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1. (WO2006051311) NITROGEN HETEROAROMATIC COMPOUNDS WHICH BIND TO THE ACTIVE SITE OF PROTEIN KINASE ENZYMES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2006/051311 International Application No.: PCT/GB2005/004358
Publication Date: 18.05.2006 International Filing Date: 11.11.2005
IPC:
C07D 213/74 (2006.01) ,C07D 401/04 (2006.01) ,C07D 401/14 (2006.01) ,C07D 405/14 (2006.01) ,A61K 31/444 (2006.01) ,A61K 31/4709 (2006.01) ,A61K 31/497 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic 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
02
having three double bonds between ring members or between ring members and non-ring members
04
having 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
60
with 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
72
Nitrogen atoms
74
Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic 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
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic 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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic 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
14
containing three or more hetero rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
444
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
47
Quinolines; Isoquinolines
4709
Non-condensed quinolines containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965
Non-condensed pyrazines
497
containing further heterocyclic rings
Applicants:
BIRAULT, Veronique [FR/GB]; GB (UsOnly)
BRAVO, Jose, Antonio [ES/GB]; GB (UsOnly)
CROSSLEY, Roger [GB/GB]; GB (UsOnly)
GALAPAGOS NV [BE/BE]; Generaal De Wittelaan L11 A3 B-2800 Mechelen, BE (AllExceptUS)
Inventors:
BIRAULT, Veronique; GB
BRAVO, Jose, Antonio; GB
CROSSLEY, Roger; GB
Agent:
MANTEN, Annemieke ; Arnold & Siedsma Sweelinkplein 1 NL-2517 GK The Hague, NL
Priority Data:
0425026.212.11.2004GB
0500245.607.01.2005GB
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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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)