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1. WO2011088140 - PEGYLATED OPIOIDS WITH LOW POTENTIAL FOR ABUSE AND SIDE EFFECTS

Publication Number WO/2011/088140
Publication Date 21.07.2011
International Application No. PCT/US2011/021017
International Filing Date 12.01.2011
IPC
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
075
Ethers or acetals
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
47
Quinolines; Isoquinolines
485
Morphinan derivatives, e.g. morphine, codeine
A61K 31/00 (2006.01)
A61K 31/075 (2006.01)
A61K 31/485 (2006.01)
CPC
A61K 31/075
A61K 31/485
Applicants
  • NEKTAR THERAPEUTICS [US/US]; 455 Mission Bay Boulevard South Suite 100 San Francisco, CA 94158, US (AllExceptUS)
  • JUDE-FISHBURN, C., Simone [GB/US]; US (UsOnly)
  • RILEY, Timothy, A. [US/US]; US (UsOnly)
  • ZACARIAS, Alberto, N. [US/US]; US (UsOnly)
  • GURSAHANI, Hema [US/US]; US (UsOnly)
Inventors
  • JUDE-FISHBURN, C., Simone; US
  • RILEY, Timothy, A.; US
  • ZACARIAS, Alberto, N.; US
  • GURSAHANI, Hema; US
Agents
  • MARQUART, Timothy, A.; Nektar Therapeutics 455 Mission Bay Boulevard South Suite 100 San Francisco, CA 94158, US
Priority Data
61/294,45712.01.2010US
61/320,29901.04.2010US
61/334,55913.05.2010US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PEGYLATED OPIOIDS WITH LOW POTENTIAL FOR ABUSE AND SIDE EFFECTS
(FR) OPIOÏDES PÉGYLÉS À FAIBLE POTENTIEL D'ABUS ET D'EFFETS SECONDAIRES
Abstract
(EN)
Provided are methods for reducing the addiction potential and/or reducing one or more CNS-side effects related to the administration of an opioid analgesic drug by administering the opioid analgesic drug in the form of an oligomeric polyethylene glycol conjugate compound. The compounds provided demonstrate notably reduced potential for substance abuse, and possess altered pharmacokinetic profiles relative to the opioid agonists alone, but are not subject to the risk of physical tampering that allows for the recovery and abuse of the opioid agonist associated with certain alternative delivery formulations.
(FR)
L'invention concerne des procédés de réduction du potentiel d'addiction et/ou de réduction d'un ou plusieurs effet(s) secondaires sur le SNC liés à l'administration d'un médicament analgésique opioïde par l'administration du médicament analgésique opioïde sous la forme d'un composé conjugué de polyéthylène glycol oligomère. Les composés décrits démontrent un potentiel remarquablement réduit d'abus de substance et possèdent des profils pharmacocinétiques altérés par rapport aux agonistes opioïdes seuls, mais ne sont pas soumis au risque d'adultération physique qui permet la récupération et l'abus de l'agoniste opioïde associé à certaines formulations alternatives d'administration.
Also published as
Latest bibliographic data on file with the International Bureau