CASOPITANT

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AZASETRON..a selective 5-HT3 receptor antagonist

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AZASETRON,  NAZASETRON

N-(1-azabicyclo[2.2.2]octan-8-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide

6-chloro-3,4-dihydro-4-methyl-3-oxo-N-(3-quinuclidinyl)-2H-1,4-benzoxazine-8-carboxamide

123039-99-6 , 123040-69-7 (free base)

141922-90-9 HYD SALT

Y-25130 (hydrochloride)LAUNCHED 1994 AS HCL SALT FORM SEROTONE

a selective 5-HT3 receptor antagonist , ANTIEMETIC

  • UNII-77HC7URR9Z

Mitsubishi Tanabe Pharma, JAPAN TOBACCO (Originator)

FOR..Nausea and Vomiting, Treatment of
Prokinetic Agents

Azasetron is an antiemetic which acts as a 5-HT3 receptorantagonist.

Chemical and Pharmaceutical Bulletin, 1992 ,  vol. 40,  3  p. 624 – 630, ENTRY 15 , MP 305 OF HCL SALT

Biological and Pharmaceutical Bulletin, 2006 ,  vol. 29,  9  p. 1931 – 1935, AS MERCK 903

US 4892872…

CN 101786963…

WO 1996001630..

WO 2006006595..

WO 2007134077..

CN 102526740,  CN 102451166, US 4892872, JP 2008297277

US5773436 A1, WO2006/119295 A2, EP1336602 A1, US4892872 A1,

US2003/18008 A1, US2002/147197 A1, US4892872

AZASETRON

 

The nitration of 5-chloro-2-hydroxybenzoic acid methyl ester (I) with nitric acid in sulfuric acid gives 5-chloro-2-hydroxy-3-nitrobenzoic acid methyl ester (II), which is reduced with Fe and NH4Cl in water yielding 3-amino-5-chloro-2-hydroxybenzoic acid methyl ester (III)…

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NETUPITANT

New Drug Approvals

NETUPITANT

  • Ro 67-3189/000
  • UNII-7732P08TIR
  • Ro-67-3189
  • Netupitant, an NK-1 antagonist is under development for the treatment of overactive bladder. HELSINN GROUP

CAS:  290297-26-6

290296-54-7 (di HCl)

U.S. Pat. Nos. 6,303,790, 6,531,597, 6,297,375 and 6,479,4836,719,996 and 6,593,472  to Hoffmann La Roche(originator).

IUPAC/Chemical name: 

2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide

Chemical Formula: C30H32F6N4O
Exact Mass: 578.24803
Molecular Weight: 578.59
Elemental Analysis: C, 62.28; H, 5.57; F, 19.70; N, 9.68; O, 2.77

Netupitant is another selective NKi receptor antagonist under development by Helsinn Healthcare, having the formula 2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2- methylphenyl)-6-(4-methylpiperazin- l-yl)pyridin-3-yl]propanamide, or Benzeneacetamide, N,a,a-trimethyl-N-[4-(2-methylphenyl)-6-(4-methyl-l-piperazinyl)-3-pyridinyl]-3,5- bis(trifluoromethyl)-, and the below chemical structure:

Figure imgf000004_0001

Netupitant is a tachykinin NK-1 antagonist which had been in phase III clinical trials at Helsinn for the prophylaxis of chemotherapy-induced nausea and vomiting and in phase II clinical studies for the treatment of overactive bladder. However, no recent development has been reported for this research.

NK-1 receptor antagonists work by blocking the action of neurokinin-1 (Substance…

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CILUPREVIR » All About Drugs

New Drug Approvals

CILUPREVIR » All About Drugs

WANT TO KNOW ABOUT VIR SERIES CLICK

click

http://drugsynthesisint.blogspot.in/p/vir-series-hep-c-virus-22.html

AND

http://medcheminternational.blogspot.in/p/vir-series-hep-c-virus.html

CILUPREVIR

CILUPREVIR
(1S,4R,6S,7Z,14S,18R)-14- {[(cyclopentyloxy)carbonyl]amino}-18-[(7-methoxy-2- {2-[(propan-2-yl)amino]-1,3-thiazol-4-yl}quinolin-4- yl)oxy]-2,15-dioxo-3,16- diazatricyclo[14.3.0.0{4,6}]nonadec-7-ene-4- carboxylic acid
Ciluprevir, BILN-2061, BILN 2061, CHEBI:161337, BILN2061, BILN 2061ZW, BILN-2061-ZW,
CAS , 300832-84-2
Molecular Formula: C40H50N6O8S   Molecular Weight: 774.9254
Abstract Image
Ciluprevir is used in the treatment of hepatitis C. It is manufactured by Boehringer Ingelheim Pharma GmbH & Co. KG under the research code of BILN-2061. It is targeted against NS2-3 protease.[1]
Ciluprevir is an HCV NS3 protease inhibitor which had been in phase II clinical trials at Boehringer Ingelheim for the treatment of hepatitis C, however, no recent developments from the company have been reported.

  1.  Abbenante, G; Fairlie, DP (2005). “Protease inhibitors in the clinic”. Medicinal chemistry 1 (1): 71–104. PMID 16789888

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Iloprost (ciloprost)

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CICAPROST , ZK-96480

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CICAPROST , ZK-96480

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