This invention provides novel compounds, pharmaceutical compositions and
methods of treating thrombotic disorders in mammals, the compounds having
the formula:
##STR1##
Wherein: Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl,
oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be
cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be
optionally substituted by 1 to 3 groups selected from C.sub.1 -C.sub.6
alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, phenyl-(CH.sub.2).sub.0-6 --,
phenyl-(CH.sub.2).sub.0-6 O--, C.sub.3 -C.sub.6 cycloalkyl,
--(CH.sub.2)--C.sub.3 -C.sub.6 cycloalkyl, halogen, C.sub.1 -C.sub.3
perflouroalkyl and C.sub.1 -C.sub.3 perfluoroalkoxy where phenyl can be
substituted with from 1 to 3 groups selected from C.sub.1 -C.sub.6 alkyl,
C.sub.1 -C.sub.6 alkoxy, phenyl, halogen, trifluoromethyl or
trifluoromethoxy; R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or
phenyl-(CH.sub.2).sub.1-6 -- where phenyl can be substituted with C.sub.1
-C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo, trifluoromethyl or
trifluoromethoxy; R.sub.2 and R.sub.3 are H, C.sub.1 -C.sub.6 alkyl,
phenyl-(CH.sub.2).sub.0-3 --, halo and C.sub.1 -C.sub.3 perfluoroalkyl
where phenyl can be substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1
-C.sub.6 alkoxy, halo, trifluoromethyl or trifluoromethoxy; R.sub.4 is
--CHR.sub.5 CO.sub.2 H or --CH.sub.2 -tetrazole where R.sub.5 is H or
benzyl; and n=0 or 1; or a pharmaceutically acceptable salt or ester form
thereof.
Deze uitvinding verstrekt nieuwe samenstellingen, farmaceutische samenstellingen en methodes om thrombotic wanorde in zoogdieren te behandelen, de samenstellingen die de formule hebben: ## STR1 ## Waarin: AR is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane waar cycloalkane cyclopropyl kan zijn, cyclobutyl, kunnen cyclopentyl of cyclohexyl en AR naar keuze door 1 tot 3 groepen worden gesubstitueerd die uit C.sub.1 - C.sub.6 alkyl, C.sub.1 worden geselecteerd - alkoxy C.sub.6, hydroxy, phenyl-(CH.sub.2).sub.0-6 --, phenyl-(CH.sub.2).sub.0-6 O --, C.sub.3 - cycloalkyl C.sub.6, -- (CH.sub.2) -- C.sub.3 - cycloalkyl C.sub.6, halogeen, C.sub.1 - perflouroalkyl C.sub.3 en C.sub.1 - perfluoroalkoxy C.sub.3 waar het fenyl met van 1 tot 3 groepen kan worden gesubstitueerd die uit C.sub.1 worden geselecteerd - C.sub.6 alkyl, C.sub.1 - alkoxy, phenyl C.sub.6, halogeen, trifluoromethyl of trifluoromethoxy; R.sub.1 is waterstof, C.sub.1 - alkyl C.sub.6 of phenyl-(CH.sub.2).sub.1-6 -- waar het fenyl met C.sub.1 kan worden gesubstitueerd - alkyl C.sub.6, C.sub.1 - alkoxy C.sub.6, halo, trifluoromethyl of trifluoromethoxy; R.sub.2 en R.sub.3 zijn H, C.sub.1 - alkyl C.sub.6, halo phenyl-(CH.sub.2).sub.0-3 --, en C.sub.1 - perfluoroalkyl C.sub.3 waar het fenyl met C.sub.1 kan worden gesubstitueerd - C.sub.6 alkyl, C.sub.1 - alkoxy C.sub.6, halo, trifluoromethyl of trifluoromethoxy; R.sub.4 is -- CHR.sub.5 CO.sub.2 H of -- CH.sub.2 - tetrazole waar R.sub.5 H of benzyl is; en n=0 of 1; of een farmaceutisch aanvaardbare zout of estervorm daarvan.
