Sunday 29 September 2013

ONE LAKH VIEWS ON ALL MY BLOGS--DR ANTHONY CRASTO


DR ANTHONY MELVIN CRASTO Ph.D

WORLDDRUGTRACKER
ANNOUNCING ONE LAKH PLUS VIEWS ON ALL BLOGS- DR ANTHONY CRASTO
SEE ALSO
DR ANTHONY MELVIN CRASTO, Worlddrugtracker, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his PhD from ICT ,1991, Mumbai, India, in Organic chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK- GENERICS LTD, Research centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Prior to joining Glenmark, he worked with major multinationals like Hoechst Marion Roussel, now sSanofi, Searle India ltd, now Rpg lifesciences, etc. he is now helping millions, has million hits on google on all organic chemistry websites. His New Drug Approvals, Green Chemistry International, Eurekamoments 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 25 year tenure, good knowledge of IPM, GMP, Regulatory aspects, he has several international drug patents published worldwide . He gas good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, polymorphism etc He suffered a paralytic stroke in dec 2007 and is bound to a wheelchair, this seems to have injected feul in him to help chemists around the world, he is more active than before and is pushing boundaries, he has one lakh connections on all networking sites, He makes himself available to all, contact him on +91 9323115463, amcrasto@gmail.com

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The Potential of Triterpenoids in the Treatment of Melanoma » All About Drugs

The Potential of Triterpenoids in the Treatment of Melanoma » All About Drugs:

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Thursday 26 September 2013

A Case of Idiopathic Pulmonary Hypertension


future--------------TYROSINE KINASE INHIBITORS CINACIGUAT,RIOCIGUAT-ACTIVATORS OF GUANYLYL CYCLASE

Primary pulmonary hypertension


FDA grants two orphan drug designations for Bayer's Riociguat


File:Riociguat structure.svg
Riociguat
Bayer HealthCare Pharmaceuticals, a subsidiary of Bayer, has obtained two separate orphan drug designations from the US Food and Drug Administration's (FDA) Office of Orphan Products Development for its investigational, oral medication riociguat, proposed trade name Adempas.

read all at
http://regulatoryaffairs.pharmaceutical-business-review.com/news/fda-grants-two-orphan-drug-designations-for-bayers-riociguat-260913
Riociguat (BAY 63-2521) is a novel drug that is in clinical development by Bayer. It is a stimulator of soluble guanylate cyclase(sGC). At the moment Phase III clinical trials investigate the use of riociguat as a new approach to treat two forms of pulmonary hypertension (PH): chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). Riociguat constitutes the first drug of a novel class of sGC stimulators.
The first nitric oxide (NO) independent, haem-dependent sGC stimulator YC-1, a synthetic benzylindazole derivative, was described in 1978. The characterisation 20 years later demonstrated that as well as increasing sGC activity, YC-1 acted in synergy with NO to stimulate sGC. However, YC-1 was a relatively weak vasodilator and had side effects. Therefore, the search began for novel indazole compounds that were more potent and more specific sGC stimulators. The result was the identification of BAY 41-2272 and BAY 41-8543. Both compounds were tested in various preclinical studies on different animal models and appeared to improve systemic arterial oxygenation. To improve the pharmacologic and pharmacokinetic profile an additional 1000 compounds were screened leading to the discovery of riociguat. Riociguat was tested in mouse and rat disease models, where it effectively reduced pulmonary hypertension and reversed the associated right heart hypertrophy and ventricular remodelling.
Several clinical trials have been undertaken to investigate and evaluate diverse aspects of riociguat and some of them are still ongoing

Riociguat (BAY 63-2521), N-[4,6-Diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl]-N-methylcarbamic acid methyl ester, is a soluble guanylate cyclase stimulator. Riociguat is under investigation for the treatment of chronic thromboembolic pulmonary hypertension, and pulmonary arterial hypertension. Michelakis et al., Eur. Respir. J., 2009, 33(4), 717-21; Ghofrani et al., Eur. Respir. Rev., 2009, 18(111), 35-41; Mittendorf et al., ChemMedChem,2009, 4, 853-65; and WO 2006037491. 

