMACEUTICALS INDUSTRIES LTD
INDIA PHARMA CORPORATE SOCIAL RESPONSIBILITY PROGRAMME OF THE YEAR AWARD ABBOTT INDIA LIMTED
INDIA PHARMA MEDICAL DEVICES COMPANY OF THE YEAR AWARD HARSORIA HEALTHCARE PVT LTD
INDIA PHARMA EXPORT COMPANY OF THE YEAR AWARD CAMUS PHARMA PVT LTD
INDIA PHARMA BULK DRUG EXPORT COMPANY OF THE YEAR SMS PHARMACEUTICALS LTD
INDIA PHARMA MEDICAL DEVICES EXPORT COMPANY OF THE YEAR AWARD SCOPE MEDICAL DEVICES PVT LTD
SPECIAL AWARD: PHARMA PSU COMPANY OF THE YEAR AWARD KARNATAKA ANTIBIOTICS AND PHARMACEUTICALS LIMITED, A PSU UNDER DEPARTMENT OF PHARMACEUTICALS

Speaking on the occasion the Shri Ananth Kumar said that the Pharma Industry in the country is growing at a higher rate than GDP and needs to be complimented for this.  He said that the government would like domestic Pharma industry to be global leaders. He said that the government and the Pharma entrepreneurs will work together as team Pharma India, with the aim of serving millions of ailing people.  Shri Ananth Kumar assured full support to the industry.

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References

http://www.pharmaceuticals.gov.in/sites/default/files/First%20India%20Pharma%20Awards%202015.pdf

http://pib.nic.in/newsite/PrintRelease.aspx?relid=134291

http://www.glenmarkpharma.com/common/pdf/Glenn_Saldanha-Profile.pdf

http://pharmaceuticals.gov.in/sites/default/files/First%20India%20Pharma%20Awards%202015%20%20Final.pdf

http://www.pharmaceuticals.gov.in/sites/default/files/First%20India%20Pharma%20Awards%202015.pdf

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Breaking and Making of Olefins Simultaneously Using Ozonolysis: Application to the Synthesis of Useful Building Blocks and Macrocyclic Core of Solomonamides


Abstract Image

A simple and practical one-pot, two-directional approach to access olefinic esters through simultaneous breaking and making of olefins using ozonolysis of alkenyl aryl selenides is disclosed. The scope of the method with a variety of examples is demonstrated, and the end products obtained here are useful building blocks. As a direct application of the present method, the macrocyclic core of potent anti-inflammatory natural cyclic peptides, solomonamides, is synthesized.

Breaking and Making of Olefins Simultaneously Using Ozonolysis: Application to the Synthesis of Useful Building Blocks and Macrocyclic Core of Solomonamides

CSIR-National Chemical Laboratory, Division of Organic Chemistry, Dr. Homi Bhabha Road, Pune 411008, India
Org. Lett., 2015, 17 (9), pp 2090–2093
DOI: 10.1021/acs.orglett.5b00637
Publication Date (Web): April 14, 2015
Copyright © 2015 American Chemical Society
Figure
GENERAL METHOD
 

Dr. D. Srinivasa Reddy

New Drug Approvals blog by Dr Anthony Crasto hits ten lakh views in 211 countries


 

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New Drug Approvals hits ten lakh views in 211 countries

https://newdrugapprovals.org/

 

 

 

 

ANTHONY MELVIN CRASTO

THANKS AND REGARD’S
DR ANTHONY MELVIN CRASTO Ph.D

amcrasto@gmail.com

MOBILE-+91 9323115463
GLENMARK SCIENTIST ,  INDIA
web link
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photo
Dr. Anthony Melvin Crasto
Principal Scientist, Glenmark Pharma
    

 

 

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DR SRINIVASA REDDY gets NASI – Reliance Industries Platinum Jubilee Award (2015) for Application Oriented Innovations in Physical Sciences.


 

DR REDDY

DR SRINIVASA REDDY  recieving NASI – Reliance Industries Platinum Jubilee Award (2015) for Application Oriented Innovations in Physical Sciences.

