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1. WO2020200335 - 3ALPHA, 5BETA-NEUROACTIVE STEROIDS FOR THE TREATMENT OF EPILEPSY AND SEIZURE DISEASES

Publication Number WO/2020/200335
Publication Date 08.10.2020
International Application No. PCT/CZ2020/050017
International Filing Date 02.04.2020
IPC
C07J 41/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
41Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C07J 43/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
43Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopentahydrophenanthrene skeleton
A61K 31/58 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
58containing heterocyclic rings, e.g. aldosterone, danazol, stanozolol, pancuronium, digitogenin
A61K 31/57 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
57substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, progesterone
A61K 31/56 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
A61P 25/00 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
CPC
C07J 41/0038
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
41Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
0033not covered by C07J41/0005
0038with an androstane skeleton, including 18- or 19-substituted derivatives, 18-nor derivatives and also derivatives where position 17-beta is substituted by a carbon atom not directly bonded to a further carbon atom and not being part of an amide group
C07J 41/005
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
41Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
0033not covered by C07J41/0005
005the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
C07J 43/003
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
43Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
003not condensed
Applicants
  • USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V. V. I. [CZ]/[CZ]
  • FYZIOLOGICKY USTAV AV CR, V. V. I. [CZ]/[CZ]
Inventors
  • KUDOVA, Eva
  • CHODOUNSKA, Hana
  • MARES, Pavel
  • VALES, Karel
Agents
  • HARTVICHOVA, Katerina
Priority Data
PV 2019-21605.04.2019CZ
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 3ALPHA, 5BETA-NEUROACTIVE STEROIDS FOR THE TREATMENT OF EPILEPSY AND SEIZURE DISEASES
(FR) STÉROÏDES 3ALPHA, 5BÊTA-NEUROACTIFS POUR LE TRAITEMENT DE L'ÉPILEPSIE ET DE MALADIES ÉPILEPTIQUES
Abstract
(EN)
The invention provides 3α5β–steroid compounds of general formula I. These compounds are useful in the treatment of epilepsy or comorbidities associated with epilepsy or conditions associated with convulsions, such as seizures associated with hypoxia; seizures associated with traumatic brain damage; seizures associated with intoxication; pathological changes caused by hyperexcitation; or in treatment of conditions accompanying epilepsy, such as affective disorders, depression, post-traumatic stress disorder (PTSD) and stress-related diseases, anxiety, schizophrenia and psychotic disorders, related ischemic CNS damage, neurodegenerative changes and disorders, multiple sclerosis. The compounds of general formula I also show age-specific efficacy.
(FR)
L'invention concerne des composés 3α5β-stéroïdes de formule générale I. Ces composés sont utiles dans le traitement de l'épilepsie ou de comorbidités associées à l'épilepsie ou à des états associés à des convulsions, telles que des crises associées à l'hypoxie ; des crises associées à une lésion cérébrale traumatique ; des crises associées à une intoxication ; des changements pathologiques provoqués par l'hyperexcitation ; ou dans le traitement d'états accompagnant l'épilepsie, tels que des troubles affectifs, la dépression, un trouble de stress post-traumatique (PTSD) et des maladies liées au stress, l'anxiété, la schizophrénie et des troubles psychotiques, des lésions ischémiques du SNC associées, des changements et des troubles neurodégénératifs, la sclérose en plaques. Les composés de formule générale I présentent également une efficacité spécifique à l'âge.
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