Treatment of ocular hypertension and glaucoma

A process for the long-term treatment or prophylactic management of ocular hypertension or glaucoma in a human patient by topical ocular administration of a therapeutically effective amount of a prostaglandin related compound, the improvement to eliminate or reduce potential pigmentation of the iris of a treated eye occurring by long-term topical ocular application of a prostaglandin related compound, wherein the compound used has the formula (I)

• 6
• wherein W1, W2 and W3 are carbon or oxygen atoms,
• L, M and N are hydrogen atom, hydroxy, halogen atom, lower alkyl, lower alkoxy, hydroxy(lower)alkyl, or oxo, wherein at least one of L and M is a group other than hydrogen, and the five-membered ring may have at least one double bond;
• A is —CH2OH, —COCH2OH, —COOH or a functional derivative thereof;
• B is single bond, —CH2—, —CH2—CH2—, —CH═CH—, —C≡C—, —CH2—CH2—CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —C≡—C—CH2—, or —CH2—C≡C—;
• R1 is a saturated or unsaturated bivalent lower or medium aliphatic hydrocarbon residue, which is unsubstituted or substituted with halogen, an alkyl group, hydroxy, oxo, aryl or heterocyclic group;
• and
• Ra is a saturated or unsaturated lower or medium aliphatic hydrocarbon residue, which is unsubstituted or substituted with halogen atom, oxo, hydroxy, lower alkyl, lower alkoxy, lower alkanoyloxy, cyclo(lower)alkyl, cyclo(lower)alkyloxy, aryl, aryloxy, heterocyclic group or heterocyclic-oxy group;
• cyclo(lower)alkyl;
• cyclo(lower)alkyloxy;
• aryl;
• aryloxy;
• heterocyclic group;
• or heterocyclic-oxy group.

A process for the long-term treatment or prophylactic management of ocular hypertension or glaucoma in a human patient by topical ocular administration of a therapeutically effective amount of a prostaglandin related compound, the improvement to eliminate or reduce potential pigmentation of the iris of a treated eye occurring by long-term topical ocular application of a prostaglandin related compound, wherein the compound used has the formula (III)

• 7
• wherein W1, W2 and W3 are carbon or oxygen atoms,
• L, M and N are hydrogen atom, hydroxy, halogen atom, lower alkyl, lower alkoxy, hydroxy(lower)alkyl, or oxo, wherein at least one of L and M is a group other than hydrogen, and the five-membered ring may have at least one double bond;
• A is —CH2OH, —COCH2OH, —COOH or a functional derivative thereof;
• B is single bond, —CH2—, —CH2—CH2—, —CH═CH—, —C≡C—,—CH2—CH2—CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —C≡C—CH2—, or —CH2—C≡C—;
• R1is a saturated or unsaturated bivalent lower or medium aliphatic hydrocarbon residue, which is unsubstituted or substituted with halogen, an alkyl group, hydroxy, oxo, aryl or heterocyclic group
• Z is
• 8
• wherein R4 and R5 are hydrogen atom, hydroxy, halogen atom, lower alkyl, lower alkoxy or hydroxy(lower)alkyl, wherein R4 and R5 are not hydroxy, lower alkoxy and/or hydroxy (lower) alkyl at the same time;
• and
• Ra′ is a saturated or unsaturated C5-C10 aliphatic hydrocarbon residue, which is unsubstituted or substituted with halogen atom, oxo, hydroxy, lower alkyl, lower alkoxy, lower alkanoyloxy, cyclo(lower)alkyl, cyclo(lower)alkyloxy, aryl, aryloxy, heterocyclic group or heterocyclic-oxy group;
• cyclo(lower)alkyl;
• cyclo(lower)alkyloxy;
• aryl;
• aryloxy;
• heterocyclic group;
• or heterocyclic-oxy group.