Riociguat has also shown promise in treating hypertension, angina pectoris, heart failure, atherosclerosis, thromboembolism, platelet activation, asthma, bronchoconstriction, chronic obstructive pulmonary disease, pulmonary vasoconstriction, acute respiratory distress syndrome, cerebral autosomal dominant arteriopathy with subcortical infarcts and leukoencephalopathy, cerebrovascular disorders, cerebrovasospasm, transient ischemic attacks, stroke, migraine, migraine with vertigo, genitourinary disorders, benign prostate syndrome, benign prostate hyperplasia, benign prostate enlargement, urinary incontinence, bladder outlet obstruction, neurogenic bladder syndrome, pelvic pain, prostate hypertrophy, sexual dysfunction, 
Raynaud's phenomenon, increased cellular proliferation, endothelial dysfunction, erectile dysfunction wounds, scarring, fibrotic disorders, renal disorders, renal failure, renal hypertension, idiopathic pulmonary fibrosis, non-alcoholic hepatosteatosis, hepatitis, diabetic nephropathy, hypercholesterolemia, osteoporosis, optic nerve damage, and glaucoma. 
Gur et al., Curr. Pharm. Design., 2010, 16, 1619-33; WO 2010081647; WO 2008138483; WO 2007009607; US 20070225299; US 20090215769; US 20090221573; and U.S. Pat. No. 7,173,037.
Figure US20110201626A1-20110818-C00002

Adverse effects associated with riociguat include headache, nasal congestion, flushing, overheating sensation, orthostatic hypotension, and heart palpitations.

SIMPONI® Receives European Commission Approval for Treatment of Moderately to Severely Active Ulcerative Colitis » All About Drugs

SIMPONI® Receives European Commission Approval for Treatment of Moderately to Severely Active Ulcerative Colitis » All About Drugs:

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Wednesday 25 September 2013

Turmeric Extract 100% Effective At Preventing Type 2 Diabetes, ADA Journal Study Finds » All About Drugs

Turmeric Extract 100% Effective At Preventing Type 2 Diabetes, ADA Journal Study Finds » All About Drugs:

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Takeda Gets Simultaneous EU OKs for Three Type 2 Diabetes Therapies » All About Drugs

Takeda Gets Simultaneous EU OKs for Three Type 2 Diabetes Therapies » All About Drugs:

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API SCALEUP (R AND D) » All About Drugs

API SCALEUP (R AND D) » All About Drugs:

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Isolation and Structural Elucidation of Novel Isomeric Process Related Impurities of Zolmitriptan » All About Drugs

Isolation and Structural Elucidation of Novel Isomeric Process Related Impurities of Zolmitriptan » All About Drugs:

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Purdue Pharma L.P. Receives FDA Approval For 15 mcg/hour Dosage Strength Of Butrans (buprenorphine) Transdermal System CIII « New Drug Approvals

Purdue Pharma L.P. Receives FDA Approval For 15 mcg/hour Dosage Strength Of Butrans (buprenorphine) Transdermal System CIII « New Drug Approvals:

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Glaxo Gets EU OK for New Revolade Indication « New Drug Approvals

Glaxo Gets EU OK for New Revolade Indication « New Drug Approvals:

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EMCURE-A SUCESS STORY « New Drug Approvals

EMCURE-A SUCESS STORY « New Drug Approvals:

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Tuesday 24 September 2013

Reliance Life Sciences taps cancer drug market in India

September 23, 2013 3:50 am by 
Cancer gene testing
MUMBAI -- Reliance Life Sciences Pvt. Ltd has introduced six anti-cancer drug brands in India, including a generic version of Swiss drugmaker Novartis AG's anti-blood cancer drug Glivec, as it seeks to tap the fast-growing market for oncology drugs in the country.


Read more: http://medcitynews.com/2013/09/reliance-life-sciences-taps-cancer-drug-market-india/#ixzz2fnylGOub

Greening the Valsartan Synthesis: Scale-up of Key Suzuki–Miyaura Coupling over SiliaCat DPP-Pd « New Drug Approvals

Greening the Valsartan Synthesis: Scale-up of Key Suzuki–Miyaura Coupling over SiliaCat DPP-Pd « New Drug Approvals:

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Greening the Valsartan Synthesis: Scale-up of Key Suzuki–Miyaura Coupling over SiliaCat DPP-Pd « New Drug Approvals

Greening the Valsartan Synthesis: Scale-up of Key Suzuki–Miyaura Coupling over SiliaCat DPP-Pd « New Drug Approvals:

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Nanomedicine » All About Drugs

Nanomedicine » All About Drugs:

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Antibiotic Resistance » All About Drugs

Antibiotic Resistance » All About Drugs:

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Combinatorial Chemistry in Drug Design « New Drug Approvals

Combinatorial Chemistry in Drug Design « New Drug Approvals:

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Bioavailability « New Drug Approvals

Bioavailability « New Drug Approvals:

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EFAVIRENZ – Huahai Pharma China-Approved to Produce AIDS Treatment « New Drug Approvals

EFAVIRENZ – Huahai Pharma China-Approved to Produce AIDS Treatment « New Drug Approvals:

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Stelara (ustekinumab) Receives FDA Approval to Treat Active Psoriatic Arthritis « New Drug Approvals

Stelara (ustekinumab) Receives FDA Approval to Treat Active Psoriatic Arthritis « New Drug Approvals:

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Glenmark receives final ANDA approval for Desoximetasone Ointment USP, 0.25% « New Drug Approvals

