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1. WO2006051311 - NITROGEN HETEROAROMATIC COMPOUNDS WHICH BIND TO THE ACTIVE SITE OF PROTEIN KINASE ENZYMES

Publication Number WO/2006/051311
Publication Date 18.05.2006
International Application No. PCT/GB2005/004358
International Filing Date 11.11.2005
IPC
C07D 213/74 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 401/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
C07D 401/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
C07D 405/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14containing three or more hetero rings
A61K 31/444 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
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
444containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4709 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
4709Non-condensed quinolines containing further heterocyclic rings
CPC
A61P 15/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
10for impotence
A61P 19/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
10for osteoporosis
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
A61P 25/28
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
A61P 27/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
A61P 27/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
06Antiglaucoma agents or miotics
Applicants
  • GALAPAGOS NV [BE]/[BE] (AllExceptUS)
  • BIRAULT, Veronique [FR]/[GB] (UsOnly)
  • BRAVO, Jose, Antonio [ES]/[GB] (UsOnly)
  • CROSSLEY, Roger [GB]/[GB] (UsOnly)
Inventors
  • BIRAULT, Veronique
  • BRAVO, Jose, Antonio
  • CROSSLEY, Roger
Agents
  • MANTEN, Annemieke
Priority Data
0425026.212.11.2004GB
0500245.607.01.2005GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) NITROGEN HETEROAROMATIC COMPOUNDS WHICH BIND TO THE ACTIVE SITE OF PROTEIN KINASE ENZYMES
(FR) COMPOSÉS HÉTÉROAROMATIQUES DE L'AZOTE QUI SE LIENT AU SITE ACTIF D'ENZYMES DE TYPE PROTÉINES KINASES
Abstract
(EN) Compounds of Formula (I) or pharmaceutically acceptable salts, hydrates, solvates, geometrical isomers, tautomers, optical isomers, or prodrug forms thereof, wherein X, Y, Z, R1, R2, R3 and R4 are as defined herein are capable of binding to the active site of protein kinase enzymes. In particular, they are inhibitors of a serine/ threonine kinase more particularly Rho kinase (ROK, ROCK). The compounds can be used in methods of treatment and in the manufacture of medicaments for application to a number of therapeutic indications including cardiovascular disease (coronary vasospasm, hypertensive disease, arteriosclerosis), stroke, cancer, erectile dysfunction, asthma, osteoporosis, AIDS or an ocular condition including glaucoma, age related macular degeneration, lacrimal gland disease, or diabetic retinopathy, or suppression of neurite growth and hence a condition requiring nerve cell extension and connectivity, neuronal regeneration, inducing new axonal growth and promotion of axonal (re)wiring, repairing damage to neurons in the CNS caused by trauma (eg stroke, traumatic brain injury etc.) or neurodegeneration (eg Alzheimer's, Parkinson's etc), repair and recovery from and treatment of disorders such as spinal cord injury and in reducing the subsequent effects thereof, or pain caused by nerve cell damage such as following trauma or amputation for example in the treatment of neuropathic pain.
(FR) Des composés de formule (I) ou des sels, hydrates, solvates, isomères géométriques, tautomères, isomères optiques ou formes de promédicaments acceptables du point de vue pharmaceutique de ceux-ci, dans laquelle formule X, Y, Z, R1, R2, R3 et R4 sont tels que définis ici, sont capables de se lier au site actifs d'enzymes de type protéines kinases. En particulier, ce sont des inhibiteurs d'une sérine/thréonine kinase plus particulièrement d'une Rho kinase (ROK, ROCK). On peut utiliser les composés dans des procédés de traitement et dans la fabrication de médicaments pour une application à un certain nombre d'indications thérapeutiques dont une maladie cardiovasculaire (angiospasme coronarien, maladie hypertensive, artériosclérose), l'accident cérébrovasculaire, le cancer, le trouble de l'érection, l'asthme, l'ostéoporose, le SIDA et une affection oculaire dont le glaucome, la dégénérescence maculaire liée à l'âge, une maladie des glandes lacrymales ou la rétinopathie diabétique, ou à la suppression du développement de neurites et donc à une affection nécessitant l'extension et la connectivité de cellules nerveuses, la régénération des neurones, l'induction du développement de nouveaux axones et la promotion du (re)câblage d'axones, la réparation de lésions des neurones dans le SNC provoquées par un traumatisme (par exemple un accident cérébrovasculaire, une lésion cérébrale traumatique, etc.) ou par une neurodégénérescence (par exemple la maladie d'Alzheimer, la maladie de Parkinson, etc.), à la réparation ou la récupération de troubles tels qu'une lésion de la moelle épinière et le traitement de ceux-ci et la réduction des effets subséquents de ceux-ci ou de la douleur provoquée par une lésion des cellules nerveuses telle que celle suivant un traumatisme ou une amputation par exemple dans le traitement de la douleur neuropathique.
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