Difluoroprostaglandin derivatives and their use
AssigneesAsahi Glass Company, Limited, Santen Pharmaceutical Co., Ltd.
InventorsEiichi Shirasawa, Masaaki Kageyama, Tadashi Nakajima, Takashi Nakano, Nobuaki Mori, Hideshi Sasakura, Yasushi Matsumura, Yoshitomi Morizawa
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Abstract
A fluorine-containing prostaglandin derivative of the formula (1) (or a salt thereof) and a medicine containing it, particularly, a preventive or therapeutic medicine for an eye disease: ##STR1## wherein A is a vinylene group or the like, R.sup.1 is an aryloxyalkyl group or the like, R.sup.2 and R.sup.3 are hydrogen atoms or the like, and Z is OR.sup.4 (wherein OR.sup.4 is a hydrogen atom or an alkyl group) or the like.
Claims14
A fluorine-containing prostaglandin derivative of the following formula (1) or a salt thereof:
- ##STR4## wherein A is an ethylene group, a vinylene group, an ethynylene group, --OCH.sub.2 -- or --SCH.sub.2 --,
- R.sup.1 is a substituted or unsubstituted aryloxyalkyl group,
- each of R.sup.2 and R.sup.3 which are independent of each other, is a hydrogen atom or an acyl group, or forms a single bond together with Z,
- X is --CH.sub.2 --, --O-- or --S--,
- Z is --OR.sup.4, --NHCOR.sup.5, --NHSO.sub.2 R.sup.6 or --SR.sup.7, or forms a single bond together with R.sup.2 or R.sup.3,
- each of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 which are independent of one another, is a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or an aralkyl group,
- and a dual line consisting of solid and broken lines is a single bond, a cis-double bond or a trans-double bond.
A medicine containing 16-phenoxy-15-deoxy-15,15-difluoro-17,18,19,20-tetranorprostaglandin F.sub.2.alpha., 16-(3-chlorophenoxy)-15-deoxy-15,15-difluoro-17,18,19,20-tetranorprostagla ndin F.sub.2.alpha., 16-phenoxy-15-deoxy-15,15-difluoro-13,14-dihydro-17,18,19,20-tetranorprost aglandin F.sub.2.alpha. or an alkyl ester or salt thereof as an active ingredient.
Dependencies are inferred from the claim text.