Patent ID: 6586468
Filing Date: 2003-07-01
Classification: A61K,C07C

Abstract:
An &ohgr;-substituted phenyl-prostaglandin E derivative of formula (I) (whereinA is C2Ëœ8 alkylene, C2Ëœ8 alkenylene, C1Ëœ4 alkylene-phenylene or C2Ëœ4 alkenylene-phenylene, R1 is hydroxy, C1Ëœ6 alkyloxy, C1Ëœ6 alkyloxy-C1Ëœ6 alkyloxy, HOâ€”C1Ëœ6 alkyloxy or a formula of NR6R7 (wherein R6 and R7 are each independently hydrogen atom or C1Ëœ4 alkyl), R2 is oxo, halogen or a group of formula R8â€”COOâ€” (wherein R8 is hydrogen, C1Ëœ4 alkyl, phenyl or phenyl(C1Ëœ4 alkyl), C1Ëœ4 alkyloxy, HOOCâ€”C1Ëœ4 alkyl, C1Ëœ4 alkyloxy-carbonyl-C1Ëœ4 alkyl, HOOCâ€”C2Ëœ4 alkenyl or C1Ëœ4 alkyloxy-carbonyl-C2Ëœ4 alkenyl), R3 is hydrogen or hydroxy, R4 is C1Ëœ4 alkylene, R5 is phenyl substituted by the following groups: i) 1Ëœ3 groups selected from C1Ëœ4 alkyloxy-C1Ëœ4 alkyl, C2Ëœ4 alkenyloxy-C1Ëœ4 alkyl, C2Ëœ4 alkynyloxy-C1Ëœ4 alkyl, C3Ëœ7 cycloalkyloxy-C1Ëœ4 alkyl, C3Ëœ7 cycloalkyl(C1Ëœ4 alkyloxy)-C1Ëœ4 alkyl, phenyloxy-C1Ëœ4 alkyl, phenyl-C1Ëœ4 alkyloxy-C1Ëœ4 alkyl, C1Ëœ4 alkylthio-C1Ëœ4 alkyl, C2Ëœ4 alkenylthio-C1Ëœ4 alkyl; C2Ëœ4 alkynylthio-C1Ëœ4 alkyl; C3Ëœ7 cycloalkylthio-C1Ëœ4 alkyl, C3Ëœ7 cycloalkyl(C1Ëœ4 alkylthio)-C1Ëœ4 alkyl, phenylthio-C1Ëœ4 alkyl and phenyl-C1Ëœ4 alkylthio-C1Ëœ4 alkyl, ii) C1Ëœ4 alkyloxy-C1Ëœ4 alkyl and C1Ëœ4 alkyl, C1Ëœ4 alkyloxy-C1Ëœ4 alkyl and C1Ëœ4 alkyloxy, C1Ëœ4 alkyloxy-C1Ëœ4 alkyl and hydroxy, C1Ëœ4 alkyloxy-C1Ëœ4 alkyl and halogen, C1Ëœ4 alkylthio-C1Ëœ4 alkyl and C1Ëœ4 alkyl, C1Ëœ4 alkylthio-C1Ëœ4 alkyl and C1Ëœ4 alkyloxy, C1Ëœ4 alkylthio-C1Ëœ4 alkyl and hydroxy or C1Ëœ4 alkylthio-C1Ëœ4 alkyl and halogen iii) mono halo-C1Ëœ4 alkyl or hydroxy-C1Ëœ4 alkyl, or iv) C1Ëœ4 alkyl and hydroxy; and wherein is a bond or a double bond, and when R2 is R8â€”COOâ€”, R8 is C1Ëœ6 alkyloxy, C1Ëœ6 alkyloxy-C1Ëœ6 alkyloxy or HOâ€”C1Ëœ6 alkyloxy and the bond in the 8-9 position is a double bond),a non-toxic salt thereof or a cyclodextrin clathrate thereof.