C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
260/302, 260/266
C07C 271/10 (2006.01) C07D 215/56 (2006.01) C07D 285/10 (2006.01) C07D 401/04 (2006.01) C07D 417/04 (2006.01)
Patent
CA 1330995
TITLE OF THE INVENTION (ACYLOXYALKOXY) CARBONYL DERIVATIVES AS BIOREVERSIBLE PRODRUG MOIETIES FOR PRIMARY AND SECONDARY AMINE FUNCTIONS IN DRUGS ABSTRACT OF THE INVENTION This invention relates to novel (acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs having a primary or secondary amine function thereon. Hydrolytic enzymes are used to trigger the regeneration of the parent amine drug of the carbamate prodrug moiety. The case also contains pharmaceutical composition, method of treatment and process claims. The novel (acyloxy alkoxy) carbonyl derivatives of the present invention are of the following formula: Image wherein RR'N represents a primary or secondary amine pharmaceutical; R1 and R2 are the same or different and are selected from the group consisting of hydrogen, and substituted C1-6alkyl or alkyl wherein the substituents are carboxy or C1-5alkoxy carbonyl with the proviso that R1 and R2 cannot be hydrogen at the same time, R3 is selected from the group consisting of C1-20 alkyl C2-20 alkenyl C2-5 alkynyl aryl selected from phenyl C6-8 aralkyl C3-8 cycloalkyl C3-10 cycloalkenyl carboxy C2-20 alkyl carboxy C5-20 cycloalkyl halo (C2-20) alkyl (C1-5) alkoxy (C2-10) carbonyl alkyl C2-20 alkyl sulfoxide carbamyl C2-20 alkyl carbamyl C2-20 aralkyl heterocyclics selected from the group consisting of furyl, morpholinyl, oxazolidinyl and 1,2,5-thiazolyl.
457139
Goudreau Gage Dubuc
Merck & Co. Inc.
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