Patent ID: 6294680
Filing Date: 2001-09-25
Classification: A61P,C07D,C07F

Abstract:
A compound of formula II, ##STR6##wherein R.sub.1, and R.sub.2, are independently selected from the group consisting of a hydrogen atom, a hydroxyl, C.sub.1-10 alkyl and C.sub.6-14 aryl and C.sub.6-14 arylC.sub.1-3 alkyl, and wherein R.sub.3 is R.sub.9 -C.dbd.O or hydrogen, and wherein each of R.sub.9, R.sub.4 and R.sub.5 are independently selected from the group consisting of:(1) C.sub.1-15 alkyl, straight or branched,(2) C.sub.3-15 cycloalkyl,(3) C.sub.2-15 alkenyl, straight or branched,(4) C.sub.2-15 alkynyl, straight or branched,(5) phenyl and(6) phenylC.sub.1-6,alkyl-and R.sub.9 may also be each of the definitions mentioned under (1) to (6) substituted with one or more of the substituents independently selected from the group consisting of halogen, C1-6alkyl, C.sub.1-6,alkoxy and C.sub.6-14 aryl, and R.sub.4 and R.sub.5 may also be hydrogen or form with the nitrogen to which they are attached, a 5, 6 or 7 membered heterocycle moiety, and wherein R.sub.6 and R.sub.7 are also independently selected from the group consisting of:(1) a dioxane moiety, ##STR7##wherein R.sub.10 and R.sub.11 are independently selected from the group consisting of:(1) C.sub.1-15 alkyl, straight or branched,(2) C.sub.3-15 cycloalkyl,(3) C.sub.2-15 alkenyl, straight or branched,(4) C.sub.2-15,alkynyl, straight or branched,(5) phenyl, and(6) phenylC.sub.1-6 alkyl-,all optionally substituted with one or more of the substituents independently selected from the group consisting of halogen C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.6-14 aryl,(7) hydrogen, with the proviso that R.sub.10 is not hydrogen,(8) R.sub.10 and R.sub.11 form an optionally substituted 5, 6, 7 or 8 membered cyclic moiety, in which one or more of the substituents; is selected from the group consisting of halogen and a lower alkyl in any combination,(2) a cyclic sulfate, ##STR8##(3) or a cyclic phosphate,in which R.sub.12 is selected from the group consisting of: ##STR9##(1) C.sub.1-15 alkyl, straight or branched,(2) C.sub.3-15 cycloalkyl,(3) phenyl,(4) phenylC.sub.1-6 alkyl-,(5) hydrogen,(6) primary amines, and(7) secondary amines, and with the proviso that when R.sub.3 is hydrogen, R.sub.6 and R.sub.7 may also form a(1) borylidene group, ##STR10##in which R.sub.8 is a phenyl optionally substituted by one to five substituents, halogen or lower alkyl in any combination, or (2) R.sub.6 and R.sub.7 are both hydrogen,and wherein the dotted lines at x, y and z represent possible double bonds, when any are present, being either x and z in combination or x, y or z alone or none; or a corresponding stereoisomer thereof.