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Showing posts with label India. Show all posts
Showing posts with label India. Show all posts

Thursday, 13 October 2016

Register Today for the ACS Symposium in India on Recent Advances in Drug Development, 11-12 November 2016 in Hyderabad, India


Inaugural ACS Industry Symposium, 11-12 November 2016 in Hyderabad, India

Recent Advances in Drug Development

Register Today for the ACS Symposium in India on Recent Advances in Drug Development
To view this email as a web page, go here.
Register now for the inaugural ACS Industry Symposium, 11-12 November 2016 in Hyderabad, India. Be sure to secure your seat today as rates will increase on 27 October!

The theme of the Symposium is Recent Advances in Drug Development. The event will feature lectures by the world's leading researchers and experts in the pharma industry, including:
  • Dr. Peter Senter of Seattle Genetics
  • Dr. Jagath Reddy Junutula of Cellerant Therapeutics, Inc.
  • Dr. Ming-Wei Wang of the Shanghai Institute of Materia Medica, Chinese Academy of Sciences
This is an exclusive event being organized in partnership with Dr. Reddy's Laboratories for pharma professionals throughout India. Space is limited so register today!
Please visit our website to learn more about the speakers and the program.
Register today to ensure your access to the ACS Industry Symposium. We look forward to seeing you in Hyderabad in November.
2540 Olentangy River Rd Columbus, OH 43202 US
/////// ACS Symposium, Recent Advances in Drug Development, 11-12 November 2016, Hyderabad, India, dr reddys, cas

Tuesday, 5 April 2016

P7435 from Piramal Enterprises Mumbai, India

Piramal Enterprises Mumbai, India
P-7435; P7435-DGAT1, P7435, P 7435
CAS 1210756-48-1,
C22 H19 F N4 O4 S
L-​Valine, N-​[[3-​[4-​[(6-​fluoro-​2-​benzothiazolyl)​amino]​phenyl]​-​5-​isoxazolyl]​carbonyl]​-
Molecular Weight, 454.47

GDAT1 inhibitor

  • Phase IDiabetes mellitus; Lipid metabolism disorders
  • ClassAntihyperglycaemics; Antihyperlipidaemics; Small molecules
  • Mechanism of ActionDiacylglycerol O acyltransferase inhibitors
Company Piramal Enterprises Ltd.
Description Diacylglycerol O-acyltransferase-1 (DGAT1) inhibitor
Molecular Target Diacylglycerol O-acyltransferase-1 (DGAT1)
Mechanism of Action Diacylglycerol O-acyltransferase-1 (DGAT1) inhibitor
Therapeutic Modality
Latest Stage of Development Phase I
Standard Indication Metabolic (unspecified)
Indication Details Treat metabolic disorders
  • 24 Nov 2014Piramal Enterprises completes a phase I trial in healthy, overweight or obese subjects in USA (NCT01910571)
  • 17 Jun 2014Adverse events and pharmacokinetics data from a phase I trial in healthy male volunteers presented at the 74th Annual Scientific Sessions of the American Diabetes Association (ADA-2014)
  • 17 Jun 2014Pharmacodynamics data from preclinical studies in Dyslipidaemia and obesity presented at the 74th Annual Scientific Sessions of the American Diabetes Association (ADA-2014)

