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13 条记录 (耗时 0.02 秒)

    Prostanoic acid derivatives as agents for lowering intraocular pressure
    4.
    发明授权
    Prostanoic acid derivatives as agents for lowering intraocular pressure 失效
    前列腺酸衍生物作为降低眼内压的药物

    公开(公告)号：US06670485B2

    公开(公告)日：2003-12-30

    申请号：US10294521

    申请日：2002-11-13

    申请人： Robert M. Burk ,  Todd S. Gac

    发明人： Robert M. Burk ,  Todd S. Gac

    IPC分类号： C07D33360

    CPC分类号： C07D333/62 ,  A61K31/381 ,  A61K31/5575 ,  C07D333/28 ,  C07D333/60

    摘要： 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.

    摘要翻译： 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C1-C5烷基，卤素，CF3，CN ，NO2，NR2，CO2R和OR。

    Cyclopentane (ene) oic acid, 2-alkenyl derivatives as therapeutic agents
    5.
    发明授权
    Cyclopentane (ene) oic acid, 2-alkenyl derivatives as therapeutic agents 失效
    环戊烷（烯）酸，2-烯基衍生物作为治疗剂

    公开(公告)号：US06258844B1

    公开(公告)日：2001-07-10

    申请号：US09194457

    申请日：1998-11-24

    申请人： Michael E. Garst ,  Michael B. Roof ,  Ming F. Chan ,  David F. Woodward ,  Robert M. Burk ,  Todd S. Gac ,  Steven W. Andrews

    发明人： Michael E. Garst ,  Michael B. Roof ,  Ming F. Chan ,  David F. Woodward ,  Robert M. Burk ,  Todd S. Gac ,  Steven W. Andrews

    IPC分类号： A67K31215

    CPC分类号： A61K31/5575 ,  C07C405/00 ,  Y10S514/913

    摘要： The invention relates to the use of omega chain modified prostaglandins as ocular hypotensive. The derivatives used in accordance with the invention are encompassed by the following structure formula I: wherein the hatched segments represent &agr; bonds; the wavy segment represents an &agr; or &bgr; bond; dashed lines represent a double bond or a single bond; X is selected from the group consisting of —OR and N(R2); Y is=O or represents 2 hydrogen radicals, provided that Y represents 2 hydrogen radicals when X is OH; R is hydrogen or a lower alkyl radical having up to six carbon atoms; R1 is=O or hydroxy; m is 0, 2, 4 or 6, provided that m is not 4 when the wavy segment represents a &bgr; bond; n is 0, 2, 4 or 6; x and y are 0 or 1, provided that x is 1 when y is 0 and y is 1 when x is 0; or 9, 11 and/or 15 ester derivatives of said compound of formula I, e.g. a C1 to C6 alkyl ester derivative; or a pharmaceutically acceptable salt thereof. In a further aspect, the present invention relates to an ophthalmic solution comprising a therapeutically effective amount of a compound of formula (I), wherein the symbols have the above meanings, in admixture with a non-toxic, ophthalmically acceptable liquid vehicle, packaged in a container suitable for metered application.

    摘要翻译： 本发明涉及使用ω-链修饰的前列腺素作为眼压降低。 根据本发明使用的衍生物包括下列结构式I：其中阴影线段代表α键; 波浪段表示α或β键; 虚线表示双键或单键; X选自-OR和N（R2）; Y为= O或表示2个氢原子，条件是当X为OH时，Y表示2个氢原子; R是氢或具有至多6个碳原子的低级烷基; R1为= O或羟基; m为0,2,4或6，条件是当波浪段代表β键时m不为4; n为0,2,4或6; x和y为0或1，条件是当y为0时x为1，当x为0时y为1; 或所述式I化合物的9,11和/或15酯衍生物，例如。 C1-C6烷基酯衍生物; 或其药学上可接受的盐。 在另一方面，本发明涉及一种眼用溶液，其包含治疗有效量的式（I）化合物，其中符号具有上述含义，与无毒的眼科可接受的液体载体混合，包装在 适用于计量应用的容器。

    Prostanoic acid derivatives as agents for lowering intraocular pressure
    9.
    发明授权
    Prostanoic acid derivatives as agents for lowering intraocular pressure 有权
    前列腺酸衍生物作为降低眼内压的药物

    公开(公告)号：US06531504B2

    公开(公告)日：2003-03-11

    申请号：US09859770

    申请日：2001-05-17

    申请人： Robert M. Burk ,  Todd S. Gac

    发明人： Robert M. Burk ,  Todd S. Gac

    IPC分类号： A61K315575

    CPC分类号： C07D333/62 ,  A61K31/381 ,  A61K31/5575 ,  C07D333/28 ,  C07D333/60

    摘要： 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.

    摘要翻译： 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。