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1. WO2014170704 - DEUTERATED MORPHINE DERIVATIVES

Publication Number WO/2014/170704
Publication Date 23.10.2014
International Application No. PCT/HU2014/000030
International Filing Date 14.04.2014
Chapter 2 Demand Filed 14.11.2014
IPC
C07D 489/02 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
489Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro furan ring systems, e.g. derivatives of -morphinan of the formula:
02with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
A61K 31/485 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
485Morphinan derivatives, e.g. morphine, codeine
A61P 25/04 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
A61P 11/14 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
14Antitussive agents
C07B 59/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
59Introduction of isotopes of elements into organic compounds
CPC
A61K 31/485
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
485Morphinan derivatives, e.g. morphine, codeine
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 11/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
14Antitussive agents
A61P 25/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
C07D 489/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
489Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
C07D 489/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
489Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
02with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
Applicants
  • SZEGEDI TUDOMÁNYEGYETEM [HU]/[HU]
Inventors
  • FÜLÖP. Ferenc
  • MÁNDITY, István
Agents
  • SBGK PATENT AND LAW OFFICES
Priority Data
P130022115.04.2013HU
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) DEUTERATED MORPHINE DERIVATIVES
(FR) DÉRIVÉS DE MORPHINE DEUTÉRÉS
Abstract
(EN) The invention relates to new morphine derivatives deuterated at the 7,8-position of the morphine ring, furthermore to a process for the preparation thereof, and to pharmaceutical compositions comprising them. The new deuterated morphine derivatives show high and selective μ-opioid receptor binding activity leading to the benefit of higher analgesic activity at lower dosages inducing thereby reduced adverse effects compared to the hydrogenated derivatives. The compounds of the invention are useful for example in the treatment of pain or can be used as antitussive agents with a reduced risk of the possibility of drug abuse.
(FR) L'invention concerne de nouveaux dérivés de morphine deutérés au niveau de la position 7,8 du cycle de morphine. L'invention concerne en outre un procédé pour leur préparation et des compositions pharmaceutiques les comprenant. Les nouveaux dérivés de morphine deutérée montrent une activité élevée et sélective de liaison à des récepteurs µ-opioïdes entraînant les bénéfices d'une meilleure activité analgésique à des doses plus faibles induisant de ce fait une baisse des effets indésirables comparativement aux dérivés hydrogénés. Les composés de l'invention sont utiles par exemple dans le traitement de la douleur ou peuvent être utilisés comme agents antitussifs présentant un risque réduit de surconsommation de médicament.
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