Chairman Ajay Piramal

Swati Piramal-The Vice Chairperson of Piramal Enterprises Ltd

Nandini Piramal, Executive Director, Piramal Enterprises

Piramal Enterprises gets US FDA approval for P7435 IND

Our Bureau, Mumbai
Tuesday, August 06, 2013, 12:25 Hrs  [IST]
Piramal Enterprises Ltd has received US Food and Drug Administration (FDA) approval for its Investigational New Drug (IND) P7435. This is a novel, potent and highly selective, oral diacylglycerolacyltransferase 1 (DGAT1) inhibitor.
P7435 has been developed by the NCE Research Division of PEL for the management of metabolic disorders such as lipid abnormalities and diabetes. It is well-established that increased lipid levels’ (including triglycerides) is one of the major risk factors for cardiovascular disease (CVD). It has been reported by the World Health Organisation, that CVD, is the number one cause of deaths globally, representing approximately 30 per cent of all deaths. Currently, there is a significant medical need for effective and safe drugs for the management of lipid abnormalities and metabolic disorders.
P7435 has demonstrated its lipid lowering potential in various preclinical studies by showing significant reduction in triglyceride levels, glucose and insulin levels,and decrease in food intake and body weight gain -factors which are associated with lipid abnormalities and metabolic disorders.
PEL has established the safety and tolerability of P7435 in a phase I trial recently completed in India. This extension trial in the US will further evaluate the safety and efficacy of P7435 in a larger population.
Dr Swati Piramal, vice chairperson, Piramal Enterprises, said, “The NCE Research division of PEL continues its ambitious diabetes/metabolic disorders programme to discover and develop NCEs to fight against diseases like diabetes and lipid disorders. With P7435 we are looking at addressing a serious need for effective and well-tolerated drugs that treat lipid disorders, which are commonly associated with diabetes and CVDs. Expansion of this trial will allow testing this NCE in a wider population,which is critical to the development of this drug and will provide therapeutic solutions not just to India but also to the rest of the world.”
The NCE Research division of Piramal Enterprises focuses on the discovery and development of innovative small molecule medicines to improve the lives of patients suffering from cancer, metabolic disorders and inflammatory conditions. The key elements of its strategy include capitalizing on Piramal’s strengths, in particular the India advantage, and leveraging external partnerships to achieve high levels of R&D productivity. Piramal’s state-of-the-art Research Centre in Mumbai has comprehensive capabilities spanning target identification all the way through clinical development. Its robust pipeline, including 8 compounds in clinical development, bears testimony to its innovative and rigorous drug discovery process.
European Journal of Medicinal Chemistry (2012), 54, 324-342
WO 2010023609
/////////Piramal Enterprises,  Mumbai, India, P-7435, P7435-DGAT1, P7435, P 7435, GDAT1 inhibitor

CFG 920, Novartis Scientists team up with Researchers at Aurigene, Bangalore, India,



Inhibitor Of Prostate Cancer With Fewer Cardiac Side Effects

Cas 1260006-20-9
Target: CYP17/CYP11B2
Disease: Castration-resistant prostate cancer
MF C14H13ClN4O
MW: 288.0778
Elemental Analysis: C, 58.24; H, 4.54; Cl, 12.28; N, 19.40; O, 5.54
Steroid 17-alpha-hydroxylase inhibitors
CFG920 is a CYP17 inhibitor, is also an orally available inhibitor of the steroid 17-alpha-hydroxylase/C17,20 lyase (CYP17A1 or CYP17), with potential antiandrogen and antineoplastic activities. Upon oral administration, CYP17 inhibitor CFG920 inhibits the enzymatic activity of CYP17A1 in both the testes and adrenal glands, thereby inhibiting androgen production. This may decrease androgen-dependent growth signaling and may inhibit cell proliferation of androgen-dependent tumor cells.
NCT01647789: A Study of Oral CFG920 in Patients With Castration Resistant Prostate Cancer2012 
  • 09 Nov 2015Adverse events, efficacy and pharmacokinetics data from the phase I part of a phase I/II trial in Prostate cancer (Metastatic disease) presented at the 27th AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics (AACR-NCI-EORTC-2015)
  • 29 Jan 2013Phase-I clinical trials in Prostate cancer in Spain (PO)
  • 10 Dec 2012Phase-I clinical trials in Prostate cancer in Canada (PO)
In August 2015, preclinical data were presented at the 250th ACS meeting in Boston, MA. In monkeys, treatment with CFG-920 (3 mg/kg, po) showed good bioavailability with F value of 93%, Tmax of 0.5 h, Cmax of 1382 nM.dn and AUC of 2364 nM.h, while CFG-920 (10 mg/kg, po) showed F value of 183%, Cmax of 1179 nM.dn and Tmax of 1.04 h
Bethany Halford on Twitter: “CFG920 – @Novartis CMOS for …
Bethany Halford on Twitter: “CFG920 – @Novartis CMOS for castration resistant prostate cancer #ACSBoston MEDI 1st disclosures http://t.co/XJJ3tCvpUk”

