Fluoro-prostaglandins
AssigneeFarmitalia Carlo Erba S.p.A.
InventorsRenato Pellegata, Carmelo Gandolfi
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Abstract
16-fluoro-substituted prostaglandin analogs of the formula: ##STR1## in which R is hydrogen, a C.sub.1 -C.sub.12 alkyl group or a cation of a pharmaceutically acceptable base; one of R.sub.1 and R.sub.2 is hydrogen and the other is hydroxy or acyloxy or R.sub.1 and R.sub.2 take together, form a oxo group; one of R.sub.4 and R.sub.5 is hydroxy and the other is hydrogen; R.sub.6 is hydrogen, methyl or fluorine; n is zero or an integer of 1 to 6; and R.sub.7 is phenyl or phenyl substituted by at least one of halogen C.sub.1 -C.sub.6 alkoxy or trihalomethyl.
Claims8
A 16-fluoro prostaglandin analog of the formula:
- ##STR30## wherein R is hydrogen, a C.sub.1 -C.sub.12 alkyl group or a cation of a pharmaceutically acceptable base;
- one of R.sub.4 and R.sub.5 is hydroxy and the other is hydrogen;
- R.sub.6 is a member selected from the group consisting of hydrogen, methyl and fluorine;
- n is zero, or an integer of 1 to 6;
- R.sub.7 is a member selected from the group consisting of phenyl and phenyl substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.6 alkoxy and trihalomethyl.
A compound selected from the group consisting of:
- 16-fluoro-18,19,20-trinor-17-phenyl-13,14-dehydro-PGF.sub.2.alpha., and
- 18,19,20-trinor-17-phenyl-16,16-difluoro-13,14-dehydro-PGF.sub.2.alpha..
A 16-fluoro-prostaglandin analog of the formula:
- ##STR31## wherein R is hydrogen, a C.sub.1 -C.sub.12 alkyl group or a cation of a pharmaceutically acceptable base;
- one of R.sub.4 and R.sub.5 is hydroxy and the other is hydrogen;
- R.sub.6 is a member selected from the group consisting of hydrogen, methyl and fluorine;
- n is zero, or an integer of 1 to 6;
- R.sub.7 is a member selected from the group consisting of phenyl and phenyl substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.6 alkoxy and trihalomethyl.
A compound selected from the group consisting of 16-fluoro-18,19,20-trinor-17-phenyl-13,14-dehydro-PGE.sub.2, and
- 18,19,20-trinor-17-phenyl-16,16-difluoro-13,14-dehydro-PGE.sub.2.
A 16-fluoro prostaglandin analog of the formula ##STR32## wherein R is hydrogen, a C.sub.1 -C.sub.12 alkyl group or a cation of a pharmaceutically acceptable base;
- one of R.sub.1 and R.sub.2 is hydrogen and the other is hydroxy or acyloxy or R.sub.1 and R.sub.2 taken together, form an oxo group;
- one of R.sub.4 and R.sub.5 is hydroxy and the other is hydrogen;
- R.sub.6 is a member selected from the group consisting of hydrogen, methyl and fluorine;
- n is zero, or an integer of 1 to 6;
- R.sub.7 is a member selected from the group consisting of phenyl and phenyl substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.6 alkoxy and trihalomethyl.
Dependencies are inferred from the claim text.