ENZALUTAMIDE

New Drug Approvals

Enzalutamide, MDV-3100

MDV3100 is an orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. MDV3100 (Enzalutamide) blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. It also induces tumour cell apoptosis, and has no agonist activity. Early preclinical studies also suggest that MDV3100 inhibits breast cancer cell growth.

1H NMR FROM THE NET

1H NMR PREDICT AND 13 C NMR PREDICT BELOW

COSY PREDICT

Synthesis pics

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PATENT
http://www.google.com/patents/WO2015063720A1?cl=en

Enzalutamide is chemically described as 4-{3-[4-cyano-3-(trifluoromethyl)phenyl] -5 ,5 -dimethyl-4-oxo-2-sulfanylideneimidazolidin- 1 -yl } -2-fluoro-N-methylbenzamide of Formula I.

FORMULA I

Processes for the preparation of enzalutamide are described in U.S. Publication Nos. 2007/0004753 and 2007/0254933 and PCT Publication Nos. WO 2007/127010, WO 2006/124118, and WO 2011/106570.

PCT Publication No. WO 2011/106570 discloses that the processes described in U.S. Publication Nos. 2007/0004753 and 2007/0254933 result in a…

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Golden Root (Rhodiola rosea)…….a queen of adaptogenic herbs

New Drug Approvals

 Golden Root (Rhodiola rosea) – Also called Arctic Root or Roseroot, golden root is considered a queen of adaptogenic herbs. As one blogger puts it, “[Golden root] allows us to regulate our immune, physiological and neurological responses to stress, allowing us to survive not only rough environmental/weather challenges, but also to adapt and adjust our often neurotic mental habits and crazy social/political climates as well.

”The Russians use it to improve physical stamina and adapt to environmental stress. In Siberia, people still say, “Those who drink Rhodiola tea will live more than 100 years old.” The extract possesses positive mood enhancing and anti-stress properties with no detectable levels of toxicity. Golden root works by enhancing the body’s ability to make serotonin, dopamine, and other neurotransmitters that aid in happiness and stress-reduction.

Rhodiola rosea (commonly golden root, rose root, roseroot, Aaron’s rod, arctic root, king’s crown, lignum rhodium, orpin rose) is…

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Gotu Kola (Centella asiatica), this herb is known for calming depressive episodes, strengthening cognitive function, and helping one deal with both mental and physical stress

New Drug Approvals

Gotu Kola (Centella asiatica) – An antiseptic, antispasmodic, peripheral vasodilator, and nerving and relaxant, this herb is known for calming depressive episodes, strengthening cognitive function, and helping one deal with both mental and physical stress.

Centella asiatica, commonly known as centella and gotu kola, is a small, herbaceous, annual plant of the family Mackinlayaceae or subfamily Mackinlayoideae of family Apiaceae, and is native to wetlands in Asia.^[2][3] It is used as a medicinal herb in Ayurvedic medicine,traditional African medicine, and traditional Chinese medicine. It is also known as the Asiatic pennywort or Indian pennywort in English, among various other names in other languages.

Description

Centella grows in tropical swampy areas.^[4] The stems are slender, creeping stolons, green to reddish-green in color, connecting plants to each other. It has long-stalked, green, reniform leaves with rounded apices which have smooth texture with palmately netted…

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Oat Straw (Avena sativa) helpful in calming the nerves of those who are detoxing from drug or alcohol addiction, and can even help curb nicotine cravings.

New Drug Approvals

Oat Straw (Avena sativa) – Not only can this herb effectively treat anxiety, it is also used to treat migraines, shingles, fatigue, and even epilepsy. This herb can be especially helpful in calming the nerves of those who are detoxing from drug or alcohol addiction, and can even help curb nicotine cravings.

Avena Sativa – Oats Benefits

Are you feeling stressed, tired, depressed, fed-up, run down or even lacking your usual sexual desire? If so, have you considered a daily dose of Avena sativa (also known as Oats or Oatstraw)?

This wonderful herb is thought to be soothing to the brain and nervous system, whilst at the same time increasing sexual desire, and performance, in both men and women!

