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N1- (3,3,3-Trifluoro-2-hydroxo-2-methylpropionyl) -piperidine derivatives as inhibitors of pyruvate dehydrogenase kinase
专利权人:
Merck Patent GmbH
发明人:
BUCHSTALLER, Hans-Peter
申请号:
ES14799674
公开号:
ES2665148T3
申请日:
2014.11.19
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
Compounds of formula I ** (See formula) ** where R indicates pyrazol-diyl, imidazol-diyl, isoxazol-diyl or triazol-diyl, each of which is unsubstituted or monosubstituted by R2, R1 indicates (CH2) nAr, (CH2) nHet, A or Cic, R2 indicates A ', methoxy, hydroxymethyl, COOA', CN, COOH, CONH2 or OH, R3 indicates H, A ', COOA' or CN, Ar indicates phenyl, which is not substituted or mono, di, tri, tetra or pentas substituted by Hal, A, CN, OA, [C (R5) 2] pOH, [C (R5) 2] pN (R5) 2, NO2, [C (R5) 2] pCOOR5, NR5COA, NR5SO2A, [C (R5) 2] pSO2N (R5) 2, S (O) nA, O [C (R5) 2] mN (R5) 2, NR5COOA, NR5CON (R5) 2 and / or COA, Het indicates a saturated, unsaturated or aromatic mono or bicyclic heterocycle with 1 to 4 atoms of N, O and / or S, which is unsubstituted or mono or disubstituted by Hal, A, CN, OA, [C (R5) 2] pOH, [C (R5) 2] pN (R5) 2, NO2, [C (R5) 2] pCOOR5, NR5COA, NR5SO2A, [C (R5) 2] pSO2N (R5) 2, S ( O) nA, O [C (R5) 2] mN (R5) 2, NR5COOA, NR5CON (R5) 2 and / or COA, Cic indicates cyclic alkyl with 3, 4, 5, 6 or 7 C atoms, which does not is replaced oe monosubstituted by OH, A indicates branched or unbranched alkyl with 1-10 C atoms, in which one or two non-adjacent CH or CH2 groups may be substituted by atoms of N, O and / or S and / or in the that 1-7 H atoms may be substituted by R4, R4 indicates F, Cl or OH, R5 indicates H or A ', A' indicates branched or unbranched alkyl with 1-6 C atoms, in which 1-5 H atoms may be substituted by F, Hal indicates F, Cl, Br or I, m indicates 1, 2, 3 or 4, n indicates 0, 1 or 2, p indicates 0, 1, 2, 3 or 4 and salts , pharmaceutically acceptable tautomers and stereoisomers thereof, including mixtures thereof in all proportions.Compuestos de fórmula I **(Ver fórmula)** donde R indica pirazol-diilo, imidazol-diilo, isoxazol-diilo o triazol-diilo, cada uno de los cuales no está sustituido o está monosustituido por R2, R1 indica (CH2)nAr, (CH2)nHet, A o Cic, R2 indica A', metoxi, hidroximetilo, COOA', CN, COOH, CONH2 u OH, R3 indica H, A
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
相关发明人
buchstaller, hans-peter
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