3, 7 or 3 and 7 thia or oxa prostanoic acid derivatives as...

A - Human Necessities – 61 – K

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A61K 31/5575 (2006.01) A61K 31/19 (2006.01) A61K 31/192 (2006.01) A61K 31/215 (2006.01) A61K 31/216 (2006.01) A61P 27/02 (2006.01) A61P 27/06 (2006.01) C07C 405/00 (2006.01)

Patent

CA 2446386

The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula (I), wherein hatched lines represent the .alpha. configuration, a triangle represents the .beta. configuration and a dotted line represents the presence or absence of a double bond; A and B are independently selected from the group consisting of O, S and CH2 provided that at least one of A or B is S; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl and R3 is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl, or substituted derivatives thereof, wherein the substituents may be selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, CO2R and OR.

L'invention porte sur un procédé de traitement d'hypertension oculaire ou de glaucome consistant à administrer à un animal souffrant d'hypertension oculaire ou d'un glaucome une quantité thérapeutiquement efficace d'un composé représenté par la formule générale I dans laquelle les lignes hachurées représentent la configuration .alpha., un triangle représente la configuration .beta. et une ligne pointillée représente la présence ou l'absence d'une liaison double ; A et B sont indépendamment choisis dans le groupe O, S et CH¿2? à condition qu'au moins un A ou B soit S ; D représente une liaison covalente ou CH¿2?, O, S ou NH ; X est CO¿2?R, CONR¿2?, CH¿2?OR, P(O)(OR)¿2?, CONRSO¿2?R SONR¿2? ou Y est O, OH, OCOR?2¿, halogène ou cyano ; Z est CH¿2? ou une liaison covalente ; R est H ou R?2¿ ; R?1¿ est H, R?2¿, phényle ou COR?2¿ ; R?2¿ est C¿1?-C¿5? alkyle inférieur et R¿3? est C¿1?-C¿5? n-alkyle, C¿3?-C¿7? cycloalkyle, phényle, furanyle, thiényle, ou des dérivés substitués de ces derniers, les substituants pouvant être choisis dans le groupe C¿1?-C¿5? alkyle, halogène, CF¿3?, CN, NO¿2?, NR¿2?, CO¿2?R et OR.

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