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1. (WO1997019065) SUBSTITUTED 2-ANILINOPYRIMIDINES USEFUL AS PROTEIN KINASE INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/019065 International Application No.: PCT/GB1996/002854
Publication Date: 29.05.1997 International Filing Date: 20.11.1996
Chapter 2 Demand Filed: 19.06.1997
IPC:
C07D 239/42 (2006.01) ,C07D 239/48 (2006.01) ,C07D 401/04 (2006.01) ,C07D 417/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
32
One oxygen, sulfur or nitrogen atom
42
One nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
48
Two nitrogen atoms
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
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
Applicants:
CELLTECH THERAPEUTICS LIMITED [GB/GB]; 216 Bath Road Slough Berkshire SL1 4EN, GB (AllExceptUS)
DAVIS, Peter, David [GB/GB]; GB (UsOnly)
MOFFAT, David, Festus, Charles [GB/GB]; GB (UsOnly)
DAVIS, Jeremy, Martin [GB/GB]; GB (UsOnly)
HUTCHINGS, Martin, Clive [GB/GB]; GB (UsOnly)
Inventors:
DAVIS, Peter, David; GB
MOFFAT, David, Festus, Charles; GB
DAVIS, Jeremy, Martin; GB
HUTCHINGS, Martin, Clive; GB
Agent:
HALLYBONE, Huw, George ; Carpmaels & Ransford 43 Bloomsbury Square London WCA 2RA, GB
Priority Data:
9523675.820.11.1995GB
Title (EN) SUBSTITUTED 2-ANILINOPYRIMIDINES USEFUL AS PROTEIN KINASE INHIBITORS
(FR) 2-ANILINOPYRIMIDINES SUBSTITUEES UTILES EN TANT QU'INHIBITEURS DE PROTEINE KINASE
Abstract:
(EN) Compounds of general formula (1) are described wherein R1 is a hydrogen or halogen atom or an optionally substitued straight or branched chain alkyl, alkenyl or alkynyl group or a group selected from hydroxyl (-OH), substituted hydroxyl, thiol (-SH), substituted thiol, amino (-NH2), or substituted amino; R2 and R3, which may be the same or different, is each an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R4 is a hydrogen atom or a straight or branched chain alkyl group; R5 is a hydrogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R6 is a hydrogen or halogen atom or an amino (-NH2), substituted amino, nitro, carboxyl (-CO2H) or esterified carboxyl group or a group -X1-R6a where X1 is a direct bond or a linker atom or group and R6a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; X is a direct bond or a linker atom or group; R7 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein kinase inhibitors, particularly the kinases p56lck, p59fyn, ZAP-70 and protein kinase C and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.
(FR) L'invention concerne des composés représentés par la formule (1), dans laquelle R1 représente un atome d'hydrogène ou d'halogène ou un groupe alkynyle, alcényle ou alkyle à chaîne droite ou ramifiée éventuellement substitué ou un groupe sélectionné parmi hydroxyle (-OH), hydroxyle substitué, thiol (-SH), thiol substitué, amino (-NH2) ou amino substitué; R2 et R3 pouvant être semblables ou différents, représentent chacun un groupe alkynyle, alcényle ou alkyle à chaîne droite ou ramifiée éventuellement substitué; R4 représente un atome d'hydrogène ou un groupe alkyle à chaîne droite ou ramifiée; R5 représente un atome d'hydrogène ou un groupe alkynyle, alcényle ou alkyle à chaîne droite ou ramifiée éventuellement substitué; R6 représente un atome d'hydrogène ou d'halogène ou un groupe amino (-NH2), amino substitué, nitro, carboxyle (-CO2H) ou carboxyle estérifié ou un groupe -X1-R6a dans lequel X1 représente une liaison directe ou un atome de liaison ou un groupe et R6a représente un groupe alkynyle, alcényle ou alkyle à chaîne droite ou ramifiée éventuellement substitué; X représente une liaison directe ou un atome ou un groupe de liaison; R7 représente un groupe aliphatique, cycloaliphatique, hétéroaliphatique, hétérocycloaliphatique, aromatique ou hétéroaromatique; ainsi que leurs sels, solvates, hydrates et N-oxydes. Ces composés sont des inhibiteurs sélectifs de protéine kinase, en particulier, les kinases p56lck, p59fyn, ZAP-70 et la protéine kinase C, et peuvent être utilisés dans la prophylaxie et le traitement de maladies immunes, hyperprolifératives et d'autres maladies dans lesquelles on pense qu'une action inadéquate de la protéine kinase joue un rôle.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, TJ, TM, TR, TT, UA, UG, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
ES2195020EP0862560US5958935US6235746DE000069627179AU1996076314