Dr. D. Srinivasa Reddy, Senior Scientist, Division of Organic Chemistry, CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune – 411 008

AWARD CLICK HERE….LINK

PUNE: Senior scientist of National Chemical Laboratory (NCL), D Srinivasa Reddy has been selected for this year’s NASI-Reliance Industries Platinum Jubilee award for the application oriented innovations in the area of physical sciences instituted by the National Academy of Sciences, India (NASI). Two awards each in physical sciences and two in biological sciences are given every year, a statement issued by NCL said.

Manindra Agrawal from Department of Computer Science and Engineering, Indian Institute of Kanpur is the other recipient of this award in physical sciences. Each award carries a plaque and Rs 2 lakh cash.

The award will be presented in the 85th annual session of National Academy of Sciences, India. Reddy’s research group interests are in the field of total synthesis and drug discovery by applying medicinal chemistry. He has also been involved in the synthesis of the agrochemicals like small molecules for crop protection, said the statement. The total synthesis of more than 20 natural products has been achieved in his lab including a sex pheromone that attracts the mealy bugs and has potential use in the crop protection.

On the medicinal chemistry front significant progress has been made by his group using a new concept called silicon-switch approach towards central nervous system drugs. Identification of new chemical entities for the potential treatment of diabetes and infectious diseases is being done in collaboration with industry partners.

Read about DR REDDY  at 

click

One Organic Chemist One Day: Dr. D. Srinivasa Reddy of …

oneorganichemistoneday.blogspot.com/2015/02/dr-d-srinivasa-reddy.html

Feb 23, 2015 – Dr. Reddy’s research group current interests are in the field of total synthesis and drug discovery by applying medicinal chemistry

Dr. D. Srinivasa Reddy of NCL winner Shanti Swarup Bhatnagar Award 2015

 

Some details

The National Academy of Sciences, India (NASI) 5, Lajpatrai Road, Allahabad – 211002 NASI-RELIANCE INDUSTRIES PLATINUM JUBILEE AWARDS FOR THE YEAR 2015 FOR APPLICATION ORIENTED INNOVATIONS COVERING BOTH PHYSICAL AND BIOLOGICAL SCIENCES NASI invites nominations for the NASI-Reliance Industries Platinum Jubilee Awards for APPLICATION ORIENTED INNOVATIONS for the year 2015. The nominee should be an Indian citizen / Overseas Citizen of India working in India and below the age of 50 years as on April 15, 2015. Areas for the Awards – Physical Sciences, including – Chemistry, Engineering, Mathematics, Physics, Electronics, Nanotechnology, Information & Computer Sciences, Earth and Atmospheric Sciences; Biological Sciences, including – Agriculture, Animal and Plant Sciences, Environment, Biotechnology, Biochemistry, Bioprocess Engineering, Bioinformatics, all branches of medical sciences and Nanotechnology. Number and Value of Awards – two in Physical Sciences and two in Biological Sciences each year. Each award carries a Plaque and Rs. 2 lakhs in cash. Nominators and Last Date – All Science Secretaries, Secretary HRD, Director Generals – CSIR, ICMR & ICAR; Directors of IITs, IIITs, National Laboratories, Industries with well recognized R&D units including private research institutions; Vice-Chancellors of all Universities – Central & State; Directors of Indian Institute of Science, Bangalore, AIIMS, New Delhi, PGI’s of Medical Research, Chairman, UGC; Presidents of all Science and Engineering Academies (Engineering, Medical, Agriculture); All Fellows of the NASI. The nomination shall be made in the prescribed format. Twenty (20) copies of the nomination form along with only one soft copy (in CD), complete in all respect with the supporting documents, must reach the Academy latest by April 15, 2015. A candidate may only be nominated once. However, a nomination will remain valid for consideration for 3 years or the age eligibility which ever expires earlier. Selection of the Awardees – As per Regulations of NASI Presentation of the Awards – The presentation of the Awards will be made at the time of 85 th Annual Session of NASI. Details and Nomination form for the award are also available on NASI’s website http://www.nasi.org.in and http://www.nasi.nic.in …………….http://www.nasi.org.in/NASI-Reliance%20Industries%20Platinum%20Jubilee%20Awards%202015.pdf

SEE

http://www.nasi.org.in/NASI-Reliance%20Industries%20Platinum%20Jubilee%20Awardees%20(2015).htm

PUNE: Senior scientist at National Chemical Laboratory (NCL) D Srinivasa Reddy has bagged yet another award, the NASI-Reliance Industries Platinum Jubilee award for the year 2015.

