| 主权项 |
1. Compounds having the general formula (I) wherein R1 is L is a bond or —CR5R6—, —CR5R6—CR7R8—, —CR5R6—CR7R8—CR9R10—, —CR5R6—CR7R8—CR9R10—CR11R12—; R5—R12 represent independently of each other —H, —CH3, —C2H5, —C3H7, —F, —Cl, —Br, —I; R3 is selected from —H, —NO2, —NH2, —CN, —F, —Cl, —Br, —I, —CH3, —C2H5, —C3H7, —CH(CH3)2, —C4H9, —CH2—CH(CH3)2, —CH(CH3)—C2H5, —C(CH3)3, —O—CH3, —O—C2H5, —O—C3H7, —O—CH(CH3)2, —O—C4H9, —O—CH2—CH(CH3)2, —O—CH(CH3)—C2H5, —O—C(CH3)3, —CR13R14R21, —CR13R14—CR15R16R21, —O—CR13R14R21, —CR13R14—CR15R16—CR17R18R21, —CR13R14—CR15R16—CR17R18—CR19R20R21, —O—CR13R14—CR15R16R21, —O—CR13R14—CR15R16—CR17R18R21, —SO2R22, —CONR23R24, —NR25COR22, —O—CR13R14—CR15R16—CR17R18—CR19R20R21, —NR25SO2NR23R24, —NR25SO2R22, —NR25CONR23R24, —SO2NR23R24, —SO(NR26)R22, —NR23R24; R13—R21 and R29—R32 represent independently of each other —H, —CH3, —C2H5, —C3H7, —C4H9, —F, —Cl, —Br, —I; R26 is —H, —CH3, —C2H5, —C3H7, —CH(CH3)2, —C4H9, —CH2—CH(CH3)2, —CH(CH3)—C2H5, —C(CH3)3, —C5H11, —CH(CH3)—C3H7, —CH2—CH(CH3)—C2H5, —CH(CH3)—CH(CH3)2, —C(CH3)2—C2H5, —CH2—C(CH3)3, —CH(C2H5)2, —C2H4—CH(CH3)2, —C6H13, —C3H6—CH(CH3)2, —C2H4—CH(CH3)—C2H5, —CH(CH3)—C4H9, —CH2—CH(CH3)—C3H7, —CH(CH3)—CH2—CH(CH3)2, —CH(CH3)—CH(CH3)—C2H5, —CH2—CH(CH3)—CH(CH3)2, —CH2—C(CH3)2—C2H5, —C(CH3)2—C3H7, —C(CH3)2—CH(CH3)2, —C2H4—C(CH3)3, —CH(CH3)—C(CH3)3, —CR13R14R21, —COR28, —CR13R14—CR15R16R21, —CR13R14—CR15R16—CR17R18—CR19R20—CR29R30R21, —CR13R14—CR15R16—CR17R18R21, —CR13R14—CR15R16—CR17R18—CR19R20R21, —CR13R14—CR15R16—CR17R18—CR19R20—CR29R30—CR31R32R21, —COOR28, —R27; R22, and R28 are independently selected from —R27′, —CR13R14R21, —CH3, —C2H5, —CR13R14—CR15R16R21, —CR13R14—CR15R16—CR17R18—CR19R20—CR29R30R21, —CR13R14—CR15R16—CR17R18R21, —CR13R14—CR15R16—CR17R18—CR19R20R21, —CR13R14—CR15R16—CR17R18—CR19R20—CR29R30—CR31R32R21, —C3H7, —CH2Ph; —CH2Ph the phenyl group of which may further be substituted by one, two, three, four or five substituents selected from the group consisting of —CH3, —C2H5, —C3H7, —F, —Cl, —Br and —I; R27, R27′ and R27″ are independently selected from these C3-C10-cycloalkyl groups may further be substituted by one, two, three, four, five or more substituents selected from the group consisting of —F, —Cl, —Br and —I; R23, R24, R77 and R78 are independently of each other selected from —H, —CH3, —C2H5, —CR13R14R21, —C3H7, —CR13R14—CR15R16R21, —CR13R14—CR15R16—CR17R18—CR19R20—CR29R30R21, —CR13R14—CR15R16—CR17R18R21, —CR13R14—CR15R16—CR17R18—CR19R20R21, —CR13R14—CR15R16—CR17R18—CR19R20—CR29R30—CR31R32R21, —CR13R14—CR15R16—O—R33, —CR13R14—CR15R16—NR33R34, —CR13R14—CR15R16—CR17R18—NR33R34, —CR13R14—CR15R16—CR17R18—CR19R20—NR33R34, —CR13R14—CR15R16—CR17R18—O—R33, —CR13R14—CR15R16—CR17R18—CR19R20—CR29R30—NR33R34, -Ph, —CH2PH, phenyl group which may further be