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1. WO2019012284 - ASK1 INHIBITING PYRROLOPYRIMIDINE AND PYRROLOPYRIDINE DERIVATIVES

Publication Number WO/2019/012284
Publication Date 17.01.2019
International Application No. PCT/GB2018/051983
International Filing Date 12.07.2018
IPC
C07D 471/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 487/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 9/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
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 25/28 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
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
CPC
A61K 31/519
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 ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
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
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
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
Applicants
  • GALAPAGOS NV [BE]/[BE]
  • CALCHAN LIMITED [GB]/[GB]
Inventors
  • AMANTINI, David
  • MESIC, Milan
  • SAXTY, Gordon
  • POLJAK, Tanja
  • VUJASINOVIC, Ines
  • ZIHER, Dinko
  • WITTY, David
  • GIBSON, Karl Richard
Agents
  • GIBSON, Mark
  • AITKEN, Elizabeth
Priority Data
1711234.312.07.2017GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) ASK1 INHIBITING PYRROLOPYRIMIDINE AND PYRROLOPYRIDINE DERIVATIVES
(FR) DÉRIVÉS DE PYRROLOPYRIMIDINE ET DE PYRROLOPYRIDINE INHIBANT ASK1
Abstract
(EN) The present invention relates to pyrrolopyrimidine compounds according to Formula (I) and their use in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases. In a particular aspect, the present compounds are ASK inhibitors, particularly ASK1 inhibitors. The present invention also provides methods for the production of a compound of the invention, pharmaceutical compositions comprising a compound of the invention, the use of the compounds in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases. (Formula (I))
(FR) La présente invention concerne des composés de pyrrolopyrimidine selon la formule (I) et leur utilisation dans la prophylaxie et/ou le traitement de la douleur, d'états inflammatoires, de maladies cardiovasculaires, de maladies neurodégénératives, de maladies neurologiques, de complications du diabète de type I, du cancer et/ou de maladies fibrotiques. Dans un aspect particulier, les présents composés sont des inhibiteurs de ASK, en particulier des inhibiteurs de ASK1. La présente invention concerne également des procédés de production d'un composé de l'invention, des compositions pharmaceutiques comprenant un composé de l'invention, l'utilisation des composés dans la prophylaxie et/ou le traitement de la douleur, d'états inflammatoires, de maladies cardiovasculaires, de maladies neurodégénératives, de maladies neurologiques, de complications du diabète de type I, du cancer et/ou de maladies fibrotiques. (Formule (I))
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