This is the second award Reddy has won in a span of less than a fortnight. Earlier, he was selected for the bronze medal presented by the Chemical Research Society of India (CRSI). He has also been a recipient of excellence award from the National Drug Research Institute.

The platinum jubilee award is being conferred for his work in application-oriented innovations in physical sciences category.

Every year, this award recognises two scientists, each working in the fields of physical and biological sciences.

The other scientist who has been awarded in this category is Manindra Agarwal from IIT, Kanpur.

Reddy along with his team has been involved in several high-end research in drug discovery, mainly by applying medicinal chemistry. Other major works he undertook also involve synthesising of agrochemicals meant to be used for crop protection.

He also has vast experience working with various pharmaceutical companies prior to joining NCL in 2010.

The award consists of cash of Rs 2 lakh.

NASI

National Academy of Sciences, India (www.nasi.org.in) was founded in 1930 with the objective to provide a national forum for the scientists to help them publish their research work and discuss the issues for the solutions. NASI-Reliance together give two awards each in the areas of physical and biological sciences for the application oriented innovations started from the year 2006. Areas for the Awards – Physical Sciences, including Chemistry, Engineering, Mathematics, Physics, Electronics, Nanotechnology, Information & Computer Sciences, Earth and Atmospheric Sciences; Biological Sciences, including Agriculture, Animal and Plant Sciences, Environment, Biotechnology, Biochemistry, Bioprocess Engineering, Bioinformatics, all branches of medical sciences and Nanotechnology.

 

Read about DR REDDY  at

One Organic Chemist One Day: Dr. D. Srinivasa Reddy of …

oneorganichemistoneday.blogspot.com/2015/02/dr-d-srinivasa-reddy.html

Feb 23, 2015 – Dr. Reddy’s research group current interests are in the field of total synthesis and drug discovery by applying medicinal chemistry

Dr. D. Srinivasa Reddy of NCL winner Shanti Swarup Bhatnagar Award 2015

 

 

Some pictures of his group


NCL, PUNE

//////////DR SRINIVASA REDDY , NASI – Reliance Industries Platinum Jubilee Award, 2015, Application Oriented Innovations in Physical Sciences,

SILICO LINEZOLID, SILINEZOLID, NDS 10024


Therapeutic options for brain infections caused by pathogens with a reduced sensitivity to drugs are limited. Recent reports on the potential use of linezolid in treating brain infections prompted us to design novel compounds around this scaffold. Herein, we describe the design and synthesis of various oxazolidinone antibiotics with the incorporation of silicon.

Our findings in preclinical species suggest that silicon incorporation is highly useful in improving brain exposures. Interestingly, three compounds from this series demonstrated up to a 30-fold higher brain/plasma ratio when compared to linezolid thereby indicating their therapeutic potential in brain associated disorders

Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure

CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411008, India
Daiichi Sankyo India Pharma Pvt. Ltd., Gurgaon, Haryana 122015, India
§ Incozen Therapeutics Pvt. Ltd., Alexandria Knowledge Park, Turkapally, Rangareddy 500078, India
ACS Med. Chem. Lett., Article ASAP
DOI: 10.1021/acsmedchemlett.5b00213
Publication Date (Web): October 26, 2015
Copyright © 2015 American Chemical Society
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SILINEZOLID, NDS 10024
CAS 1430321-45-1
C18 H26 F N3 O3 Si, 379.50
Acetamide, N-​[[(5S)​-​3-​[4-​(4,​4-​dimethyl-​1-​aza-​4-​silacyclohex-​1-​yl)​-​3-​fluorophenyl]​-​2-​oxo-​5-​oxazolidinyl]​methyl]​-
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Examples from patent

Figure US20140296133A1-20141002-C00027
    (S)—N((3-(4-(4,4-dimethyl-1,4-azasilinan-1-yl)-3-fluorophenyl)-2 oxooxazolidin-5-yl)methyl)acetamide
    NDS 10024
Patent   US20140296133
SEE
AUTHORS
    Preparation of (S)—N((3-(4-(4,4-dimethyl-1,4-azasilinan-1-yl)-3-fluorophenyl)-2 oxooxazolidin-5-yl)methyl)acetamide (12)

