SUBSTITUTED CYCLOPENTANES HAVING PROSTAGLANDIN ACTIVITY
    1.
    发明申请
    SUBSTITUTED CYCLOPENTANES HAVING PROSTAGLANDIN ACTIVITY 审中-公开
    具有PROSTAGLANDIN活性的取代环孢菌素

    公开(公告)号:WO2009100057A1

    公开(公告)日:2009-08-13

    申请号:PCT/US2009/032943

    申请日:2009-02-03

    发明人: BURK, Robert, M.

    CPC分类号: C07C405/00 C07C405/0008

    摘要: 11,15, 19-trihydroxy-9-halo-prostaglandin analogues and its use as ocular hypotensive agents. Ocular hypotensive agents are useful in the treatment of a number of various ocular hypertensive conditions, such as post-surgical and post-laser trabeculectomy ocular hypertensive episodes, glaucoma, and as presurgical adjuncts.

    摘要翻译: 11,15,19-三羟基-9-卤代 - 前列腺素类似物及其用作眼压降血压药。 眼部降血压药物可用于治疗许多各种眼部高血压病症,如手术后和激光后小梁切除术眼高压发作,青光眼,以及作为手术前辅助治疗。

    CO-CYCLOALKYL 17-HETEROARYL PROSTAGLANDIN E2 ANALOGS AS EP2-RECEPTOR AGONISTS
    8.
    发明申请
    CO-CYCLOALKYL 17-HETEROARYL PROSTAGLANDIN E2 ANALOGS AS EP2-RECEPTOR AGONISTS 审中-公开
    CO-CYCLOALKYL 17-HETEROARYL PROSTAGLANDIN E2模拟物作为EP2受体激动剂

    公开(公告)号:WO2003037433A1

    公开(公告)日:2003-05-08

    申请号:PCT/US2001/028609

    申请日:2001-10-26

    申请人: ALLERGAN, INC.

    IPC分类号: A61P27/06

    CPC分类号: C07D333/24 A61K31/559

    摘要: The invention relates to the use of derivatives of E-type prostaglandins as EP 2 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 α bonds, the solid triangle represents a β bond, the wavy segments represent a α or β bond, dashed lines represent a double bond or a single bond, R 3 is heteroaryl or a substituted heteroaryl radical, R 1 and R 2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO 2 R 4 , CONR 4 2?, CH 2 OR 4 , CONR 4 SO 2 R 4 , P(O)(OR 4 ) and wherein R 4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is O or an integer of from 1 to 4.

    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 3是杂芳基或取代的杂芳基,R 1和R 2独立地选自氢或具有至多6个碳原子的低级烷基或低级 具有至多6个碳原子的酰基,R选自CO 2 R 4,CONR 4,CH 2,或OR 4,CONR 4 SO 2 R 4,P(O )(OR 4),并且其中R 4选自H,苯基和具有1至6个碳原子且n为0或1至4的整数的低级烷基。