MERCK PATENT GESELLSCHAFT MIT BESCHRAENKTER HAFTUNG
发明人:
DR. BUCHSTALLER HANS,PETER - DRA. WUCHERER-PLIETKER MARGARITA,DR. HEINRICH TIMO
申请号：
ARP110104498
公开号：
AR084083A1
申请日:
2011.12.02
申请国别(地区):
AR
年份:
2013
代理人:
摘要：
They are PDK1 inhibitors that can be used to treat tumors.Requirement 1: formula compound (1),Q is het DIL, R1 is br, het1 or monophenyl oxide, replaced by CH2OH； R2 and R3 are independent of each other,h. Hal, a, AR, [C (R5) 2] NOA, [C (R5) 2] NOA or [C (R5) 2] NN (R5)； R2 and R3 are equal to or = CH2 or asphalt chain with 2-5 C atoms； R4 is h, AR or het2； R5 is h or a rsque；；Het1 is a pyrazole that can be replaced by a, CH2OH, (CH2) 2OH, COOH, ch2cohet3, COOA or CONH2 alone； AR is phenyl, nafilo or unsubstituted biphenyl, or monkey.di- or trisubstituted with Hal, A, (CH2) nOR5, (CH2) nN (R5) 2, SR5, NO2, COOR5, CON (R5) 2, NR5COA, NR5SO2A, SO2N (R5) 2, COR5, (CH2) nCN and / or S (O) mA； Het is an unsubstituted or mono- or disubstituted mono- or bicyclic saturated, unsaturated or aromatic heterocycle with Hal, A, [C (R5) 2] nOR5, [C (R5) 2] nN (R5) 2, NO2, CN , COOR5, CON (R5) 2, NR5COA, NR5SO2A, COR5, SO2NR5, S (O) mA, = S, = NH, = NA and / u = O (carbonyl oxygen) with 1 to 4 N atoms, and / or O and / or S； Het2 is an unsubstituted or mono- or disubstituted monocyclic saturated, unsaturated or aromatic heterocycle with Hal, A, OR5, N (R5) 2, NO2, CN, COOR5, CON (R5) 2, NR5COA, NR5SO2A, COR5, SO2NR5, S (O) mA, = S, = NH,= NA and / or = O (carbonyl oxygen) with 1 to 4 N atoms, and / or O and / or S； Het3 is an unsubstituted monocyclic saturated heterocycle with 1 to 4 N atoms, and / or O and / or S； A is unbranched or branched alkyl with 1-10 C atoms, where 1-7 H atoms may be replaced by F, Cl and / or Br, and / or where one or two non-adjacent groups CH and / or CH2 can be replaced by NR5, O, S, SO, SO2, C ° C and / or CH = CH groups, or cyclic alkyl with 3-7 C atoms； A is unbranched or branched alkyl with 1-6 C atoms, or cyclic alkyl with 3-7 C atoms； Hal is F, Cl, Br or l； m is 0, 1 or 2； n is 0, 1, 2, 3, or 4； as well as its salts,6. Acceptable Dow and stereoisomers of drugs, including mixtures in various proportions.Son inhibidores de PDK1 y se pueden emplear