  • Figure US20140296133A1-20141002-C00027
  • To a solution of 8 (50 mg, 0.135 mmol) in dimethylformamide (DMF), lithium-t-butoxide (LiOtBu) (32.3 mg, 0.4 mmol) is added. The mixture is stirred at 25° C. for 15 min, followed by the addition of MeOH (0.01 mL, 0.27 mmol). 6 (52 mg, 0.27 mmol) is then added and the reaction mixture is allowed to stir at 25° C. for 24 h. Glacial acetic acid is then added and the organic phase is extracted with EtOAc and washed with brine solution. The crude material is purified by column chromatography on silica gel using hexane-EtOAC mixtures to furnish the pure product 12. The analogous procedure for the corresponding morpholine analogue was adapted from Lu, C. V.; Chen, J. J.; Perrault, W. R.; Conway, B. G.; Maloney, M. T.; Wang, Y. Org. Pro. Res. and Development. 2006, 10, 272-277.
  • 1H NMR (200 MHz, CDCl3): δ 7.33 (d, J=13.8 Hz, 1H), 7.02-6.94 (m, 2H), 6.52 (t, J=5.8 Hz, 1H), 4.77-4.73 (m, 1H), 3.99 (t, J=9.04 Hz, 1H), 3.72 (dd, J=9.0 Hz, 6.8 Hz, 1H), 3.69-3.58 (m, 2H), 3.31 (t, J=5.5 Hz, 4H), 2.01 (s, 3H), 0.89 (t, J=5.5 Hz, 4H), 0.10 (s, 6H). 13C NMR (100 MHz, CDCl3): δ171.2, 155.0 (d, J=244.3 Hz), 154.5, 138.2 (d, J=9.3 Hz), 131.5, 119.9, 114.0 (d, J=3.4 Hz), 107.6 (d, J=27.1 Hz), 71.9, 50.9, 47.7, 41.9, 23.0, 14.3, −2.9.
    Preparation of Bis(bromomethyl)dimethylsilane (2) (as per scheme 2)

  • Figure US20140296133A1-20141002-C00028
  • HBr gas is bubbled to a solution of dimethyl divinylsilane 1 (10.0 g, 89.28 mmols), and dibenzoylperoxide (DBP, 100 mg), in heptane (100 mL) at 0° C. for 30 min. The Reaction mixture (RM) is allowed to stir at room temperature (25° C.) for 18 h, water (200 mL) is added to the reaction mixture and the organic layer is separated. The heptane layer is washed with 2N NaOH (2 100 mL), dried and concentrated to obtain the product 2 as a colourless liquid (24.5 g) in 100% yield.
  • 1H NMR (200 MHz, CDCl3): δ 3.58-3.49 (m, 4H), 1.45-1.40 (m, 4H), 0.09 (s, 6H).
      Preparation of 1-benzyl-4,4-dimethyl-1,4-azasilinane (3)

    • Figure US20140296133A1-20141002-C00029
    • Benzylamine (20 mL, 182 mmol) and Et3N (15.2 mL, 109 mmol) are added to a solution of bis-(bromomethyl) dimethylsilane 2 (10 g, 36.5 mmol) in chloroform (100 mL). The mixture is then refluxed for 16 h. 5% sodiumhydroxide solution (150 mL) is then added and the aqueous layer is extracted with dichloromethane (DCM, 2×100 mL). It is then washed with brine (200 mL), dried and concentrated. The product is purified by column chromatography on silica gel using hexane-EtOAc mixtures to obtain the product 3 as a light yellow liquid (4.3 g) in 54% yield.
    • 1H NMR (200 MHz, CDCl3): δ 7.23-7.35 (m, 5H), 3.66 (s, 2H), 2.68 (t, J=6.3 Hz, 4H), 0.75 (t, J=6.3 Hz, 4H), 0.04 (s, 6H).

