ES2587953T3 - Amidas cíclicas como inhibidores de MetAP-2 - Google Patents

Amidas cíclicas como inhibidores de MetAP-2 Download PDF

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Publication number
ES2587953T3
ES2587953T3 ES13711291.8T ES13711291T ES2587953T3 ES 2587953 T3 ES2587953 T3 ES 2587953T3 ES 13711291 T ES13711291 T ES 13711291T ES 2587953 T3 ES2587953 T3 ES 2587953T3
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atoms
unsubstituted
mono
cooa
hal
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Timo Heinrich
Frank Zenke
Mireille Krier
Manja FRIESE-HAMIM
Jeyaprakashnarayanan SEENISAMY
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Merck Patent GmbH
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Merck Patent GmbH
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    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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Abstract

Compuestos de fórmula I**Fórmula** en la que R significa NR2R4, Alk, C(>=CH2)[C(R4)2]nAr2, Het2, 5 O[C(R4)2]nAr2 u OA, X significa CO o CH2, Y significa CO o CH2, R1 significa 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 o [C(R4)2]nCONHCR4[(CH2)nN(R4)2]CON(R4)2, R2 significa H, [C(R4)2]nAr2, (CH2)nCOHet1, (CH2)nCOAr2, (CH2)mNA2 o (CH2)nHet, R3 significa OH u OCOA, R4 significa H o alquilo con 1, 2, 3 ó 4 átomos de C, R2 y R4 juntos también significan alquileno con 2, 3, 4 ó 5 átomos de C, pudiendo también estar un grupo CH2 reemplazado por N(CH2)mOH o SO2, R5, R6 en cada caso independientemente entre sí significan H, F o A, R5 y R6 juntos también significan alquileno con 2, 3, 4 ó 5 átomos de C, pudiendo también estar un grupo CH2 reemplazado por NCOA u O, R7 significa H o A, Ar1 significa fenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, OH, OA, CONH2, CONHA, CONA2, NHSO2A, CONHCyc, NHSO2Cyc, CONHAr2, COHet1 y/o NASO2A, Ar2 significa fenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, A, CONH2, y/u OAr3, Ar3 significa fenilo no sustituido o monosustituido con NH2, Het significa un heterociclo con uno o dos núcleos saturado, insaturado o aromático con de 1 a 4 átomos de 25 N y/u O y/o S, no sustituido o mono-, di- o trisustituido con 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 y/o Ar3, Het1 significa un heterociclo saturado con un núcleo con de 1 a 4 átomos de N y/u O y/o S, no sustituido o mono-, di- o trisustituido con >=O y/o COOA, Het2 significa isoindolilo, A significa alquilo no ramificado o ramificado con 1-10 átomos de C, en el que 1-7 átomos de H pueden estar reemplazados por F, Cl, Br, OH, CHO, COA, COOA, CN, CONA2, CONHA y/o CONH2, y/o en el que uno o dos grupos CH y/o CH2 no adyacentes pueden estar reemplazados por O, o Cyc,Alk significa alquenilo con 2, 3, 4, 5 ó 6 átomos de C Cyc significa alquilo cíclico con 3-7 átomos de C no sustituido o mono-, di- o trisustituido con NHCOA, NHSO2, OH, OA, A, NH2, NHA, NA2, COOA, COOH y/o CONHA, Hal significa F, Cl, Br o I, m significa 1, 2, 3 ó 4, n significa 0, 1, 2, 3 ó 4, p significa 1, 2 ó 3, así como sus sales, tautómeros y estereoisómeros farmacéuticamente útiles, incluyendo sus mezclas en todas las proporciones, excluyendo los siguientes compuestos: éster metílico del ácido 3-hidroxipiperidin-3-carboxílico, éster terc-butílico y metílico del ácido 3-hidroxipiperidin-1,3-dicarboxílico, éster terc-butílico del ácido 3-alil-3-hidroxipirrolidin-1-carboxílico, éster terc-butílico del ácido 3-alil-3-hidroxipiperidin-1-carboxílico.
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