| 主权项 |
1. A compound of formula 1, wherein A is CH2, O or N—C1-6-alkyl; R1 is selected from
NHR1.1, NMeR1.1;NHR1.2, NMeR1.2;NHCH2—R1.3;NH—C3-6-cycloalkyl, whereas optionally one carbon atom is replaced by a nitrogen atom, whereas the ring is optionally substituted with one or two residues selected from the group consisting of C1-6-alkyl, O—C1-6-alkyl, NHSO2-phenyl, NHCONH-phenyl, halogen, CN, SO2—C1-6-alkyl, COO—C1-6-alkyl;a C9 or 10-bicyclic-ring, whereas one or two carbon atoms are replaced by nitrogen atoms and the ring system is bound via a nitrogen atom to the basic structure of formula 1 and whereas the ring system is optionally substituted with one or two residues selected from the group consisting of C1-6-alkyl, COO—C1-6-alkyl, C1-6-haloalkyl, O—C1-6-alkyl, NO2, halogen, CN, NHSO2—C1-6-alkyl, methoxyphenyl;a group selected from NHCH(pyridinyl)CH2COO—C1-6-alkyl, NHCH(CH2O—C1-6-alkyl)-benzoimidazolyl, optionally substituted with halogen or CN;or 1-aminocyclopentyl, optionally substituted with methyl-oxadiazole;R1.1 is phenyl, optionally substituted with one or two residues selected from the group consisting of C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C1-6-haloalkyl, C1-6-alkylene-OH, C2-6-alkenylene-OH, C2-6-alkynylene-OH, CH2CON(C1-6-alkyl)2, CH2NHCONH—C3-6-cycloalkyl, CN, CO-pyridinyl, CONR1.1.1R1.1.2, COO—C1-6-alkyl, N(SO2—C1-6-alkyl)(CH2CON(C1-4-alkyl)2) O—C1-6-alkyl, O-pyridinyl, SO2—C1-6-alkyl, SO2—C1-6-alkylen-OH, SO2—C3-6-cycloalkyl, SO2-piperidinyl, SO2NH—C1-6-alkyl, SO2N(C1-6-alkyl)2, halogen, CN, CO-morpholinyl, CH2-pyridinyl or a heterocyclic ring optionally substituted with one or two residues selected from the group consisting of C1-6-alkyl, NHC1-6-alkyl and ═O;
R1.1.1 H, C1-6-alkyl, C3-6-cycloalkyl, C1-6-haloalkyl, CH2CON(C1-6-alkyl)2, CH2CO-azetindinyl, C1-6-alkylen-C3-6-cycloalkyl, CH2-pyranyl, CH2-tetrahydrofuranyl, CH2-furanyl, C1-6-alkylen-OH or thiadiazolyl, optionally substituted with C1-6-alkyl;R1.1.2 H, C1-6-alkyl, SO2C1-6-alkyl;or R1.1.1 and R1.1.2 together are forming a four-, five- or six-membered carbocyclic ring, optionally containing one N or O, replacing a carbon atom of the ring, optionally substituted with one or two residues selected from the group consisting of C1-6-alkyl, C1-4-alkylene-OH, OH, ═O;orR1.1 is phenyl, wherein two adjacent residues are together forming a five- or six-membered carbocyclic aromatic or non-aromatic ring, optionally containing independently from each other one or two N, S, or SO2, replacing a carbon atom of the ring, wherein the ring is optionally substituted with C1-4-alkyl or ═O;R1.2 is selected from
heteroaryl, optionally substituted with one or two residues selected from the group consisting of C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, CH2COO—C1-6-alkyl, CONR1.2.1R1.2.2, COR1.2.3, COO—C1-6-alkyl, CONH2, O—C1-6-alkyl, halogen, CN, SO2N(C1-6-alkyl)2 or heteroaryl optionally substituted with one or two residues selected from the group consisting of C1-6-alkyl;heteroaryl, optionally substituted with a five- or six-membered carbocyclic non-aromatic ring containing independently from each other two N, O, S, or SO2, replacing a carbon atom of the ring;an aromatic or non-aromatic C9 or 10-bicyclic-ring, whereas one or two carbon atoms are replaced by N, O or S each optionally substituted with one or two residues selected from the group consisting of N(C1-6-alkyl)2, CONH—C1-6-alkyl, ═O;a heterocyclic non-aromatic ring, optionally substituted with pyridinyl;4,5-dihydro-naphtho[2,1-d]thiazole, optionally substituted with NHCO—C1-6-alkyl,R1.2.1 H, C1-6-alkyl, C1-6-alkylene-C3-6-cycloalkyl, C1-4-alkylene-phenyl, C1-4-alkylene-furanyl, C3-6-cycloalkyl, C1-4-alkylene-O—C1-4-alkyl, C1-6-haloalkyl or a five- or six-membered carbocyclic non-aromatic ring, optionally containing independently from each other one or two N, O, S, or SO2, replacing a carbon atom of the ring, optionally substituted with 4-cyclopropylmethyl-piperazinylR1.2.2 H, C1-6-alkyl;R1.2.3 a five- or six-membered carbocyclic non-aromatic ring, optionally containing independently from each other one or two N, O, S, or SO2, replacing a carbon atom of the ring;R1.3 is selected from phenyl, heteroaryl or indolyl, each optionally substituted with one or two residues selected from the group consisting of C1-6-alkyl, C3-6-cycloalkyl, O—C1-6-alkyl, O—C1-6-haloalkyl, phenyl, heteroaryl; R2 is selected from the group consisting of C1-6-alkylene-phenyl, C1-6-alkylene-naphthyl, and C1-6-alkylene-heteroaryl; each optionally substituted with one, two or three residues selected from the group consisting of C1-6-alkyl, C1-6-haloalkyl, O—C1-6-alkyl, O—C1-6-haloalkyl, halogen; R3 is H, C1-6-alkyl; R4 is H, C1-6-alkyl;
or R3 and R4 together are forming a CH2—CH2 group. |
