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1. (WO1992011255) N-SUBSTITUTED N-($g(a)-TRIAZOLYL-TOLUYL)PYRROLE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1992/011255    International Application No.:    PCT/US1991/008726
Publication Date: 09.07.1992 International Filing Date: 26.11.1991
Chapter 2 Demand Filed:    22.05.1992    
IPC:
C07D 403/10 (2006.01), C07D 403/14 (2006.01)
Applicants: G.D. SEARLE & CO. [US/US]; P.O. Box 5110, Chicago, IL 60680-5110 (US) (For All Designated States Except US).
BOVY, Philippe, R. [BE/US]; (US) (For US Only).
REITZ, David, B. [US/US]; (US) (For US Only).
MANNING, Robert, E. [US/US]; (US) (For US Only)
Inventors: BOVY, Philippe, R.; (US).
REITZ, David, B.; (US).
MANNING, Robert, E.; (US)
Agent: KEANE, J., Timothy; G.D. Searle & Co., Corporate Patent Department, P.O. Box 5110, Chicago, IL 60680-5110 (US)
Priority Data:
630,714 20.12.1990 US
Title (EN) N-SUBSTITUTED N-($g(a)-TRIAZOLYL-TOLUYL)PYRROLE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS
(FR) COMPOSES DE N-($g(a)-TRIAZOLYL-TOLUYL)PYRROLE A SUBSTITUTION N POUR LE TRAITEMENT DES TROUBLES CIRCULATOIRES
Abstract: front page image
(EN)A class of N-substituted N-($g(a)-triazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of formula (I), wherein m is one; wherein R?1¿ is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R?2¿ is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R?3¿, R?4¿, R?5¿, R?6¿, R?7¿, R?8¿, R?9¿ and R?10¿ is independently selected from hybrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R?5¿ and R?8¿ must be selected from COOH, SH, PO¿3?H¿2?, SO¿3?H, CONHNH¿2?, CONHNHSO¿2?CF¿3?, OH, a), b) and c) wherein each of R?42¿ and R?43¿ is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
(FR)L'invention se rapporte à une classe de composés de N-($g(a)-triazolyl-toluyl)pyrrole à substitution N, qui sont conçus pour être utilisés dans le traitement des troubles circulatoires, et plus particulièrement à des composés antagonistes de l'angiotensine II représentés par la formule (I), où: m est égal à 1; R?1¿ est choisi parmi méthyle, éthyle, n-propyle, isopropyle, n-butyle, sec-butyle, isobutyle, tert-butyle, 4-méthylbutyle, n-pentyle, néopentyle, phényle, benzyle, phénéthyle, cyclohexyle, cyclohexylméthyle, cyclohexyléthyle, cyclohexanoyle, 1-oxo-2-cyclohexyléthyle, benzoyle, 1-oxo-2-phénéthyle, 1-oxopropyle, 1-oxobutyle, 1-oxopentyle et 2-hydroxybutyle; R?2¿ est choisi parmi méthyle, éthyle, n-propyle, isopropyle, n-butyle, sec-butyle, isobutyle, tert-butyle, n-pentyle, isopentyle, néopentyle, phényle, benzyle, phénéthyle, cyclohexyle, cyclohexylméthyle, propylthio, butylthio et hydroxyalkyle; chacun des éléments R?3¿, R?4¿, R?5¿, R?6¿, R?7¿, R?8¿, R?9¿ et R?10¿ est choisi séparément parmi hydrido, halo, nitro, trifluorométhyle, hydroxy, alcoxy, cyano, carboxyle et méthoxycarbonyle; à condition qu'au moins l'un des éléments R?5¿ et R?8¿ soit choisi parmi COOH, SH, PO¿3?H¿2?, SO¿3?H, CONHNH¿2?, CONHNHSO¿2?CF¿3?, OH, (a), (b) et (c) où chacun des éléments R?42¿ et R?43¿ est choisi séparément parmi chloro, cyano, nitro, trifluorométhyle, méthoxycarbonyle et trifluorométhylsulfonyle; ou à un tautomère de ces composés ou à un sel pharmaceutiquement acceptable de ces composés. Ceux-ci sont particulièrement utiles pour traiter ou combattre l'hypertension et les défaillances cardiaques congestives.
Designated States: AT, AU, BB, BG, BR, CA, CH, CS, DE, DK, ES, FI, GB, HU, JP, KP, KR, LK, LU, MC, MG, MN, MW, NL, NO, PL, RO, SD, SE, SU, US.
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)