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1. (WO1991017148) 1H-SUBSTITUTED-1,2,4-TRIAZOLE COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISORDERS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/017148 International Application No.: PCT/US1991/002926
Publication Date: 14.11.1991 International Filing Date: 06.05.1991
Chapter 2 Demand Filed: 29.11.1991
IPC:
C07D 249/08 (2006.01) ,C07D 249/10 (2006.01) ,C07D 403/10 (2006.01) ,C07D 521/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
249
Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
08
1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
249
Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
08
1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
521
Heterocyclic compounds containing unspecified hetero rings
Applicants:
G.D. SEARLE & CO. [US/US]; P.O. Box 5110 Chicago, IL 60680-5110, US (AllExceptUS)
REITZ, David, B. [US/US]; US (UsOnly)
Inventors:
REITZ, David, B.; US
Agent:
KEANE, J., Timothy ; G.D. Searle & Co. P.O. Box 5110 Chicago, IL 60680-5110, US
WOLFF, Hans, Joachim; Adelonstrasse 58 Postfach 80 01 40 D-6230 Frankfurt am Main 80, DE
Priority Data:
519,38004.05.1990US
Title (EN) 1H-SUBSTITUTED-1,2,4-TRIAZOLE COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISORDERS
(FR) COMPOSES DE 1,2,4-TRIAZOLE A SUBSTITUTION 1H UTILISES DANS LE TRAITEMENT DE TROUBLES CARDIOVASCULAIRES
Abstract:
(EN) A class of 1H-substituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders, especially cardiovascular disorders. Compounds of interest are angiotensin II antagonists of formula (II), wherein R1 is selected from hydroxy, formyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, n-hexyl, n-heptyl, n-octyl, n-nonyl, carboxyethyl, phenyl, benzyl, phenethyl, cyclopentyl, cyclohexyl, cyclopentylmethyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, adamantyl, adamantylmethyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, dimethoxymethyl, diethoxymethyl, 1,1-dimethoxypropyl, 1,1-dimethoxybutyl, 1,1-dimethoxypentyl, hydroxypropyl, halo, monofluoromethyl, difluoromethyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, pentafluoroethyl, heptafluoropropyl, phenylacetyl, phenyldifluoroethyl, aminomethyl, aminoethyl, aminopropyl, acetylaminomethyl, t-butoxycarbonylaminoethyl, glutamic acid methyl ester and glutamic acid ethyl ester; wherein R2 is selected from carboxyethyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl and neopentyl; wherein each of R3 through R11 is hydrido with the proviso that at least one of R5 and R9 must be selected from COOH, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (III), (IV) and (V), wherein each of R40 and R41 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
(FR) L'invention concerne une classe de composés de 1,2,4-triazole à substitution 1H utilisés dans le traitement de troubles circulatoires, notamment de troubles cardiovasculaires. Les composés d'intérêt sont des antagonistes d'angiotensine II de la formule (II), dans laquelle R1 est choisi parmi hydroxy, formyle, méthyle, éthyle, n-propyle, isopropyle, n-butyle, sec-butyle, isobutyle, tert-butyle, 4-méthylbutyle, n-pentyle, néopenthyle, n-hexyle, n-heptyle, n-octyle, n-nonyle, carboxyéthyle, phényle, benzyle, phénéthyle, cyclopentyle, cyclohexyle, cyclopentylméthyle, cyclohexylméthyle, cyclohexyléthyle, cyclohexylpropyle, adamantyle, adamantylméthyle, 1-oxoéthyle, 1-oxopropyle, 1-oxobutyle, 1-oxopentyle, diméthoxyméthyle, diéthoxyméthyle, 1,1-diméthoxypropyle, 1,1-diméthoxybutyle, 1,1-diméthoxypentyle, hydroxypropyle, halo, monofluorométhyle, difluorométhyle, 1,1-difluoroéthyle, 1,1-difluoropropyle, 1,1-difluorobutyle, 1,1-difluoropentyle, pentafluoroéthyle, heptafluoropropyle, phénylacétyle, phényldifluoroéthyle, aminométhyle, aminoéthyle, aminopropyle, acétylaminométhyle, t-butoxycarbonylaminoéthyle, ester méthylique d'acide glutamique et ester éthylique d'acide glutamique; dans laquelle R2 est choisi parmi carboxyéthyle, éthyle, n-propyle, isopropyle, n-butyle, sec-butyle, isobutyle, 4-méthylbutyle, tert-butyle, n-pentyle et néopentyle; dans laquelle R3 à R11 représentent chacun hydrido à condition que R5 et/ou R9 soient choisis parmi COOH, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, les formules (III), (IV) et (V), dans lesquelles R40 et R41 sont chacun indépendamment choisis parmi chloro, cyano, nitro, trifluorométhyle, méthoxycarbonyle et trifluorométhylsulfonyle. Ces composés sont particulièrement utiles dans le traitement ou la maîtrise de l'hypertension et de l'insuffisance cardiaque.
Designated States: AT, AU, BB, BG, BR, CA, CH, DE, DK, ES, FI, GB, HU, JP, KP, KR, LK, LU, MC, MG, 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, ML, MR, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0527851JPH05507079CA2082074AU1991077924DK0527851