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1. (WO1998002438) BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/1998/002438 International Application No.: PCT/EP1997/003674
Publication Date: 22.01.1998 International Filing Date: 11.07.1997
Chapter 2 Demand Filed: 09.01.1998
IPC:
C07D 209/08 (2006.01) ,C07D 231/56 (2006.01) ,C07D 235/08 (2006.01) ,C07D 401/06 (2006.01) ,C07D 407/12 (2006.01) ,C07D 471/04 (2006.01) ,C07D 493/08 (2006.01) ,C07D 519/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
08
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
54
condensed with carbocyclic rings or ring systems
56
Benzopyrazoles; Hydrogenated benzopyrazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
08
Radicals containing only hydrogen and carbon 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
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
407
Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/183
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic 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
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
493
Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02
in which the condensed system contains two hetero rings
08
Bridged systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
519
Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
Applicants: COCKERILL, George, Stuart[GB/GB]; GB (UsOnly)
CARTER, Malcolm, Clive[GB/GB]; GB (UsOnly)
GUNTRIP, Stephen, Barry[GB/GB]; GB (UsOnly)
SMITH, Kathryn, Jane[GB/GB]; GB (UsOnly)
GLAXO GROUP LIMITED[GB/GB]; Glaxo Wellcome House Berkeley Avenue Greenford Middlesex UB6 0NN, GB (AllExceptUS)
Inventors: COCKERILL, George, Stuart; GB
CARTER, Malcolm, Clive; GB
GUNTRIP, Stephen, Barry; GB
SMITH, Kathryn, Jane; GB
Agent: REED, Michael, A.; Glaxo Wellcome plc Glaxo Wellcome House Berkeley Avenue Greenford Middlesex UB6 0NN, GB
Priority Data:
9614763.213.07.1996GB
9625492.507.12.1996GB
Title (EN) BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
(FR) COMPOSES HETEROAROMATIQUES BICYCLIQUES EN TANT QU'INHIBITEURS DE LA PROTEINE TYROSINE KINASE
Abstract:
(EN) Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O)m, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O)m atoms. U represents a 5 to 10-membered mono or bicyclic ring system in which one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S(O)m, wherein m is 0,1 or 2 and wherein the ring system is substituted by at least one independently selected R6 group and is optionally substituted by at least one indepenently selected R4 group, with the proviso that U does not represent phenyl; are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.
(FR) L'invention a trait à des composés hétéroaromatiques substitués, et en particulier à des composés hétéroaromatiques de la formule (I), où X est N ou CH. A représente un noyau hétérocyclique condensé à 5, 6 ou 7 chaînons contenant de 1 à 5 hétéroatomes pouvant être les mêmes ou différents, sélectionnés parmi N, O ou S(O)m, où m est tel que défini plus bas, le noyau hétérocyclique contenant un total de 1, 2 ou 3 doubles liaisons, y compris la liaison dans le noyau pyridine ou pyrimidine auquel il est condensé, à condition que le noyau hétérocyclique ne forme pas une partie d'une purine, et que le noyau hétérocyclique condensé ne contienne pas deux atomes O ou S(O)m adjacents. U représente un noyau mono ou bicyclique doté de 5 à 10 chaînons, dans lequel un ou plusieurs atomes de carbone est remplacé optionnellement par un hétéroatome sélectionné indépendamment parmi N, O et S(O)m, où m a pour valeur 0, 1 ou 2, et où le noyau est substitué par au moins un groupe R6 sélectionné indépendamment, et substitué optionnellement par au moins un groupe R4 sélectionné indépendamment, à condition que U ne représente pas du phényle. Les composés décrits sont des inhibiteurs de la protéine tyrosine kinase. Les composés sont décrits, ainsi que leurs procédés de préparation, des compositions pharmaceutiques contenant de tels composés et leur utilisation médicale, par exemple dans le traitement du cancer et du psoriasis.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, 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, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (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)