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    • 8. 发明申请
    • 3, 7 OR 3 AND 7 THIA OR OXA PROSTANOIC ACID DERIVATIVES AS AGENTS FOR LOWERING INTRAOCULAR PRESSURE
    • 3,7 OR 3和7 THIA或OXA PROSTANOIC酸性衍生物作为降低室内压力的代理
    • WO02089813A2
    • 2002-11-14
    • PCT/US0214331
    • 2002-05-06
    • ALLERGAN INCBURK ROBERT MHOLOBOSKI MARKPOSNER MARI F
    • BURK ROBERT MHOLOBOSKI MARKPOSNER MARI F
    • A61K31/5575A61P27/02A61P27/06C07C405/00A61K31/19A61K31/192A61K31/215A61K31/216
    • C07C405/0033A61K31/5575
    • The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I, wherein hatched lines represent the alpha configuration, a triangle represents the beta configuration and a dotted line represents the presence or absence of a double bond; A and B are independently selected from the group consisting of O, S and CH2 provided that at least one of A or B is S; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR , halogen or cyano; Z is CH2 or a covalent bond; R is H or R ; R is H, R , phenyl, or COR ; R is C1-C5 lower alkyl and R3 is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl, or substituted derivatives thereof, wherein the substituents may be selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, CO2R and OR.
    • 本发明提供一种治疗眼高血压或青光眼的方法,其包括向具有高眼压症或青光眼的动物施用治疗有效量的由通式I表示的化合物,其中阴影线表示α构型,三角形表示β构型 虚线表示双键的存在或不存在; A和B独立地选自O,S和CH 2,条件是A或B中的至少一个为S; D表示共价键或CH 2,O,S或NH; X是CO 2 R,CONR 2,CH 2 OR,P(O)(OR)2,CONRSO 2 R SONR2或Y是O,OH,OCOR 2,卤素或氰基; Z是CH 2或共价键; R是H或R 2; R 1是H,R 2,苯基或COR 2; R 2是C 1 -C 5低级烷基,R 3是C 1 -C 5正烷基,C 3 -C 7环烷基,苯基,呋喃基,噻吩基或取代的衍生物,其中取代基可以选自C1-C5 烷基,卤素,CF 3,CN,NO 2,CO 2 R和OR。