Preparation of 4,4-dimethyl-1,4-azasilinane hydrochloride (4)

    • Figure US20140296133A1-20141002-C00030
    • To a solution of 4,4-dimethyl-1,4-azasilinane 3 (2.3 g, 10.5 mmol) in EtOH (20 mL), 6N hydrochloricacid (1.75 mL, 10.5 mmol) is added and the solvent is removed under reduced pressure. The reaction mixture is co-evaporated with EtOH (2×10 mL) and recrystallized from EtOH-diethyl ether. To a slurry of Pd/C (50 mg) in EtOH (15 mL) an ethanolic solution of above prepared HCl salt is added drop wise and stirred at 25° C. under hydrogen atmosphere for 20 h. The reaction mixture is filtered through celite and washed with 2×20 mL of MeOH. The filtrate is then concentrated under reduced pressure to give viscous oil which was triturated with diethyl ether to obtain the product 4 as a white solid (950 mg) in 70% yield.

Preparation of 1-(2-fluoro-4-nitrophenyl)-4,4-dimethyl-1,4-azasilinane (9)

    • Figure US20140296133A1-20141002-C00031
    • To a solution of 4,4-dimethyl-1,4-azasilinane hydrochloride 4 (500 mg, 3.85 mmol) in EtOAc (15 mL), triethylamine (1.3 mL, 9.63 mmol) is added and stirred at 25° C. for 10 min. The reaction mixture is cooled to 0° C. and 3,4-difluoronitrobenzene (612 mg, 3.85 mmol) is added drop wise and allowed to stir at 25° C. for 6 h. Water is then added and the organic layer is separated. The aqueous layer is extracted with EtOAc (2×10 mL) and the solvent is removed under reduced pressure. The product is purified by column chromatography using hexane-EtOAc mixtures and a crystalline yellow solid 9 (721 mg) is obtained in 70% yield.
    • 1H NMR (200 MHz, CDCl3): δ 7.93-7.84 (m, 2H), 6.86 (t, J=4 Hz, 1H), 3.70-3.67 (m, 4H), 0.91-0.85 (m, 4H), 0.12 (s, 6H). 13C NMR (50 MHz, CDCl3): δ 151.1 (d, J=246.71 Hz), 144.4 (d, J=7.13 Hz), 137.8 (d, J=8.59 Hz), 121.4, 115.9 (d, J=4.61 Hz), 113.2 (J=27.78 Hz), 49.4, 13.8, −2.8. IR (CHCl3): ν 2948, 2894, 1603, 1523, 1492, 1400, 1342, 1223, 983, 832, 742 cm−1′. M.P: 70-72° C.

Preparation of benzyl 4-(4,4-dimethyl-1,4-azasilinan-1-yl)-3-fluorophenylcarbamate (10)

    • Figure US20140296133A1-20141002-C00032
    • To a solution of compound 9 (610 mg, 2.28 mmol) in THF (25 mL), Pd/C (30 mg) is added and hydrogenated under a pressure of 35 psi in a par hydrogenator for 8 h. The reaction mixture is filtered through celite. Celite pad is washed with THF (2×20 mL). To the filtrate, saturated NaHCO3 (420 mg, 5.01 mmol) and CBzCl (427 mg, 2.5 mmol) are added at 0° C. and stirred at 25° C. for 5 h. 10 mL water is added to reaction mixture and the aqueous layer is extracted with EtOAc (2×20 mL). The crude mixture is then subjected to column chromatography on silica gel using hexane-EtOAc mixtures to afford the product as a viscous liquid 10 (690 mg) in 82% yield.
    • 1H NMR (200 MHz, CDCl3): δ 7.41-7.37 (m, 5H), 6.94-6.93 (m, 2H), 6.68 (s, 1H), 5.21 (s, 1H), 3.3 (t, J=6.38 Hz, 4H), 0.93 (t, J=6.08 Hz, 4H), −0.13 (s, 6H). 13C NMR (50 MHz, CDCl3): 155.4 (d, 244.4 Hz), 153.6, 136.1, 135.9, 128.6, 128.5, 128.3, 120.4, 117.2 (d, 18.7 Hz), 114.7, 108.3 (20.5 Hz), 67.1, 51.4, 14.4, −3.0. IR (CHCl3): ν 3317, 2953, 2803, 1706, 1594, 1521, 1271, 1221, 1058, 869, 759 cm−1. M.P: 80-82° C.

