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Cyclic amides as MetAP-2 inhibitors
专利权人:
Merck Patent GmbH
发明人:
HEINRICH, Timo,ZENKE, Frank,KRIER, Mireille,FRIESE-HAMIM, Manja,SEENISAMY, Jeyaprakashnarayanan
申请号:
ES13711291
公开号:
ES2587953T3
申请日:
2013.03.21
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
Compounds of formula I ** Formula ** in which R means NR2R4, Alk, C (>; = CH2) [C (R4) 2] nAr2, Het2, 5 O [C (R4) 2] nAr2 or OA, X means CO or CH2, Y means CO or CH2, R1 means H, [C (R4) 2] nAr1, (CH2) nHet, (CH2) nCyc, [C (R4) 2] nCOOH, [C (R4) 2] nCONHAr1 , [C (R4) 2] nCONH2, [C (R4) 2] nNHA, [C (R4) 2] nNA2, O [C (R4) 2] nAr1, [C (R4) 2] nOR7, [C ( R4) 2] nCOO (CH2) nAr1, [C (R4) 2] nCOOA, [C (R4) 2] nCONH [C (R4) 2] pCON (R4) 2 or [C (R4) 2] nCONHCR4 [( CH2) nN (R4) 2] CON (R4) 2, R2 means H, [C (R4) 2] nAr2, (CH2) nCOHet1, (CH2) nCOAr2, (CH2) mNA2 or (CH2) nHet, R3 means OH or OCOA, R4 means H or alkyl with 1, 2, 3 or 4 C atoms, R2 and R4 together also mean alkylene with 2, 3, 4 or 5 C atoms, and a CH2 group can also be replaced by N (CH2 ) mOH or SO2, R5, R6 in each case independently of each other means H, F or A, R5 and R6 together also means alkylene with 2, 3, 4 or 5 C atoms, and a CH2 group may also be replaced by NCOA or Or, R7 means H or A, Ar1 means unsubstituted phenyl gone or mono-, di-, tri-, tetra- or pentas substituted with Hal, OH, OA, CONH2, CONHA, CONA2, NHSO2A, CONHCyc, NHSO2Cyc, CONHAr2, COHet1 and / or NASO2A, Ar2 means unsubstituted or mono- , di-, tri-, tetra- or pentasubstituted with Hal, A, CONH2, and / or OAr3, Ar3 means phenyl unsubstituted or monosubstituted with NH2, Het means a heterocycle with one or two saturated, unsaturated or aromatic nuclei with 1 at 4 atoms of 25 N and / or O and / or S, unsubstituted or mono-, di- or trisubstituted with Hal, A, OA, CN, NH2, NHA, NA2, NO2, CN, COOH, COOA, (CH2 ) nCONH2, (CH2) nCONHA, (CH2) nCONA2, NHCOA, COA, CHO, Het1, SO2A, SO2NH2, SO2NHA, SO2NA2, CONHNH2, CONHAr3,>; = O and / or Ar3, Het1 means a heterocycle saturated with a nucleus with from 1 to 4 atoms of N and / or O and / or S, unsubstituted or mono-, di- or trisubstituted with>; = O and / or COOA, Het2 means isoindolyl, A means unbranched or branched alkyl with 1-10 C atoms, in which 1-7 H atoms can be replaced by F, Cl, Br, OH
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