Global Patent Index - EP 1267898 A4

EP 1267898 A4 20060201 - BILE ACID CONTAINING PRODRUGS WITH ENHANCED BIOAVAILABILITY

Title (en)

BILE ACID CONTAINING PRODRUGS WITH ENHANCED BIOAVAILABILITY

Title (de)

GALLENSÄURE ENTHALTEND PROPHARMAKA MIT ERHÖHTER BIOAVIBILITÄT

Title (fr)

PROMEDICAMENTS CONTENANT UN ACIDE BILIAIRE ET PRESENTANT UNE MEILLEURE BIODISPONIBILITE

Publication

EP 1267898 A4 20060201 (EN)

Application

EP 01926709 A 20010406

Priority

  • US 0111327 W 20010406
  • US 19585400 P 20000407
  • US 26990601 P 20010221

Abstract (en)

[origin: WO0176531A2] Many compounds have poor bioavailability or variable bioavailability because of poor absorption of the compound in the small intestine. Conjugation of the compound with bile acid to form a prodrug will increase the bioavailibility of the compound and/or reduce the bioavailability variability of the compound because of the active transport of the prodrug by the intestinal bile acid transporter and because of increased lipophilic nature of the prodrug. A linker group can be used between the bile acid and the compound. One example of a bile acid containing prodrug is acyclovir valylchenodeoxycholate, where valine is the linker group. Another example of this prodrug is atenolol cholic acid amide.

IPC 1-7

A61K 35/50; A61K 39/40; A61K 39/42; A61K 39/44; A61K 39/395; C07J 43/00; C07J 9/00; C07J 41/00; A61P 31/12

IPC 8 full level

A61K 47/48 (2006.01); A61K 31/165 (2006.01); A61K 31/522 (2006.01); A61K 31/575 (2006.01); A61K 31/58 (2006.01); A61K 35/50 (2006.01); A61K 39/395 (2006.01); A61K 39/40 (2006.01); A61K 39/42 (2006.01); A61K 39/44 (2006.01); A61P 9/04 (2006.01); A61P 31/12 (2006.01); A61P 43/00 (2006.01); C07J 9/00 (2006.01); C07J 41/00 (2006.01); C07J 43/00 (2006.01)

IPC 8 main group level

A61K (2006.01)

CPC (source: EP)

A61K 47/554 (2017.07); A61P 9/04 (2017.12); A61P 31/12 (2017.12); A61P 43/00 (2017.12); C07J 9/005 (2013.01); C07J 41/0061 (2013.01); C07J 43/003 (2013.01)

Citation (search report)

  • [X] WO 9912927 A1 19990318 - COMMW SCIENT IND RES ORG [AU], et al
  • [PX] WO 0120331 A1 20010322 - XENOPORT INC [US], et al
  • [PX] WO 0058337 A1 20001005 - KAROBIO AB [SE], et al
  • [X] KRAMER ET AL (ED PAUMGARTNER ET AL): "Bile Acids and the Hepatobiliary System (ISBN 0792388291)", 1993, KLUWER, DORDRECHT, NETHERLANDS, XP008056225
  • [X] KRAMER W ET AL: "Modified bile acids as carriers for peptides and drugs", JOURNAL OF CONTROLLED RELEASE, ELSEVIER, AMSTERDAM, NL, vol. 46, no. 1-2, 5 May 1997 (1997-05-05), pages 17 - 30, XP004096309, ISSN: 0168-3659
  • [X] KRAMER W ET AL: "LIVER-SPECIFIC DRUG TARGETING BY COUPLING TO BILE ACIDS", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY OF BIOLOCHEMICAL BIOLOGISTS, BIRMINGHAM,, US, vol. 267, no. 26, 15 September 1992 (1992-09-15), pages 18598 - 18604, XP000453577, ISSN: 0021-9258
  • [X] KRAMER W ET AL: "Bile acid derived HMG-CoA reductase inhibitors", BIOCHIMICA ET BIOPHYSICA ACTA - MOLECULAR BASIS OF DISEASE 1994 NETHERLANDS, vol. 1227, no. 3, 1994, pages 137 - 154, XP002355916, ISSN: 0925-4439
  • [X] STEPHAN Z F ET AL: "REDUCTION OF CARDIOVASCULAR AND THYROXINE-SUPPRESSING ACTIVITIES OFL-T3 BY LIVER TARGETING WITH CHOLIC ACID", BIOCHEMICAL PHARMACOLOGY, PERGAMON, OXFORD, GB, vol. 43, no. 9, 8 May 1992 (1992-05-08), pages 1969 - 1974, XP000982833, ISSN: 0006-2952
  • [X] SWAAN P W ET AL: "Enhanced transepithelial transport of peptides by conjugation to cholic acid", BIOCONJUGATE CHEMISTRY, ACS, WASHINGTON, DC, US, vol. 8, no. 4, 1997, pages 520 - 525, XP002158726, ISSN: 1043-1802
  • [X] MILLS C O ET AL: "BILIARY EXCRETION OF CHENODEOXYCHOLYLLYSYLRHODAMINE IN WISTAR RATS A POSSIBLE ROLE OF A BILE ACID AS A CARRIER FOR DRUGS", BIOCHIMICA ET BIOPHYSICA ACTA, vol. 1126, no. 1, 1992, pages 35 - 40, XP002355917, ISSN: 0006-3002
  • See references of WO 0176531A2

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 0176531 A2 20011018; WO 0176531 A3 20020214; AU 2001253226 B2 20060608; AU 2006202213 A1 20060615; AU 5322601 A 20011023; CA 2405151 A1 20011018; EP 1267898 A2 20030102; EP 1267898 A4 20060201; JP 2003530329 A 20031014

DOCDB simple family (application)

US 0111327 W 20010406; AU 2001253226 A 20010406; AU 2006202213 A 20060525; AU 5322601 A 20010406; CA 2405151 A 20010406; EP 01926709 A 20010406; JP 2001574050 A 20010406