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US 4,285,966 AGranted
Certain 15-epi-prostacyclins
AssigneeFarmitalia Carlo Erba S.p.A.
InventorsCarmelo Gandolfi, Carlo Passarotti, Alessandro Andreoni, Angelo Fumagalli, Franco Faustini, Roberto Cesarani
Life of this patent
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Abstract
The present invention relates to 15-epi-derivatives of prostacyclin and its analogs, to a process for their preparation and to pharmaceutical and veterinary compositions containing them.
Claims12
A 15-epi compound of the formula ##STR28## wherein R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;
- p is zero or an integer of 1-7;
- R.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, benzyloxy, or acyloxy;
- Y is chosen from the group:
- ##STR29## R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl;
- R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl;
- n.sub.1 and n.sub.2, whether the same or different, are zero or an integer of 1 to 6,;
- R.sub.3 and R.sub.4, whether the same or different, are hydrogen, C.sub.1 -C.sub.6 alkyl or may form a ##STR30## group with a carbon atom to which they are bound;
- X is chosen from --O-- or --S--;
- R.sub.6 is a substituent chosen from (a) C.sub.1 -C.sub.4 alkyl, (b) a C.sub.3 -C.sub.9 cycloalkyl, C.sub.3 -C.sub.9 cycloalkenyl, norbornyl, or adamantyl radical each of which radicals may be substituted by one or more C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 - alkoxy groups;
- and a pharmaceutically or veterinarily acceptable salt thereof.
7 more elements
A compound selected from the group consisting of:
- 15-epi-17-oxa-PGI.sub.2 ;
- 15-epi-17-oxa-20-methyl-PGI.sub.2 ;
- 15-epi-17-trinor-16-methyl-16-butoxy-PGI.sub.2 ;
- 15-epi-17-trinor-16-methyl-16-propoxy-PGI.sub.2 ;
- 15-epi-17-trinor-16-methyl-16-amyloxy-PGI.sub.2 ;
- 15-epi-16-tetranor-16-butoxy-PGI.sub.2 ;
- and a pharmaceutically or veterinarily acceptable salt thereof.
4 more elements
Dependencies are inferred from the claim text.