substituted by one, two, three, four or five substituents selected from the group consisting of —CH3, —C2H5, —C3H7, —F, —Cl, —Br and —I; —CH2Ph the phenyl group of which may further be substituted by one, two, three, four or five substituents selected from the group consisting of —CH3, —C2H5, —C3H7, —F, —Cl, —Br and —I; or both residues R23 and R24 together form with the nitrogen atom to which they are attached a azetidine, pyrrolidine, piperidine, piperazine, azepane, or morpholine ring; R33 and R34 represent independently of each other —H, —CH3, —C2H5, —C3H7, —C4H9, —CH2Ph, —COOC(CH3)3, —COOCH3, —COOCH2CH3, —COOCH2CH2CH3, —COOCH(CH3)2, —COOCH2Ph, —COCH3; and R25 is selected from —H, —CH3, —C2H5, —C3H7, —CH(CH3)2, —C4H9, —CH2—CH(CH3)2, —CH(CH3)—C2H5 or —C(CH3)3; R4 is selected from —H, —NO2, —CN, —F, —Cl, —Br, —I, —CR35R36R37, —CR35R36—CR38R39—CR40R41—CR42R43R37, —O—CR35R36—CR38R39R37, —O—CR35R36—CR38R39—CR40R41R37, —CR35R36—CR38R39—CR40R41R37, —O—CR35R36—CR38R39—CR40R41—CR42R43R37, —CR35R36—CR38R39R37, —O—CR35R36—CR38R39—CR40R41—CR42R43—CR44R45R37, —O—CR35R36R37, —O—CR35R36—CR38R39—CR40R41—CR42R43—CR44R45—CR46R47R37, —CR35R36—CR38R39—CR40R41—CR42R43—CR44R45R37, —CR35R36—CR38R39—CR40R41—CR42R43—CR44R45—CR46R47R37, —OCH2Ph, —R27″, —O—R27″; R35—R47 and R62—R74 represent independently of each other —H, —CR48R49R50, —CR48R49—CR51R52R50, —CR48R49—CR51R52—CR53R54R50, —CR48R49—CR51R52—CR53R54—CR55R56R50, —F, —Cl, —Br, —I; R48—R56 represent independently of each other —H, —F, —Cl, —Br, —I; R4 together with R22 or R23 or R24 or R25 may form a group —CH2CH2— or —CH2CH2CH2— if R4 is attached ortho to -L-R3; R2 is R57 is selected from —H, —OH, —NO2, —CN, —F, —Cl, —Br, —I, —NR60R61, -D-R64, -D-NR60R61, —O-D-R64, —CHO, —CH2OH, —CO—R60, —CH2OR60; D, D′ and D″ represent independently of each other —CR62R63—, —CR62R63—CR65R66—, —CR62R63—CR65R66—CR67R68—, —CR62R63—CR65R66—CR67R68—CR69R70—; R60, R61, R75 and R76 represent independently of each other —H, —CH3, —C2H5, —C3H7, —CH(CH3)2, —C4H9, —CH2—CH(CH3)2, —CH(CH3)—C2H5, —C(CH3)3, -(cyclo-C3H5); x is 0, 1, 2 or 3; B is a bond, -D′-, -E-; E and E′ represent independently of each other —CR62R63—CR65R66—CR67R68—CR69R70—CR71R72—, —CR62R63—CR65R66—CR67R68—CR69R70—CR71R72—CR73R74—; Y is a bond, —O—, —S—, —SO—, —SO2—, —SO2NH—, —NHSO2—, —CO—, —COO—, —OOC—, —CONH—, —NHCO—, —NH—, —N(CH3)—, —NH—CO—NH—, —O—CO—NH—, —NH—CO—O—; R58 is selected from a bond, -D″-, -E′-; R59 is selected from (i) —H, —OH, —OCH3, —OC2H5, —OC3H7, —O-cyclo-C3H5, —OCH(CH3)2, —OC(CH3)3, —OC4H9, -Ph, —OPh, —OCH2-Ph, —OCPh3, —SH, —SCH3, —SC2H5, —SC3H7, —S-cyclo-C3H5, —SCH(CH3)2, —SC(CH3)3, —SC4H9, —NO2, —F, —Cl, —Br, —I, —P(O)(OH)2, —P(O)(OCH3)2, —P(O)(OC2H5)2, —P(O)(OCH(CH3)2)2, —Si(CH3)2(C(CH3)3), —Si(C2H5)3, —Si(CH3)3, —CN, —CHO, —COCH3, —COC2H5, —COC3H7, —CO-cyclo-C3H5, —COCH(CH3)2, —COC(CH3)3, —COC4H9, —COOH, —COOCH3, —COOC2H5, —COOC3H7, —COOC4H9, —COO-cyclo-C3H5, —COOCH(CH3)2, —COOC(CH3)3, —OOC—CH3, —OOC—C2H5, —OOC—C3H7, —OOC—C4H9, —OOC-cyclo-C3H5, —OOC—CH(CH3)2, —OOC—C(CH3)3, —CONR75R76, —NHCOCH3, —NHCOC2H5, —NHCOC3H7, —NHCO-cyclo-C3H5, —NHCO—CH(CH3)2, —NHCOC4H9, —NHCO—C(CH3)3, —NHCO—OCH3, —NHCO—OC2H5, —NHCO—OC3H7, —NHCO—O-cyclo-C3H5, —NHCO—OC4H9, —NHCO—OCH(CH3)2, —NHCO—OC(CH3)3, —NHCO—OCH2Ph, —NR77R78, —SOCH3, —SOC2H5, —SOC3H7, —SO-cyclo-C3H5, —SOCH(CH3)2, —SOC(CH3)3, —SO2CH3, —SO2C2H5, —SO2C3H7, —SO2-cyclo-C3H5, —SO2CH(CH3)2, —SO2C4H9, —SO2C(CH3)3, —SO3H, —SO2NR75R76, —OCF3, —OC2F5, —O—COOCH3, —O—COOC2H5, —O—COOC3H7, —O—COO-cyclo-C3H5, —O—COOC4H9, —O—COOCH(CH3)2, —O—COOCH2Ph, —O—COOC(CH3)3, —NH—CO—NH2, —NH—CO—NHCH3, —NH—CO—NHC2H5, —NH—CO—NHC3H7, —NH—CO—NHC4H9, —NH—CO—NH-cyclo-C3H5, —NH—CO—NH[CH(CH3)2], —NH—CO—NH[C(CH3)3], —NH—CO—N(CH3)2, —NH—CO—N(C2H5)2, —NH—CO—N(C3H7)2, —NH—CO—N(C4H9)2, —NH—CO—N (cyclo-C3H5)2, —NH—CO—N[CH(CH3)2]2, —NH—CO—N[C(CH3)3]2, —NH—C(═NH)—NH2, —NH—C(═NH)—NHCH3, —NH—C(═NH)—NHC2H5, —NH—C(═NH)—NHC3H7, —NH—C(═NH)—NHC4H9, —NH—C(═NH)—NH-cyclo-C3H5, —NH—C(═NH)—NH[CH(CH3)2], —NH—C(═NH)—NH[C(CH3)3], —NH—C(═NH)—N(CH3)2, —NH—C(═NH)—N(C2H5)2, —NH—C(═NH)—N(C3H7)2, —NH—C(═NH)—N(cyclo-C3H5)2, —NH—C(═NH)—N(C4H9)2, —NH—C(═NH)—N[CH(CH3)2]2, —NH—C(═NH)—N[C(CH3)3]2, —O—CO—NH2, —O—CO—NHCH3, —O—CO—NHC2H5, —O—CO—NHC3H7, —O—CO—NHC4H9, —O—CO—NH-cyclo-C3H5, —O—CO—NH[CH(CH3)2], —O—CO—NH[C(CH3)3], —O—CO—N(CH3)2, —O—CO—N(C2H5)2, —O—CO—N(C3H7)2, —O—CO—N(C4H9)2, —O—CO—N(cyclo-C3H5)2, —O—CO—N[CH(CH3)2]2, —O—CO—N[C(CH3)3]2; (ii) an aromatic or heteroaromatic mono- or bicyclic ring selected from 2-thienyl, 3-thienyl, 2-furanyl, 3-furanyl, 2-oxazolyl, 3-oxazolyl, 4-oxazolyl, 2-thiazolyl, 3-thiazolyl, 4-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 4-pyrazolyl, 5-pyrazolyl, 1-imidazolyl, 2-imidazolyl, 4-imidazolyl, 5-imidazolyl, phenyl, 1-naphthyl, 2-naphthyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 2-pyrazinyl, 3-pyridazinyl, 4-pyridazinyl, 1,3,5-triazin-2-yl, which optionally may be substituted by one or two substituents selected from —F, —Cl, —Br, —I, —OCH3, —CH3, —NO2, —CN, —CF3; (iii) a saturated ring selected from R79 represents —H, —CH3, —CH2Ph, —COOC(CH3)3, —COOCH3, —COOCH2CH3, —COOCH2CH2CH3, —COOCH(CH3)2, —COOCH2Ph, —COCH3; the group —B—Y—R58—R59 together with one substituent R57 may form a group —OCH2O—, if R57 is attached in position ortho to —B—Y—R58—R59; with the proviso that R59 is not —H, if B, Y and R58 are bonds; and enantiomers, stereoisomeric forms, mixtures of enantiomers, diastereomers, mixtures of diastereomers, prodrugs, hydrates, solvates, acid salt forms, tautomers, and racemates of the above mentioned compounds and pharmaceutically acceptable salts thereof. |
