2,4-DI(PHENYLAMINO)PYRIMIDINES, APPLIED IN TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY DISORDERS AND IMMUNE SYSTEM DISORDERS

FIELD: medicine. ^ SUBSTANCE: invention relates to novel pyrimidine derivatives of formula (I) or their pharmaceutically acceptable salts which possess inhibiting activity with respect to focal adhesion kinase (FAK), proteintyrosinekinase ZAP-70, receptor of insulin-like growth factor 1 (IGF-1R), ty...

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Hauptverfasser: MASUJA KEJICHI, MATSUURA NAOKO, MIJAKE TAKAKHIRO, GARSIJA-EHCHEVERRIJA KARLOS, OKHMORI OSAMU, KANAZAVA TAKANORI, UMEMURA ICHIRO, KAVAKHARA EHJDZHI
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: medicine. ^ SUBSTANCE: invention relates to novel pyrimidine derivatives of formula (I) or their pharmaceutically acceptable salts which possess inhibiting activity with respect to focal adhesion kinase (FAK), proteintyrosinekinase ZAP-70, receptor of insulin-like growth factor 1 (IGF-1R), tyrosinekinase activity of anaplastic lymphoma (ALK) and fusion protein NPM-ALK. In formula (I) , R0, R1 and R2 independently represent hydrogen, C1-C8 alkyl, 5- or 6-member heterocycle, containing 1,2 or 3 heteroatoms, selected from N, O and S, C1-C8alkoxy group, C1-C8alkylsulphinyl, C1-C8alkylsulphonyl, C5-C10arylsulphonyl, halogen, carbamoyl, sulphamoyl, etc.; R3 represents C1-C8alkylsulphinyl, C1-C8alkylsulphonyl, C5-C10arylsulphonyl, carbamoyl or sulphamoyl; R4 represents hydrogen or C1-C8alkyl; R5 represents chlorine or bromine; R6 represents hydrogen; R7, R8, R9 and R10 independently represent C1-C8alkyl, C5-C10aryl, possibly substituted by 5- or 6-member heterocycle, containing 1, 2 or 3 heteroatoms, selected from N, O and S, where substituents are selected from C1-C8alkyl, hydroxy, hydroxy-C1-C8alkyl, C1-C8alkoxy C1-C8alkyl, cyano, oxo, C1-C8alkylamino, diC1-C8alkylamino, carbamoyl, C1-C8alkylcaronyl, 5-10-member heterocycle, containing 1, 2 or 3 heteroatoms, selected from N and O, which is probably substituted by C1-C8alkyl; C1-C8alkoxy group, halogen- C1-C8alkoxy group, etc; A represents C. Invention also relates to pharmaceutical composition and to application of compounds of formula (I) for preparation of medication. ^ EFFECT: novel compounds possess useful biologic activity. ^ 15 cl, 61 ex Изобретение относится к новым производным пиримидина формулы (I) или их фармацевтически приемлемым солям, обладающим ингибирующей активностью в отношении киназы фокальной адгезии (FАК), протеинтирозинкиназы ZAP-70, рецептора инсулиноподобного фактора роста 1 (IGF-1R), тирозинкиназной активности анапластической лимфомы (ALK) и слитого белка NPM-ALK. В формуле (I) ! R0, R1 и R2 независимо обозначают водород, С1-С8алкил, 5- или 6-членный гетероциклил, содержащий 1, 2 или 3 гетероатома, выбранных из N, О и S, С1-С8алкоксигруппу, С1-С8алкилсульфинил, С1-С8алкилсульфонил, С5-С10арилсульфонил, галоген, карбамоил, сульфамоил и т.д.; R3 обозначает С1-С8алкилсульфинил, С1-С8алкилсульфонил, С5-С10арилсульфонил, карбамоил или сульфамоил; R4 обозначает водород или С1-С8алкил; R5 обозначает хлор или бром; R6 обозначает водород; R7, R8, R9 и R10 независимо обозначают С1-С8алкил,