Avena sativa is quickly becoming a popular natural alternative to pharmaceutical erection enhancers without the dangerous side effects. Also known as Oats Milky Seed or Oatstraw, Avena Sativa is used to stimulate both men…

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Mom will teach you NMR

New Drug Approvals

Dedicated to all moms in the world

ETHYL PROPIONATE NMR, carbonyl is dad and oxygen mom, a methyl gets more attention

ORIGINALLY IN http://orgspectroscopyint.blogspot.in/2014/07/ethyl-propionate-nmr-carbonyl-is-dad.html

C=O group is dad

O atom is mom

Carbonyl is dad and oxygen mom hence c labelled methyl has higher chemical shift  and gets a little more attention

SEE BELOW

NMR IS EASY

A chemical has Formula: C₅H₁₀O₂

C₅H₁₀O₂
Rule 2, omit O, gives C₅H₁₀
5 – 10/2 + 1 = 1 degree of unsaturation.
Look for 1 pi bond or aliphatic ring.

IR

The band at 1740 indicates a carbonyl, probably a saturated aliphatic ester. The bands at 3000-2850 indicate C-H alkane stretches. The bands in the region 1320-1000 could be due to C-O stretch, consistent with an ester.

 Structure answer

This is the structure. See if you can assign the peaks on your…

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How To Treat Migraines With Red Raspberry Leaf

New Drug Approvals

http://www.selfsufficiencymagazine.com/how-to-treat-migraines-with-red-raspberry-leaf/

If you, or someone close to you, suffers from migraines then you’ll know just how frustrating it can be. You can try all sorts of approaches and conventional medications, but often they don’t work!

Why not try some red raspberry leaf tea? It’s packed full of essential vitamins and minerals and is widely used for helping to cure those painful headaches.

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Social Media in Pharma: Should you bother?….Genericpharma

New Drug Approvals

Social Media in Pharma: Should you bother?

http://links.genericpharma20.mkt6146.com/servlet/MailView?ms=NjY5NjcyNQS2&r=NTEzNjM3NjI3NDgS1&j=NDYyOTA1OTY2S0&mt=2&rj=NDYyOTA1OTY1S0&rt=0

Generic Pharma 2.0
Our mailing address is: 12 Dunlop Street E.

Barrie, Ontario L4M 1A3

info@genericpharma20.com

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XenoPort begins phase II trial of XP-23829 in patients with psoriasis

New Drug Approvals

XP 23829  from Xenoport is an interesting molecule and as on 27 July 2014, I did not find conclusive evidence

See some structures below

Not sure about the structure of XP 23829

OR

Best fit

OR

Not sure?

(N,N-dimethylcarbamoyl)methyl methyl(2E)but-2-ene-1,4-dioate.

OR

I AM NOT SURE ABOUT THIS ONE ALSO????????

As Football worldcup2014 goes on in Brazil

A thought for it is due…………

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Best fit is probably is as shown below, and there are reasons

(N,N- Diethylcarbamoyl)methyl methyl (2E)but-2-ene-l,4-dioate 

Introduction

(N,​N-​Diethylcarbamoyl)​methyl methyl (2E)​-​but-​2-​ene-​1,​4-​dioate

As per patent……..http://www.google.com/patents/WO2014031844A1?cl=en

C₁₁ H₁₇ N O_{5, mw 243.13}

M.p.: 53-56 °C.

¹ H NMR (CDCI₃, 400 MHz): δ 6.99-6.90 (m, 2H), 4.83 (s, 2H), 3.80 (s, 3H), 3.39 (q, J = 1.1 Hz, 2H), 3.26 (q, J = 7.2 Hz, 2H), 1 .24 (t, J = 7.2 Hz, 3H), 1 .14 (t, J = 7.2 Hz, 3H). MS (ESI): m/z…

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API SCALEUP (R AND D)

New Drug Approvals

The ultimate goal of drug synthesis is to scale up from producing milligram quantities in a laboratory to producing kilogram to ton quantities in a plant, all while maintaining all at http://www.allfordrugs.com/api-scaleup-r-and-d/

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Cocrystals

New Drug Approvals

Active pharmaceutical ingredients (APIs) are frequently delivered to the patient in the solid state as part of such dosage forms as tablets, capsules, etc.In this context the ability to deliver the drug to the patient in a safe, efficacious and cost-effective way depends largely on the physicochemical properties of the APIs in the solid state, and ……..read more

http://www.allfordrugs.com/cocrystals/

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