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31. 发明授权

US06767920B2 3, 7 or 3 and 7 thia or oxa prostanoic acid derivatives as agents for lowering intraocular pressure 失效
标题翻译： 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
公开(公告)号：US06767920B2
公开(公告)日：2004-07-27
申请号：US10346828
申请日：2003-01-16
申请人： Robert M. Burk , Mark Holoboski , Mari F. Posner
发明人： Robert M. Burk , Mark Holoboski , Mari F. Posner
IPC分类号： A61K315575
CPC分类号： A61K31/559 , A61K31/5575 , Y10S514/913
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, 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.
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。

32. 发明授权

US06586462B2 &ohgr;-Cycloalkyl 17-heteroaryl prostaglandin E2 analogs as EP2-receptor agonists 有权
标题翻译： ω-环烷基17-杂芳基前列腺素E2类似物作为EP2-受体激动剂
公开(公告)号：US06586462B2
公开(公告)日：2003-07-01
申请号：US10104433
申请日：2002-05-24
申请人： Robert M. Burk , Mark Holoboski , Mari F. Posner
发明人： Robert M. Burk , Mark Holoboski , Mari F. Posner
IPC分类号： A61K3138
CPC分类号： A61K31/38 , A61K31/41 , C07D333/16 , C07D333/22
摘要： The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an &agr; bonds, the solid triangle represents a &bgr; bond, the wavy segments represent &agr; or &bgr; bond, dashed lines represent a double bond or a single bond R, , R1, R2 and R3 are as defined in the specification.
摘要翻译：本发明涉及E型前列腺素衍生物作为EP2激动剂的用途，一般而言，特别是作为眼睛低血压剂。根据本发明使用的PGE衍生物由下式I表示：其中阴影线段表示α键，实心三角形表示β键，波浪段表示α或β键，虚线表示双键或单键R 1，R 1，R 2和R 3如本说明书中所定义。

33. 发明授权

US06410591B1 3,7 or 3 and 7 thia or oxa prostanoic acid derivatives as agents for lowering intraocular pressure 失效
标题翻译： 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
公开(公告)号：US06410591B1
公开(公告)日：2002-06-25
申请号：US09851296
申请日：2001-05-08
申请人： Robert M. Burk , Mark Holoboski , Mari F. Posner
发明人： Robert M. Burk , Mark Holoboski , Mari F. Posner
IPC分类号： A01N3708
CPC分类号： C07C405/0033 , A61K31/5575
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 a therapeutically effective amount of a 3, 7 or 3 and 7 thia or oxa prostanoic acid derivative.
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3,7或3和7和硫代前列腺酸衍生物。

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