Claims for Patent: 5,886,035

Summary for Patent: 5,886,035

Title:	Difluoroprostaglandin derivatives and their use
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: (1) wherein A is a vinylene group or the like, R1 is an aryloxyalkyl group or the like, R2 and R3 are hydrogen atoms or the like, and Z is OR4 (wherein OR4 is a hydrogen atom or an alkyl group) or the like.
Inventor(s):	Eiichi Shirasawa, Masaaki Kageyama, Tadashi Nakajima, Takashi Nakano, Nobuaki Mori, Hideshi Sasakura, Yasushi Matsumura, Yoshitomi Morizawa
Assignee:	Santen Pharmaceutical Co Ltd , AGC Inc
Application Number:	US08/993,017
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 5,886,035
Patent Claims:	1. 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, --OCH2 -- or --SCH2 --,R1 is a substituted or unsubstituted aryloxyalkyl group, each of R2 and R3 which are independent of each other, is a hydrogen atom or an acyl group, or forms a single bond together with Z, X is --CH2 --, --O-- or --S--, Z is --OR4, --NHCOR5, --NHSO2 R6 or --SR7, or forms a single bond together with R2 or R3, each of R4, R5, R6 and R7 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. 2. The compound according to claim 1, wherein R1 is a phenoxymethyl group, a 3,5-dichlorophenoxymethyl group or a 3-chlorophenoxymethyl group. 3. The compound according to claim 1, which is 16-phenoxy-15-deoxy-15,15-difluoro-17,18,19,20-tetranorprostaglandin F2α, 16-(3-chlorophenoxy)-15-deoxy-15,15-difluoro-17,18,19,20-tetranorprostaglandin F2α, 16-phenoxy-15-deoxy-15,15-difluoro-13,14-dihydro-17,18,19,20-tetranorprostaglandin F2α or an alkyl ester or a salt thereof. 4. A medicine containing the compound according to claim 1 as an active ingredient. 5. The medicine according to claim 4, which is a preventive or therapeutic medicine for an eye disease. 6. The medicine according to claim 5, wherein the eye disease is glaucoma or ocular hypertension. 7. The medicine according to claim 4, 5 or 6, wherein A is an ethylene group or a vinylene group. 8. The medicine according to claim 4, 5 or 6, wherein X is --CH2 --. 9. The medicine according to claim 4, 5 or 6, wherein both R2 and R3 are hydrogen atoms. 10. The medicine according to claim 4, 5 or 6, wherein Z is --OR4. 11. The medicine according to claim 9, wherein R1 is a phenoxymethyl group, a 3,5-dichlorophenoxymethyl group or a 3-chlorophenoxymethyl group. 12. A medicine containing 16-phenoxy-15-deoxy-15,15-difluoro-17,18,19,20-tetranorprostaglandin F2α, 16-(3-chlorophenoxy)-15-deoxy-15,15-difluoro-17,18,19,20-tetranorprostaglandin F2α, 16-phenoxy-15-deoxy-15,15-difluoro-13,14-dihydro-17,18,19,20-tetranorprostaglandin F2α or an alkyl ester or salt thereof as an active ingredient. 13. The medicine according to claim 12, which is a preventive or therapeutic medicine for an eye disease. 14. The medicine according to claim 13, wherein the eye disease is glaucoma or ocular hypertension.