发明名称 PYRIMIDINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3-KINASE
摘要 The invention provides compounds which are pyrimidines of formula (I): wherein Ris bonded at ring position 2 and-YRis bonded at ring position 5 or 6, or YRis bonded at ring position 2 and Ris bonded at ring position 6; R is an indol-4-yl group which is substituted at the 5-or 6-position; either: (a) Y is selected from-O-(CH)-,-NH-(CH)-,.-NHC(O)-(CH)n and-C(O)NH-(CH2)-wherein n is 0 or an integer of 1 to 3, and Ris selected from an unsaturated 5-to 12-membered carbocyclic or heterocyclic group which is unsubstituted or substituted and a group-NRRwherein Rand R, which are the same or different, are each independently selected from H, C-Calkyl which is unsubstituted or substituted, C-Ccycloalkyl which is unsubstituted or substituted,-C(O)R,-C(O)N(R)and-S(O)R, or Rand R4 together form, with the nitrogen atom to which they are attached, a saturated 5-, 6-or 7-membered N-containing heterocyclic group which is unsubstituted or substituted; (b) Y is a direct bond and Ris selected from an unsaturated 5-to 12-membered carbocyclic or heterocyclic group which is unsubstituted or substituted, and a group-NR3R4 wherein Rand R, which are the same or different, are each independently selected from H, C-Calkyl which is unsubstituted or substituted, C-Ccycloalkyl which is unsubstituted or substituted,-C(O)R,-C(O)N(R)and-S(O)R; R is selected from H, C-Calkyl, C-Ccycloalkyl and a 5-to 12-membered aryl or heteroaryl group, which group is unsubstituted or substituted; and m is 1 or 2; or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of PO K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PB kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
申请公布号 KR20100016433(A) 申请公布日期 2010.02.12
申请号 KR20097023504 申请日期 2008.04.14
申请人 F. HOFFMANN-LA ROCHE AG;THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL 发明人 GOLDSMITH PAUL JOHN;HANCOX TIMOTHY COLIN;PEGG NEIL ANTHONY;SHUTTLEWORTH STEPHEN JOSEPH;DECHAUX ELSA AMANDINE;PRICE STEPHEN;LARGE JONATHAN MARTIN;MCDONALD EDWARD
分类号 C07D417/14;A61K31/506;A61P35/00;C07D403/04 主分类号 C07D417/14
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