C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 237/22 (2006.01) A61K 38/00 (2006.01) A61K 47/48 (2006.01) A61P 35/00 (2006.01) C07C 69/96 (2006.01) C07C 271/16 (2006.01) C07C 271/22 (2006.01) C07D 207/16 (2006.01) C07D 213/68 (2006.01)
Patent
CA 2309954
The present invention is directed to double prodrugs containing polymeric- based transport forms. These polymeric compounds comprise the formula (I), wherein: B is H, OH, OSiR13, a residue of an amine-containing target moiety or a residue of a hydroxyl-containing moiety; L1 and L2 are bifunctional linking moieties; Y2 is O or S; R2 is selected from the group consisting of C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloakyls, C1-6 substituted alkyls, C3-8 substituted cyloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy, and C1-6 heteroalkoxy; R9, R10, R13 are independently one of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy, and C1-6 heteroalkoxy; Ar is a moiety which when included in formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or one; and R11 is a polymer residue. The first prodrug is generated when the polymeric portion of the double prodrug is cleaved and the parent molecule is generated rapidly thereafter <u>in vivo</u>, as a result of a trialkyl lock type lactonization-type reaction.
L'invention porte sur des formes de transport à base de polymères à deux bioprécurseurs, de formule (I) dans laquelle: B est H, OH, OSiR¿13?, un résidu de fragment cible à contenu amine, ou un résidu de fragment à contenu hydroxy; L¿1? et L¿2? sont des fragments de liaison bifonctionnels; Y¿2? est O ou S; R¿2? est choisi parmi C¿1-6? alkyles, C¿3-12? alkyles ramifiés, C¿3-8? cycloalkyles, C¿1-6? alkyles substitués, C¿3-8? cycloalkyles substitués, aryles; aryles substitués, aralkyles, C¿1-6? hétéroalkyles; C¿1-6? hétéroalkyles substitués, C¿1-6? alkoxy, phénoxy, et C¿1-6? hétéroalkoxy; R¿9?, R¿10?, R¿13? sont indépendamment l'un de H, C¿1-6? alkyles, C¿3-12? alkyles ramifiés, C¿3-8? cycloalkyles, C¿1-6? alkyles substitués, C¿3-8? cycloalkyles substitués, aryles; aryles substitués, aralkyles, C¿1-6? hétéroalkyles; C¿1-6? hétéroalkyles substitués, C¿1-6? alkoxy, phénoxy, et C¿1-6? hétéroalkoxy; Ar est un fragment qui une fois inclus dans la formule (I) forme un hydrocarbure aromatique multisubstitué ou un groupe hétérocyclique multisubstitué; (m) est 0 ou 1; et R¿11? est un résidu polymère. Le premier bioprécurseur est produit lorsque la partie polymère du bioprécurseur double se scinde et que la molécule parente se forme rapidement in vivo comme résultat d'une réaction de lactonisation du type à blocage trialkyle.
Choe Yun E.
Greenwald Richard B.
Pendri Annapurna
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Enzon Inc.
LandOfFree
Trialkyl-lock-facilitated polymeric prodrugs of... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Trialkyl-lock-facilitated polymeric prodrugs of..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Trialkyl-lock-facilitated polymeric prodrugs of... will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-1399487