802904-66-1 Usage
Uses
AZD 1981 is an orally available selective DP2 antagonist in the treatment of asthma.
Biological Activity
azd1981 is a selective, orally bioavailable and potent antagonist of the chemoattractant receptor-homologous expressed on th2 lymphocytes receptor (crth2 or dp2) with an ic50 value of 4 nm [1].azd1981 has shown to inhibit eosinophil migration with a pic50 value of 7.6±0.1. azd1981 could block chemotaxis of dp2+ t-cell lines with a pic50 value of 7.5±0.1. azd1981 has been demonstrated to inhibit pgd2 binding to mouse, rat, rabbit, dog, guinea pig and human dp2. azd1981 could inhibit shape change induced by dp2 in dog and guinea pig granulocytes as well as in human eosinophils and basophils in blood [2].
references
[1] luker t1, bonnert r, brough s, cook ar, dickinson mr, dougall i, logan c, mohammed rt, paine s, sanganee hj, sargent c, schmidt ja,teague s, thom s. substituted indole-1-acetic acids as potent and selective crth2 antagonists-discovery of azd1981. bioorg med chem lett. 2011 nov 1;21(21):6288-92. [2] schmidt ja1, bell fm, akam e, marshall c, dainty ia, heinemann a, dougall ig, bonnert rv, sargent ca. biochemical and pharmacological characterization of azd1981, an orally available selective dp2 antagonist in clinical development for asthma. br j pharmacol. 2013 apr;168(7):1626-38.
Check Digit Verification of cas no
The CAS Registry Mumber 802904-66-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,0,2,9,0 and 4 respectively; the second part has 2 digits, 6 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 802904-66:
(8*8)+(7*0)+(6*2)+(5*9)+(4*0)+(3*4)+(2*6)+(1*6)=151
151 % 10 = 1
So 802904-66-1 is a valid CAS Registry Number.
802904-66-1Relevant articles and documents
Development of scalable manufacturing routes to AZD1981. Application of the Semmler-Wolff aromatisation for synthesis of the indole-4-amide Core
Sulur, Manjunatha,Sharma, Parhalad,Ramakrishnan, Ravi,Naidu, Ravi,Merifield, Eric,Gill, Duncan M.,Clarke, Adrian M.,Thomson, Colin,Butters, Michael,Bachu, Sreekanth,Benison, Colin H.,Dokka, Nagaraju,Fong, Emily R.,Hose, David R. J.,Howell, Gareth P.,Mobberley, Siobhan E.,Morton, Simon C.,Mullen, Alexander K.,Rapai, Jayan,Tejas, Bharathi
, p. 1746 - 1753 (2013/01/15)
A safe and efficient synthesis of AZD1981 is described in which the indole 4-amide core is formed by a Semmler-Wolff aromatisation of a cyclohexenone oxime fused to a pyrrole ring. The substrate was obtained via Paal-Knorr pyrrole synthesis, followed by i
INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF 4- (ACETYLAMINO) ) -3- [ (4-CHLORO-PHENYL) THIO] -2-METHYL-1H-INDOLE-1-ACETIC ACID
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, (2011/02/24)
The invention relates to compounds of formula (X), and salts thereof, and their use as intermediates in improved manufacturing processes for the synthesis of pharmaceutical compound of formula (I): X is =0, =N-0H or =N-OC(O)Me; Y is hydrogen, PhS- or p-ch
NOVEL SUBSTITUTED 3-SULFUR INDOLES
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, (2008/06/13)
The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.