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ORGANIC SPECTROSCOPY

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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 30 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, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, 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 Open superstar 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 30 year tenure till date Dec 2017, Around 35 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, 50 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 19 lakh plus views on New Drug Approvals Blog in 216 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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Zydus receives approval from USFDA to initiate Phase II clinical studies of Saroglitazar Magnesium in patients with Primary Biliary Cholangitis (PBC)


Zydus receives approval from USFDA to initiate Phase II clinical studies of Saroglitazar Magnesium in patients with Primary Biliary Cholangitis (PBC) Read more: https://goo.gl/eugRnZ #ZydusAnnouncement

Zydus receives approval from USFDA to initiate Phase II clinical studies of Saroglitazar Magnesium in patients with Primary Biliary Cholangitis (PBC)

Ahmedabad, India, February 23, 2017

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Zydus Cadila, a research-driven, global healthcare provider, today announced that the USFDA has approved the group’s plans to initiate a Phase 2 clinical trial of Saroglitazar Magnesium (Mg) in patients with Primary Biliary Cholangitis (PBC) of the liver. This randomized, double-blind Phase 2 trial will evaluate Saroglitazar Magnesium 2mg and 4 mg Vs. Placebo.

Speaking on the development, Mr. Pankaj R. Patel, Chairman and Managing Director, Zydus Cadila said, “We are very thankful to the USFDA for their timely and useful feedback on the clinical trial designs of Saroglitazar Mg in patients with Primary Biliary Cholangitis (PBC). This development underlines our commitment to bridging unmet healthcare needs with innovative therapies.”

Primary Biliary Cholangitis (PBC) is a liver disease, caused due to progressive destruction of the bile ducts in the liver which leads to reduction of bile flow – a condition referred to as cholestasis. PBC is often discovered incidentally due to abnormal results on routine liver blood tests. Progression of PBC leads to symptoms of cirrhosis like yellowing of the skin, swelling of legs and feet (edema), ascites, internal bleeding (varices) and thinning of the bones (osteoporosis). The buildup of toxic bile in the liver leads to liver inflammation and fibrosis which can progress to cirrhosis. People with cirrhosis are at increased risk of hepatocellular carcinoma or liver cancer, which is a leading cause of liver transplants or death.

With an increasing number of people being affected by PBC which can lead to progressive cholestasis and even turn fatal, there is a pressing need to develop therapies which help to achieve an adequate reduction in alkaline phosphotase (ALP) or bilirubin and bring in better tolerance and efficacy.

About Lipaglyn™ Lipaglyn™ is a prescription drug authorized for sale in India only. Lipaglyn™ was launched in India during Sept 2013 for the treatment of Hypertriglyceridemia and Diabetic Dyslipidemia in Patients with Type 2 Diabetes not controlled by statins. Saroglitazar Mg is an investigational new drug with the USFDA, and is currently under clinical investigation for three significant unmet medical needs in the United States – Primary Biliary Cholangitis (PBC), Non-alcoholic Steatohepatitis (NASH) and Severe Hypertriglyceridemia (TG>500).

About Zydus Zydus Cadila is an innovative, global healthcare provider that discovers, develops, manufactures and markets a broad range of healthcare therapies, including small molecule drugs, biologic therapeutics and vaccines. The group employs over 19,500 people worldwide, including 1200 scientists engaged in R & D, and is dedicated to creating healthier communities globally. For more information, please visit http://www.zyduscadila.com

http://zyduscadila.com/wp-content/uploads/2017/02/USFDA-approval-for-clinical-trial-of-Saro-Mg.pdf

Image result for Saroglitazar Magnesium

Image result for Saroglitazar Magnesium

Saroglitazar magnesium
CAS: 1639792-20-3

Molecular Formula, 2C25-H28-N-O4-S.Mg,

Molecular Weight, 901.4354

Magnesium, bis((alphaS)-alpha-(ethoxy-kappaO)-4-(2-(2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-1-yl)ethoxy)benzenepropanoato-kappaO)-, (T-4)-

(2S)-2-Ethoxy-3-(4-(2-(2-methyl-5-(4-(methylsulfanyl)phenyl)-1H-pyrrol-1-yl(ethoxy)phenyl)propanoic acid, magnesium salt (2:1)

Image result for RANJIT DESAI ZYDUS

DR RANJIT DESAI

ZYDUS

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//////////Zydus,  USFDA, Phase II,  clinical studies, Saroglitazar Magnesium,  Primary Biliary Cholangitis,  (PBC)

[Mg+2].CCO[C@@H](Cc1ccc(OCCn2c(C)ccc2c3ccc(SC)cc3)cc1)C(=O)[O-].CCO[C@@H](Cc4ccc(OCCn5c(C)ccc5c6ccc(SC)cc6)cc4)C(=O)[O-]

Saroglitazar magnesium….New patent WO 2015029066 Cadila Healthcare Ltd


SAROGLITAZAR
Saroglitazar skeletal.svg

WO  2015029066

Dwivedi, Shri Prakash Dhar; Singh, Ramesh Chandra; Patel, Vikas; Desai, Amar Rajendra

Cadila Healthcare Ltd

Polymorphic form of pyrrole derivative and intermediate thereof

The present invention relates to Saroglitazar free acid of Formula (IA) or its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable esters, stereoisomers, tautomers, analogs and derivs. thereof. The present invention also provides an amorphous form of saroglitazar free acid and processes of prepn. thereof. The present invention also provides pharmaceutical compn. comprising an amorphous form saroglitazar magnesium.

