Global Patent Index - EP 1569648 A4

EP 1569648 A4 20061004 - PRODRUGS FOR USE A OPHTHALMIC AGENTS

Title (en)

PRODRUGS FOR USE A OPHTHALMIC AGENTS

Title (de)

PRODRUGS FÜR OPHTHALMIKA

Title (fr)

PRODROGUES UTILISEES COMME AGENTS OPHTALMIQUES

Publication

EP 1569648 A4 20061004 (EN)

Application

EP 03796804 A 20031209

Priority

  • US 0338987 W 20031209
  • US 43235402 P 20021209
  • US 40541303 A 20030401

Abstract (en)

[origin: WO2004069248A1] The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcorneal penetration and are readily reduced into parent phenolic A-ring steroid compounds to provide protection or treatment against various ocular symptoms and disorders. The compounds according to the subject invention appear to be highly advantageous as prodrugs to provide protection and/or treatment against ocular disorders. These prodrugs confer lipid solubility optimal for transocorneal penetration and are readily converted to endogenous reducing agents into active phenolic A-ring steroid compounds. To the extent that these prodrugs have reduced feminizing effects and systemic toxicity, they would be expected to be quite advantageous for protecting or treating the eye against ocular disorders such as cataract or glaucoma without undesired (systemic) side effects).

IPC 8 full level

A61K 31/47 (2006.01); A61K 31/565 (2006.01); A61K 31/566 (2006.01); A61K 31/567 (2006.01)

CPC (source: EP)

A61K 31/565 (2013.01); A61K 31/566 (2013.01); A61P 27/02 (2017.12); C07J 1/0059 (2013.01)

Citation (search report)

  • [PXPY] WO 03084978 A1 20031016 - UNIV FLORIDA [US], et al
  • [Y] WO 0236605 A2 20020510 - UNIV WASHINGTON [US]
  • [Y] DE 19654750 A1 19980702 - ZANDER HELMUT DR MED [DE]
  • [Y] US 5041434 A 19910820 - LUBKIN VIRGINIA [US]
  • [A] US 2910486 A 19591027 - JAMES JIU
  • [A] US 5646136 A 19970708 - PETROW VLADIMIR [US], et al
  • [PY] PROKAI L ET AL: "CHEMICAL SHIELD MECHANISM FOR ESTROGEN NEUROPROTECTION: STEROIDAL QUINOLS AS NEW MOLECULE LEADS", AMERICAN CHEMICAL SOCIETY. ABSTRACTS OF PAPER. AT THE NATIONAL MEETING, AMERICAN CHEMICAL SOCIETY, WASHINGTON, DC, US, vol. 225, no. 1/2, 23 March 2003 (2003-03-23) - 27 March 2003 (2003-03-27), XP008042778, ISSN: 0065-7727
  • [PY] PROKAI L: "QUINOL-BASED METABOLIC CYCLE FOR ESTROGENS IN RAT LIVER MICROSOMES", DRUG METABOLISM AND DISPOSITION, WILLIAMS AND WILKINS., BALTIMORE, MD, US, vol. 31, no. 6, June 2003 (2003-06-01), pages 701 - 704, XP008042777, ISSN: 0090-9556
  • [Y] BIGSBY R M ET AL: "Protective effects of estrogen in a rat model of age-related cataracts", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF USA, NATIONAL ACADEMY OF SCIENCE, WASHINGTON, DC, US, vol. 96, August 1999 (1999-08-01), pages 9328 - 9332, XP002980815, ISSN: 0027-8424
  • [A] MCKINNEY K A ET AL: "Hormone replacement therapy and the eye", JOURNAL OF THE BRITISH MENOPAUSE SOCIETY, BRITISH MENOPAUSE SOCIETY, MARLOW, GB, vol. 6, no. 1, 2000, pages 15 - 17, XP002980814, ISSN: 1362-1807
  • See references of WO 2004069248A1

Designated contracting state (EPC)

AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LI LU MC NL PT RO SE SI SK TR

DOCDB simple family (publication)

WO 2004069248 A1 20040819; AU 2003297739 A1 20040830; AU 2003297739 A8 20040830; EP 1569648 A1 20050907; EP 1569648 A4 20061004

DOCDB simple family (application)

US 0338987 W 20031209; AU 2003297739 A 20031209; EP 03796804 A 20031209