Novartis is developing CFG-920 (structure shown), an oral CYP17 inhibitor, for the potential treatment of metastatic castration-resistant prostate cancer. In March 2013, a phase I/II trial was initiated and at that time, the study was expected to complete in January 2015; in August 2015, clinical data were presented
2015 250th (August 19) Abs MEDI 341
Discovery of CFG920, a dual CYP17/CYP11B2 inhibitor, for the treatment of castration resistant prostate cancer
American Chemical Society National Meeting and Exposition
Christoph Gaul, Prakash Mistry, Henrik Moebitz, Mark Perrone, Bjoern Gruenenfelder, Nelson Guerreiro, Wolfgang Hackl, Peter Wessels, Estelle Berger, Mark Bock, Saumitra Sengupta, Venkateshwar Rao, Murali Ramachandra, Thomas Antony, Kishore Narayanan, Samiulla Dodheri, Aravind Basavaraju, Shekar Chelur
Novartis-Aurigene team: (from left) Brahma Reddy V, Thomas Antony, Murali Ramachandra, Venkateshwar Rao G, Wesley Roy Balasubramanian, Kishore Narayanan, Samiulla DS, Aravind AB, and Shekar Chelur. Not pictured: Björn Grünenfelder, Saumitra Sengupta, Nelson Guerreiro, Andrea Gerken, Mark Perrone, Mark Bock, Wolfgang Hackl, Henrik Möbitz, Peter Wessels, Christoph Gaul, Prakash Mistry, and Estelle Marrer.
Credit: Aurigene

Preclinical and clinical studies were performed to evaluate the efficacy of CFG-920, a dual cytochrome P450 (CYP)17 and CYP11B2 dual inhibitor, for the potential treatment of castration resistant prostate cancer. CFG-920 showed potent activity against human CYP17 and CYP11B2 enzymes with IC50 values of 0.023 and 0.034 microM, respectively. In monkeys, treatment with CFG-920 (3 mg/kg, po) showed good bioavailability (93%), Tmax of 0.5 h, Cmax of 1382 nM.dn and AUC of 2364 nM.h, while CFG-920 (10 mg/kg, po) showed F value of 183%, Cmax of 1179 nM.dn and Tmax of 1.04 h. In a phase I, first-in-man study, patients received continuous po dosing of CFG-920 (50 mg, bid) plus prednisone (5 mg) in 28-day cycles. At the time of presentation, CFG-920 was under phase II development.
WO 2010149755
Novartis team: (clockwise from left) Wolfgang Hackl, Henrik Möbitz, Peter Wessels, Christoph Gaul, Prakash Mistry, and Estelle Marrer., Credit: Novartis
Prostate cancer is the most commonly occurring cancer in men. Doctors often treat the metastatic stage of the disease by depriving the patient of sex hormones via chemical or surgical castration. But if it progresses far enough, the cancer can survive this therapy, transforming into the castration-resistant form. “Once the cancer becomes castration-resistant, the prognosis is poor,” said Novartis’s Christoph Gaul.
In recent years, CYP17, a bifunctional 17α-hydroxylase/17,20-lyase cytochrome P450 enzyme, has emerged as a target for treating castration-resistant prostate cancer. The enzyme catalyzes the biosynthesis of sex hormones, including testosterone, and blocking it can starve prostate cancer of the androgens it needs to thrive.
Johnson & Johnson’s CYP17 inhibitor, abiraterone acetate (Zytiga), a steroid that binds irreversibly to CYP17, was approved by the Food & Drug Administration in 2011. But Novartis scientists thought they could make a better CYP17 inhibitor, Gaul told C&EN. They teamed up with researchers at Aurigene, in Bangalore, India, and came up with their clinical candidate, CFG920.
Unlike abiraterone, CFG920 isn’t a steroid, and it inhibits CYP17 reversibly. It also reversibly inhibits another cytochrome P450 enzyme, CYP11B2, which is involved in the synthesis of the mineralocorticoids, hormones that regulate cardiac function.
Treating prostate cancer patients by lowering their androgen levels turns out to have negative cardiac side effects: Patients’ lipid metabolism is thrown off and their mineralocorticoid levels jump, leading to increases in blood pressure. Those changes can be stressful for the heart. “If prostate cancer patients don’t die because of the cancer, a lot of times they die because of cardiac disease,” Gaul said.
Because CFG920 also keeps mineralocorticoid levels in check, Novartis is hoping the drug candidate will ameliorate some of the cardiac side effects of inhibiting CYP17. The compound is currently in Phase I clinical trials.
WO 2010149755
Example 58
Prύpιn”ation ofI'(2’ChIoroψ}ri(ibi-^’\l)’3’f4’metMψ}τUin’3’yl)-imiJazoliJin’2’θne (5HA)-
Figure imgf000079_0001
Using the same reaction conditions as in Example 14. 1-(4-methyl-pyridin-3-yl)- itnida/olidin-2-onc ().-.!.4b: 600 mg. 3.3898 mmol) uas reacted with 2-chloro-4-iodo- py.idine (974 mg.4.067 mmol). 1 , 4-dioxane (60 mL). copper iodide (65 mg, 0.3398 mmol), /r<w.v-1.2-diamino cycK)hexane (0.12 ml,, 1.0169 mmol) and potassium phosphate (2.15 g, 10.1694 mmol) to afford 810 mg of the product (83% yield).
1H NMR (C1DCI3. 300 Mi l/): 6 8.5-8.4 (m. 211). 8.3 (d. IH), 7.6-7.5 (m, 2H). 7.2 (S. 111). 4.1-3.9 (ni. 4H), 2.35 <s. 3H)
LCVIS puιϊt>: 90.8%. nι-7 – 289.1 (M M)
HPl C: 97.14%
1: Gomez L, Kovac JR, Lamb DJ. CYP17A1 inhibitors in castration-resistant prostate cancer. Steroids. 2015 Mar;95:80-7. doi: 10.1016/j.steroids.2014.12.021. Epub 2015 Jan 3. Review. PubMed PMID: 25560485; PubMed Central PMCID: PMC4323677.
2: Yin L, Hu Q, Hartmann RW. Recent progress in pharmaceutical therapies for castration-resistant prostate cancer. Int J Mol Sci. 2013 Jul 4;14(7):13958-78. doi: 10.3390/ijms140713958. Review. PubMed PMID: 23880851; PubMed Central PMCID: PMC3742227.
///////CFG-920,  CYP17 inhibitor (prostate cancer), Novartis, CFG 920, Novartis scientists,   team up , researchers ,  Aurigene, Bangalore, India,

