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1. WO2020115683 - 5-HYDROXY-7-OXABICYCLO[2.2.1]HEPTANE-2-CARBOXAMIDE DERIVATIVES FOR INDUCING CHONDROGENESIS FOR TREATING JOINT DAMAGE

Publication Number WO/2020/115683
Publication Date 11.06.2020
International Application No. PCT/IB2019/060454
International Filing Date 04.12.2019
IPC
C07D 493/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
493Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02in which the condensed system contains two hetero rings
08Bridged systems
A61K 31/34 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
34having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
A61K 31/443 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
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
443containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/5377 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
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/4155 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4151,2-Diazoles
4155not condensed and containing further heterocyclic rings
A61K 31/506 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
CPC
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
C07D 493/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
493Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02in which the condensed system contains two hetero rings
08Bridged systems
Applicants
  • NOVARTIS AG [CH]/[CH]
Inventors
  • LAJINESS, James Paul
  • VALIERE, Andrew
Agents
  • NOVARTIS AG
Priority Data
62/776,26706.12.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 5-HYDROXY-7-OXABICYCLO[2.2.1]HEPTANE-2-CARBOXAMIDE DERIVATIVES FOR INDUCING CHONDROGENESIS FOR TREATING JOINT DAMAGE
(FR) DÉRIVÉS DE 5-HYDROXY-7-OXABICYCLO[2.2.1]HEPTANE-2-CARBOXAMIDE PERMETTANT D'INDUIRE UNE CHONDROGENÈSE POUR TRAITER DES LÉSIONS ARTICULAIRES
Abstract
(EN)
The present invention provides 5-hydroxy-7- oxabicyclo[2.2.1]heptane-2-carboxamide derivatives of Formula (1) wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds. The compounds are used for inducing chondrogenesis, in methods of treating or preventing joint damage, resulting from joint injury or arthritis, and for inducing hyaline cartilage production. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (examples 1 to 89; tables 1 and 2). An exemplary compound is e.g. rac-(1R,2R,3S,4R,5S)-N-(2-fluoro-5- (trifluoromethyl)phenyl)-5-hydroxy-3-(3-(trifluoromethyl)phenyl)-7- oxabicyclo[2.2.1]heptane-2-carboxamid (example 1).
(FR)
La présente invention concerne des dérivés de 5-hydroxy-7-oxabicyclo[2.2.1]heptane-2-carboxamide de formule (1), les variables étant telles que définies dans la description. La présente invention concerne en outre des compositions pharmaceutiques comprenant de tels composés. Les composés sont utilisés pour induire une chondrogenèse, dans des méthodes de traitement ou de prévention de lésions articulaires, résultant d'une lésion articulaire ou d'une arthrite, lesdits composés pouvant induire une production de cartilage hyalin. La présente invention concerne la préparation de composés donnés à titre d'exemple ainsi que des données pharmacologiques de ceux-ci (exemples 1 à 89; tableaux 1 et 2). Un composé donné à titre d'exemple est par exemple, rac-(1R,2R,3S,4R,5S)-N-(2-fluoro-5- (trifluorométhyl)phényl)-5-hydroxy-3-(3-(trifluorométhyl)phényl)-7- oxabicyclo[2.2.1]heptane-2-carboxamide (exemple 1).
Latest bibliographic data on file with the International Bureau