169545-92-0Relevant academic research and scientific papers
Endothelin receptor antagonists
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, (2008/06/13)
The present invention provides novel compounds represented by the general formula I: STR1 wherein R 1 is a straight or branched lower alkyl, a cycloalkyl-lower alkyl, an aryl-lower alkyl, a cycloalkyl, an aryl an aryl-cycloalkyl, lower alkoxy, an aryloxy, or a heteroaryl;R 2 is hydrogen, a straight or branched lower alkyl, a cycloalkyl, or a cycloalkyl-lower alkyl;R 3 and R 3 '' are each the same or different and each is hydrogen atom, a straight or branched lower alkyl, a cycloalkyl, an aryl-lower alkyl, an aryl, or a heteroaryl; orR 3 and R 3 '' together form a ring structure;R 3 "" is hydrogen, lower alkyl or an aryl; orR 2 and R 3 "" together form a lower alkylene group --(CH 2) n -- wherein n is an integer of 1, 2 or 3; orR 2 and R 3 "" together form a group represented by the formula: --(CH 2) p --Ar-- or --Ar--(CH 2) p --, respectively, wherein p is zero or an integer of 1 or 2, and Ar is an arylene or heteroarylene;C( X) is C( O), C( S), C( NH), C( N-lower alkyl); C NH--OH, or CH 2 ;Y is a direct bond, --NH--, a lower alkyl-N, an oxygen atom, or methylene; orC( X) is CHOH and Y is a direct bond or methylene;R 4 is --(CH 2) s --Ar'' wherein s is zero or an integer of 1, 2 or 3; and Ar'' is an aryl, or a heteroaryl; andR 5 is carboxy, substituted or unsubstituted carboxamide, PO(OH) 2, tetrazole, CH 2 OH, CN, or hydrogen;and salts thereof.
IRL 2500: A potent ET(B) selective endothelin antagonist
Frueh,Saika,Svensson,Pitterna,Sakaki,Okada,Urade,Oda,Fujitani,Takimoto,Yamamura,Inui,Makatani,Takai,Umemura,Teno,Toh,Hayakawa,Murata
, p. 2323 - 2328 (2007/10/03)
Combination of a glycine substitution scan on the C-terminal dodecapeptide analog of ET-1 and a substance P antagonist screen on the basis of a homology study of the rhodopsin superfamily of seven-transmembrane receptors yielded in the development of IRL 2500, a potent ET(B) selective endothelin antagonist.
