BENAZEPRIL SYNTHESIS

New Drug Approvals

BENAZEPRIL

CAS NO AS HCl SALT

86541-75-5
Benazepril, brand name Lotensin (Novartis), is a medication used to treat high blood pressure (hypertension), congestive heart failure, and chronic renal failure. Upon cleavage of its ester group by the liver, benazepril is converted into its active form benazeprilat, a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor.
Benazepril, brand name Lotensin, is a medication used to treat high blood pressure (hypertension), congestive heart failure, and chronic renal failure. Upon cleavage of its ester group by the liver, benazepril is converted into its active form benazeprilat, a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor.
The reaction of 2,3,4,5-tetrahydro-1H-(1)benzazepin-2-one (I) with PCl5 in hot xylene gives 3,3-dichloro-2,3,4,5-tetrahydro-1H-(1)benzazepin-2-one (II), which is treated with sodium acetate and reduced with H2 over Pd/C in acetic acid yielding 3-chloro-2,3,4,5-tetrahydro-1H-(1)benzazepin-2-one (III). The reaction of (III) with sodium azide in DMSO affords 3-azido-2,3,4,5-tetrahydro-1H-(1)benzazepin-2-one (IV), which is…

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Sponge molecules isolated and synthesized for drug trials

New Drug Approvals

A structure of PM060184.

By scouring the oceans for disease-fighting molecules, researchers have identified two new anticancer compounds. Isolated from a sea sponge, the compounds represent a new class of the natural products called polyketides, many of which have biological activity. Because it’s not possible to extract sufficient amounts of the molecules from the sponges, the researchers also devised chemical syntheses that allowed them to make enough material to initiate clinical trials on one of the substances,

Cancer Fighters From The Sea

Natural Products: Sponge molecules isolated and synthesized for drug trials.

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http://cen.acs.org/articles/91/i25/Cancer-Fighters-Sea.html

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Novartis First-Generation Lung Cancer Drug Tweaked To Reduce Potential Side Effects

New Drug Approvals

Structures of anaplastic lymphoma kinase inhibitors
IMPROVING A DRUG
Novartis’ first-generation inhibitor of the enzyme anaplastic lymphoma kinase (TAE684, left) formed potentially harmful protein adducts in the body. To reduce side effects, chemists moved the position of a troublesome nitrogen to make the current version of the drug (LDK378, right).
Credit: J. Med. Chem.
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QUINAPRIL

New Drug Approvals

QUINAPRIL HYDROCHLORIDE

Quinapril (marketed under the brand name Accupril by Pfizer) is an angiotensin-converting enzyme inhibitor (ACE inhibitor) used in the treatment of hypertension andcongestive heart failure.

Quinapril inhibits angiotensin converting enzyme, an enzyme which catalyses the formation of angiotensin II from its precursor, angiotensin I. Angiotensin II is a powerfulvasoconstrictor and increases blood pressure through a variety of mechanisms. Due to reduced angiotensin production, plasma concentrations of aldosterone are also reduced, resulting in increased excretion of sodium in the urine and increased concentrations ofpotassium in the blood.

  • The condensation of alanine tert-butyl ester (I) with ethyl 2-bromo-4-phenylbutanoate (II) by means of triethylamine in hot DMF gives ethyl 2-[[1-(tert-butoxycarbonyl)ethyl]amino]-4-phenylbutanoate (III), which is partially hydrolyzed with trifluoroacetic acid yielding ethyl 2-[[1-carboxyethyl]amino]-4-phenylbutanoate (IV). The condensation of (IV) with tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (VIII) [prepared from the corresponding acid (VI) and isobutylene (B) by means of H2SO4] as before gives tert-butyl-2-[2-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (IX), which is finally hydrolyzed partially by treatment with trifluoroacetic acid.
    Hoefle, M.L.; Klutchko, S. (Pfizer…

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FDA Approves Xgeva,denosumab to Treat Giant Cell Tumor of the Bone

New Drug Approvals

June 13, 2013 — The U.S. Food and Drug Administration today expanded the approved use of Xgeva (denosumab) to treat adults and some adolescents with giant cell tumor of the bone (GCTB), a rare and usually non-cancerous tumor.

GCTB generally occurs in adults between the ages of 20 and 40 years. In most cases, GCTB does not spread to other parts of the body but destroys normal bone as it grows, causing pain, limited range of motion and bone fractures. Rarely, GCTB can transform into a cancerous tumor and spread to the lungs.

Xgeva is a monoclonal antibody that binds to RANKL, a protein essential for maintenance of healthy bone. RANKL is also present in GCTB. Xgeva is intended for patients whose GCTB cannot be surgically removed (unresectable) or when surgery is likely to result in severe morbidity, such as loss of limbs or joint removal. It should only be…

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Cempra Provides Guidance on the Clinical Program Required for Regulatory Approval for Solithromycin for Community-Acquired Bacterial Pneumonia (CABP)

New Drug Approvals

solithromycin

(3aS,4R,7S,9R,10R,11R,13R,15R,15aR)-1-[4-[4-(3-aminophenyl)-1H-1,2,3-triazol-1-yl]butyl]-4-ethyl-7-fluorooctahydro-11-methoxy-3a,7,9,11,13,15-hexamethyl-10-{[3,4,6-trideoxy-3-(dimethylamino)-β-Dxylo-hexopyranosyl]oxy}-2H-Oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(1H,7H,9H)-tetrone

   
Legal status Phase III clinical trials, North America, South America, Europe
Routes oral, intravenous
Identifiers
CAS number 760981-83-7 
   

Cempra Provides Guidance on the Clinical Program Required for Regulatory 
The Herald | HeraldOnline.com
The Phase 3 solithromycin clinical program in CABP will be planned to consist of an oral trial and an intravenous (IV)-to-oral clinical trial. Cempra followed the CABP guidance that the FDA proposed in a November, 2011, meeting of the Anti-Infective 

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http://www.heraldonline.com/2013/06/13/4944834/cempra-provides-guidance-on-the.html

 

Solithromycin (formerly known as CEM-101 and OP-1068) is a novel ketolide antibiotic undergoing clinical development for the treatment of community-acquired pneumonia (CAP) and other infections.It is expected to be the first macrolide

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