| abstract |
Compound of the general formula I ** (See formula) ** or stereoisomer or pharmaceutically acceptable salt or solvate thereof, in which: R1 is hydroxyalkyl (C1-6), HOCH2 (cyclopropylidine) CH2-, (C1- alkoxy) 4) (1-6C) hydroxyalkyl, (hydroxy) trifluoro (1-6C) alkyl, (2-6C) dihydroxyalkyl, (3-6C) H2Nhydroxyalkyl, (1-3C) NHhydrox (C3-6) alkyl, (3-6C) alkyl C1-3) 2Nhydroxyalkyl (C3-6), H2N (C1-4 alkoxy) alkyl (C3-6), Cyc1 (CH2) m-, hetCyc1, hetCyc2CH2-, RaRbNC (= O) CH2-, hetCyc3a (C1- 3), hetCyc3bhydroxyalkyl (C2-3), RcRdNalkyl (C2-3), (C1-3 alkyl) 2NSO2 (C2-3) alkyl, hetCyc4, alkyl (C1-6) or CH3SO2 (C1-6) alkyl; Cyc1 is a 4-6 membered cycloalkyl substituted with 1-2 substituents independently selected from the group consisting of HO, HOCH2-, (C1-3) alkyl, H2NHC (= O) -, (C1-3 alkyl) 2NC (= O) -, and HOCH2CH2NHC (= O) -; m is 0 or 1; hetCyc1 is a 4-6 membered heterocyclic ring having a ring heteroatom selected from N, O and S, wherein S is optionally oxidized to SO2, wherein said heterocyclic ring is optionally substituted with a substituent selected from the group consisting of OH, (C1-3 alkyl) C (= O) -, (C1-3 alkyl) SO2-, (C1-3 alkyl) NHC (= O) - and NH2CH2C (= O) -; hetCyc2 is a 4-6 membered heterocyclic ring having a ring S atom, in which S is oxidized to SO2; Ra and Rb are independently H or (1-3C) alkyl, or Ra and Rb together with the nitrogen atom to which they are attached form a 4-6 membered ring optionally having a ring oxygen atom; hetCyc3a and hetCyc3b are independently a 4-6 membered heterocyclic ring having 1-2 ring heteroatoms independently selected from N and O, wherein said heterocyclic ring is optionally substituted with 1-2 substituents independently selected from the group consisting in halogen, OH, (1-4C) alkoxy, HOCH2-, (1-3C alkyl) C (= O) - and oxo; Rc is H or (1-3C) alkyl; Rd is (C1-3) alkyl, (C1-3 alkyl) SO2-, hetCyca, or (C3-6) cycloalkyl optionally substituted with HOCH2-; hetCyca is a 5-6 membered azacyclic ring optionally substituted with 1-2 substituents independently selected from oxo and (1-3C) alkyl; hetCyc4 is azetidinyl substituted with ((CH3) 2N) 2P (= O) - or Y-C (= O) -; Y is ReRfN (CH2) n-, hetCycbCH2-, Cyc2, hydroxy (C1-3 alkyl), (C1-3 alkyl) 2NC (= O) -, (C1-3) alkyl SO2- or (C1- alkyl) 3); n is 0 or 1; Re and Rf are independently H or (1-3C) alkyl; hetCycb is a 4-5 membered azacyclic ring optionally substituted with OH; Cyc2 is a (3-6C) cycloalkyl optionally substituted with OH; R2 is (C1-6) alkyl, (C1-6) trifluoroalkyl, (C1-6) difluoroalkyl, (C1-6) fluoroalkyl, (C1-6) hydroxyalkyl, (C1-6) alkoxy, (C3-6) cycloalkyl (optionally substituted with one or two halogens), (C3-6) cycloalkyl, CH2-, HOC (= O) - or phenyl, and R3 is (C1-6) alkyl or (C3-6) cycloalkyl, or R2 and R3 together with the carbon atom to which they are attached they form a 3-7 membered cycloalkyl ring optionally substituted with one or two substituents independently selected from OH, (C1-6) alkyl and hydroxyalkyl (C1-6), or R2 and R3 together with the carbon atom to which they are attached they form a 4-membered saturated azacyclic ring substituted with SO2CF3; and R4 is hydrogen or (1-6C) alkyl. |