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    • 6. 发明授权
    • 3, 7 or 3 and 7 thia or oxa prostanoic acid derivatives as agents for lowering intraocular pressure
    • 3,7或3和7和硫代前列腺酸衍生物作为降低眼内压的药物
    • US06767920B2
    • 2004-07-27
    • US10346828
    • 2003-01-16
    • Robert M. BurkMark HoloboskiMari F. Posner
    • Robert M. BurkMark HoloboskiMari F. Posner
    • A61K315575
    • A61K31/559A61K31/5575Y10S514/913
    • 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 &agr; configuration, a triangle represents the &bgr; configuration, a wavy line represents the &agr; configuration or the &bgr; 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, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR2, 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 波浪线表示α构型或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;条件是至少一个A 或B是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, 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 或烯基,R 3是苯并噻吩基,苯并呋喃基,萘基或其取代的衍生物,其中取代基可以选自 由C 1 -C 5烷基,卤素,CF 3,CN,NO 2,NR 2,CO 2 R和OR组成的组。
    • 7. 发明授权
    • Cyclopentane heptan(ene) acyl sulfonamide, 2-alkyl or 2-arylalkyl, or 2-heteroarylalkenyl derivatives as therapeutic agents
    • 环戊烷庚烷(烯)酰基磺酰胺,2-烷基或2-芳基烷基或2-杂芳基烯基衍生物作为治疗剂
    • US06706755B2
    • 2004-03-16
    • US10228412
    • 2002-08-26
    • David W. OldRobert M. Burk
    • David W. OldRobert M. Burk
    • A61K315575
    • C07C405/0041
    • 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 a hatched line represents the &agr; configuration, a triangle represents the &bgr; configuration, a straight line, e.g. at the 9, 11 or 15 position represents either the &agr; or &bgr; configuration, a dotted line represents the presence or absence of a double bond; a wavy line represents a cis or trans bond; X is O, S, NH or (CH2)n; n is 0 or an integer of from 1 to 4; Y is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl, pyridinyl, thiazolyl, benzothienyl, benzofuranyl, naphthyl, or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, N(R2)2, CO2R2 and OR2; Z is (CH2)n or a covalent bond; R is C1-C6 lower alkyl or Z-CF3 or mesylate or triflate; R1 is H, R2 or COR2; and R2 is H or C1-C5 lower alkyl or 9, 11 or 15 esters thereof.
    • 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 配置,直线,例如 在9,11或15位置表示α或β构型,虚线表示存在或不存在双键; 波浪线代表顺式或反式键; X为O,S,NH或(CH 2)n; n为0或1至4的整数; Y为C 1 -C 5正烷基,C 3 -C 7环烷基,苯基 呋喃基,噻吩基,吡啶基,噻唑基,苯并噻吩基,苯并呋喃基,萘基或其取代的衍生物,其中取代基可以选自C 1 -C 5烷基,卤素,CF 3,CN,NO 2,N(R 2) 2,CO 2 R 2和OR 2; Z是(CH 2)n或共价键; R是C 1 -C 6低级烷基或Z-CF 3或甲磺酸酯或三氟甲磺酸酯; R 1是H,R 2, 或COR 2; 和R 2是H或C 1 -C 5低级烷基或9,11或15个酯。
    • 8. 发明授权
    • Prostanoic acid derivatives as agents for lowering intraocular pressure
    • 前列腺酸衍生物作为降低眼内压的药物
    • US06531504B2
    • 2003-03-11
    • US09859770
    • 2001-05-17
    • Robert M. BurkTodd S. Gac
    • Robert M. BurkTodd S. Gac
    • A61K315575
    • C07D333/62A61K31/381A61K31/5575C07D333/28C07D333/60
    • 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 &agr; configuration, a triangle represents the &bgr; configuration and a dotted line represents the presence or absence of a double bond; A and B are CH2; 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, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR2, 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 并且虚线表示双键的存在或不存在; A和B为CH 2; D表示共价键或CH 2,O,S或NH; X为CO 2 R,CONR 2,CH 2 OR,P(O) ,CONRSO 2 R SONR2或Y为O,OH,OCOR 2,卤素或氰基; Z为CH 2或共价键; R为H或R 2; R 1为H,R 2,苯基或COR 2; R 2为C 1 -C 5低级烷基或烯基, R3是苯并噻吩基,苯并呋喃基,萘基或其取代衍生物,其中取代基可以选自C1-C5烷基,卤素,CF3,CN,NO2,NR2,CO2R和OR。