Tuesday, 17 November 2015

New route for Expensive drug Ivacaftor synthesis from CSIR-NCL, Pune, India

Cover image for Vol. 2015 Issue 32


Breaking and Making of Rings: A Method for the Preparation of 4-Quinolone-3-carb­oxylic Acid Amides and the Expensive Drug Ivacaftor

  1. N. Vasudevan,
  2. Gorakhnath R. Jachak and
  3. D. Srinivasa Reddy*
Article first published online: 3 NOV 2015
DOI: 10.1002/ejoc.201501048
SUPPORTING INFO……….http://onlinelibrary.wiley.com/store/10.1002/ejoc.201501048/asset/supinfo/ejoc_201501048_sm_miscellaneous_information.pdf?v=1&s=2b5b6ac6456ec88f478c07a692e49254e7239f80


A simple and convenient method to access 4-quinolone-3-carboxylic acid amides from indole-3-acetic acid amides through one-pot oxidative cleavage of the indole ring followed by condensation (Witkop–Winterfeldt type oxidation) was explored. The scope of the method was confirmed with more than 20 examples and was successfully applied to the synthesis of the drug Ivacaftor, the most expensive drug on the market.


N. Vasudevan, Gorakhnath R. Jachak And D. Srinivasa Reddy, Breaking and Making of Rings: A Method for the Preparation of 4-Quinolone-3-carb­oxylic Acid Amides and the Expensive Drug Ivacaftor, Eur. J. Org. Chem., , 0000 (2015), DOI:10.1002/ejoc.201501048.

Breaking and Making of Rings: A Method for the Preparation …

onlinelibrary.wiley.com › … › Early View
6 days ago – European Journal of Organic Chemistry … 20 examples and was successfully applied to the synthesis of the drug Ivacaftor, the most expensive …

European Journal of Organic Chemistry – Wiley Online Library

onlinelibrary.wiley.com › … › European Journal of Organic Chemistry
European Journal of Organic Chemistry ….. examples and is successfully applied to the synthesis of the drug Ivacaftor, the most expensive drug on the market.

Breaking and making – Wiley Online Library

onlinelibrary.wiley.com › … › Early View › Abstract
6 days ago – … for the Preparation of 4-Quinolone-3-carboxylic Acid Amides and the Expensive Drug IvacaftorEuropean Journal of Organic Chemistry.



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
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.
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.
s reddy ncl

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