发明名称 Polar C-1 esters of prostaglandins
摘要 The present invention provides a method of treating ocular hypertension which comprises applying to the eye an amount sufficient to treat ocular hypertension of a compound of formula (I) (* CHEMICAL STRUCTURE *) (I) wherein the wavy line attachments indicate either alpha ((alpha)) or beta ((beta)) configuration; hatched lines indicate (alpha) configuration, solid triangles are used to indicate (beta) configuration; the dashed bonds represent a single bond or a double bond which can be in the cis or trans configuration; X is selected from the group consisting of O, NH, S and NR, where R is an aliphatic hydrocarbon group of about 1 to about 6 carbon atoms; Y is a polar functional group; one of R1 and R2 is =O, -OH or a -O(CO)R4 group, and the other one is -OH or a -O(CO)R4 group or R1 is =O and R2 is is H; R3 is -OH or -O(CO)R4, wherein R4 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or -(CH2)nR5 wherein n is 0-10, and R5 is an aliphatic ring from about 3 to about 7 carbon atoms, or an aromatic or heteroaromatic ring; or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions including an effective amount of the compound of formula I or a pharmaceutically-acceptable salt thereof, in admixture with a nontoxic pharmaceutical carrier and ophthalmic solutions comprising a compound of formula I packaged for metered application. Finally, novel compounds according to Formula I are disclosed.
申请公布号 US5288754(A) 申请公布日期 1994.02.22
申请号 US19920831023 申请日期 1992.02.04
申请人 ALLERGAN, INC. 发明人 WOODWARD, DAVID F.;CHAN, MING F.
分类号 A61K31/557;C07C405/00;(IPC1-7):A61K31/557 主分类号 A61K31/557
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