Glenmark receives final ANDA approval for Desoximetasone Ointment USP, 0.25% « New Drug Approvals:

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Health Canada Approves Bayer’s Hypertension Drug » All About Drugs

Health Canada Approves Bayer’s Hypertension Drug » All About Drugs:

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Roche Gets Breakthrough Status for Lung Cancer Drug » All About Drugs

Roche Gets Breakthrough Status for Lung Cancer Drug » All About Drugs:

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Saturday 21 September 2013

VITAMINS, COMMON INFORMATION


A vitamin (US /ˈvtəmɪn/ or UK /ˈvɪtəmɪn/) is an organic compound required by an organism as a vital nutrient in limited amounts. An organic chemical compound (or related set of compounds) is called a vitamin when it cannot be synthesized in sufficient quantities by an organism, and must be obtained from the diet. Thus, the term is conditional both on the circumstances and on the particular organism. For example, ascorbic acid (vitamin C) is a vitamin for humans, but not for most other animals, and biotin (vitamin H) and vitamin D are required in the human diet only in certain circumstances.





Thiamin
What it does:
  • helps convert the food we eat to the energy we need
Foods that have thiamin:
  • spinach, tomato juice, watermelon, sunflower seeds, ham
Deficiency problems:
  • weakness, tingling in feet and hands, poor coordination
Thiamin
Riboflavin - named for its yellow color (flavus means yellow in Latin)
What it does:
  • helps convert the food we eat to the energy we need
Foods that have riboflavin:
  • milk, cheese, liver, broccoli, asparagus, spinach
Deficiency problems:
  • eye disorders, cracks at corners of mouth, swollen tongue
riboflavin
Niacin
What it does:
  • helps our body use the fat and sugar we eat for energy
  • helps keep our skin healthy
Foods that have niacin:
  • mushrooms, tuna, green beans, broccoli, spinach, breakfast cereals
Deficiency problems:
  • diarrhea, skin problems, mental disorientation
niacin
Vitamin B6
What it does:
  • helps make red blood cells
  • helps our body use the fat and protein we eat for energy
Foods that have vitamin B6:
  • spinach, broccoli, tomato juice, banana, watermelon, chicken breast
Deficiency problems:
  • headache, convulsions, vomiting, flaky skin, sore tongue
b6
Folate
What it does:
  • helps to make new cells
  • helps prevent heart disease
Foods that have folate:
  • asparagus, broccoli, corn flakes, green beans, tomato juice, beans
Deficiency problems:
  • diarrhea, mental disorders, poor growth
folate
Vitamin B12
What it does:
  • helps to make new cells
Foods that have vitamin B12:
  • meat, fish, poultry, milk, cheese, eggs
Deficiency problems:
  • anemia, poor nerve function
b12
Vitamin C- almost all animals make vitamin C in their bodies (only humans, guinea pigs, some bats, and some fish don't)vitamin c
What it does:
  • protects cells from damage
  • helps keep bones and skin healthy
  • may help prevent cancer and heart disease
Foods that have vitamin C:
  • oranges, strawberries, peppers, kiwi, brussel sprouts, broccoli, spinach
Deficiency problems:
  • bleeding gums, tiredness, weakness, sore muscle








Vitamin A - discovered in 1913
What it does:
  • helps with eyesight
  • keeps skin healthy
  • helps with growth of body organs (like bones)
Foods that have vitamin A:
  • liver, fish, milk, butter, eggs, carrots
Deficiency problems:
  • night blindness, poor growth, dry skin
vitamin a
Vitamin D - made in the skin by the sun
What it does:
  • helps bones grow strong
Foods that have vitamin D:
  • egg yolks, liver, butter, milk
Deficiency problems:
  • rickets (deformed bones), weak bones
vitamin d
Vitamin E - called the antiaging vitamin
What it does:
  • protects lungs against pollution damage
  • helps keep heart healthy
  • may help protect against cancer
Foods that have vitamin E:
  • sweet potatoes, peanut butter, sunflower seeds, spinach, nuts
Deficiency problems:
  • nerve destruction, red blood cell destruction
vitamin e
Vitamin K - made by bacteria in our intestines
What it does:
  • helps make blood clot
  • helps keep bones healthy
Foods that have vitamin K:
  • liver, cabbage, lettuce, spinach, milk, meat, eggs
Deficiency problems:
  • hemorrhage
vitamin k
..........
By convention, the term vitamin includes neither other essential nutrients, such as dietary mineralsessential fatty acids, or essential amino acids (which are needed in larger amounts than vitamins) nor the large number of other nutrients that promote health but are otherwise required less often. Thirteen vitamins are universally recognized at present.
Vitamins are classified by their biological and chemical activity, not their structure. Thus, each "vitamin" refers to a number of vitamer compounds that all show the biological activity associated with a particular vitamin. Such a set of chemicals is grouped under an alphabetized vitamin "generic descriptor" title, such as "vitamin A", which includes the compounds retinalretinol, and four known carotenoids. Vitamers by definition are convertible to the active form of the vitamin in the body, and are sometimes inter-convertible to one another, as well.
itamins have diverse biochemical functions. Some, such as vitamin D, have hormone-like functions as regulators of mineral metabolism, or regulators of cell and tissue growth and differentiation (such as some forms of vitamin A). Others function as antioxidants (e.g., vitamin E and sometimesvitamin C). The largest number of vitamins, the B complex vitamins, function as precursors for enzyme cofactors, that help enzymes in their work as catalysts in metabolism. In this role, vitamins may be tightly bound to enzymes as part of prosthetic groups: For example, biotin is part of enzymes involved in making fatty acids. They may also be less tightly bound to enzyme catalysts as coenzymes, detachable molecules that function to carry chemical groups or electrons between molecules. For example, folic acid may carry methylformyl, and methylene groups in the cell. Although these roles in assisting enzyme-substrate reactions are vitamins' best-known function, the other vitamin functions are equally important.

