177202-68-5Relevant articles and documents
Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists
Nitta, Aiko,Iura, Yosuke,Inoue, Hideki,Imaoka, Takayuki,Takahashi, Toshiya,Sato, Ippei,Morihira, Koichiro,Kubota, Hirokazu,Morokata, Tatsuaki,Takeuchi, Makoto,Ohta, Mitsuaki,Tsukamoto, Shin-Ichi
, p. 6876 - 6881,6 (2020/09/02)
Optimization starting with our lead compound 1 (IC50 = 4.9 nM) led to the identification of pyrrolidinyl phenylurea derivatives. Further modification toward improvement of the bioavailability provided (R)-1-(1-((6-fluoronaphthalen-2-yl)methyl)pyrrolidin-3-yl)-3-(2-(2- hydroxyethoxy)phenyl)urea 32 (IC50 = 1.7 nM), a potent and orally active CCR3 antagonist.
2,9-DIAMINO- AND 2-AMINO-8-CARBAMOYL-4-HYDROXY-ALKANOIC ACID AMIDE DERIVATIVES
-
, (2008/06/13)
Compounds of the formula I STR1 in which R 1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a carbonyl or methylene group, R 2 and R 3 independently of one another are hydrogen or lower alkyl or, together with the carbon atom with which they are bonded, are a cycloalkylidene radical, R 4 is hydrogen, lower alkyl, lower alkanoyl or lower alkoxycarbonyl, R 5 is hydroxyl, lower alkanoyloxy or lower alkoxycarbonyloxy, R 6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, aryl-lower alkyl or heteroaryl-lower alkyl having 5 to 7 ring atoms in the heteroaryl ring and R 7 is hydrogen or lower alkyl, or R 6 and R. sub.7, together with the carbon atom with which they are bonded, are a cydoalkylidene radical and R 8 denotes an aliphatic, cycloaliphatic-aliphatic or heteroarylaliphatic radical, and their salts can be used as active ingredients for medicaments for treatment of high blood pressure.