Amorphous forms of saroglitazar free acid and its salt form are claimed. Also claims the process for the synthesis the same compound. Useful for treating obesity, hyperlipidemia and hypercholesteremia. Picks up from WO2015011730, claiming the stable composition comprising saroglitazar magnesium or its derivatives. Zydus-Cadila has developed and launched saroglitazar for treating diabetic dyslipidemia and hypertriglyceridemia.

In September 2013, saroglitazar was launched for treating dyslipidemia and hypertriglyceridemia.

As of March 2015, Zydus-Cadila is developing saroglitazar for treating nonalcoholic steatohepatitis and type II diabetes (both in phase III clainical trials).

Pyrrole derivative of present invention is chemically 2-ethoxy-3-(4-(2-(2-methyl- 5-(4-(methylthio)phenyl)-lH-pyrrol-l-yl)ethoxy)ph’enyl)propanoate, which may be optically active or racemic and its pharmaceutically acceptable salts, hydrates, solvates, polymorphs or intermediates thereof. The INN name for pyrrole derivative is Saroglitazar® which is magnesium salt of pyrrole compound o f saroglitazar,

 

the process comprising: 5WO 2015/029066 PCT/IN2014/000551 (a) dissolving saroglitazar magnesium of Formula (I) in one or more organic solvents to obtain a solution, (b) adding the solution in one or more o f anti-solvent at temperature from about -80°C to about 150°C to obtain saroglitazar magnesium o f Formula (I); and (c) obtaining the amorphous saroglitazar magnesium by removal of anti-solvent.

 

Example-1: Preparation of saroglitazar magnesium (Ί) In a 5 Liter three necked round bottom flask equipped with nitrogen atmosphere facility, mechanical stirrer, thermometer and an addition funnel, 2-ethoxy-3-(4-hydroxy-phenyl)- propionic acid ethyl ester (A) (100.0 g) and cyclohexane (1300.0 ml) were charged and reaction mixture was heated to 45° to 55°C. Potassium carbonate (58.0 g) was added and stirred for 30 min. methanesulfonic acid 2-[2-methyl-5-(4-methyIsulfanyl-phenyl)-pyrroll-yl]-ethyl ester (A l) (150.24 g) and THF (200.0 ml) were added and heated to 75°C to 85°C for 36 hour. The reaction mixture was cooled to 25° to 35°C and water (1000.0 ml) was added and stirred for 15 min. The separated aqueous layer was treated with cyclohexane (200.0 ml) and stirred for 15 min. The organic layers were combined and washed with caustic solution (600.0 ml). The separated organic layer was washed with water (600.0 ml) and characoalized with (5.0 g) charcoal and stirred for 30 min and filtered. The filtrate was distilled to remove cyclohexane and the residue was collected (residue-A). The residue-A as obtained was treated with ethanol (400.0 ml) and stirred for 15 min. Sodium hydroxide 20.14 g solution in water (200.0 ml) was added and the reaction mixture was stirred for 3 hours. The reaction mixture was diluted with water (1800.0 ml) and stirred for 15 min. The separated aqueous layer was washed with n-butyl acetate. The separated aqueous layer was added magnesium acetate tetrahydrate solution (90.0 g) in water (100.0 ml) and stirred for I hour. The aqueous layer was extracted with methylene dichloride (200 ml). The separated organic layer was washed with sodium chloride solution and charcoalized. The charcoalized solution was filtered and filtrate was distilled to remove methylene dichloride completely. The residue was diluted with methylene dichloride (1000 ml) and stirred for 30 min. The organic solution was added into n-heptane (1500 mL) and stirred for 3 hours. The product was filtered and washed with n-heptane and dried in vacuum tray dryer at 25°C to 30°C for 3 hours. The product was sieved through 0.5 mm sieve and milled through jet-milled. The product was further dried in vacuum tray drier at 40°C to 50°C for 6 hours followed by drying at 55°C to 65°C for 40 hours to obtain substantially amorphous saroglitazar magnesium (I). The compound is characterized by x-ray power diffraction (FIG.I).

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WO/2015/011730

 https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2015011730

The present invention relates to the stable pharmaceutical composition of a suitable hypolipidemic agent. Preferably, the present invention discloses novel formulations of the compound of formula (I), or pharmaceutically acceptable salts of compounds of formula (I). More particularly the present invention relates to the stable pharmaceutical composition of compounds of formula (I) comprising compounds of formula (I) or its pharmaceutically acceptable salts, wherein the pH of the formulation is maintained above 7. formula (I)

 

 

front page image

The compounds of formula (I) are new synthetic compounds having hypolipidemic activity. The compounds of formula (I) are used primarily for triglyceride lowering, with concomitant beneficial effect on glucose lowering and cholesterol lowering.

The structural formula of compounds of formula (I) is shown below.

wherein ‘R’ is selected from hydroxy, hydroxyalkyl, acyl, alkoxy, alkylthio, thioalkyl, aryloxy, arylthio and M+ represents suitable metal cations such as Na+, K+, Ca+2, Mg+2 and the like. Preferably, R is selected from alkylthio or thioalkyl groups; most preferably R represents -SCH3.The Mg+2 salt is preferred. The compounds of formula (I) are generally insoluble in water, but freely soluble in dimethyl sulfoxide, dichloromethane & slightly soluble in methanol and IPA.

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see also my full fledged article on its synthesis

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

 

see also my full fledged article on its synthesis

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

 

see also my full fledged article on its synthesis

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

 

see also my full fledged article on its synthesis

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

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