Until the mid-1930s, when the first commercial yeast-extract vitamin B complex and semi-synthetic vitamin C supplement tablets were sold, vitamins were obtained solely through food intake, and changes in diet (which, for example, could occur during a particular growing season) usually greatly altered the types and amounts of vitamins ingested. However, vitamins have been produced as commodity chemicals and made widely available as inexpensive semisynthetic and synthetic-source multivitamin dietary and food supplements and additives, since the middle of the 20th century.,,,,,,,

List of vitamins

Each vitamin is typically used in multiple reactions, and, therefore, most have multiple functions.

Vitamin generic
descriptor name
Vitamerchemical name(s) (list not complete)SolubilityRecommended dietary allowances
(male, age 19–70)[6]
Deficiency diseaseUpper Intake Level
(UL/day)[6]
Overdose diseaseFood sources
Vitamin ARetinolretinal, and
four carotenoids
including beta carotene
Fat900 µgNight-blindness,Hyperkeratosis, andKeratomalacia[7]3,000 µgHypervitaminosis AOrange, ripe yellow fruits, leafy vegetables, carrots, pumpkin, squash, spinach, liver, soy milk, milk
Vitamin B1ThiamineWater1.2 mgBeriberiWernicke-Korsakoff syndromeN/D[8]Drowsiness or muscle relaxation with large doses.[9]Pork, oatmeal, brown rice, vegetables, potatoes, liver, eggs
Vitamin B2RiboflavinWater1.3 mgAriboflavinosisN/DDairy products, bananas, popcorn, green beans, asparagus
Vitamin B3NiacinniacinamideWater16.0 mgPellagra35.0 mgLiver damage (doses > 2g/day)[10] and other problemsMeat, fish, eggs, many vegetables, mushrooms, tree nuts
Vitamin B5Pantothenic acidWater5.0 mg[11]ParesthesiaN/DDiarrhea; possibly nausea and heartburn.[12]Meat, broccoli, avocados
Vitamin B6Pyridoxine,pyridoxamine,pyridoxalWater1.3–1.7 mgAnemia[13] peripheral neuropathy.100 mgImpairment ofproprioception, nerve damage (doses > 100 mg/day)Meat, vegetables, tree nuts, bananas
Vitamin B7BiotinWater30.0 µgDermatitisenteritisN/DRaw egg yolk, liver, peanuts, certain vegetables
Vitamin B9Folic acidfolinic acidWater400 µgMegaloblastic anemiaand Deficiency during pregnancy is associated with birth defects, such as neural tube defects1,000 µgMay mask symptoms of vitamin B12 deficiency;other effects.Leafy vegetables, pasta, bread, cereal, liver
Vitamin B12Cyanocobalamin,hydroxycobalamin,methylcobalaminWater2.4 µgMegaloblastic anemia[14]N/DAcne-like rash [causality is not conclusively established].Meat and other animal products
Vitamin CAscorbic acidWater90.0 mgScurvy2,000 mgVitamin C megadosageMany fruits and vegetables, liver
Vitamin DCholecalciferolFat10 µg[15]Rickets andOsteomalacia50 µgHypervitaminosis DFish, eggs, liver, mushrooms
Vitamin ETocopherols,tocotrienolsFat15.0 mgDeficiency is very rare; mild hemolytic anemiain newborn infants.[16]1,000 mgIncreased congestive heart failure seen in one large randomized study.[17]Many fruits and vegetables, nuts and seeds
Vitamin Kphylloquinone,menaquinonesFat120 µgBleeding diathesisN/DIncreases coagulation in patients taking warfarin.[18]Leafy green vegetables such as spinach, egg yolks, liver