EP 1343494 A2 20030917 - TETRAPARTATE PRODRUGS
Title (en)
TETRAPARTATE PRODRUGS
Title (de)
TETRAPARTAT-PRODRUGS
Title (fr)
PROMEDICAMENTS TETRAPARTATES
Publication
Application
Priority
- US 0145127 W 20011130
- US 72851200 A 20001201
- US 75899301 A 20010112
Abstract (en)
[origin: WO0243663A2] A compound of Formula I, providing a tetrapartate prodrugs is provided, wherein L1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be delivered into a cell; Z is covalently linked to [D]y, wherein Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof; Y1, Y2, Y3 and Y4 are each independently O, S, or NR12; R11 is a mono- or divalent polymer residue; R1, R4, R9, R10 and R12 are independently selected from the group consisting 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 and substituted C1-6 heteroalkyls; R2, R3, R5 and R6 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C1-6 alkoxy, phenoxy, C1-8 heteroalkyls, C1-8 heteroalkoxy, substituted C1-6 alkyls, C3-8 cycloalkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, halo-, nitro- and cyano-, carboxy-, C1-6 carboxyalkyls and C1-6 alkylcarbonyls; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; (m), (r), (s), (t), and (u) are independently zero or one; (p) is zero or a positive integer; and (y) is 1 or 2; together with methods of preparing and using these new tetrapartate prodrugs.
IPC 1-7
IPC 8 full level
A61K 31/4745 (2006.01); A61K 31/65 (2006.01); A61K 31/704 (2006.01); A61K 47/48 (2006.01); A61P 35/00 (2006.01); A61P 43/00 (2006.01); C08G 65/329 (2006.01)
CPC (source: EP)
A61K 47/60 (2017.07); A61P 35/00 (2017.12); A61P 43/00 (2017.12)
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR
DOCDB simple family (publication)
WO 0243663 A2 20020606; WO 0243663 A3 20020725; AU 3940502 A 20020611; CA 2428018 A1 20020606; EP 1343494 A2 20030917; EP 1343494 A4 20050803; JP 2004518776 A 20040624
DOCDB simple family (application)
US 0145127 W 20011130; AU 3940502 A 20011130; CA 2428018 A 20011130; EP 01987164 A 20011130; JP 2002545642 A 20011130