144062-72-6Relevant articles and documents
Nonpeptide angiotensin II antagonists: N-phenyl-1H-pyrrole derivatives are angiotensin II receptor antagonists
Bovy,Reitz,Collins,Chamberlain,Olins,Corpus,McMahon,Palomo,Koepke,Smits,McGraw,Gaw
, p. 101 - 110 (1993)
A series of 5-[1-[4-[(4,5-disubstituted-1H-imidazol-1-yl)methyl]- substituted]-1H-pyrrol-2-yl]-1H-tetrazoles and 5-[1-[4-[(3,5-dibutyl-1H- 1,2,4-triazol-1-yl)methyl]-substituted]-1H-pyrrol-2-yl]-1H-tetrazoles were investigated as novel AT1-sele
FUSED HETEROCYCLIC COMPOUNDS, HAVING ANGIOTENSIN II ANTAGONISTIC ACTIVITY
-
, (2008/06/13)
Fused heterocyclic compounds of the formula (I): STR1 wherein R. sup.1 is an optionally substituted hydrocarbon residue which may be attached through a hetero atom; R 2 is a group capable of forming an anion or a group convertible thereinto; R 3 is an optionally substituted aromatic hydrocarbon or heterocyclic residue which contains at least one hetero atom; X is a direct bond or a spacer having an atomic length of two or less between the R 3 group and the ring W group; W is an optionally substituted aromatic hydrocarbon or heterocyclic residue which contains at least one hereto atom; a,c and d are independently selected from the group consisting of one or two optionally substituted carbon atoms and one or two optionally substituted hetero atoms; b and e are independently selected from the group consisting of one optionally substituted carbon atom and one optionally substituted nitrogen atom wherein one of b or e must be nitrogen; the dotted line is a bond to form one double bond; n is an integer of 1 or 2 and when a, which is an optionally substituted carbon atom, is taken together with R 1, the following group: STR2 may form a ring group; provided that when STR3 is a benzimidazole, thieno[3,4-d] imidazole, or thieno[2,3-d] imidazole ring, at least one of the group: STR4 and R 3 is an optionally substituted heterocyclic residue; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.
N-SUBSTITUTED N-(ALPHA-TRIAZOLYL-TOLUYL)PYRROLE COMPOUNDS AND USE FOR TREATMENT OF CIRCULATORY DISORDERS
-
, (2008/06/13)
A class of N-substituted N-(α-triazolyltoluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula STR1 wherein m is one; wherein R 1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R 2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R 3, R 4, R 5, R 6, R 7, R 8, R 9 and R. sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R 5 and R 8 must be selected from COOH, SH, PO 3 H 2, SO 3 H, CONHNH 2, CONHNHSO 2 CF 3, OH, STR2 wherein each of R 42 and R 43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
