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1. WO2020070099 - ADMINISTRATION OF CATECHOLAMINE PRODRUGS IN COMBINATION WITH A 5-HT2B ANTAGONIST

Publication Number WO/2020/070099
Publication Date 09.04.2020
International Application No. PCT/EP2019/076529
International Filing Date 01.10.2019
IPC
A61P 25/16 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
14for treating abnormal movements, e.g. chorea, dyskinesia
16Anti-Parkinson drugs
C07D 491/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02in which the condensed system contains two hetero rings
06Peri-condensed systems
A61K 31/47 2006.01
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
CPC
A61K 31/4741
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
4738ortho- or peri-condensed with heterocyclic ring systems
4741condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
A61P 25/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
14for treating abnormal movements, e.g. chorea, dyskinesia
16Anti-Parkinson drugs
C07D 491/056
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
056with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
Applicants
  • H. LUNDBECK A/S [DK]/[DK]
Inventors
  • FLAGSTAD, Peter
  • BREYSSE, Nathalie
  • CHRISTOFFERSEN, Claus, Tornby
  • JØRGENSEN, Morten
Priority Data
PA20180066002.10.2018DK
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ADMINISTRATION OF CATECHOLAMINE PRODRUGS IN COMBINATION WITH A 5-HT2B ANTAGONIST
(FR) ADMINISTRATION DE PROMÉDICAMENTS DE CATÉCHOLAMINE EN COMBINAISON AVEC UN ANTAGONISTE DE 5-HT2B
Abstract
(EN)
The present invention provides combinations comprising treatment with compounds that are prodrugs of the dopamine agonist (4aR,10aR)-1-n-Propyl-1,2,3,4,4a,5,10,10a- octahydro-benzo[g]quinoline-6,7-diol, in particular compounds of formula (Ia) below or a pharmaceutically acceptable salt thereof, together with a 5-HT2B antagonist. R1 and R2 are selected independently from the group consisting of H, C1-6 alkyl and saturated monocyclic C3-6 cycloalkyl, or one of R1 and R2 is H and the other is phenyl, or R1 and R2 are connected to form a saturated monocyclic 3-6 cycloalkyl.Especially, the invention is directed to the combined use of said compounds in the treatment of Parkinson's disease and/or other conditions for which treatment with a dopamine agonist is therapeutically beneficial. The present invention also provides pharmaceutical compositions comprising said compounds and a 5-HT2B antagonist. In a separate aspect, the invention relates to new compounds that are prodrugs of (4aR,10aR)-1-n-Propyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoline-6,7-diol wherein R1 and R2 are individually selected from the group consisting of H, C1-6 alkyl and saturated monocyclic C3-6 cycloalkyl; or a pharmaceutically acceptable salt thereof; with the proviso that both R1 and R2 cannot be H at the same time.
(FR)
La présente invention porte sur des combinaisons qui comprennent un traitement avec des composés qui sont des promédicaments de l'agoniste de la dopamine (4aR,10aR)-1-n-Propyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoléines-6,7-diol, en particulier des composés de la formule (Ia) ci-dessous ou un sel de qualité pharmaceutique de ces derniers, conjointement avec un antagoniste de 5-HT2B. R1 et R2 sont choisis indépendamment parmi le groupe constitué par H, alkyle en C1-6 et cycloalkyle en C3-6 monocyclique saturé, ou R1 ou R2 est H et l'autre est un phényle, ou R1 et R2 sont reliés pour former un cycloalkyle en 3-6 monocyclique saturé. En particulier, l'invention concerne l'utilisation combinée desdits composés dans le traitement de la maladie de Parkinson et/ou d'autres conditions pathologiques pour lesquelles un traitement avec un agoniste de la dopamine est thérapeutiquement bénéfique. La présente invention porte également sur des compositions pharmaceutiques comprenant ces composés et un antagoniste de 5-HT2B. Selon un autre aspect, l'invention décrit de nouveaux composés qui sont des promédicaments de (4aR,10aR)-1-n-Propyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoléines-6,7-diol, R1 et R2 étant individuellement choisis parmi le groupe constitué par H, alkyle en C1-6 et cycloalkyle en C3-6 monocyclique saturé; ou un sel de qualité pharmaceutique de ces derniers; à condition que R1 et R2 ne puissent pas être H en même temps.
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