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PYRIMIDINE-SUBSTITUTED PURINE DERIVATIVES, PHARMACEUTICAL COMPOSITION BASED THEREON, METHOD OF PROTEIN KINASE INHIBITION, METHOD OF TREATING OR PREVENTING DISEASES SENSITIVE TO PROTEIN KINASE INHIBITION AND METHOD OF TREATING PROLIFERATIVE DISEASES
专利权人:
VERASTEHM;INK.
发明人:
NAGARADZh Kharish Kumar Majsur (IN),НАГАРАДЖ Хариш Кумар Майсур (IN),UIL'JaMS Meredit (GB),УИЛЬЯМС Мередит (GB),NAGARADZH KHARISH KUMAR MAJSUR,НАГАРАДЖ Хариш Кумар Майсур,UILJAMS MEREDIT,УИЛЬЯМС Мередит
申请号:
RU2010117737/04
公开号:
RU0002518098C2
申请日:
2008.10.03
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to purine compounds of the formula (I):,wherein R1 is specified in a group containing H, halogen and C1-C6alkyl, R2 is specified in a group containing H, CN, an optionally substituted C1-C12alkyl, an optionally substituted C3-C12cycloalkyl, an optionally substituted C2-C12heterocycloalkyl, an optionally substituted C6-C18aryl, an optionally substituted C1-C12alkyloxy, COR8, COOH, COOR8, CONR8R9 and acyl; if R2 represents the optionally substituted C6-C18aryl, the above optional substitute is specified in F and CH3; if R2 represents the optionally substituted C1-C12alkyl, the above optional substitute is specified in CH3, OCH3 and O-C(CH3)3; if R2 represents the optionally substituted C3-C12cycloalkyl, the above optional substitute represents CH3; if R2 represents the optionally substituted C2-C12heterocycloalkyl, the above optional substitute is specified in a group consisting of COOC(CH3)3, CO(CH2)2CH3, COPh and CO(5-methylthiophen-2-yl), each R3 and R4 is independently specified in a group containing H, C1-C6alkyl and OR8, R6 is specified in a group containing H, OH, OR8, CH2OH, NH2 and NR8R9, or R8 and R9 if taken together with atoms attached thereto form a cyclic group, each R8 and R9 is independently specified in a group containing H and C1-C12alkyl; each R2 independently represents C1-C6alkyl, q represents an integer specified in a group containing 0 and 1, X represents a group of formula (CR10 2)m, each R10 is independently specified in a group containing H and C1-C6 alkyl, m represents an integer specified in a group containing 0, 1, 2 and 3, C2-C12heterocycloalkyl contains at least one heteroatom specified in a group containing O, N and S, in at least one ring; each ring is 3- to 10-merous, or their pharmaceutically acceptable salts or N-oxides.EFFECT: compounds may be effective as agents for a number of proliferative diseases or disorders, including tumours and malignant growth, as well as other PI
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