Hydroxy-and amino prodrugs

Details Hydroxy-and amino prodrugs Hydroxy-and amino prodrugs

C - Chemistry, Metallurgy

07

J

C07J 41/00 (2006.01) A61K 31/24 (2006.01) A61K 31/505 (2006.01) A61K 31/56 (2006.01) A61K 31/70 (2006.01) C07C 229/38 (2006.01) C07C 233/18 (2006.01) C07C 233/25 (2006.01) C07C 233/47 (2006.01) C07C 235/06 (2006.01) C07C 271/22 (2006.01) C07D 233/74 (2006.01) C07D 233/92 (2006.01) C07D 239/553 (2006.01) C07D 263/58 (2006.01) C07D 285/135 (2006.01) C07D 295/155 (2006.01) C07D 473/02 (2006.01) C07D 473/06 (2006.01) C07D 473/08 (2006.01) C07D 473/18 (2006.01) C07D 487/04 (2006.01) C07H 17/08 (2006.01) C07H 19/

Patent

CA 2045591

2045591 9008128 PCTABS00001 Compounds of formula (I), wherein D represents the dehydrogenated residue of a hydroxyl group-containing drug or the dehydrogenated residue of an NH-acidic group-containing drug; the substituents in the phenyl ring .alpha. and .beta. are in either meta- or para-position to each other; and the phenyl ring additionally may be substituted; m is an integer of 0 or 1; p is an integer of 0 or 1; n is an integer from 1 to 4; R1 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl, a group having the formula -COOR5, wherein R5 is an alkyl or aralkyl group, or a carbamoyl group of the formula -CONR6R7, wherein R6 and R7 are the same or different and are hydrogen, an alkyl group, or together with the adjacent nitrogen atom form a 4-, 5-, 6-, or 7-membered heterocyclic ring; R2 is hydrogen or an alkyl group; R3 and R4 are the same or different and are hydrogen, or optionally substituted alkyl, aralkyl, alkenyl or cycloalkyl; or R3 and R4 are combined so that -NR3R4 forms an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from nitrogen, oxygen, and sulfur; with the proviso that m is 0 when D represents the dehydrogenated residue of a hydroxyl group-containing drug and m is 1 when D represents the dehydrogenated residue of an NH-acidic group-containing drug; and the pharmaceutically acceptable acid addition salts or quaternary ammonium salts thereof.

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