Preparation of (S)-5-(aminomethyl)-3-(4-(4,4-dimethyl-1,4-azasilinan-1-yl)-3-fluorophenyl)oxazolidin-2-one (11) (NDS-10057)

    • Figure US20140296133A1-20141002-C00033
    • To a solution of 10 (1.20 g, 3.23 mmol) and (S)-tert-butyl 3-chloro-2-hydroxypropylcarbamate (1.35 g, 6.47 mmol) in DMF (10 mL), LiOtBu (1.03 g, 12.94 mmol) is added at 0° C. The mixture is stirred at 25° C. for 45 h. The starting material 10 is not consumed completely. Saturated NH4Cl is then added; the organic phase is extracted with EtOAc (2×20 mL), washed with brine solution, dried and concentrated. The crude residue is dissolved in 20 mL of DCM-TFA mixture (8:2) and stirred at 25° C. for 3 h. RM is concentrated and dissolved in water (10 mL), the aqueous layer is washed with diethyl ether (2×50 mL), basified with saturated NaHCO3 and extracted with DCM (2×50 mL). The DCM layer is dried and concentrated. The crude is purified by column chromatography on silica gel using hexane-EtOAc mixtures to obtain the product as an off-white solid (500 mg) in 45% (based on recovery of starting material) over 2 steps.
    • 1H NMR (400 MHz, CDCl3): δ 7.36 (dd, J=14.2 Hz, 2.3 Hz, 1H), 7.09 (dd, J=8.8 Hz, 1.7 Hz, 1H), 6.96 (t, J=9.5 Hz, 1H), 4.72-4.59 (m, 1H), 4.00 (t, J=8.3 Hz, 1H), 3.79 (dd, J=8.7 Hz, 6.8 Hz, 1H), 3.30 (t, J=6.2 Hz, 4H), 3.03 (dq, J=13.6 Hz, 4.2 Hz, 2H), 0.90 (t, J=6.2 Hz, 4H), 0.10 (s, 6H). 13C NMR (100 MHz, CDCl3): δ 155.1 (d, J=244.3 Hz), 154.7, 137.9 (d, J=9.0 Hz), 132.1 (d, J=10.3 Hz), 112.0 (d, J=4.3 Hz), 113.8 (d, J=3.2 Hz), 107.4 (d, J=26.9 Hz), 73.8, 51.0, 47.8, 45.01, 14.4, −2.9. IR (CHCl3): ν 3685, 3021, 2955, 2809, 2401, 1747, 1515, 1416, 1219, 1029, 991, 870, 771, 667 cm−1. M.P: 94-96° C. ESI-MS: 360.11 (M+Na).

Preparation of (S)—N-((3-(4-(4,4-dimethyl-1,4-azasilinan-1-yl)-3-fluorophenyl)-2-oxooxazolidin-5-yl)methy)acetamide (12) (NDS 10024)

  • Figure US20140296133A1-20141002-C00034
  • To solution of amine 11 (300 mg, 0.9 mmol) and DIPEA (0.3 mL, 1.78 mmol) in dry THF (4.0 mL), acetylchloride (0.08 mL, 1.07 mmol) is added at 0° C., and stirred at 25° C. for 3 h. Further, saturated NaHCO3 (5.0 mL) is added to the reaction mixture and extracted with EtOAc (2×5 mL). The organic layer is washed with brine, dried and concentrated. The product is purified by column chromatography on silica gel using hexane-EtOAc mixtures to obtain the product as an off-white solid (170 mg) in 50% yield.
  • 1HNMR (400 MHz, CDCl3): δ 7.33 (d, J=13.8 Hz, 1H), 7.02-6.94 (m, 2H), 6.52 (t, J=5.8 Hz, 1H), 4.77-4.73 (m, 1H), 3.99 (t, J=9.04 Hz, 1H), 3.72 (dd, J=9.0 Hz, 6.8 Hz, 1H), 3.69-3.58 (m, 2H), 3.31 (t, J=5.5 Hz, 4H), 2.01 (s, 3H), 0.89 (t, J=5.5 Hz, 4H), 0.10 (s, 6H). 13C NMR (100 MHz, CDCl3): δ171.2, 155.0 (d, J=244.3 Hz), 154.5, 138.2 (d, J=9.3 Hz), 131.5, 119.9, 114.0 (d, J=3.4 Hz), 107.6 (d, J=27.1 Hz), 71.9, 50.9, 47.7, 41.9, 23.0, 14.3, −2.9. IR (CHCl3): ν 2401, 1759, 1675, 1519, 1216, 759, 669 cm−1 M.P: 123-126° C. ESI-MS: 380.10 (M+H).
SCHEME 1
  • Figure US20140296133A1-20141002-C00015
    Figure US20140296133A1-20141002-C00016

