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Novel heterocyclic compounds as MetAP-2 inhibitors
专利权人:
Merck Patent GmbH
发明人:
HEINRICH, Timo,ZENKE, Frank,KRIER, Mireille,SCHIEMANN, Kai
申请号:
ES09796971
公开号:
ES2575687T3
申请日:
2009.12.22
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
Compounds of formula I ** Formula ** in which pyrrolidinyl, imidazolinyl, pyrazolyl, 2-oxa-5-aza-bicyclo [2,2,1] hept-5-yl, morpholinyl or N, Z means imidazopyrimidinyl, triazolopyrimidinyl or pyrrolopyrimidinyl, where Z is attached to a nitrogen of the moiety D, Y means (CH2) is not present, X means O (CH2) r, NH, NA, OC (>; = O), NHSO2 or not present, R1 means H, A or COA, R means Het, Het means a saturated, unsaturated or aromatic heterocycle with two nuclei, unsubstituted or mono-, di- or trisubstituted with Hal, A, (CH2) mOR6, (CH2) mN ( R6) 2, (CH2) mCN, (CH2) mCOOR6, CONH (CH2) mCOOH, CONH (CH2) mHet2, CO (CH2) mN (R6) 2, CO (CH2) mNH (CH2) rCOOA, (CH2) rCONH (CH2) mAr1, COCH [(CH2) mCONH2] NH2, COCH [(CH2) mCONH2] NHCOOA, COCH [(CH2) mHet2] NHCOOA, COCH (NHCOA) CH2CONH2, (CH2) mNHCOOA, COCH [(CH2) mCN] NHCOOA, COO (CH2) mCN, COO (CH2) mN (R6) 2, CO (CH2) mCON (R6) 2, COR6, COHet2, O (CH2) mAr1 and / or>; = O (carbonyl oxygen) with 1 at 4 atoms of N, and / or O and / or S, Het2 means imidazolyl, indolyl, isoxazolyl, pyridazinyl, pyrazolyl, benzimidazolyl, pyridyl, dibenzofuranyl, carbazolyl, benzofuranyl, isoindolyl, quinazolinyl, quinoxalinyl, pyrimidinyl, indazolyl, furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, triazolyl, tetrazolyl, thiadiazole, benzothiazolyl, imidazo [ 1,2-a] pyridinyl or 1,3-benzodioxolyl, R6 means H or alkyl with 1-6 C atoms, Ar1 means unsubstituted or mono-, di- or trisubstituted phenyl with Hal and / or SO2NH2, A means alkyl with 1-10 unbranched or branched C atoms, in which 1-7 H atoms can be substituted by F, Cl, Br and / or OH, or cyclic alkyl with 3-7 C atoms, Hal means F, Cl, Br or I, m means 0, 1, 2, 3, 4, 5 or 6, n means 1 or 2, which means 0, 1, 2, 3 or 4, r means 0, 1 or 2, as well as its pharmaceutically useful salts, tautomers and stereoisomers, including mixtures in all proportions.Compuestos de fórmula I**Fórmula** en la que significa pirrolidinilo, imidazolinilo, pirazolilo, 2-oxa-5-aza-biciclo[2,2,1]hept-5-ilo, mo
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