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    • 8. 发明申请
    • CO-CYCLOALKYL 17-HETEROARYL PROSTAGLANDIN E2 ANALOGS AS EP2-RECEPTOR AGONISTS
    • CO-CYCLOALKYL 17-HETEROARYL PROSTAGLANDIN E2模拟物作为EP2受体激动剂
    • WO2003037433A1
    • 2003-05-08
    • PCT/US2001/028609
    • 2001-10-26
    • ALLERGAN, INC.
    • BURK, Robert, M.HOLOBOSKI, MarkPOSNER, Mari, F.
    • A61P27/06
    • C07D333/24A61K31/559
    • 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.
    • 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。