SCHEME2

  • Figure US20140296133A1-20141002-C00018
    Figure US20140296133A1-20141002-C00019

SCHEME 3

  • Figure US20140296133A1-20141002-C00020

SCHEME 4

  • Figure US20140296133A1-20141002-C00021

str1

str1

Dr. D. Srinivasa Reddy of NCL winner Shanti Swarup Bhatnagar Award 2015

see

http://oneorganichemistoneday.blogspot.in/2015/02/dr-d-srinivasa-reddy.html

Dr. Srinivasa Reddy of CSIR-NCL bags the

prestigious Shanti Swarup Bhatnagar Prize

The award comprises a citation, a plaque, a cash prize of Rs 5 lakh

dr

The Shanti Swarup Bhatnagar Prize for the year 2015 in chemical sciences has been awarded to Dr. D. Srinivasa Reddy of CSIR-National Chemical Laboratory (CSIR-NCL), Pune for his outstanding contributions to the area of total synthesis of natural products and medicinal chemistry.
This is a most prestigious award given to the scientists under 45 years of age and who have demonstrated exceptional potential in Science and Technology. The award derives its value from its rich legacy of those who won this award before and added enormous value to Indian Science.
Dr. Reddy will be bestowed with the award at a formal function, which shall be presided over by the honourable Prime Minister. The award, named after the founder director general of Council of Scientific & Industrial Research (CSIR), Dr. Shanti Swarup Bhatnagar, comprises a citation, a plaque, a cash prize of Rs 5 lakh.
Dr. Reddy’s research group current interests are in the field of total synthesis and drug discovery by applying medicinal chemistry. He has also been involved in the synthesis of the agrochemicals like small molecules for crop protection. The total synthesis of more than twenty natural products has been achieved in his lab including a sex pheromone that attracts the mealy bugs and has potential use in the crop protection. On the medicinal chemistry front significant progress has been made by his group using a new concept called “Silicon-switch approach” towards central nervous system drugs. Identification of New Chemical Entities for the potential treatment of diabetes and infectious diseases is being done in collaboration with industry partners.
His efforts are evidenced by 65 publications and 30 patents. He has recently received the NASI-Reliance industries platinum jubilee award-2015 for application oriented innovations and the CRSI bronze medal. In addition, he is also the recipient of Central Drug Research Institute award for excellence in the drug research in chemical sciences and scientist of the year award by the NCL Research Foundation in the year 2013. Dr. Reddy had worked with pharmaceutical companies for seven years before joining CSIR-NCL in 2010.

AN INTRODUCTION

Ph.D., University of Hyderabad, 2000 (Advisor: Professor Goverdhan Mehta).

Post-doctoral with Profs. Sergey A. Kozmin(University of Chicago, USA) and Prof.

Jeffrey Aubé (University of Kansas, USA)

Experienced in leading drug discovery programs (Dr. Reddy’s & TATA Advinus – 7

years of pharma experience)

Acquired skills in designing novel small molecules and lead optimization

Experienced in planning and execution of total synthesis of biologically active

molecules with moderate complexity

One of the molecules is currently in human clinical trials.

MYSELF WITH HIM

s reddy ncl
DEC2014 NCL PUNE INDIA
DR ANTHONY WITH DR REDDY

OTHER AUTHORS

Remya Ramesh

Remya Ramesh

M.Sc Applied Chemistry
Senior Researcher
Seetharamsingh Balamkundu
Pankaj Khairnar
Srikant Viswanadha

Srikant Viswanadha

Ph.D.
Vice President
Incozen Therapeutics Pvt. Ltd. · Drug Discovery

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C[Si]1(C)CCN(CC1)c2ccc(cc2F)N3C[C@H](CNC(C)=O)OC3=O

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