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US 2011/0257170 A1Published application
4-morpholino-pyrido[3,2-d]pyrimidines
AssigneeMerck Serono SA
InventorsVincent Pomel, Pascale Gaillard, Gwenaelle Desforges, Anna Quattropani, Cyril Montagne
Life of this patent
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Abstract
This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.
Claims16
1-15. (canceled)
A compound of Formula (I)
- Wherein
- R1 denotes H, perfluoroalkyl, —NH2, —NA2, A, —NH-A, —NH—(CH2)p-A, —SO-A, SO2-A, —COORT, —(CH2)p—ORT, —(CH2)p—SRT, —COA, —CO-Het, —CO—N(H)2-m(A)m;
- —SO—N(H)2-m(A)m, SO2—N(H)2-m(A)m, —(CH2)p—N(H)2-m(A)m, —CO—NH—(CH2)p—N(H)2-m(A)m, —(CH2)p—NH—(CH2)p—N(H)2-m(A)m, Ar, or Het;
- R2 denotes H, Hal, CF3, A, Ar, Het, SA, OA, OH, —SOA, —SO2A, —OCO-A, —N(H)2-m(A)m, —NH—(CH2)p—N(H)2-m(A)m, —NA-(CH2)p—ORT, —NH—(CH2)p—OA, or —(CH2)pHet, —(CH2)p—N(H)2-m(A)m;
- R3 denotes Hal, Ar, OA, SA, —SOA, —SO2A, —NH—SO2A, CF3, —CN, A, or —NH—SO2Ar, or if at least one of R1 or R2 are different from H, R3 also denotes Het;
- RT denotes H, A, Ar, or Het;
- Ar denotes a monocyclic or bicyclic, aromatic carbocyclic ring having 6 to 14 carbon atoms, which is unsubstituted or monosubstituted, disubstituted or trisubstituted by, Hal, CF3, OCF3, NO2, CN, perfluoroalkyl, A, OA, NH2, COH, CONH2, —NHCOA, —NHSO2A, —NHSO2—N(H)2-m(A)m, N(H)1-qAqCOA, N(H)1-qAqSO2—N(H)2-m(A)m, —N(H)1-qAqCON(H)2-m(A)m, —COOA, —SO2A, —SO2N(H)2-m(A)m, —SO2Het, or —(CH2)p—N(H)2-m(A)m, —(CH2)p—ORT, or disubstituted or trisubstituted by OH and 1 or 2 of above described substituents;
- Het denotes a monocyclic or bicyclic saturated, unsaturated or aromatic heterocyclic ring having 1, 2, 3 or 4 N, O and/or S atoms which is unsubstituted or monosubstituted, disubstituted or trisubstituted by alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 8 carbon atoms, Hal, CF3, OCF3, NO2, CN, perfluoroalkyl, A, OA, OH, NH2, COH, CONH2, —NHCOA, —NHSO2A, —NHSO2—N(H)2-m(A)m, N(H)1-qAqCOA, N(H)1-qAqSO2—N(H)2-m(A)m, —N(H)1-qAqCON(H)2-m(A)m, —COOA, —SO2A, —SO2N(H)2-m(A)m, —SO2Het, —(CH2)p—N(H)2-m(A)m, or —(CH2)p—ORT;
- m denotes 0, 1 or 2;
- p denotes 0, 1, 2, 3 or 4;
- q denotes 0 or 1;
- A is a branched or linear alkyl having 1 to 12 C-atoms, wherein one or more, H-atoms may be replaced by Hal, Ar, Het, OR6, —CN, —COOalkyl or N(R6)2 and wherein one or more, non-adjacent CH2-groups, excluding the carbon atom which is linked to the rest of the molecule, may be replaced by O, NR6 or S and/or by —CH═CH— or —C≡C— groups, or denotes cycloalkyl or cycloalkylalkylene having 3-7 ring C atoms;
- and
- R6 is H, A, —(CH2)p—N(H)2-m(A)m, —(CH2)p—OA or CH2NH2,
- with the proviso that the following compound is excluded:
- and pharmaceutically acceptable solvates, tautomers, salts and stereoisomers thereof.
13 more elements
Dependencies are inferred from the claim text.