Use of cloprostenol and fluprostenol analogues to treat glaucoma and ocular hypertension

CAFC
  • US 5,889,052 A
  • Filed: 08/21/1997
  • Issued: 03/30/1999
  • Est. Priority Date: 08/03/1993
  • Status: Expired due to Term
First Claim
Patent Images

1. A method of treating glaucoma and ocular hypertension which comprises topically administering to the affected eye a composition comprising a therapeutically effective amount of a compound having the absolute stereochemical structure of the following formula (IV), and being substantially free of the enantiomer of said compound:

  • ##STR11## wherein;

    R1 =H;

    C1 -C12 straight-chain or branched alkyl;

    C1 -C12 straight-chain or branched acyl;

    C3 -C3 cycloalkyl;

    or a cationic salt moiety;

    R2, R3 =H, or C1 -C5 straight-chain or branched alkyl;

    or R2 and R3 taken together may represent O;

    X=O, S, or CH2 ;

    represents any combination of a single bond, or a cis or trans double bond for the alpha (upper) chain; and

    a single bond or trans double bond for the omega (lower) chain;

    R9 =H, C1 -C10 straight-chain or branched alkyl, or C1 -C10 straight-chain or branched acyl;

    R11 =H, C1 -C10 straight-chain or branched alkyl, or C1 -C10 straight-chain or branched acyl;

    Y=O;

    or H and OR15 in either configuration wherein R15 =H, C1 -C10 straightchain or branched alkyl, or C1 -C10 straight-chain or branched acyl; and

    Z=Cl or CF3 ;

    with the proviso that when R2 and R3 taken together represent O, then R1

    C1 -C12 straight-chain or branched acyl; and

    when R2 =R3 =H, then R1

    a cationic salt moiety; and

    with the further proviso that the following compound be excluded;

    cyclopentane heptenol-5-cis-2-(3-α

    hydroxy-4-m-chlorophenoxy-1-transbutenyl)-3,5 dihydroxy, 1.sub.α

    , 2.sub.β

    , 3.sub.α

    , 5.sub.α

    !.

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