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US 8,999,986 B2Granted
Pyrrolo [2,3—D] pyrazin—7—ylpyrimidine compounds
AssigneeMerck Patent GmbH
InventorsMargarita Wucherer-Plietker, Christina Esdar
Life of this patent
Estimating the term…
Abstract
Pyrrolo[2,3-d]pyrazin-7-ylpyrimidine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumors.
Claims5
A compound of formula I
- in which
- R1 H, A, Hal, [C(R3)2]mCN, [C(R3)2]mHet1, [C(R3)2]mAr′, [C(R3)2]mCyc, [C(R3)2]mR3 or [C(R3)2]mN(R3)2,
- R2 A, C(R3)(R4)Ar, C(R3)(R4)Het or C(R3)(R4)Cyc,
- R3 Hor A′,
- R4 H, A, [C(R3)2]mOH, [C(R3)2]mOA, [C(R3)2]mN(R3)2 or [C(R3)2]mHet,
- R5 H, A, N(R3)2, OR3 or SR3,
- R6 H or Hal,
- Ar phenyl, naphthyl or biphenyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, A, (CH2)mOR3, (CH2)—N(R3)2, SR3, NO2, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, COR3, (CH2)nCN and/or S(O)nA,
- Ar′ phenyl, naphthyl or biphenyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, A, (CH2)mOR3, SR3, NO2, (CH2)mCN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, [C(R3)2]nCOHet2, [C(R3)2]mN(R3)2, [C(R3)2]mHet2, O[C(R3)2]mHet2, O[C(R3)2]pN(R3)2, O[C(R3)2]mHet2, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]pN(R3)2, NHCOO[C(R3)2]pHet2, OCONH[C(R3)2]nN(R3)2, CHO and/or COA,
- Het a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, and/or O and/or S atoms which is unsubstituted or mono- or disubstituted by Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3 and/or S(O)nA,
- Het1 a mono-, bi- or tricyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which is unsubstituted or may be mono- or disubstituted by Hal, A, OR3, SR3, NO2, [C(R3)2]nCOOR3, [C(R3)2]mCON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, COR3, [C(R3)2]mCOHet2, (CH2)nCN, [C(R3)2]mN(R3)2, [C(R3)2]mHet2, O[C(R3)2]mHet2, O[C(R3)2]pN(R3)2, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]pN(R3)2, NHCOO[C(R3)2]nHet2, CHO, NHCONH[C(R3)2]mN(R3)2, NHCONH[C(R3)2]mHet2, OCONH[C(R3)2]mN(R3)2, OCONH[C(R3)2]mHet2, COA, [C(R3)2]mCONH[C(R3)2]mN(R3)2, ═S, ═NH, =NA and or ═O (carbonyl oxygen)
- Het2 a mono- or bicyclic aromatic, unsaturated or saturated heterocycle having 1 to 2 N and/or O atoms, which may be mono- or disubstituted by A, OA, OH, Hal and/or ═O (carbonyl oxygen),
- A unbranched or branched alkyl having 1-10 C atoms,
- in which 1-7 H atoms may be replaced by F, Cl and/or Br,
- and/or in which one or two non-adjacent CH and/or CH2 groups may be replaced by NR3, O, S, SO, SO2, C≡C and/or CH═CH groups,
- or
- cyclic alkyl having 3-7 C atoms,
- A′ unbranched or branched alkyl having 1-6 C atoms, in which 1-5 H atoms may be replaced by F,
- Cyc cycloalkyl having 3-7 C atoms,
- Hal F, Cl, Br or I,
- n 0, 1 or 2,
- m 0, 1, 2, 3 or 4,
- p 1, 2, 3 or 4,
- or a pharmaceutically usable salt, tautomer, stereoisomer or mixture thereof in all ratios.
21 more elements
Dependencies are inferred from the claim text.