Global Patent Index - EP 1343494 A4

EP 1343494 A4 20050803 - TETRAPARTATE PRODRUGS

Title (en)

TETRAPARTATE PRODRUGS

Title (de)

TETRAPARTAT-PRODRUGS

Title (fr)

PROMEDICAMENTS TETRAPARTATES

Publication

EP 1343494 A4 20050803 (EN)

Application

EP 01987164 A 20011130

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

A61K 31/21; A61K 31/33; A61K 31/765; A61K 38/02

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)

Citation (search report)

  • No further relevant documents disclosed
  • See references of WO 0243663A2

Citation (examination)

  • US 2001031873 A1 20011018 - GREENWALD RICHARD B [US], et al
  • SENTER P.D. ET AL: "POLY(ETHYLENE GLYCOL)-DOXURUBICIN CONJUGATES CONTAINING-LACTAMASE-SENSITIVE LINKERS", BIOCONJUGATE CHEMISTRY, vol. 6, no. 4, 1 July 1995 (1995-07-01), ACS, WASHINGTON, DC, US, pages 389 - 394, XP000517227
  • PECHAR ET AL: "Poly(ethylene glycol) multiblock copolymer as a carrier of anti-cancer drug doxorubicin.", BIOCONJUGATE CHEMISTRY, vol. 11, 15 February 2000 (2000-02-15), pages 131 - 139, XP002961562
  • GREENWALD ET AL: "Poly(ethylene glycol) conjugates drugs and prodrugs: a comprehensive review", CRITICAL REVIEWS IN THERAPEUTIC DRUG CARRIER SYSTEMS, vol. 17, 2000, pages 101 - 161
  • CONOVER ET AL: "Camptothecin delivery systems: the utility of amino acid spacers for the conjugation of camptothecin with polyethylene glycol to create prodrugs.", ANTI-CANCER DRUG DESIGN, vol. 14, 1999, pages 499 - 506
  • BAURAIN ET AL: "Amino acid and dipeptide derivatives of daunorubicin. 2. Cellular pharmacology and antitumor activity on L1210 leukemic cells in vitro and in vivo.", J. MED. CHEM., vol. 23, 1980, pages 1171 - 1174
  • BALIMANE ET AL: "Diret evidence for peptide transporter (PepT1)-Mediated Uptake of a nonpeptide prodrug, valacyclovir.", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, vol. 250, 1998, pages 246 - 251
  • HAN ET AL: "Cellular uptake mechanism of amino acid ester prodrugs in caco-2/hPEPT1 cells overexpressing a humna peptide transporter.", PHARMACEUTICAL RESEARCH, vol. 15, 1998, pages 1382 - 1386

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